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1. 发明申请

US20100168156A1 Novel Benzoxathiine Derivative 失效
标题翻译：新型苯并噻嗪衍生物
公开(公告)号：US20100168156A1
公开(公告)日：2010-07-01
申请号：US12084017
申请日：2006-10-25
申请人： Takashi Mizutani , Nagaaki Sato , Takahide Sasaki , Toshiyuki Takahashi
发明人： Takashi Mizutani , Nagaaki Sato , Takahide Sasaki , Toshiyuki Takahashi
IPC分类号： A61K31/4365 , A61K31/4523 , A61K31/4436 , A61K31/39 , C07D497/04 , C07D401/12 , C07D411/04 , C07D411/12 , A61P25/30 , A61P3/06 , A61P19/06 , A61P1/16 , A61P9/10 , A61P25/28 , A61P25/16 , A61P25/18 , A61P25/32 , A61P25/08
CPC分类号： C07D327/06 , C07D497/04
摘要： Disclosed is a compound represented by the formula (I) below and a pharmaceutically acceptable salt thereof. This compound is useful for treatment of obesity, diabetes and the like. [In the formula (I), Ar represents a benzene ring or the like; X1 represents a nitrogen atom, a sulfur atom or the like; R1 represents an aryl group or the like; X2 represents a group represented by the following formula (II): (wherein R4 and R5 respectively represent a lower alkyl group or the like, and m represents a number of 2-4) or the like; one of X and Y represents an oxygen atom and the other represents a sulfanyl group or the like; and X3-X6 respectively represent —CH—, a nitrogen atom or the like.
摘要翻译：公开了由下式（I）表示的化合物及其药学上可接受的盐。该化合物可用于治疗肥胖症，糖尿病等。 [式（I）中，Ar表示苯环等， X1表示氮原子，硫原子等; R1表示芳基等; X2表示由下式（II）表示的基团：（其中R4和R5分别表示低级烷基等，m表示2-4的数）等; X和Y中的一个表示氧原子，另一个表示硫烷基等; X3-X6分别表示-CH-，氮原子等。

2. 发明授权

US08163770B2 Benzoxathiin derivative 失效
标题翻译：苯并硫堇衍生物
公开(公告)号：US08163770B2
公开(公告)日：2012-04-24
申请号：US12084017
申请日：2006-10-25
申请人： Takashi Mizutani , Nagaaki Sato , Takahide Sasaki , Toshiyuki Takahashi
发明人： Takashi Mizutani , Nagaaki Sato , Takahide Sasaki , Toshiyuki Takahashi
IPC分类号： C07D513/02 , C07D515/02 , C07D211/22 , C07D327/06 , A01N43/42 , A01N43/40 , A61K31/44 , A61K31/445
CPC分类号： C07D327/06 , C07D497/04
摘要： Disclosed is a compound represented by the formula (I) below and a pharmaceutically acceptable salt thereof. This compound is useful for treatment of obesity, diabetes and the like. [In the formula (I), Ar represents a benzene ring or the like; X1 represents a nitrogen atom, a sulfur atom or the like; R1 represents an aryl group or the like; X2 represents a group represented by the following formula (II): (wherein R4 and R5 respectively represent a lower alkyl group or the like, and m represents a number of 2-4) or the like; one of X and Y represents an oxygen atom and the other represents a sulfanyl group or the like; and X3-X6 respectively represent —CH—, a nitrogen atom or the like.
摘要翻译：公开了由下式（I）表示的化合物及其药学上可接受的盐。该化合物可用于治疗肥胖症，糖尿病等。 [式（I）中，Ar表示苯环等， X1表示氮原子，硫原子等; R1表示芳基等; X2表示由下式（II）表示的基团：（其中R4和R5分别表示低级烷基等，m表示2-4的数）等; X和Y中的一个表示氧原子，另一个表示硫烷基等; X3-X6分别表示-CH-，氮原子等。

3. 发明申请

US20120028990A1 3 ARYL OR HETEROARYL-SUBSTITUTED INDOLE DERIVATIVE 审中-公开
标题翻译： 3 ARYL或HETEROARYL取代的INDOLE DERIVATIVE
公开(公告)号：US20120028990A1
公开(公告)日：2012-02-02
申请号：US13260746
申请日：2010-04-14
申请人： Takashi Fujimura , Hiroyuki Kishino , Takashi Mizutani , Shunji Sakuraba , Takahide Sasaki , Nagaaki Sato
发明人： Takashi Fujimura , Hiroyuki Kishino , Takashi Mizutani , Shunji Sakuraba , Takahide Sasaki , Nagaaki Sato
IPC分类号： A61K31/404 , A61K31/4439 , A61K31/4725 , A61P3/04 , C07D403/12 , A61K31/496 , C07D417/14 , C07D409/14 , C07D405/14 , A61K31/454
CPC分类号： C07D405/04 , C07D209/18 , C07D405/14 , C07D409/04 , C07D417/04
摘要： A 3-aryl or heteroaryl-substituted indole derivative which is effective as a preventive or remedy for various diseases is provided. [Means for Resolution] A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof is provided. In the formula, R1 represents a hydrogen atom, C1-6 alkyl et al; R2 represents a hydrogen atom, C1-6 alkyl et al; Z represents aryl or heteroaryl (with the proviso that imidazolyl is excluded); and W represents a group represented by the formula (w-1) or (w-2). In the formula, R3 represents C1-6 alkyl et al; Yl and Y2 both represent a hydrogen atom or Y1 and Y2 together form —CH2-CH2-; Q represents CH or N; Ar represents phenyl, furyl et al; R4 and R5 each independently represent a hydrogen atom or C1-6 alkyl or R4 and R5 together with the nitrogen atom form pyrrolidine et al.
摘要翻译：提供作为各种疾病的预防或治疗有效的3-芳基或杂芳基取代的吲哚衍生物。 [解决方法]提供由式（I）表示的化合物或其药学上可接受的盐。在该式中，R 1表示氢原子，C 1-6烷基等; R2表示氢原子，C1-6烷基等; Z表示芳基或杂芳基（条件是不包括咪唑基）; W表示由式（w-1）或（w-2）表示的基团。在该式中，R 3表示C 1-6烷基等; Y 1和Y 2均表示氢原子或Y 1和Y 2一起形成-CH 2 -CH 2 - ; Q表示CH或N; Ar表示苯基，呋喃基等; R4和R5各自独立地表示氢原子或C1-6烷基或R4和R5以及氮原子形成吡咯烷等。

4. 发明申请

US20080275069A1 Quinazoline Derivative 失效
标题翻译：喹唑啉衍生物
公开(公告)号：US20080275069A1
公开(公告)日：2008-11-06
申请号：US11628087
申请日：2005-05-30
申请人： Takashi Mizutani , Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
发明人： Takashi Mizutani , Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
IPC分类号： A61K31/519 , C07D239/91 , A61P1/16 , A61P3/04 , A61P9/00 , A61P9/12 , A61P25/00 , A61P25/14 , A61P25/18 , C07D471/04 , C07D401/12 , A61P43/00 , A61P25/32 , A61P25/28 , A61P25/24 , A61P25/22 , A61P25/16 , A61P25/02 , A61P13/12 , A61P9/10 , A61P3/10 , A61P3/00 , A61K31/517
CPC分类号： C07D239/91 , C07D401/12 , C07D403/04 , C07D471/04
摘要： This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein R1 represents a lower alkyl group et al; R2 and R3 are same and different and represents hydrogen atm et al; R4 represents the substituent of the formula (I) et al; X1 represents NH, O or S; Y represents N or C; Ar is a divalent substituent derived from aryl et al, by removing two hydrogen atoms therefrom; the ring A represents a 5- or 6-membered heteroaryl group; this compounds has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for preventive or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.
摘要翻译：本发明提供式（I）的化合物或其药学上可接受的盐，其中R 1表示低级烷基等; R 2和R 3相同且不同，表示氢原子; R 4表示式（I）等的取代基; X 1表示NH，O或S; Y表示N或C; Ar是通过从其中除去两个氢原子而衍生自芳基等的二价取代基; 环A表示5-或6-元杂芳基; 该化合物具有组胺H3受体拮抗作用或组胺H3受体反向激动作用，可用于预防或治疗代谢系统疾病，循环系统疾病或神经系统疾病。

5. 发明授权

US08314094B2 Benzoxazinone derivative 有权
标题翻译：苯并恶嗪酮衍生物
公开(公告)号：US08314094B2
公开(公告)日：2012-11-20
申请号：US12678785
申请日：2008-10-02
申请人： Shiho Ishikawa , Takashi Mizutani , Tsuyoshi Nagase , Nagaaki Sato , Hidekazu Takahashi
发明人： Shiho Ishikawa , Takashi Mizutani , Tsuyoshi Nagase , Nagaaki Sato , Hidekazu Takahashi
IPC分类号： A61K31/536 , A61K31/5365 , C07D265/14 , C07D413/02 , C07D498/04
CPC分类号： C07D239/80 , C07D265/18 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D498/04
摘要： [PROBLEMS]To provide a compound useful as an agent for the treatment of circulatory diseases, nervous system diseases, metabolic diseases, reproductive system diseases, and digestive tract diseases.[MEANS FOR SOLVING PROBLEMS]The compound, which is for use as an active ingredient, is represented by the formula (I): [wherein R1 represents optionally halogenated C1-6 alkyl, etc.; R2 represents, e.g., a group represented by the formula (II-1) or (II-4) (wherein W represents C1-6 alkylene, etc. and R represents C1-6 alkyl, etc.); R3 represents hydrogen, C1-6 alkyl, etc.; X represents —O—, —NH—, etc.; and Y1, Y2, Y3, and Y4 each independently represents —CH—, —N—, etc.].
摘要翻译： [问题]提供可用作治疗循环系统疾病，神经系统疾病，代谢疾病，生殖系统疾病和消化道疾病的药剂的化合物。用于解决问题的方法用作活性成分的化合物由式（I）表示：其中R 1表示任选卤代的C 1-6烷基等; R2表示例如由式（II-1）或（II-4）表示的基团（其中W表示C1-6亚烷基等，R表示C1-6烷基等）; R3代表氢，C1-6烷基等; X表示-O-，-NH-等; Y1，Y2，Y3和Y4各自独立地表示-CH-，-N-等〕。

6. 发明授权

US07960394B2 Quinazoline derivative 失效
标题翻译：喹唑啉衍生物
公开(公告)号：US07960394B2
公开(公告)日：2011-06-14
申请号：US11628087
申请日：2005-05-30
申请人： Takashi Mizutani , Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
发明人： Takashi Mizutani , Tsuyoshi Nagase , Nagaaki Sato , Akio Kanatani , Shigeru Tokita
IPC分类号： A01N43/00 , C07D239/70
CPC分类号： C07D239/91 , C07D401/12 , C07D403/04 , C07D471/04
摘要： This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein R1 represents a lower alkyl group et al; R2 and R3 are same and different and represents hydrogen atm et al; R4 represents the substituent of the formula (II) et al; X1 represents NH, O or S; Y represents N or C; Ar is a divalent substituent derived from aryl et al, by removing two hydrogen atoms therefrom; the ring A represents a 5- or 6-membered heteroaryl group; this compounds has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for preventive or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.
摘要翻译：本发明提供式（I）的化合物或其药学上可接受的盐，其中R 1表示低级烷基等; R2和R3相同且不同，代表氢原子; R4表示式（II）等的取代基; X1表示NH，O或S; Y表示N或C; Ar是通过从其中除去两个氢原子而衍生自芳基等的二价取代基; 环A表示5-或6-元杂芳基; 该化合物具有组胺H3受体拮抗作用或组胺H3受体反向激动作用，可用于预防或治疗代谢系统疾病，循环系统疾病或神经系统疾病。

7. 发明申请

US20100210636A1 BENZOXAZINONE DERIVATIVE 有权
标题翻译：苯并咪唑衍生物
公开(公告)号：US20100210636A1
公开(公告)日：2010-08-19
申请号：US12678785
申请日：2008-10-02
申请人： Shiho Ishikawa , Takashi Mizutani , Tsuyoshi Nagase , Nagaaki Sato , Hidekazu Takahashi
发明人： Shiho Ishikawa , Takashi Mizutani , Tsuyoshi Nagase , Nagaaki Sato , Hidekazu Takahashi
IPC分类号： A61K31/536 , C07D265/14 , C07D413/02 , C07D498/04 , A61K31/5365 , A61P3/00 , A61P3/06 , A61P1/16 , A61P3/04 , A61P3/10 , A61P35/00
CPC分类号： C07D239/80 , C07D265/18 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D498/04
摘要： [PROBLEMS]To provide a compound useful as an agent for the treatment of circulatory diseases, nervous system diseases, metabolic diseases, reproductive system diseases, and digestive tract diseases.[MEANS FOR SOLVING PROBLEMS]The compound, which is for use as an active ingredient, is represented by the formula (I): [wherein R1 represents optionally halogenated C1-6 alkyl, etc.; R2 represents, e.g., a group represented by the formula (II-1) or (II-4) (wherein W represents C1-6 alkylene, etc. and R represents C1-6 alkyl, etc.); R3 represents hydrogen, C1-6 alkyl, etc.; X represents —O—, —NH—, etc.; and Y1, Y2, Y3, and Y4 each independently represents —CH—, —N—, etc.].
摘要翻译： [问题]提供可用作治疗循环系统疾病，神经系统疾病，代谢疾病，生殖系统疾病和消化道疾病的药剂的化合物。用于解决问题的方法用作活性成分的化合物由式（I）表示：其中R 1表示任选卤代的C 1-6烷基等; R2表示例如由式（II-1）或（II-4）表示的基团（其中W表示C1-6亚烷基等，R表示C1-6烷基等）; R3代表氢，C1-6烷基等; X表示-O-，-NH-等; Y1，Y2，Y3和Y4各自独立地表示-CH-，-N-等〕。

8. 发明申请

US20100056597A1 INDOLEDIONE DERIVATIVE 有权
标题翻译：绝对衍生
公开(公告)号：US20100056597A1
公开(公告)日：2010-03-04
申请号：US12532182
申请日：2008-03-27
申请人： Toshiyuki Takahashi , Tsuyoshi Nagase , Nagaaki Sato
发明人： Toshiyuki Takahashi , Tsuyoshi Nagase , Nagaaki Sato
IPC分类号： A61K31/4155 , C07D403/02 , A61P3/10
CPC分类号： C07D403/04
摘要： A compound represented by the general formula (I-a): [wherein R1a and R2a each means hydrogen, lower cycloalkyl, lower alkyl, etc.; R3a means hydrogen, lower cycloalkyl, lower alkyl, etc.; R4a and R5a each means lower alkyl, lower cycloalkyl, etc. or R4a and R5a are bonded to each other to form lower cycloalkylidene; and R6a means lower alkyl, lower haloalkyl, etc.]. This compound functions as an LCE inhibitor and is useful as a therapeutic agent for various circulatory diseases, nervous diseases, metabolic diseases, reproductive diseases, digestive tract diseases, neoplasm, infectious diseases, etc.
摘要翻译：由通式（I-a）表示的化合物：[其中R 1a和R 2a各自表示氢，低级环烷基，低级烷基等; R3a表示氢，低级环烷基，低级烷基等; R4a和R5a各自表示低级烷基，低级环烷基等，或者R4a和R5a彼此键合形成较低环烷叉基; R6a表示低级烷基，低级卤代烷基等〕。该化合物作为LCE抑制剂起作用，可用作各种循环系统疾病，神经疾病，代谢疾病，生殖疾病，消化道疾病，肿瘤，感染性疾病等的治疗剂。

9. 发明授权

US08106086B2 Indoledione derivative 有权
标题翻译：吲哚二酮衍生物
公开(公告)号：US08106086B2
公开(公告)日：2012-01-31
申请号：US12532182
申请日：2008-03-27
申请人： Toshiyuki Takahashi , Tsuyoshi Nagase , Nagaaki Sato
发明人： Toshiyuki Takahashi , Tsuyoshi Nagase , Nagaaki Sato
IPC分类号： A61K31/4155 , C07D403/02
CPC分类号： C07D403/04
摘要： A compound represented by the general formula (I-a): [wherein R1a and R2a each means hydrogen, lower cycloalkyl, lower alkyl, etc.; R3a means hydrogen, lower cycloalkyl, lower alkyl, etc.; R4a and R5a each means lower alkyl, lower cycloalkyl, etc. or R4a and R5a are bonded to each other to form lower cycloalkylidene; and R6a means lower alkyl, lower haloalkyl, etc.]. This compound functions as an LCE inhibitor and is useful as a therapeutic agent for various circulatory diseases, nervous diseases, metabolic diseases, reproductive diseases, digestive tract diseases, neoplasm, infectious diseases, etc.
摘要翻译：由通式（I-a）表示的化合物：[其中R 1a和R 2a各自表示氢，低级环烷基，低级烷基等; R3a表示氢，低级环烷基，低级烷基等; R4a和R5a各自表示低级烷基，低级环烷基等，或者R4a和R5a彼此键合形成较低环烷叉基; R6a表示低级烷基，低级卤代烷基等〕。该化合物作为LCE抑制剂起作用，可用作各种循环系统疾病，神经疾病，代谢疾病，生殖疾病，消化道疾病，肿瘤，感染性疾病等的治疗剂。

10. 发明申请

US20120022078A1 ARYL INDOLE DERIVATIVES 审中-公开
标题翻译： ARYL INDOLE DORIVATIVES
公开(公告)号：US20120022078A1
公开(公告)日：2012-01-26
申请号：US13258006
申请日：2010-04-07
申请人： Hiroyuki Kishino , Sayaka Mizutani , Shunji Sakuraba , Nagaaki Sato
发明人： Hiroyuki Kishino , Sayaka Mizutani , Shunji Sakuraba , Nagaaki Sato
IPC分类号： A61K31/496 , A61P3/04 , C07D403/10 , C07D417/14 , C07D401/14
CPC分类号： C07D401/04 , A61K31/496 , C07D209/14 , C07D417/04
摘要： A novel aryl indole derivative is provided that is effective as a preventive or remedy for various diseases. A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R1 is a hydrogen atom, halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkyloxy, or haloC1-6alkyloxy; R2 represents C1-6alkyl or haloC1-6alkyl; R3 represents a hydrogen atom, C1-6alkyl, or haloC1-6alkyl; and Ar represents an aryl or heteroaryl, wherein the aryl or the heteroaryl may be substituted with 1 to 3 substituents such as halogen, C1-6alkyl, haloC1-6alkyl, and C1-6alkyloxy.
摘要翻译：提供了一种新的芳基吲哚衍生物，其作为各种疾病的预防或补救是有效的。由式（I）表示的化合物或其药学上可接受的盐：（I）其中R 1是氢原子，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基或卤代C 1-6烷氧基; R 2表示C 1-6烷基或卤代C 1-6烷基; R 3表示氢原子，C 1-6烷基或卤代C 1-6烷基; 并且Ar表示芳基或杂芳基，其中芳基或杂芳基可以被1至3个取代基例如卤素，C 1-6烷基，卤代C 1-6烷基和C 1-6烷氧基取代。

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