公开(公告)号：US20050187222A1

公开(公告)日：2005-08-25

申请号：US11109761

申请日：2005-04-20

申请人： David Garvey ,  Inigo De Tejada ,  Ricky Gaston ,  Subhash Khanapure ,  Tatiana Shelekhin ,  Tiansheng Wang

发明人： David Garvey ,  Inigo De Tejada ,  Ricky Gaston ,  Subhash Khanapure ,  Tatiana Shelekhin ,  Tiansheng Wang

IPC分类号： A61K45/06 ,  C07C381/00 ,  C07D211/62 ,  C07D233/24 ,  C07D239/95 ,  C07D401/04 ,  C07D405/12 ,  C07D459/00 ,  C07D43/02 ,  A61K31/517

CPC分类号： C07D459/00 ,  A61K45/06 ,  C07C381/00 ,  C07D211/62 ,  C07D233/24 ,  C07D239/95 ,  C07D401/04 ,  C07D405/12

摘要： The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.

摘要翻译： 本发明描述了新的亚硝化和/或亚硝基化的α-肾上腺素能受体拮抗剂，以及含有至少一种亚硝化和/或亚硝基化的α-肾上腺素能受体拮抗剂的新组合物，以及任选的一种或多种捐赠，转移或释放一氧化氮的化合物 提高内源性舒张因子的内源水平，刺激一氧化氮的内源性合成，或是一氧化氮合酶的底物和/或一种或多种血管活性剂。 本发明还提供含有至少一种α-肾上腺素能受体拮抗剂和一种或多种捐赠，转移或释放一氧化氮的化合物的新型组合物，提高内源性内皮水平的内源性松弛因子，刺激一氧化氮的内源性合成，或是一种 一氧化氮合酶的底物和/或一种或多种血管活性剂。 本发明还提供了用于治疗或预防男性和女性性功能障碍的方法，用于增强男性和女性的性反应，以及用于治疗或预防良性前列腺增生，高血压，充血性心力衰竭，变体（印刷金属）心绞痛，青光眼，神经变性 疾病，血管痉挛性疾病，认知障碍，急迫性尿失禁或膀胱过度活动，以及扭转麻醉状态。

公开(公告)号：US20050065161A1

公开(公告)日：2005-03-24

申请号：US10951778

申请日：2004-09-29

申请人： David Garvey ,  Joseph Schroeder ,  Inigo De Tejada

发明人： David Garvey ,  Joseph Schroeder ,  Inigo De Tejada

IPC分类号： A61K45/06 ,  C07C381/00 ,  C07D211/62 ,  C07D233/24 ,  C07D239/95 ,  C07D401/04 ,  C07D405/12 ,  C07D459/00 ,  A61K31/517 ,  C07D43/02

CPC分类号： C07D459/00 ,  A61K45/06 ,  C07C381/00 ,  C07D211/62 ,  C07D233/24 ,  C07D239/95 ,  C07D401/04 ,  C07D405/12

摘要： The invention is directed to nitrosated or nitrosylated alpha-adrenergic receptor antagonists, compositions comprising alpha-adrenergic receptor antagonists that are optionally substituted with at least one NO or NO2 moiety and compounds that donate, transfer or release nitric oxide or elevate levels of endogenous endothelium-derived relaxing factor, and methods for treating sexual dysfunctions in males and females. The invention also provides methods for treating female sexual dysfunctions by administering S-nitrosothiol compounds.

摘要翻译： 本发明涉及亚硝化或亚硝酰化的α-肾上腺素能受体拮抗剂，包含任选被至少一个NO或NO 2部分取代的α-肾上腺素能受体拮抗剂的组合物和捐赠，转移或释放一氧化氮或提高内源性内皮 - 衍生松弛因子，以及治疗男性和女性性功能障碍的方法。 本发明还提供了通过施用S-亚硝基硫醇化合物治疗女性性功能障碍的方法。