公开(公告)号：BG63382B1

公开(公告)日：2001-12-31

申请号：BG10348599

申请日：1999-06-11

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  MOELLER ACHIM ,  TREIBER HANS-JOERG

IPC: C07D295/12 ,  A61K31/16 ,  A61K31/166 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4164 ,  A61K31/4402 ,  A61K31/4409 ,  A61K31/4439 ,  A61K31/4453 ,  A61K31/4468 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/496 ,  A61K31/498 ,  A61K31/5355 ,  A61K31/5375 ,  A61K31/5377 ,  A61P9/10 ,  A61P25/00 ,  A61P25/08 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07C233/87 ,  C07C237/22 ,  C07C237/36 ,  C07C237/42 ,  C07C311/19 ,  C07C311/21 ,  C07D211/58 ,  C07D213/56 ,  C07D215/12 ,  C07D215/36 ,  C07D215/48 ,  C07D233/54 ,  C07D233/61 ,  C07D241/42 ,  C07D241/44 ,  C07D295/02 ,  C07D295/13 ,  C07D333/38 ,  C07D333/56 ,  C07D333/60 ,  C07D401/12 ,  C07D521/00 ,  C07K5/02

Abstract: The compounds are administered in medicine. They have the formula wherein R1, R2, R3, R4, X and n have the meanings given in the description. The invention also relates to their preparation. 14 claims

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

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.

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

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.

公开(公告)号：CZ9902084A3

公开(公告)日：2000-09-13

申请号：CZ208499

申请日：1997-11-28

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  MOELLER ACHIM ,  TREIBER HANS-JOERG

IPC: A61K31/165 ,  A61K31/395 ,  A61P9/10 ,  A61P25/16 ,  A61P25/28 ,  A61P35/00 ,  C07C233/87 ,  C07C311/21 ,  C07D215/36 ,  C07D241/42 ,  C07D295/02 ,  C07D295/12

公开(公告)号：BG103831A

公开(公告)日：2000-07-31

申请号：BG10383199

申请日：1999-10-22

Applicant: BASF AG

Inventor： LERCHI JENS ,  MOELLER ACHIM ,  SCHMIDT RALF-MICHAEL ,  SCHIFFER HELMUT ,  RABE UDO ,  CONRAD UDO

IPC: A01H5/00 ,  C07K16/44 ,  C12N1/21 ,  C12N5/10 ,  C12N15/09 ,  C12N15/13 ,  C12N15/82 ,  G06Q50/20 ,  A01N63/00

Abstract: The method for forming tolerance to herbicides is effected by expression of herbicidebinding antibody in the plants. 27 claims

公开(公告)号：BG103485A

公开(公告)日：2000-01-31

申请号：BG10348599

申请日：1999-06-11

Applicant: BASF AG

Inventor： LUBISCH WILFRIED ,  MOELLER ACHIM ,  TREIBER HANS-JOERG

IPC: C07D295/12 ,  A61K31/16 ,  A61K31/166 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4164 ,  A61K31/4402 ,  A61K31/4409 ,  A61K31/4439 ,  A61K31/4453 ,  A61K31/4468 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/496 ,  A61K31/498 ,  A61K31/5355 ,  A61K31/5375 ,  A61K31/5377 ,  A61P9/10 ,  A61P25/00 ,  A61P25/08 ,  A61P25/28 ,  A61P35/00 ,  A61P43/00 ,  C07C233/87 ,  C07C237/22 ,  C07C237/36 ,  C07C237/42 ,  C07C311/19 ,  C07C311/21 ,  C07D211/58 ,  C07D213/56 ,  C07D215/12 ,  C07D215/36 ,  C07D215/48 ,  C07D233/54 ,  C07D233/61 ,  C07D241/42 ,  C07D241/44 ,  C07D295/02 ,  C07D295/13 ,  C07D333/38 ,  C07D333/56 ,  C07D333/60 ,  C07D401/12 ,  C07D521/00 ,  C07K5/02

Abstract: The ketobenzamides have the formula where R1, R2, R3, R4, X & n have the meanings listed in the description. The invention also relates to the preparation of the above compounds which are applied in medicine. 14 claims

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

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