公开(公告)号：EP1020451B1

公开(公告)日：2005-06-15

申请号：EP98911008.5

申请日：1998-03-25

申请人： Kowa Co., Ltd.

发明人： SHIBUYA, Kimiyuki ,  KAWAMINE, Katsumi ,  SATO, Yukihiro ,  EDANO, Toshiyuki ,  HIRATA, Mitsuteru ,  OZAKI, Chiyoka

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

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

摘要： 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.

公开(公告)号：EP1020451A1

公开(公告)日：2000-07-19

申请号：EP98911008.5

申请日：1998-03-25

申请人： Kowa Co., Ltd.

发明人： SHIBUYA, Kimiyuki ,  KAWAMINE, Katsumi ,  SATO, Yukihiro ,  EDANO, Toshiyuki ,  HIRATA, Mitsuteru ,  OZAKI, Chiyoka

IPC分类号： C07D233/84 ,  C07D235/28 ,  C07D263/58 ,  C07D277/70 ,  C07D413/04 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  A61K31/435

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

摘要： The invention relates to a novel anilide compound and a pharmaceutical composition comprising the same. The invention relates to a compound represented by the following general formula:
   represents a divalent residue of benzene with a substituent(s), heterocycle-condensed benzene which may or may not have a substituent, pyridine which may or may not have a substituent, cyclohexane or naphthalene
or


Ar represents an aryl group which may or may not have a substituent;
X represents -NH-, oxygen atom or sulfur atom;
Y represents -NR 4 -, oxygen atom, sulfur atom, sulfoxide or sulfone;
Z represents single bond or -NR 5 -;
R 4 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent;
R 5 represents hydrogen atom, a lower alkyl group, an aryl group or a silylated lower alkyl group which may or may not have a substituent; and
n represents an integer of 0 to 15.

The inventive compounds are useful in the form of pharmaceutical composition, specifically as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitor.

摘要翻译： 本发明涉及一种新的酰苯胺化合物和包含其的药物组合物。 本发明涉及由以下通式表示的化合物：表示具有取代基的苯的二价残基，可以具有也可以不具有取代基的杂环稠合苯，可以不具有取代基的吡啶，也可以不具有 取代基，环己烷或萘或 Ar表示可以具有或不具有取代基的芳基; X表示-NH-，氧原子或硫原子; Y代表-NR4-，氧原子，硫原子，亚砜或砜; Z表示单键或-NR5-; R4代表氢原子，低级烷基，芳基或甲硅烷基化的低级烷基，可以或不具有取代基; R5表示氢原子，低级烷基，芳基或甲硅烷基化的低级烷基，其可以具有或不具有取代基; 并且n表示0至15的整数。本发明化合物可用作药物组合物的形式，特别是酰基辅酶A胆固醇酰基转移酶（ACAT）抑制剂。