NOVEL PHENYLPYRIDINE DERIVATIVE AND DRUG CONTAINING SAME
    1.
    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

    IPC分类号: C07D413/14 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
    2.
    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

    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
    4.
    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

    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。

    Compound having 3-heteroarylpyrimidin-4-(3H)-one structure and pharmaceutical preparation containing same
    5.
    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

    IPC分类号: C07D401/14 A61K31/506

    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。]