公开(公告)号：CA2322541A1

公开(公告)日：1999-09-10

申请号：CA2322541

申请日：1999-02-25

Applicant: BASF AG

Inventor： HERGENRODER STEFAN ,  RASCHACK MANFRED ,  RIECHERS HARTMUT ,  UNGER LILIANE ,  KLINGE DAGMAR ,  AMBERG WILHELM ,  JANSEN ROLF

IPC: C07D251/22 ,  A61K31/192 ,  A61K31/216 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/53 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07C59/66 ,  C07C59/68 ,  C07C69/734 ,  C07D213/63 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D405/12 ,  C07D491/048 ,  C07D403/12 ,  C07D213/64

Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein R1-R6, Q, W, X, Y and Z have the meanings given in the description. The novel compounds are suitable for combating diseases.

公开(公告)号：CA2321182A1

公开(公告)日：1999-08-26

申请号：CA2321182

申请日：1999-02-05

Applicant: BASF AG

Inventor： KLINGE DAGMAR ,  KLING ANDREAS ,  AMBERG WILHELM ,  UNGER LILIANE ,  RIECHERS HARTMUT ,  JANSEN ROLF ,  RASCHACK MANFRED ,  HERGENRODER STEFAN

IPC: A61K31/505 ,  A61K31/506 ,  A61P5/14 ,  A61P9/02 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/46 ,  C07D239/52 ,  C07D239/60 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D239/36

Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the following meanings; R1= tetrazole or a group (1); R = a radical OR7(2), (3), a 5-membe red heteroaromatic bonded by a nitrogen atom such a pyrrolyl, pyrazolyl, imidazolyl and trizolyl; R2, R3 = hydrogen, hydroxy, NH2, NH(C1-C4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkinyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy, C1-C4-halogen alkyl, C1-C4-alkoxy, C1-C4-halogen alkoxy or C1-C4-alkythio; X = halogen, C1-C4-halogen alkyl, hydroxy; R4 and R5 = phenyl or naphthyl, C3-C7-cycloalkyl, phenyl or naphthyl which are bonded in ortho position by a direct bond, a methylene, ethylene or ethenylene group, an oxygen or sulfur atom or an SO2-NH or an N-alkyl group or a 5-membered or 6-membered heteroaromatic; R6 = hydrogen, phenyl or naphthyl, a five or six-membered heteroaromatic, C1-C8-alkyl, C3-C6-alkenyl, C3-C6-alkinyl or C3-C8-cycloalkyl, whereby said radicals can be substituted once or many times, with the proviso that R6 can only stand for hydrogen if Z does not represent a single bond; Z = sulfur, oxygen or a single bond, in addition to the physiologically compatible salts and the enantiomeric-pure and diastereomeric-pure forms. The novel compounds are suitable for combating diseases, especially as endothelin antagonists.

公开(公告)号：CA2308746A1

公开(公告)日：1999-05-27

申请号：CA2308746

申请日：1998-11-04

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  UNGER LILIANE ,  HILLEN HEINZ ,  HERGENRODER STEFAN ,  RASCHACK MANFRED ,  JANSEN ROLF

IPC: C07D249/12 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/433 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D231/20 ,  C07D233/70 ,  C07D261/12 ,  C07D263/38 ,  C07D271/06 ,  C07D271/10 ,  C07D273/01 ,  C07D275/02 ,  C07D275/03 ,  C07D277/20 ,  C07D277/32 ,  C07D277/34 ,  C07D277/60 ,  C07D277/68 ,  C07D285/00 ,  C07D285/08 ,  C07D285/12 ,  C07D291/04 ,  C07D413/12 ,  C07D417/12

Abstract: The invention relates to carboxylic acid derivatives of formula (I) wherein A represents NR8R9, azido, OR10, SR10 or C1-C4 alkyl, R1 represents tetrazole or a group (1), wherein R has the following meaning: a) a radical OR5; b) a 5membered heteroaromat bonded by a nitrogen atom; c) a group (2); d) a radical (3), and the remaining substituents have the meanings given in the description. The invention also relates to production of the inventive derivatives and to their use as endothelin receptor antagonists.

公开(公告)号：AU9533398A

公开(公告)日：1999-03-22

申请号：AU9533398

申请日：1998-08-24

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  HERGENRODER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: A61K31/421 ,  A61K31/426 ,  A61K31/428 ,  A61K31/496 ,  A61K31/505 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D239/34 ,  C07D239/52 ,  C07D263/38 ,  C07D277/20 ,  C07D277/34 ,  C07D277/68 ,  C07D409/12 ,  C07D239/04

Abstract: The invention relates to carboxylic acid derivatives of formula (I) wherein the radicals are defined in the description, and to the use of these derivatives as ETA/ETB endothelin-receptor antagonists.

公开(公告)号：CZ9800641A3

公开(公告)日：1998-09-16

申请号：CZ64198

申请日：1996-08-29

Applicant: BASF AG

Inventor： AMBERG WILHELM DR ,  KLING ANDREAS DR ,  KLINGE DAGMAR DR ,  REICHERS HARTMUT DR ,  UNGER LILIANE DR ,  RASCHACK MANFRED DR ,  HERGENRODER STEFAN ,  ELGER BERND ,  SCHULT SABINE DR

IPC: C07D317/02 ,  A61K31/00 ,  A61K31/19 ,  A61K31/192 ,  A61K31/34 ,  A61K31/341 ,  A61K31/343 ,  A61K31/35 ,  A61K31/352 ,  A61K31/357 ,  A61K31/36 ,  A61K31/435 ,  A61K31/44 ,  A61K31/505 ,  A61P9/00 ,  A61P9/08 ,  C07C53/134 ,  C07C57/30 ,  C07C57/32 ,  C07C57/38 ,  C07C59/64 ,  C07C69/616 ,  C07C69/734 ,  C07C255/00 ,  C07D213/55 ,  C07D213/64 ,  C07D221/04 ,  C07D239/26 ,  C07D239/34 ,  C07D239/52 ,  C07D239/70 ,  C07D257/04 ,  C07D307/79 ,  C07D317/50 ,  C07D317/60 ,  C07D319/02 ,  C07D319/18

CPC classification number: C07D213/64 ,  C07C57/30 ,  C07C57/38 ,  C07C59/64 ,  C07C69/616 ,  C07C69/734 ,  C07D213/55 ,  C07D221/04 ,  C07D239/26 ,  C07D239/34 ,  C07D239/52 ,  C07D239/70 ,  C07D307/79 ,  C07D317/60 ,  C07D319/18

公开(公告)号：CZ64198A3

公开(公告)日：1998-09-16

申请号：CZ64198

申请日：1996-08-29

Applicant: BASF AG

Inventor： AMBERG WILHELM DR ,  KLING ANDREAS DR ,  KLINGE DAGMAR DR ,  REICHERS HARTMUT DR ,  UNGER LILIANE DR ,  RASCHACK MANFRED DR ,  HERGENRODER STEFAN ,  ELGER BERND ,  SCHULT SABINE DR

IPC: C07D317/02 ,  A61K31/00 ,  A61K31/19 ,  A61K31/192 ,  A61K31/34 ,  A61K31/341 ,  A61K31/343 ,  A61K31/35 ,  A61K31/352 ,  A61K31/357 ,  A61K31/36 ,  A61K31/435 ,  A61K31/44 ,  A61K31/505 ,  A61P9/00 ,  A61P9/08 ,  C07C53/134 ,  C07C57/30 ,  C07C57/32 ,  C07C57/38 ,  C07C59/64 ,  C07C69/616 ,  C07C69/734 ,  C07C255/00 ,  C07D213/55 ,  C07D213/64 ,  C07D221/04 ,  C07D239/26 ,  C07D239/34 ,  C07D239/52 ,  C07D239/70 ,  C07D257/04 ,  C07D307/79 ,  C07D317/50 ,  C07D317/60 ,  C07D319/02 ,  C07D319/18

Abstract: PCT No. PCT/EP96/03793 Sec. 371 Date Feb. 24, 1998 Sec. 102(e) Date Feb. 24, 1998 PCT Filed Aug. 29, 1996 PCT Pub. No. WO97/09294 PCT Pub. Date Mar. 13, 1997Carboxylic acid derivatives of the formula I here R1 is a tetrazole [sic], nitrile [sic], a group COOH or a radical which can be hydrolyzed to COOH, and the other substituents have the meaning explained in the description.

公开(公告)号：NZ502660A

公开(公告)日：2002-02-01

申请号：NZ50266098

申请日：1998-08-24

Applicant: BASF AG

Inventor： RASCHACK MANFRED ,  UNGER LILIANE ,  HERGENRODER STEFAN ,  AMBERG WILHELM ,  JANSEN ROLF ,  KLINGE DAGMAR ,  RIECHERS HARTMUT

IPC: A61K31/421 ,  A61K31/426 ,  A61K31/428 ,  A61K31/496 ,  A61K31/505 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D239/34 ,  C07D239/52 ,  C07D263/38 ,  C07D277/20 ,  C07D277/34 ,  C07D277/68 ,  C07D409/12 ,  C07D239/04 ,  A61K31/517 ,  A61K31/519 ,  C07D239/70 ,  C07D491/048

Abstract: A carboxylic acid derivative or a physiologically tolerated salts or enantiomerically pure forms thereof has the formula (I) wherein: R is tetrazole or -C(O)-R1; R1 is OR7, cycloalkyl, alkyl, or optionally substituted CH2-phenyl, alkenyl, alkynyl or phenyl; R4 and R5 are independently optionally substituted phenyl or naphthoyl or phenyl or naphthyl which are linked together in the ortho positions by a direct linkage, methylene, ethylene or ethenylene, oxygen, sulphur, SO2, NH or N-alkyl; R6 is H, or optionally substituted alkyl, alkenyl, alkynyl, phenyl, naphthyl, a five or six membered heteroaromatic system comprising one to three nitrogens and/or sulphur or oxygen or cycloalkyl; Z is sulphur or oxygen; B is alkylene; Het is a heterocyclic radical of formula Ia or Ib'; R2 is H, OH, N(R')2, halo, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, haloalkoxy, alkylthio or CR2 is linked to C10 to form a 5 or 6 membered ring defined below or if Het is a 5 membered ring, CR2 together with CR3 can be an optionally substituted 5- or 6- membered alkenyl or alkylenyl ring; X and Y are independently nitrogen or methane; W is nitrogen or CR10; R10 is H, halo or alkyl or CR10 forms together with CR2 or CR3 an optionally substituted 5 or 6 membered alkylene or alkenylene ring wherein one or more of the methylene groups can be replaced by oxygen, sulphur or NR'; R3 is H, OH, N(R')2, halo, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, halolkoxy, alkylthio or CR3 is linked to C10 to form a 5 or 6 membered ring defined above; R' is H or alkyl; T is O, S or NR8 and R8 is alkyl. A pharmaceutical composition thereof is useful as an endothelin receptor antagonist.

公开(公告)号：SK832001A3

公开(公告)日：2001-11-06

申请号：SK832001

申请日：1999-08-07

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  HERGENRODER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: C07D251/22 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K45/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D251/52 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D491/048 ,  C07D495/04 ,  A61K31/503

Abstract: The invention relates to new carboxylic acid derivatives of the formula (I), where the substituents have the meaning given in the description, their production and their use as endothelin-receptor antagonists.

公开(公告)号：ID27965A

公开(公告)日：2001-05-03

申请号：ID20010326

申请日：1999-08-07

Applicant: BASF AG

Inventor： AMBERG WIHELM ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  HERGENRODER STEFAN ,  RASCHAK MANFRED ,  UNGER LILIANE

IPC: C07D251/22 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K45/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D251/52 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D491/048 ,  C07D495/04

Abstract: The invention relates to new carboxylic acid derivatives of the formula (I), where the substituents have the meaning given in the description, their production and their use as endothelin-receptor antagonists.

公开(公告)号：BG104022A

公开(公告)日：2001-04-30

申请号：BG10402299

申请日：1999-12-16

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  HERGENRODER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: C07D251/16 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61P7/02 ,  A61P9/02 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/08 ,  A61P13/12 ,  A61P25/06 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07C247/12 ,  C07D213/68 ,  C07D237/14 ,  C07D237/16 ,  C07D239/34 ,  C07D239/52 ,  C07D239/56 ,  C07D239/60 ,  C07D239/70 ,  C07D239/80 ,  C07D239/95 ,  C07D241/18 ,  C07D251/22 ,  C07D251/34 ,  C07D251/52 ,  C07D253/06 ,  C07D403/12 ,  C07D491/048 ,  C07C235/12 ,  C07C233/63 ,  C07C229/22 ,  C07C233/47 ,  C07C235/34

Abstract: The invention relates to carboxylic acid derivatives of formula wherein the constituents have the meaning given in the description. The invention also relates to the production of said derivatives, and to their use as endothelin receptor antagonists. 10 claims