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    • 4. 发明申请
    • Novel Pyrrole Derivatives with Angiotensin II Antagonist Activity
    • 新型吡咯衍生物与血管紧张素II拮抗剂活性
    • US20070244170A1
    • 2007-10-18
    • US11568362
    • 2005-04-27
    • Francesco MakovecRoberto ArtusiAntonio GiordaniSimona ZanzolaLucio Rovati
    • Francesco MakovecRoberto ArtusiAntonio GiordaniSimona ZanzolaLucio Rovati
    • A61K31/41A61P9/12C07D207/00C07D257/10C07D403/10
    • C07D403/10
    • Compounds which may be represented by the general formula (I) shown below and in which: R1 is a group independently selected from among: CHO, —COOH, —CH2OH R2 is hydrogen or a linear or branched C1-C6 alkyl group R3 is hydrogen or a halogen group selected from among Cl and Br R4 is a linear or branched C3-C5 alkyl group and the pharmaceutically acceptable salts thereof such as the sodium or potassium salt. The compounds exhibit potent and selective All antagonist activity and are useful for the treatment of any disorders in which elevated synthesis of All or overexpression of the AT1 receptor may play a primary pathological role, as in the case of arterial hypertension, congestive cardiac insufficiency, platelet aggregation and disorders associated therewith such as for example myocardial and cerebral infarction, renal ischaemia, venous and arterial thrombosis, peripheral vasculopathy, pulmonary hypertension, diabetes mellitus, diabetic neuropathy, glaucoma and diabetic retinopathy.
    • 可以由下述通式(I)表示的化合物,其中:R 1是独立地选自:CHO,-COOH,-CH 2, OH R 2是氢或直链或支链C 1 -C 6烷基R 3是氢或 选自Cl和Br R 4的卤素基团是直链或支链C 3 -C 5烷基和其药学上可接受的盐 例如钠盐或钾盐。 所述化合物表现出有效和选择性的所有拮抗剂活性,并且可用于治疗其中AT 1受体的全部或过表达的合成升高可能起主要病理学作用的任何障碍,如在 动脉高血压,充血性心功能不全,血小板聚集和与之相关的病症,例如心肌和脑梗塞,肾缺血,静脉和动脉血栓形成,外周血管病变,肺动脉高压,糖尿病,糖尿病性神经病,青光眼和糖尿病性视网膜病变。