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1. 发明授权

US08063034B2 Oxadiazole derivatives and thiadiazole derivatives having neovascularization inhibitory activity 失效
标题翻译：具有新血管形成抑制活性的恶二唑衍生物和噻二唑衍生物
公开(公告)号：US08063034B2
公开(公告)日：2011-11-22
申请号：US12449159
申请日：2008-01-29
申请人： Takahiro Honda , Koushi Fujisawa , Hiroyuki Aono , Masakazu Ban
发明人： Takahiro Honda , Koushi Fujisawa , Hiroyuki Aono , Masakazu Ban
IPC分类号： A61K31/397 , A61K31/4245 , C07D271/07 , C07D413/08
CPC分类号： C07D285/135 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to Compounds represented by the formula (I) or salts thereof. In the formula (I), the ring A represents a benzene ring, a thiophene ring, or a pyridine ring; Ra represents a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group; the ring B represents a pyridine ring, a pyrimidine ring, or a quinoline ring; the ring C represents a benzene ring; a pyridine ring, a quinoline ring, or an isoquinoline ring; X and Y, the same or different, represent an oxygen atom or a sulfur atom, with the proviso that the case X is a sulfur atom and Y is an oxygen atom be excluded; R1 represents a hydrogen atom, a halogen atom, an amino group, a cycloalkylamino group, an alkylcarbonylamino group, an alkyloxycarbonylamino group, an alkylaminocarbonyl group, or a non-aromatic heterocyclic group; and R2 and R2′, the same or different, represent a hydrogen atom, a halogen atom, an alkyl group, a halogeno-alkyl group, or a halogeno-alkoxy group.
摘要翻译：本发明涉及由式（I）表示的化合物或其盐。在式（I）中，环A表示苯环，噻吩环或吡啶环; Ra表示氢原子，卤素原子，烷基或烷氧基; 环B表示吡啶环，嘧啶环或喹啉环; 环C表示苯环; 吡啶环，喹啉环或异喹啉环; X和Y相同或不同，表示氧原子或硫原子，条件是情况X为硫原子，Y为氧原子排除; R1表示氢原子，卤素原子，氨基，环烷基氨基，烷基羰基氨基，烷氧基羰基氨基，烷基氨基羰基或非芳香族杂环基; 和R2和R2'相同或不同，表示氢原子，卤素原子，烷基，卤代烷基或卤代 - 烷氧基。

2. 发明申请

US20100016354A1 NOVEL OXADIAZOLE DERIVATIVES AND THIADIAZOLE DERIVATIVES HAVING NEOVASCULARIZATION INHIBITORY ACTIVITY 失效
标题翻译：新型氧化氮衍生物和具有新鲜血液活性抑制活性的噻唑衍生物
公开(公告)号：US20100016354A1
公开(公告)日：2010-01-21
申请号：US12449159
申请日：2008-01-29
申请人： Takahiro Honda , Koushi Fujisawa , Hiroyuki Aono , Masakazu Ban
发明人： Takahiro Honda , Koushi Fujisawa , Hiroyuki Aono , Masakazu Ban
IPC分类号： A61K31/4725 , C07D413/12 , A61K31/4439 , C07D413/14 , A61K31/444 , A61P35/00 , A61P3/10 , A61P19/02
CPC分类号： C07D285/135 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to Compounds represented by the formula (I) or salts thereof. In the formula (I), the ring A represents a benzene ring, a thiophene ring, or a pyridine ring; Ra represents a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group; the ring B represents a pyridine ring, a pyrimidine ring, or a quinoline ring; the ring C represents a benzene ring; a pyridine ring, a quinoline ring, or an isoquinoline ring; X and Y, the same or different, represent an oxygen atom or a sulfur atom, with the proviso that the case X is a sulfur atom and Y is an oxygen atom be excluded; R1 represents a hydrogen atom, a halogen atom, an amino group, a cycloalkylamino group, an alkylcarbonylamino group, an alkyloxycarbonylamino group, an alkylaminocarbonyl group, or a non-aromatic heterocyclic group; and R2 and R2′, the same or different, represent a hydrogen atom, a halogen atom, an alkyl group, a halogeno-alkyl group, or a halogeno-alkoxy group.
摘要翻译：本发明涉及由式（I）表示的化合物或其盐。在式（I）中，环A表示苯环，噻吩环或吡啶环; Ra表示氢原子，卤素原子，烷基或烷氧基; 环B表示吡啶环，嘧啶环或喹啉环; 环C表示苯环; 吡啶环，喹啉环或异喹啉环; X和Y相同或不同，表示氧原子或硫原子，条件是情况X为硫原子，Y为氧原子排除; R1表示氢原子，卤素原子，氨基，环烷基氨基，烷基羰基氨基，烷氧基羰基氨基，烷基氨基羰基或非芳香族杂环基; 和R2和R2'相同或不同，表示氢原子，卤素原子，烷基，卤代烷基或卤代 - 烷氧基。

3. 发明申请

US20100056522A1 INTRAOCULAR PRESSURE-LOWERING AGENT COMPRISING COMPOUND HAVING HISTONE DEACETYLASE INHIBITOR EFFECT AS ACTIVE INGREDIENT 审中-公开
标题翻译：含有HISTONE脱乙酰壳多糖酶抑制剂作为活性成分的化合物的内用降压药物
公开(公告)号：US20100056522A1
公开(公告)日：2010-03-04
申请号：US12450388
申请日：2008-03-28
申请人： Shinji Yoneda , Koushi Fujisawa , Katsuhiko Watanabe , Junko Fujikawa , Atsushi Shimazaki , Tomoko Kirihara , Hisashi Tajima
发明人： Shinji Yoneda , Koushi Fujisawa , Katsuhiko Watanabe , Junko Fujikawa , Atsushi Shimazaki , Tomoko Kirihara , Hisashi Tajima
IPC分类号： A61K31/165 , C07C237/20 , C07C311/21 , C07D207/337 , C07D407/06 , C07D213/55 , C07D471/04 , C07D401/04 , C07D213/81 , C07D413/12 , A61K31/167 , A61K31/18 , A61K31/40 , A61K31/336 , A61K31/44 , A61K31/4353 , A61K31/506 , A61K31/5377 , A61P27/02
CPC分类号： C07D213/81 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/5377 , C07D207/333 , C07D211/32 , C07D401/04 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
摘要： An object of the present invention is to find a novel pharmacological effect of a compound having an HDAC inhibitory effect. The compound having an HDAC inhibitory effect of the invention has an excellent effect of cell morphological change on trabecular meshwork cells and/or effect of intraocular pressure reduction, and is therefore useful as a preventive and/or therapeutic agent for a disease considered to be associated with aqueous humor circulation and/or intraocular pressure, particularly as a preventive and/or therapeutic agent for glaucoma or ocular hypertension.
摘要翻译：本发明的目的在于找到具有HDAC抑制作用的化合物的新药理作用。具有本发明的HDAC抑制作用的化合物对小梁网细胞的细胞形态学变化和/或眼内压降低的效果具有优异的效果，因此可用作被认为相关的疾病的预防和/或治疗剂具有房水循环和/或眼内压，特别是作为青光眼或高眼压症的预防和/或治疗剂。

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