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    NOVEL SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL PRODUCT CONTAINING SAME
    1.
    发明申请
    NOVEL SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL PRODUCT CONTAINING SAME 审中-公开
    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）

    COMPOUND CONTAINING A NOVEL 4-ALKOXYPYRIMIDINE STRUCTURE AND MEDICINE CONTAINING SAME
    2.
    发明申请
    COMPOUND CONTAINING A NOVEL 4-ALKOXYPYRIMIDINE STRUCTURE AND MEDICINE CONTAINING SAME 审中-公开
    含有新型4-烷氧基嘧啶结构的化合物和含有其的药物

    公开(公告)号：US20120322819A1

    公开(公告)日：2012-12-20

    申请号：US13580056

    申请日：2011-02-25

    申请人： Toru Miura ,  Kazuhiro Onogi ,  Junya Tagashira ,  Gen Watanabe ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

    发明人： Toru Miura ,  Kazuhiro Onogi ,  Junya Tagashira ,  Gen Watanabe ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

    IPC分类号： A61K31/506 ,  C07D413/14 ,  A61P9/00 ,  A61P3/04 ,  A61P9/10 ,  A61P3/00 ,  A61P3/10 ,  C07D413/10 ,  A61P9/12

    CPC分类号： C07D413/10 ,  C07D413/14

    摘要： Disclosed is novel compound and medicinal formulation containing same, possessing both angiotensin II receptor blocking and PPARγ activation effect, of use as a medicine for prevention and/or treatment of hypertension, heart disease, angina pectoris, cerebrovascular disorder, cerebral circulatory disturbances, post-ischemic peripheral circulatory damage, renal disease, arteriosclerosis, inflammatory disorder, type 2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinaemia. Further disclosed is the general formula I (where one or both of R1 and R2 represent a C1-6 alkyl group, R3 represents a C1-6 alkyl group which may contain one or more substituent groups selected from group A, or a C3-8 cycloalkyl group which may contain one or more substituent groups selected from group B.) which represents the compound, and salts thereof, solvates thereof, and medicinal compositions containing any of these.

    摘要翻译： 公开了含有血管紧张素II受体阻断和PPARγ活化作用的新型化合物和药物制剂，用作预防和/或治疗高血压，心脏病，心绞痛，脑血管障碍，脑循环障碍， 缺血性外周循环损伤，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。 进一步公开的是通式I（其中R 1和R 2中的一个或两个表示C 1-6烷基，R 3表示可以含有一个或多个选自A组的取代基的C 1-6烷基或C 3-8 可以含有一个或多个选自B组的取代基的环烷基），其代表该化合物及其盐，其溶剂合物，以及含有这些中的任何一种的药物组合物。

    Compound having 3-heteroarylpyrimidin-4-(3H)-one structure and pharmaceutical preparation containing same
    4.
    发明授权
    Compound having 3-heteroarylpyrimidin-4-(3H)-one structure and pharmaceutical preparation containing same 失效
    具有3-杂芳基嘧啶-4-（3H） - 酮结构的化合物和含有它们的药物制剂

    公开(公告)号：US08664226B2

    公开(公告)日：2014-03-04

    申请号：US13263023

    申请日：2010-04-16

    申请人： Toru Miura ,  Kazuhiro Onogi ,  Seiichi Sato ,  Junya Tagashira ,  Gen Watanabe ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

    发明人： Toru Miura ,  Kazuhiro Onogi ,  Seiichi Sato ,  Junya Tagashira ,  Gen Watanabe ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

    IPC分类号： C07D401/14 ,  A61K31/506

    CPC分类号： C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14

    摘要： Disclosed is a compound which has both an angiotensin-II receptor antagonistic activity and a PPARγ activation 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, renal diseases, arteriosclerosis, inflammatory diseases, type-2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. [In the formula, A represents a 5- to 10-membered heteroaryl group; R1 and R2 independently represent a C1-6 alkyl group; and each of R3 to R5 is absent or represents H, a halogen atom, OH, NO2, a halo-C1-6 alkyl group, a (substituted) C1-6 alkoxy group, a (substituted) C3-6 cycloalkyloxy group, or a 5- to 10-membered heteroaryl group.]

    摘要翻译： 公开了具有血管紧张素-II受体拮抗作用和PPARγ活化活性的化合物，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的预防和/或治疗剂 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。 [式中，A表示5至10元杂芳基; R1和R2独立地表示C1-6烷基; 并且R 3至R 5不存在或表示H，卤素原子，OH，NO 2，卤代C 1-6烷基，（取代的）C 1-6烷氧基，（取代的）C 3-6环烷氧基或 5至10元杂芳基。]

    NOVEL ALPHA-PHENOXYBENZENEACETIC ACID DERIVATIVE AND PHARMACEUTICAL PREPARATION COMPRISING SAME
    5.
    发明申请
    NOVEL ALPHA-PHENOXYBENZENEACETIC ACID DERIVATIVE AND PHARMACEUTICAL PREPARATION COMPRISING SAME 审中-公开
    新型ALPHA-苯氧基苯甲酸衍生物和包含其的药物制备

    公开(公告)号：US20120046308A1

    公开(公告)日：2012-02-23

    申请号：US13318750

    申请日：2010-05-28

    申请人： Toru Miura ,  Kazuhiro Onogi ,  Junya Tagashira ,  Gen Watanabe ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

    发明人： Toru Miura ,  Kazuhiro Onogi ,  Junya Tagashira ,  Gen Watanabe ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

    IPC分类号： A61K31/506 ,  C07D401/14 ,  A61P9/00 ,  A61P9/12 ,  A61P9/10 ,  C07D239/52 ,  A61P3/10

    CPC分类号： C07D401/04 ,  C07D239/34 ,  C07D239/36 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D413/14

    摘要： An α-phenoxybenzeneacetic acid derivative represented by general formula (I), which has both an angiotensin II receptor antagonistic activity and a PPARγ activation activity and is useful as a prophylactic and/or therapeutic agent for hypertension, metabolic syndrome or the like, a salt of the derivative, or a solvate of the derivative or the salt; and a pharmaceutical composition containing the derivative, the salt or the solvate. [In the formula, Q represents a group represented by formula (II) or (III) [wherein R1 and R1′ independently represent a C1-6 alkyl group; R2 and R2′ independently represent a substituted or unsubstituted C1-6 alkyl group; R3 represents a hydrogen atom, a substituted or unsubstituted C1-6 alkyl group, or a group represented by formula (IV) [wherein X and Y independently represent CH or N; Z represents a C1-6 alkylene chain, or the like; R11 represents a hydrogen atom, a C6-10 aryl group, or the like; and m represents 0 or 1]; and R4 represents a substituted C1-6 alkyl group]; R5 and R6 independently represent a C1-6 alkyl group: R7 represents a carboxyl group, or the like; R8, R9 and R10 independently represent a hydrogen atom, a halogen atom, or the like; and n represents an integer of 1 to 3.]

    摘要翻译： 由通式（I）表示的α-苯氧基苯乙酸衍生物，其具有血管紧张素II受体拮抗作用和PPARγ活化活性，可用作高血压，代谢综合征等的预防和/或治疗剂，盐 的衍生物，或衍生物或盐的溶剂合物; 和含有该衍生物，盐或溶剂化物的药物组合物。 [式中，Q表示由式（II）或（III）表示的基团[式中，R1和R1'独立地表示C1-6烷基; R2和R2'独立地表示取代或未取代的C1-6烷基; R3表示氢原子，取代或未取代的C1-6烷基或由式（IV）表示的基团[其中X和Y独立地表示CH或N; Z表示碳原子数1〜6的亚烷基链等。 R 11表示氢原子，C 6-10芳基等; m表示0或1]; 并且R 4表示取代的C 1-6烷基]; R5和R6独立地表示C1-6烷基：R7表示羧基等; R 8，R 9和R 10独立地表示氢原子，卤素原子等; n表示1〜3的整数。

    NOVEL PHENYLPYRIDINE DERIVATIVE AND DRUG CONTAINING SAME
    6.
    发明申请
    NOVEL PHENYLPYRIDINE DERIVATIVE AND DRUG CONTAINING SAME 有权
    新颖的吡啶衍生物和含有其的药物

    公开(公告)号：US20140011823A1

    公开(公告)日：2014-01-09

    申请号：US14005046

    申请日：2012-03-13

    申请人： Toru Miura ,  Seiichi Sato ,  Hajime Yamada ,  Junya Tagashira ,  Toshiaki Watanabe ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

    发明人： Toru Miura ,  Seiichi Sato ,  Hajime Yamada ,  Junya Tagashira ,  Toshiaki Watanabe ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

    IPC分类号： C07D413/14 ,  C07D401/14

    CPC分类号： C07D413/14 ,  A61K31/506 ,  C07D401/14

    摘要： The present invention provides: a compound represented by general formula (I) below, that has both angiotensin II receptor antagonism and a PPARγ activation effect and that is useful as a preventative and/or therapeutic agent for high blood pressure, cardiac disease, arteriosclerosis, type-2 diabetes, and the like; and a drug composition containing the compound. General formula (I) (in the formula: ring A represents a pyridine ring; ring B represents a tetrazole ring or an oxadiazol-5(4H)-one ring; X represents C—R5 or a nitrogen atom; R1 represents an alkyl group; R2 represents an alkyl group or a cycloalkyl group; and R3, R4, and R5 each independently represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or similar.

    摘要翻译： 本发明提供：下述通式（I）表示的化合物，既具有血管紧张素II受体拮抗作用又具有PPARγ活化作用，可用作高血压，心脏病，动脉硬化等的预防和/或治疗剂， 2型糖尿病等; 和含有该化合物的药物组合物。 通式（I）（式中，环A表示吡啶环;环B表示四唑环或恶二唑-5（4H） - 酮环; X表示C-R5或氮原子; R1表示烷基 ; R 2表示烷基或环烷基; R 3，R 4和R 5各自独立地表示氢原子，卤素原子，烷基，烷氧基等。

    NOVEL PHENYLPYRIDINE DERIVATIVE AND MEDICINAL AGENT COMPRISING SAME
    7.
    发明申请
    NOVEL PHENYLPYRIDINE DERIVATIVE AND MEDICINAL AGENT COMPRISING SAME 有权
    新颖的苯丙氨酸衍生物和药物包括它们

    公开(公告)号：US20120165353A1

    公开(公告)日：2012-06-28

    申请号：US13394266

    申请日：2010-09-29

    申请人： Toru Miura ,  Seiichi Sato ,  Hajime Yamada ,  Junya Tagashira ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

    发明人： Toru Miura ,  Seiichi Sato ,  Hajime Yamada ,  Junya Tagashira ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

    IPC分类号： A61K31/506 ,  C07D413/14 ,  A61P9/00 ,  A61P13/12 ,  A61P3/10 ,  A61P9/10 ,  A61P9/12 ,  C07D401/14 ,  A61P3/00

    CPC分类号： C07D401/14 ,  A61K31/422 ,  A61K31/4427 ,  C07D413/14

    摘要： Disclosed are: a novel compound which has both an antagonistic activity on an angiotensin II receptor and a PPARγ-activating activity and is therefore useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, arteriosclerosis, type-2 diabetes, diabetic complications, metabolic syndrome or the like; and a pharmaceutical composition containing the compound. Specifically disclosed are: a compound represented by general formula (I) (wherein the ring A represents a pyridine ring; the ring B represents a tetrazole ring or an oxadiazol-5(4H)-one ring; X represents C—R5 or a nitrogen atom; R1 represents a C1-6 alkyl group; R2 represents a C1-6 alkyl group or a C3-8 cycloalkyl group; and R3, R4, R5 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halo-C1-6 alkyl group, or a C1-6 alkoxy group which may have a substituent), a salt of the compound, or a solvate of the compound or the salt; and a pharmaceutical composition containing the compound, the salt or the solvate.

    摘要翻译： 公开了一种对血管紧张素II受体具有拮抗作用和PPARγ活化活性的新型化合物，因此可用作高血压，心脏病，动脉硬化，2型糖尿病，糖尿病并发症的预防和/或治疗剂 ，代谢综合征等; 和含有该化合物的药物组合物。 具体公开的是：由通式（I）表示的化合物（其中环A表示吡啶环;环B表示四唑环或恶二唑-5（4H） - 酮环; X表示C-R5或氮 原子; R1表示C1-6烷基; R2表示C1-6烷基或C3-8环烷基; R3，R4，R5分别表示氢原子，卤素原子，C1-6烷基， 卤代C 1-6烷基或可具有取代基的C 1-6烷氧基），化合物的盐或化合物或其盐的溶剂合物; 和含有该化合物，该盐或溶剂化物的药物组合物。

    Phenylpyridine derivative and medicinal agent comprising same
    10.
    发明授权
    Phenylpyridine derivative and medicinal agent comprising same 有权
    苯基吡啶衍生物和含有它们的药剂

    公开(公告)号：US08778954B2

    公开(公告)日：2014-07-15

    申请号：US13394266

    申请日：2010-09-29

    申请人： Toru Miura ,  Seiichi Sato ,  Hajime Yamada ,  Junya Tagashira ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

    发明人： Toru Miura ,  Seiichi Sato ,  Hajime Yamada ,  Junya Tagashira ,  Ryohei Sekimoto ,  Rie Ishida ,  Hitomi Aoki ,  Tadaaki Ohgiya

    IPC分类号： C07D401/14 ,  A61K31/422 ,  A61K31/4427

    CPC分类号： C07D401/14 ,  A61K31/422 ,  A61K31/4427 ,  C07D413/14

    摘要： Disclosed are: a novel compound which has both an antagonistic activity on an angiotensin II receptor and a PPARγ-activating activity and is therefore useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, arteriosclerosis, type-2 diabetes, diabetic complications, metabolic syndrome or the like; and a pharmaceutical composition containing the compound. Specifically disclosed are: a compound represented by general formula (I) (wherein the ring A represents a pyridine ring; the ring B represents a tetrazole ring or an oxadiazol-5(4H)-one ring; X represents C—R5 or a nitrogen atom; R1 represents a C1-6 alkyl group; R2 represents a C1-6 alkyl group or a C3-8 cycloalkyl group; and R3, R4, R5 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halo-C1-6 alkyl group, or a C1-6 alkoxy group which may have a substituent), a salt of the compound, or a solvate of the compound or the salt; and a pharmaceutical composition containing the compound, the salt or the solvate.

    摘要翻译： 公开了一种对血管紧张素II受体具有拮抗作用和PPARγ活化活性的新型化合物，因此可用作高血压，心脏病，动脉硬化，2型糖尿病，糖尿病并发症的预防和/或治疗剂 ，代谢综合征等; 和含有该化合物的药物组合物。 具体公开的是：由通式（I）表示的化合物（其中环A表示吡啶环;环B表示四唑环或恶二唑-5（4H） - 酮环; X表示C-R5或氮 原子; R1表示C1-6烷基; R2表示C1-6烷基或C3-8环烷基; R3，R4，R5分别表示氢原子，卤素原子，C1-6烷基， 卤代C 1-6烷基或可具有取代基的C 1-6烷氧基），化合物的盐或化合物或其盐的溶剂合物; 和含有该化合物，该盐或溶剂化物的药物组合物。