首页> 外国专利> New 2-pyridin-2-yl-pyrazol-3(2H)-one compounds are hypoxia inducible factor activators, useful for the treatment of hypertension, heart failure, diabetes, anemia, angina pectoris or myocardial infarction and pulmonary hypertension

New 2-pyridin-2-yl-pyrazol-3(2H)-one compounds are hypoxia inducible factor activators, useful for the treatment of hypertension, heart failure, diabetes, anemia, angina pectoris or myocardial infarction and pulmonary hypertension

机译：新的2-吡啶-2-基-吡唑-3（2H）-一化合物是缺氧诱导因子激活剂，可用于治疗高血压，心力衰竭，糖尿病，贫血，心绞痛或心肌梗塞和肺动脉高压

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摘要

2-Pyridin-2-yl-pyrazol-3(2H)-one compounds (I) and their base or acid addition salts are new. 2-Pyridin-2-yl-pyrazol-3(2H)-one compounds of formula (I) and their base or acid addition salts are new. n : 1-4; m, o : 0 or 1; X : -CHR1a-, -NHR1a-, or heteroatom comprising O or S; R1a : 1-5C alkyl, 1-5C alkoxy, -CH 2-aryl, -COR 5 or -COOR 5; R 1 : oxo; R 2 : H, 1-5C alkyl, 1-5C alkoxy, -COOR 5, NR 5R 6, CONR 5R 6, or SO 2NR 3R 4; either R 3, R 4 : H, 1-5C alkyl, 3-6C cycloalkyl, (hetero)aryl, -CH 2-heteroaryl, -1-5C alkyl-NR 5R 6; or NR 3R 4 : heterocycloalkyl optionally substituted by 1-5C alkyl or -CH 2-aryl; and R 5, R 6 : H or 1-5C alkyl. Independent claims are included for: (1) the preparation of (I); (2) a combination of (I) with other active compounds useful in the treatment of hypertension, heart failure, diabetes and anemia; and (3) phenyl-hydrazine ester compounds of formula (IVa) or (IVb). [Image] [Image] ACTIVITY : Cardiovascular-Gen.; Vasotropic; Cardiant; Antianginal; Antiarteriosclerotic; Cerebroprotective; Hypotensive; Respiratory-Gen.; Antidiabetic; Antianemic; Ophthalmological; Nephrotropic; Neuroprotective. MECHANISM OF ACTION : Hypoxia inducible factor (HIF) activator. Tests details are described but no results given.

机译：2-吡啶-2-基-吡唑-3（2H）-一化合物（I）及其碱或酸加成盐是新的。式（I）的2-吡啶-2-基-吡唑-3（2H）-一化合物及其碱或酸加成盐是新的。 n：1-4; m，o：0或1; X：-CHR1a-，-NHR1a-或包含O或S的杂原子; R1a：1-5C烷基，1-5C烷氧基，-CH 2-芳基，-COR 5>或-COOR 5>; R 1>：氧代; R 2>：H，1-5C烷基，1-5C烷氧基，-COOR 5>，NR 5> R 6>，CONR 5> R 6>或SO 2NR 3> R 4>; R 3>，R 4>：H，1-5C烷基，3-6C环烷基，（杂）芳基，-CH 2杂芳基，-1-5C烷基-NR 5> R 6>;或NR 3＞ R 4＞：任选被1-5C烷基或-CH 2-芳基取代的杂环烷基;或R 5>，R 6>：H或1-5C的烷基。独立索赔包括：（1）（I）的制备; （2）（I）与可用于治疗高血压，心力衰竭，糖尿病和贫血的其他活性化合物的组合; （3）式（IVa）或（IVb）的苯基肼酯化合物。 [图像] [图像]活动：心血管创。变压性卡迪恩抗心绞痛抗动脉硬化;脑保护降压;呼吸器;抗糖尿病抗贫血;眼科嗜肾具有神经保护作用。作用机理：缺氧诱导因子（HIF）激活剂。描述了测试细节，但未给出结果。

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公开/公告号FR2940652A1

专利类型
公开/公告日2010-07-02

原文格式PDF
申请/专利权人 SANOFI AVENTIS;
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申请/专利号FR20080007475
发明设计人 ALTENBURGER JEAN MICHEL;FOSSEY VALERIE;ILLIANO STEPHANE;MANETTE GERALDINE;
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申请日2008-12-29
分类号C07D495/04;C07D471/04;C07D401/14;C07D401/04;C07D333/38;C07D231/56;C07D231/54;C07D231/08;C07D213/77;C07D211/96;C07D211/78;A61K31/4162;A61K31/4427;A61K31/4152;A61P27/06;A61P25/28;A61P17/02;A61P13/12;A61P9;A61P7/06;A61P7;A61P3/10;
国家 FR
入库时间 2022-08-21 18:26:38

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