Substituted dimethylcyclobutyl compounds, their preparation and use in medicaments

The present invention relates to substituted dimethylcyclobutyl compounds of general formula I,

I,

a process for their preparation, medicaments comprising said substituted dimethylcyclobutyl compounds as well as the use of said substituted dimethylcyclobutyl compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via sigma receptors.

The search for new therapeutic agents has been greatly aided in recent years by better understanding of the structure of proteins and other biomolecules associated with target diseases. One important class of these proteins is the sigma receptor, a cell surface receptor of the central nervous system (CNS) which may be related to the dysphoric, hallucinogenic and cardiac stimulant effects of opioids.

From studies of the biology and function of sigma receptors, evidence has been presented that sigma receptor ligands may be useful in the treatment of psychosis and movement disorders such as dystonia and tardive dyskinesia, and motor disturbances associated with Huntington's chorea or Tourette's syndrome and in Parkinson's disease (Walker, J. M. et al, Pharmacological

Reviews, 1990, 42, 355). It has been reported that the known sigma receptor ligand rimcazole clinically shows effects in the treatment of psychosis (Snyder, S. H., Largent, B. L. J. Neuropsychiatry 1989, 1 , 7). The sigma binding sites have preferential affinity for the dextrorotatory isomers of certain opiate benzomorphans, such as (+)SKF 10047, (+)cyclazocine, and

(+)pentazocine and also for some narcoleptics such as halopehdol.

The sigma receptor has at least two subtypes, which may be discriminated by stereoselective isomers of these pharmacoactive drugs. Possible sigma- site-mediated drug effects include modulation of glutamate receptor function, neurotransmitter response, neuroprotection, behaviour, and cognition (Quirion, R. et al. Trends Pharmacol. Sci., 1992, 13:85-86). Most studies have implied that sigma binding sites (receptors) are plasmalemmal elements of the signal transduction cascade. Drugs reported to be selective sigma ligands have been evaluated as antipsychotics (Hanner, M. et al. Proc. Natl.

Acad. Sci., 1996, 93:8072-8077). The existence of sigma receptors in the CNS, immune and endocrine systems have suggested a likelihood that it may serve as link between the three systems.

Thus, there is a need to find compounds that have pharmacological activity towards the sigma receptor, being both effective and selective, and having good "drugability" properties, i.e. good pharmaceutical properties related to administration, distribution, metabolism and excretion.

Therefore an object of the present invention was to provide compounds that are particularly suitable as active ingredients in medicaments, especially in medicaments for the prophylaxis and/or treatment of disorders or diseases related to sigma receptors, preferably sigma-1 receptors, such as food intake related disorders or pain.

Surprisingly, it has been found that the substituted dimethylcyclobutyl compounds of general formula I given below show good to excellent affinity for sigma receptors, in particular they show good to excellent affinity to sigma-1 receptors. These compounds are therefore particularly suitable as pharmacologically active agents in a medicament for the prophylaxis and/or treatment of disorders or diseases related to sigma receptors, preferably related to sigma-1 receptors.

Thus, in one of its aspects the present invention relates to a dimethylcyclobutyl compound of general formula I,

wherein

m is 1 , 2, 3 or 4;

is O, 1 , 2 or 3;

X represents a -OR moiety or a -NR 6iR-)7 moiety;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic

radical, which may be condensed with an unsubstituted or at least mono- substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least- mono substituted alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated or unsaturated, but not aromatic, mono- or bicyclic ring system;

Y represents a -OR ⁸ moiety; a -NR ⁹ R ¹⁰ moiety; a -C(=O)-OR 11 moiety;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be condensed with an unsubstituted or at least mono- substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least- mono substituted alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated or unsaturated, but not aromatic, mono- or bicyclic ring system;

R ¹ represents a hydrogen atom or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

R ² represents a hydrogen atom;

a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least-mono substituted alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least- mono substituted alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated or unsaturated, but not aromatic, mono- or bicyclic ring system;

R ³ and R ⁴ , independently of one another, each represent a hydrogen atom or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

R ⁵ and R ⁸ , independently of one another, each represent a hydrogen atom or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least-mono substituted alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least-mono substituted alkylene, alkenylene or alkinylene group and which may be

condensed with an unsubstituted or at least mono-substituted saturated or unsaturated, but not aromatic, mono- or bicyclic ring system;

or a -C(=O)-R ¹² moiety;

R ⁶ , R ⁷ , R ⁹ and R ¹⁰ , independently of one another, each represent a hydrogen atom or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least-mono substituted alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least- mono substituted alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated or unsaturated, but not aromatic, mono- or bicyclic ring system;

or R ⁶ and R ⁷ , together with the bridging nitrogen atom form an unsubstituted or at least mono-substituted, saturated, unsaturated or aromatic heterocyclic ring which may contain one or more additional heteroatom(s) as ring member(s) and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

or R ⁹ and R ¹⁰ , together with the bridging nitrogen atom form an unsubstituted or at least mono-substituted, saturated, unsaturated or

aromatic heterocyclic ring which may contain one or more additional heteroatom(s) as ring member(s) and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

and

R ¹¹ and R ¹² , independently of one another, represent a hydrogen atom or a linear or branched, saturated or unsaturated, unsubstituted or at least mono- substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least-mono substituted alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least- mono substituted alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated or unsaturated, but not aromatic, mono- or bicyclic ring system;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a salt thereof, or a corresponding solvate thereof.

Preferred is a compound of general formula I, wherein

X and Y are different; wherein

if R ⁵ represents hydrogen and m is 1 , R ¹ represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical; R ² represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical; a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least-mono substituted alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system; or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least-mono substituted alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated or unsaturated, but not aromatic, mono- or bicyclic ring system; wherein

R ⁶ , R ⁷ , R ⁹ and R ¹⁰ , independently of one another, each represent a linear or branched, saturated or unsaturated, unsubstituted or at least mono- substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least-mono substituted alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system; or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least- mono substituted alkylene, alkenylene or alkinylene group and which may be

condensed with an unsubstituted or at least mono-substituted saturated or unsaturated, but not aromatic, mono- or bicyclic ring system;

or R ⁶ and R ⁷ , together with the bridging nitrogen atom form an unsubstituted or at least mono-substituted, saturated, unsaturated or aromatic heterocyclic ring which may contain one or more additional heteroatom(s) as ring member(s) and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

or R ⁹ and R ¹⁰ , together with the bridging nitrogen atom form an unsubstituted or at least mono-substituted, saturated, unsaturated or aromatic heterocyclic ring which may contain one or more additional heteroatom(s) as ring member(s) and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

R ¹¹ represents a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical;

a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least-mono substituted alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system;

or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least- mono substituted alkylene, alkenylene or alkinylene group and which may be

condensed with an unsubstituted or at least mono-substituted saturated or unsaturated, but not aromatic, mono- or bicyclic ring system; and

R ¹² represents a hydrogen atom or a linear or branched, saturated or unsaturated, unsubstituted or at least mono-substituted aliphatic radical; a saturated or unsaturated, unsubstituted or at least mono-substituted, optionally at least one heteroatom as a ring member containing cycloaliphatic radical, which may be bonded via a linear or branched, unsubstituted or at least-mono substituted alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated, unsaturated or aromatic mono- or bicyclic ring system; or an unsubstituted or at least mono-substituted aryl or heteroaryl radical, which may be bonded via a linear or branched, unsubstituted or at least- mono substituted alkylene, alkenylene or alkinylene group and which may be condensed with an unsubstituted or at least mono-substituted saturated or unsaturated, but not aromatic, mono- or bicyclic ring system.

If any of the substituents in any of the above defined formulae represents or comprises a 3-, A-, 5-, 6-, 7-, 8-, 9-, 10-, 11 -, 12-, 13- or 14-membered heterocyclic ring, 3- to 9-membered (hetero)cycloaliphatic radical, C _3- g cycloalkyl radical or C _4-9 cycloalkenyl radical, said heterocyclic ring, (hetero)cycloaliphatic radical, C _3- g cycloalkyl radical or C _4- 9 cycloalkenyl radical may - if not defined otherwise - be unsubstituted or substituted by one or more substituents, preferably unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s). Said substituent(s) may preferably be selected independently from the group consisting of oxo (=O), thioxo (=S), Ci _-5 -alkyl, - O-Ci.s-alkyl, -S-Ci _-5 -alkyl, -C(=O)-OH, -C(=O)-Ci _-5 -alkyl, -C(=O)-O-Ci _-5 -alkyl, -O-C(=O)-Ci _-5 -alkyl, F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , - NH(Ci _-5 -alkyl), -N(Ci _-5 -alkyl) ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , - C(=O)-NH(Ci _-5 -alkyl), -C(=O)-N(Ci _-5 -alkyl) ₂ , -S(=O) ₂ -Ci _-5 -alkyl, -S(=O) ₂ - phenyl, -0-CFH ₂ , -0-CF ₂ H, -S-CFH ₂ , -S-CF ₂ H, -SO ₃ H, -NH-C(=O)-Ci _-5 -alkyl,

-N(Ci-5-alkyl)-C(=O)-Ci-5-alkyl, -C(=O)-Ci _-5 -perfluoroalkyl, -S(=O) ₂ -NH ₂ , - S(=O) ₂ -NH-Ci _-5 -alkyl, -S(=O) ₂ -NH-phenyl, -NH-S(=O) ₂ -Ci _-5 -alkyl, cyclobutyl, cyclopropyl, cyclopentyl, cyclohexyl, pyrrol id inyl, piperidinyl, morpholinyl, phenyl, phenethyl, phenoxy and benzyl; whereby in each occurrence Ci _-5 - alkyl may be linear or branched and whereby said cyclic substituents may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ and - NO ₂ .

More preferably said substituents may be selected independently from the group consisting of oxo (=0), thioxo (=S), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -O-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ - CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , -O-C(CH ₃ ) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S- CH(CHs) ₂ , -S-C(CHs) ₃ , -C(=O)-OH, -C(=O)-O-CH ₃ , -C(=O)-O-C ₂ H ₅ , -C(=O)-

0-CH ₂ -CH ₂ -CH ₃ , -C(=O)-O-CH(CHs) ₂ , -C(=O)-O-C(CH ₃ ) ₃ , -C(=O)-CH ₃ , - C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CHs, -C(=O)-CH(CH ₃ ) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , -NH-CH ₃ , -NH-C ₂ H ₅ , -NH- CH ₂ -CH ₂ -CH ₃ , -NH-CH(CHs) ₂ , -NH-C(CH ₃ ) ₃ , -N(CH ₃ ) ₂ , -N(C ₂ H ₅ ) ₂ , -NO ₂ , - CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH-CH ₃ , -C(=O)-NH-C ₂ H ₅ , -C(=O)-

N(CH ₃ ) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ , -S(=O) ₂ -CH ₃ , -S(=O) ₂ -phenyl, phenyl, phenethyl, phenoxy and benzyl; whereby in each occurrence said cyclic substituents may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br ₁ -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ and -

NO ₂ .

If any of the substituents in any of the above defined formulae represents or comprises a cycloaliphatic radical, C _3- 9 cycloalkyl radical or C _4- 9 cycloalkenyl radical which contains one or more, preferably 1 , 2 or 3 heteroatom(s) as ring member(s), unless defined otherwise, each of these heteroatom(s) may

preferably be selected independently from the group consisting of N, O and S.

If any of the substituents in any of the above defined formulae represents or comprises a heterocyclic ring which contains one or more, preferably 1 , 2 or

3, additional heteroatom(s) as ring member(s), unless defined otherwise, each of these heteroatom(s) may preferably be selected independently from the group consisting of N, O and S.

Suitable saturated or unsaturated, optionally at least one heteroatom as ring member containing cycloaliphatic radicals, Cs-g cycloalkyl radicals or C _4- g cycloalkenyl radicals may preferably be selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, aziridinyl, azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, azepanyl, diazepanyl, azocanyl, (2,5)-dihydrofuranyl, (2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl, (2,3)-dihydrofuranyl, (2,5)- dihydro-1 H-pyrrolyl, (2,3)-dihydro-1 H-pyrrolyl, tetrahydrothiopyranyl, tetrahydropyranyl, (3,4)-dihydro-2H-pyranyl, (3,4)-dihydro-2H-thiopyranyl,

(1 ,2,3,6)-tetrahydropyridinyl, (1 ,2,3,4)-tetrahydropyridinyl, (1 ,2,5,6)- tetrahydropyridinyl, [1 ,3]-oxazinanyl, hexahydropyhmidinyl, (5,6)-dihydro-4H- pyrimidinyl, oxazolidinyl, (1 ,3)-dioxanyl, (1 ,4)-dioxanyl and (1 ,3)-dioxolanyl.

Suitable saturated or unsaturated, optionally at least one heteroatom as ring member containing cycloaliphatic radicals, C _3- 9 cycloalkyl radicals or C _4-9 cycloalkenyl radicals which are condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system may preferably be selected from the group consisting of indolinyl, isoindolinyl, decahydronaphthyl, (1 ,2,3,4)-tetrahydroquinolinyl, (1 ,2,3,4)-tetrahydroisoquinolinyl, (1 ,2,3,4)- tetrahydronaphthyl, octahydro-cyclopenta[c]pyrrolyl, (1 , 3,4,7, 9a)-hexahydro-

2H-quinolizinyl, (1 ,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl, dodecahydrocarbazolyl, 9H-carbazolyl, decahydroisoquinolinyl, (6,7)-dihydro- 4H-thieno[3,2-c]pyridinyl, (2,3)-dihydro-1 H-benzo[de]isoquinolinyl, fluorenyl and (1 ,2,3,4)-tetrahydroquinoxazlinyl.

Suitable saturated, unsaturated or aromatic heterocyclic rings may preferably be selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, aziridinyl, azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl, azepanyl, diazepanyl, azocanyl, (1 ,2,3,6)- tetrahydropyridinyl, (1 ,2,3,4)-tetrahydropyhdinyl, (1 ,2,5,6)-tetrahydropyhdinyl, hexahydropyrimidinyl, (5,6)-dihydro-4H-pyhmidinyl, pyrrolyl, imidazolyl, pyrazolyl and triazolyl.

Suitable saturated, unsaturated or aromatic heterocyclic rings which are condensed with an unsubstituted or at least mono-substituted mono- or bicyclic ring system may preferably be selected from the group consisting of indolinyl, isoindolinyl, (1 ,2,3,4)-tetrahydroquinolinyl, (1 ,2,3,4)- tetrahydroisoquinolinyl, octahydro-cyclopenta[c]pyrrolyl, decahydroquinolinyl, dodecahydrocarbazolyl, 9H-carbazolyl, decahydroisoquinolinyl, (2,3)-dihydro- 1 H-cyclopenta[b]indolyl, [1 ,2,3,4]-tetrahydroquinazolinyl, [3,4]-dihydro-2H- benzo[1 ,4]oxazinyl and (4,5,6,7)-tetrahydro-1 H-indolyl.

If any of the substituents in any of the above defined formulae represents an alkylene group, preferably an Ci _-6 alkylene group, an alkenylene group, preferably an C _2- 6 alkenylene group or an alkinylene group, preferably an C _2- 6 alkinylene group, which may be substituted, said alkylene group, C _2- 6 alkylene group, alkenylene group, C _2- 6 alkenylene group, alkinylene group or C _2- 6 alkinylene group may be unsubstituted or substituted by one or more substituents, preferably unsubstituted or optionally substituted with 1 , 2 or 3 substituent(s). Said substituent(s) may preferably be selected independently from the group consisting of -O-Ci _-5 -alkyl, -S-Ci _-5 -alkyl, -F, Cl, Br, I, -CN, -

CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , -NH(Ci _-5 -alkyl) and -N(Ci _-5 -alkyl) ₂ , whereby in each occurrence Ci _-5 -alkyl may be linear or branched. An alkenylene group comprises at least one carbon-carbon double bond, an alkinylene group comprises at least one carbon-carbon triple bond.

Suitable alkylene groups include -(CH ₂ )-, -CH(CH ₃ )-, -CH(phenyl), -(CH ₂ ) ₂ -, - (CH ₂ ) ₃ -,-(CH ₂ ) ₄ -, -(CH ₂ ) ₅ and -(CH ₂ ) ₆ -, suitable alkenylene groups include - CH=CH-, -CH ₂ -CH=CH- and -CH=CH-CH ₂ - and suitable alkinylene groups include -C≡C- , -CH ₂ -C≡C- and -C≡C-CH ₂ -.

If any of the substituents in any of the above defined formulae represents or comprises an aryl radical, including a 6-membered aryl radical such as phenyl or a 10-membered aryl radical such as naphthyl or a 14-membered aryl radical such as anthracenyl, said aryl radical may - if not defined otherwise - be unsubstituted or substituted by one or more substituents, preferably unsubstituted or substituted with 1 , 2, 3, 4 or 5 substituent(s). Said substituent(s) may preferably be selected independently from the group consisting of Ci _-5 -alkyl, -O-Ci _-5 -alkyl, -S-Ci _-5 -alkyl, -C(=O)-OH, -C(=O)-Ci _-5 - alkyl, -C(=O)-O-Ci _-5 -alkyl, -O-C(=O)-Ci _-5 -alkyl, F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -SH, -NH ₂ , -NH(Ci _-5 -alkyl), -N(Ci _-5 -alkyl) ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ ,

-C(=O)-NH ₂ , -C(=O)-NH(Ci _-5 -alkyl), -C(=O)-N(Ci _-5 -alkyl) ₂ , -S(=O) ₂ -Ci _-5 -alkyl, -S(=O) ₂ -phenyl, -0-CFH ₂ , -0-CF ₂ H, -S-CFH ₂ , -S-CF ₂ H, -SO ₃ H, -NH-C(=O)- Ci.s-alkyl, -N(Ci _-5 -alkyl)-C(=O)-Ci _-5 -alkyl, -C(=O)-Ci _-5 -perfluoroalkyl, -S(=O) ₂ - NH ₂ , -S(=O) ₂ -NH-Ci _-5 -alkyl, -S(=O) ₂ -NH-phenyl, -NH-S(=O) ₂ -Ci _-5 -alkyl, cyclobutyl, cyclopropyl, cyclopentyl, cyclohexyl, pyrrol id inyl, piperidinyl, morpholinyl, phenyl, phenethyl, phenoxy and benzyl; whereby in each occurrence Ci _-5 -alkyl may be linear or branched and whereby said cyclic substituent(s) may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -

NH ₂ and -NO ₂

More preferably said substituents may be selected independently from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec- butyl, isobutyl, n-pentyl, -0-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , - O-C(CH ₃ ) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CH ₃ ) ₂ , -S-C(CH ₃ ) ₃ , - C(=O)-OH, -C(=O)-O-CH ₃ , -C(=O)-O-C ₂ H ₅ , -C(=O)-O-CH ₂ -CH ₂ -CH ₃ , -C(=O)-

O-CH(CH ₃ ) ₂ , -C(=O)-O-C(CH ₃ )s, -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ - CH ₂ -CH ₃ , -C(=O)-CH(CHs) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , - SCF ₃ , -OH, -SH, -NH ₂ , -NH-CH ₃ , -NH-C ₂ H ₅ , -NH-CH ₂ -CH ₂ -CH ₃ , -NH- CH(CHs) ₂ , -NH-C(CHs) ₃ , -N(CH ₃ ) ₂ , -N(C ₂ H ₅ ) ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , - C(=O)-NH ₂ , -C(=O)-NH-CHs, -C(=O)-NH-C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)-

N(C ₂ Hs) ₂ and -S(=O) ₂ -CH ₃ .

Preferred aryl radicals, which may optionally be at least mono-substituted, are phenyl and naphthyl.

If any of the substituents in any of the above defined formulae represents or comprises a heteroaryl radical, including a monocyclic 5- or 6-membered heteroaryl radical or a bi- or tricyclic 8-, 9-, 10-, 11 -, 12-, 13- or 14- membered heteroaryl radical, said heteroaryl radical may - if not defined otherwise - be unsubstituted or substituted by one or more substituents, preferably unsubstituted or substituted with 1 , 2, 3, 4 or 5 substituent(s). Said substituent(s) may preferably be selected independently from the group consisting of Ci _-5 -alkyl, -O-Ci _-5 -alkyl, -S-Ci _-5 -alkyl, -C(=O)-OH, -C(=O)-Ci _-5 - alkyl, -C(=O)-O-Ci _-5 -alkyl, -O-C(=O)-Ci _-5 -alkyl, F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -SH, -NH ₂ , -NH(Ci _-5 -alkyl), -N(Ci _-5 -alkyl) ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ ,

-C(=O)-NH ₂ , -C(=O)-NH(Ci _-5 -alkyl), -C(=O)-N(Ci _-5 -alkyl) ₂ , -S(=O) ₂ -Ci _-5 -alkyl, -S(=O) ₂ -phenyl, -0-CFH ₂ , -0-CF ₂ H, -S-CFH ₂ , -S-CF ₂ H, -SO ₃ H, -NH-C(=O)- Ci _-5 -alkyl, -N(Ci _-5 -alkyl)-C(=O)-Ci _-5 -alkyl, -C(=O)-Ci _-5 -perfluoroalkyl, -S(=O) ₂ - NH ₂ , -S(=O) ₂ -NH-Ci _-5 -alkyl, -S(=O) ₂ -NH-phenyl, -NH-S(=O) ₂ -Ci _-5 -alkyl, cyclobutyl, cyclopropyl, cyclopentyl, cyclohexyl, pyrrol id inyl, piperidinyl, morpholinyl, phenyl, phenethyl, phenoxy and benzyl; whereby in each

occurrence Ci _-5 -alkyl may be linear or branched and whereby said cyclic substituent(s) may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, - NH ₂ and -NO ₂

More preferably said substituents may be selected independently from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec- butyl, isobutyl, n-pentyl, -O-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , - O-C(CH ₃ ) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CH ₃ ) ₂ , -S-C(CH ₃ ) ₃ , -

C(=O)-OH, -C(=O)-O-CH ₃ , -C(=O)-O-C ₂ H ₅ , -C(=O)-O-CH ₂ -CH ₂ -CH ₃ , -C(=O)- O-CH(CH ₃ ) ₂ , -C(=O)-O-C(CH ₃ )s, -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ - CH ₂ -CH ₃ , -C(=O)-CH(CHs) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , - SCF ₃ , -OH, -SH, -NH ₂ , -NH-CH ₃ , -NH-C ₂ H ₅ , -NH-CH ₂ -CH ₂ -CH ₃ , -NH- CH(CHs) ₂ , -NH-C(CHs) ₃ , -N(CH ₃ ) ₂ , -N(C ₂ H ₅ ) ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -

C(=O)-NH ₂ , -C(=O)-NH-CHs, -C(=O)-NH-C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)- N(C ₂ Hs) ₂ and -S(=O) ₂ -CH ₃ .

The heteroatom(s), which are present as ring member(s) in the heteroaryl radical, may, unless defined otherwise, independently be selected from the group consisting of nitrogen, oxygen and sulphur. Preferably the heteroaryl radical comprises 1 , 2, 3 or 4 heteroatom(s).

Suitable bi- or tricyclic heteroaryl radicals, which may optionally be at least mono-substituted, may preferably be selected from the group consisting of indolyl, isoindolyl, quinolinyl, isoquinolinyl, benzo[b]furanyl, benzo[b]thiophenyl, benzo[2,1 ,3]thiadiazolyl, [1 ,2,3]-benzothiadiazolyl, [2,1 ,3]-benzoxadiazolyl, [1 ,2,3]-benzoxadiazolyl, benzoxazolyl, benzothiazolyl, benzisoxazolyl, benzisothiazolyl, imidazo[2,1-b]thiazolyl, 2H- chromenyl, indazolyl and quinazolinyl.

Suitable mono-, bi- or tricyclic heteroaryl radicals, which are condensed with an unsubstituted or at least mono-substituted saturated or unsaturated mono- or bicyclic ring system, may preferably be selected from the group consisting of (4,5,6,7)-tetrahydro-1 H-indolyl, [1 ,3]-benzodioxolyl, [1 ,4]-benzodioxanyl, [1 ,2,3,4]-tetrahydronaphthyl, (2,3)-dihydro-1 H-cyclopenta[b]indolyl, [1 ,2,3,4]- tetrahydroquinolinyl, [1 ,2,3,4]-tetrahydroisoquinolinyl, [1 ,2,3,4]- tetrahydroquinazolinyl and [3,4]-dihydro-2H-benzo[1 ,4]oxazinyl.

Suitable monocyclic heteroaryl radicals, which may optionally be at least mono-substituted, may preferably be selected from the group consisting of pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, thazolyl, pyhdazinyl, pyhmidinyl, pyrazinyl and pyranyl.

A mono- or bicyclic ring system according to the present invention - if not defined otherwise - means a mono- or bicyclic hydrocarbon ring system that may be saturated, unsaturated or aromatic. Each of its different rings may show a different degree of saturation, i.e. it may be saturated, unsaturated or aromatic. Optionally each of the rings of the mono- or bicyclic ring system may contain one or more, preferably 1 , 2 or 3, heteroatom(s) as ring member(s), which may be identical or different and which can preferably be selected from the group consisting of N, O and S. The rings of the mono- or bicyclic ring system are preferably 5-, 6- or 7-membered.

Preferably a mono-or bicyclic ring system according to the present invention is a phenyl or naphthyl ring system.

The term "condensed" according to the present invention means that a ring or ring system is attached to another ring or ring system, whereby the terms "annulated" or "annelated" are also used by those skilled in the art to

designate this kind of attachment.

Such a mono- or bicyclic ring system may - if not defined otherwise - be unsubstituted or substituted by one or more substituents, preferably unsubstituted or substituted with 1 , 2, 3, 4 or 5 substituent(s). Said substituents may preferably be selected independently from the group consisting of Ci _-5 -alkyl, -O-Ci _-5 -alkyl, -S-Ci _-5 -alkyl, -C(=O)-OH, oxo (=O), thioxo (=S), -C(=O)-O-Ci _-5 -alkyl, -O-C(=O)-Ci _-5 -alkyl, F, Cl, Br, I, -CN, -CF ₃ , - OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , -NH(Ci _-5 -alkyl), -N(Ci _-5 -alkyl) ₂ , -NO ₂ , -CHO, - CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH(Ci _-5 -alkyl), -C(=O)-N(Ci _-5 -alkyl) ₂ , -

S(=O) ₂ -Ci _-5 -alkyl, -S(=O) ₂ -phenyl, -0-CFH ₂ , -0-CF ₂ H, -S-CFH ₂ , -S-CF ₂ H, - SO ₃ H, -NH-C(=O)-Ci _-5 -alkyl, -N(Ci _-5 -alkyl)-C(=O)-Ci _-5 -alkyl, -C(=O)-Ci _-5 - perfluoroalkyl, -S(=O) ₂ -NH ₂ , -S(=O) ₂ -NH-Ci _-5 -alkyl, -S(=O) ₂ -NH-phenyl, -NH- S(=O) ₂ -Ci- ₅ -alkyl, cyclobutyl, cyclopropyl, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, morpholinyl, phenyl, phenethyl, phenoxy and benzyl; whereby in each occurrence Ci _-5 -alkyl may be linear or branched and whereby said cyclic substituents may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , -OCF ₃ , - SCF ₃ , -OH, -SH, -NH ₂ and -NO ₂ .

More preferably said substituents may be selected from the group consisting of oxo (=0), thioxo (=S), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -0-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -O- CH(CHs) ₂ , -O-C(CH ₃ ) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CH ₃ ) ₂ , -S-

C(CH ₃ ) ₃ , -C(=O)-OH, -C(=O)-O-CH ₃ , -C(=O)-O-C ₂ H ₅ , -C(=O)-O-CH ₂ -CH ₂ - CH ₃ , -C(=O)-O-CH(CHs) ₂ , -C(=O)-O-C(CH ₃ )s, -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , - C(=O)-CH ₂ -CH ₂ -CHs, -C(=O)-CH(CH ₃ ) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, - CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , -NH-CH ₃ , -NH-C ₂ H ₅ , -NH-CH ₂ -CH ₂ -CH ₃ , -NH-CH(CHs) ₂ , -NH-C(CH ₃ ) ₃ , -N(CH ₃ ) ₂ , -N(C ₂ H ₅ ) ₂ , -NO ₂ , -CHO, -CF ₂ H, -

CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH-CHs, -C(=O)-NH-C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -

C(=O)-N(C ₂ H ₅ )2, -S(=O) ₂ -CH ₃ , -S(=O) ₂ -phenyl, phenyl, phenethyl, phenoxy and benzyl; whereby in each occurrence said cyclic substituents may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ and -

NO ₂ .

If any of the substituents in any of the above defined formulae represents a saturated or unsaturated aliphatic radical, i.e. an alkyl radical, preferably an Ci-io alkyl radical; an alkenyl radical, preferably an C _2- - _I0 alkenyl radical or an alkinyl radical, preferably an C2-10 alkinyl radical; said aliphatic radical may - if not defined otherwise - be unsubstituted or substituted by one or more substituents, preferably unsubstituted or substituted with 1 , 2, 3, 4 or 5 substituent(s). Said substituent(s) may preferably be selected independently from the group consisting of -O-Ci _-5 -alkyl, -S-Ci _-5 -alkyl, F, Cl, Br, I, -CN, -CF ₃ ,

-OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , -NH(Ci _-5 -alkyl) and -N(Ci _-5 -alkyl) ₂ , whereby in each occurrence Ci _-5 -alkyl may be linear or branched. More preferably said substituent(s) may preferably be selected independently from the group consisting Of -O-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , -O-C(CH ₃ ) ₃ , - S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CH ₃ ) ₂ , -S-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN,

-CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , NH-CH ₃ , -NH-C ₂ H ₅ , -NH-CH ₂ -CH ₂ -CH ₃ , -NH-CH(CHs) ₂ , -NH-C(CHs) ₃ , -N(CH ₃ ) ₂ , -N(C ₂ H ₅ ) ₂ .

An alkenyl radical comprises at least one carbon-carbon double bond, an alkinyl radical comprises at least one carbon-carbon triple bond.

Suitable alkyl radicals, which may be substituted by one or more substituents, may preferably be selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, neo- pentyl, n-hexyl, n-heptyl, n-octyl, n-nonyl and n-decyl.

Suitable alkenyl radicals, which may be substituted by one or more substituents, may preferably be selected from the group consisting of vinyl, 1- propenyl, 2-propenyl, 1 -butenyl, 2-butenyl and 3-butenyl.

Suitable alkinyl radicals, which may be substituted by one or more substituents, may preferably be selected from the group consisting of ethinyl, 1 -propinyl, 2-propinyl, 1 -butinyl, 2-butinyl and 3-butinyl.

Preferred is a substituted dimethylcyclobutyl compound of general formula I, wherein the stereoisomers have the general formulae Ia or Ib or Ic or Id,

Ia, Ib,

Ic, Id,

wherein

m, X, Y, R >1 , i R-)2 , i R-)3 , i R-)4 and n have the above defined meanings.

Also preferred is a dimethylcyclobutyl compound of general formula I, wherein n is 0 or 1 ;

and the other substituents have any of the above defined meanings, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding solvate thereof.

Also preferred is a dimethylcyclobutyl compound of general formula I, wherein m is 1 ;

and the other substituents have any of the above defined meanings, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding solvate thereof.

Also preferred is a dimethylcyclobutyl compound of general formula I, wherein

X represents a -OR ⁵ moiety or a -NR ⁶ R ⁷ moiety; a (hetero)cycloaliphatic radical selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl, imidazolidinyl, aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl, pyrazolidinyl, azepanyl (1 ,2,3,6)-tetrahydropyridinyl, (1 ,2,3,4)- tetrahydropyridinyl, (1 ,2,5,6)-tetrahydropyhdinyl, hexahydropyhmidinyl, (5,6)- dihydro-4H-pyrimidinyl, indolinyl, isoindolinyl, (1 ,2,3,4)-tetrahydroquinolinyl, (1 ,2,3,4)-tetrahydroisoquinolinyl and octahydro-cyclopenta[c]pyrrolyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=O), thioxo (=S), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -O-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , -O- C(CHs) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CH ₃ ) ₂ , -S-C(CH ₃ ) ₃ , -

C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=O)-CH(CH ₃ ) ₂ , -C(=O)-

C(CHs) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , -NH-CH ₃ , - NH-C ₂ H ₅ , -NH-CH ₂ -CH ₂ -CH ₃ , -NH-CH(CH ₃ ) ₂ , -NH-C(CH ₃ ) ₃ , -N(CH ₃ J ₂ , - N(C ₂ Hs) ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH-CH ₃ , -C(=O)- NH-C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ and -S(=O) ₂ -CH ₃ ; or an aryl or heteroaryl radical selected from the group consisting of phenyl, naphthyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridinyl, pyhdazinyl, pyrimidinyl, pyrazinyl, quinolinyl, isoquinolinyl, benzo[b]furanyl, benzo[b]thiophenyl, benzothiadiazolyl and imidazo[2,1 -b]thiazolyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -0-CH ₃ , -0-C ₂ H ₅ , - 0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , -O-C(CH ₃ ) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ - CH ₃ , -S-CH(CHs) ₂ , -S-C(CHs) ₃ , -C(=O)-OH, -C(=0)-0-CH _3> -C(=O)-O-C ₂ H ₅ , - C(=O)-O-CH ₂ -CH ₂ -CHs, -C(=O)-O-CH(CH ₃ ) _2> -C(=O)-O-C(CH ₃ ) _3> -C(=0)-

CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CHs, -C(=O)-CH(CH ₃ ) _2> -C(=O)-C(CH ₃ ) _3> F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , -NH-CH ₃ , -NH-C ₂ H ₅ , - NH-CH ₂ -CH ₂ -CH ₃ , -NH-CH(CHs) ₂ , -NH-C(CHs) ₃ , -N(CHs) ₂ , -N(C ₂ H ₅ ) ₂ , -NO ₂ , - CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH _2> -C(=0)-NH-CH _3> -C(=O)-NH-C ₂ H ₅ , -C(=0)- N(CHs) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ and -S(=O) ₂ -CH ₃ ;

and the other substituents have any of the above defined meanings, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding solvate thereof.

Also preferred is a dimethylcyclobutyl compound of general formula I, wherein Y represents a -OR ⁸ moiety; a -NR ⁹ R ¹⁰ moiety; a -C(=O)-OR ¹¹ moiety; a

(hetero)cycloaliphatic radical selected from the group consisting of

cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl, imidazolidinyl, aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl, pyrazolidinyl, azepanyl, (1 ,2,3,6)- tetrahydropyridinyl, (1 ,2,3,4)-tetrahydropyridinyl, (1 ,2,5,6)-tetrahydropyridinyl, hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrinnidinyl, indolinyl, isoindolinyl,

(1 ,2,3,4)-tetrahydroquinolinyl, (1 ,2,3,4)-tetrahydroisoquinolinyl and octahydro- cyclopenta[c]pyrrolyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=O), thioxo (=S), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -O-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -

O-CH(CH ₃ ) ₂ , -0-C(CHs) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CH ₃ ) ₂ , - S-C(CHs) ₃ , -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=O)- CH(CH ₃ ) ₂ , -C(=O)-C(CH ₃ )s, F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, - NH ₂ , -NH-CH ₃ , -NH-C ₂ H ₅ , -NH-CH ₂ -CH ₂ -CH ₃ , -NH-CH(CH ₃ ) ₂ , -NH-C(CH ₃ ) ₃ , - N(CH ₃ ) ₂ , -N(C ₂ Hs) ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH-

CH ₃ , -C(=O)-NH-C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ and -S(=O) ₂ -CH ₃ ; or an aryl or heteroaryl radical selected from the group consisting of phenyl, naphthyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, quinolinyl, isoquinolinyl, benzo[b]furanyl, benzo[b]thiophenyl, benzothiadiazolyl and imidazo[2,1 - b]thiazolyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n- pentyl, -0-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , -O-C(CH ₃ ) ₃ , -S-

CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CH ₃ ) ₂ , -S-C(CH ₃ ) ₃ , -C(=O)-OH, - C(=O)-O-CH ₃ , -C(=O)-O-C ₂ H ₅ , -C(=O)-O-CH ₂ -CH ₂ -CH ₃ , -C(=O)-O-CH(CH ₃ ) ₂ , -C(=O)-O-C(CH ₃ ) ₃ , -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=O)- CH(CH ₃ ) ₂ , -C(=O)-C(CH ₃ )s, F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, - NH ₂ , -NH-CH ₃ , -NH-C ₂ H ₅ , -NH-CH ₂ -CH ₂ -CH ₃ , -NH-CH(CH ₃ ) ₂ , -NH-C(CH ₃ ) ₃ , -

N(CH ₃ ) ₂ , -N(C ₂ Hs) ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH-

CH ₃ , -C(=O)-NH-C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ and -S(=O) ₂ -CH ₃ ;

and the other substituents have any of the above defined meanings, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding solvate thereof.

Also preferred is a dimethylcyclobutyl compound of general formula I, wherein

R ¹ represents a hydrogen atom or a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, neo-pentyl, n-hexyl, vinyl, allyl, ethinyl, -CF ₃ , -CFH ₂ , - CF ₂ H, -CH ₂ -CF ₃ , -CF ₂ -CF ₃ , -CH ₂ -CN, -CH ₂ -CH ₂ -CN, -CH ₂ -OH, -CH ₂ -CH ₂ - OH, -CH ₂ -SH, -CH ₂ -CH ₂ -SH, -CH ₂ -NH ₂ , -CH ₂ -NH-CH ₃ , -CH ₂ -N(CHs) ₂ , -CH ₂ -

N(C ₂ Hs) ₂ , -CH ₂ -NH-C ₂ H ₅ , -CH ₂ -CH ₂ -NH ₂ , -CH ₂ -CH ₂ -NH-CH ₃ , -CH ₂ -CH ₂ - N(CH ₃ ) ₂ , -CH ₂ -CH ₂ -N(C ₂ Hs) ₂ , -CH ₂ -CH ₂ -NH-C ₂ H ₅ , -CH ₂ -CH ₂ -CH ₂ -NH-CH ₃ , - CH ₂ -CH ₂ -CH ₂ -N(CHs) ₂ , -CH ₂ -CH ₂ -CH ₂ -N(C ₂ Hs) ₂ and -CH ₂ -CH ₂ -CH ₂ -NH- C ₂ Hs;

and the other substituents have any of the above defined meanings, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding solvate thereof.

Also preferred is a dimethylcyclobutyl compound of general formula I, wherein

R ² represents a hydrogen atom; a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n- pentyl, neo-pentyl, n-hexyl, vinyl, allyl, ethinyl, -CF ₃ , -CFH ₂ , -CF ₂ H, -CH ₂ -CF ₃ ,

-CF ₂ -CF ₃ , -CH ₂ -CN, -CH ₂ -CH ₂ -CN, -CH ₂ -OH, -CH ₂ -CH ₂ -OH, -CH ₂ -SH, -CH ₂ - CH ₂ -SH, -CH ₂ -NH ₂ , -CH ₂ -NH-CH ₃ , -CH ₂ -N(CHs) ₂ , -CH ₂ -N(C ₂ Hs) ₂ , -CH ₂ -NH- C ₂ H ₅ , -CH ₂ -CH ₂ -NH ₂ , -CH ₂ -CH ₂ -NH-CH ₃ , -CH ₂ -CH ₂ -N(CHs) ₂ , -CH ₂ -CH ₂ - N(C ₂ Hs) ₂ , -CH ₂ -CH ₂ -NH-C ₂ H ₅ , -CH ₂ -CH ₂ -CH ₂ -NH-CH ₃ , -CH ₂ -CH ₂ -CH ₂ - N(CH ₃ ) ₂ , -CH ₂ -CH ₂ -CH ₂ -N(C ₂ Hs) ₂ and -CH ₂ -CH ₂ -CH ₂ -NH-C ₂ H ₅ ; a

(hetero)cycloaliphatic radical selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl, imidazolidinyl, aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl, pyrazolidinyl and azepanyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=0), thioxo (=S), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -O-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , -O- C(CHs) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CH ₃ ) ₂ , -S-C(CH ₃ ) ₃ , - C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=O)-CH(CH ₃ ) ₂ , -C(=O)-

C(CHs) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , -NH-CH ₃ , - NH-C ₂ H ₅ , -NH-CH ₂ -CH ₂ -CH ₃ , -NH-CH(CH ₃ ) ₂ , -NH-C(CH ₃ ) ₃ , -N(CH ₃ ) ₂ , - N(C ₂ Hs) ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH-CH ₃ , -C(=O)- NH-C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ and -S(=O) ₂ -CH ₃ ; or an aryl or heteroaryl radical selected from the group consisting of phenyl, naphthyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridinyl, pyhdazinyl, pyhmidinyl, pyrazinyl, quinolinyl, isoquinolinyl, benzo[b]furanyl, benzo[b]thiophenyl, benzothiadiazolyl and imidazo[2,1 -b]thiazolyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -0-CH ₃ , -0-C ₂ H ₅ , - 0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , -O-C(CH ₃ ) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ - CH ₃ , -S-CH(CHs) ₂ , -S-C(CHs) ₃ , -C(=O)-OH, -C(=O)-O-CH ₃ , -C(=O)-O-C ₂ H ₅ , - C(=O)-O-CH ₂ -CH ₂ -CHs, -C(=O)-O-CH(CH ₃ ) ₂ , -C(=O)-O-C(CH ₃ ) ₃ , -C(=O)-

CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=O)-CH(CH ₃ ) ₂ , -C(=O)-C(CH ₃ ) ₃ ,

F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , -NH-CH ₃ , -NH-C ₂ H ₅ , - NH-CH ₂ -CH ₂ -CH ₃ , -NH-CH(CHs) ₂ , -NH-C(CH ₃ ) ₃ , -N(CH ₃ J ₂ , -N(C ₂ Hs) ₂ , -NO ₂ , - CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH-CH ₃ , -C(=O)-NH-C ₂ H ₅ , -C(=O)- N(CHs) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ and -S(=O) ₂ -CH ₃ ;

and the other substituents have any of the above defined meanings, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding solvate thereof.

Also preferred is a dimethylcyclobutyl compound of general formula I, wherein R ³ and R ⁴ both represent a hydrogen atom;

and the other substituents have any of the above defined meanings, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding solvate thereof.

Also preferred is a dimethylcyclobutyl compound of general formula I, wherein

R ⁵ and R ⁸ , independently of one another, each represent a hydrogen atom; a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, neo-pentyl, n-hexyl, vinyl, allyl, ethinyl, -CF ₃ , -CFH ₂ , -CF ₂ H, -CH ₂ -CF ₃ , -CF ₂ -CF ₃ , -CH ₂ -CN, -CH ₂ - CH ₂ -CN, -CH ₂ -OH, -CH ₂ -CH ₂ -OH, -CH ₂ -SH, -CH ₂ -CH ₂ -SH, -CH ₂ -NH ₂ , -CH ₂ - NH-CH ₃ , -CH ₂ -N(CHs) ₂ , -CH ₂ -N(C ₂ Hs) ₂ , -CH ₂ -NH-C ₂ H ₅ , -CH ₂ -CH ₂ -NH ₂ , -CH ₂ - CH ₂ -NH-CH ₃ , -CH ₂ -CH ₂ -N(CHs) ₂ , -CH ₂ -CH ₂ -N(C ₂ Hs) ₂ , -CH ₂ -CH ₂ -NH-C ₂ H ₅ , - CH ₂ -CH ₂ -CH ₂ -NH-CH ₃ , -CH ₂ -CH ₂ -CH ₂ -N(CHs) ₂ , -CH ₂ -CH ₂ -CH ₂ -N(C ₂ Hs) ₂ and

-CH ₂ -CH ₂ -CH ₂ -NH-C ₂ H ₅ ; a (hetero)cycloaliphatic radical selected from the

group consisting of imidazolidinyl, aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl, pyrazolidinyl, azepanyl, (1 ,2,3,6)-tetrahydropyhdinyl, (1 ,2,3,4)-tetrahydropyridinyl, (1 ,2,5,6)- tetrahydropyridinyl, hexahydropyrimidinyl, (5,6)-dihydro-4H-pyhmidinyl, indolinyl, isoindolinyl, (1 ,2,3,4)-tetrahydroquinolinyl, (1 ,2,3,4)- tetrahydroisoquinolinyl and octahydro-cyclopenta[c]pyrrolyl; which may be bonded via a -(CH ₂ )i, 2or3-group and which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=O), thioxo (=S), methyl, ethyl, n- propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -O-CH ₃ , -O-

C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , -O-C(CH ₃ ) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ - CH ₂ -CH ₃ , -S-CH(CHs) ₂ , -S-C(CH ₃ ) ₃ , -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ - CH ₂ -CH ₃ , -C(=O)-CH(CH ₃ ) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , - SCF ₃ , -OH, -SH, -NH ₂ , -NH-CH ₃ , -NH-C ₂ H ₅ , -NH-CH ₂ -CH ₂ -CH ₃ , -NH- CH(CHs) ₂ , -NH-C(CHs) ₃ , -N(CH ₃ ) ₂ , -N(C ₂ H ₅ ) ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -

C(=O)-NH ₂ , -C(=O)-NH-CHs, -C(=O)-NH-C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)- N(C ₂ H ₅ ) ₂ and -S(=O) ₂ -CH ₃ ; an aryl or heteroaryl radical selected from the group consisting of phenyl, naphthyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, quinolinyl, isoquinolinyl, benzo[b]furanyl, benzo[b]thiophenyl, benzothiadiazolyl and imidazo[2,1 -b]thiazolyl, which may be bonded via a - (CH ₂ )i, _{2 θ} r3-group and which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -0-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , -O- C(CHs) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CH ₃ ) ₂ , -S-C(CH ₃ ) ₃ , - C(=O)-OH, -C(=O)-O-CH ₃ , -C(=O)-O-C ₂ H ₅ , -C(=O)-O-CH ₂ -CH ₂ -CH ₃ , -C(=O)- O-CH(CH ₃ ) ₂ , -C(=O)-O-C(CH ₃ )s, -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ - CH ₂ -CH ₃ , -C(=O)-CH(CH ₃ ) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -

SCF ₃ , -OH, -SH, -NH ₂ , -NH-CH ₃ , -NH-C ₂ H ₅ , -NH-CH ₂ -CH ₂ -CH ₃ , -NH-

CH(CHs) ₂ , -NH-C(CHs) ₃ , -N(CH ₃ ) ₂ , -N(C ₂ Hs) ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , - C(=O)-NH _2j -C(=O)-NH-CH ₃ , -C(=O)-NH-C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)- N(C ₂ Hs) ₂ and -S(=O) ₂ -CH ₃ or a -C(=O)-R ¹² moiety;

and the other substituents have any of the above defined meanings, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding solvate thereof.

Also preferred is a dimethylcyclobutyl compound of general formula I, wherein R ⁶ , R ⁷ , R ⁹ and R ¹⁰ , independently of one another, each represent a hydrogen atom; a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, neo-pentyl, n-hexyl, vinyl, allyl, ethinyl, -CF ₃ , -CFH ₂ , -CF ₂ H, -CH ₂ -CF ₃ , -CF ₂ -CF ₃ , -CH ₂ -CN, -CH ₂ - CH ₂ -CN, -CH ₂ -OH, -CH ₂ -CH ₂ -OH, -CH ₂ -SH, -CH ₂ -CH ₂ -SH, -CH ₂ -NH ₂ , -CH ₂ - NH-CH ₃ , -CH ₂ -N(CHs) ₂ , -CH ₂ -N(C ₂ Hs) ₂ , -CH ₂ -NH-C ₂ H ₅ , -CH ₂ -CH ₂ -NH ₂ , -CH ₂ -

CH ₂ -NH-CH ₃ , -CH ₂ -CH ₂ -N(CHs) ₂ , -CH ₂ -CH ₂ -N(C ₂ Hs) ₂ , -CH ₂ -CH ₂ -NH-C ₂ H ₅ , - CH ₂ -CH ₂ -CH ₂ -NH-CHs, -CH ₂ -CH ₂ -CH ₂ -N(CHS) ₂ , -CH ₂ -CH ₂ -CH ₂ -N(C ₂ HS) ₂ and -CH ₂ -CH ₂ -CH ₂ -NH-C ₂ H ₅ ; a (hetero)cycloaliphatic radical selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl, imidazolidinyl, aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl, pyrazolidinyl and azepanyl, which may be bonded via a -(CH ₂ )i, _{2 or 3} -group and which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=0), thioxo (=S), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n- pentyl, -Q-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , -O-C(CH ₃ ) ₃ , -S-

CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CH ₃ ) ₂ , -S-C(CH ₃ ) ₃ , -C(=O)-CH ₃ , - C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=O)-CH(CH ₃ ) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , -NH-CH ₃ , -NH-C ₂ H ₅ , -NH- CH ₂ -CH ₂ -CH ₃ , -NH-CH(CHs) ₂ , -NH-C(CH ₃ ) ₃ , -N(CH ₃ ) ₂ , -N(C ₂ H ₅ ) ₂ , -NO ₂ , - CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH-CH ₃ , -C(=O)-NH-C ₂ H ₅ , -C(=O)-

N(CH ₃ ) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ and -S(=O) ₂ -CH ₃ ; or an aryl or heteroaryl radical selected from the group consisting of phenyl, naphthyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridinyl, pyhdazinyl, pyhmidinyl, pyrazinyl, quinolinyl, isoquinolinyl, benzo[b]furanyl, benzo[b]thiophenyl, benzothiadiazolyl and imidazo[2,1 -b]thiazolyl, which may be bonded via a - (CH ₂ )i, _{2 θ} r3-group and which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -0-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , -O-

C(CHs) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CH ₃ ) ₂ , -S-C(CH ₃ ) ₃ , - C(=O)-OH, -C(=O)-O-CH ₃ , -C(=O)-O-C ₂ H ₅ , -C(=O)-O-CH ₂ -CH ₂ -CH ₃ , -C(=O)- O-CH(CH ₃ ) ₂ , -C(=O)-O-C(CH ₃ )s, -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ - CH ₂ -CH ₃ , -C(=O)-CH(CHs) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , - SCF ₃ , -OH, -SH, -NH ₂ , -NH-CH ₃ , -NH-C ₂ H ₅ , -NH-CH ₂ -CH ₂ -CH ₃ , -NH-

CH(CHs) ₂ , -NH-C(CHs) ₃ , -N(CH ₃ ) ₂ , -N(C ₂ H ₅ ) ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , - C(=O)-NH ₂ , -C(=O)-NH-CHs, -C(=O)-NH-C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)- N(C ₂ Hs) ₂ and -S(=O) ₂ -CH ₃ ;

and the other substituents have any of the above defined meanings, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding solvate thereof.

Also preferred is a dimethylcyclobutyl compound of general formula I, wherein

R ⁶ and R ⁷ together with the bridging nitrogen atom form a heterocyclic ring selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, aziridinyl, azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl, azepanyl, diazepanyl, azocanyl, (1 ,2,3,6)- tetrahydropyridinyl, (1 ,2,3,4)-tetrahydropyhdinyl, (1 ,2,5,6)-tetrahydropyhdinyl, hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl, indolinyl, isoindolinyl, (1 ,2,3,4)-tetrahydroquinolinyl, (1 ,2,3,4)-tetrahydroisoquinolinyl, octahydro- cyclopenta[c]pyrrolyl, decahydroquinolinyl, dodecahydrocarbazolyl, 9H- carbazolyl, decahydroisoquinolinyl, (2,3)-dihydro-1 H-cyclopenta[b]indolyl, [1 ,2,3,4]-tetrahydroquinazolinyl, [3,4]-dihydro-2H-benzo[1 ,4]oxazinyl, (4,5,6,7)-tetrahydro-1 H-indolyl, pyrrolyl, imidazolyl, pyrazolyl and triazolyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=O), thioxo (=S), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -O-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , -O- C(CHs) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CH ₃ ) ₂ , -S-C(CH ₃ ) ₃ , - C(=O)-OH, -C(=O)-O-CH ₃ , -C(=O)-O-C ₂ H ₅ , -C(=O)-O-CH ₂ -CH ₂ -CH ₃ , -C(=O)- O-CH(CH ₃ ) ₂ , -C(=O)-O-C(CH ₃ )s, -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -

CH ₂ -CH ₃ , -C(=O)-CH(CHs) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , - SCF ₃ , -OH, -SH, -NH ₂ , -NH-CH ₃ , -NH-C ₂ H ₅ , -NH-CH ₂ -CH ₂ -CH ₃ , -NH- CH(CHs) ₂ , -NH-C(CHs) ₃ , -N(CH ₃ ) ₂ , -N(C ₂ H ₅ ) ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , - C(=O)-NH ₂ , -C(=O)-NH-CHs, -C(=O)-NH-C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)- N(C ₂ H ₅ ) ₂ , -S(=O) ₂ -CH ₃ , phenyl, phenethyl, phenoxy and benzyl, whereby said cyclic substituents may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , -OCF ₃ , - SCF ₃ , -OH, -SH, -NH ₂ and -NO ₂ ;

and the other substituents have any of the above defined meanings, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding solvate thereof.

Also preferred is a dimethylcyclobutyl compound of general formula I, wherein

R ⁹ and R ¹⁰ together with the bridging nitrogen atom form a heterocyclic ring selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, aziridinyl, azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl, azepanyl, diazepanyl, azocanyl, (1 ,2,3,6)- tetrahydropyridinyl, (1 ,2,3,4)-tetrahydropyhdinyl, (1 ,2,5,6)-tetrahydropyhdinyl, hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl, indolinyl, isoindolinyl, (1 ,2,3,4)-tetrahydroquinolinyl, (1 ,2,3,4)-tetrahydroisoquinolinyl, octahydro- cyclopenta[c]pyrrolyl, decahydroquinolinyl, dodecahydrocarbazolyl, 9H- carbazolyl, decahydroisoquinolinyl, (2,3)-dihydro-1 H-cyclopenta[b]indolyl, [1 ,2,3,4]-tetrahydroquinazolinyl, [3,4]-dihydro-2H-benzo[1 ,4]oxazinyl, (4,5,6,7)-tetrahydro-1 H-indolyl, pyrrolyl, imidazolyl, pyrazolyl and triazolyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=O), thioxo (=S), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -O-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , -O- C(CHs) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CH ₃ ) ₂ , -S-C(CH ₃ ) ₃ , - C(=O)-OH, -C(=O)-O-CH ₃ , -C(=O)-O-C ₂ H ₅ , -C(=O)-O-CH ₂ -CH ₂ -CH ₃ , -C(=O)-

O-CH(CH ₃ ) ₂ , -C(=O)-O-C(CH ₃ )s, -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ - CH ₂ -CH ₃ , -C(=O)-CH(CHs) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , - SCF ₃ , -OH, -SH, -NH ₂ , -NH-CH ₃ , -NH-C ₂ H ₅ , -NH-CH ₂ -CH ₂ -CH ₃ , -NH- CH(CHs) ₂ , -NH-C(CHs) ₃ , -N(CH ₃ ) ₂ , -N(C ₂ H ₅ ) ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , - C(=O)-NH ₂ , -C(=O)-NH-CHs, -C(=O)-NH-C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)-

N(C ₂ H ₅ ) ₂ , -S(=O) ₂ -CH ₃ , phenyl, phenethyl, phenoxy and benzyl, whereby

said cyclic substituents may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , -OCF ₃ , - SCF ₃ , -OH, -SH, -NH ₂ and -NO ₂ ;

and the other substituents have any of the above defined meanings, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding solvate thereof.

Also preferred is a dimethylcyclobutyl compound of general formula I, wherein

R ¹¹ and R ¹² , independently of one another, represent a hydrogen atom; a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, neo-pentyl, n-hexyl, vinyl, allyl, ethinyl, -CF ₃ , -CFH ₂ , -CF ₂ H, -CH ₂ -CF ₃ , -CF ₂ -CF ₃ , -CH ₂ -CN, -CH ₂ - CH ₂ -CN, -CH ₂ -OH, -CH ₂ -CH ₂ -OH, -CH ₂ -SH, -CH ₂ -CH ₂ -SH, -CH ₂ -NH ₂ , -CH ₂ - NH-CH ₃ , -CH ₂ -N(CHs) ₂ , -CH ₂ -N(C ₂ Hs) ₂ , -CH ₂ -NH-C ₂ H ₅ , -CH ₂ -CH ₂ -NH ₂ , -CH ₂ - CH ₂ -NH-CH ₃ , -CH ₂ -CH ₂ -N(CHs) ₂ , -CH ₂ -CH ₂ -N(C ₂ Hs) ₂ , -CH ₂ -CH ₂ -NH-C ₂ H ₅ , -

CH ₂ -CH ₂ -CH ₂ -NH-CH ₃ , -CH ₂ -CH ₂ -CH ₂ -N(CHs) ₂ , -CH ₂ -CH ₂ -CH ₂ -N(C ₂ Hs) ₂ and -CH ₂ -CH ₂ -CH ₂ -NH-C ₂ H ₅ ; a (hetero)cycloaliphatic radical selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl, imidazolidinyl, aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl, pyrazolidinyl and azepanyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=0), thioxo (=S), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -0-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -O- CH(CHs) ₂ , -0-C(CHs) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CHs) ₂ , -S-

C(CHs) ₃ , -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=O)-CH(CH ₃ ) ₂ ,

-C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , -NH- CH ₃ , -NH-C ₂ H ₅ , -NH-CH ₂ -CH ₂ -CH ₃ , -NH-CH(CH ₃ ) ₂ , -NH-C(CH ₃ ) ₃ , -N(CH ₃ ) ₂ , - N(C ₂ Hs) ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH-CH ₃ , -C(=O)- NH-C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ and -S(=O) ₂ -CH ₃ ; or an aryl or heteroaryl radical selected from the group consisting of phenyl, naphthyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridinyl, pyhdazinyl, pyhmidinyl, pyrazinyl, quinolinyl, isoquinolinyl, benzo[b]furanyl, benzo[b]thiophenyl, benzothiadiazolyl and imidazo[2,1-b]thiazolyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -0-CH ₃ , -0-C ₂ H ₅ , - 0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , -O-C(CH ₃ ) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ - CH ₃ , -S-CH(CHs) ₂ , -S-C(CHs) ₃ , -C(=O)-OH, -C(=O)-O-CH ₃ , -C(=O)-O-C ₂ H ₅ , - C(=O)-O-CH ₂ -CH ₂ -CHs, -C(=O)-O-CH(CH ₃ ) ₂ , -C(=O)-O-C(CH ₃ ) ₃ , -C(=O)-

CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=O)-CH(CH ₃ ) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , -NH-CH ₃ , -NH-C ₂ H ₅ , - NH-CH ₂ -CH ₂ -CH ₃ , -NH-CH(CHs) ₂ , -NH-C(CH ₃ ) ₃ , -N(CH ₃ ) ₂ , -N(C ₂ H ₅ ) ₂ , -NO ₂ , - CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH-CH ₃ , -C(=O)-NH-C ₂ H ₅ , -C(=O)- N(CHs) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ and -S(=O) ₂ -CH ₃ ;

and the other substituents have any of the above defined meanings, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding solvate thereof.

Particularly preferred is a dimethylcyclobutyl compound of general formula I, wherein

m is 1 or 2;

n is 0 or 1 ;

X represents a -OR ⁵ moiety or a -NR ⁶ R ⁷ moiety; or a (hetero)cycloaliphatic radical selected from the group consisting of pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl, pyrazolidinyl, azepanyl, (1 ,2,3,6)- tetrahydropyridinyl, (1 ,2,3,4)-tetrahydropyhdinyl, (1 ,2,5,6)-tetrahydropyhdinyl, hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl, indolinyl, isoindolinyl, (1 ,2,3,4)-tetrahydroquinolinyl, (1 ,2,3,4)-tetrahydroisoquinolinyl and octahydro- cyclopenta[c]pyrrolyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=O), thioxo (=S), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -O-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , - O-CH(CH ₃ ) ₂ , -0-C(CHs) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CH ₃ ) ₂ , - S-C(CHs) ₃ , -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=O)- CH(CHs) ₂ , -C(=O)-C(CH ₃ )s, F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH and -NH ₂ ;

Y represents a -OR ⁸ moiety; a -NR ⁹ R ¹⁰ moiety; a -C(=O)-OR ¹¹ moiety; or a (hetero)cycloaliphatic radical selected from the group consisting of pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl, piperazinyl, pyrazolidinyl, azepanyl, (1 ,2,3,6)-tetrahydropyridinyl, (1 ,2,3,4)- tetrahydropyridinyl, (1 ,2,5,6)-tetrahydropyhdinyl, hexahydropyrimidinyl, (5,6)- dihydro-4H-pyrimidinyl, indolinyl, isoindolinyl, (1 ,2,3,4)-tetrahydroquinolinyl, (1 ,2,3,4)-tetrahydroisoquinolinyl and octahydro-cyclopenta[c]pyrrolyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=0), thioxo (=S), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -0-CH ₃ , -0-C ₂ H ₅ , -0-CH ₂ -CH ₂ -CH ₃ , -O-CH(CH ₃ ) ₂ , -O- C(CHs) ₃ , -S-CH ₃ , -S-C ₂ H ₅ , -S-CH ₂ -CH ₂ -CH ₃ , -S-CH(CH ₃ ) ₂ , -S-C(CH ₃ ) ₃ , - C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=O)-CH(CH ₃ ) ₂ , -C(=O)-

C(CHs) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH and -NH ₂ ;

R ¹ represents a hydrogen atom or a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, -CF ₃ , -CFH ₂ , -CF ₂ H, -CH ₂ -CF ₃ , -CF ₂ -CF ₃ , -CH ₂ -CN, -CH ₂ - CH ₂ -CN, -CH ₂ -OH, -CH ₂ -CH ₂ -OH, -CH ₂ -SH and -CH ₂ -CH ₂ -SH;

R ² represents a hydrogen atom; a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n- pentyl, -CF ₃ , -CFH ₂ , -CF ₂ H, -CH ₂ -CF ₃ , -CF ₂ -CF ₃ , -CH ₂ -CN, -CH ₂ -CH ₂ -CN, - CH ₂ -OH, -CH ₂ -CH ₂ -OH, -CH ₂ -SH and -CH ₂ -CH ₂ -SH; or an aryl or heteroaryl radical selected from the group consisting of phenyl, naphthyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, thazolyl and pyridinyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -O- CH ₃ , -0-C ₂ H ₅ -S-CH ₃ , -S-C ₂ H ₅ , -C(=O)-OH, -C(=O)-O-CH ₃ , -C(=O)-O-C ₂ H ₅ , - C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, - NH ₂ , -NO ₂ , -CHO, -CF ₂ H and -CFH ₂ ;

R ³ and R ⁴ both represent a hydrogen atom;

R ⁵ and R ⁸ , independently of one another, each represent a hydrogen atom; a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, -CF ₃ , -CFH ₂ , -CF ₂ H,

-CH ₂ -CF ₃ , -CF ₂ -CF ₃ , -CH ₂ -CN, -CH ₂ -CH ₂ -CN, -CH ₂ -OH, -CH ₂ -CH ₂ -OH and - CH ₂ -SH; an aryl or heteroaryl radical selected from the group consisting of phenyl, naphthyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, quinolinyl, isoquinolinyl, benzo[b]furanyl, benzo[b]thiophenyl, benzothiadiazolyl and

imidazo[2,1-b]thiazolyl, which may be bonded via a -(CH ₂ )i, 2 or3-group and which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -O- CH ₃ , -0-C ₂ H ₅ , -S-CH ₃ , -S-C ₂ H ₅ , -C(=O)-OH, -C(=O)-O-CH ₃ , -C(=O)-O-C ₂ H ₅ ,

-C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, - NH ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ and -S(=O) ₂ -CH ₃ or a -C(=O)-R ¹² moiety;

R ⁶ , R ⁷ , R ⁹ and R ¹⁰ , independently of one another, each represent a hydrogen atom; a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, -CF ₃ , -CFH ₂ , -CF ₂ H, -CH ₂ -CF ₃ , -CF ₂ -CF ₃ , -CH ₂ -CN, -CH ₂ -CH ₂ -CN, -CH ₂ -OH, -CH ₂ -CH ₂ -OH, -CH ₂ - SH and -CH ₂ -CH ₂ -SH, ; or an aryl or heteroaryl radical selected from the group consisting of phenyl, naphthyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, quinolinyl, isoquinolinyl, benzo[b]furanyl, benzo[b]thiophenyl, benzothiadiazolyl and imidazo[2,1 -b]thiazolyl, which may be bonded via a - (CH ₂ )i, _{2 θ} r3-group and which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, -0-CH ₃ , -0-C ₂ H ₅ , -S-CH ₃ , -S-C ₂ H ₅ , -C(=O)-OH, -C(=O)-O-CH ₃ , - C(=O)-O-C ₂ H ₅ , -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , - SCF ₃ , -OH, -SH, -NH ₂ -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ and -S(=O) ₂ -

CH ₃ ;

or R ⁶ and R ⁷ together with the bridging nitrogen atom form a heterocyclic ring selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, aziridinyl, azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl, azepanyl, diazepanyl, azocanyl, (1 ,2,3,6)-

tetrahydropyridinyl, (1 ,2,3,4)-tetrahydropyridinyl, (1 ,2,5,6)-tetrahydropyridinyl, hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl, indolinyl, isoindolinyl, (1 ,2,3,4)-tetrahydroquinolinyl, (1 ,2,3,4)-tetrahydroisoquinolinyl, octahydro- cyclopenta[c]pyrrolyl, decahydroquinolinyl, dodecahydrocarbazolyl, 9H- carbazolyl, decahydroisoquinolinyl, (2,3)-dihydro-1 H-cyclopenta[b]indolyl,

[1 ,2,3,4]-tetrahydroquinazolinyl, [3,4]-dihydro-2H-benzo[1 ,4]oxazinyl, (4,5,6,7)-tetrahydro-1 H-indolyl, pyrrolyl, imidazolyl, pyrazolyl and triazolyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=O), thioxo (=S), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, -

0-CH ₃ , -0-C ₂ H ₅ , -S-CH ₃ , -S-C ₂ H ₅ , -C(=O)-OH, -C(=O)-O-CH ₃ , -C(=O)-O- C ₂ H ₅ , -C(=O)-O-CH ₂ -CH ₂ -CH ₃ , -C(=O)-O-CH(CH ₃ ) ₂ , -C(=O)-O-C(CH ₃ ) ₃ , - C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=O)-CH(CH ₃ ) ₂ , -C(=O)- C(CHs) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH-CH ₃ , -C(=O)-NH-C ₂ H ₅ , -C(=O)-

N(CH ₃ ) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ , -S(=O) ₂ -CH ₃ ; phenyl, phenethyl and benzyl, whereby said cyclic substituents may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , - OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ and -NO ₂ ;

or R ⁹ and R ¹⁰ together with the bridging nitrogen atom form a heterocyclic ring selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, aziridinyl, azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl, azepanyl, diazepanyl, azocanyl, (1 ,2,3,6)- tetrahydropyridinyl, (1 ,2,3,4)-tetrahydropyhdinyl, (1 ,2,5,6)-tetrahydropyhdinyl, hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl, indolinyl, isoindolinyl, (1 ,2,3,4)-tetrahydroquinolinyl, (1 ,2,3,4)-tetrahydroisoquinolinyl, octahydro- cyclopenta[c]pyrrolyl, decahydroquinolinyl, dodecahydrocarbazolyl, 9H- carbazolyl, decahydroisoquinolinyl, (2,3)-dihydro-1 H-cyclopenta[b]indolyl,

[1 ,2,3,4]-tetrahydroquinazolinyl, [3,4]-dihydro-2H-benzo[1 ,4]oxazinyl,

(4,5,6,7)-tetrahydro-1 H-indolyl, pyrrolyl, imidazolyl, pyrazolyl and triazolyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, -0-CH ₃ , -O-C ₂ H ₅ , -S- CH ₃ , -S-C ₂ H ₅ , -C(=O)-OH, -C(=O)-O-CH ₃ , -C(=O)-O-C ₂ H ₅ , -C(=O)-O-CH ₂ -

CH ₂ -CH ₃ , -C(=O)-O-CH(CH ₃ ) ₂ , -C(=O)-O-C(CH ₃ ) ₃ , -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=O)-CH(CH ₃ ) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, - CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=O)- NH ₂ , -C(=O)-NH-CH ₃ , -C(=O)-NH-C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ , - S(=O) ₂ -CH ₃ , phenyl, phenethyl and benzyl, whereby said cyclic substituents may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ and - NO ₂ ;

and R ¹¹ and R ¹² , independently of one another, represent a hydrogen atom; a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, -CF ₃ , -CFH ₂ , -CF ₂ H, -CH ₂ -CF ₃ , -CF ₂ -CF ₃ , -CH ₂ -CN, -CH ₂ -CH ₂ -CN, -CH ₂ -OH, -CH ₂ -CH ₂ -OH, -CH ₂ - SH and -CH ₂ -CH ₂ -SH; or an aryl or heteroaryl radical selected from the group consisting of phenyl, naphthyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl, and pyridinyl, which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -0-CH ₃ , -0-C ₂ H ₅ , -S-CH ₃ , -S-C ₂ H ₅ , F, CI, Br, I, -CN, -CF ₃ , -

OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , - C(=O)-NH-CH ₃ , -C(=O)-NH-C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ and - S(=O) ₂ -CH ₃ ;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its

stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a salt thereof, or a corresponding solvate thereof.

More particularly preferred is a dimethylcyclobutyl compound of general formula I, wherein

m is 1 ; n is 0 or 1 ;

X represents a -OR ⁵ moiety or a -NR ⁶ R ⁷ moiety;

Y represents a -OR ⁸ moiety; a -NR ⁹ R ¹⁰ moiety or a -C(=O)-OR ¹¹ moiety;

R ¹ represents a hydrogen atom or a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl;

R ² represents a hydrogen atom; a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or an aryl radical selected from the group consisting of phenyl and naphthyl, which may be unsubstituted or substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n-pentyl, -O- CH ₃ , -0-C ₂ H ₅ -S-CH ₃ , -S-C ₂ H ₅ , -C(=O)-OH, -C(=O)-O-CH ₃ , -C(=O)-O-C ₂ H ₅ , - C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -

NH ₂ , -NO ₂ , -CHO, -CF ₂ H and -CFH ₂ ;

R ³ and R ⁴ both represent a hydrogen atom;

R ⁵ and R ⁸ , independently of one another, each represent a hydrogen atom; a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; an aryl radical

selected from the group consisting of phenyl and naphthyl, which may be bonded via a -(CH ₂ )i, 2or3-group and which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n- butyl, tert-butyl, -O-CH ₃ , -0-C ₂ H ₅ -F, CI, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -

SH, -NH ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ and -S(=O) ₂ -CH ₃ or a -C(=O)-R ¹² moiety;

R ⁶ , R ⁷ , R ⁹ and R ¹⁰ , independently of one another, each represent a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n- butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or an aryl or heteroaryl radical selected from the group consisting of phenyl and naphthyl, which may be bonded via a -(CH ₂ )i, _{2 or} 3-group and which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n- butyl, tert-butyl, sec-butyl, isobutyl, -O-CH ₃ , -0-C ₂ H ₅ , -S-CH ₃ , -S-C ₂ H ₅ , F, CI, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , - C(=O)-NH ₂ and -S(=O) ₂ -CH ₃ ;

or R ⁶ and R ⁷ together with the bridging nitrogen atom form a moiety selected from the group consisting of

which may be unsubstituted or optionally substituted in any position including the -NH-groups with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=O), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, -0-CH ₃ , -0-C ₂ H ₅ , -S-CH ₃ , -S-C ₂ H ₅ , -C(=O)-OH, -C(=O)- O-CH ₃ , -C(=O)-O-C ₂ H ₅ , -C (=O)-O-CH ₂ -CH ₂ -CH ₃ , -C(=O)-O-CH(CH ₃ ) ₂ , - C(=O)-O-C(CH ₃ ) ₃ , -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=0)- CH(CH ₃ ) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, - NH ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH-CH ₃ , -C(=O)-NH-

C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ , -S(=O) ₂ -CH ₃ , phenyl, phenethyl and benzyl, whereby said cyclic substituents may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , - OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ and -NO ₂ ;

or R ⁹ and R ¹⁰ together with the bridging nitrogen atom form a moiety selected from the group consisting of

which may be unsubstituted or optionally substituted in any position including the -NH-groups with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=O), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, -O-CH ₃ , -0-C ₂ H ₅ , -S-CH ₃ , -S-C ₂ H ₅ , -C(=O)-OH, -C(=O)- O-CH ₃ , -C(=O)-O-C ₂ H ₅ , -C(=O)-O-CH ₂ -CH ₂ -CH ₃ , -C(=O)-O-CH(CH ₃ ) ₂ , - C(=O)-O-C(CH ₃ ) ₃ , -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=0)- CH(CH ₃ ) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, - NH ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH-CH ₃ , -C(=O)-NH- C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ , -S(=O) ₂ -CH ₃ , phenyl, phenethyl and benzyl, whereby said cyclic substituents may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , - OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ and -NO ₂ ;

and R ¹¹ and R ¹² , independently of one another, represent a hydrogen atom; or a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a salt thereof, or a corresponding solvate thereof.

Even more particularly preferred is a dimethylcyclobutyl compound of general formula I, wherein

m is 1 ; n is 0 or 1 ;

X represents a -OR ⁵ moiety or a -NR ⁶ R ⁷ moiety;

Y represents a -OR ⁸ moiety; a -NR ⁹ R ¹⁰ moiety or a -C(=O)-OR ¹¹ moiety;

R ¹ represents a hydrogen atom or a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl;

R ² represents a hydrogen atom; a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or a phenyl radical which may be unsubstituted or substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n- pentyl, -O-CH ₃ , -0-C ₂ H ₅ , F, CI, Br, I, -CN, -CF ₃ , -OCF ₃ and -SCF ₃ ;

R ³ and R ⁴ both represent a hydrogen atom;

R ⁵ and R ⁸ , independently of one another, each represent a hydrogen atom; a phenyl radical, which may be bonded via a -(CH ₂ )i, 2 or 3-group and which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, -0-CH ₃ , -0-C ₂ H ₅ , F, Cl, Br, I, -CN, -CF ₃ and -

OCF ₃ Or a -C(=O)-R ¹² moiety;

R ⁶ , R ⁷ , R ⁹ and R ¹⁰ , independently of one another, each represent a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n- butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or a phenyl radical, which may be bonded via a -(CH ₂ )i, 2or3-group and which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n- butyl, tert-butyl, sec-butyl, isobutyl, -O-CH ₃ , -0-C ₂ H ₅ , F, CI, Br, I, -CN, -CF ₃ , - OCF ₃ and -SCF ₃ ;

or R ⁶ and R ⁷ together with the bridging nitrogen atom form a moiety selected from the group consisting of

which may be unsubstituted or optionally substituted in any position including the -NH-groups with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=0), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, phenyl, phenethyl and benzyl, whereby said cyclic substituents may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, - NH ₂ and -NO ₂ ;

or R ⁹ and R ¹⁰ together with the bridging nitrogen atom form a moiety selected from the group consisting of

which may be unsubstituted or optionally substituted in any position including the -NH-groups with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=0), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, phenyl, phenethyl and benzyl, whereby said cyclic substituents may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, - NH ₂ and -NO ₂ ;

and R ¹¹ and R ¹² , independently of one another, represent a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec- butyl, isobutyl, tert-butyl and n-pentyl;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its

stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a salt thereof, or a corresponding solvate thereof.

Also even more particularly preferred is a dimethylcyclobutyl compound of general formula I, wherein

m is 1 ; n is 0 or 1 ;

X represents a -OR ⁵ moiety or a -NR ⁶ R ⁷ moiety;

Y represents a -OR ⁸ moiety; a -NR ⁹ R ¹⁰ moiety or a -C(=O)-OR ¹¹ moiety;

R ¹ represents a hydrogen atom or a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl;

R ² represents a hydrogen atom; a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or a phenyl radical which may be unsubstituted or substituted with

1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, n- pentyl, -O-CH ₃ , -0-C ₂ H ₅ , F, CI, Br, I, -CN, -CF ₃ , -OCF ₃ and -SCF ₃ ;

R ³ and R ⁴ both represent a hydrogen atom;

R ⁵ and R ⁸ , independently of one another, each represent a hydrogen atom; a phenyl radical, which may be bonded via a -(CH ₂ )i, 2 or 3-group and which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl,

isopropyl, n-butyl, tert-butyl, -0-CH ₃ , -0-C ₂ H ₅ , F, CI, Br, I, -CN, -CF ₃ and - OCF ₃ Or a -C(=O)-R ¹² moiety;

R ⁶ , R ⁷ , R ⁹ and R ¹⁰ , independently of one another, each represent a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n- butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or a phenyl radical, which is bonded via a -(CH ₂ )i, 2or3-group and which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n- butyl, tert-butyl, sec-butyl, isobutyl, -O-CH ₃ , -0-C ₂ H ₅ , F, CI, Br, I, -CN, -CF ₃ , -

OCF ₃ and -SCF ₃ ;

or R ⁶ and R ⁷ together with the bridging nitrogen atom form a moiety selected from the group consisting of

or R ⁹ and R ¹⁰ together with the bridging nitrogen atom form a moiety selected from the group consisting of

and R ¹¹ and R ¹² , independently of one another, represent a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec- butyl, isobutyl, tert-butyl and n-pentyl;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a salt thereof, or a corresponding solvate thereof.

Also preferred is a dimethylcyclobutyl compound of general formula Ie,

Ie, wherein

ne is O or i ;

R ^6e and R ^7e , independently of one another, each represent a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec- butyl, isobutyl, tert-butyl and n-pentyl; or an aryl or heteroaryl radical selected from the group consisting of phenyl and naphthyl, which may be bonded via a -(CH ₂ )i, 2or3-group and which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, isobutyl, -O-CH ₃ , -0-C ₂ H ₅ , -S-CH ₃ , -S-C ₂ H ₅ , F, CI, Br, I, -CN, -CF ₃ , -OCF ₃ , - SCF ₃ , -OH, -SH, -NH ₂ -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ and -S(=O) ₂ - CH ₃ ;

or R ^6e and R ^7e together with the bridging nitrogen atom form a moiety selected from the group consisting of

which may be unsubstituted or optionally substituted in any position including the -NH-groups with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=O), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, -O-CH ₃ , -0-C ₂ H ₅ , -S-CH ₃ , -S-C ₂ H ₅ , -C(=O)-OH, -C(=O)- O-CH ₃ , -C(=O)-O-C ₂ H ₅ , -C(=O)-O-CH ₂ -CH ₂ -CH ₃ , -C(=O)-O-CH(CH ₃ ) ₂ , - C(=O)-O-C(CH ₃ ) ₃ , -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=O)- CH(CH ₃ ) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, - NH ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH-CH ₃ , -C(=O)-NH- C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ , -S(=O) ₂ -CH ₃ , phenyl, phenethyl and benzyl, whereby said cyclic substituents may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , - OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ and -NO ₂ ;

R ₅ 8e represents a hydrogen atom; a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and

n-pentyl; an aryl radical selected from the group consisting of phenyl and naphthyl, which may be bonded via a -(CH ₂ )i, 2 or3-group and which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, -0-CH ₃ , -0-C ₂ H ₅ -F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , SCF ₃ , -OH, -SH, -NH ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ and -S(=O) ₂ -CH ₃ or a - C(=O)-R ^12e moiety;

and R ^12e represents a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a salt thereof, or a corresponding solvate thereof.

Preferred is a substituted dimethylcyclobutyl compound of general formula Ie, wherein the stereoisomers have the general formulae If or Ig or Ih or Ij,

If, ig,

Ih, U,

wherein ne, R ^6e , R ^7e and R ^8e have the above defined meanings.

Also preferred is a dimethylcyclobutyl compound of general formula Ik,

wherein

nk is O or i ;

R ^6k , R ^7k , R ^9k and R ^1Ok , independently of one another, each represent a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-

butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or an aryl or heteroaryl radical selected from the group consisting of phenyl and naphthyl, which may be bonded via a -(CH ₂ )i, ₂ o _r 3-group and which may be unsubstituted or optionally substituted with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n- butyl, tert-butyl, sec-butyl, isobutyl, -0-CH ₃ , -0-C ₂ H ₅ , -S-CH ₃ , -S-C ₂ H ₅ , F, CI, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , - C(=0)-NH ₂ and -Sl=O) ₂ -CH ₃ ;

or R ^6k and R ^7k together with the bridging nitrogen atom form a moiety selected from the group consisting of

which may be unsubstituted or optionally substituted in any position including the -NH-groups with 1 , 2, 3, 4 or 5 substιtuent(s) independently selected from the group consisting of oxo (=0), methyl, ethyl, n-propyl, isopropyl, n-butyl, tert-butyl, sec-butyl, -Q-CH ₃ , -0-C ₂ H ₅ , -S-CH ₃ , -S-C ₂ H ₅ , -C(=O)-OH, -C(=O)-

0-CH ₃ , -C(=O)-O-C ₂ H ₅ , -CC=O)-O-CH ₂ -CH ₂ -CH ₃ , -C(=O)-O-CH(CH ₃ ) ₂ , - C(=O)-O-C(CH ₃ ) _3> -C(=O)-CH ₃ , -C(=O)-C ₂ H _5> -CC=O)-CH ₂ -CH ₂ -CH ₃ , -C(=0)- CH(CHs) ₂ , -CC=O)-C(CHs) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, - NH ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=0)-NH ₂ , -C(=0)-NH-CH ₃ , -C(=0)-NH- C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ , -SC=O) ₂ -CH ₃ , phenyl, phenethyl and benzyl, whereby said cyclic substituents may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , - OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ and -NO ₂ ;

or R ^9k and R ^1Ok together with the bridging nitrogen atom form a moiety selected from the group consisting of

which may be unsubstituted or optionally substituted in any position including the -NH-groups with 1 , 2, 3, 4 or 5 substituent(s) independently selected from the group consisting of oxo (=0), methyl, ethyl, n-propyl, isopropyl, n-butyl,

tert-butyl, sec-butyl, -0-CH ₃ , -0-C ₂ H ₅ , -S-CH ₃ , -S-C ₂ H ₅ , -C(=O)-OH, -C(=O)- 0-CH ₃ , -C(=O)-O-C ₂ H ₅ , -C(=O)-O-CH ₂ -CH ₂ -CH ₃ , -C(=O)-O-CH(CH ₃ ) ₂ , - C(=O)-O-C(CH ₃ ) ₃ , -C(=O)-CH ₃ , -C(=O)-C ₂ H ₅ , -C(=O)-CH ₂ -CH ₂ -CH ₃ , -C(=O)- CH(CH ₃ ) ₂ , -C(=O)-C(CH ₃ ) ₃ , F, Cl, Br, I, -CN, -CF ₃ , -OCF ₃ , -SCF ₃ , -OH, -SH, - NH ₂ , -NO ₂ , -CHO, -CF ₂ H, -CFH ₂ , -C(=O)-NH ₂ , -C(=O)-NH-CH ₃ , -C(=O)-NH- C ₂ H ₅ , -C(=O)-N(CH ₃ ) ₂ , -C(=O)-N(C ₂ H ₅ ) ₂ , -S(=O) ₂ -CH ₃ , phenyl, phenethyl and benzyl, whereby said cyclic substituents may be unsubstituted or substituted by 1 , 2 or 3 substituent(s) independently selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, methoxy, ethoxy, F, Cl, Br, -CN, -CF ₃ , - OCF ₃ , -SCF ₃ , -OH, -SH, -NH ₂ and -NO ₂ ;

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a salt thereof, or a corresponding solvate thereof.

Preferred is a substituted dimethylcyclobutyl compound of general formula Ik, wherein the stereoisomers have the general formulae Im or In or Io or Ip,

Im, In ₁

lo, Ip-

wherein nk, R ^6k , R ^7k , R ^9k and R ^1Ok have the above defined meanings.

Most particularly preferred is a dimethylcyclobutyl compound selected from the group consisting of

[1 ] 4-(((1 S,3S)-3-(2-(benzyloxy)ethyl)-2,2-dimethylcyclobutyl)methyl)- morpholine

[2] 1 -(((1 S,3S)-3-(2-(benzyloxy)ethyl)-2,2-dimethylcyclobutyl)methyl)- piperidine

[3] 1 -(((1 S,3S)-3-(2-(benzyloxy)ethyl)-2,2-dimethylcyclobutyl)methyl)- 4- phenylpiperidine [4] 1 -(((1 S,3S)-3-(2-(benzyloxy)ethyl)-2,2-dimethylcyclobutyl)methyl)- 4- phenylpiperazine [5] 1 -(((1 S,3S)-3-(2-(benzyloxy)ethyl)-2,2-dimethylcyclobutyl)methyl)- 4- methylpiperazine

[6] 4-(((1 R,3S)-3-(benzyloxymethyl)-2,2-dimethylcyclobutyl)methyl)- morpholine

[7] 1 -(((1 R.SSJ-S-φenzyloxymethyl^^-dimethylcyclobutyOmethyl)- piperidine

[8] 1 -(((1 R.SSJ-S-φenzyloxymethyl^^-dimethylcyclobutyOmethylH- phenylpiperidine [9] 1 -(((1 R.SSJ-S-φenzyloxymethyl^^-dimethylcyclobutyOmethylH- phenylpiperazine [10] 1 -(((1 R.SSJ-S-φenzyloxymethyO^-dimethylcyclobutyOmethylH- methylpiperazine

[11] 1 -((1 R,3R)-2,2-dimethyl-3-(2-morpholinoethyl)cyclobutyl)ethanol [12] 1 -((1 R,3R)-2,2-dimethyl-3-(2-(piperidin-1 -yl)ethyl)cyclobutyl)ethanol [13] 1 -((1 R,3R)-2,2-dimethyl-3-(2-morpholinoethyl)cyclobutyl)-1- phenylethanol

[14] 1 -((1 R,3R)-2,2-dimethyl-3-(2-(piperidin-1 -yl)ethyl)cyclobutyl)-1 - phenylethanol

[15] 4-(((1 R,3R)-2,2-dimethyl-3-(2-phenoxyethyl)cyclobutyl)methyl)- morpholine [16] 1 -(((1 R,3R)-2,2-dimethyl-3-(2- phenoxyethyl)cyclobutyl)methyl)piperidine

[17] 2-((1 R,3R)-2,2-dimethyl-3-(piperidin-1 -ylmethyl)cyclobutyl)ethanol

[18] 2-((1 S,3S)-2,2-dimethyl-3-(piperidin-1 -ylmethyl)cyclobutyl)ethanol

[19] 2-((1 R.SR^^-dimethyl-S-CmorpholinomethyOcyclobutyOethanol [20] 2-((1 S.SS^^-dimethyl-S-CmorpholinomethyOcyclobutyOethanol

[21 ] 2-((1 R,3R)-2,2-dimethyl-3-((4-methylpiperidin-1 -yl)methyl)cyclobutyl)- ethanol

[22] 2-((1 R,3R)-2,2-dimethyl-3-((4-phenylpiperidin-1 -yl)methyl)cyclobutyl)- ethanol [23] 2-((1 R,3R)-3-(((2S,6R)-2,6-dimethylmorpholino)methyl)-2,2- dimethylcyclobutyl)ethanol

[24] 2-((1 R,3R)-3-(N-benzyl-N-methylamino)methyl)-2,2- dimethylcyclobutyl)-ethanol

[25] ((1 R,3R)-3-(2-(4-benzylpiperidin-1 -yl)ethyl)-2,2-dimethylcyclobutyl)- methanol

[26] methyl 2-((1 R,3R)-2,2-dimethyl-3-(piperidin-1 -ylmethyl)cyclobutyl)- acetate

[27] 1 -(((1 R,3R)-3-(2-(benzyloxy)ethyl)-2,2-dimethylcyclobutyl)methyl)- piperidine [28] 1 -(((1 R _J 3R)-3-(2-(benzyloxy)ethyl)-2 _> 2-dimethylcyclobutyl)methyl)-4- methylpiperidine

[29] 1 -(((1 R,3R)-3-(2-(benzyloxy)ethyl)-2,2-dimethylcyclobutyl)methyl)- 4- phenylpiperidine

[30] 4-(((1 R,3R)-3-(2-(benzyloxy)ethyl)-2,2-dimethylcyclobutyl)methyl)- thiomorpholine

[31 ] 4-(((1 R _> 3R)-3-(2-(benzyloxy)ethyl)-2 _> 2-dimethylcyclobutyl)methyl)- morpholine

[32] (2S,6R)-4-(((1 R _J 3R)-3-(2-(benzyloxy)ethyl)-2 _J 2-dimethylcyclobutyl)- methyl)-2,6-dinnethylnnorpholine [33] 1 -(((1 R _J 3R)-3-(2-(benzyloxy)ethyl)-2 _> 2-dimethylcyclobutyl)methyl)- pyrrolidine [34] 1 -(((1 R,3R)-3-(2-(benzyloxy)ethyl)-2,2-dimethylcyclobutyl)methyl)- 4- methylpiperazine

[35] 1 -(((1 R,3R)-3-(2-(benzyloxy)ethyl)-2,2-dimethylcyclobutyl)methyl)- 4- methylpiperazine oxalate

[36] 1 -(((1 R,3R)-3-(2-(benzyloxy)ethyl)-2,2-dimethylcyclobutyl)methyl)- 4- phenylpiperazine [37] 1 -(((1 R,3R)-3-(2-(benzyloxy)ethyl)-2,2-dimethylcyclobutyl)methyl)- 4- phenylpiperazine oxalate [38] 1 -(2-((1 R^RJ-S-Cbenzyloxymethyl^^-dimethylcyclobutyOethyl)- piperidine

[39] 4-(2-((1 R,3R)-3-(benzyloxymethyl)-2,2-dimethylcyclobutyl)ethyl)- morpholine

[40] 4-(((1 R,3R)-2,2-dimethyl-3-(2-(3-phenylpiperidin-1 -y I )ethy I )cyclobuty I )- methyl)-nnorpholine

[41 ] 4-(((1 R,3R)-2,2-dimethyl-3-(2-(4-phenylpiperidin-1 -y I )ethy I )cyclobuty I )- methyl)nnorpholine [42] 4-(((1 R,3R)-3-(2-(4-benzylpiperidin-1 -yl)ethyl)-2,2-dimethylcyclobutyl)- methyl)nnorpholine [43] 4-(((1 R,3R)-3-(2-(1 H-imidazol-1 -yl)ethyl)-2,2-dimethylcyclobutyl)- methyl)nnorpholine [44] 4-(((i R,3R)-3-(2-(1 H-pyrazol-1 -yl)ethyl)-2,2-dimethylcyclobutyl)- methyl)nnorpholine

[45] 4-(((1 R,3R)-3-(2-(1 H-1 ,2,4-triazol-i -yl)ethyl)-2,2-dimethylcyclobutyl)- methyl)nnorpholine

[46] 1 -(2-((1 R.SR^^-dimethyl-S-CmorpholinomethyOcyclobutyOethyO-ej- dihydro-1 H-indol-4(5H)-one [47] 2-(2-((1 R,3R)-2,2-dimethyl-3-(morpholinomethyl)cyclobutyl)ethyl)-

1 ,2,3,4-tetrahydroisoquinoline [48] 1 -(((1 R,3R)-3-(2-(1 H-imidazol-1 -yl)ethyl)-2,2-dimethylcyclobutyl)- methyl)piperidine [49] 1 -(((1 R,3R)-3-(2-(1 H-pyrazol-1 -yl)ethyl)-2,2-dimethylcyclobutyl)- methyl)piperidine

[50] 1 -(((1 R,3R)-3-(2-(1 H-1 ,2,4-triazol-1 -yl)ethyl)-2,2-dimethylcyclobutyl)- methyl)piperidine

[51 ] 1 -(2-((1 R,3R)-2,2-dimethyl-3-(piperidin-1 -ylmethyl)cyclobutyl)ethyl)-4- phenylpiperidine [52] 4-benzyl-1 -(2-((1 R,3R)-2,2-dimethyl-3-(piperidin-1 - ylmethyl)cyclobutyl)-ethyl)piperidine [53] 1 -(2-((1 R,3R)-2,2-dimethyl-3-(piperidin-1 -ylmethyl)cyclobutyl)ethyl)-

6,7-dihydro-1 H-indol-4(5H)-one and [54] 2-(2-((1 R,3R)-2,2-dimethyl-3-(piperidin-1 -ylmethyl)cyclobutyl)ethyl)-

1 ,2,3,4-tetrahydroisoquinoline;

[55] 2-((1 R3R)-2,2-Dimethyl-3-((piperidin-1 -yl)methyl)cyclobutyl)ethyl pivalate

[56] 2-((1 R3R)-2,2-Dimethyl-3-((piperidin-1 -yl)methyl)cyclobutyl)ethyl acetate

optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two of its stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a salt thereof, or a corresponding solvate thereof.

In still another aspect the present invention relates to a process for the preparation of a substituted dimethylcyclobutyl compound of general formula

I, wherein at least one compound of general formula II,

wherein m, R ¹ and R ² have the meaning given above and R represents a linear or branched Ci _-5 -alkyl radical, is reacted with methane sulfonylchloride, p-toluene sulfonylchloride, trifluormethane sulfonylchloride, thionyl chloride or tetrabromethane, preferably in a reaction medium selected from the group consisting of diethylether, tetrahydrofuran, tert-butylmethylether and dichloromethane or a mixture thereof, more preferably in dichloromethane, preferably in the presence of at least one base selected from the group consisting of pyridine, triethylamine, diisopropylamine, diisopropylethylamine, 4-methylmorpholine and morpholine, to yield at least one compound of general formula III,

wherein m, R ¹ and R ² have the meaning given above, R represents a linear or branched Ci _-5 -alkyl radical and LG represents -O-S(=O)2-CH ₃ , -O-S(=O)2- p-toluyl, -O-S(=O)2-CF ₃ , Cl or Br, which is optionally purified and/or isolated,

and at least one compound of general formula III is reacted with at least one compound of general formula HNR ⁶ R ⁷ , wherein R ⁶ and R ⁷ have the meaning given above, preferably in a reaction medium selected from the group consisting of dimethylformamide, acetonitrile, dichloromethane and tetrahydrofuran or a mixture thereof, more preferably in tetrahydrofuran, preferably in the presence of at least one base selected from the group consisting of pyridine, thethylamine, diisopropylamine, diisopropylethylamine, 4-methylmorpholine and morpholine, to yield at least one compound of general formula IV,

IV,

wherein m, R ¹ , R ² , R ⁶ and R ⁷ have the meaning given above and R represents a linear or branched Ci _-5 -alkyl radical, which is optionally purified and/or isolated,

and at least one compound of general formula IV is reacted with at least one reducing agent selected from the group consisting of lithium borohydride, sodium borohydride, lithium aluminium hydride and diborane, preferably with lithium borohydride, preferably in a reaction medium selected from the group consisting of methanol, ethanol, hexane and tetrahydrofuran or a mixture thereof, more preferably in methanol and/or tetrahydrofuran, to yield at least one compound of general formula V,

V,

wherein m, R ¹ , R ² , R ⁶ and R ⁷ have the meaning given above, which is optionally purified and/or isolated,

and at least one compound of general formula V is reacted with methane sulfonylchlohde, p-toluene sulfonylchloride, trifluormethane sulfonylchlohde, thionyl chloride or tetrabromethane, preferably in a reaction medium preferably selected from the group consisting of tetrahydrofurane, diethylether, tert-butylmethylether and dichloromethane or a mixture thereof, more preferably in dichloromethane, preferably in the presence of at least one base selected from the group consisting of pyridine, triethylamine, diisopropylamine, diisopropylethylamine, 4-methylmorpholine and morpholine, to yield at least one compound of general formula Vl,

Vl,

wherein m, R ¹ , R ² , R ⁶ and R ⁷ have the meaning given above and LG represents -O-S(=O) ₂ -CH ₃ , -O-S(=O) ₂ -p-toluyl, -O-S(=O) ₂ -CF ₃ , Cl or Br, which is optionally purified and/or isolated,

and at least one compound of general formula Vl is reacted with at least one compound of general formula HNR ⁹ R ¹⁰ , wherein R ⁹ and R ¹⁰ have the meaning given above, preferably in a reaction medium selected from the group consisting of dimethylformamide, acetonitrile, dichloromethane and tetrahydrofuran or a mixture thereof, preferably in the presence of at least one base selected from the group consisting of pyridine, triethylamine, diisopropylamine, diisopropylethylamine, 4-methylmorpholine and morpholine, to yield at least one compound of general formula VII,

VII,

wherein m, R ¹ , R ² , R ⁶ , R ⁷ , R ⁹ and R ¹⁰ have the meaning given above, which is optionally purified and/or isolated,

or at least one compound of general formula Vl is reacted with at least one compound of general formula M-OR ⁸ , wherein R ⁸ has the meaning given above and M represents a monovalent kation selected from the group consisting of sodium, magnesium, potassium and lithium, preferably M represents a lithium kation, preferably in a reaction medium selected from the group consisting of dimethylformamide, dichloromethane and tetrahydrofuran or a mixture thereof, more preferably in tetrahydrofuran, preferably in the presence of at least one base selected from the group consisting of pyridine, triethylamine, diisopropylamine, diisopropylethylamine, 4-methylmorpholine and morpholine, to yield at least one compound of general formula VIII,

VIII,

wherein m, R ¹ , R ² , R ⁶ , R ⁷ and R ⁸ have the meaning given above, which is optionally purified and/or isolated;

and optionally at least one compound of general formula VIII, wherein R ⁸ represents hydrogen, is reacted with at least one compound of general formula LG-C(=O)-R ¹² , wherein R ¹² has the above defined meaning and LG represents a leaving group, preferably a leaving group selected from the group consisting of chlorine and bromine, preferably in a reaction medium, preferably in the presence of at least one base selected from the group consisting of pyridine, thethylamine, diisopropylamine, diisopropylethylamine, 4-methylmorpholine and morpholine, or with at least one compound of general formula HO-C(=O)-R ¹² , wherein R ¹² has the above defined meaning, preferably in a reaction medium, preferably in the presence of at least one base selected from the group consisting of pyridine, triethylamine, diisopropylamine, diisopropylethylamine, 4- methylmorpholine and morpholine, preferably in the presence of at least one coupling agent,

to yield at least one compound of general formula Villa,

Villa,

wherein m, R ¹ , R ² , R ⁶ , R ⁷ and R ¹² have the meaning given above, which is optionally purified and/or isolated.

In still another aspect the present invention relates to a process for the preparation of a substituted dimethylcyclobutyl compound of general formula I, wherein at least one compound of general formula II,

wherein m, R ¹ and R ² have the meaning given above and R represents a linear or branched Ci _-5 -alkyl radical, is reacted with at least one compound of general formula R ⁵ -LG, wherein R ⁵ has the meaning given above and LG represents a leaving group, preferably LG represents a leaving group selected from the group consisting of chlorine, bromine, -O-S(=O) ₂ -CH ₃ , -O- S(=O) ₂ -CF ₃ and -O-S(=O) ₂ -p-toluyl, more preferably LG represents bromine, preferably in a reaction medium selected from the group consisting of tetrahydrofuran, diethylether, tert-butylmethylether and dichloromethane or a mixture thereof, more preferably in dichloromethane, preferably in the presence of at least one base, more preferably in the presence of at least one base selected from the group consisting of sodium hydride, butyllithium, sodium ethoxide, potassium tert-butoxide and potassium hydride, to yield at least one compound of general formula IX,

IX,

wherein m, R ¹ , R ² and R ⁵ have the meaning given above and R represents a linear or branched Ci _-5 -alkyl radical, which is optionally purified and/or isolated,

and at least one compound of general formula IX is reacted with at least one reducing agent selected from the group consisting of lithium borohydhde, lithium aluminium hydride and diborane, sodium borohydride, preferably with lithium borohydride, preferably in a reaction medium selected from the group consisting of methanol, ethanol, hexane and tetrahydrofuran or a mixture thereof, more preferably in methanol and/or tetrahydrofuran,, to yield at least one compound of general formula X,

X,

wherein m, R , R and R have the meaning given above, which is optionally purified and/or isolated,

and optionally at least one compound of general formula X, is reacted with at least one compound of general formula LG-C(=O)-R ¹² , wherein R ¹² has the meaning given above and LG represents a leaving group, preferably a

leaving group selected from the group consisting of chlorine and bromine, preferably in a reaction medium, preferably in the presence of at least one base selected from the group consisting of pyridine, triethylamine, diisopropylamine, diisopropylethylamine, 4-methylmorpholine and morpholine, or with at least one compound of general formula HO-C(=O)-R ¹² , wherein R ¹² has the meaning given above, preferably in a reaction medium, preferably in the presence of at least one base, preferably in the presence of at least one coupling agent, to yield at least one compound of general formula Xa,

Xa,

wherein m, R ¹ , R ² and R ⁵ have the meaning given above, which is optionally purified and/or isolated,

and at least one compound of general formula X is reacted with methane sulfonylchloride, p-toluene sulfonylchloride, trifluormethane sulfonylchlohde, thionyl chloride or tetrabromethane, preferably in a reaction medium selected from the group consisting of diethylether, tetrahydrofuran, tert- butylmethylether and dichloromethane or a mixture thereof, more preferably in dichloromethane, preferably in the presence of at least one base selected from the group consisting of pyridine, triethylamine, diisopropylamine, diisopropylethylamine, 4-methylmorpholine and morpholine, to yield at least one compound of general formula Xl,

Xl,

wherein m, R ¹ , R ² and R ⁵ have the meaning given above and LG represents -O-S(=O) ₂ -CH _3> -O-S(=O) ₂ -p-toluyl, -O-S(=O) ₂ -CF ₃ , Cl or Br, which is optionally purified and/or isolated,

and at least one compound of general formula Xl is reacted with at least one compound of general formula HNR ⁹ R ¹⁰ , wherein R ⁹ and R ¹⁰ have the meaning given above, preferably in a reaction medium selected from the group consisting of dimethylformamide, acetonitrile, dichloromethane and tetrahydrofuran or a mixture thereof, preferably in the presence of at least one base selected from the group consisting of pyridine, triethylamine, diisopropylamine, diisopropylethylamine, 4-methylmorpholine and morpholine, to yield at least one compound of general formula XII,

XII,

wherein m, R , R , R , R and R ,10 have the meaning given above, which is optionally purified and/or isolated.

In still another aspect the present invention relates to a process for the preparation of a substituted dimethylcyclobutyl compound of general formula I, wherein at least one compound of general formula XIII,

wherein R ¹ , R ³ and R ⁴ have the meaning given above, is reacted with methane sulfonylchloride, p-toluene sulfonylchloride, trifluormethane sulfonylchloride, thionyl chloride or tetrabromethane, preferably in a reaction medium selected from the group consisting of diethylether, tetrahydrofuran, tert-butylmethylether and dichloromethane or a mixture thereof, more preferably in dichloromethane, preferably in the presence of at least one base selected from the group consisting of pyridine, thethylamine, diisopropylamine, diisopropylethylamine, 4-methylmorpholine and morpholine,to yield at least one compound of general formula XIV,

XIV,

wherein R ¹ , R ³ and R ⁴ have have the meaning given above and LG represents -O-S(=O) ₂ -CH ₃ , -O-S(=O) ₂ -p-toluyl, -O-S(=O) ₂ -CF ₃ , Cl or Br, which is optionally purified and/or isolated,

and at least one compound of general formula XIV is reacted with at least one compound of general formula HNR ⁹ R ¹⁰ , wherein R ⁹ and R ¹⁰ have the

meaning given above, preferably in a reaction medium selected from the group consisting of dimethylformamide, acetonitrile, dichloromethane and tetrahydrofuran or a mixture thereof, preferably in the presence of at least one base selected from the group consisting of pyridine, triethylamine, diisopropylamine, diisopropylethylamine, 4-methylmorpholine and morpholine, to yield at least one compound of general formula XV,

XV,

wherein R ¹ , R ³ , R ⁴ , R ⁹ and R ¹⁰ have the meaning given above, which is optionally purified and/or isolated,

and at least one compound of general formula XV is reacted with at least one reagent selected from the group consisting of hydrochloric acid, pyhdinium p- toluenesulfonate, sulfonic acid and trifluoroacetic acid, preferably with pyhdinium p-toluenesulfonate, preferably in a reaction medium selected from the group consisting of acetone and water or a mixture thereof, to yield at least one compound of general formula XVI,

XVI,

wherein R ¹ , R ³ , R ⁴ , R ⁹ and R ¹⁰ have the meaning given above, which is optionally purified and/or isolated,

and at least one compound of general formula XVI is reacted with at least one compound of general formula R ² -Li, wherein R ² has the meaning given above, or R ² -Mg-Z, wherein R ² has the meaning given above, and Z represents an anion selected from the group consisting of bromide and chloride, preferably in a reaction medium, selected from the group consisting of ether and tetrahydrofurane, to yield at least one compound of general formula XVII,

XVII,

wherein R ¹ , R ² , R ³ , R ⁴ , R ⁹ and R ¹⁰ have the meaning given above, which is optionally purified and/or isolated,

and optionally at least one compound of general formula XVII is reacted with at least one compound of general formula R ⁵ -LG, wherein R ⁵ has the meaning given above and LG represents a leaving group, preferably LG represents a leaving group selected from the group consisting of chlorine, bromine, -O-S(=O) ₂ -CH ₃ , -O-S(=O) ₂ -CF ₃ and -O-S(=O) ₂ -p-toluyl, more preferably LG represents bromine, preferably in a reaction medium selected from the group consisting of tetrahydrofuran, diethylether, tert- butylmethylether and dichloromethane or a mixture thereof, more preferably in dichloromethane, preferably in the presence of at least one base, more preferably in the presence of at least one base selected from the group consisting of sodium hydride, butyllithium, sodium ethoxide, potassium tert- butoxide and potassium hydride, to yield at least one compound of general formula XVIII,

XVIII,

wherein R ¹ , R ² , R ³ , R ⁴ , R ⁵ , R ⁹ and R ¹⁰ have the meaning given above, which is optionally purified and/or isolated.

The compounds of general formulae I, Ia, Ib, Ic, Id, Ie, If, Ig, Ih, Ij, Ik, Im, In, Io and Ip given above may be purified and/or isolated according to methods well known to those skilled in the art. Preferably, the compounds of general formulae I, Ia, Ib, Ic, Id, Ie, If, Ig, Ih, Ij, Ik, Im, In, Io and Ip may be isolated by evaporating the reaction medium, addition of water and adjusting the pH value to obtain the compound in form of a solid that can be isolated by filtration, or by extraction with a solvent that is not miscible with water such as chloroform and purification by chromatography or recrystallisation from a suitable solvent.

The compounds of general formulae HNR ⁶ R ⁷ , HNR ⁹ R ¹⁰ , MOR ⁸ , R ⁵ -LG, R ² -Li and R ² -Mg-Z are commercially available or may also be prepared according to standard methods known in the prior art.

During some synthetic reactions described above or while preparing the compounds of general formulae I, Ia, Ib, Ic, Id, Ie, If, Ig, Ih, Ij, Ik, Im, In, Io and Ip the protection of sensitive or reactive groups may be necessary and/or desirable. This can be performed by using conventional protective groups like those described in Protective groups in Organic Chemistry, ed. J. F. W. McOmie, Plenum Press, 1973; T.W. Greene & P. G. M. Wuts and Protective Groups in Organic Chemistry, John Wiley & sons, 1993, 3 ^rd edition. The

respective parts of the description is hereby incorporated by reference and forms part of the disclosure. The protective groups may be eliminated when convenient by means well-known to those skilled in the art.

If the substituted dimethylcyclobutyl compounds of general formulae I, Ia, Ib,

Ic, Id, Ie, If, Ig, Ih, Ij, Ik, Im, In, Io and Ip are obtained in form of a mixture of stereoisomers, particularly enantiomers or diastereomers, said mixtures may be separated by standard procedures known to those skilled in the art, e.g. chromatographic methods or crystallization with chiral reagents.

The substituted dimethylcyclobutyl compounds of general formulae I, Ia, Ib, Ic, Id, Ie, If, Ig, Ih, Ij, Ik, Im, In, Io and Ip and in each case stereoisomers thereof may be obtained in form of a corresponding salt according to methods well known to those skilled in the art, e.g. by reacting said compound with at least one inorganic and/or organic acid, preferably in a suitable reaction medium. Suitable reaction media include, for example, any of the ones given above. Suitable inorganic acids include but are not limited to hydrochloric acid, hydrobromic acid, phosphoric acid, oxalic acid, sulfuric acid, nitric acid, suitable organic acids include but are not limited to citric acid, maleic acid, fumaric acid, tartaric acid, or derivatives thereof, p- toluenesulfonic acid, methanesulfonic acid or camphersulfonic acid.

The term "salt" is to be understood as meaning any form of the substituted dimethylcyclobutyl compounds in which they assume an ionic form or are charged and are coupled with a counter-ion (a cation or anion) or are in solution. By this are also to be understood complexes of the active compound with other molecules and ions, in particular complexes which are complexed via ionic interactions.

The term "physiologically acceptable salt" is understood in particular, in the context of this invention, as salt (as defined above) formed either with a

physiologically tolerated acid, that is to say salts of the particular active compound with inorganic or organic acids which are physiologically tolerated - especially if used on humans and/or mammals - or with at least one, preferably inorganic, cation which are physiologically tolerated - especially if used on humans and/or mammals. Examples of physiologically tolerated salts of particular acids are salts of: hydrochloric acid, hydrobromic acid, sulfuric acid, hydrobromide, monohydrobromide, monohydrochlohde or hydrochloride, methiodide, methanesulfonic acid, formic acid, acetic acid, oxalic acid, succinic acid, malic acid, tartaric acid, mandelic acid, fumaric acid, lactic acid, citric acid, glutamic acid, hippuric acid picric acid and/or aspartic acid. Examples of physiologically tolerated salts of particular bases are salts of alkali metals and alkaline earth metals and with NH ₄ .

Solvates, preferably hydrates, of the substituted dimethylcyclobutyl compounds of general formulae I, Ia, Ib, Ic, Id, Ie, If, Ig, Ih, Ij, Ik, Im, In, Io and

Ip and in each case of corresponding stereoisomers may also be obtained by standard procedures known to those skilled in the art.

The term "solvate" according to this invention is to be understood as meaning any form of the substituted dimethylcyclobutyl compounds in which they have attached to it via non-covalent binding another molecule (most likely a polar solvent) especially including hydrates and alcoholates, e.g. ethanolate.

A further aspect of the present invention relates to a medicament comprising at least one substituted dimethylcyclobutyl compound of general formulae I,

Ia, Ib, Ic, Id, Ie, If, Ig, Ih, Ij, Ik, Im, In, Io and Ip given above, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, and optionally at least one physiologically acceptable auxiliary agent.

Said medicament is particularly suitable for sigma receptor regulation, preferably for sigma-1 receptor regulation, and can therefore be used for the prophylaxis and/or treatment of a disorder or a disease that is least partially mediated via sigma receptors, preferably sigma-1 receptors.

Preferably said medicament is suitable for the prophylaxis and/or treatment of a disorder or disease related to food intake, preferably for the regulation of appetite, for the maintenance, increase or reduction of body weight, for the prophylaxis and/or treatment of obesity, bulimia, anorexia, cachexia, type Il diabetes (non insulin dependent diabetes mellitus), preferably type Il diabetes that is caused by obesity; for the prophylaxis and/or treatment of diarrhoea; lipoprotein disorders, preferably selected from the group consisting of hypercholesterolemia (type Il hyperlipoproteinemia); hypertriglyceridemia; hypoalphalipoproteinemia and high lipoprotein(a) levels; arthritis; hypertension; arrhythmia; ulcer; tardive dyskinesia; stress; cancer; stroke; ischemic stroke; migraine; epilepsy; anxiety; panic attacks; depression; cognitive disorders; cognitive dysfunction associated with psychiatric diseases; memory disorders; psychosis; schizophrenia; for the prophylaxis and/or treatment of drug addiction and/or withdrawal or for the prophylaxis and/or treatment of cocaine addiction and/or withdrawal.

Also preferably said medicament is suitable for the prophylaxis and/or treatment of pain, preferably neuropathic pain, allodynia, analgesia, causalgia, central pain, dysesthesia, hyperesthesia, hyperalgesia, hypoalgesia, hypoesthesia, or neuralgia, more preferably neuropathic pain, hyperalgesia or allodynia.

In another aspect the present invention relates to the use of at least one substituted dimethylcyclobutyl compound of general formulae I, Ia, Ib, Ic, Id, Ie, If, Ig, Ih, Ij, Ik, Im, In, Io and Ip given above, optionally in form of one of their stereoisomers, preferably enantiomers or diasteromers, a racemate or

in form of a mixture of at least two stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, for the preparation of a medicament suitable for sigma receptor regulation, preferably for sigma-1 receptor regulation and/or preferably for the prophylaxis and/or treatment of a disorder or a disease that is least partially mediated via sigma receptors, preferably sigma-1 receptors.

The use of at least one substituted dimethylcyclobutyl compound of general formulae I, Ia, Ib, Ic, Id, Ie, If, Ig, Ih, Ij, Ik, Im, In, Io and Ip given above, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, for the manufacture of a medicament for the prophylaxis and/or treatment of a disorder or disease related to food intake, preferably for the regulation of appetite, for the maintenance, increase or reduction of body weight, for the prophylaxis and/or treatment of obesity, bulimia, anorexia, cachexia, type Il diabetes (non insulin dependent diabetes mellitus), preferably type Il diabetes that is caused by obesity; for the prophylaxis and/or treatment of diarrhoea; lipoprotein disorders, preferably selected from the group consisting of hypercholesterolemia (type Il hyperlipoproteinemia); hypertriglyceridemia; hypoalphalipoproteinemia and high lipoprotein(a) levels; arthritis; hypertension; arrhythmia; ulcer; tardive dyskinesia; stress; cancer; stroke; ischemic stroke; migraine; epilepsy; anxiety; panic attacks; depression; cognitive disorders; cognitive dysfunction associated with psychiatric diseases; memory disorders; psychosis; schizophrenia; for the prophylaxis and/or treatment of drug addiction and/or withdrawal or for the prophylaxis and/or treatment of cocaine addiction and/or withdrawal is preferred.

The use of at least one substituted dimethylcyclobutyl compound of general formulae I, Ia, Ib, Ic, Id, Ie, If, Ig, Ih, Ij, Ik, Im, In, Io and Ip given above, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, for the manufacture of a medicament for the prophylaxis and/or treatment of pain, preferably neuropathic pain, allodynia, analgesia, causalgia, central pain, dysesthesia, hyperesthesia, hyperalgesia, hypoalgesia, hypoesthesia, or neuralgia, more preferably neuropathic pain, hyperalgesia or allodynia, is preferred.

The use of at least one substituted dimethylcyclobutyl compound of general formulae I, Ia, Ib, Ic, Id, Ie, If, Ig, Ih, Ij, Ik, Im, In, Io and Ip given above, optionally in form of one of its stereoisomers, preferably enantiomers or diasteromers, a racemate or in form of a mixture of at least two stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a physiologically acceptable salt thereof, or a corresponding solvate thereof, as pharmacological tool or as anxiolytic or as immunosuppressant is preferred.

Any medicament according to the present invention may be in any form suitable for the application to humans and/or animals, preferably humans including infants, children and adults. The medicament can be produced by standard procedures known to those skilled in the art, e.g. from the table of contents of

"Pharmaceutics: The Science of Dosage Forms", Second Edition, Aulton, M. E. (ED. Churchill Livingstone, Edinburgh (2002); "Encyclopedia of Pharmaceutical Technology", Second Edition, Swarbrick, J. and Boylan J. C. (Eds.), Marcel Dekker, Inc. New York (2002); "Modern Pharmaceutics", Fourth Edition, Banker G.S. and Rhodes CT. (Eds.) Marcel Dekker, Inc. New York 2002 y "The Theory and Practice of Industrial Pharmacy", Lachman L., Lieberman H. And Kanig J.

(Eds.), Lea & Febiger, Philadelphia (1986). The respective descriptions are hereby incorporated by reference and form part of the disclosure. The composition of the medicament may vary depending on the route of administration.

The medicament of the present invention may, for example, be administered parentally in combination with conventional injectable liquid carriers, such as water or suitable alcohols. Conventional pharmaceutical excipients for injection, such as stabilizing agents, solubilizing agents, and buffers, may be included in such injectable compositions. These medicaments may for example be injected intramuscularly, intraperitoneally, or intravenously.

Medicaments according to the present invention may also be formulated into orally administrable compositions containing one or more physiologically compatible carriers or excipients, in solid or liquid form. These compositions may contain conventional ingredients such as binding agents, fillers, lubricants, and acceptable wetting agents. The compositions may take any convenient form, such as tablets, pellets, granules, capsules, lozenges, aqueous or oily solutions, suspensions, emulsions, or dry powdered forms suitable for reconstitution with water or other suitable liquid medium before use, for immediate or retarded release. The multiparticulate forms, such as pellets or granules, may e.g. be filled into a capsule, compressed into tablets or suspended in a suitable liquid.

Suitable controlled release formulations, materials and methods for their preparation are known from the prior art, e.g. from the table of contents of "Modified-Release Drug Delivery Technology", Rathbone, M.J. Hadgraft, J. and Roberts, M.S. (Eds.), Marcel Dekker, Inc., New York (2002); "Handbook of Pharmaceutical Controlled Release Technology", Wise, D. L. (Ed.), Marcel Dekker, Inc. New York, (2000); "Controlled Drug Delivery", VoI, I, Basic

Concepts, Bruck, S. D. (Ed.), CRD Press Inc., Boca Raton (1983) y de Takada, K. and Yoshikawa, H., "Oral Drug Delivery", Encyclopedia of

Controlled Drug Delivery, Mathiowitz, E. (Ed.), John Wiley & Sons, Inc., New York (1999), Vol. 2, 728-742; Fix, J., "Oral drug delivery, small intestine and colon", Encyclopedia of Controlled Drug Delivery, Mathiowitz, E. (Ed.), John Wiley & Sons, Inc., New York (1999), Vol. 2, 698-728. The respective descriptions are hereby incorporated by reference and form part of the disclosure.

Medicaments according to the present invention may also comprise an enteric coating, so that their dissolution is dependent on pH-value. Due to said coating the medicament can pass the stomach undissolved and the respective dimethylcyclobutyl compound is liberated in the intestinal tract. Preferably the enteric coating is soluble at a pH value of 5 to 7.5. Suitable materials and methods for the preparation are known from the prior art.

Typically, the medicaments according to the present invention may contain 1 -

60 % by weight of one or more substituted dimethylcyclobutyl compounds as defined herein and 40-99 % by weight of one or more auxiliary substances (additives).

The liquid oral forms for administration may also contain certain additives such as sweeteners, flavoring, preservatives, and emulsifying agents. Nonaqueous liquid compositions for oral administration may also be formulated, containing edible oils. Such liquid compositions may be conveniently encapsulated in e.g., gelatin capsules in a unit dosage amount.

The compositions of the present invention may also be administered topically or via a suppository.

The daily dosage for humans and animals may vary depending on factors that have their basis in the respective species or other factors, such as age, sex, weight or degree of illness and so forth. The daily dosage for humans may preferably be in the range fromi to 2000 mg, preferably 1 to 1500 mg,

more preferably 1 to 1000, even more preferably 1 to 500 mg, most preferably 1 to 100 mg of active substance to be administered during one or several intakes per day.

In the following methods for determining the pharmacological activity of the substituted dimethylcyclobutyl compounds are described.

PHARMACOLOGICAL METHODS:

Some representative compounds of the invention were tested for their activity as sigma (sigma-1 and sigma-2) inhibitors. The following protocols were followed:

Sigma-1 receptor binding

Brain membrane preparation and binding assays for the sigma-1 receptor were performed as described (DeHaven-Hudkins et al., Characterization of the binding of [ ³ H]-(+)-pentazocine to recognition sites in guinea pig brain, Eur. J. Pharmacol. 227, 371-378) with some modifications.

In brief, guinea pig brains were homogenized in 10 vols. (w/v) of Tris-HCI 50 mM, 0.32 M sucrose, pH 7.4, with a Kinematica Polytron PT 3000 at 15000 r.p.m. for 30 s. The homogenate was centhfuged at 1000 g for 10 min at 4 ⁰ C and the supernatants collected and centrifuged again at 48000 g for 15 min at 4 ⁰ C. The pellet was resuspended in 10 volumes of Tris-HCI buffer (50 mM, pH 7.4), incubated at 37 ⁰ C for 30 min, and centrifuged at 48000 g for 20 min at 4 ⁰ C. Following this, the pellet was resuspended in fresh Tris-HCI buffer (50 mM, pH 7.4) and stored on ice until use.

Each assay tube contained 10 μL of [ ³ H]-(+)-pentazocine (final concentration of 0.5 nM), 900 μL of the tissue suspension to a final assay volume of 1 mL

and a final tissue concentration of approximately 30 mg tissue net weight/mL. Non-specific binding was defined by addition of a final concentration of 1 M haloperidol. All tubes were incubated at 37 ⁰ C for 150 min before termination of the reaction by rapid filtration over Schleicher & Schuell GF 3362 glass fibre filters [previously soaked in a solution of 0,5% polyethylenimine for at least 1 h]. Filters were then washed with four times with 4 ml_ of cold Tris-HCI buffer (50 mM, pH 7.4). Following addition of scintillation cocktail, the samples were allowed to equilibrate overnight. The amount of bound radioactivity was determined by liquid scintillation spectrometry using a Wallac Winspectral 1414 liquid scintillation counter. Protein concentrations were determined by the method of Lowry et al. (Protein measurement with the FoNn phenol reagent, J. Biol. Chem, 193, 265).

Sigma-2 receptor binding

Binding studies for sigma-2 receptor were performed as described (Radesca et al., Synthesis and Receptor Binding of Enantiomeric N-Substituted cis-N- [2-(3,4-Dichlorophenyl)ethyl]-2-(1 -pyrrolidinyl)ciclohexylamines as High- Affinity Receptor Ligands, J. Med. Chem. 34, 3065-3074) with some modifications. In brief, brains from sigma receptor type I (sigma-1 ) knockout mice (Langa, F., Codony X., Tovar V., Lavado A., Gimenez E., Cozar P., Cantero M., Dordal A., Hernandez E., Perez R., Monroy X., Zamanillo D., Guitart X., Montoliu LL, 2003, Generation and phenotypic analysis of sigma receptor type I (Sigmal ) knockout mice, European Journal of Neuroscience, Vol. 18, 2188-2196) were homogenized in a volume of 10 mL/g tissue net weight of ice-cold 10 mM Tris-HCI, pH 7.4, containing 320 mM sucrose (Tris- sucrose buffer) with a Potter-Elvehjem homogenizer (10 strokes at 500 r.p.m.) The homogenates were then centrifuged at 1000g for 10 min at 4 ⁰ C, and the supernatants were saved. The pellets were resuspended by vortexing in 2 mL/g ice-cold Tris-sucrose buffer and centrifuged again at

1000 g for 10 min. The combined 1000g supernatants were centrifuged at

31000 g for 15 min at 4 ⁰ C. The pellets were resuspended by vortexing in 3 mL/g 10 mM Tris-HCI, pH 7.4, and the suspension was kept at 25 ⁰ C for 15 min. Following centrifugation at 31000 g for 15 min, the pellets were resuspended by gentle Potter Elvehjem homogenisation to a volume of 1.53 mL/g in 1 O mM Tris-HCI pH 7.4.

The assay tubes contained 10 μL of [ ³ H]-DTG (final concentration of 3 nM), 400 μL of the tissue suspension (5.3 mL/g in 50 mM Tris-HCI, pH 8.0) to a final assay volume of 0.5 mL. Non-specific binding was defined by addition of a final concentration of 1 M halopehdol. All tubes were incubated at 25 ⁰ C for

120 min before termination of the reaction by rapid filtration over Schleicher & Schuell GF 3362 glass fibre filters [previously soaked in a solution of 0,5% polyethylenimine for at least 1 h]. Filters were washed with three times with 5 mL volumes of cold Tris-HCI buffer (10 mM, pH 8.0). Following addition of scintillation cocktail samples were allowed to equilibrate overnight. The amount of bound radioactivity was determined by liquid scintillation spectrometry using a Wallac Winspectral 1414 liquid scintillation counter. Protein concentrations were determined by the method of Lowry et al. (Protein measurement with the FoNn phenol reagent, J. Biol. Chem, 193, 265).

The present invention is illustrated below with the aid of examples. These illustrations are given solely by way of example and do not limit the general spirit of the present invention.

Examples

A compound of general formula II, wherein both R ¹ and R ² represent hydrogen and R represents tert-butyl, can be prepared starting from (-)-α- pinene as depicted in scheme 1. below.

NaOBr MeI, Cs ₂ CO ₃ dioxane

B

II; R ¹ , R ² = H; R = tert-Butyl scheme 1.

Exact reaction conditions for the each reaction step in scheme 1. are given in A. G. Moglioni et al. J. Org. Chem. 2000, 65, 3934-3940. The respective part of the literature is hereby incorporated by reference.

Preparation of Compound C1 : (1R,3R)-3-((tert-Butoxycarbonyl)methyl)-2,2- dimethylcyclobutanecarboxylic acid

C1

Aqueous NaOBr prepared from bromine (9.4 ml_, 183.2 mmol), NaOH (28.4 g, 710.9 mmol) and water (237 ml_) was added to a solution of tert-butyl 2- ((1 R,3R)-3-acetyl-2,2-dimethylcyclobutyl)acetate (5.5 g, 22.9 mmol) in 1 ,4-

dioxane (138 ml_) and water (38 ml_). The reaction mixture was cooled to -5 ⁰ C and stirred at temperature between -5 and 0 ⁰ C for 5 h. The reaction mixture was washed with dichloromethane (4 x 200 ml_). 40% aqueous NaHS2θ3 was added to the basic aqueous layer at 0 ⁰ C until pH 5-6 was reached and the solution was acidified to pH 2 with cone, aqueous HCI. The acidic solution was extracted with dichloromethane (6x200 ml_) and the organic extracts were dried over MgSO ₄ . The solvent was evaporated under reduced pressure to afford 4.9 g of (1 R,3R)-3-((te/t-butoxycarbonyl)methyl)- 2,2-dimethylcyclobutanecarboxylic acid (90% yield), which was used in the next step without further purification.

• ¹ H-NMR (250 MHz, CDCI ₃ )

1 .0 (S, 3H), 1 .3 (s, 3H), 1 .5 (s, 9H), 2.0 (m, 1 H), 2.1 (m, 1 H), 2.3 (m, 2H), 2.5 (m, 1 H), 2.8 (dd, J=10 Hz, J=10.5 Hz, 1 H).

Compound C2 (1 S,3S)-3-((te/t-Butoxycarbonyl)methyl)-2,2- dimethylcyclobutanecarboxylic acid was prepared analogous to compound C1.

Preparation of Compound D1 :

Methyl (1 R,3R)-3-((tert-butoxycarbonyl)methyl)-2,2- dimethylcyclobutane-carboxylate

C1 D1

Cs ₂ CO ₃ (7.9 g, 24.2 mmol) and MeI (1.5 ml_, 24.2 mmol) were added to an ice-cooled solution of (1 R,3R)-3-((te/t-butoxycarbonyl)methyl)-2,2- dimethylcyclobutanecarboxylic acid (4.9 g, 20.2 mmol) in DMF (150 ml_), and the reaction mixture was stirred at room temperature for 8 h. The reaction

mixture was poured into EtOAc (200 ml_) and the solution was washed with saturated aqueous NaHCO ₃ (6 x 100 ml_). The organic layer was dried over MgSO ₄ and the solvents were removed under vacuo to afford 4.1 g of methyl (1 R,3R)-3-((fe/t-butoxycarbonyl)methyl)-2,2-dimethylcyclobutan ecarboxylate (80% yield), which was used in the next step without further purification.

• ¹ H-NMR (250 MHz, CDCI ₃ )

0.9 (s, 3H), 1.2 (s, 3H), 1.5 (s, 9H), 2.0 (m, 1 H), 2.1 (m, 1 H), 2.3 (m, 2H), 2.4 (m, 1 H), 2.8 (dd, J= 10.5 Hz, J= 11 Hz, 1 H), 3.7 (s, 3H).

Compound D2 Methyl (1 S,3S)-3-((te/t-butoxycarbonyl)methyl)-2,2- dimethylcyclobutanecarboxylate was prepared analogous to compound D1.

Preparation of compounds of general formula II:

terf-Butyl 2-((1R,3/?)-3-(hydroxymethyl)-2,2-dimethylcyclobutyl)acetate

D1 II; R ¹ , R ² = H

2 M LiBH ₄ in THF (40 ml_, 80.0 mmol) and dry MeOH (4 ml_) was successively added to a solution of methyl (1 R,3R)-3-((te/t- butoxycarbonyl)methyl)-2,2-dimethylcyclobutanecarboxylic acid (4.1 g, 16.0 mmol) in anhydrous THF under nitrogen atmosphere. The mixture was allowed to stand for 15 min then heated to reflux for 12 h. Excess hydride was destroyed with MeOH and water, and the solution was extracted with CH ₂ Cb (4x150 ml_). The organic extracts were dried over MgSO ₄ and the solvents were evaporated at reduced pressure to afford tert-butyl 2-((1 R,3R)-

3-(hydroxymethyl)-2,2-dinnethylcyclobutyl)acetate (2.9 g, 79% yield), which was used in the next step without further purification.

• ¹ H-NMR (250 MHz, CDCI ₃ ) 0.9 (s, 3H), 1.2 (s, 3H), 1.5 (s, 9H), 2.1 (m, 3H), 2.2 (m, 3H), 3.6 (m, 2H).

The compound te/t-Butyl 2-((1 S,3S)-3-(hydroxymethyl)-2,2- dimethylcyclobutyl)-acetate was prepared as described above.

Preparation of compounds of general formula III:

((1 R,3R)- 3-((fe/t-Butoxycarbonyl)methyl)-2,2-dimethylcyclobutyl)methy l methanesulfonate

I; R ¹ , R ² = H I; R ¹ , R ² = H

Thethylamine (1.5 ml_, 10.4 mmol) and mesyl chloride (0.8 ml_, 9.6 mmol) were added to an ice-cooled solution of tert-butyl 2-((1 R,3R)-3- (hydroxymethyl)-2,2-dimethylcyclobutyl)acetate (1.7 g, 7.4 mmol) in anhydrous dichloromethane (70 ml_) under nitrogen atmosphere. After stirring at 0 ⁰ C for 1 h, the reaction mixture was washed with saturated aqueous NaHCO3 (4 x 50 ml_) and dried over MgSO ₄ . The solvent was removed to afford ((1 R3R)- 3-((te/t-butoxycarbonyl)methyl)-2,2- dimethylcyclobutyl)methyl methanesulfonate (1.9 g, 83% yield) that was used in the next step without further purification.

• ¹ H-NMR (250 MHz, CDCI ₃ )

1.0 (S, 3H), 1.1 (s, 3H), 1.5 (s, 9H), 2.2 (m, 6H), 3.0 (s, 3H), 4.2 (m, 2H).

The compounds ((1 S,3S)- 3-((te/t-Butoxycarbonyl)methyl)-2,2- dimethylcyclobutyl)methyl methanesulfonate and 2-((1 R,3R)-2,2-Dimethyl-3- (2-methyl-1 ,3-dioxolan-2-yl)cyclobutyl)ethyl methanesulfonate (compound of general formula (XIV) were prepared as described above.

Preparation of compounds of general formula IV:

tert-Butyl 2-((1 R,3R)- 2,2-dimethyl-3-

(morpholinomethyl)cyclobutyl)acetate

I; R ¹ , R ² = H IV; R ¹ , R ² = H

A mixture of ((1 R3R)- 3-((te/t-butoxycarbonyl)methyl)-2,2- dimethylcyclobutyl)methyl methanesulfonate (1 g, 1.5 mmol) and morpholine

(25 ml_, 287 mmol) were heated at 80 ⁰ C for 7 days under nitrogen atmosphere. Then the mixture was cooled, EtOAc (25 ml_) was added and the resultant solution was subsequently washed with saturated sodium NaHCOs and dried over MgSO ₄ . Solvent was removed to provide tert-butyl 2- ((1 R.SR^^-dimethyl-S^morpholinomethyOcyclobutyOacetate (920 mg, 95% yield).

• ¹ H-NMR (250 MHz, CDCI ₃ )

0.9 (s, 3H), 1.1 (s, 3H), 1.5 (s, 9H), 2.2 (m, 5H), 2.4 (m, 7H), 3.7 (m, 4H).

The following compounds of general formula IV were prepared as described above:

te/t-Butyl 2-((1 S,3S)- 2,2-dimethyl-3-(morpholinomethyl)cyclobutyl)acetate

te/t-Butyl 2-((1 R,3R)- 2,2-Dimethyl-3-((piperidin-1 - yl)methyl)cyclobutyl)acetate

• ¹ H-NMR (250 MHz, CDCI ₃ ) 0.9 (s, 3H), 1.1 (s, 3H), 1.4 (s, 9H), 1.6 (m, 6H), 2.1 (m, 8H), 2.3 (m, 4H).

te/t-Butyl 2-((1 S,3S)- 2,2-Dimethyl-3-((piperidin-1 - yl)methyl)cyclobutyl)acetate

Preparation of compounds of general formula V:

2-((1R,3R)-2,2-Dimethyl-3-(morpholinomethyl)cyclobutyl)et hanol

IV; R ¹ , R ² = H V; R ¹ , R ² = H

2 M LiBH ₄ in THF (10 ml_, 20.0 mmol) and dry methanol (1 ml_) was successively added to a solution of tert-butyl 2-((1 R,3R)-2,2-dimethyl-3- (morpholinomethyl)cyclobutyl)acetate (720 mg, 2.4 mmol) in anhydrous THF

(20 ml_) under nitrogen atmosphere. After 15 minutes standing, the mixture was heated to reflux for 24 h. Excess hydride was destroyed with methanol and the reaction mixture was poured into water. The resultant solution was extracted with CH ₂ CI ₂ (5x60 ml_) and the organic extracts were dried over MgSO ₄ . Solvents were removed under reduced pressure to afford 700 g of a residue that was chromatographed on Baker ^® silica gel using 1 % TEA - 1 :9

MeOH-CH ₂ CI ₂ as eluent to give pure 2-((1 R,3R)-2,2-dimethyl-3- (morpholinomethyl)cyclobutyl)ethanol (410 mg, 75% yield).