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    1-ADAMANTYLAZETIDIN-2-ONE DERIVATIVES AND DRUGS CONTAINING SAME
    4.
    发明申请
    1-ADAMANTYLAZETIDIN-2-ONE DERIVATIVES AND DRUGS CONTAINING SAME 有权
    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

    Applicant: Hisashi Nakashima ,  Takahiro Mori ,  Takaaki Araki ,  Takahisa Ogamino ,  Kazutoyo Abe ,  Tadaaki Ohgiya ,  Ryoko Mori

    Inventor： Hisashi Nakashima ,  Takahiro Mori ,  Takaaki Araki ,  Takahisa Ogamino ,  Kazutoyo Abe ,  Tadaaki Ohgiya ,  Ryoko Mori

    IPC: A61K31/397 ,  C07D205/04 ,  A61P3/00

    CPC classification number: C07D205/08 ,  A61K31/397 ,  C07D401/04 ,  C07D401/08 ,  C07D405/04

    Abstract: 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]

    Abstract translation: 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]

    PPAR-activating compound and pharmaceutical composition comprising the compound
    5.
    发明授权
    PPAR-activating compound and pharmaceutical composition comprising the compound 有权
    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

    Applicant: Yukiyoshi Yamazaki ,  Tsutomu Toma ,  Masahiro Nishikawa ,  Hidefumi Ozawa ,  Ayumu Okuda ,  Takaaki Araki ,  Kazutoyo Abe ,  Soichi Oda

    Inventor： Yukiyoshi Yamazaki ,  Tsutomu Toma ,  Masahiro Nishikawa ,  Hidefumi Ozawa ,  Ayumu Okuda ,  Takaaki Araki ,  Kazutoyo Abe ,  Soichi Oda

    IPC: A61K31/4439 ,  C07D413/12 ,  C07D411/12 ,  C07D401/12

    CPC classification number: C07D413/12 ,  C07D263/58

    Abstract: 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.

    Abstract translation: 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

    PPAR-activating compound and pharmaceutical composition comprising the compound
    7.
    发明申请
    PPAR-activating compound and pharmaceutical composition comprising the compound 有权
    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

    Applicant: Yukiyoshi Yamazaki ,  Tsutomu Toma ,  Masahiro Nishikawa ,  Hidefumi Ozawa ,  Ayumu Okuda ,  Takaaki Araki ,  Kazutoyo Abe ,  Soichi Oda

    Inventor： Yukiyoshi Yamazaki ,  Tsutomu Toma ,  Masahiro Nishikawa ,  Hidefumi Ozawa ,  Ayumu Okuda ,  Takaaki Araki ,  Kazutoyo Abe ,  Soichi Oda

    IPC: A61K31/428 ,  A61K31/423

    CPC classification number: C07D413/12 ,  C07D263/58

    Abstract: 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.

    Abstract translation: 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

    PPAR-activating compound
    9.
    发明授权
    PPAR-activating compound 失效
    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

    Applicant: Yukiyoshi Yamazaki ,  Tsutomu Toma ,  Masahiro Nishikawa ,  Hajime Yamada ,  Hidefumi Ozawa ,  Ayumu Okuda ,  Kazutoyo Abe

    Inventor： Yukiyoshi Yamazaki ,  Tsutomu Toma ,  Masahiro Nishikawa ,  Hajime Yamada ,  Hidefumi Ozawa ,  Ayumu Okuda ,  Kazutoyo Abe

    IPC: C07D263/58 ,  A61K31/423

    CPC classification number: C07D263/58

    Abstract: 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.

    Abstract translation: 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。

    1-adamantyl azetidin-2-one derivatives and drugs containing same
    10.
    发明授权
    1-adamantyl azetidin-2-one derivatives and drugs containing same 有权
    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

    Applicant: Hisashi Nakashima ,  Takahiro Mori ,  Ryoko Mori, legal representative ,  Takaaki Araki ,  Takahisa Ogamino ,  Kazutoyo Abe ,  Tadaaki Ohgiya

    Inventor： Hisashi Nakashima ,  Takahiro Mori ,  Takaaki Araki ,  Takahisa Ogamino ,  Kazutoyo Abe ,  Tadaaki Ohgiya

    IPC: C07D205/08 ,  C07D227/087 ,  A61K31/397 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4725 ,  A61P3/10 ,  A61P3/04 ,  A61P9/12 ,  A61P3/06

    CPC classification number: C07D205/08 ,  A61K31/397 ,  C07D401/04 ,  C07D401/08 ,  C07D405/04

    Abstract: 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].

    Abstract translation: 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]。

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