公开(公告)号：WO9809953A3

公开(公告)日：1998-10-29

申请号：PCT/EP9704688

申请日：1997-09-02

Applicant: BASF AG ,  AMBERG WILHELM ,  JANSEN ROLF ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

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

IPC: A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61P9/04 ,  A61P9/08 ,  A61P9/12 ,  A61P43/00 ,  C07C59/66 ,  C07C69/734 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D491/04 ,  C07D491/048

CPC classification number: C07D239/70 ,  C07C59/66 ,  C07C69/734 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D491/04

Abstract: Carboxylic acid derivatives have the formula (I), in which R1 stands for tetrazole or a group (a); R2 stands for hydrogen, hydroxy, NH¿2?, NH(C1-c4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkinyl, C1-C4-halogenalkyl, C1-C4-alkoxy, C1-C4-halogenalkoxy or C1-C4-alkylthio, or CR?2¿ is linked with CR10, as indicated below, into a 5- or 6-membered ring; X stands for nitrogen or methine; Y stands for nitrogen or methine; Z stands for nitrogen or CR10, wherein R10 is hydrogen or C¿1?-C4-alkyl or CR?10¿ forms together with CR?2 or CR3¿ an optionally substituted 5- or 6-membered alkylene or alkenylene ring, and wherein one or more methylene groups can be substituted by oxygen, sulphur, -NH or -N(C¿1?-C4-alkyl); R?3¿ stands for hydrogen, hydroxy, NH¿2?, NH(C1-C4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkinyl, C1-C4-hydroxyalkyl, C1-C4-halogenalkyl, C1-C4-alkoxy, C1-C4-halogenalkoxy, C1-C4-alkylthio; or CR?3¿ is linked to CR10 as indicated above into a 5- or 6-membered ring, R?4 and R5¿ (which may be identical or different) stand for optionally substituted phenyl or naphthyl, or for phenyl or naphthyl which are linked to each other at the ortho-position by a direct bond, a methylene, ethylene or ethenylene group, an oxygen or sulphur atom or an SO¿2?, NH or N-alkyl group; optionally substituted C3-C8-cycloalkyl; R?6¿ stands for optionally substituted C¿3?-C8-cycloalkyl; optionally substituted phenyl or naphthyl, a 5- or 6-membered, optionally substituted heteroaromatic compound containing one to three nitrogen atoms and/or one sulphur or oxygen atom; W stands for sulphur or oxygen; Q is a spacer with a length that corresponds to a C2-C4 chain. Also disclosed are the physiologically tolerable salts of these compounds, as well as their pure enantiomer and diastereoisomer forms, their preparation and use as mixed ETA/ETB-receptor antagonists.

公开(公告)号：WO9923078A3

公开(公告)日：1999-09-10

申请号：PCT/EP9806571

申请日：1998-10-16

Applicant: BASF AG ,  AMBERG WILHELM ,  JANSEN ROLF ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61P9/02 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/36 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D401/12 ,  C07D403/12 ,  C07D491/048

CPC classification number: C07D239/36 ,  C07D239/52 ,  C07D239/60 ,  C07D401/12

Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein R represents a group (a) or (b), R and R being the same or different and having the following meaning: hydrogen; on the condition that R and R are not hydrogen at the same time, C1-C8-alkyl, C3-C8-cycloalkyl, C3-C8-alkenyl, C3-C8-alkinyl, benzyl, phenyl, naphthyl, optionally substituted; or R and R together form an optionally substituted C3-C7-alkylene chain which is closed in a ring and in which an alkylene group can be replaced by oxygen, sulphur or nitrogen; or R and R together form an optionally substituted C3-7-alkylene chain or C3-C7-alkenylene chain which is closed in a ring and to which an optionally substituted phenyl ring is anellated. The other substituents have the meanings given in the description. The invention also relates to the production of the novel carboxylic acid derivatives and to their use as endothelin receptor antagonists.

Abstract translation: 本发明涉及式（I）式的羧酸衍生物，其中R <6>是基团（a）或（b）具有R <13>和R <14>可以相同或不同，且定义如下; 前提氢是R <13>和R <14>决不能同时为氢，C1-C8烷基，C3-C8环烷基，C3-C8链烯基，C3-C8炔基，苄基，苯基，萘基 中，每个任选地被取代，或R <13>和R <14>一起形成，以形成闭环，其中的亚烷基可以被氧，硫或氮，或者R来代替任选取代的C3-C7亚烷基链<13> 且R <14>一起形成环的闭合，任选取代的C 3 -C 7 - 亚烷基或C 3 -C 7 - 亚烯基链，其中苯基环稠合任选被取代; 并且其中，所述其它取代基是在说明书，用作内皮素受体拮抗剂的制备所述的相同。

公开(公告)号：NO313519B1

公开(公告)日：2002-10-14

申请号：NO992976

申请日：1999-06-17

Applicant: BASF AG

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

IPC: C07D253/06 ,  A61K31/495 ,  A61K31/50 ,  A61K31/505 ,  A61K31/53 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/08 ,  C07D237/14 ,  C07D237/16 ,  C07D241/18 ,  C07D253/07 ,  C07D253/075 ,  C07D253/10 ,  C07D403/12 ,  C07D491/04

Abstract: The present invention relates to carboxylic acid derivatives of the formula Iwhere the substituents have the meanings explained in the description, and to preparation and use as endothelin receptor antagonists.

公开(公告)号：HU0100054A2

公开(公告)日：2002-02-28

申请号：HU0100054

申请日：1998-10-16

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  HERGENROEDER STEFAN ,  JANSEN ROLF ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61P9/02 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/36 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D401/12 ,  C07D403/12 ,  C07D491/048

Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the meaning as commented in the description. It also relates to the production and use of same as endothelin receptor antagonists.

公开(公告)号：HRP960400B1

公开(公告)日：2001-08-31

申请号：HRP960400

申请日：1996-09-03

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  UNGER LILIANE ,  RASCHACK MANFRED ,  HERGENROEDER STEFAN ,  ELGER BERND ,  SCHULT SABINE

IPC: A61K31/00 ,  A61K31/19 ,  A61K31/192 ,  A61K31/34 ,  A61K31/341 ,  A61K31/343 ,  C07D317/02 ,  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：PL342806A1

公开(公告)日：2001-07-02

申请号：PL34280699

申请日：1999-02-25

Applicant: BASF AG

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

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 ,  C07D239/42 ,  C07D239/47 ,  C07D213/64 ,  A61K31/44

Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein R -R , 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：BG63202B1

公开(公告)日：2001-06-29

申请号：BG10277098

申请日：1998-09-15

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  BAUMANN ERNST ,  UNGER LILIANE ,  RASCHACK MANFRED ,  HERGENROEDER STEFAN ,  SCHULT SABINE

IPC: A61K31/00 ,  A61K31/47 ,  A61K31/505 ,  A61P9/00 ,  A61P9/12 ,  A61P13/00 ,  A61P13/12 ,  C07D215/22 ,  C07D215/227 ,  C07D239/34 ,  C07D239/60 ,  C07D401/12 ,  C07D403/12

Abstract: The invention relates to derivatives of caboxylic acids with the formula where the radicals have the meanings listed in the description well as to their preparation and to application as medicamentous forms. 10 claims

公开(公告)号：CZ20010437A3

公开(公告)日：2001-05-16

申请号：CZ20010437

申请日：1999-08-07

Applicant: BASF AG

Inventor： AMBERG WILHEM ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: A61K31/505 ,  A61P9/00 ,  C07D239/34 ,  C07D239/52 ,  C07D239/70 ,  C07D403/12

公开(公告)号：PL340871A1

公开(公告)日：2001-03-12

申请号：PL34087198

申请日：1998-10-16

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61P9/02 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/36 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D401/12 ,  C07D403/12 ,  C07D491/048 ,  A61P9/04

Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the meaning as commented in the description. It also relates to the production and use of same as endothelin receptor antagonists.

公开(公告)号：AT197448T

公开(公告)日：2000-11-11

申请号：AT96930125

申请日：1996-08-29

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  UNGER LILIANE ,  RASCHACK MANFRED ,  HERGENROEDER STEFAN ,  ELGER BERND ,  SCHULT SABINE

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.