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公开(公告)号:CZ20003844A3
公开(公告)日:2001-01-17
申请号:CZ20003844
申请日:1999-04-20
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS-JOERG , KNOPP MONIKA
IPC: A61K31/435 , A61K31/44 , A61K31/495 , A61K31/5375 , A61P25/28 , C07D207/09 , C07D213/56 , C07D237/04 , C07D265/28 , C07D401/02 , C07D413/00
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公开(公告)号:NO20005929D0
公开(公告)日:2000-11-23
申请号:NO20005929
申请日:2000-11-23
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOELLER ACHIM , TREIBER HANS-JOERG , KNOPP MONIKA
IPC: C07D215/08 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/4427 , A61K31/4433 , A61K31/4439 , A61K31/4545 , A61K31/47 , A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/5377 , A61P9/08 , A61P9/10 , A61P13/12 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/28 , A61P27/12 , A61P29/00 , A61P35/00 , A61P35/04 , A61P43/00 , C07D209/14 , C07D209/44 , C07D215/06 , C07D217/06 , C07D217/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D409/14 , C07D
Abstract: Fused heterocyclic-substituted (hetero)aromatic carboxylic acid alkylamides (I) are new. Amides of formula (I) and their tautomers, enantiomers, diastereomers, E- and Z-isomers and salts are new. [Image] A : fused cyclic group such as 1,2,3,4-tetrahydroquinolin-1-yl, 1,2,3,4-tetrahydroisoquinolin-2-yl, isoindolin-2-yl or indolin-1-yl, all substituted by (R 4) n in the benzene ring; B' : phenyl, naphthyl, pyridyl, pyrimidyl, pyrazyl, pyridazyl, quinolyl, quinazyl, quinoxalyl, thienyl, benzothienyl, benzofuranyl, furanyl or indolyl; R 1H, alkyl, alkoxy, alkenyl, alkynyl, alkylphenyl, alkenylphenyl, alkynylphenyl, OH, halo, CF 3, NO 2, NH 2, CN, COOH, COOT, NHC(O)T, NHC(O)Ph, C(O)NHR 11, NHSO 2T, NHSO 2Ph, SO 2T or SO 2Ph; T : 1-4C alkyl; R 2alkyl (optionally substituted by phenyl, cyclohexyl, pyridyl, thienyl, indolyl or naphthyl, themselves all optionally substituted by 1 or 2 R 1 groups); R 3H, COOR 5 or C(O)Z; Z : NR 6R 7, 4-(R 15)-piperazino, R 15-substituted pyrrolidino or R 15-substituted piperidino; R 4H, (CH 2) mNR 8R 9, (CH 2) mQ or O(CH 2) mQ'; Q : 4-(R 8)-piperazino, 4-(R 8)-homopiperazino, R 15-substituted pyrrolidino, R 15-substituted piperidino, morpholino, 4-(R 8)-1-piperidinyl or R 8-substituted hexamethyleneimino; Q' : 4-(R 8)-piperazino, 4-(R 8)-homopiperazino, R 8-substituted pyrrolidino, R 15-substituted piperidino, morpholino or 4-(R 8)-1-piperidinyl; R 5, R 8, R 9alkyl (optionally substituted by phenyl, itself optionally substituted by 1 or 2 R 10); R 6H or alkyl; R 7H or alkyl (optionally substituted by phenyl or pyridyl (both optionally substituted by R 10) or by 4-(R 8)-piperazino, 4-(R 8)-homopiperazino, R 15-substituted pyrrolidino, R 15-substituted piperidino, R 8-substituted 1-imidazolyl, morpholino, 4-(R 8)-1-piperidinyl or -(CH 2) oNR 8R 9); R 10H, T, OT, OH, halo, CF 3, NO 2, NH 2, CN, CONH 2, COOH, COOT, NHC(O)T, NHC(O)Ph, NHSO 2T, NHSO 2Ph, SO 2T or SO 2Ph; R 11H or alkyl; R 15H or as R 8; m : 1-6; n : 0-2; o : 0-4; unless specified otherwise alkyl moieties have 1-6C and alkenyl or alkynyl moieties 2-6C. ACTIVITY : Neuroprotective; spasmolytic; antiischemic; cytoprotective; cardiovascular; antitumor; antiinflammatory; antirheumatic. MECHANISM OF ACTION : Cystiene protease inhibitor; calpain inhibitor; cathepsin inhibitor; interleukin-1 antagonist. No results of biological activity tests are given, although test procedures are described.
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公开(公告)号:NO20005265A
公开(公告)日:2000-10-19
申请号:NO20005265
申请日:2000-10-19
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
CPC classification number: C07D295/096 , C07C233/78 , C07C235/42 , C07C237/34 , C07C311/21 , C07D213/56
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公开(公告)号:NO20005237D0
公开(公告)日:2000-10-18
申请号:NO20005237
申请日:2000-10-18
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOELLER ACHIM , KNOPP MONIKA , TREIBER HANS-JOERG
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 , C07D
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:AU2433800A
公开(公告)日:2000-08-01
申请号:AU2433800
申请日:1999-12-24
Applicant: BASF AG
Inventor: STEINER 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 , A61K31/495 , A61K31/55
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:CA2359253A1
公开(公告)日:2000-07-20
申请号:CA2359253
申请日:1999-12-24
Applicant: BASF AG
Inventor: EMLING FRANZ , GARCIA-LADONA FRANCISCO JAVIER , SZABO LASZLO , LUBISCH WILFRIED , SCHELLHAAS KURT , HOFMANN HANS-PETER , UNGER LILIANE , STEINER GERD , HOLZENKAMP UTA , STARCK DOROTHEA , KNOPP MONIKA
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 formul a (I), 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 an d strokes.
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公开(公告)号:AU3927199A
公开(公告)日:1999-11-08
申请号:AU3927199
申请日:1999-04-19
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , MOLLER ACHIM , TREIBER HANS-JORG , 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:CA2328438A1
公开(公告)日:1999-10-28
申请号:CA2328438
申请日:1999-04-19
Applicant: BASF AG
Inventor: KNOPP MONIKA , MOLLER ACHIM , TREIBER HANS-JORG , LUBISCH WILFRIED
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: The invention relates to amides of the general formula (I) and their tautomeric and isomeric forms, their possible enantiomeric and diastereomeric forms and possible physiologically compatible salts, where the variables have the meanings given in the description. The invention also relates to their production and their use as calpain inhibitors.
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公开(公告)号:CA2328435A1
公开(公告)日:1999-10-28
申请号:CA2328435
申请日:1999-04-19
Applicant: BASF AG
Inventor: TREIBER HANS-JORG , KNOPP MONIKA , MOLLER ACHIM , LUBISCH WILFRIED
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 , A61K31/19 , A61K31/195 , A61K31/44 , A61K31/505 , C07C237/52 , C07C235/82
Abstract: The invention relates to amides of general formula (I) and their tautomeric and isomeric forms, their possible enantiomeric and diastereomeric forms and possible physiologically compatible salts, where the variables have the following meanings: R1 is C1-C6 alkyl, phenyl, naphthyl, quinolyl, pyridyl, pyrimidyl, pyridazyl, quinazolyl and quinoxalyl, whereby the rings can still be substituted with up to 2 R4 rests; R2 is -(CH2)m-R8, where R8 is phenyl, cyclohexyl or indolyl and m is 1 to 6; X is a bond, -CH2-, -CH2CH2-, -CH=CH-, CC-, -CONH-, -, -SO2NH-, and R1-X together can also be formula (a), R3 is hydrogen and CO-NR6R7; R4 is hydrogen, branched or unbranched C1-C4 alkyl and O-C1-C4-alkyl; R5 is hydrogen, branched or unbranched C1-C4 alkyl and O-C1-C4-alkyl; R6 is hydrogen, branched or unbranched C1-C6 alkyl; R7 is hydrogen, branched or unbranched C1-C6 alkyl; and n is 0, 1 or 2. The amides of formula (I) are inhibitors of enzymes, especially cysteine proteases such as calpains (calcium dependent cysteine proteases) and their isoenzymes and cathepsins, such as B and L.
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公开(公告)号:CA2328430A1
公开(公告)日:1999-10-28
申请号:CA2328430
申请日:1999-04-19
Applicant: BASF AG
Inventor: TREIBER HANS-JORG , KNOPP MONIKA , MOLLER ACHIM , LUBISCH WILFRIED
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 claim 1. The invention also relates to their use as inhibitors of cysteine proteases.
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