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公开(公告)号:CA2328396A1
公开(公告)日:1999-10-28
申请号:CA2328396
申请日:1999-04-20
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , TREIBER HANS-JORG , MOLLER ACHIM , KNOPP MONIKA
IPC: C07D295/08 , A61K31/16 , A61K31/166 , A61K31/27 , A61K31/395 , A61K31/40 , A61K31/455 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P9/00 , A61P13/12 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P27/12 , A61P29/00 , A61P35/00 , A61P35/04 , A61P37/02 , A61P43/00 , C07C229/38 , C07C237/20 , C07C237/22 , C07C237/32 , C07C237/36 , C07D209/14 , C07D213/82 , C07D233/64 , C07D237/32 , C07D237/36 , C07D295/14 , C07D295/155
Abstract: The invention relates to cysteine protease inhibitors of the general formula (I), in which A is -(CH2)p-R1, where R1 can be pyrrolidine, morpholine, piperidine, -NR5R6 and formula (a) and p can be 1 or 2; B can be possibly substituted phenyl, pyridyl, pyrimidyl and pyridazyl; D is a bond, -(CH2)m-, - CH=CH-, -CC-; R2 is chlorine, bromine, fluorine, alkyl, NHCO alkyl, NHSO2 alkyl, NO2, -O-alkyl and NH2; R3 is an alkyl which can carry a possibly substituted phenyl ring, indolyl ring and cyclohexyl ring; and Y is phenyl, pyridine, pyrimidine and pyrazine; R4 is hydrogen, COOR9 and CO-Z, where Z i s NR10R11 and and formulae (b), (c), (d); n is 0, 1 or 2 and m is 0, 1, 2, 3 o r 4.
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公开(公告)号:DE19818614A1
公开(公告)日:1999-10-21
申请号:DE19818614
申请日:1998-04-20
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS-JOERG , KNOPP MONIKA
IPC: A61K31/196 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/47 , A61K31/517 , A61P9/08 , A61P9/10 , A61P13/12 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P27/12 , A61P43/00 , C07C233/76 , C07C237/22 , C07C311/21 , C07D213/56 , C07D215/36 , C07D239/70 , C07D239/96 , C07D227/00 , A61K31/18 , A61K31/435 , A61K31/505
Abstract: Carboxybenzamide derivatives (I) are new.- DETAILED DESCRIPTION - Carboxybenzamide derivatives of formula (I) and their tautomers, isomers and salts are new: - R1 = 1-6C alkyl, phenyl, naphthyl, quinolyl, pyridyl, pyrimidinyl, pyridazinyl, quinazolinyl or quinoxalinyl, all optionally substituted by 1-2 R4 groups; - R2 = (CH2)mR8; - R8 = phenyl, cyclohexyl or indolyl; - m = 1-6; - X = a bond; CH2, CH2CH2, CH=CH, ethynylene, CONH or SO2NH; or - R1-X = a group of formula (i) or (ii): - R3 = H or CONR6R7; - R4, R5 = H, 1-4C alkyl or 1-4C alkoxy; - R6, R7 = H or 1-6C alkyl; - n = 0-2.- ACTIVITY - None given.- MECHANISM OF ACTION - Cysteine protease inhibitor
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公开(公告)号:DE19817459A1
公开(公告)日:1999-10-21
申请号:DE19817459
申请日:1998-04-20
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS-JOERG , KNOPP MONIKA
IPC: A61K31/4164 , A61K31/426 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/455 , A61K31/4709 , A61K31/4725 , A61K31/4965 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P9/04 , A61P9/08 , A61P9/10 , A61P13/12 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/28 , A61P27/12 , A61P43/00 , C07D213/81 , C07D213/82 , C07D233/90 , C07D239/28 , C07D239/30 , C07D239/42 , C07D241/28 , C07D277/20 , C07D277/44 , C07D277/56 , C07D401/04 , C07D401/12 , C07D413/12 , C07D401/06 , C07D403/04 , C07D213/78 , C12N9/99 , C12N9/48
Abstract: Heterocyclic amide derivatives (I) are new.- DETAILED DESCRIPTION - Heterocyclic amide derivatives of formula (I) and their tautomers, isomers and salts are new: - R1 = phenyl, naphthyl, quinolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinazolinyl, isoquinolyl, quinoxalinyl, thienyl, benzothienyl, benzofuranyl, furyl or indolyl, all optionally substituted by 1-3 R5 groups; - R2 = Cl, Br, F, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl, CF3, (1-6C alkyl)phenyl, (2-6C alkenyl)phenyl, (2-6C alkynyl)phenyl (correction; original text repeats 1-6C alkylphenyl), phenyl, 2-5C alkanoylamino, 1-4C alkylsulfonylamino, benzamido, naphthoylamino, NO2, 1-4C alkoxy or NH2, where the aromatic rings are optionally substituted by 1-2 R5 groups, or two R2 groups form a fused benzene ring optionally substituted by R5; - R3 = 1-6C alkyl optionally substituted by a phenyl, pyridyl or naphthyl group optionally substituted by 1-2 R5 groups; - R5 = H, 1-4C alkyl, 1-4C alkoxy, OH, halogen, CF3, NO2, NH2, CN, COOH, (1-4C alkoxy)carbonyl, 2-5C alkanoyl-amino, benzamido, 1-4C alkylsulfonylamino, phenylsulfonylamino, 1-4C alkylsulfonyl or phenylsulfonyl; - X = a bond; (CH2)m, (CH2)mQ(CH2)o, CH=CH, ethynylene, COCH=CH, NHCOCH=CH, CH=CHCONH, or phenylene monosubstituted by R5; - Q = O, S, SO, SO2, CO, NHCO, CONH, NHSO2 or SO2NH; or - R1-X = a group of formula (i) or (ii): - Y = an unsaturated heterocyclic ring, e.g. pyridine, pyrimidine, pyrazine, imidazole or thiazole; - R4 = H, COOR6 or COZ; - Z = NR7R8 or a group of formula (iii)-(v): - R6 = H, or 1-6C alkyl optionally substituted by phenyl (itself optionally substituted by 1-2 R9 groups); - R7 = H or 1-6C alkyl; - R8 = H, or 1-6C alkyl optionally substituted by phenyl (itself optionally substituted by a R9 group) or by a group of formula (iii)-(v) or by morpholino, 1-R10-4-piperidinyl or (CH2)oNR10R11; - R9 = H, 1-4C alkyl, 1-4C alkoxy, OH, halogen, CF3, NO2, NH2, CN, COOH, (1-4C alkoxy)-carbonyl, 2-5C alkanoyl-amino, benzamido, 1-4C alkylsulfonylamino, phenylsulfonylamino, 1-4C alkylsulfonyl or phenylsulfonyl; - R10, R11 = H, or 1-6C alkyl optionally substituted by phenyl (optionally substituted by 1-2 R9 groups); - n = 0-2; - m, o = 0-4.- ACTIVITY - None given.- MECHANISM OF ACTION - Cysteine protease inhibitor
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公开(公告)号:CA2328396C
公开(公告)日:2009-02-10
申请号:CA2328396
申请日:1999-04-20
Applicant: BASF AG
Inventor: KNOPP MONIKA , TREIBER HANS-JORG , MOLLER ACHIM , LUBISCH WILFRIED
IPC: C07C237/36 , C07D295/08 , A61K31/16 , A61K31/166 , A61K31/27 , A61K31/395 , A61K31/40 , A61K31/455 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P9/00 , A61P13/12 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P27/12 , A61P29/00 , A61P35/00 , A61P35/04 , A61P37/02 , A61P43/00 , C07C229/38 , C07C237/20 , C07C237/22 , C07C237/32 , C07D209/14 , C07D213/82 , C07D233/64 , C07D237/32 , C07D237/36 , C07D295/14 , C07D295/155
Abstract: The invention relates to cysteine protease inhibitors of the general formula (I), in which A is -(CH2)p-R1, where R1 can be pyrrolidine, morpholine, piperidine, -NR5R6 and formula (a) and p can be 1 or 2; B can be possibly substituted phenyl, pyridyl, pyrimidyl and pyridazyl; D is a bond, -(CH2)m-, -CH=CH-, -C.ident.C-; R2 is chlorine, bromine, fluorine, alkyl, NHCO alkyl, NHSO2 alkyl, N02, -O-alkyl and NH2; R3 is an alkyl which can carry a possibly substituted phenyl ring, indolyl ring and cyclohexyl ring; and Y is phenyl, pyridine, pyrimidine and pyrazine; R4 is hydrogen, COOR9 and CO-Z, where Z is NR10R11 and and formula (b); n is 0, 1 or 2 and m is 0, 1, 2, 3 or 4.
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公开(公告)号:CA2380169C
公开(公告)日:2007-01-09
申请号:CA2380169
申请日:2000-07-11
Applicant: BASF AG
Inventor: SCHAFER BERND , KOSER STEFAN , KNOPP MONIKA
IPC: C07D277/20 , C07D277/56
Abstract: The present invention relates to a method for producing 2-amino-methyl-4-cya no- thiazol, including a step in which an aminonitrile is stirred with a cystein ester.
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公开(公告)号:HU0201977A2
公开(公告)日:2002-09-28
申请号:HU0201977
申请日:2000-07-11
Applicant: BASF AG
Inventor: KNOPP MONIKA , KOSER STEFAN , SCHAEFER BERND
IPC: C07D277/20 , C07D277/56
Abstract: The invention relates to processes for preparing 2-aminomethyl-4-cyanothiazole and its salts of the formulae Ia and Ibin whichn=1 or 2 andfor n=1, X is chloride, bromide, triflate and hydrogen sulfate andfor n=2, X is sulfate, which comprises the process step where the aminonitrile of the formula IIis stirred with a cysteine ester of the formula III,in which R is branched or linear C1-10-alkyl orwhere n=0, 1 or 2 and R is branched or linear C1-C10C10-alkyl or C1-C4-alkoxy or C1-C4-dialkylamino in an inert solvent in the presence of a base at from 0° C. to 80° C. until the reaction has essentially proceeded to completion, and to the compounds of the formulae Ia and Ib.
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公开(公告)号:BG105689A
公开(公告)日:2002-02-28
申请号:BG10568901
申请日:2001-07-10
Applicant: BASF AG
Inventor: STEINER GERD , SCHNELLHAAS KURT , LUBISCH WILFRIED , HOLZENKAMP UTA , STARCK DOROTHEA , KNOPP MONIKA , SZABO LASZLO , EMLING FRANZ , GARCIA-LADONA FRANCISCO J , HOFMANN HANS-PETER , UNGER LILIANE
IPC: C07D495/04 , A61K31/505 , A61K31/519 , A61P9/10 , C07D495/14 , A61K31/495 , A61K31/55
Abstract: The invention relates to the utilization of pyrimidine derivatives of formula wherein the substituents have the meaning cited in the description, and to the utilization of the physiologically compatible salts thereof for producing medicaments used for preventing and treating cerebral ischaemia and strokes. 1 claim
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公开(公告)号:NO20020328A
公开(公告)日:2002-01-31
申请号:NO20020328
申请日:2002-01-22
Applicant: BASF AG
Inventor: KNOPP MONIKA , KOSER STEFAN , SCHAEFER BERND
IPC: C07D277/20 , C07D277/56
CPC classification number: C07D277/56
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公开(公告)号:NO20020328D0
公开(公告)日:2002-01-22
申请号:NO20020328
申请日:2002-01-22
Applicant: BASF AG
Inventor: KNOPP MONIKA , KOSER STEFAN , SCHAEFER BERND
IPC: C07D277/20 , C07D277/56 , C07D
Abstract: The invention relates to processes for preparing 2-aminomethyl-4-cyanothiazole and its salts of the formulae Ia and Ibin whichn=1 or 2 andfor n=1, X is chloride, bromide, triflate and hydrogen sulfate andfor n=2, X is sulfate, which comprises the process step where the aminonitrile of the formula IIis stirred with a cysteine ester of the formula III,in which R is branched or linear C1-10-alkyl orwhere n=0, 1 or 2 and R is branched or linear C1-C10C10-alkyl or C1-C4-alkoxy or C1-C4-dialkylamino in an inert solvent in the presence of a base at from 0° C. to 80° C. until the reaction has essentially proceeded to completion, and to the compounds of the formulae Ia and Ib.
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公开(公告)号:HU0102732A2
公开(公告)日:2001-12-28
申请号:HU0102732
申请日:1999-04-20
Applicant: BASF AG
Inventor: KNOPP MONIKA , LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS-JOERG
IPC: C07D295/08 , A61K31/16 , A61K31/166 , A61K31/27 , A61K31/395 , A61K31/40 , A61K31/455 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P9/00 , A61P13/12 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P27/12 , A61P29/00 , A61P35/00 , A61P35/04 , A61P37/02 , A61P43/00 , C07C229/38 , C07C237/20 , C07C237/22 , C07C237/32 , C07C237/36 , C07D209/14 , C07D213/82 , C07D233/64 , C07D237/32 , C07D237/36 , C07D295/14 , C07D295/155
Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH═CH—, —C═C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, —NHSO2—C1-C4-alkyl and —SO2—C1-C4-alkyl; and Y is phenyl, pyridine, pyrimidine and pyrazine and R4 is hydrogen, COOR9 and CO—Z in which Z is NR10R11 and R9 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and R10 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which itself may also be substituted by one or two R12 radicals, and R11 is hydrogen, C1-C6-alkyl, branched or unbranched, which may also be and substituted by a phenyl ring which may also carry an R9 radical, and R12 can be hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, J, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, —NHCO—C1-C4-alkyl, —NHCO-phenyl, —NHSO2—C1-C4-alkyl, NHSO2-phenyl, —SO2—C1-C4-alkyl and —SO2-phenyl, R13 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and R14 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and n is a number 0, 1 or 2, and m,q are, independently of one another, a number 0, 1, 2, 3 or 4.
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