首页> 外国专利> DERIVATIVES OF HEXAHYDROPIRAZINE (1'2 ': 1,6) -PIRIDO (3,4-B) INDOL-1,4-DIONA FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS AND ERECTILE DYSFUNCTION.

DERIVATIVES OF HEXAHYDROPIRAZINE (1'2 ': 1,6) -PIRIDO (3,4-B) INDOL-1,4-DIONA FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS AND ERECTILE DYSFUNCTION.

机译:六氢吡嗪(1'2':1,6)-PIRIDO(3,4-B)INDOL-1,4-Diona的衍生物,用于治疗心血管疾病和勃起功能障碍。

摘要

The biochemical, physiological and clinical effects of PDE5 inhibitors suggest its usefulness in a variety of pathological conditions, in which modulation of smooth muscles, renal, hemostatic, inflammatory, and / or endocrine function is desirable. The compounds of formula (I) are therefore useful in the treatment of a number of disorders, such as temple, stable, unstable, and variant angina pectoris, (Prinzmetal), hypertension, pulmonary hypertension, congestive heart disease, acute dysneic syndrome, acute and chronic renal failure, atherosclerosis, clinical pictures of reduced permeability of blood vessels (for example, post-percutaneous transluminal carotid or coronary angioplasty or graft stenosis in post-bypass surgery), peripheral vasculopathy, vascular disorders, such as Raynaud's disease, thrombocythemia, inflammatory diseases, stroke, bronchitis, chronic asthma, allergic asthma, allergic rhinitis, glaucoma, osteoporosis, premature delivery, benign prostatic hypertrophy, peptic ulcer, male erectile dysfunction, female sexual dysfunction and diseases characterized by disorders of the intestinal motility (for example, bowel irritation syndrome able). An especially important use is the treatment of male erectile dysfunction, which is a form of impotence and constitutes a common medical problem. Impotence can be defined as lack of power, in the male, to copulate and may mean the inability to achieve an erection or ejaculation or both. The incidence of erectile dysfunction increases with age, and approximately 50% of men over 40 suffer from erectile dysfunction to some extent. In addition, another important use is the treatment of female arousal disorder. Female arousal disorders are defined as a recurring inability to achieve or maintain an adequate lubrication / tumescence response of sexual arousal until sexual activity ends. The excitement response consists of vasocongestion in the pelvis, vaginal lubrication and expansion and tumescence of the external genitalia.
机译:PDE5抑制剂的生化,生理和临床效果表明,它可用于多种病理状况,其中需要调节平滑肌,肾脏,止血,炎性和/或内分泌功能。因此,式(I)化合物可用于治疗许多病症,例如太阳穴,稳定,不稳定和变异型心绞痛(Prinzmetal),高血压,肺动脉高压,充血性心脏病,急性呼吸困难综合症,急性慢性肾功能衰竭,动脉粥样硬化,血管通透性降低的临床表现(例如,旁路手术后经皮腔内颈动脉或冠状动脉成形术或移植狭窄),周围血管病变,血管疾病(如雷诺氏病,血小板增多症,炎症性疾病,中风,支气管炎,慢性哮喘,变应性哮喘,变应性鼻炎,青光眼,骨质疏松症,早产,良性前列腺肥大,消化性溃疡,男性勃起功能障碍,女性性功能障碍和以肠蠕动障碍为特征的疾病(例如,肠刺激性综合征能力)。特别重要的用途是治疗男性勃起功能障碍,这是阳imp的一种形式,构成了常见的医学问题。阳可以定义为男性无力进行交配,这可能意味着无法勃起或射精或两者兼而有之。勃起功能障碍的发生率随着年龄的增长而增加,大约40%的40岁以上的男性在一定程度上患有勃起功能障碍。此外,另一个重要用途是治疗女性唤醒障碍。女性唤醒性疾病的定义是,在性活动结束之前,反复出现无法实现或维持性唤醒的适当润滑/肿胀反应的情况。兴奋反应包括骨盆血管收缩,阴道润滑,外生殖器扩张和肿胀。

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