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公开(公告)号:US20050038035A1
公开(公告)日:2005-02-17
申请号:US10496967
申请日:2002-10-24
申请人: Hisashi Takasugi , Yoshikazu Inoue , Takeshi Terasawa , Akira Nagayoshi , Yoshiro Furukawa , Masafumi Mikami , Kazumasa Hinoue , Makoto Ohtsubo , Daisuke Fukumoto
发明人: Hisashi Takasugi , Yoshikazu Inoue , Takeshi Terasawa , Akira Nagayoshi , Yoshiro Furukawa , Masafumi Mikami , Kazumasa Hinoue , Makoto Ohtsubo , Daisuke Fukumoto
IPC分类号: A61K31/27 , A61K31/395 , A61K31/4035 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/472 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/506 , A61P1/18 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P43/00 , C07C231/02 , C07C233/62 , C07C269/06 , C07C271/24 , C07D207/32 , C07D207/335 , C07D209/44 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/50 , C07D213/53 , C07D213/56 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/89 , C07D217/04 , C07D217/18 , C07D217/20 , C07D233/54 , C07D233/64 , C07D239/26 , C07D239/42 , C07D241/04 , C07D249/08 , C07D277/20 , C07D277/24 , C07D277/28 , C07D277/40 , C07D277/46 , C07D277/48 , C07D295/02 , C07D295/033 , C07D295/12 , C07D295/135 , C07D295/14 , C07D295/15 , C07D295/155 , C07D295/18 , C07D295/192 , C07D295/20 , C07D295/205 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D417/06 , C07D417/12 , C07D43/02
CPC分类号: C07D207/335 , C07C271/24 , C07C2601/10 , C07C2602/08 , C07D209/44 , C07D213/30 , C07D213/38 , C07D213/40 , C07D213/50 , C07D213/56 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/81 , C07D217/04 , C07D217/18 , C07D217/20 , C07D233/64 , C07D239/26 , C07D239/42 , C07D249/08 , C07D277/24 , C07D277/28 , C07D277/40 , C07D277/46 , C07D277/48 , C07D295/033 , C07D295/135 , C07D295/15 , C07D295/155 , C07D295/192 , C07D295/205 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D409/06 , C07D409/12 , C07D417/06 , C07D417/12
摘要: The present invention relates to a compound of the formula (I) wherein R1 is optionally substituted aryl; R2 is optionally substituted aryl, optionally substituted heteroaryl, optionally substituted lower cycloalkyl, optionally substituted aryloxy, optionally substituted arylsulfonyl, vinyl, carbamoyl, protected carboxy or protected amino; ring A is bivalent residue derived from optionally substituted aryl or optionally substituted heteroaryl; X is bivalent residue derived from the group consisting of cycloalkene, naphthalene, unsaturated 5 or 6-membered heteromonocyclic group, each of which is optionally substituted, and substituted benzene; Y is -(A1)m1-(A2)m2-; and Z is direct bond or piperazine, or a salt thereof. The compound of the present invention and a salt thereof inhibit apolipoprotein B (Apo B) secretion and are useful as a medicament for prophylactic and treatment of diseases or conditions resulting from elevated circulating levels of Apo B.
摘要翻译: 本发明涉及式(I)化合物,其中R 1为任选取代的芳基; R 2是任选取代的芳基,任选取代的杂芳基,任选取代的低级环烷基,任选取代的芳氧基,任选取代的芳基磺酰基,乙烯基,氨基甲酰基,保护的羧基或被保护的氨基; 环A是衍生自任选取代的芳基或任选取代的杂芳基的二价残基; X是衍生自环烯,萘,不饱和5或6元杂单环基团的二价残基,各自任选被取代,取代的苯; Y为 - (A 1)m1-(A 2)m2-; Z是直接键合或哌嗪或其盐。 本发明化合物及其盐抑制载脂蛋白B(Apo B)分泌,可用作预防和治疗由ApoB升高的循环水平引起的疾病或病症的药物。
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公开(公告)号:US20090281142A1
公开(公告)日:2009-11-12
申请号:US12064267
申请日:2006-08-30
申请人: Masahiko Hayakawa , Takahiro Nigawara , Kazuyuki Tsuchiya , Naoki Ishibashi , Mitsuaki Okumura , Yuichiro Kawamoto , Akira Nagayoshi
发明人: Masahiko Hayakawa , Takahiro Nigawara , Kazuyuki Tsuchiya , Naoki Ishibashi , Mitsuaki Okumura , Yuichiro Kawamoto , Akira Nagayoshi
IPC分类号: A61K31/4709 , A61K31/426 , A61K31/427 , C07D215/12 , C07D215/38 , C07D277/40 , C07D277/46 , C07D417/12 , A61P3/10
CPC分类号: C07D277/46 , C07D417/04 , C07D417/12
摘要: [Problem] To provide a compound which is useful as a GK activator.[Means for Resolution] As a result of an extensive study on thiazole derivatives, the present inventors have found that a compound having an oxamoyl group, a glycol group or the like on a thiazole ring and a compound having an acetamide group substituted by a bicyclic heteroaryl group such as a quinolyl have a good GK activation effect, and thereby have accomplished the present invention.Since the compounds of the present invention have a good GK activation effect, these are useful as therapeutic agents for diabetes, particularly type II diabetes.
摘要翻译: [问题]提供可用作GK活化剂的化合物。 [解决手段]作为对噻唑衍生物的广泛研究的结果,本发明人已经发现,在噻唑环上具有氨酰氧基,二醇基等的化合物和具有被双环取代的乙酰胺基的化合物 杂环基如喹啉基具有良好的GK活化作用,从而完成了本发明。 由于本发明的化合物具有良好的GK活化作用,因此可用作糖尿病,特别是II型糖尿病的治疗剂。
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