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WO/1997/047621A1 |
The invention provides a process for the preparation of compounds of formula (I) wherein R1, R2, R3 R4 and R5 are as defined in the specification; and wherein any functional groups are optionally protected; and salts thereof; which proce...
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WO/1997/047194A1 |
Compounds represented by formula (I), and pharmaceutically acceptacle salts thereof; and their method of preparation are provided. Compounds of the above formula are influenza virus neuraminidase inhibitors and can be used in treating pa...
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WO/1997/046577A1 |
There is provided compounds of formula (I), wherein R1, R2, R3, Rx, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatm...
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WO/1997/045406A1 |
The invention relates to a process for producing a compound of formula (I) wherein R1, R2 and R3 are as defined in the specification, which comprises reacting a lactone with an imine to obtain a chiral diol of formula (IV) oxidizing the ...
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WO/1997/045115A1 |
The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.
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WO/1997/043255A1 |
Compounds are provided which inhibit micromosal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure (1) or (2) wherein R1 to R6, ...
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WO/1997/042170A1 |
There is described the preparation of 4-acetoxy-3-acylaminoazetidin-2-ones through the introduction of an acetoxy group in the 4 position of a 3-(N-acyl-N-protected)aminoazetidin-2-one not subtituted in the 1 position and the removal of ...
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WO/1997/041099A1 |
Compounds of formula (I) in which inter alia X is a linker group A-B in which A is bond, CH2O, CO, CONR6, COO, CONR6CO, or CONR6O in which R6 is hydrogen or C(1-6)alkyl and B is (CH2)pCO(CH2)q in which p is an integer from 1 to 8, prefer...
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WO/1997/041098A1 |
Selected compounds of formula (I) in which: R1 is hydrogen or a corresponding pharmaceutically acceptable ester or a pharmaceutically acceptable salt thereof; R2 and R3 which may be the same or different is each selected from hydrogen or...
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WO/1997/041084A1 |
The invention relates to a process for the production of enantiomerically-pure AzeOH which comprises selective crystallisation of a diastereomerically-pure AzeOH-tartrate salt from a homogeneous solution of AzeOH, optically-active tartar...
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WO/1997/036867A1 |
A compound of formula (I) wherein R1 is a group of formula G1, G2, G3, G4 or G5; R2 is hydrogen, (C1-C4)alkyl, phenyl or naphthyl, wherein said phenyl or naphthyl may optionally be substituted with one or more substituents, preferably fr...
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WO/1997/033891A1 |
A process for preparing allenyl-'beta'-lactam compounds of general formula (II) or 3-halocephem compounds of general formula (III) from halogenated 'beta'-lactam compounds of general formula (I) under reaction conditions selected dependi...
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WO/1997/031922A1 |
It is described a process for the preparation of 2-halomethyl-penems (in particular 2-chloromethyl-penems) comprising, as intermediate step, the formation of the corresponding 2-haloacetylthio-azetidone.
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WO/1997/027175A1 |
The invention relates to substituted ethyl 'alpha','alpha' - diarylmethyl ether derivatives and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, and methods of treating cocaine addiction and ove...
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WO/1997/025309A1 |
Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful...
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WO/1997/025322A1 |
The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof. Such compounds and salts are tachykinin antogonists.
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WO/1997/021675A1 |
Compounds of formula (I) are prodrugs of the corresponding compounds in which CO2R3 is CO2H. These are inhibitors of the phospholipase A2 enzyme Lp-PLA2 and of use in treating atherosclerosis.
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WO/1997/021676A1 |
Azetidinone compounds of formula (I) in which inter alia: R0 is CR4R5-X1-Y1 or (CH2)pX2(CH2)qY2; R4 and R5 which may be the same or different is each selected from hydrogen and C(1-6)alkyl, or R4 and R5 may be linked together to form the...
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WO/1997/020848A1 |
The following description sets forth a reductive cyclization induced by a trialkyl phosphite of a derivative of formula (II) to give a cephalosporin of formula (I), where A is a protective group of the amino function, R1A is H, a cation ...
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WO/1997/019059A1 |
In accordance with the present invention, a novel class of substituted aryl compounds (containing ether, ester, amide, ketone or thioether substitution) that promote the release of ligands involved in neurotransmission have been discover...
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WO/1997/017958A1 |
The present invention relates to novel compounds which have hemoregulatory activities and can be used to stimulate hematopoiesis and for the treatment of viral, fungal and bacterial infectious diseases.
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WO/1997/016448A1 |
The present invention relates to the process for the preparation of the substituted azetidinone having formula (I) comprising a convergent synthesis.
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WO/1997/016424A1 |
A process for preparing a compound of formula (I) wherein X is H or F, comprising: (a) alkylation of a 3-unsubstituted chiral azetidinone of formula (II) with cinnamyl bromide or 4-fluorocinnamyl bromide; (b) Wacker oxidation of the prod...
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WO/1997/013750A1 |
A compound of formula (I) wherein: R1 is C1-6 alkyl-R5; R2 is hydrogen, C1-6 alkyl or C1-6 alkyl-R5, wherein R1 and R2 may be the same or different; R3 is COR7 or S(O)0-2R8; R4 is COR9 or SO2R10.
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WO/1997/011068A1 |
Pyridonecarboxylic acid derivatives represented by general formula (1) or their salts, wherein R1 represents hydrogen or a carboxyl protecting group; R2 represents hydroxy, lower alkoxy or optionally substituted amino; R3 represents hydr...
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WO/1997/011073A1 |
The present invention relates to therapeutically active heterocyclic compounds, to methods for their preparation and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the cent...
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WO/1997/010713A1 |
Plant-microbicidal compositions which comprise, as active ingredient, a 'beta'-lactam of the general formula (I), in which R is hydrogen; unsubstituted or substituted C1-C8alkyl, C3-C8alkenyl or C3-C8alkynyl; a group COR3; a group COOR4;...
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WO/1997/009328A1 |
A compound of formula (I), or pharmaceutical acceptable salts thereof wherein X is NR1, S(O)g, or O; R1 is H, C1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R1 is -(CH2)h-aryl, -COR1-1, -COOR1-2, -CO-(CH2)h-COR1-1...
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WO/1997/007112A1 |
A stoichiometric acid moiety transfer reaction for the preparation of an acid salt of an amine compound is disclosed. The acid moiety transfer reaction provides amine acid salts of high purity and having crytalline structure of uniform s...
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WO/1997/006174A1 |
A process for the preparation of a compound of formula (I), wherein R is a hydroxyl protecting group which comprises isomerisation of a compound of formula (II), wherein R is a hydroxyl protecting group.
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WO/1997/005105A1 |
Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, AA and Y are as defined herein, inhibit phosphodiesterase type IV or inhibit the production of tumor necrosis factor, and therefore are useful in the...
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WO/1997/005111A1 |
Novel N-(4-substituted-benzyl)-2-aminolactams compounds, having antiepileptic, anti-Parkinson, neuroprotective, anti-depressant, antispastic and/or hypnotic activity, of general formula (I) wherein: m is zero, 1, 2 or 3; n is zero, 1, 2 ...
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WO/1997/003953A1 |
Compounds of the formula (I) in which A is oxygen, sulphur or NH; B is a group of the formula (IIa) or (IIb); and the other variables have the meaning given in claim 1, may be used as inhibitors of the enzyme cyclo-oxygenase II.
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WO/1997/002242A1 |
Azetidinone compounds of formule (I) in which: R1 and R2, which may be the same or different, is each selected from hydrogen, halogen or C(1-8)alkyl; R4 and R5 which may be the same or different is each selected from hydrogen, C(1-6)alky...
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WO/1997/002284A1 |
There is provided amino acid derivatives of formula (I), wherein p, q, R1, R2, R3, R4, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in parti...
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WO/1997/002241A1 |
The invention relates to a process for the production of enantiomerically-pure AzeOH which comprises selective crystallisation of a diastereomerically-pure tartrate salt thereof, followed by liberation of the free amino acid, as well as ...
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WO/1997/001564A1 |
A process of synthesizing a compound of formula (1) or (2) is disclosed wherein R represents H or methyl and P represents triethylsilyl or trimethylsilyl. A compound of formula (3) or (4) is reacted with P-C1 wherein P is as defined abov...
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WO/1996/040679A1 |
The compounds of formula (I) exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they ...
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WO/1996/039384A1 |
Compounds of Formula (1) wherein R6 is carboxy, (C1-C8)alkoxycarbonyl, benzyloxycarbonyl, C(O)NR8R9 or C(O)R12 as glucogen phosphorylase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to...
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WO/1996/036602A1 |
A process for preparing N-acetyl-3,3-dinitroazetidine (ADNAZ) is disclosed. ADNAZ may form a eutectic with trinitroazetidine (TNAZ) or it can be readily nitrated to form TNAZ by removal of the acetyl group. Additional processes for prepa...
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WO/1996/034852A1 |
The present invention relates to novel tetracycline derivatives, to intermediates used in their preparation, to pharmaceutical compositions containing them and to their medicinal use. The active compounds of the present invention are use...
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WO/1996/035122A1 |
This invention relates to libraries of azetidinone peptide-like compounds and a combinatorial process for synthesis. Selected compounds are biologically active as inhibitors of the Vasopressin (V1a) receptor.
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WO/1996/034857A1 |
Compound represented by structural formula (I) or a pharmaceutically acceptable salt thereof, wherein: a is 0, 1, 2 or 3; b, d and e are independently 0, 1 or 2; R is H, C1-6 alkyl, -OH or C2-C6 hydroxyalkyl; A is an optionally substitut...
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WO/1996/029307A1 |
Diphenylmethyl-azetidinone compounds represented by general formula (I) or pharmacologically acceptable salts thereof, and medicinal compositions, elastase inhibitor and antiinflammatory agent containing the same; wherein R1 and R2 repre...
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WO/1996/029334A1 |
A process for the preparation of an allenyl-'beta'-lactam compound which comprises reacting the hydroxyl group of a 'beta'-lactam compound of general formula (1) with a reactive functional derivative of a sulfonic acid of the general for...
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WO/1996/028421A1 |
A process for producing a halogenated 'beta'-lactam compound, comprising halogenating the allenyl group of an allenyl-'beta'-lactam compound of general formula (1) with a cupric halide and a metal halide into a halogenated 'beta'-lactam ...
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WO/1996/028453A1 |
A process for producing a 2-isocephem derivative which comprises treating, in a water-containing organic solvent, a 2-azetidinyl-3,4-dihalogeno-2-butenoic acid compound represented by general formula (1) with a thioacetic acid derivative...
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WO/1996/028422A1 |
A process for the production of a halogenated 'beta'-lactam compound represented by general formula (2) which comprises replacing the hydroxyl group of a halogenated 'beta'-lactam compound represented by general formula (1) with a haloge...
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WO/1996/027587A1 |
A process for producing a compound of formula (1.0) comprises the sequence of steps: (2.0), (3.0), (5.0) or (5.1), (8.0) or (8.1), (9.0) and (1.0); wherein the various radicals are as defined in the specification.
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WO/1996/025426A1 |
The description relates to compounds of formula (I) in which A, B, D, R1 and R2 have the meanings given in the specification. The compounds are suitable for the treatment of diseases. The novel compounds are produced via compounds of the...
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