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公开(公告)号：US06218390B1
公开(公告)日：2001-04-17
申请号：US09213539
申请日：1998-12-17
IPC分类号： A61K315375
CPC分类号： C07D413/12 , A61K31/5375 , A61K31/5377 , C07D265/32 , C07D413/14
摘要： This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
摘要翻译： 本发明涉及作为人α1a受体的选择性拮抗剂的吗啉酮和吗啉衍生物。 本发明还涉及这些化合物降低眼内压，抑制胆固醇合成，放松下尿路组织，治疗良性前列腺增生，阳ency，心律失常，交感神经介导的疼痛，偏头痛以及用于治疗任何疾病的用途 其中α1a受体的拮抗作用可能是有用的。 本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。
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公开(公告)号：US06531471B2
公开(公告)日：2003-03-11
申请号：US10017263
申请日：2001-12-14
IPC分类号： A61K315375
CPC分类号： C07D413/12 , A61K31/5375 , A61K31/5377 , C07D265/32 , C07D413/14
摘要： This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
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公开(公告)号：US06362182B1
公开(公告)日：2002-03-26
申请号：US09702015
申请日：2000-10-30
IPC分类号： A61K31537
CPC分类号： C07D413/12 , A61K31/5375 , A61K31/5377 , C07D265/32 , C07D413/14
摘要： This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia, sympathetic mediated pain, migraine, and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
摘要翻译： 本发明涉及作为人α1a受体的选择性拮抗剂的吗啉酮和吗啉衍生物。 本发明还涉及这些化合物降低眼内压，抑制胆固醇合成，放松下尿路组织，治疗良性前列腺增生，阳ency，心律失常，交感神经介导的疼痛，偏头痛以及用于治疗任何疾病的用途 其中α1a受体的拮抗作用可能是有用的。 本发明还提供了包含治疗有效量的上述化合物和药学上可接受的载体的药物组合物。
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