Title:
【発明の名称】エンドセリン・レセプター・アンタゴニスト
Document Type and Number:
Japanese Patent JPH09504302
Kind Code:
A
Abstract:
PCT No. PCT/EP94/03418 Sec. 371 Date Apr. 30, 1996 Sec. 102(e) Date Apr. 30, 1996 PCT Filed Oct. 17, 1994 PCT Pub. No. WO95/12611 PCT Pub. Date May 11, 1995The present invention provides novel compounds represented by the general formula I: (I) wherein R1 is a straight or branched lower alkyl, a cycloalkyl-lower alkyl, an aryl-lower alkyl, a cycloalkyl, an aryl an aryl-cycloalkyl, lower alkoxy, an aryloxy, or a heteroaryl; R2 is hydrogen, a straight or branched lower alkyl, a cycloalkyl, or a cycloalkyl-lower alkyl; R3 and R3' are each the same or different and each is hydrogen atom, a straight or branched lower alkyl, a cycloalkyl, an aryl-lower alkyl, an aryl, or a heteroaryl; or R3 and R3' together form a ring structure; R3'' is hydrogen, lower alkyl or an aryl; or R2 and R3'' together form a lower alkylene group -(CH2)n- wherein n is an integer of 1, 2 or 3; or R2 and R3'' together form a group represented by the formula: -(CH2)p-Ar- or -Ar-(CH2)p-, respectively, wherein p is zero or an integer of 1 or 2, and Ar is an arylene or heteroarylene; C(=X) is C(=O), C(=S), C(=NH), C(=N-lower alkyl); C=NH-OH, or CH2; Y is a direct bond, -NH-, a lower alkyl-N<, an oxygen atom, or methylene; or C(=X) is CHOH and Y is a direct bond or methylene; R4 is -(CH2)s-Ar' wherein s is zero or an integer of 1, 2 or 3; and Ar' is an aryl, or a heteroaryl; and R5 is carboxy, substituted or unsubstituted carboxamide, PO(OH)2, tetrazole, CH2OH, CN, or hydrogen; and salts thereof.
Inventors:
Hideyuki Saiga
Toshiki Murata
Thomas Piterna
Freey, thomas
Svenson, Rene Day.
Uraide Yoshihiro
Yamaki Yuuki
Toshikazu Okada
Toshiki Murata
Thomas Piterna
Freey, thomas
Svenson, Rene Day.
Uraide Yoshihiro
Yamaki Yuuki
Toshikazu Okada
Application Number:
JP51298295A
Publication Date:
April 28, 1997
Filing Date:
October 17, 1994
Export Citation:
Assignee:
Nippon Ciba Geigy Co., Ltd.
International Classes:
A61K31/40; A61K31/403; A61K31/404; A61K31/405; A61K31/44; A61K31/4427; A61K31/4433; A61K31/47; A61K31/472; A61K38/00; A61K38/04; A61P1/04; A61P3/08; A61P9/00; C07D215/50; A61P9/10; A61P9/12; A61P11/00; A61P27/02; C07D209/16; C07D209/18; C07D209/20; C07D209/26; C07D217/26; C07D261/08; C07D401/06; C07D409/06; C07K5/02; C07K5/06; C07K5/065; C07K5/078; (IPC1-7): C07D209/16; A61K31/40; A61K31/44; A61K31/47; A61K38/00; C07D209/18; C07D209/20; C07D215/50; C07D217/26; C07D261/08; C07D401/06; C07D409/06; C07K5/065; C07K5/078
Domestic Patent References:
| JPS62117566A | 1987-05-29 | |||
| JP3058434B | ||||
| JPS5841567A | 1983-03-10 | |||
| JPS486593A | ||||
| JPS5623142B2 | 1981-05-29 | |||
| JP48092791B | ||||
| JPS58133260A | 1983-08-08 |
Attorney, Agent or Firm:
Takashi Ishida (3 others)