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1. 发明申请

US20100022572A1 NOVEL SPIRO COMPOUND AND MEDICINE COMPRISING THE SAME 审中-公开
标题翻译：新型SPIRO化合物和包括其的药物
公开(公告)号：US20100022572A1
公开(公告)日：2010-01-28
申请号：US12504075
申请日：2009-07-16
申请人： Hisashi Nakashima , Takahisa Ogamino , Takaaki Araki , Noriaki Gomi , Yasushi Kaneko , Kazutoyo Abe , Tadaaki Ohgiya , Kimiyuki Shibuya
发明人： Hisashi Nakashima , Takahisa Ogamino , Takaaki Araki , Noriaki Gomi , Yasushi Kaneko , Kazutoyo Abe , Tadaaki Ohgiya , Kimiyuki Shibuya
IPC分类号： A61K31/438 , C07D221/20 , A61P3/00 , A61P3/04 , A61P9/12
CPC分类号： A61K31/438 , C07D221/20 , C07D471/10
摘要： It is to provide a novel compound useful for preventing and/or treating diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome.A spiro compound represented by the following general formula (1) or salt thereof, or their solvate.
摘要翻译：提供可用于预防和/或治疗糖尿病，胰岛素抵抗，糖尿病并发症，肥胖症，血脂异常，高血压，脂肪肝或代谢综合征的新型化合物。由以下通式（1）表示的螺环化合物或其盐或其溶剂化物。

2. 发明授权

US08252781B2 1,2-diazetidin-3-one derivatives and drugs containing same 有权
标题翻译： 1,2-二氮杂环丁烷-3-酮衍生物和含有它们的药物
公开(公告)号：US08252781B2
公开(公告)日：2012-08-28
申请号：US12607650
申请日：2009-10-28
申请人： Hisashi Nakashima , Takaaki Araki , Takahisa Ogamino , Noriaki Gomi , Yasushi Kaneko , Kazutoyo Abe , Tadaaki Ohgiya
发明人： Hisashi Nakashima , Takaaki Araki , Takahisa Ogamino , Noriaki Gomi , Yasushi Kaneko , Kazutoyo Abe , Tadaaki Ohgiya
IPC分类号： C07D229/00 , C07D409/04 , C07D405/12 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , A61K31/397 , A61K31/4427 , A61K31/498 , A61P9/12 , A61P3/10 , A61P3/04 , A61P3/06
CPC分类号： C07D229/00 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/04 , C07D405/06 , C07D409/04
摘要： [Object]It is to provide a novel compound useful for preventing and/or treating diseases that involves 11β-hydroxysteroid dehydrogenase 1 (in particular diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome).[Means to Solve the Object]A 1,2-diazetidin-3-one derivative represented by the following general formula (1) or salt thereof, or their solvate.
摘要翻译：提供一种可用于预防和/或治疗涉及11-羟基类固醇脱氢酶1（特别是糖尿病，胰岛素抵抗，糖尿病并发症，肥胖，血脂异常，高血压，脂肪肝或代谢综合征）的疾病的新化合物。。解决对象的方法由下述通式（1）表示的1,2-二氮杂环丁-3-酮衍生物或其盐或其溶剂化物。

3. 发明申请

US20100144694A1 1,2-DIAZETIDIN-3-ONE DERIVATIVES AND DRUGS CONTAINING SAME 有权
标题翻译： 1,2-DIAZETIDIN-3-ONE衍生物和含有其的药物
公开(公告)号：US20100144694A1
公开(公告)日：2010-06-10
申请号：US12607650
申请日：2009-10-28
申请人： Hisashi Nakashima , Takaaki Araki , Takahisa Ogamino , Noriaki Gomi , Yasushi Kaneko , Kazutoyo Abe , Tadaaki Ohgiya
发明人： Hisashi Nakashima , Takaaki Araki , Takahisa Ogamino , Noriaki Gomi , Yasushi Kaneko , Kazutoyo Abe , Tadaaki Ohgiya
IPC分类号： A61K31/397 , C07D229/00 , A61P3/04 , A61P3/10
CPC分类号： C07D229/00 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/04 , C07D405/06 , C07D409/04
摘要： [Object]It is to provide a novel compound useful for preventing and/or treating diseases that involves 11β-hydroxysteroid dehydrogenase 1 (in particular diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome).[Means to Solve the Object]A 1,2-diazetidin-3-one derivative represented by the following general formula (1) or salt thereof, or their solvate.
摘要翻译：提供一种可用于预防和/或治疗涉及11-羟基类固醇脱氢酶1（特别是糖尿病，胰岛素抵抗，糖尿病并发症，肥胖，血脂异常，高血压，脂肪肝或代谢综合征）的疾病的新化合物。。解决对象的方法由下述通式（1）表示的1,2-二氮杂环丁-3-酮衍生物或其盐或其溶剂化物。

4. 发明申请

US20100075943A1 1-ADAMANTYLAZETIDIN-2-ONE DERIVATIVES AND DRUGS CONTAINING SAME 有权
标题翻译： 1-ADAMANTYLAZETIDIN-2-ONE衍生物和含有其的药物
公开(公告)号：US20100075943A1
公开(公告)日：2010-03-25
申请号：US12550206
申请日：2009-08-28
申请人： Hisashi Nakashima , Takahiro Mori , Takaaki Araki , Takahisa Ogamino , Kazutoyo Abe , Tadaaki Ohgiya , Ryoko Mori
发明人： Hisashi Nakashima , Takahiro Mori , Takaaki Araki , Takahisa Ogamino , Kazutoyo Abe , Tadaaki Ohgiya , Ryoko Mori
IPC分类号： A61K31/397 , C07D205/04 , A61P3/00
CPC分类号： C07D205/08 , A61K31/397 , C07D401/04 , C07D401/08 , C07D405/04
摘要： It is to provide a novel compound useful for preventing and/or treating diseases that involves 11β-hydroxysteroid dehydrogenase 1, particularly diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome. It is an 1-adamantyl azetidin-2-one derivative represented by the following general formula (1) or salt thereof, or their solvate. [wherein A ring represents C6-10 aryl group, 5- to 14-membered heteroaryl group, R1 is a hydrogen atom, halogen atom, C1-6 alkoxycarbonyl group, hydroxyl group, carboxyl group or carbamoyl group; R2 and R3 are the same or different and are a C1-6 alkyl group; R4, R5, and R6 are same or different, and are a hydrogen atom, halogen atom, C1-6 alkyl group, C1-6 alkoxy group, C6-10 aryl group, or R4 and R5, or R5 and R6 may together form a C1-3 alkylenedioxy group, R7 and R8 are the same of different and represent a hydrogen atom or C1-6 alkyl group, or may together form a C3-6 cyclic hydrocarbon group, n represents an integer of 0 or 1]
摘要翻译：提供一种可用于预防和/或治疗涉及11-羟基类固醇脱氢酶1，特别是糖尿病，胰岛素抵抗，糖尿病并发症，肥胖，血脂异常，高血压，脂肪肝或代谢综合征的疾病的新化合物。它是由以下通式（1）表示的1-金刚烷基氮杂环丁-2-酮衍生物或其盐或其溶剂合物。 [其中A环表示C6-10芳基，5〜14元杂芳基，R1表示氢原子，卤素原子，C1-6烷氧基羰基，羟基，羧基或氨基甲酰基。 R2和R3相同或不同，为C1-6烷基; R 4，R 5和R 6相同或不同，为氢原子，卤素原子，C 1-6烷基，C 1-6烷氧基，C 6-10芳基或R 4和R 5，或者R 5和R 6可以一起形成 C 1-3亚烷基二氧基，R 7和R 8相同，表示氢原子或C 1-6烷基，或一起形成C 3-6环烃基，n表示0或1的整数]

5. 发明授权

US08236789B2 1-adamantyl azetidin-2-one derivatives and drugs containing same 有权
标题翻译： 1-金刚烷基氮杂环丁烷-2-酮衍生物和含有它们的药物
公开(公告)号：US08236789B2
公开(公告)日：2012-08-07
申请号：US12550206
申请日：2009-08-28
申请人： Hisashi Nakashima , Takahiro Mori , Ryoko Mori, legal representative , Takaaki Araki , Takahisa Ogamino , Kazutoyo Abe , Tadaaki Ohgiya
发明人： Hisashi Nakashima , Takahiro Mori , Takaaki Araki , Takahisa Ogamino , Kazutoyo Abe , Tadaaki Ohgiya
IPC分类号： C07D205/08 , C07D227/087 , A61K31/397 , A61K31/4427 , A61K31/443 , A61K31/4725 , A61P3/10 , A61P3/04 , A61P9/12 , A61P3/06
CPC分类号： C07D205/08 , A61K31/397 , C07D401/04 , C07D401/08 , C07D405/04
摘要： It is to provide a novel compound useful for preventing and/or treating diseases that involves 11β-hydroxysteroid dehydrogenase 1, particularly diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome. It is an 1-adamantyl azetidin-2-one derivative represented by the following general formula (1) or salt thereof, or their solvate. [wherein A ring represents C6-10 aryl group, 5- to 14-membered heteroaryl group, R1 is a hydrogen atom, halogen atom, C1-6 alkoxycarbonyl group, hydroxyl group, carboxyl group or carbamoyl group; R2 and R3 are the same or different and are a C1-6 alkyl group; R4, R5, and R6 are same or different, and are a hydrogen atom, halogen atom, C1-6 alkyl group, C1-6 alkoxy group, C6-10 aryl group, or R4 and R5, or R5 and R6 may together form a C1-3 alkylenedioxy group, R7 and R8 are the same of different and represent a hydrogen atom or C1-6 alkyl group, or may together form a C3-6 cyclic hydrocarbon group, n represents an integer of 0 or 1].
摘要翻译：提供一种可用于预防和/或治疗涉及11-羟基类固醇脱氢酶1，特别是糖尿病，胰岛素抵抗，糖尿病并发症，肥胖，血脂异常，高血压，脂肪肝或代谢综合征的疾病的新型化合物。它是由以下通式（1）表示的1-金刚烷基氮杂环丁-2-酮衍生物或其盐或其溶剂合物。 [其中A环表示C6-10芳基，5〜14元杂芳基，R1表示氢原子，卤素原子，C1-6烷氧基羰基，羟基，羧基或氨基甲酰基。 R2和R3相同或不同，为C1-6烷基; R 4，R 5和R 6相同或不同，为氢原子，卤素原子，C 1-6烷基，C 1-6烷氧基，C 6-10芳基或R 4和R 5，或者R 5和R 6可以一起形成 C 1-3亚烷基二氧基，R 7和R 8相同，表示氢原子或C 1-6烷基，或一起形成C 3-6环烃基，n表示0或1的整数]。

6. 发明授权

US09045460B2 Production method for isoquinoline derivatives and salts thereof 有权
标题翻译：异喹啉衍生物及其盐的制备方法
公开(公告)号：US09045460B2
公开(公告)日：2015-06-02
申请号：US13816534
申请日：2011-08-25
申请人： Noriaki Gomi , Tadaaki Ohgiya , Kimiyuki Shibuya
发明人： Noriaki Gomi , Tadaaki Ohgiya , Kimiyuki Shibuya
IPC分类号： C07D401/12 , C07D243/08
CPC分类号： C07D401/12 , C07D243/08
摘要： The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.
摘要翻译：本发明提供一种能够工业生产目标产物的方法，即由上述式（I）表示的化合物或其盐，其可用于预防和治疗脑梗塞，脑出血，蛛网膜下腔出血等脑血管疾病，脑水肿，特别是预防和治疗青光眼，即使大规模高产，也不会对环境造成负面影响。本发明提供一种由式（I）表示的化合物或其盐的制备方法，其中所述方法包括使式（III）表示的化合物或其盐与式（II）表示的化合物反应的步骤，在选自腈溶剂，酰胺溶剂，亚砜溶剂和尿素溶剂中的至少一种溶剂和碱存在下进行。

7. 发明申请

US20130144054A1 NOVEL PRODUCTION METHOD FOR ISOQUINOLINE DERIVATIVES AND SALTS THEREOF 有权
公开(公告)号：US20130144054A1
公开(公告)日：2013-06-06
申请号：US13816534
申请日：2011-08-25
申请人： Noriaki Gomi , Tadaaki Ohgiya , Kimiyuki Shibuya
发明人： Noriaki Gomi , Tadaaki Ohgiya , Kimiyuki Shibuya
IPC分类号： C07D401/12 , C07D243/08
CPC分类号： C07D401/12 , C07D243/08
摘要： The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base.

8. 发明申请

US20120122906A1 NOVEL SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL PRODUCT CONTAINING SAME 审中-公开
标题翻译：新型磺酰胺衍生物和含有其的药物产品
公开(公告)号：US20120122906A1
公开(公告)日：2012-05-17
申请号：US13384519
申请日：2010-08-27
申请人： Toru Miura , Kazuhiro Onogi , Noriaki Gomi , Takaaki Araki , Junya Tagashira , Ryohei Sekimoto , Rio Ishida , Hitomi Aoki , Tadaaki Ohgiya
发明人： Toru Miura , Kazuhiro Onogi , Noriaki Gomi , Takaaki Araki , Junya Tagashira , Ryohei Sekimoto , Rio Ishida , Hitomi Aoki , Tadaaki Ohgiya
IPC分类号： A61K31/513 , A61P9/00 , A61P3/10 , A61P9/10 , A61P13/12 , A61P3/00 , C07D403/04 , A61P9/12
CPC分类号： C07D403/04
摘要： Disclosed is a novel compound which has both angiotensin II receptor antagonist activity and PPARγ activating activity, and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, kidney diseases, arteriosclerosis, inflammatory diseases, type 2 diabetes, diabetic complication, insulin resistant syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. Also disclosed is a pharmaceutical composition which contains the novel compound. Specifically disclosed are: a sulfonamide derivative represented by general formula (I), a salt thereof, or a solvate of the derivative or salt; and a pharmaceutical composition which contains the sulfonamide derivative, a salt thereof, or a solvate of the derivative or salt. (In the formula, R1 represents a C1-6 alkyl group; R2 and R3 each represents a C1-6 alkyl group or the like; and R4 represents a hydrogen atom, a C1-6 alkyl group, a C1-6 alkanoyl group or a C3-8 cycloalkylcarbonyl group.)
摘要翻译：公开了具有血管紧张素II受体拮抗剂活性和PPARγ活化活性两者的新型化合物，可用作高血压，心脏病，心绞痛，脑血管障碍，脑循环障碍，缺血性外周循环障碍等的预防和/ 肾脏疾病，动脉硬化，炎性疾病，2型糖尿病，糖尿病并发症，胰岛素抵抗综合征，X综合征，代谢综合征和高胰岛素血症。还公开了含有新化合物的药物组合物。具体公开的是：由通式（I）表示的磺酰胺衍生物，其盐或衍生物或盐的溶剂合物; 以及含有磺酰胺衍生物，其盐或衍生物或盐的溶剂合物的药物组合物。（式中，R1表示碳原子数1〜6的烷基，R2，R3各自表示C1-6烷基等，R4表示氢原子，C1-6烷基，C1-6烷酰基或 C3-8环烷基羰基）

9. 发明申请

US20130225618A1 AGENT FOR INHIBITING EXPRESSION OF LIPID METABOLISM RELATED MRNA 审中-公开
公开(公告)号：US20130225618A1
公开(公告)日：2013-08-29
申请号：US13824782
申请日：2011-10-03
申请人： Kimiyuki Shibuya , Tadaaki Ohgiya , Takeshi Murakami
发明人： Kimiyuki Shibuya , Tadaaki Ohgiya , Takeshi Murakami
IPC分类号： A61K31/505
CPC分类号： A61K31/505 , C07D239/47
摘要： The present invention is intended to provide a pharmaceutical product for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the present invention is also intended to provide a preventive and/or therapeutic agent for various diseases based on inhibition of expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and the present invention relates to an agent for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and relates also to a preventive and/or therapeutic agent for various diseases based on the inhibition of the expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the agent comprising a compound represented by Formula (I), its salt, or a solvate of any of them as an active ingredient: wherein the symbols are the same as those given in the description.

10. 发明授权

US08012989B2 Substituted pyrimidine compounds and their utility as CETP inhibitors 有权
标题翻译：取代的嘧啶化合物及其作为CETP抑制剂的用途
公开(公告)号：US08012989B2
公开(公告)日：2011-09-06
申请号：US12815905
申请日：2010-06-15
申请人： Tadaaki Ohgiya , Toru Miura , Ayumu Okuda , Toshiharu Arai , Koichi Yamazaki , Taro Aoki , Katsutoshi Miyosawa , Haruki Shibata , Kimiyuki Shibuya
发明人： Tadaaki Ohgiya , Toru Miura , Ayumu Okuda , Toshiharu Arai , Koichi Yamazaki , Taro Aoki , Katsutoshi Miyosawa , Haruki Shibata , Kimiyuki Shibuya
IPC分类号： A61K31/505
CPC分类号： C07D401/12 , C07D403/12 , C07D471/04
摘要： A compound represented by the following general formula (I), wherein R1, R2, R3, R4 and R5 represent hydrogen atom, a halogen atom, a lower alkyl group and the like, R6 represents an alkyl group, a cycloalkyl group and the like, R7 and R8 represent hydrogen atom, a lower alkyl group, a (lower cycloalkyl)(lower alkyl) group and the like, R9 represents hydrogen atom, a halogen atom, a lower alkoxy group and the like, R10 and R11 represent hydrogen atom, a lower alkyl group, a lower alkoxy group, a halo(lower alkyl) group and the like, and A represents a heterocyclic ring constituted by 6 to 10 atoms, which has potent inhibitory activity on cholesterol ester transfer protein (CETP).
摘要翻译：由下列通式（I）表示的化合物，其中R 1，R 2，R 3，R 4和R 5表示氢原子，卤原子，低级烷基等，R 6表示烷基，环烷基等，R7和R8表示氢原子，低级烷基，（低级环烷基）（低级烷基）等，R9表示氢原子，卤素原子，低级烷氧基等，R10和R11表示氢原子，低级烷基，低级烷氧基，卤代（低级烷基）等，A表示6〜10个原子构成的杂环，对胆固醇酯转移蛋白（CETP）具有有效的抑制活性。

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