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WO/1995/015951A1 |
A novel imidazole derivative represented by general formula (1) or (2) to be used as a selective muscarine antagonist, wherein R1 represents optionally substitued phenyl or thienyl; R2 represents cyano, hydroxy, carboxy, CONR7R8 (wherein...
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WO/1995/015954A1 |
A compound of formula (I) or a salt thereof, wherein P is a 5 to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur; A is CONH or NHCO; B is oxygen, S(O)p where p is O, 1 or 2, or NR12; m...
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WO/1995/014726A1 |
A process for preparing polyazamacrocyclic compounds using a nucleophilic imidazoline with (A) an ethylene oxide or an ethylene carbonate, in an aprotic solvent, followed by intramolecular amination, and then either basic or acidic hydro...
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WO/1995/014461A1 |
The present invention provides therapeutically useful substituted guanidines and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
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WO/1995/014383A1 |
The use of branched, cyclic or substituted alkyl or alkyl-N-pyrroles for the protection of materials is disclosed, as well as new and known S-alkyl-N-pyrroles and a process for preparing the same.
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WO/1995/014688A1 |
The application relates to derivatives of 2,3,5,6-tetrafluorobenzoic acid of formula (I) wherein Y represents oxygen or sulphur and X represents the groups -O- N=CR1R2, -OR3, -OCHR4-CO-NR5R6 or -NR7R8 as well as a process for manufacturi...
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WO/1995/014467A1 |
The present invention provides N,N'-diaryl substituted guanidines having therapeutic utility. The compounds of the present invention are represented by formula (I), wherein R and R1 represent hydrogen or other group and Ar and Ar1 repres...
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WO/1995/013262A1 |
Compounds of formula (I) are described wherein R1 is hydrogen, -(lower alkyl)q(CO2R6 or OH), -CN, -C(R7)=NOR8, NO2, -O(lower alkyl)R9, -CC-R10, -CR11=C(R12)(R13), -C(=O)CH2C(=O)CO2H, -CO(R14), alkylthio, alkylsulphinyl, alkylsulphonyl, c...
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WO/1995/013276A1 |
The present invention relates to a thiophenesulfonylurea derivative represented by general formula (I), the process for preparation thereof, and herbicide using it; and a salt thereof, in which T represents a group T1, T2, or T3 having g...
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WO/1995/012583A1 |
Compounds having a quinazolin-2-one nucleus with a substituted alkynyl or substituted alkenyl at the 4-position are described. These compounds are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties),...
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WO/1995/011889A1 |
A thiazole derivative represented by general formula (1), a tautomer thereof, a salt thereof, a medicine containing the same, and an intermediate for producing the compound. In formula (1) A represents an optionally substituted heterocyc...
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WO/1995/010507A1 |
Compounds are disclosed having the formula (I), as well as their salts, as they are defined in the first claim. In the formula (I), R1 stands for CO-Q-R8, in which R8 = H or R; R2, R3 stand for H or (C1-C4)alkyl; R4 stands for H, R, RO, ...
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WO/1995/010513A1 |
Benzothiophenes and related compounds of formula (1), wherein A, B, Z are independently -CH=, -CR4= or =N-; X is -S-, -O-, -NH-, -NR2, -CH2-CH2-, -CH2-CH2-CH2-, -CH2-O-; -OCH2-, -CH2-S-, -CO-, -SCH2-, -N=CR2- or -R2C=N-; Y is optionally ...
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WO/1995/010516A1 |
A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of formula (1.0) to a biological system. In particular, the method inhibits the...
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WO/1995/010508A1 |
A compound represented by general formula (I), and having an intracellular phospholipase A2 inhibitor activity, and a composition containing the same, wherein a and b represent each a carbon atom and the bond -- between the atoms a and b...
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WO/1995/009157A1 |
An azole derivative represented by general formula (I), a salt thereof, a hydrate thereof, or a solvate thereof, wherein R1 and R2 may be the same or different and each represents hydrogen, lower alkyl, or optionally halogenated phenyl; ...
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WO/1995/008462A1 |
The hydraulic system (12) has a metal valve body (11) with at least one stepped drilling (15) for the hydraulic section of an electromagnetically actuated valve (10). The hydraulic section (13) has a securing flange (30) inserted into a ...
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WO/1995/008543A1 |
The invention relates to novel substituted propane-2-ol derivatives of formula (I), wherein R1 represents a C1-10alkyl group, a phenyl group or a phenyl-C1-6alkyl group, and the phenyl moiety of the two latter groups may carry at least o...
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WO/1995/007884A1 |
A compound of formula (I) or a salt thereof, or a solvate thereof, wherein A and B each independently represents a C1-4 n-alkylene group wherein each carbon is optionally substituted by a C1-6 alkyl group; D represents CO, SO2, NH-CO or ...
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WO/1995/007895A1 |
A process for making fluconazole comprising the steps shown above.
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WO/1995/007896A1 |
Novel hydroxy ethyl azolyl derivatives of formula (I), in which: X is hydrogen, halogen, alkyl with 1 to 4 carbon atoms or alkoxy with 1 to 4 carbon atoms; Z is halogen, alkyl with 1 to 4 carbon atoms, halogen alkyl with 1 to 4 carbon at...
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WO/1995/007903A1 |
A compound of formula (I), or a salt thereof, or a solvate thereof, wherein A and B each independently represents a C1-4 n-alkylene group wherein each carbon is optionally substituted by a C1-6 alkyl group; D represents CO, SO2, NH-CO or...
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WO/1995/007269A1 |
The invention relates to retroviral protease inhibitors of the general formula (I): W-(A)n-B-(A*)m-V where W, A, B, A*, V, n and m are as defined herein, including related prodrugs of general formula (I) comprising a solubilising group w...
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WO/1995/007267A1 |
A quinazoline compound represented by general formula (I), which is useful as a medicine having the activity as a calmodulin-dependent cGMP-PDE inhibitor, or a pharmacologically acceptable salt thereof wherein R1, R2, R3, R4 and R5 repre...
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WO/1995/006645A1 |
The present invention relates to benzofuran derivatives of formula (I) wherein R represents a hydrogen atom or a C1-4alkoxy group; R1 is selected from phenyl, optionally substituted by a group -(CH2)nCONR3R4 or S(O)mR3; or a 5- or 6-memb...
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WO/1995/006049A1 |
Compounds of formula (I) or salts thereof, wherein R1-R4, W, A, n and m are defined as in claim 1, e.g. R1, R2 represent H, (subst.) alkyl, (subst.) alkenyl or alkinyl, (subst.) cycloalkyl, (subst.) aryl or acyl, and A represents (subst....
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WO/1995/006036A1 |
A process is disclosed for preparing pyrazole and its derivatives having formula (I), in which the residues R1, R2, R3 and R4 stand for hydrogen, halogen, nitro, carboxyl, sulfonyl or C-organic residues, from alpha,beta-unsaturated carbo...
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WO/1995/006047A1 |
A compound of formula (I) in which R1 and R2 are each hydrogen or lower alkyl, R3 is optionally substituted quinolyl or oxide thereof, and X and Y are each hydrogen, halogen, cyano or lower alkyl, or pharmaceutically acceptable salts the...
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WO/1995/006046A1 |
Compounds of formula (I) and pharmaceutically acceptable salts and biolabile esters thereof, wherein R1 is H, C1-C4 alkyl, phenyl optionally substituted by up to three substituents independently selected from C1-C4 alkyl, C1-C4 alkoxy, h...
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WO/1995/006035A1 |
A benzazepine derivative, represented by general formula (I), useful as an arginine vasopressing antagonist; a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing the same; and difluorobenzazepinone derivati...
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WO/1995/004729A1 |
Novel amide derivatives, processes for their preparation, and pharmaceutical compositions containing them.
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WO/1995/004723A1 |
An imidazolylalkylamine derivative represented by general formula (I) useful as a steroid 17-20 lyase, a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same as the active ingredient, wherein R1 ...
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WO/1995/003700A1 |
Carbapenems of formula (I) are disclosed as useful antibacterial agents.
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WO/1995/004052A1 |
Methylguanidine derivatives, for use as drugs, having general formula (I), wherein the asterisk is an asymmetrical carbon; each of R1, R2 and R3, which are the same or different, is hydrogen, halogen, a C1-4 alkyl radical, C1-4 alkoxy, p...
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WO/1995/003277A1 |
A novel pyrrolidine derivative represented by general formula (1) or a pharmaceutically acceptable salt thereof, having a prolyl endopeptidase inhibitor activity and promising as an active ingredient of an antiamnetic. In said formula R1...
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WO/1995/002405A1 |
Compounds of formula (I), in which X is -O-, -NH- and -NR8-; Y is -CH2-, -CHR8- and -C(R8)2-; R1 is camphor-10-yl, C1-5 alkoxyl, styryl, hydroxystyryl, furyl, unsubstituted or substituted thienyl, naphthyl, indolyl, tetrahydronaphthyl, u...
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WO/1995/001332A1 |
An arylsulfonamide derivative represented by general formula (I), which has a thromboxane A2 antagonism, or a salt thereof, a process for producing the same, and a pharmaceutical composition containing the same, wherein R1 represents uns...
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WO/1995/001344A1 |
The invention concerns compounds of formula (I), or salts thereof0, in which G is a group of the formula G1, G2 or G3; R1 is H or alkyl; R2 is COOH, CSOH or a carboxylic- or thiocarboxylic-group derivative with 1 to 20 C-atoms or an acyl...
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WO/1995/001326A1 |
The present invention is concerned with diaryl compounds of formula (I) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidae...
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WO/1995/000507A1 |
A compound of formula (I) having immunomodulatory activity or a pharmaceutically acceptable salt thereof, in which R1, R2 and R3 are hydrogen; halo; cyano; hydroxy(C1-6)-alkyl; C1-6 alkyl; C1-6 alkoxy; C2-6 alkanoyl; C2-6 alkoxycarbonyl;...
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WO/1995/000468A1 |
The present invention provides novel fluorenone derivatives represented by formula (A) (wherein Ra-Rg are defined in the specification), and a method for repairing and protecting central or peripheral nerve degeneration comprising use of...
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WO/1995/000509A1 |
An indazolesulfonylurea derivative represented by general formula (I) or (II), a herbicide containing the same as the active ingredient, and an intermediate for the production thereof, wherein R1 represents hydrogen, alkyl, etc.; R2 and ...
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WO/1995/000493A1 |
Compounds of formula (I) and pharmaceutically acceptable salts thereof in which R1 represents hydrogen, halo, cyano, cyanoalkyl, alkyl, alkoxy, phenoxy, phenyl, alkoxycarbonyl, -NR13R14, -N(R15)SO2R16, halogenated alkoxy, halogenated alk...
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WO/1994/029269A1 |
A process for the production of guanidino protected omega-aminoalkyl guanidines comprising reacting a diamine selectively at one amino group with an alkoxycarbonyl or aralkoxycarbonyl protected electrophilic guanylation reagent. The proc...
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WO/1994/029281A1 |
The invention concerns cyclobutylazoles of formula (I) in which R is optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl or aryl, X is a nitrogen atom or CH group and Z is a carbonyl or -CH(OH)- group, as well as their acid additi...
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WO/1994/029313A1 |
A novel beta-lactam compound represented by general formula [1] and having an excellent antibacterial activity against gram-positive bacteria, in particular, methicillin-resistant staphylococci and methicillin-resistant coagulase-negativ...
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WO/1994/029299A1 |
Certain novel imidazole derivatives having the ability to inhibit the lipoxygenase enzyme and having formula (I), wherein Y is hydrogen, C1-C8 alkyl, halosubstituted C1-C4 alkyl, phenyl, substituted phenyl, C7-C14 phenylalkyl, C7-C14 (su...
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WO/1994/029276A1 |
3-arylpyrazole derivatives of formula (I) in which X, X2, X3, X4 and X5, which are the same or different, are H, Hal, nitro, alkyl, alkoxy, Y is H, Hal, nitro, CN, alkyl, alkoxy, alkylthio or an optionally substituted amino; Ra is H, R(a...
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WO/1994/027971A1 |
A compound of formula (I) or a salt thereof, or a solvate thereof, wherein A represents CH2, (CH2)2, CO, COCH2, CH2CO, CSCH2 or CH=CH; B represents CH2 or CO; Z represents a bond, CH2, (CH2)2 or X-CH2-CH2 wherein X represents O or S; D r...
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WO/1994/027989A1 |
This invention relates to substituted carbazole derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine for the reduction of oestrogen and/or androgen levels. Particula...
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