公开(公告)号：NO995783D0

公开(公告)日：1999-11-25

申请号：NO995783

申请日：1999-11-25

Applicant: KOWA CO

Inventor： SHIBUYA KIMIYUKI ,  KAWAMINE KATSUMI ,  SATO YUKIHIRO ,  MIURA TORU ,  OZAKI CHIYOKA ,  EDANO TOSHIYUKI ,  HIRATA MITSUTERU

IPC: C07D413/12 ,  A61K31/496 ,  A61K31/506 ,  A61K31/55 ,  A61K31/5513 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  C07D233/70 ,  C07D235/28 ,  C07D263/58 ,  C07D277/74 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  C07F9/6509 ,  C07F9/6558 ,  C07D

公开(公告)号：AU1053899A

公开(公告)日：1999-06-07

申请号：AU1053899

申请日：1998-11-16

Applicant: KOWA CO

Inventor： SHIBUYA KIMIYUKI ,  MIURA TORU ,  KAWAMINE KATSUMI ,  SATO YUKIHIRO ,  OHGIYA TADAAKI ,  KITAMURA TAKAHIRO ,  OZAKI CHIYOKA ,  EDANO TOSHIYUKI ,  HIRATA MITSUTERU

IPC: C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D403/12 ,  A61K31/44 ,  A61K31/505

Abstract: The present invention provides to a novel compound having an ACAT inhibiting activity. The present invention relates to compounds represented by formula (I) wherein represents an optionally substituted divalent residue such as benzene, pyridine, cyclohexane or naphthalene, or a group, Het represents a 5- to 8-membered, substituted or unsubstituted heterocyclic group containing at least one heteroatom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, such as a monocyclic group, a polycyclic group or a group of a fused ring, X represents -NH-, an oxygen atom or a sulfur atom, Y represents -NR4-, an oxygen atom, a sulfur atom, a sulfoxide or a sulfone, Z represents a single bond or -NR5-, R4 represents a hydrogen atom, a lower alkyl group, an aryl group or an optionally substituted silyl lower alkyl group, R5 represents a hydrogen atom, a lower alkyl group, an aryl group or an optionally substituted silyl lower alkyl group, and n is an integer of from 1 to 15, or salts or solvates thereof, and a pharmaceutical composition containing at least one of these compounds.

公开(公告)号：SI0653426T1

公开(公告)日：1998-12-31

申请号：SI9430179

申请日：1994-10-28

Applicant: KOWA CO

Inventor： KYOTANI YOSHINORI ,  KAWAMINE KATSUMI ,  TOMA TSUTOMU ,  OHGIYA TADAAKI ,  YAMAGUCHI TAKASHI ,  ONOGI KAZUHIRO ,  SATO SEIICHI ,  SHIMIZU NOBORU ,  SHIGYO HIROMICHI ,  OHTA TOMIO ,  ODA TOSHIAKI ,  OKUNO YUKIHIRO ,  SHIBUYA KIMIYUKI ,  TAKAHASHI YOSHIO ,  FUJII MIKIO ,  UCHIDA YASUMI

IPC: A61K31/40 ,  C07D491/04 ,  C07D491/048

Abstract: An indole derivative represented by formula (1), wherein A is a group or wherein R is hydrogen or lower alkyl, dotted lines may optionally be resent, and R -R represents various substitutional groups. The compound (1) exhibits a positive inotropic action on cardiac muscle, an anti-arrhythmic action, and a vasodilation action without increasing the heart rate. A heart affection therapeutic agent comprising this compound as an effective component is extremely effective for treating heart failures and arrhythmia.

公开(公告)号：DE69411852T2

公开(公告)日：1998-12-03

申请号：DE69411852

申请日：1994-10-28

Applicant: KOWA CO

Inventor： KYOTANI YOSHINORI ,  KAWAMINE KATSUMI ,  TOMA TSUTOMU ,  OHGIYA TADAAKI ,  YAMAGUCHI TAKASHI ,  ONOGI KAZUHIRO ,  SATO SEIICHI ,  SHIMIZU NOBORU ,  SHIGYO HIROMICHI ,  OHTA TOMIO ,  ODA TOSHIAKI ,  OKUNO YUKIHIRO ,  SHIBUYA KIMIYUKI ,  TAKAHASHI YOSHIO ,  FUJII MIKIO ,  UCHIDA YASUMI

IPC: A61K31/40 ,  C07D491/04 ,  C07D491/048

Abstract: An indole derivative represented by formula (1), wherein A is a group or wherein R is hydrogen or lower alkyl, dotted lines may optionally be resent, and R -R represents various substitutional groups. The compound (1) exhibits a positive inotropic action on cardiac muscle, an anti-arrhythmic action, and a vasodilation action without increasing the heart rate. A heart affection therapeutic agent comprising this compound as an effective component is extremely effective for treating heart failures and arrhythmia.

公开(公告)号：ES2119945T3

公开(公告)日：1998-10-16

申请号：ES94117102

申请日：1994-10-28

Applicant: KOWA CO

Inventor： KYOTANI YOSHINORI ,  KAWAMINE KATSUMI ,  TOMA TSUTOMU ,  OHGIYA TADAAKI ,  YAMAGUCHI TAKASHI ,  ONOGI KAZUHIRO

IPC: A61K31/40 ,  C07D491/04 ,  C07D491/048

Abstract: An indole derivative represented by formula (1), wherein A is a group or wherein R is hydrogen or lower alkyl, dotted lines may optionally be resent, and R -R represents various substitutional groups. The compound (1) exhibits a positive inotropic action on cardiac muscle, an anti-arrhythmic action, and a vasodilation action without increasing the heart rate. A heart affection therapeutic agent comprising this compound as an effective component is extremely effective for treating heart failures and arrhythmia.

公开(公告)号：EP1431294A4

公开(公告)日：2004-09-15

申请号：EP02760658

申请日：2002-08-19

Applicant: KOWA CO

Inventor： SHIBUYA KIMIYUKI ,  KAWAMINE KATSUMI ,  OOGIYA TADAAKI ,  KITAMURA TAKAHIRO ,  MIURA TORU ,  EDANO TOSHIYUKI ,  YOSHINAKA YASUNOBU ,  YAMADA YOUICHI

IPC: A61K31/496 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07D263/58 ,  C07C233/25

CPC classification number: C07D263/58 ,  A61K31/496

Abstract: It is intended to provide a novel compound, which sustains an ACAT inhibitory activity and a macrophage-selectivity to a certain degree as a practically usable drug and can maintain an excellent oral absorbability and a favorable drug concentration in case of tested in vivo; a process for producing the same; medicinal compositions comprising the same and its intermediate. Namely, 2-[4-[2[(7-trifluoromethylbenzoxazol-2-ylthio)ethyl]piperadin-1-yl]-N-(2,6-diisopropyl-4-hydroxyphenyl)acetamide represented by the following formula: salts thereof or solvates of the same; and medicinal compositions comprising the compound represented by the above formula, salts thereof or solvates of the same together with pharmaceutically acceptable carriers.

公开(公告)号：EP1020451A4

公开(公告)日：2001-06-13

申请号：EP98911008

申请日：1998-03-25

Applicant: KOWA CO

Inventor： SHIBUYA KIMIYUKI ,  KAWAMINE KATSUMI ,  SATO YUKIHIRO ,  EDANO TOSHIYUKI ,  HIRATA MITSUTERU ,  OZAKI CHIYOKA

IPC: C07D233/84 ,  C07D235/28 ,  C07D263/58 ,  C07D263/60 ,  C07D277/74 ,  C07D413/04 ,  C07D413/12 ,  C07D471/04 ,  C07D498/04 ,  A61K31/415 ,  A61K31/42 ,  A61K31/695 ,  C07D277/70 ,  C07D513/04 ,  C07F7/10

CPC classification number: C07D263/58 ,  C07D233/84 ,  C07D235/28 ,  C07D263/60 ,  C07D277/74 ,  C07D413/04 ,  C07D413/12 ,  C07D471/04

Abstract: Novel compounds represented by general formula (1), salts thereof and solvated of the same, which are useful as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors and medicinal compositions containing the same, wherein (A) represents a divalent residue of substituted benzene, benzene fused with an optionally substituted heterocycle, optionally substituted pyridine, cyclohexane or naphthalene, or (B); Ar represents optionally substituted aryl; X represents -NH-, oxygen or sulfur; Y represents -NR4-, oxygen, sulfur, sulfoxy or sulfone; Z represents a single bond or -NR5-; R4 and R5 represent each hydrogen, lower alkyl, aryl or optionally substituted, silylated lower alkyl; and n is an integer of from 0 to 15.