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Title:
GEMINALLY SUBSTITUTED THIAHETEROCYCLIC CARBOXYLIC ACID AND DERIVATIVE THEREOF
Document Type and Number:
Japanese Patent JPH0320264
Kind Code:
A
Abstract:

NEW MATERIAL: A geminally substituted thiaheterocyclic carboxylic acid of formula I (A is an aryl which is, if required, substituted with at least one of a halogen, a lower alkoxy, a carboalkoxy, a lower alkyl, an alkylamino or a phenyl; X1 is CH2, NH; R1 is COOH, a COO-alkali metal, a COO-lower alkyl, CONHSO2R2 or a 5-tetrazolyl; R2 is a lower alkyl or an aryl; m is 0, 1 or 2; p is 2-5), a salt or a stereoisomer thereof.

EXAMPLE: 4-[3-(tetrahydro-3-phenyl-3-thienyl)propyl]benzene-acetic acid.S,S- dioxide.

USE: Useful as a thromboxane receptor antagonist useful for treating thrombosis. Also effective for diabetic retinopathy.

PREPARATION: A bromophenylalkanoic acid is subjected to reduction reaction with a borane in tetrahydrofuran and by several subsequent steps a compound of formula I is obtained.


Inventors:
FUIRITSUPU EMU SHIYAA
SUTEIIBUN II HOORU
Application Number:
JP14526190A
Publication Date:
January 29, 1991
Filing Date:
June 01, 1990
Export Citation:
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Assignee:
BRISTOL MYERS SQUIBB CO
International Classes:
A61K31/38; A61K31/381; A61K31/425; A61K45/00; A61P3/00; A61P7/02; A61P9/00; A61P9/08; A61P9/10; A61P11/08; A61P13/02; A61P15/00; A61P17/00; A61P43/00; C07D275/02; C07D333/48; C07F7/18; (IPC1-7): A61K31/38; A61K31/425; A61K45/00; C07D275/02; C07D333/48; C07F7/18
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)