公开(公告)号：US20120122906A1

公开(公告)日：2012-05-17

申请号：US13384519

申请日：2010-08-27

申请人： Toru Miura ,  Kazuhiro Onogi ,  Noriaki Gomi ,  Takaaki Araki ,  Junya Tagashira ,  Ryohei Sekimoto ,  Rio Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

发明人： Toru Miura ,  Kazuhiro Onogi ,  Noriaki Gomi ,  Takaaki Araki ,  Junya Tagashira ,  Ryohei Sekimoto ,  Rio Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

IPC分类号： A61K31/513 ,  A61P9/00 ,  A61P3/10 ,  A61P9/10 ,  A61P13/12 ,  A61P3/00 ,  C07D403/04 ,  A61P9/12

CPC分类号： C07D403/04

摘要： Disclosed is a novel compound which has both angiotensin II receptor antagonist activity and PPARγ activating activity, and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, kidney diseases, arteriosclerosis, inflammatory diseases, type 2 diabetes, diabetic complication, insulin resistant syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. Also disclosed is a pharmaceutical composition which contains the novel compound. Specifically disclosed are: a sulfonamide derivative represented by general formula (I), a salt thereof, or a solvate of the derivative or salt; and a pharmaceutical composition which contains the sulfonamide derivative, a salt thereof, or a solvate of the derivative or salt. (In the formula, R1 represents a C1-6 alkyl group; R2 and R3 each represents a C1-6 alkyl group or the like; and R4 represents a hydrogen atom, a C1-6 alkyl group, a C1-6 alkanoyl group or a C3-8 cycloalkylcarbonyl group.)

摘要翻译： 公开了具有血管紧张素II受体拮抗剂活性和PPARγ活化活性两者的新型化合物，可用作高血压，心脏病，心绞痛，脑血管障碍，脑循环障碍，缺血性外周循环障碍等的预防和/ 肾脏疾病，动脉硬化，炎性疾病，2型糖尿病，糖尿病并发症，胰岛素抵抗综合征，X综合征，代谢综合征和高胰岛素血症。 还公开了含有新化合物的药物组合物。 具体公开的是：由通式（I）表示的磺酰胺衍生物，其盐或衍生物或盐的溶剂合物; 以及含有磺酰胺衍生物，其盐或衍生物或盐的溶剂合物的药物组合物。 （式中，R1表示碳原子数1〜6的烷基，R2，R3各自表示C1-6烷基等，R4表示氢原子，C1-6烷基，C1-6烷酰基或 C3-8环烷基羰基）