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公开(公告)号:PL343467A1
公开(公告)日:2001-08-13
申请号:PL34346799
申请日:1999-04-19
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 , C07D239/44 , 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:NO20013409D0
公开(公告)日:2001-07-10
申请号:NO20013409
申请日:2001-07-10
Applicant: BASF AG
Inventor: STEINLER GERD , SCHELLHAAS KURT , LUBISCH WILFRIED , HOLZENKAMP UTA , STARCK DOROTHEA , KNOPP MONIKA , SZABO LASZLO , EMLING FRANZ , GARCIA-LADONA FRANCISCO-JAVIER , HOFMANN HANS PETER , UNGER LILIANE
IPC: C07D495/04 , A61K31/505 , A61K31/519 , A61P9/10 , C07D495/14 , A61K
Abstract: Use of pyrimidine derivatives of the formula Iwhere the substituents are as defined in the description, and of their physiologically tolerated salts for producing medicaments for the prophylaxis and treatment of cerebral ischemia and strokes.
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公开(公告)号:BG104856A
公开(公告)日:2001-05-31
申请号:BG10485600
申请日:2000-10-13
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS-JOERG , 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: The invention relates to benzamides of general formula (I) and their tautomeric forms, as well as to possible enantiomeric and diastereomeric forms, to their E and Z forms and to possible physiologically compatible salts, where the variables R1, R2, R3, A and B have the meanings given in the description. The invention also relates to their use as inhibitors of cysteine proteases. 21 claims
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公开(公告)号:SK14512000A3
公开(公告)日:2001-04-09
申请号:SK14512000
申请日:1999-04-20
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOLLER ACHIM , TREIBER HANS-JORG , 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:ID26728A
公开(公告)日:2001-02-01
申请号:ID20002133
申请日:1999-04-19
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOLLER ACHIM , TREIBER HANS JORG , 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 , C07D215/24 , 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:ID26402A
公开(公告)日:2000-12-21
申请号:ID20002112
申请日:1999-04-19
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOLLER ACHIM , TREIBER HANS-JORG , 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 , C07C235/82 , A61K31/195 , A61K31/44 , A61K31/505 , A61K31/19
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: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:NO20005266L
公开(公告)日:2000-10-19
申请号:NO20005266
申请日:2000-10-19
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 , A61K31/195 , 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 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:NO20005264D0
公开(公告)日:2000-10-19
申请号:NO20005264
申请日:2000-10-19
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 , C07D
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:NO20005263A
公开(公告)日:2000-10-19
申请号:NO20005263
申请日:2000-10-19
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS-JOERG , KNOPP MONIKA
IPC: C07D295/08 , A61K31/166 , A61K31/27 , 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 , C07D213/82 , C07D295/14 , C07D295/155 , C07D237/00 , C07D239/00
CPC classification number: C07D213/82 , A61K31/195 , A61K31/5375 , C07C229/38 , C07C237/22 , C07C237/32 , C07C2601/14 , C07D295/155
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