Selective melanin concentrating hormone-1 (MCH1) receptor antagonists and uses thereof
    6.
    发明授权
    Selective melanin concentrating hormone-1 (MCH1) receptor antagonists and uses thereof 失效
    选择性黑色素浓缩激素-1(MCH1)受体拮抗剂及其用途

    公开(公告)号:US06720324B2

    公开(公告)日:2004-04-13

    申请号:US09899635

    申请日:2001-07-05

    IPC分类号: C07D23932

    摘要: This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of modifying feeding behavior of a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. This invention further provides a method of treating a feeding disorder in a subject which comprises administering to the subject an amount of a compound of the invention effective to decrease the consumption of food by the subject. In an embodiment of the invention, the feeding disorder is bulimia, bulimia nervosa or obesity.

    摘要翻译: 本发明涉及作为黑色素浓缩激素-1(MCH1)受体的选择性拮抗剂的化合物。 本发明提供了包含治疗有效量的本发明化合物和药学上可接受的载体的药物组合物。 本发明提供通过将治疗有效量的本发明化合物与药学上可接受的载体组合而成的药物组合物。 本发明还提供了制备药物组合物的方法,其包括将治疗有效量的本发明化合物和药学上可接受的载体组合。本发明还提供了改变受试者进食行为的方法,其包括向受试者施用量 的有效减少受试者食物消耗的本发明化合物。 本发明进一步提供了治疗受试者进食障碍的方法,其包括向受试者施用一定量的有效降低受试者食物消耗的本发明化合物。 在本发明的一个实施方案中,喂食障碍是贪食症,神经性贪食症或肥胖症。

    Morpholinone and morpholine derivatives and uses thereof
    9.
    发明授权
    Morpholinone and morpholine derivatives and uses thereof 失效
    吗啉酮和吗啉衍生物及其用途

    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

    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。

    Morpholinone and morpholine derivatives and uses thereof
    10.
    发明授权
    Morpholinone and morpholine derivatives and uses thereof 失效
    吗啉酮和吗啉衍生物及其用途

    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

    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。