公开(公告)号：EP2939668A1

公开(公告)日：2015-11-04

申请号：EP13869345.2

申请日：2013-12-26

申请人： The Kitasato Institute ,  Tokushima University ,  Nobelpharma Co., Ltd.

发明人： OMURA, Satoshi ,  NAKANO, Hirofumi ,  YAMAJI, Kenzaburo ,  YAMAMOTO, Tsuyoshi ,  KIDO, Hiroshi ,  YAMANE, Kazuhiko ,  SUNAZUKA, Toshiaki ,  HIROSE, Tomoyasu

IPC分类号： A61K31/015 ,  A61K31/122 ,  A61P1/14 ,  A61P13/02 ,  A61P31/16 ,  A61P35/00 ,  A61P43/00

CPC分类号： C07C69/95 ,  A61K8/355 ,  A61K8/368 ,  A61K8/37 ,  A61K8/40 ,  A61K8/42 ,  A61K31/122 ,  A61K31/136 ,  A61K31/166 ,  A61K31/192 ,  A61K31/198 ,  A61K31/216 ,  A61K31/235 ,  A61K31/37 ,  A61K31/47 ,  A61K2800/782 ,  A61Q19/00 ,  A61Q19/08 ,  C07C50/38 ,  C07C66/00 ,  C07C235/66 ,  C07C235/84 ,  C07C251/32 ,  C07C251/40 ,  C07D493/20

摘要： The present invention to provide a novel pyruvate dehydrogenase kinase inhibitors. A pyruvate dehydrogenase kinase inhibitor comprising a compound represented by the general formula (I) as an active ingredient (wherein, ring A represents a 6-membered aromatic hydrocarbon ring optionally substituted with 2-4 substituents,
R 1 and R 4 , which are the same or different, represent a hydrogen atom, a hydroxyl group, an optionally substituted C1-6 alkyl group, R 2 and R 3 , which are the same or different, represent a hydrogen atom, a carboxyl group, an optionally substituted C1-6 alkyl group, an optionally substituted C6-10 aryl group, or a group represented by -C (=R 9 )-R 10 ), a pharmaceutical composition for treatment or prophylaxis of diseases or disorders that pyruvate dehydrogenase kinase relates to its development or aggravation, and a cosmetic composition, and the like.

摘要翻译： 本发明提供了一种新的丙酮酸脱氢酶激酶抑制剂。 丙酮酸脱氢酶激酶抑制剂，其包含由通式（I）表示的化合物作为活性成分（其中，环A表示任选被2-4个取代基取代的6元芳族烃环，R 1和R 4是 相同或不同，表示氢原子，羟基，任选取代的C 1-6烷基，R 2和R 3相同或不同，表示氢原子，羧基，任选取代的C 1-6 烷基，任选取代的C 6-10芳基或由-C（= R 9）-R 10表示的基团），用于治疗或预防丙酮酸脱氢酶激酶涉及其发展或恶化的疾病或病症的药物组合物 ，和化妆品组合物等。