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1. 发明授权

US06355672B1 Benzothiepin derivatives, process for the preparation of the same and uses thereof 失效
标题翻译：苯并噻吩衍生物，其制备方法及其用途
公开(公告)号：US06355672B1
公开(公告)日：2002-03-12
申请号：US09744857
申请日：2001-01-30
申请人： Tsuneo Yasuma , Haruhiko Makino , Akira Mori
发明人： Tsuneo Yasuma , Haruhiko Makino , Akira Mori
IPC分类号： C07D33708
CPC分类号： C07D263/44 , C07D211/88 , C07D233/74 , C07D277/04 , C07D295/135 , C07D495/04
摘要： The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.
摘要翻译：本发明提供下式的化合物：其中环A是任选取代的苯环; R1是任选取代的非芳族杂环基; R2和R3独立地为氢原子或任选取代的烃基; n为0-3的整数; 或其盐，其可用作具有成骨促进作用的药物和软骨素促进作用。本发明涉及具有抑制淀粉样蛋白b蛋白的产生和/或分泌的优异效果的胺化合物及其制备和用途。特别地，对于预防和/或治疗例如神经变性疾病，淀粉样血管病，由脑血管障碍引起的神经障碍等是有效的。

2. 发明授权

US06531604B2 Benzothiepine derivatives, their production and use 失效
标题翻译：苯并噻吩衍生物，其生产和使用
公开(公告)号：US06531604B2
公开(公告)日：2003-03-11
申请号：US10044787
申请日：2002-01-11
申请人： Tsuneo Yasuma , Haruhiko Makino , Akira Mori
发明人： Tsuneo Yasuma , Haruhiko Makino , Akira Mori
IPC分类号： C07D21140
CPC分类号： C07D263/44 , C07D211/88 , C07D233/74 , C07D277/04 , C07D295/135 , C07D495/04
摘要： The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.
摘要翻译：本发明提供下式的化合物：其中环A是任选取代的苯环; R1是任选取代的非芳族杂环基; R2和R3独立地为氢原子或任选取代的烃基; n为0-3的整数; 或其盐，其可用作具有成骨促进作用的药物和软骨素促进作用。本发明涉及具有抑制淀粉样蛋白b蛋白的产生和/或分泌的优异效果的胺化合物及其制备和用途。特别地，对于预防和/或治疗例如神经变性疾病，淀粉样血管病，由脑血管障碍引起的神经障碍等是有效的。

3. 发明授权

US06653476B2 Thienopyridine derivatives, their production and use 失效
标题翻译：噻吩并吡啶衍生物，其生产和使用
公开(公告)号：US06653476B2
公开(公告)日：2003-11-25
申请号：US10204593
申请日：2002-08-22
申请人： Tsuneo Yasuma , Atsuo Baba , Haruhiko Makino , Isao Aoki , Toshiaki Nagata
发明人： Tsuneo Yasuma , Atsuo Baba , Haruhiko Makino , Isao Aoki , Toshiaki Nagata
IPC分类号： A61K314365
CPC分类号： C07D495/04 , C07D495/14
摘要： The present invention provides thienopyridine derivatives, which are useful as anti-inflammatory drugs, particularly as remedies for arthritis; processes for producing them, and pharmaceutical compositions containing them. The thienopyridine derivatives are represented by the formula (I): wherein G is a halogen atom, hydroxyl group, an optionally substituted amino group, etc.; alk is an optionally substituted lower alkylene group; X is O, S, —(CH2)q—, etc.; R is an optionally substituted amino group, etc.; ring B is an optionally substituted Y-containing 5- to 8-membered ring whose ring constituent atoms contain no nitrogen atom; Y is O, S, a group of (wherein Ra, Rb and Rc are the same or different and, each is H, a halogen atom, an optionally substituted hydrocarbon group, etc.), etc.; and ring A may be substituted.
摘要翻译：本发明提供可用作抗炎药物的噻吩并吡啶衍生物，特别是作为关节炎的补救剂; 制备它们的方法和含有它们的药物组合物。噻吩并吡啶衍生物由式（I）表示：其中G是卤素原子，羟基，任选取代的氨基等; 烷基是任选取代的低级亚烷基; X是O，S， - （CH 2）q - 等; R是任选取代的氨基等; 环B是任选取代的含有Y的5至8元环，其环组成原子不含氮原子; Y是O，S，（其中Ra，Rb和Rc相同或不同，并且各自为H，卤素原子，任选取代的烃基等）等; 并且环A可以被取代。

4. 发明授权

US07067527B2 Thienopyridine derivatives, their production and use 失效
标题翻译：噻吩并吡啶衍生物，其生产和使用
公开(公告)号：US07067527B2
公开(公告)日：2006-06-27
申请号：US10662165
申请日：2003-09-03
申请人： Tsuneo Yasuma , Atsuo Baba , Haruhiko Makino , Isao Aoki , Toshiaki Nagata
发明人： Tsuneo Yasuma , Atsuo Baba , Haruhiko Makino , Isao Aoki , Toshiaki Nagata
IPC分类号： C07D495/14 , A61K31/38
CPC分类号： C07D495/04 , C07D495/14
摘要： The present invention provides thienopyridine derivatives, which are useful as anti-inflammatory drugs, particularly as remedies for arthritis; processes for producing them, and pharmaceutical compositions containing them. The thienopyridine derivatives are represented by the formula (I): wherein G is a halogen atom, hydroxyl group, an optionally substituted amino group, etc.; alk is an optionally substituted lower alkylene group; X is O, S, —(CH2)q—, etc.; R is an optionally substituted amino group, etc.; ring B is an optionally substituted Y-containing 5- to 8-membered ring whose ring constituent atoms contain no nitrogen atom; Y is O, S, a group of (wherein Ra, Rb and Rc are the same or different and, each is H, a halogen atom, an optionally substituted hydrocarbon group, etc.), etc.; and ring A may be substituted.
摘要翻译：本发明提供可用作抗炎药物的噻吩并吡啶衍生物，特别是作为关节炎的补救剂; 制备它们的方法和含有它们的药物组合物。噻吩并吡啶衍生物由式（I）表示：其中G是卤素原子，羟基，任选取代的氨基等; 烷基是任选取代的低级亚烷基; X是O，S， - （CH 2 CH 2）q - 等; R是任选取代的氨基等; 环B是任选取代的含有Y的5至8元环，其环组成原子不含氮原子; Y是O，S，（其中Ra，Rb和Rc相同或不同，并且各自为H，卤素原子，任选取代的烃基等）等; 并且环A可以被取代。

5. 发明申请

US20090215746A1 SUBSTITUTED PYRAZOLO[1,5-A]PYRIMIDINES AS CALCIUM RECEPTOR MODULATING AGENTS 审中-公开
标题翻译：作为钙受体调节剂的取代的吡唑并[1,5-A]嘧啶
公开(公告)号：US20090215746A1
公开(公告)日：2009-08-27
申请号：US12263426
申请日：2008-10-31
申请人： Tsuneo Yasuma , Akira Mori , Masahiro Kawase , Hiroyuki Kimura , Masato Yoshida , Albert Charles Gyorkos , Scott Alan Pratt , Christopher Peter Corrette
发明人： Tsuneo Yasuma , Akira Mori , Masahiro Kawase , Hiroyuki Kimura , Masato Yoshida , Albert Charles Gyorkos , Scott Alan Pratt , Christopher Peter Corrette
IPC分类号： A61K31/519 , A61K31/55 , A61K31/541 , A61K31/5377 , C07D487/10 , C07D487/04 , A61P19/00
CPC分类号： C07D487/04
摘要： There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided.Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.
摘要翻译：提供了包含式（I）化合物的钙受体调节剂：其中环A是任选取代的5至7元环; 环B是任选取代的5-至7-元杂环; X1是CR1，CR1R2，N或NR13; X2是N或NR3; Y为C，CR4或N，Z为CR5，CR5R6，N或NR7; Ar是任选取代的环状基团; R为H，任选取代的烃基等; ＆lt; img id =“CUSTOM-CHARACTER-00001”he =“3.13mm”wi =“8.47mm”file =“US20090215746A1-20090827-P00001.TIF”img-content =“character”img-format =“tif”/ >是单键或双键; R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 13独立地为H，任选取代的烃基; 或其盐或其前药。式（II）和（III）的化合物：其中环A是任选取代的5-至7-元环; Q为C，CR5或N; R8，R9，R10，R11和R12独立地为氢，任选取代的烃基等，或其盐。也如前所述，在式（II）和（III）中指定X1，R3，R1，Y和X3。

6. 发明授权

US06552054B1 Chromone derivatives, process for the preparation of the same and uses thereof 失效
标题翻译：色酮衍生物，其制备方法及其用途
公开(公告)号：US06552054B1
公开(公告)日：2003-04-22
申请号：US10070150
申请日：2002-03-01
申请人： Tsuneo Yasuma , Masahiro Kawase , Akira Mori
发明人： Tsuneo Yasuma , Masahiro Kawase , Akira Mori
IPC分类号： A61K31425
CPC分类号： C07D405/12 , C07D311/24 , C07D413/12 , C07D417/12 , C07D493/04
摘要： The invention provides chromone derivatives of the following general formula, a process for preparing such chromone derivatives and a prophylactic and therapeutic agent comprising such chromone derivatives for bone diseases and chondropathy: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 is a hydrogen atom or hydrocarbon group; R3 is a hydrogen atom, hydrocarbon group or halogen; n is an integer of 0-3; or a salt thereof.
摘要翻译：本发明提供以下通式的色酮衍生物，这种色酮衍生物的制备方法和包含骨疾病和软骨病的色酮衍生物的预防和治疗剂：其中环A为任选取代的苯环; R1是任选取代的非芳族杂环基; R2是氢原子或烃基; R3是氢原子，烃基或卤素; n为0-3的整数; 或其盐。

7. 发明申请

US20060079536A1 Calcium receptor modulating compound and use thereof 有权
标题翻译：钙受体调节化合物及其用途
公开(公告)号：US20060079536A1
公开(公告)日：2006-04-13
申请号：US10525158
申请日：2003-08-21
申请人： Tsuneo Yasuma , Akira Mori , Masahiro Kawase , Hiroyuki Kimura , Masato Yoshida , Albert Gyorkos , Scott Pratt , Christopher Corrette
发明人： Tsuneo Yasuma , Akira Mori , Masahiro Kawase , Hiroyuki Kimura , Masato Yoshida , Albert Gyorkos , Scott Pratt , Christopher Corrette
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.
摘要翻译：提供了包含式（I）化合物的钙受体调节剂：其中环A是任选取代的5-至7-元环; 环B是任选取代的5-至7-元杂环; X 1是CR 1，CR 1，R 2，N或NR 13， ; X 2是N或NR 3; Y是C，CR 4或N，Z是CR 5，CR 5，R 6，N或NR 7 ; Ar是任选取代的环状基团; R为H，任选取代的烃基等; “img id =”custom-character-00001“he =”1.78mm“wi =”2.12mm“file =”US20060079536A1-20060413-P00001.TIF“alt =”custom character“img-content =”character“img- format =“tif”/>是单键或双键; R 1，R 2，R 3，R 4，R 5， R 6，R 7和R 13独立地是H，任选取代的烃基; 或其盐或其前药。式（II）和（III）的化合物：其中环A是任选取代的5-至7-元环; Q是C，CR 5或N; R 9，R 9，R 10，R 11和R 12都是还可以提供H，任选取代的烃基等，或其盐。还可以在式（II）中指定X 1，R 3，R 3，R 3，Y和X 3，和（ III）。

8. 发明授权

US07514441B2 Substituted pyrazolo [1,5-A]pyrimidines as calcium receptor modulating agents 有权
标题翻译：取代的吡唑并[1,5-A]嘧啶作为钙受体调节剂
公开(公告)号：US07514441B2
公开(公告)日：2009-04-07
申请号：US10525158
申请日：2003-08-21
申请人： Tsuneo Yasuma , Akira Mori , Masahiro Kawase , Hiroyuki Kimura , Masato Yoshida , Albert Charles Gyorkos , Scott Alan Pratt , Christopher Peter Corrette
发明人： Tsuneo Yasuma , Akira Mori , Masahiro Kawase , Hiroyuki Kimura , Masato Yoshida , Albert Charles Gyorkos , Scott Alan Pratt , Christopher Peter Corrette
IPC分类号： C07D487/04 , A61K31/519 , A61P19/08 , A61P19/10
CPC分类号： C07D487/04
摘要： There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.
摘要翻译：提供了包含式（I）化合物的钙受体调节剂：其中环A是任选取代的5-至7-元环; 环B是任选取代的5-至7-元杂环; X1是CR1，CR1R2，N或NR13; X2是N或NR3; Y为C，CR4或N，Z为CR5，CR5R6，N或NR7; Ar是任选取代的环状基团; R为H，任选取代的烃基等; “=”1.78mm“wi =”3.89mm“file =”US07514441-20090407-P00001.TIF“alt =”自定义字符“img-content =”character“img- format =“tif”/>是单键或双键; R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 13独立地为H，任选取代的烃基; 或其盐或其前药。式（II）和（III）的化合物：其中环A是任选取代的5-至7-元环; Q为C，CR5或N; R8，R9，R10，R11和R12独立地为氢，任选取代的烃基等，或其盐。也如前所述，在式（II）和（III）中指定X1，R3，R1，Y和X3。

9. 发明授权

US08318746B2 Nitrogen-containing five-membered heterocyclic compound 失效
标题翻译：含氮五元杂环化合物
公开(公告)号：US08318746B2
公开(公告)日：2012-11-27
申请号：US12451130
申请日：2008-04-25
申请人： Tsuneo Yasuma , Kentaro Hashimoto , Masahiro Ito
发明人： Tsuneo Yasuma , Kentaro Hashimoto , Masahiro Ito
IPC分类号： A61K31/496 , A61K31/4427 , A61K31/427 , C07D403/14 , C07D401/14 , C07D277/20
CPC分类号： C07D207/34 , C07D233/64 , C07D233/68 , C07D401/04 , C07D401/14 , C07D405/06 , C07D413/06 , C07D417/04 , C07D417/14
摘要： The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof. The compound of the present invention has a glucokinase activity, and is useful as a medicament such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like.
摘要翻译：本发明提供由式（I）表示的化合物：其中每个符号如说明书中所定义，或其盐。本发明的化合物具有葡糖激酶活性，可用作糖尿病，肥胖等的预防或治疗药物等药物。

10. 发明申请

US20120046338A1 FUSED CYCLIC COMPOUNDS 失效
标题翻译：熔融循环化合物
公开(公告)号：US20120046338A1
公开(公告)日：2012-02-23
申请号：US13287639
申请日：2011-11-02
申请人： Tsuneo Yasuma , Nobuyuki Negoro , Masayuki Yamashita , Masahiro Itou
发明人： Tsuneo Yasuma , Nobuyuki Negoro , Masayuki Yamashita , Masahiro Itou
IPC分类号： A61K31/382 , C07D307/84 , A61P3/10 , A61K31/343
CPC分类号： C07D409/12 , C07D307/80
摘要： The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof. The compound or a salt thereof or a prodrug thereof has a GPR40 receptor function modulating action and is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.
摘要翻译：本发明提供由式（I）表示的化合物：其中每个符号如说明书中所定义，或其盐。化合物或其盐或其前药具有GPR40受体功能调节作用，并且可用作胰岛素促分泌素或用于预防或治疗糖尿病等的药剂。

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