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1. 发明授权

US06787650B1 Urea compounds, process for producing the same and use thereof 失效
标题翻译：尿素化合物，其制造方法及其用途
公开(公告)号：US06787650B1
公开(公告)日：2004-09-07
申请号：US10089961
申请日：2002-04-05
申请人： Osamu Kurasawa , Shinichi Imamura , Shohei Hashiguchi , Osamu Nishimura , Naoyuki Kanzaki , Masanori Baba
发明人： Osamu Kurasawa , Shinichi Imamura , Shohei Hashiguchi , Osamu Nishimura , Naoyuki Kanzaki , Masanori Baba
IPC分类号： C07D41700
CPC分类号： C07D211/14
摘要： A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; R3 is halogen atoms, a carbamoyl group which may be substituted, a sulfamoyl group which may be substituted, an acyl group derived from sulfonic acid, a C1-4 alkyl group which may be substituted, a C1-4 alkoxy group which may be substituted, an amino group which may be substituted, a nitro group or a cyano group; R4 is hydrogen atoms or a hydroxy group; n is 0 or 1; and p is 0 or 1 to 4]; or a salt thereof, has potent CCR5 antagonistic activity and can be advantageously used as a medicament for inhibition of HIV infection to human peripheral blood mononuclear cells, especially for the treatment or prevention of AIDS.
摘要翻译：下式的化合物：其中R 1为可被取代的烃基; R 2为可被取代的环状烃基或可被取代的杂环基; R 3为卤素原子，可以被取代的氨基甲酰基，可以被取代的氨磺酰基，可以被取代的酰基，可以被取代的C1-4烷基，可被取代的C1-4烷氧基，氨基其可以被取代，硝基或氰基; R 4是氢原子或羟基; n是0或1; 和p为0或1至4];或其盐具有有效的CCR5拮抗活性，并且可有利地用作抑制人外周血单核细胞的HIV感染的药物，特别是用于治疗或预防AIDS。

2. 发明授权

US08691828B2 Thienopyrimidine as CDC7 kinase inhibitors 有权
标题翻译：噻吩并嘧啶作为CDC7激酶抑制剂
公开(公告)号：US08691828B2
公开(公告)日：2014-04-08
申请号：US13254551
申请日：2010-03-04
申请人： Yuya Oguro , Osamu Kurasawa
发明人： Yuya Oguro , Osamu Kurasawa
IPC分类号： C07D495/04 , A61K31/519 , A61P35/00
CPC分类号： C07D495/04
摘要： The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
摘要翻译：本发明涉及由式（I）表示的化合物：其中每个符号如说明书中所定义，或其盐或其前药，其可用于预防或治疗癌症。

3. 发明申请

US20070072865A1 Bicyclic piperazine compound and use thereof 失效
标题翻译：双环哌嗪化合物及其用途
公开(公告)号：US20070072865A1
公开(公告)日：2007-03-29
申请号：US10570270
申请日：2004-08-26
申请人： Kohji Fukatsu , Yutaka Nakayama , Naoki Tarui , Masaaki Mori , Hirokazu Matsumoto , Osamu Kurasawa , Hiroshi Banno
发明人： Kohji Fukatsu , Yutaka Nakayama , Naoki Tarui , Masaaki Mori , Hirokazu Matsumoto , Osamu Kurasawa , Hiroshi Banno
IPC分类号： A61K31/498 , C07D498/04 , C07D491/04 , C07D487/04
CPC分类号： C07D487/04 , C07D513/04
摘要： The present invention provides a compound represented by the formula: wherein R1 is an acyl group, R2 is a hydrocarbon group which may be substituted or the like, R3 is a hydrocarbon group which may be substituted or the like, R4 is a hydrocarbon group which may be substituted or the like, n is from 0 to 4, and X is an oxygen atom, a sulfur atom or the like, or a salt thereof. The invention also provides a compound which has a TGR23 antagonist activity and thus is useful for prevention and treatment of cancer.
摘要翻译：本发明提供由下式表示的化合物：其中R 1是酰基，R 2是可以被取代的烃基，等等，R SUP > 3为可以被取代的烃基等，R 4为可以被取代的烃基等，n为0〜4，X为氧原子，硫原子等，或其盐。本发明还提供具有TGR23拮抗剂活性的化合物，因此可用于预防和治疗癌症。

4. 发明授权

US09090601B2 Thiazole derivatives 有权
标题翻译：噻唑衍生物
公开(公告)号：US09090601B2
公开(公告)日：2015-07-28
申请号：US12657854
申请日：2010-01-28
申请人： Hiroshi Banno , Masaaki Hirose , Osamu Kurasawa
发明人： Hiroshi Banno , Masaaki Hirose , Osamu Kurasawa
IPC分类号： C07D417/14 , C07D487/04 , C07D513/04 , C07D495/04 , A61K9/20 , C07D417/04 , C07D471/04
CPC分类号： C07D417/14 , A61K9/2059 , C07D417/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to a compound represented by the formula (I) or (I′): wherein each symbol is as defined in the specification, or a salt thereof, and a PI3K and(or) mTOR inhibitor containing the compound or a prodrug thereof.
摘要翻译：本发明涉及由式（I）或（I'）表示的化合物：其中每个符号如说明书中所定义，或其盐，和含有该化合物或前药的PI3K和（或）mTOR抑制剂其中。

5. 发明申请

US20120040981A1 THIENOPYRIMIDINE AS CDC7 KINASE INHIBITORS 有权
标题翻译：三硝基嘧啶作为CDC7激酶抑制剂
公开(公告)号：US20120040981A1
公开(公告)日：2012-02-16
申请号：US13254551
申请日：2010-03-04
申请人： Yuya Oguro , Osamu Kurasawa
发明人： Yuya Oguro , Osamu Kurasawa
IPC分类号： A61K31/519 , A61P35/00 , A61K31/5377 , C07D495/04 , C07D495/20
CPC分类号： C07D495/04
摘要： The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
摘要翻译：本发明涉及由式（I）表示的化合物：其中每个符号如说明书中所定义，或其盐或其前药，其可用于预防或治疗癌症。

6. 发明申请

US20110003807A1 Thiazole derivatives 有权
标题翻译：噻唑衍生物
公开(公告)号：US20110003807A1
公开(公告)日：2011-01-06
申请号：US12657854
申请日：2010-01-28
申请人： Hiroshi Banno , Masaaki Hirose , Osamu Kurasawa
发明人： Hiroshi Banno , Masaaki Hirose , Osamu Kurasawa
IPC分类号： A61K31/5377 , C07D417/04 , A61K31/4439 , C07D413/14 , C07D471/02 , A61K31/437 , C07D513/04 , A61K31/429 , C07D487/02 , A61K31/5025 , C07D409/14 , A61K31/444 , A61K31/496 , A61P35/00 , A61P29/00 , A61P9/00
CPC分类号： C07D417/14 , A61K9/2059 , C07D417/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to a compound represented by the formula (I) or (I′): wherein each symbol is as defined in the specification, or a salt thereof, and a PI3K and(or) mTOR inhibitor containing the compound or a prodrug thereof.
摘要翻译：本发明涉及由式（I）或（I'）表示的化合物：其中每个符号如说明书中所定义，或其盐，和含有该化合物或前药的PI3K和（或）mTOR抑制剂其中。

7. 发明申请

US20100004238A1 FUSED HETEROCYCLIC COMPOUND 审中-公开
标题翻译：熔融杂环化合物
公开(公告)号：US20100004238A1
公开(公告)日：2010-01-07
申请号：US12518596
申请日：2007-12-11
申请人： Tomoyasu Ishikawa , Hiroshi Banno , Youichi Kawakita , Tomohiro Ohashi , Osamu Kurasawa
发明人： Tomoyasu Ishikawa , Hiroshi Banno , Youichi Kawakita , Tomohiro Ohashi , Osamu Kurasawa
IPC分类号： A61K31/5377 , C07D487/04 , A61K31/519 , A61K31/4985
CPC分类号： C07D487/04
摘要： The present invention provides a fused heterocyclic compound having a tyrosine kinase inhibitory action, which is represented by the formula: wherein R1 is a hydrogen atom, a halogen atom, or an optionally substituted group bonded via a carbon atom, a nitrogen atom or an oxygen atom; R2 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom or a sulfur atom, or R1 and R2, or R2 and R3 are optionally bonded to each other to form an optionally substituted ring structure; R3 is a hydrogen atom or an optionally substituted aliphatic hydrocarbon group, or R3 is optionally bonded to the carbon atom on ring A to form an optionally substituted ring structure; ring A is an optionally substituted benzene ring; and ring B is (i) an optionally substituted fused ring, or (ii) a pyridine ring having optionally substituted carbamoyl (the pyridine ring is optionally further substituted).
摘要翻译：本发明提供具有酪氨酸激酶抑制作用的稠合杂环化合物，其由下式表示：其中R1是氢原子，卤原子或经由碳原子，氮原子或氧键键合的任意取代的基团原子; R2是氢原子，或通过碳原子或硫原子键合的任选取代的基团，或者R 1和R 2，或R 2和R 3相互结合形成任选取代的环结构; R3是氢原子或任选取代的脂族烃基，或R3任选地键合到环A上的碳原子上以形成任选取代的环结构; 环A是任选取代的苯环; 和环B是（i）任选取代的稠合环，或（ii）具有任选取代的氨基甲酰基的吡啶环（吡啶环任选进一步被取代）。

8. 发明授权

US07582651B2 Pyrrolopyridine derivative and use thereof 失效
标题翻译：吡咯并吡啶衍生物及其用途
公开(公告)号：US07582651B2
公开(公告)日：2009-09-01
申请号：US10520784
申请日：2003-07-10
申请人： Takahiro Matsumoto , Osamu Kurasawa , Tsuneo Oda , Hiroshi Nagabukuro , Manabu Mochizuki
发明人： Takahiro Matsumoto , Osamu Kurasawa , Tsuneo Oda , Hiroshi Nagabukuro , Manabu Mochizuki
IPC分类号： A61K31/44 , C07D513/02
CPC分类号： C07D471/04
摘要： A novel pyrrolopyridine derivative which is a compound represented by the formula wherein Ring A represents an optionally substituted pyridine ring; X represents an electron-attracting group; Y represents an optionally substituted divalent C1-6 chain hydrocarbon group; R1 represents an optionally substituted hydrocarbon group; and R2 and R3 each independently represents hydrogen, an optionally substituted hydrocarbon group or an optionally-substituted heterocyclic group, or R2 and R3 may form an optionally substituted ring in cooperation with the adjacent nitrogen atom, or a salt of the compound. The pyrrolopyridine derivative has vanilloid receptor agonist activity and is useful as medicines such as a preventive/therapeutic agent and analgesic for overactive bladder.
摘要翻译：一种新的吡咯并吡啶衍生物，其为下式表示的化合物：其中环A表示任选取代的吡啶环; X表示吸电子基团; Y表示任选取代的二价C 1-6链烃基; R1表示任选取代的烃基; 并且R 2和R 3各自独立地表示氢，任选取代的烃基或任选取代的杂环基，或者R 2和R 3可以与相邻的氮原子或化合物的盐协合形成任选取代的环。吡咯并吡啶衍生物具有香草素受体激动剂活性，并且可用作药物，例如预防/治疗剂和膀胱过度活动症的止痛剂。

9. 发明申请

US20130029969A1 HETEROCYCLIC COMPOUND 有权
公开(公告)号：US20130029969A1
公开(公告)日：2013-01-31
申请号：US13578959
申请日：2011-02-16
申请人： Misaki Homma , Toru Miyazaki , Yuya Oguro , Osamu Kurasawa
发明人： Misaki Homma , Toru Miyazaki , Yuya Oguro , Osamu Kurasawa
IPC分类号： C07D495/04 , A61P35/00 , A61K31/541 , A61K31/55 , A61K31/519 , A61K31/5377
CPC分类号： A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/55 , C07D495/04 , C07D498/20
摘要： Provided is a compound useful for the prophylaxis or treatment of cancer.The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.

10. 发明授权

US07795267B2 Bicyclic piperazine compound having TGR23 antagonistic activity 失效
标题翻译：具有TGR23拮抗活性的双环哌嗪化合物
公开(公告)号：US07795267B2
公开(公告)日：2010-09-14
申请号：US10570270
申请日：2004-08-26
申请人： Kohji Fukatsu , Yutaka Nakayama , Naoki Tarui , Masaaki Mori , Hirokazu Matsumoto , Osamu Kurasawa , Hiroshi Banno
发明人： Kohji Fukatsu , Yutaka Nakayama , Naoki Tarui , Masaaki Mori , Hirokazu Matsumoto , Osamu Kurasawa , Hiroshi Banno
IPC分类号： A61K31/4965
CPC分类号： C07D487/04 , C07D513/04
摘要： The present invention provides a compound represented by the formula: wherein R1 is —(C═O)—NR7R8 or —(C═O)—OR6, R2 is a hydrocarbon group which may be substituted or the like, R3 is a hydrocarbon group which may be substituted or the like, R4 is a hydrocarbon group which may be substituted or the like, n is from 0 to 4, and X is an oxygen atom, or a salt thereof. The invention also provides a compound which has a TGR23 antagonist activity and thus is useful for prevention and treatment of cancer.
摘要翻译：本发明提供由下式表示的化合物：其中R 1为 - （C = O）-NR 7 R 8或 - （C = O）-OR 6，R 2为可被取代的烃基等，R 3为烃基其可以被取代或类似，R 4是可以被取代的烃基等，n是0-4，X是氧原子或其盐。本发明还提供具有TGR23拮抗剂活性的化合物，因此可用于预防和治疗癌症。

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