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Title:
【発明の名称】選択的トロンビン抑制剤
Document Type and Number:
Japanese Patent JP2844329
Kind Code:
B2
Abstract:
The present invention relates to a novel selective thrombin inhibitor having the following formula (I), which is also effective by oral administration: in which R<1> represents acetyl substituted with aryl or aryloxy, or represents sulfonyl substituted with substituted or unsubstituted aryl or N-containing heterocyclic group, X represents a group of formula R<2> and R<3> independently of one another represent hydrogen; cycloalkyl substituted or unsubstituted with carboxyl or alkoxycarbonyl; arylalkyloxy; hydroxy; or lower alkyl substi tuted or unsubstituted with carboxyl, alkoxycarbonyl or hydroxy, or R<2> and R<3> together with nitrogen atom to which they are attached can form a piperidine group substituted with carboxyl or alkoxycarbonyl, R<4> represents hydrogen, lower alkyl or lower alkoxy, R<5> represents alkanesulfonyl; alkoxycarbonyl; alkylcarbonyl; formyl; lower alkyl; aryl substituted or unsubstituted with alkoxy or haloalkyl; or hydroxy-substituted lower alkyl, and R<6> and R<7> independently of one another represent hydrogen, lower alkyl or amino, and to a process for preparation thereof and a pharmaceutical composition for thrombin inhibition which comprises the compound of formula (I) as an active ingredient.

Inventors:
O YONSU
KIMU SANSU
FUAN SANYORU
YUN MIKYON
FUAN SUNRYURU
PPON SONUON
I YONHI
JON INA
I GU
SHIN YUSUN
Application Number:
JP614396A
Publication Date:
January 06, 1999
Filing Date:
January 17, 1996
Export Citation:
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Assignee:
ERU JII CHEM LTD
International Classes:
C07C257/18; A61K31/155; A61K31/165; A61K31/18; A61K31/445; A61K31/495; A61P7/02; A61P43/00; C07C257/22; C07C311/19; C07C311/29; C07C311/42; C07C311/45; C07D211/34; C07D211/60; C07D241/04; C07D295/10; C07D295/16; C07D295/185; C07D295/205; C07D295/26; (IPC1-7): C07C311/19; A61K31/18
Other References:
【文献】国際公開94/18185(WO,A)
【文献】国際公開92/16549(WO,A)
Attorney, Agent or Firm:
Takashima Hajime