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1. 发明申请

US20050239829A1 Novel piperidine compound 失效
标题翻译：新型哌啶化合物
公开(公告)号：US20050239829A1
公开(公告)日：2005-10-27
申请号：US10515845
申请日：2003-05-29
申请人： Masami Takahashi , Tsutomu Miyake , Yasunori Moritani , Hidetoshi Asai , Taketoshi Ishii , Rikako Kono
发明人： Masami Takahashi , Tsutomu Miyake , Yasunori Moritani , Hidetoshi Asai , Taketoshi Ishii , Rikako Kono
IPC分类号： A61K31/445 , A61K31/451 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/497 , A61K31/513 , A61K38/00 , C07D211/46 , C07D211/54 , C07D211/58 , C07D211/62 , C07D211/74 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/04 , C07D417/12 , C07D473/34 , C07K5/02 , C07K5/06 , C07K5/083 , C07K5/087 , C07K5/097 , C07K5/103 , C07D43/02
CPC分类号： C07D211/46 , A61K38/00 , C07D211/54 , C07D211/58 , C07D211/62 , C07D211/74 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/04 , C07D417/12 , C07D473/34 , C07K5/0202 , C07K5/06191 , C07K5/0808 , C07K5/0812 , C07K5/0821 , C07K5/1008
摘要： The present invention provides a novel piperidine compound of the formula [I]: wherein Ring A represents an optionally substituted benzene ring, Ring B represents an optionally substituted benzene ring, R1 represents an optionally substituted alkyl group, an optionally substituted hydroxyl group, etc., or a group of the formula: (a) wherein R11 and R12 are the same or different, and each represents hydrogen atom, a substituted carbonyl group, a substituted sulfonyl group, an optionally substituted alkyl group, etc., R2 represents hydrogen atom, etc., Z represents oxygen atom or a group represented by —N(R3)—, R3 represents hydrogen atom or an alkyl group, etc., R4 represents hydrogen atom or an alkyl group, etc., or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供式[I]的新的哌啶化合物：其中环A表示任选取代的苯环，环B表示任选取代的苯环，R 1表示任选取代的烷基，任选取代的羟基等，或下式的基团：（a）其中R 11和R 12相同或不同，并且各自表示氢原子取代的羰基，取代的磺酰基，任意取代的烷基等，R 2表示氢原子等，Z表示氧原子或-N（R' R 3表示氢原子或烷基等，R 4表示氢原子或烷基等，或其药学上可接受的盐。

2. 发明授权

US07619092B2 Piperidine compounds 失效
标题翻译：哌啶化合物
公开(公告)号：US07619092B2
公开(公告)日：2009-11-17
申请号：US10515845
申请日：2003-05-29
申请人： Masami Takahashi , Tsutomu Miyake , Yasunori Moritani , Hidetoshi Asai , Taketoshi Ishii , Rikako Kono
发明人： Masami Takahashi , Tsutomu Miyake , Yasunori Moritani , Hidetoshi Asai , Taketoshi Ishii , Rikako Kono
IPC分类号： C07D211/30 , A61K31/445
CPC分类号： C07D211/46 , A61K38/00 , C07D211/54 , C07D211/58 , C07D211/62 , C07D211/74 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/04 , C07D409/12 , C07D417/04 , C07D417/12 , C07D473/34 , C07K5/0202 , C07K5/06191 , C07K5/0808 , C07K5/0812 , C07K5/0821 , C07K5/1008
摘要： The present invention provides a novel piperidine compound of the formula [I]: wherein Ring A represents an optionally substituted benzene ring, Ring B represents an optionally substituted benzene ring, R1 represents an optionally substituted alkyl group, an optionally substituted hydroxyl group, etc., or a group of the formula: (a) wherein R11 and R12 are the same or different, and each represents hydrogen atom, a substituted carbonyl group, a substituted sulfonyl group, an optionally substituted alkyl group, etc., R2 represents hydrogen atom, etc., Z represents oxygen atom or a group represented by —N(R3)—, R3 represents hydrogen atom or an alkyl group, etc., R4 represents hydrogen atom or an alkyl group, etc., or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供式[I]的新型哌啶化合物：其中环A表示任选取代的苯环，环B表示任选取代的苯环，R 1表示任选取代的烷基，任选取代的羟基等或下式的基团：（a）其中R 11和R 12相同或不同，各自表示氢原子，取代的羰基，取代的磺酰基，任选取代的烷基等，R 2表示氢原子等等，Z表示氧原子或由-N（R3） - 表示的基团，R3表示氢原子或烷基等，R4表示氢原子或烷基等，或其药学上可接受的盐。

3. 发明授权

US08921380B2 Pyrazolo[1,5-a] pyrimidine compounds as CB1 receptor antagonist 有权
标题翻译：吡唑并[1,5-a]嘧啶化合物作为CB1受体拮抗剂
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。

4. 发明授权

US08188097B2 Pyrazolo[1,5-A]pyrimidine compounds 失效
标题翻译：吡唑并[1,5-A]嘧啶化合物
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。

5. 发明授权

US07872006B2 Pyrazole compounds having cannabinoid receptor (CB1) antagonizing activity 有权
标题翻译：具有大麻素受体（CB1）拮抗活性的吡唑化合物
公开(公告)号：US07872006B2
公开(公告)日：2011-01-18
申请号：US12083610
申请日：2006-10-20
申请人： Yasunori Moritani , Ritsuo Imashiro , Atsushi Sato
发明人： Yasunori Moritani , Ritsuo Imashiro , Atsushi Sato
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/435 , A61K31/4155 , C07D413/02 , C07D403/02 , C07D401/02 , C07D231/10
CPC分类号： C07D413/12 , C07D231/18 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula: —N(R7)—, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula: —N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: —N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及具有强的CB1拮抗活性的吡唑化合物，具有下式[I]：其中R1和R2相同或不同，可以具有取代基的芳基等，R3是烷基等，E 是式（i）至（iv）中的下列基团之一：Q 1是单键，亚烷基或下式基团-N（R 7） - ，R 7是氢原子或烷基， Q2是单键，氧原子或亚烷基，R4是环烷基，下式-N（R5）（R6）等基团，R5和R6之一是氢原子或烷基另一个是烷基，下式为-N（R 8）（R 9）等的基团，D为氧原子等，RA 1为氨基等，RA 2为任选取代的脂族杂环基， R是任选被1至3个卤素原子等取代的烷基，R 8和R 9中的一个是氢原子或烷基，另一个是烷基等，或药学上其表面盐。

6. 发明申请

US20050065349A1 Asymmetric 1,4-reductions of and 1,4-additions to enoates and related systems 审中-公开
标题翻译：对于烯烃和相关体系的不对称1,4-减少和1,4-加成
公开(公告)号：US20050065349A1
公开(公告)日：2005-03-24
申请号：US10935535
申请日：2004-09-07
申请人： Stephen Buchwald , Daniel Appella , Yasunori Moritani , Ryo Shintani , Valdas Jurkauskas
发明人： Stephen Buchwald , Daniel Appella , Yasunori Moritani , Ryo Shintani , Valdas Jurkauskas
IPC分类号： C07B53/00 , C07B57/00 , C07B61/00 , C07C45/58 , C07C45/62 , C07C45/68 , C07C45/78 , C07C67/303 , C07C67/347 , C07C253/30 , C07C255/33 , C07F7/24 , C07D213/57
CPC分类号： C07C253/30 , C07B53/00 , C07B57/00 , C07C45/58 , C07C45/62 , C07C45/68 , C07C45/78 , C07C67/303 , C07C67/347 , C40B40/00 , C07C255/33
摘要： One aspect of the present invention relates to methods for the transition-metal-catalyzed asymmetric 1,4-addition of a nucleophile, e.g., hydride, to cyclic and acyclic enoates and enones. In certain embodiments of the methods of the present invention, the transition metal catalyst consists essentially of copper and an asymmetric bidentate bisphosphine ligand.
摘要翻译：本发明的一个方面涉及过渡金属催化的亲核试剂例如氢化物的不对称1,4-加成到环状和无环烯醇酯和烯酮的方法。在本发明方法的某些实施方案中，过渡金属催化剂基本上由铜和不对称双齿二膦配体组成。

7. 发明授权

US08163759B2 Pyrazolo[1,5-A] pyrimidine compounds as CB1 receptor antagonist 失效
标题翻译：吡唑并[1,5-A]嘧啶化合物作为CB1受体拮抗剂
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。

8. 发明申请

US20090069298A1 Pyrazolo[1,5-A]Pyrimidine Compounds 失效
标题翻译：吡唑并[1,5-A]嘧啶化合物
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。

9. 发明申请

US20070167440A1 Novel pyrrolidine compound and a process for preparing the same 有权
标题翻译：新型吡咯烷化合物及其制备方法
公开(公告)号：US20070167440A1
公开(公告)日：2007-07-19
申请号：US11579950
申请日：2005-05-27
申请人： Yasunori Moritani , Shigeru Furukubu , Yasunori Tsuboi , Chieko Okagaki , Akira Oku , Naomitsu Hirano
发明人： Yasunori Moritani , Shigeru Furukubu , Yasunori Tsuboi , Chieko Okagaki , Akira Oku , Naomitsu Hirano
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/5415 , A61K31/538
CPC分类号： C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/04 , C07D491/04
摘要： The present invention relates to a novel pyrrolidine compound, which has a potent antagonistic activity against central cannabinoid (CB1) receptor, having the formula [I]: wherein each of R1 and R2 is (A) optionally substituted aryl (or heteroaryl) group, or (B) both of the groups combine to form a group of the formula: one of R3 and R4 is hydrogen and another is hydrogen, hydroxyl, hydroxyalkyl, etc., or both of R3 and R4 combine to form oxo group, R5 is hydrogen or alkyl, Y is single bond, oxygen atom or a group of the formula: —N(R7)—, R6 is optionally substituted hydrocarbon group or optionally substituted cyclic group, R7 is alkyl or alkyloxycarbonylalkyl, provided that R6 is not 4-amino-5-chloro-2-methoxyphenyl group when Y is single bond and one of the R3 and R4 is hydrogen and another is hydroxymethyl, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及一种新的吡咯烷化合物，其具有对中大麻素（CB1）受体的有效拮抗作用，具有式[I]：其中R 1和R 2各自为 /（A）任选取代的芳基（或杂芳基）基团，或（B）两个基团结合形成下式的基团：R 3和R 4中的一个氢和氢是氢，羟基，羟基烷基等，或者R 3和R 4两者结合形成氧代基，R“ 5是氢或烷基，Y是单键，氧原子或下式基团-N（R 7） - ，R 6是任选的取代的烃基或任选取代的环状基团，R 7是烷基或烷氧基羰基烷基，条件是R 6不是4-氨基-5-氯-2-甲氧基苯基，当Y 是单键，R 3和R 4之一是氢，另一个是羟甲基或药学上可接受的sa 其中。

10. 发明授权

US08034949B2 Pyrrolidine compound and a process for preparing the same 有权
标题翻译：吡咯烷化合物及其制备方法
公开(公告)号：US08034949B2
公开(公告)日：2011-10-11
申请号：US11579950
申请日：2005-05-27
申请人： Yasunori Moritani , Shigeru Furukubu , Yasunori Tsuboi , Chieko Okagaki , Akira Oku , Naomitsu Hirano
发明人： Yasunori Moritani , Shigeru Furukubu , Yasunori Tsuboi , Chieko Okagaki , Akira Oku , Naomitsu Hirano
IPC分类号： C07D213/72 , C07D207/00 , A61K31/44
CPC分类号： C07D207/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/04 , C07D491/04
摘要： The present invention relates to a novel pyrrolidine compound, which has a potent antagonistic activity against central cannabinoid (CB1) receptor, having the formula [I]: wherein each of R1 and R2 is (A) optionally substituted aryl (or heteroaryl) group, or (B) both of the groups combine to form a group of the formula: one of R3 and R4 is hydrogen and another is hydrogen, hydroxyl, hydroxyalkyl, etc., or both of R3 and R4 combine to form oxo group, R5 is hydrogen or alkyl, Y is single bond, oxygen atom or a group of the formula: —N(R7)—, R6 is optionally substituted hydrocarbon group or optionally substituted cyclic group, R7 is alkyl or alkyloxycarbonylalkyl, provided that R6 is not 4-amino-5-chloro-2-methoxyphenyl group when Y is single bond and one of the R3 and R4 is hydrogen and another is hydroxymethyl, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及一种新的吡咯烷化合物，其具有对中大麻素（CB1）受体的有效拮抗活性，其具有式[I]：其中R1和R2各自为（A）任选取代的芳基（或杂芳基）或（B）两个基团结合形成下式的基团：R 3和R 4中的一个是氢，另一个是氢，羟基，羟基烷基等，或者R 3和R 4都结合形成氧代基，R 5是氢或烷基，Y是单键，氧原子或下式的基团-N（R7） - ，R6是任选取代的烃基或任选取代的环状基团，R 7是烷基或烷氧基羰基烷基，条件是R 6不是4- 氨基-5-氯-2-甲氧基苯基或其药学上可接受的盐，当Y为单键且R 3和R 4中的一个为氢时，另一个为羟甲基。

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