公开(公告)号：US20120165353A1

公开(公告)日：2012-06-28

申请号：US13394266

申请日：2010-09-29

Applicant: Toru Miura ,  Seiichi Sato ,  Hajime Yamada ,  Junya Tagashira ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

Inventor： Toru Miura ,  Seiichi Sato ,  Hajime Yamada ,  Junya Tagashira ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

IPC: A61K31/506 ,  C07D413/14 ,  A61P9/00 ,  A61P13/12 ,  A61P3/10 ,  A61P9/10 ,  A61P9/12 ,  C07D401/14 ,  A61P3/00

CPC classification number: C07D401/14 ,  A61K31/422 ,  A61K31/4427 ,  C07D413/14

Abstract: Disclosed are: a novel compound which has both an antagonistic activity on an angiotensin II receptor and a PPARγ-activating activity and is therefore useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, arteriosclerosis, type-2 diabetes, diabetic complications, metabolic syndrome or the like; and a pharmaceutical composition containing the compound. Specifically disclosed are: a compound represented by general formula (I) (wherein the ring A represents a pyridine ring; the ring B represents a tetrazole ring or an oxadiazol-5(4H)-one ring; X represents C—R5 or a nitrogen atom; R1 represents a C1-6 alkyl group; R2 represents a C1-6 alkyl group or a C3-8 cycloalkyl group; and R3, R4, R5 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halo-C1-6 alkyl group, or a C1-6 alkoxy group which may have a substituent), a salt of the compound, or a solvate of the compound or the salt; and a pharmaceutical composition containing the compound, the salt or the solvate.

Abstract translation: 公开了一种对血管紧张素II受体具有拮抗作用和PPARγ活化活性的新型化合物，因此可用作高血压，心脏病，动脉硬化，2型糖尿病，糖尿病并发症的预防和/或治疗剂 ，代谢综合征等; 和含有该化合物的药物组合物。 具体公开的是：由通式（I）表示的化合物（其中环A表示吡啶环;环B表示四唑环或恶二唑-5（4H） - 酮环; X表示C-R5或氮 原子; R1表示C1-6烷基; R2表示C1-6烷基或C3-8环烷基; R3，R4，R5分别表示氢原子，卤素原子，C1-6烷基， 卤代C 1-6烷基或可具有取代基的C 1-6烷氧基），化合物的盐或化合物或其盐的溶剂合物; 和含有该化合物，该盐或溶剂化物的药物组合物。