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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。

3. 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。

4. 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]。

5. 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]

6. 发明授权

US07183295B2 PPAR-activating compound and pharmaceutical composition comprising the compound 有权
标题翻译： PPAR活化化合物和包含该化合物的药物组合物
公开(公告)号：US07183295B2
公开(公告)日：2007-02-27
申请号：US11407076
申请日：2006-04-20
申请人： Yukiyoshi Yamazaki , Tsutomu Toma , Masahiro Nishikawa , Hidefumi Ozawa , Ayumu Okuda , Takaaki Araki , Kazutoyo Abe , Soichi Oda
发明人： Yukiyoshi Yamazaki , Tsutomu Toma , Masahiro Nishikawa , Hidefumi Ozawa , Ayumu Okuda , Takaaki Araki , Kazutoyo Abe , Soichi Oda
IPC分类号： A61K31/4439 , C07D413/12 , C07D411/12 , C07D401/12
CPC分类号： C07D413/12 , C07D263/58
摘要： A compound represented by the following formula (1): (wherein each of R1 and R2, which may be identical to or different from each other, represents a hydrogen atom, a methyl group, or an ethyl group; each of R3a, R3b, R4a, and R4b, which may be identical to or different from each other, represents a hydrogen atom, a halogen atom, a nitro group, a hydroxyl group, a C1-4 alkyl group, a trifluoromethyl group, a C1-4 alkoxy group, a C1-4 alkylcarbonyloxy group, a di-C1-4 alkylamino group, a C1-4 alkylsulfonyloxy group, a C1-4 alkylsulfonyl group, a C1-4 alkylsulfinyl group, or a C1-4 alkylthio group, or R3a and R3b, or R4a and R4b may be linked together to form an alkylenedioxy group; X represents an oxygen atom, a sulfur atom, or N—R5 (R5 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkylsulfonyl group, or a C1-4 alkyloxycarbonyl group); Y represents an oxygen atom, S(O)l (l is a number of 0 to 2), a carbonyl group, a carbonylamino group, an aminocarbonyl group, a sulfonylamino group, or an aminosulfonyl group; Z represents CH or N; n is a number of 1 to 6; and m is a number of 2 to 6) or a salt thereof; and therapeutic drugs containing any of such a compound or salt.
摘要翻译：由下式（1）表示的化合物：其中R 1和R 2各自可以相同或不同，表示氢原子，甲基或乙基; R 3a，R 3b，R 4a和R 4b中的每一个，它们可以相同或不同，表示氢原子，卤素原子，硝基，羟基，C 1-4烷基，三氟甲基， C 1-4烷氧基，C 1-4烷基羰基氧基，二-C 1-4烷基氨基，C 1 -C 4烷基氨基， C 1-4烷基磺酰氧基，C 1-4烷基磺酰基，C 1-4烷基亚磺酰基或C 1〜 4个烷硫基或R 3a和R 3b，或R 4a和R 4b可以是连接在一起形成亚烷基二氧基; X表示氧原子，硫原子或NR 5（R 5）表示氢原子，C

7. 发明授权

US07109226B2 PPAR-activating compound and pharmaceutical composition comprising the compound 有权
标题翻译： PPAR活化化合物和包含该化合物的药物组合物
公开(公告)号：US07109226B2
公开(公告)日：2006-09-19
申请号：US10933467
申请日：2004-09-03
申请人： Yukiyoshi Yamazaki , Tsutomu Toma , Masahiro Nishikawa , Hidefumi Ozawa , Ayumu Okuda , Takaaki Araki , Kazutoyo Abe , Soichi Oda
发明人： Yukiyoshi Yamazaki , Tsutomu Toma , Masahiro Nishikawa , Hidefumi Ozawa , Ayumu Okuda , Takaaki Araki , Kazutoyo Abe , Soichi Oda
IPC分类号： A61K31/423 , C07D263/58
CPC分类号： C07D413/12 , C07D263/58
摘要： A compound represented by the following formula (1): Or a salt thereof; and therapeutic durgs containing the compound. The compound selectively activates PPARα.
摘要翻译：由下式（1）表示的化合物：或其盐; 和含有该化合物的治疗剂。该化合物选择性地激活PPARα。

8. 发明申请

US20060189667A1 PPAR-activating compound and pharmaceutical composition comprising the compound 有权
标题翻译： PPAR活化化合物和包含该化合物的药物组合物
公开(公告)号：US20060189667A1
公开(公告)日：2006-08-24
申请号：US11407076
申请日：2006-04-20
申请人： Yukiyoshi Yamazaki , Tsutomu Toma , Masahiro Nishikawa , Hidefumi Ozawa , Ayumu Okuda , Takaaki Araki , Kazutoyo Abe , Soichi Oda
发明人： Yukiyoshi Yamazaki , Tsutomu Toma , Masahiro Nishikawa , Hidefumi Ozawa , Ayumu Okuda , Takaaki Araki , Kazutoyo Abe , Soichi Oda
IPC分类号： A61K31/428 , A61K31/423
CPC分类号： C07D413/12 , C07D263/58
摘要： A compound represented by the following formula (1): (wherein each of R1 and R2, which may be identical to or different from each other, represents a hydrogen atom, a methyl group, or an ethyl group; each of R3a, R3b, R4a, and R4b, which may be identical to or different from each other, represents a hydrogen atom, a halogen atom, a nitro group, a hydroxyl group, a C1-4 alkyl group, a trifluoromethyl group, a C1-4 alkoxy group, a C1-4 alkylcarbonyloxy group, a di-C1-4 alkylamino group, a C1-4 alkylsulfonyloxy group, a C1-4 alkylsulfonyl group, a C1-4 alkylsulfinyl group, or a C1-4 alkylthio group, or R3a and R3b, or R4a and R4b may be linked together to form an alkylenedioxy group; X represents an oxygen atom, a sulfur atom, or N—R5 (R5 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkylsulfonyl group, or a C1-4 alkyloxycarbonyl group); Y represents an oxygen atom, S(O)l (l is a number of 0 to 2), a carbonyl group, a carbonylamino group, an aminocarbonyl group, a sulfonylamino group, or an aminosulfonyl group; Z represents CH or N; n is a number of 1 to 6; and m is a number of 2 to 6) or a salt thereof; and therapeutic drugs containing any of such a compound or salt.
摘要翻译：由下式（1）表示的化合物：其中R 1和R 2各自可以相同或不同，表示氢原子，甲基或乙基; R 3a，R 3b，R 4a和R 4b中的每一个，它们可以相同或不同，表示氢原子，卤素原子，硝基，羟基，C 1-4烷基，三氟甲基， C 1-4烷氧基，C 1-4烷基羰基氧基，二-C 1-4烷基氨基，C 1 -C 4烷基氨基， C 1-4烷基磺酰氧基，C 1-4烷基磺酰基，C 1-4烷基亚磺酰基或C 1〜 4个烷硫基或R 3a和R 3b，或R 4a和R 4b可以是连接在一起形成亚烷基二氧基; X表示氧原子，硫原子或NR 5（R 5）表示氢原子，C

9. 发明申请

US20050101636A1 PPAR-activating compound and pharmaceutical composition comprising the compound 有权
标题翻译： PPAR活化化合物和包含该化合物的药物组合物
公开(公告)号：US20050101636A1
公开(公告)日：2005-05-12
申请号：US10933467
申请日：2004-09-03
申请人： Yukiyoshi Yamazaki , Tsutomu Toma , Masahiro Nishikawa , Hidefumi Ozawa , Ayumu Okuda , Takaaki Araki , Kazutoyo Abe , Soichi Oda
发明人： Yukiyoshi Yamazaki , Tsutomu Toma , Masahiro Nishikawa , Hidefumi Ozawa , Ayumu Okuda , Takaaki Araki , Kazutoyo Abe , Soichi Oda
IPC分类号： A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4439 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P29/00 , C07D263/58 , C07D413/02 , C07D417/02 , C07D43/02
CPC分类号： C07D413/12 , C07D263/58
摘要： A compound represented by the following formula (1): Or a salt thereof; and therapeutic durgs containing the compound. The compound selectively activates PPARα.
摘要翻译：由下式（1）表示的化合物：或其盐; 和含有该化合物的治疗剂。该化合物选择性地激活PPARα。

10. 发明授权

US07301033B2 PPAR-activating compound 失效
标题翻译： PPAR活化化合物
公开(公告)号：US07301033B2
公开(公告)日：2007-11-27
申请号：US11335669
申请日：2006-01-20
申请人： Yukiyoshi Yamazaki , Tsutomu Toma , Masahiro Nishikawa , Hajime Yamada , Hidefumi Ozawa , Ayumu Okuda , Kazutoyo Abe
发明人： Yukiyoshi Yamazaki , Tsutomu Toma , Masahiro Nishikawa , Hajime Yamada , Hidefumi Ozawa , Ayumu Okuda , Kazutoyo Abe
IPC分类号： C07D263/58 , A61K31/423
CPC分类号： C07D263/58
摘要： The present invention provides a compound selectively activating PPARα, which is useful as a medicament. The present invention is specifically directed to a benzoic acid derivative represented by the following general formula (1): wherein A represents an oxygen atom, a nitrogen atom, or a sulfur atom; R represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkyl-alkyl group, an aryl group, an aryl-alkyl group an aryl-oxy-alkyl group, a pyridyl-alkyl group, an alkoxycarbonyl-alkyl group, or a carboxy-alkyl group; X represents an oxygen atom, an NH group, or an S(O)n group (wherein n represents an integer of 0, 1, or 2); and m represents an integer from 2 to 8; or a salt thereof. The present invention also provides a medicament comprising the benzoic acid derivative or the salt thereof as an active ingredient.
摘要翻译：本发明提供选择性活化PPARα的化合物，其可用作药物。本发明具体涉及由以下通式（1）表示的苯甲酸衍生物：其中A表示氧原子，氮原子或硫原子; R表示氢原子，烷基，烯基，炔基，环烷基，环烷基 - 烷基，芳基，芳基 - 烷基，芳氧基 - 烷基，吡啶基 - 烷基，烷氧基羰基 - 烷基或羧基 - 烷基; X表示氧原子，NH基或S（O）n N（其中n表示0,1或2的整数）; m表示2〜8的整数，或其盐。本发明还提供了包含苯甲酸衍生物或其盐作为活性成分的药物。

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