公开(公告)号：US20090258867A1

公开(公告)日：2009-10-15

申请号：US12303177

申请日：2007-07-04

申请人： Koichi Tanimoto ,  Mariko Oi ,  Yasunori Tsuboi ,  Yasunori Moritani

发明人： Koichi Tanimoto ,  Mariko Oi ,  Yasunori Tsuboi ,  Yasunori Moritani

IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/519 ,  C07D487/04

CPC分类号： C07D487/04

摘要： The present invention provides a pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of the following formula [I]: in which R1 and R2 are the same or different and each an optionally substituted aryl group etc, R0 is hydrogen atom, an alkyl group etc, E is a group of the formula: —C(═O)— or —SO2—, R is a group of the following formula [i], [ii] or [iii] etc: Ring A is (a) a C3-8 cycloalkyl group optionally fused to a benzene ring or (b) a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom etc, R3 is an alkyl group optionally substituted by an alkylthio group, R4 is hydrogen atom, an alkyl group etc, one of RA and RB is an alkyl group etc, and the other is hydrogen atom, an alkyl group etc, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明提供具有下式[I]的具有CB1受体拮抗活性的吡唑并[1,5-a]嘧啶化合物：其中R 1和R 2相同或不同，各自为任选取代的芳基等， R 0是氢原子，烷基等，E是下式的基团-C（-O） - 或-SO 2 - ，R是下式[i]，[ii]或[iii]等的基团 ：环A是（a）任选地与苯环稠合的C 3-8环烷基或（b）苯环，Q是单键或亚甲基，环B是4-至7-元脂族杂环基 所述环状基团通过其环碳原子与相邻的氮原子结合，X是硫原子等，R 3是任选被烷硫基取代的烷基，R 4是氢原子，烷基等，RA和RB之一 是烷基等，另一个是氢原子，烷基等，或其药学上可接受的盐。

公开(公告)号：US08921380B2

公开(公告)日：2014-12-30

申请号：US13418811

申请日：2012-03-13

申请人： Koichi Tanimoto ,  Mariko Oi ,  Yasunori Tsuboi ,  Yasunori Moritani

发明人： Koichi Tanimoto ,  Mariko Oi ,  Yasunori Tsuboi ,  Yasunori Moritani

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D487/04

CPC分类号： C07D487/04

摘要： Pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of formula [I]: wherein R1 and R2 are the same or different and each is an optionally substituted aryl group, etc., R0 is hydrogen, an alkyl group, etc., E is —C(═O)— or —SO2—, R is a group of formula [i], [ii] or [iii], etc: Ring A is a C3-8 cycloalkyl group optionally fused to a benzene ring or a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom, etc., R3 is an alkyl group optionally substituted by an alkylthio group, R4 is hydrogen atom, an alkyl group, etc., one of RA and RB is an alkyl group, etc., and the other is hydrogen, an alkyl group, etc., or a pharmaceutically acceptable salt thereof.

摘要翻译： 具有式[I]的CB 1受体拮抗活性的吡唑并[1,5-a]嘧啶化合物：其中R1和R2相同或不同，并且各自为任选取代的芳基等，R 0是氢， 烷基等，E是-C（= O） - 或-SO 2 - ，R是式[ⅰ]，[ⅱ]或[ⅲ]等基团：环A是任选的C 3-8环烷基 稠合到苯环或苯环，Q是单键或亚甲基，环B是4-至7-元脂族杂环基，所述环状基团通过其环碳原子与相邻氮原子结合， X是硫原子等，R 3是任选被烷硫基取代的烷基，R 4是氢原子，烷基等，RA和RB之一是烷基等，另一个是氢 ，烷基等，或其药学上可接受的盐。

公开(公告)号：US20120202992A1

公开(公告)日：2012-08-09

申请号：US13418811

申请日：2012-03-13

申请人： Koichi TANIMOTO ,  Mariko OI ,  Yasunori TSUBOI ,  Yasunori MORITANI

发明人： Koichi TANIMOTO ,  Mariko OI ,  Yasunori TSUBOI ,  Yasunori MORITANI

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： Pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of formula [I]: wherein R1 and R2 are the same or different and each is an optionally substituted aryl group, etc., R0 is hydrogen, an alkyl group, etc., E is —C(═O)— or —SO2—, R is a group of formula [i], [ii] or [iii], etc: Ring A is a C3-8 cycloalkyl group optionally fused to a benzene ring or a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom, etc., R3 is an alkyl group optionally substituted by an alkylthio group, R4 is hydrogen atom, an alkyl group, etc., one of RA and RB is an alkyl group, etc., and the other is hydrogen, an alkyl group, etc., or a pharmaceutically acceptable salt thereof.

摘要翻译： 具有式[I]的CB 1受体拮抗活性的吡唑并[1,5-a]嘧啶化合物：其中R1和R2相同或不同，并且各自为任选取代的芳基等，R 0是氢， 烷基等，E是-C（= O） - 或-SO 2 - ，R是式[ⅰ]，[ⅱ]或[ⅲ]等基团：环A是任选的C 3-8环烷基 稠合到苯环或苯环，Q是单键或亚甲基，环B是4-至7-元脂族杂环基，所述环状基团通过其环碳原子与相邻氮原子结合， X是硫原子等，R 3是任选被烷硫基取代的烷基，R 4是氢原子，烷基等，RA和RB之一是烷基等，另一个是氢 ，烷基等，或其药学上可接受的盐。

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：US08163759B2

公开(公告)日：2012-04-24

申请号：US12303177

申请日：2007-07-04

申请人： Koichi Tanimoto ,  Mariko Oi ,  Yasunori Tsuboi ,  Yasunori Moritani

发明人： Koichi Tanimoto ,  Mariko Oi ,  Yasunori Tsuboi ,  Yasunori Moritani

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

CPC分类号： C07D487/04

摘要： The present invention provides a pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of the following formula [I]: in which R1 and R2 are the same or different and each an optionally substituted aryl group etc, R0 is hydrogen atom, an alkyl group etc, E is a group of the formula: —C(═O)— or —SO2—, R is a group of the following formula [i], [ii]or [iii] etc: Ring A is (a) a C3-8 cycloalkyl group optionally fused to a benzene ring or (b) a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom etc, R3 is an alkyl group optionally substituted by an alkylthio group, R4 is hydrogen atom, an alkyl group etc, one of RA and RB is an alkyl group etc, and the other is hydrogen atom, an alkyl group etc, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明提供具有下式[I]的具有CB1受体拮抗活性的吡唑并[1,5-a]嘧啶化合物：其中R1和R2相同或不同，各自为任选取代的芳基等， R 0是氢原子，烷基等，E是下式的基团-C（= O） - 或-SO 2 - ，R是下式[i]，[ii]或[iii]等的基团 ：环A是（a）任选地与苯环稠合的C 3-8环烷基或（b）苯环，Q是单键或亚甲基，环B是4-至7-元脂族杂环基 所述环状基团通过其环碳原子与相邻的氮原子结合，X是硫原子等，R 3是任选被烷硫基取代的烷基，R 4是氢原子，烷基等，RA和RB之一 是烷基等，另一个是氢原子，烷基等，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。