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1. 发明授权

US06576656B1 Oxindole derivative 失效
标题翻译：羟吲哚衍生物
公开(公告)号：US06576656B1
公开(公告)日：2003-06-10
申请号：US09763241
申请日：2001-03-22
申请人： Teruhisa Tokunaga , Takashi Umezome , W. Ewan Hume , Ryu Nagata , Kazuhiko Okazaki , Yasuyuki Ueki , Kazuo Kumagai
发明人： Teruhisa Tokunaga , Takashi Umezome , W. Ewan Hume , Ryu Nagata , Kazuhiko Okazaki , Yasuyuki Ueki , Kazuo Kumagai
IPC分类号： A61K3140
CPC分类号： C07D401/04 , C07D209/38 , C07D209/40 , C07D403/06 , C07D405/04 , C07D409/04 , C07D413/06 , C07D417/04
摘要： An oxindole of Formula 1 or a prodrug thereof, or a pharmaceutically acceptable salt thereof is useful for growth hormone releaser: wherein R1, R2, R3 and R4 are independently hydrogen, optionally substituted alkyl etc; R5 is optionally substituted aryl or optionally substituted heteroaryl; Z is —O— or —NH—; one of W1 and W2 is hydrogen, alkyl or —Y—CON(R10)R11; the other of W1 and W2 is n is 1, 2 or 3; m is 0, 1, 2 or 3; Y is single bond or C1-C3 alkylene; R6 and R7 are independently hydrogen, optionally substituted alkyl etc; R8 and R9 are independently hydrogen, optionally substituted alkyl etc; R10 and R11 are independently hydrogen, alkyl etc.
摘要翻译：式1的羟吲哚或其前药或其药学上可接受的盐可用于生长激素释放剂：其中R 1，R 2，R 3和R 4独立地为氢，任选取代的烷基等; R 5为任选取代的芳基或任选取代的杂芳基; Z 是-O-或-NH-; W1和W2之一是氢，烷基或-Y-CON（R10）R11; W1和W2中的另一个是1,2或3; m是0,1,2或3; Y是单键或C1-C3亚烷基; R6和R7独立地是氢，任选取代的烷基等; R 8和R 9独立地是氢，任选取代的烷基等; R 10和R 11独立地是氢，烷基等

2. 发明申请

US20050227978A1 Fibrosis inhibitor 审中-公开
标题翻译：纤维化抑制剂
公开(公告)号：US20050227978A1
公开(公告)日：2005-10-13
申请号：US10502933
申请日：2003-01-28
申请人： Teruhisa Tokunaga , Willian Hume , Makoto Kitoh , Ryu Nagata , Michiko Kishino , Tsutomu Nakagawa , Jun Nagamine , Mutsuo Taiji
发明人： Teruhisa Tokunaga , Willian Hume , Makoto Kitoh , Ryu Nagata , Michiko Kishino , Tsutomu Nakagawa , Jun Nagamine , Mutsuo Taiji
IPC分类号： A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4174 , A61K31/425 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/5377 , A61P11/00 , A61P13/12 , A61P17/00 , A61P43/00 , C07D207/32 , C07D207/333 , C07D233/64 , C07D401/06 , A61K31/401 , A61K31/4164
CPC分类号： C07D207/333 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/404 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4174 , A61K31/425 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/498 , A61K31/4985 , A61K31/5377 , C07D401/06
摘要： Medicament being useful as a fibrosis inhibitor for organs or tissues, which comprises a compound of the formula (I): wherein Ring Z is optionally substituted pyrrole ring, etc.; W2 is —CO—, —SO2—, optionally substituted C1-C4 alkylene, etc.; Ar2 is optionally substituted aryl, etc.; W1 and Ar1 mean the following (1) and (2): (1) W1 is optionally substituted C1-C4 alkylene, etc.; Ar1 is optionally substituted bicyclic heteroaryl having 1 to 4 nitrogen atoms as ring-forming atoms: (2) W1 is optionally substituted C2-C5 alkylene, optionally substituted C2-C5 alkenylene, etc.; and Ar1 is aryl or monocyclic heteroaryl, which is substituted by carboxyl, alkoxycarbonyl, etc. at the ortho- or meta-position thereof with respect to the binding position of W1, or a pharmaceutically acceptable salt thereof.
摘要翻译：药物用作器官或组织的纤维化抑制剂，其包含式（I）的化合物：其中环Z是任选取代的吡咯环等; W 2是-CO - ， - SO 2 - ，任选取代的C 1 -C 4亚烷基等。 Ar 2是任选取代的芳基等; （1）和（2）：（1）W 1是任选取代的C 1 亚烷基等; 任选取代的具有1至4个氮原子的双环杂芳基作为成环原子：（2）W 1是任选取代的C 2 - -C 5亚烷基，任选取代的C 2 -C 5亚烯基等; 和Ar 1是在相邻或相对于W 1的结合位置的邻位或间位被羧基，烷氧基羰基等取代的芳基或单环杂芳基 >，或其药学上可接受的盐。

3. 发明授权

US07825155B2 Oxindole derivative as feeding control agent 失效
标题翻译：氧吲哚衍生物作为饲料控制剂
公开(公告)号：US07825155B2
公开(公告)日：2010-11-02
申请号：US12066251
申请日：2006-09-13
申请人： Teruhisa Tokunaga , Tsuyoshi Takasaki , Kozo Yoshida , Ryu Nagata
发明人： Teruhisa Tokunaga , Tsuyoshi Takasaki , Kozo Yoshida , Ryu Nagata
IPC分类号： C07D403/06 , C07D403/02 , C07D405/04 , C07D413/04 , C07D403/04 , C07D417/06 , C07D417/02 , C07D417/04 , C07D401/12 , C07D401/02 , C07D401/06 , C07D409/04 , C07D413/02 , C07D413/06 , C07D209/34 , C07D209/38 , A61K31/541 , A61K31/5377 , A61K31/497 , A61K31/496 , A61K31/4439 , A61K31/454 , A61K31/427 , A61K31/422 , A61K31/4245 , A61K31/4178 , A61K31/4155 , A61K31/404
CPC分类号： C07D403/06 , C07D209/34 , C07D209/38 , C07D405/04 , C07D413/04 , C07D413/06 , C07D417/04
摘要： Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.)
摘要翻译：公开了由下式（1）表示的化合物，其前药或其药学上可接受的盐，其可用作糖尿病等的治疗性预防或改善剂。（式中，R 3表示可以具有取代基的氨基甲酰基等，X表示羟基等; W 1和W 2分别表示单键或亚甲基，R 7，R 8分别表示氢原子，可以具有取代基的烷基或类似物; Ar表示任选取代的芳基等）。

4. 发明授权

US06759429B2 Pyrrole derivatives 失效
标题翻译：吡咯衍生物
公开(公告)号：US06759429B2
公开(公告)日：2004-07-06
申请号：US10352067
申请日：2003-01-28
申请人： Teruhisa Tokunaga , William Ewan Hume , Makoto Kitoh , Ryu Nagata
发明人： Teruhisa Tokunaga , William Ewan Hume , Makoto Kitoh , Ryu Nagata
IPC分类号： A61K304015
CPC分类号： C07D207/33 , C07D207/333 , C07D401/06 , C07D403/06 , C07D471/04
摘要： Pyrrole derivatives represented by the following formula: wherein Ring Z is an optionally substituted pyrrole ring, etc.; W2 is —CO—, —SO2—, an optionally substituted C1-C4 alkylene, etc.; Ar2 is an optionally substituted aryl, etc.; W1 and Ar1 mean the following (1) and (2): (1) W1 is an optionally substituted C1-C4 alkylene, etc.; Ar1 is an optionally substituted bicyclic heteroaryl having 1 to 4 nitrogen atoms as ring-forming atoms: (2) W1 is an optionally substituted C2-C5 alkylene, an optionally substituted C2-C5 alkenylene, etc.; and Ar1 is an aryl or monocyclic heteroaryl, which are substituted by carboxyl, an alkoxycarbonyl, etc. at the ortho- or meta-position thereof with respect to the binding position of W1, or a pharmaceutically acceptable salt thereof. These compounds are useful as medicaments such as a fibrosis inhibitor for organs or tissues.
摘要翻译：由下式表示的吡咯衍生物：其中环Z是任选取代的吡咯环等; W 2是-CO - ， - SO 2 - ，任选取代的C 1 -C 4亚烷基等; Ar 2是任选取代的芳基等; W 1和Ar 1表示以下（1）和（2）：（1）W 1是任选取代的C 1 -C 4亚烷基等; Ar 1是具有1-4个氮原子的任选取代的双环杂芳基作为成环原子：（2）W 1是任选取代的C 2 -C 5亚烷基，任选取代的C 2 -C 5亚烯基等; 并且Ar 1是在相对于W 1的结合位置的邻位或间位被羧基，烷氧基羰基等取代的芳基或单环杂芳基，或其药学上可接受的盐。这些化合物可用作药物如用于器官或组织的纤维化抑制剂。

5. 发明申请

US20090131398A1 OXINDOLE DERIVATIVE AS FEEDING CONTROL AGENT 失效
标题翻译：氧化物衍生物作为饲料控制剂
公开(公告)号：US20090131398A1
公开(公告)日：2009-05-21
申请号：US12066251
申请日：2006-09-13
申请人： Teruhisa Tokunaga , Tsuyoshi Takasaki , Kozo Yoshida , Ryu Nagata
发明人： Teruhisa Tokunaga , Tsuyoshi Takasaki , Kozo Yoshida , Ryu Nagata
IPC分类号： A61K31/404 , C07D209/38 , A61P3/10 , C07D403/06
CPC分类号： C07D403/06 , C07D209/34 , C07D209/38 , C07D405/04 , C07D413/04 , C07D413/06 , C07D417/04
摘要： Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.)
摘要翻译：公开了由下式（1）表示的化合物，其前药或其药学上可接受的盐，其可用作糖尿病等的治疗性预防或改善剂。（式中，R 3表示可以具有取代基的氨基甲酰基等，X表示羟基等; W 1和W 2分别表示单键或亚甲基，R 7，R 8分别表示氢原子，可以具有取代基的烷基或类似物; Ar表示任选取代的芳基等）。

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