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1. 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。

2. 发明申请

US20090048256A1 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：US20090048256A1
公开(公告)日：2009-02-19
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： A61K31/541 , C07D413/12 , C07D401/12 , C07D279/12 , C07D409/14 , A61P25/34 , A61P25/18 , A61P25/28 , A61P25/24 , A61K31/497 , C07D241/02 , A61K31/5377 , A61K31/444
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是任选被一至三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，或药学上可接受的其它。

3. 发明授权

US09302996B2 Continuous arycyclic compound 有权
标题翻译：连续的芳环化合物
公开(公告)号：US09302996B2
公开(公告)日：2016-04-05
申请号：US13994543
申请日：2011-12-16
申请人： Osamu Sakurai , Kunio Saruta , Norimitsu Hayashi , Takashi Goi , Kenji Morokuma , Hidekazu Tsujishima , Hiroaki Sawamoto , Hiroaki Shitama , Ritsuo Imashiro
发明人： Osamu Sakurai , Kunio Saruta , Norimitsu Hayashi , Takashi Goi , Kenji Morokuma , Hidekazu Tsujishima , Hiroaki Sawamoto , Hiroaki Shitama , Ritsuo Imashiro
IPC分类号： A61K31/44 , C07D211/72 , C07D233/64 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/14
CPC分类号： C07D401/04 , C07D233/64 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/14
摘要： This is to provide a continuous arycyclic compound having a DGAT1 inhibitory activity, and useful for prophylaxis and/or treatment of obesity or hyperlipidemia caused by obesity, hypertriglyceridemia, lipid metabolism disorder, fatty liver, hypertension, arteriosclerosis, diabetes, etc., as well as to provide a DGAT1 inhibitor comprising the continuous arycyclic compound or a pharmaceutically acceptable salt thereof as an effective ingredient. Disclosed is the continuous arycyclic compound is represented by the formula: wherein the substituents in the formula are the same as defined in the specification, or a pharmaceutically acceptable salt thereof.
摘要翻译：这是提供具有DGAT1抑制活性的连续的芳环化合物，并且可用于预防和/或治疗由肥胖，高甘油三酯血症，脂质代谢障碍，脂肪肝，高血压，动脉硬化，糖尿病等引起的肥胖症或高脂血症，以及以提供包含连续的芳环化合物或其药学上可接受的盐作为有效成分的DGAT1抑制剂。公开了连续的芳环化合物由下式表示：其中式中的取代基与说明书中所定义的相同，或其药学上可接受的盐。

4. 发明申请

US20130261128A1 CONTINUOUS ARYCYCLIC COMPOUND 有权
标题翻译：连续的芳香化合物
公开(公告)号：US20130261128A1
公开(公告)日：2013-10-03
申请号：US13994543
申请日：2011-12-16
申请人： Osamu Sakurai , Kunio Saruta , Norimitsu Hayashi , Takashi Goi , Kenji Morokuma , Hidekazu Tsujishima , Hiroaki Sawamoto , Hiroaki Shitama , Ritsuo Imashiro
发明人： Osamu Sakurai , Kunio Saruta , Norimitsu Hayashi , Takashi Goi , Kenji Morokuma , Hidekazu Tsujishima , Hiroaki Sawamoto , Hiroaki Shitama , Ritsuo Imashiro
IPC分类号： C07D233/64 , C07D401/10 , C07D403/10 , C07D401/14 , C07D405/14 , C07D401/04 , C07D403/04
CPC分类号： C07D401/04 , C07D233/64 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/14
摘要： This is to provide a continuous arycyclic compound having a DGAT1 inhibitory activity, and useful for prophylaxis and/or treatment of obesity or hyperlipidemia caused by obesity, hypertriglyceridemia, lipid metabolism disorder, fatty liver, hypertension, arteriosclerosis, diabetes, etc., as well as to provide a DGAT1 inhibitor comprising the continuous arycyclic compound or a pharmaceutically acceptable salt thereof as an effective ingredient. Disclosed is the continuous arycyclic compound is represented by the formula: wherein the substituents in the formula are the same as defined in the specification, or a pharmaceutically acceptable salt thereof.
摘要翻译：这是提供具有DGAT1抑制活性的连续的芳环化合物，并且可用于预防和/或治疗由肥胖，高甘油三酯血症，脂质代谢障碍，脂肪肝，高血压，动脉硬化，糖尿病等引起的肥胖症或高脂血症，以及以提供包含连续的芳环化合物或其药学上可接受的盐作为有效成分的DGAT1抑制剂。公开了连续的芳环化合物由下式表示：其中式中的取代基与说明书中所定义的相同，或其药学上可接受的盐。

5. 发明申请

US20090088422A1 4-IMIDAZOLIN-2-ONE COMPOUNDS 失效
标题翻译： 4-咪唑烷-2-酮化合物
公开(公告)号：US20090088422A1
公开(公告)日：2009-04-02
申请号：US12270826
申请日：2008-11-13
申请人： Akira Kubo , Ritsuo Imashiro , Hiroaki Sakurai , Hidetaka Miyoshi , Akihito Ogasawara , Hajime Hiramatsu , Tatsuo Nakajima , Tetsu Nakane
发明人： Akira Kubo , Ritsuo Imashiro , Hiroaki Sakurai , Hidetaka Miyoshi , Akihito Ogasawara , Hajime Hiramatsu , Tatsuo Nakajima , Tetsu Nakane
IPC分类号： A61K31/541 , C07D401/04 , A61K31/4439 , C07D417/14 , A61K31/513 , C07D403/04
CPC分类号： C07D401/04 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/506 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14
摘要： The present invention relates to a compound of the formula [I]: wherein G1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula: wherein ring B is benzene ring which may be substituted, etc., Q1 and Q2 may be the same or different, and each is hydrogen atom, a halogen atom or an alkyl, n is 0, 1, 2, 3 or 4, R1 is hydrogen atom, an alkyl which may be substituted, a cycloalkyl which may be substituted, a phenyl which may be substituted, etc., Z1, Z2, Z3 and Z4 may be the same or different, and each is CH or N, provided that 3 or more of Z1, Z2, Z3 and Z4 should not be N at the same time, G2 is hydrogen atom, —NR3R4, —OR5, etc., where R3 to R8 each is independently hydrogen atom, an alkyl which may be substituted, an alkenyl, an alkynyl, etc., or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及式[I]化合物：其中，G1是被卤素原子或烷氧基取代的烷基，或下式的基团：其中环B是可被取代的苯环等。，Q1和Q2可以相同或不同，各自为氢原子，卤素原子或烷基，n为0,1,2,3或4，R1为氢原子，可被取代的烷基，环烷基可以被取代的苯基，Z1，Z2，Z3和Z4可以相同或不同，并且各自为CH或N，条件是Z1，Z2，Z3和Z4中的3个或更多个应该不是同时为N，G 2为氢原子，-NR 3 R 4，-OR 5等，其中R 3至R 8各自独立地为氢原子，可被取代的烷基，烯基，炔基等，或其药学上可接受的盐。

6. 发明授权

US07846933B2 4-imidazolin-2-one compounds 失效
标题翻译： 4-咪唑啉-2-酮化合物
公开(公告)号：US07846933B2
公开(公告)日：2010-12-07
申请号：US12270826
申请日：2008-11-13
申请人： Akira Kubo , Ritsuo Imashiro , Hiroaki Sakurai , Hidetaka Miyoshi , Akihito Ogasawara , Hajime Hiramatsu , Tatsuo Nakajima , Tetsu Nakane
发明人： Akira Kubo , Ritsuo Imashiro , Hiroaki Sakurai , Hidetaka Miyoshi , Akihito Ogasawara , Hajime Hiramatsu , Tatsuo Nakajima , Tetsu Nakane
IPC分类号： C07D403/04 , A61K31/4439
CPC分类号： C07D401/04 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/506 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14
摘要： The present invention relates to a compound of the formula [I]: wherein G1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula: wherein ring B is benzene ring which may be substituted, etc., Q1 and Q2 may be the same or different, and each is hydrogen atom, a halogen atom or an alkyl, n is 0, 1, 2, 3 or 4, R1 is hydrogen atom, an alkyl which may be substituted, a cycloalkyl which may be substituted, a phenyl which may be substituted, etc., Z1, Z2, Z3 and Z4 may be the same or different, and each is CH or N, provided that 3 or more of Z1, Z2, Z3 and Z4 should not be N at the same time, G2 is hydrogen atom, —NR3R4, —OR5, etc., where R3 to R8 each is independently hydrogen atom, an alkyl which may be substituted, an alkenyl, an alkynyl, etc., or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及式[I]化合物：其中，G1是被卤素原子或烷氧基取代的烷基，或下式的基团：其中环B是可被取代的苯环等。，Q1和Q2可以相同或不同，各自为氢原子，卤素原子或烷基，n为0,1,2,3或4，R1为氢原子，可被取代的烷基，环烷基可以被取代的苯基，Z1，Z2，Z3和Z4可以相同或不同，并且各自为CH或N，条件是Z1，Z2，Z3和Z4中的3个或更多个应该不是同时为N，G 2为氢原子，-NR 3 R 4，-OR 5等，其中R 3至R 8各自独立地为氢原子，可被取代的烷基，烯基，炔基等，或其药学上可接受的盐。

7. 发明授权

US07473695B2 4-imidazolin-2-one compounds 有权
标题翻译： 4-咪唑啉-2-酮化合物
公开(公告)号：US07473695B2
公开(公告)日：2009-01-06
申请号：US10827294
申请日：2004-04-20
申请人： Akira Kubo , Ritsuo Imashiro , Hiroaki Sakurai , Hidetaka Miyoshi , Akihito Ogasawara , Hajime Hiramatsu , Tatsuo Nakajima , Tetsu Nakane
发明人： Akira Kubo , Ritsuo Imashiro , Hiroaki Sakurai , Hidetaka Miyoshi , Akihito Ogasawara , Hajime Hiramatsu , Tatsuo Nakajima , Tetsu Nakane
IPC分类号： C07D403/04 , A61K31/4439
CPC分类号： C07D401/04 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/506 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14
摘要： The present invention relates to a compound of the formula [I]: wherein G1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula: wherein ring B is benzene ring which may be substituted, etc., Q1 and Q2 maybe the same or different, and each is hydrogen atom, a halogen atom or an alkyl, n is 0, 1, 2, 3 or 4, R1 is hydrogen atom, an alkyl which may be substituted, a cycloalkyl which may be substituted, a phenyl which may be substituted, etc., Z1, Z2, Z3 and Z4 may be the same or different, and each is CH or N, provided that 3 or more of Z1, Z2, Z3 and Z4 should not be N at the same time, G2 is hydrogen atom, —NR3R4, —OR5, etc., where R3 to R8 each is independently hydrogen atom, an alkyl which may be substituted, an alkenyl, an alkynyl, etc., or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及式[I]化合物：其中，G1是被卤素原子或烷氧基取代的烷基，或下式的基团：其中环B是可被取代的苯环等。，Q1和Q2可以相同或不同，各自为氢原子，卤素原子或烷基，n为0,1,2,3或4，R1为氢原子，可被取代的烷基，环烷基，可以被取代的苯基，Z 1，Z 2，Z 3和Z 4可以相同或不同，并且各自为CH或N，条件是Z1，Z2，Z3和Z4中的3个或更多不应该同时为N，G 2为氢原子，-NR 3 R 4，-OR 5等，其中R 3至R 8各自独立地为氢原子，可被取代的烷基，烯基，炔基等，或药学上其可接受的盐。

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