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Title:
AROMATIC AMIDINE DERIVATIVE OR ITS SALT AND ITS INTERMEDIATE
Document Type and Number:
Japanese Patent JP3461441
Kind Code:
B2
Abstract:

PROBLEM TO BE SOLVED: To subject new compound which possesses potent FXa inhibitory activity and is useful as a protective and therapeutic medicine for various diseases caused by thrombus and embolus.
SOLUTION: The compound of formula I [R1-R4 are each H and the like; (n) is an integer of 0-4; A is a (substituted) 1-4C alkylene and the like; X is a single bond and the like; Y is a (substituted) 5-6 membered heterocyclic ring group; formula II is indolyl, benzofuranyl, etc.]. For example, 2-[4-[((3S)-1- acetoimidoyl-3-pyrrolidinyl)oxy]phenyl]-3-(7-amidino-2-naphthyl)-propionic acid. The compound is obtained by reacting a nitrile compound of formula III with an alcohol to give a compound of formula IV (R5 is a lower alkyl) and then reacting it with ammonia in a solvent such as ethanol and the like at 10-140°C for 0.5-200 hrs.


Inventors:
Takayasu Nagahara
Naoaki Kanaya
Kazue Inamura
Yukio Yokoyama
Application Number:
JP8545498A
Publication Date:
October 27, 2003
Filing Date:
March 31, 1998
Export Citation:
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Assignee:
Daiichi Pharmaceutical Co., Ltd.
International Classes:
A61K31/165; A61K31/19; A61K31/195; A61K31/215; A61K31/235; A61K31/33; A61K31/40; A61K31/4025; A61K31/443; A61K31/4433; A61K31/445; A61K31/4465; A61K31/451; A61K31/495; A61K31/155; A61K31/50; A61K31/505; A61P7/02; A61P43/00; C07C255/52; C07C255/54; C07C255/56; C07C255/58; C07C257/18; C07C323/31; C07C323/32; C07D207/09; C07D207/12; C07D209/04; C07D211/22; C07D211/44; C07D211/46; C07D239/02; C07D239/20; C07D241/02; C07D307/78; C07D307/79; C07D307/80; C07D307/84; C07D333/60; C07D333/68; C07D401/12; C07D403/10; C07D403/12; C07D405/12; C07D409/10; C07D409/12; C07D417/12; C07D521/00; (IPC1-7): C07C255/52; C07C255/54; C07C255/56; C07C255/58; C07D207/12; C07D211/46; C07D307/84; C07D333/60; C07D403/12; C07D405/12; C07D409/12; C07D417/12
Domestic Patent References:
JP4891128A
Attorney, Agent or Firm:
Miyuki Ariga (3 outside)