Fibrinogen receptor antagonists
    12.
    发明授权
    Fibrinogen receptor antagonists 失效
    纤维蛋白原受体拮抗剂

    公开(公告)号:US5786373A

    公开(公告)日:1998-07-28

    申请号:US416772

    申请日:1995-05-31

    摘要: Novel fibrinogen receptor antagonists of the formula: X--Y--Z-Aryl-A--B and the pharmaceutically acceptable salts thereof, wherein Aryl is a 5-membered aromatic ring system containing 1 or 2 heteroatoms chosen from N, O or S wherein ring atoms may be unsubstituted or substituted with R.sup.5 and wherein S may be substituted with 0, 1 or 2 oxygen atoms; and X comprises various Nitrogen substituents including aromatic or nonaromatic systems; Y comprises, for example, alkyl or alkylaminocarbonylalkyl groups and Z and A are substituents which when present are independently chosen from alkyl or alkyloxyalkyl or other groups as defined herein; B is (a) or (b). The claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating or preventing thrombus formation.

    摘要翻译: PCT No.PCT / US93 / 09750 Sec。 371日期:1995年5月31日 102(e)日期1995年5月31日PCT提交1993年10月12日PCT公布。 第WO94 / 08577号公报 日期1994年04月28日图像(a)<图像>(b)新型的具有下式的纤维蛋白原受体拮抗剂:XYZ-Aryl-AB及其药学上可接受的盐,其中芳基是含有1个 或选自N,O或S的2个杂原子,其中环原子可以是未取代的或被R 5取代,并且其中S可以被0,1或2个氧原子取代; X包括各种氮取代基,包括芳族或非芳族体系; Y包括例如烷基或烷基氨基羰基烷基,Z和A是当存在时独立地选自烷基或烷氧基烷基或本文定义的其它基团的取代基; B是(a)或(b)。 所要求保护的化合物显示纤维蛋白原受体拮抗剂活性,抑制血小板聚集,因此可用于调节或预防血栓形成。

    Androgen receptor modulators and methods for use thereof
    18.
    发明授权
    Androgen receptor modulators and methods for use thereof 失效
    雄激素受体调节剂及其使用方法

    公开(公告)号:US06645974B2

    公开(公告)日:2003-11-11

    申请号:US10205634

    申请日:2002-07-25

    IPC分类号: A61K3158

    摘要: Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of agonizing the androgen receptor in a patient, and in particular the method wherein the androgen receptor is antagonized in the prostate of a male patient or in the uterus of a female patient and agonized in bone and/or muscle tissue. These compounds are useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, arthritis and joint repair, alone or in combination with other active agents. In addition, these compounds are useful as pharmaceutical composition ingredients alone and in combination with other active agents.

    摘要翻译: 公开了本文定义的结构式(I)的化合物可用于在需要这种调节的患者中以组织选择性方式调节雄激素受体的方法,以及在患者中激动雄激素受体的方法 ,特别是其中雄性受体在男性患者的前列腺或女性患者的子宫中被拮抗并在骨和/或肌肉组织中激动的方法。 这些化合物可用于治疗由雄激素缺乏引起的或可由雄激素施用而改善的病症,包括:骨质疏松症,牙周病,骨折,骨重建手术后的骨损伤,肌肉减少症,虚弱,衰老皮肤,男性性腺机能减退 妇女的绝经症状,动脉粥样硬化,高胆固醇血症,高脂血症,再生障碍性贫血和其他造血障碍,胰腺癌,肾癌,关节炎和关节修复,单独或与其他活性剂组合。 此外,这些化合物可单独用作药物组合物成分并与其它活性剂组合使用。