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：WO1997022621A2

公开(公告)日：1997-06-26

申请号：PCT/EP1996005518

申请日：1996-12-11

Applicant: BASF AKTIENGESELLSCHAFT ,  AMBERG, Wilhelm ,  BARLOZZARI, Teresa ,  BERNARD, Harald ,  BUSCHMANN, Ernst ,  HAUPT, Andreas ,  HEGE, Hans-Guenther ,  JANSSEN, Bernd ,  KLING, Andreas ,  LIETZ, Helmut ,  RITTER, Kurt ,  ULLRICH, Martina ,  WEYMANN, Jürgen ,  ZIERKE, Thomas

Inventor： BASF AKTIENGESELLSCHAFT

IPC: C07K07/06

CPC classification number: A61K38/08

Abstract: Novel peptides of the following formula (I): R R N-CHX-CO-A-B-D-E-(G)s-K in which R , R , A, B, D, E, G, K, X, and s have the meanings stated in the description, and the preparation thereof are described. The novel peptides have an antineoplastic effect.

Abstract translation: 下式（I）的新肽：R 1 R 2 N-CHX-CO-ABDE-（G）sK，其中R 1，R 2，A，B，D，E， G，K，X和S具有说明书中所述的含义，并描述其制备。 新型肽具有抗肿瘤作用。