公开(公告)号：US20120016119A1

公开(公告)日：2012-01-19

申请号：US13145627

申请日：2010-01-22

申请人： Yasunori Tsuboi ,  Kimihiro Shirai

发明人： Yasunori Tsuboi ,  Kimihiro Shirai

IPC分类号： C07D487/04

CPC分类号： A61K31/519 ,  C07D487/04

摘要： Disclosed is a novel pyrrolo[2,3-d]pyrimidine compound represented by formula [I] or a pharmacologically acceptable salt thereof, which has a GPR119 receptor agonistic activity and is useful for a pharmaceutical. In formula [I], E represents a group represented by formula: —NH—, or the like; ring A represents a 6-membered aromatic ring which may contain 1 to 2 nitrogen atoms as heteroatoms (the aromatic ring may be substituted by a halogen atom, a group represented by formula: —CONRaRb, or the like; Ra and Rb are the same or different and independently represent hydrogen, alkyl, hydroxyalkyl, or the like); R1 represents an acyl group or the like; and R2 represents a halogen atom or a cyano group.

摘要翻译： 公开了由式[I]表示的新颖的吡咯并[2,3-d]嘧啶化合物或其药理学上可接受的盐，其具有GPR119受体激动活性，可用于药物。 在式[I]中，E表示由式-NH-等表示的基团; 环A表示可以含有1〜2个氮原子作为杂原子的6元芳香环（芳香环可以被卤素原子取代，由式-CONRaRb表示的基团等），Ra和Rb相同 或不同且独立地表示氢，烷基，羟基烷基等）; R1表示酰基等; R 2表示卤素原子或氰基。

公开(公告)号：US08188097B2

公开(公告)日：2012-05-29

申请号：US12083268

申请日：2006-10-20

申请人： Yasunori Moritani ,  Kimihiro Shirai ,  Mariko Oi

发明人： Yasunori Moritani ,  Kimihiro Shirai ,  Mariko Oi

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00

CPC分类号： C07D487/04

摘要： The present invention relates to a novel pyrazolo[1,5-a]pyrimidine compound of the formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc. Q is single bond, a methylene group or a group of the formula: —N(RQ)—, RQ is an alkyl group, Ring A is a substituted pyrazole ring fused to the adjacent pyrimidine ring having the following formula (A), (B) or (C), R3 and R4 are the same or different and a hydrogen atom, a cyano group etc. E is one of the following groups (i) to (v): R00 is an alkyl group, Q1 is a single bond etc., Q2 is a single bond or an alkylene group, one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., one of R50 and R60 is a hydrogen atom or an alkyl group and the other is a hydrogen atom, an alkyl group etc., R51 is an alkyl group or an optionally substituted arylsulfonyl group, R61 is an alkylamino group or an azido group, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及式[I]的新型吡唑并[1,5-a]嘧啶化合物：其中R 1和R 2相同或不同，可以具有取代基的芳基等.Q是单键，亚甲基或 式（N）（RQ） - ，RQ为烷基，环A为与具有下式（A），（B）或（C）的相邻嘧啶环稠合的取代的吡唑环，R3和 R4是相同或不同的，氢原子，氰基等.E是下列基团之一（i）至（v）：R00是烷基，Q1是单键等，Q2是单键 或亚烷基，R 5和R 6中的一个是氢原子或烷基，另一个是烷基等，R 50和R 60之一是氢原子或烷基，另一个是氢原子， 烷基等，R 51为烷基或任选取代的芳基磺酰基，R 61为烷基氨基或叠氮基，或其药学上可接受的盐。

公开(公告)号：US20090069298A1

公开(公告)日：2009-03-12

申请号：US12083268

申请日：2006-10-20

申请人： Yasunori Moritani ,  Kimihiro Shirai ,  Mariko Oi

发明人： Yasunori Moritani ,  Kimihiro Shirai ,  Mariko Oi

IPC分类号： A61K31/519 ,  C07D487/04 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/55 ,  A61P25/00 ,  A61P25/30 ,  A61K31/541 ,  C07D417/14 ,  C07D403/14

CPC分类号： C07D487/04

摘要： The present invention relates to a novel pyrazolo[1,5-a]pyrimidine compound of the formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc. Q is single bond, a methylene group or a group of the formula: —N(RQ)—, RQ is an alkyl group, Ring A is a substituted pyrazole ring fused to the adjacent pyrimidine ring having the following formula (A), (B) or (C), R3 and R4 are the same or different and a hydrogen atom, a cyano group etc. E is one of the following groups (i) to (v): R00 is an alkyl group, Q1 is a single bond etc., Q2 is a single bond or an alkylene group, one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., one of R50 and R60 is a hydrogen atom or an alkyl group and the other is a hydrogen atom, an alkyl group etc., R51 is an alkyl group or an optionally substituted arylsulfonyl group, R61 is an alkylamino group or an azido group, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及式[I]的新型吡唑并[1,5-a]嘧啶化合物：其中R 1和R 2相同或不同，可以具有取代基的芳基等.Q是单键，亚甲基或 式（N）（RQ） - ，RQ为烷基，环A为与具有下式（A），（B）或（C）的相邻嘧啶环稠合的取代的吡唑环，R 3和 R4是相同或不同的，氢原子，氰基等.E是下列基团之一（i）至（v）：R00是烷基，Q1是单键等，Q2是单键 或亚烷基，R 5和R 6中的一个是氢原子或烷基，另一个是烷基等，R 50和R 60之一是氢原子或烷基，另一个是氢原子， 烷基等，R 51为烷基或任选取代的芳基磺酰基，R 61为烷基氨基或叠氮基，或其药学上可接受的盐。