公开(公告)号：JP2000198776A

公开(公告)日：2000-07-18

申请号：JP31928198

申请日：1998-11-10

Applicant: KOWA CO

Inventor： OGUCHI MASAO ,  KYOTANI YOSHINORI ,  SHIGYO HIROMICHI ,  KOSHI TOMOYUKI ,  KITAMURA TAKAHIRO ,  OGIYA TADAAKI ,  MATSUDA TAKAYUKI ,  YAMAZAKI YUKIYOSHI ,  KUMAI NATSUYO ,  KOTAKI KYOKO

IPC: C07D237/04 ,  A61K31/00 ,  A61K31/50 ,  A61K31/535 ,  A61K31/5375 ,  A61K31/5377 ,  A61P1/00 ,  A61P1/16 ,  A61P9/00 ,  A61P9/10 ,  A61P13/00 ,  A61P19/10 ,  A61P29/00 ,  A61P31/00 ,  A61P37/00 ,  A61P37/02 ,  A61P43/00 ,  C07D237/14 ,  C07D401/04 ,  C07D401/06

Abstract: PROBLEM TO BE SOLVED: To obtain the subject new derivative excellent in suppressing action on a specific interleukin production, and useful as a preventing and treating agent for an immune system disease, an inflammatory disease, an ischemic disease, or the like. SOLUTION: This new piridazine derivative is a compound of formula I [R1 is a (substituted) aryl; R2 is a phenyl substituted at least with a lower alkoxy or the like at its 4 position and other positions thereof are substitutable; R3 is H or the like; A is a single bond or the like; X is O or the like; a broken line is a single bond or the like; provided that such conditions must be satisfied when the R3 is a halogenated lower alkyl, the A is a single bond, or the like], preferably 5,6-bis(4-methoxyphenyl)-2-(4-chlorocinnamyl)-2H-piridazin-3-one, or the like. The compound of formula I is obtained e.g. by reacting a compound of formula II with glyoxalic acid, reacting a hydrated hydrazine with the obtained compound, then performing dehydration reaction, and then reacting the obtained compound of formula III with a compound of the formula: R3-A-Y (Y is a halogen). The obtained compound has an interleukin-1β production- suppressing activity.

公开(公告)号：JPH09227562A

公开(公告)日：1997-09-02

申请号：JP3616796

申请日：1996-02-23

Applicant: KOWA CO

Inventor： KYOTANI YOSHINORI ,  SHIMIZU NOBORU ,  SATO SEIICHI ,  YAMAGUCHI TAKASHI ,  KITAMURA TAKAHIRO ,  OGIYA TADAAKI ,  KAWAMINE KATSUMI

IPC: C07D491/048 ,  A61K31/40 ,  A61P9/00 ,  B01J23/44 ,  C07B61/00

Abstract: PROBLEM TO BE SOLVED: To obtain an indole derivative useful e.g. as pharmaceuticals having a cardiopathy curative action under mild reaction condition in high yield in a mass by the catalytic reduction of a specific benzylamine compound in the presence of a palladium-carbon catalyst. SOLUTION: The compound of formula III can be produced by reacting 2,3-dihydro-4-hydroxy-5-(1,2-dimethyl-2-propenyl)-3,3,7-trimethyl-1H-i ndol-2-one of formula I with a halogenation agent in an alcohol or a hydrated alcohol solvent in the presence of a base and reacting the resulting halogenated compound of formula II (X is a halogen) with benzylamine. The objective indole derivative having cardiopathy curative action and expressed by formula IV can be produced in a mass in high yield by the catalytic reduction of the benzylamine compound of formula III in the presence of a palladium-carbon catalyst.