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公开(公告)号:CZ183399A3
公开(公告)日:1999-08-11
申请号:CZ183399
申请日:1997-11-11
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MULLER ACHIM , TREIBER HANS-JORG
IPC: A61K31/16 , A61K31/166 , A61K31/18 , A61K31/4045 , A61K31/435 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61P9/10 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/28 , A61P27/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07C233/76 , C07C235/42 , C07C235/46 , C07C235/58 , C07C235/60 , C07C235/84 , C07C237/42 , C07C311/08 , C07C311/21 , C07C317/44 , C07C323/42 , C07C323/60 , C07D209/14 , C07D209/16 , C07D213/30 , C07D213/56 , C07D213/71 , C07D213/82 , C07D215/36 , C07D215/14
Abstract: Compounds of the formulawhere R1, R2, R3, X and n are as defined in the description, are inhibitors of cysteine protease.
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公开(公告)号:BR9909776A
公开(公告)日:2000-12-19
申请号:BR9909776
申请日:1999-04-19
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MULLER ACHIM , TREIBER HANS-JURG , KNOPP MONIKA
IPC: C07D295/08 , A61K31/18 , A61K31/27 , A61K31/4409 , A61K31/4418 , A61P9/00 , A61P13/12 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P29/00 , A61P35/00 , A61P35/04 , A61P37/02 , A61P43/00 , C07C233/78 , C07C235/42 , C07C237/34 , C07C311/21 , C07D213/56 , C07D295/096 , A61K31/44
Abstract: Benzamides of the formula Iand 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:R1-C1-C6-alkyl, branched or unbranched, where one of the C atoms in this chain may be substituted by a phenyl ring, cyclohexyl ring, indolyl ring and an SCH3 group, and the phenyl ring in turn is substituted by by [sic] a maximum of two R4 radicals, where R4 [lacuna] 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, andR2 can be NR5CO-R6 and NHR5SO2-R6, andR3 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO-C1-C4-alkyl, NHSO2-C1-C4-alkyl, NO2, -O-C1-C4-alkyl, CN, COOH, CONH2, COO-C1-C4-alkyl, SO2-C1-C4-alkyl, -SO2Ph, SO2NH-C1-C4-alkyl, iodine, SO2NH2 and NH2, andA can be aromatic rings and heteroaromatic rings such as naphthyl, quinolyl, quinoxyl, benzimidazolyl, benzothienyl, quinazolyl, phenyl, thienyl, imidazolyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by by [sic] R9 and up to 2 R8 radicals, andB a bond, -(CH2)m-, -(CH2)m-O-(CH2)o-, -(CH2)o-S-(CH2)m-, -(CH2)o-SO-(CH2)m-, -(CH2)o-SO2-(CH2)m-, -CH=CH-, -C=C-, -CO-CH=CH-, -(CH2)o-CO-(CH2)m-, -(CH2)m-NHCO-(CH2)o-, -(CH2)m-CONH-(CH2)o-, -(CH2)m-NHSO2-(CH2)o-, -NH-CO-CH=CH-, -(CH2)m-SO2NH-(CH2)o-,A-B together alsoR5 hydrogen and C1-C4-alkyl andR6 is hydrogen, phenyl, naphthyl, C1-C6-alkyl, linear or branched, it being possible for a C atom in the chain to be substituted by a phenyl ring which itself may also be substituted by one or two R4 radicals, andR8 can be 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, phenyl, NHCO-phenyl, -NHSO2-C1-C4-alkyl, -NHSO2-phenyl, -SO2-C1-C4-alkyl, pyridine [sic] and SO2-phenyl,R9 hydrogen, -CHR14-(CH2)p-R12 where R12 pyrrolidine [sic], morpholine [sic], piperidine [sic], hexahydroazepine [sic], homopiperazine [sic], and R10 [lacuna] C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring which is in turn substituted by by [sic] a maximum of two R11 radicals, where R11 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; andR13 is hydrogen and C1-C6-alkyl, branched or unbranched, andn,p is [sic], independently of one another, a number 0, 1 or 2, andm,o is [sic], independently of one another, a number 0, 1, 2, 3 or 4.
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公开(公告)号:BR9909774A
公开(公告)日:2000-12-19
申请号:BR9909774
申请日:1999-04-20
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MULLER ACHIM , TREIBER HANS-JURG , 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 , C07D237/00
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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公开(公告)号:BR9909819A
公开(公告)日:2000-12-19
申请号:BR9909819
申请日:1999-04-19
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MULLER ACHIM , TREIBER HANS-JURG , KNOPP MONIKA
IPC: C07D295/14 , A61K31/18 , A61K31/357 , A61K31/36 , A61K31/40 , A61K31/437 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/445 , A61K31/4453 , A61K31/453 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/5375 , A61P9/08 , A61P9/10 , A61P13/12 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P29/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07C237/32 , C07C311/08 , C07C311/21 , C07D207/06 , C07D207/36 , C07D211/14 , C07D213/30 , C07D213/36 , C07D213/40 , C07D213/48 , C07D213/56 , C07D213/71 , C07D213/76 , C07D215/06 , C07D215/36 , C07D215/40 , C07D217/04 , C07D239/28 , C07D295/13 , C07D295/155 , C07D317/54 , C07D317/58 , C07D401/12 , C07D403/04 , C07D498/04 , C07D295/12 , A61K31/50 , C07D213/70
Abstract: The invention relates to amides of the general formula (I), which are inhibitors of enzymes, especially cysteine proteases.
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公开(公告)号:BR9909772A
公开(公告)日:2000-12-19
申请号:BR9909772
申请日:1999-04-19
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MULLER ACHIM , TREIBER HANS-JURG , 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 , A61K31/44
Abstract: Amides of the general formula Iand their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the meanings stated in the description, their preparation and use as calpain inhibitors.
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公开(公告)号:BR9909775A
公开(公告)日:2000-12-19
申请号:BR9909775
申请日:1999-04-19
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MULLER ACHIM , TREIBER HANS-JURG , 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 , C07C237/52
Abstract: Amides of the general formula Iand their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the following meanings:R1 [sic] can be C1-C6-alkyl, phenyl, naphthyl, quinolyl, pyridyl, pyrimidyl, pyridazyl, quinazolyl and quinoxalyl, where the rings can additionally be substituted by up to 2 radicals R4 [sic], andR2 [sic] is -(CH2)m-R8 [sic], where R8 [sic] can be phenyl, cyclohexyl- or indolyl and m=1 to 6, andX is a bond, -CH2-, -CH2CH2-, -CH=CH-, -C=C-, -CONH-, -SO2NH- [sic], and and [sic]R1-X [sic] together are also andR3 [sic] is hydrogen and CO-NR6R7 [sic],R4 [sic] is hydrogen, C1-C4-alkyl [sic], which is branched and unbranched, and -O-C1-C4-alkyl [sic];R5 [sic] is hydrogen, C1-C4-alkyl [sic], which is branched or unbranched, and -O-C1-C4-alkyl [sic];R6 [sic] is hydrogen, C1-C6-alkyl, which is branched and unbranched, andR7 [sic] is hydrogen, C1-C6-alkyl, which is branched or unbranched, andn is is [sic] a number 0, 1 or 2.
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公开(公告)号:BR9909773A
公开(公告)日:2000-12-19
申请号:BR9909773
申请日:1999-04-20
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MULLER ACHIM , TREIBER HANS-JURG , KNOPP MONIKA
IPC: C07D295/12 , A61K31/4402 , A61K31/4406 , A61K31/4418 , A61K31/4425 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5355 , A61K31/5375 , A61K31/5377 , A61K31/551 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P43/00 , C07D213/80 , C07D213/81 , C07D213/82 , C07D215/50 , C07D239/42 , C07D295/192 , C07D401/04 , C07D401/14 , C07D405/12 , C07D413/12 , C07D317/60 , C07D295/155 , A61K31/495 , A61K31/505 , A61K31/455 , A61K31/44
Abstract: Heterocyclically substituted amides of the general formula Iwherein the variables as defined in the specification are useful in pharmaceuticals for the treatment of diseases in which increased interleuken-1 levels occur.
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公开(公告)号:CZ9901833A3
公开(公告)日:1999-08-11
申请号:CZ183399
申请日:1997-11-11
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MULLER ACHIM , TREIBER HANS-JORG
IPC: A61K31/16 , A61K31/166 , A61K31/18 , A61K31/4045 , A61K31/435 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61P9/10 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/28 , A61P27/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07C233/76 , C07C235/42 , C07C235/46 , C07C235/58 , C07C235/60 , C07C235/84 , C07C237/42 , C07C311/08 , C07C311/21 , C07C317/44 , C07C323/42 , C07C323/60 , C07D209/14 , C07D209/16 , C07D213/30 , C07D213/56 , C07D213/71 , C07D213/82 , C07D215/36 , C07D215/14
CPC classification number: C07D213/82 , C07C233/76 , C07C235/42 , C07C235/46 , C07C235/60 , C07C235/84 , C07C237/42 , C07C311/21 , C07C317/44 , C07C323/42 , C07C323/60 , C07C2601/14 , C07D209/16 , C07D215/36
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