首页> 外国专利> Cis isomer compound use of a compound process for the treatment of unstable and variable stable angina pulmonary hypertension chronic obstructive pulmonary disease congestive heart failure renal failure atherosclerosis sick states of reduced blood vessel clearance peripheral vascular disease vascular disorders inflammatory diseases heart attack bronchitis chronic asthma asthma allergic allergic rhinitis claucoma or disorders of intestinal mobility disorders in a human or non-human animal body pharmaceutical composition process for the preparation of a pharmaceutical composition and process for preparing a compound

Cis isomer compound use of a compound process for the treatment of unstable and variable stable angina pulmonary hypertension chronic obstructive pulmonary disease congestive heart failure renal failure atherosclerosis sick states of reduced blood vessel clearance peripheral vascular disease vascular disorders inflammatory diseases heart attack bronchitis chronic asthma asthma allergic allergic rhinitis claucoma or disorders of intestinal mobility disorders in a human or non-human animal body pharmaceutical composition process for the preparation of a pharmaceutical composition and process for preparing a compound

机译:顺式异构体化合物用于治疗不稳定和可变稳定型心绞痛的方法肺动脉高压慢性阻塞性肺疾病充血性心力衰竭肾衰竭动脉粥样硬化血管清除率降低的病态周围血管疾病血管疾病炎症性疾病心脏病发作支气管炎慢性哮喘哮喘过敏人类或非人类动物体内的变应性鼻炎性青光眼或肠道活动障碍疾病药物组合物的制备方法,药物组合物的制备方法以及化合物的制备方法

摘要

A compound of formula (I) and salts and solvates thereof, in which: R0 represents hydrogen, halogen or C1-6 alkyl; R1 represents hydrogen, C1-6alkyl, C2-6 alkenyl, C2-6 alkynyl, haloC1-6alkyl, C3-8cyloalkyl, C3-8cycloalkylC1-3alkyl, arylC1-3alkyl or heteroarylC1-3alkyl; R2 represents an optionally substituted monocyclic aromatic ring selected from benzene, thiophene, furan and pyridine or an optionally substituted bicyclic ring attached to the rest of the molecule via one of the benzene ring carbon atoms and wherein the fused ring A is a 5- or 6-membered ring which may be saturated or partially or fully unsaturated and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulphur and nitrogen; and R3 represents hydrogen or C1-3 alkyl, or R1 and R3 together represent a 3- or 4-membered alkyl or alkenyl chain. A compound of formula (I) is a potent and selective inhibitor of cyclic guanosine 3'5'-monophosphate specific phosphodiesterase (cGMP specific PDE) having a utility in a variety of therapeutic areas where such inhibition is beneficial, including the treatment of cardiovascular disorders.
机译:式(I)化合物及其盐和溶剂化物,其中:R 0代表氢,卤素或C 1-6烷基; R1代表氢,C1-6烷基,C2-6链烯基,C2-6炔基,卤代C1-6烷基,C3-8环烷基,C3-8环烷基C1-3烷基,芳基C1-3烷基或杂芳基C1-3烷基; R 2代表选自苯,噻吩,呋喃和吡啶的任选取代的单环芳环或通过苯环碳原子之一连接至分子其余部分的任选取代的双环,且其中稠合环A为5-或6 -可以是饱和的或部分或完全不饱和的并包含碳原子和任选地一个或两个选自氧,硫和氮的杂原子的元环; R 3代表氢或C 1-3烷基,或R 1和R 3一起代表3或4元烷基或烯基链。式(I)化合物是环状鸟苷3'5'-单磷酸特异性磷酸二酯酶(cGMP特异性PDE)的有效和选择性抑制剂,可在多种有益于该抑制作用的治疗领域中使用,包括治疗心血管疾病。

著录项

  • 公开/公告号BR9506559A

    专利类型

  • 公开/公告日1997-10-28

    原文格式PDF

  • 申请/专利权人 LABORATOIRES GLAXO WELLCOME S.A.;

    申请/专利号BR19959506559

  • 发明设计人 ALAIN CLAUDE-MARIE DAUGAN;

    申请日1995-01-19

  • 分类号C07D471/14;A61K31/395;C07D471/04;C07D209/14;

  • 国家 BR

  • 入库时间 2022-08-22 03:27:41

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