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    Androgen receptor modulators and methods for use thereof
    1.
    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

    申请人： John H. Hutchinson ,  Michael J. Breslin ,  Gideon A. Rodan ,  Soumya P. Sahoo ,  Mark E. Duggan ,  Shun-Ichi Harada ,  Azriel Schmidt ,  Wasyl Halczenko ,  Dwight A. Towler

    发明人： John H. Hutchinson ,  Michael J. Breslin ,  Gideon A. Rodan ,  Soumya P. Sahoo ,  Mark E. Duggan ,  Shun-Ichi Harada ,  Azriel Schmidt ,  Wasyl Halczenko ,  Dwight A. Towler

    IPC分类号： A61K3158

    CPC分类号： C07J73/005 ,  A61K31/435 ,  A61K31/473 ,  A61K31/58 ,  C07D221/18 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

    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。

    Novel inhibitor peptides
    2.
    发明授权
    Novel inhibitor peptides 失效
    新型抑制剂肽

    公开(公告)号：US4709012A

    公开(公告)日：1987-11-24

    申请号：US894185

    申请日：1986-08-07

    申请人： Steven P. Adams ,  Dwight A. Towler ,  Luis Glaser

    发明人： Steven P. Adams ,  Dwight A. Towler ,  Luis Glaser

    IPC分类号： A61K38/55 ,  C07K7/06 ,  C12N9/99

    CPC分类号： C07K7/06

    摘要： An octapeptide inhibitor of myristoylating enzymes is disclosed having an amino acid sequence selected from the group consisting of the following sequences or a physiologically acceptable amide or salt derivative thereof: ##STR1## wherein R=Leu, Phe, Tyr or Val.

    摘要翻译： 公开了肉豆蔻酰化酶的八肽抑制剂，其具有选自以下序列或其生理上可接受的酰胺或盐衍生物的氨基酸序列：其中R = Leu，Phe，Tyr或 瓦尔

    Novel substrate peptides
    4.
    发明授权
    Novel substrate peptides 失效
    新型底物肽

    公开(公告)号：US4740588A

    公开(公告)日：1988-04-26

    申请号：US924543

    申请日：1986-10-29

    申请人： Steven P. Adams ,  Dwight A. Towler ,  Luis Glaser

    发明人： Steven P. Adams ,  Dwight A. Towler ,  Luis Glaser

    IPC分类号： C12P21/00 ,  C07K1/00 ,  C07K1/06 ,  C07K7/06 ,  C12N9/80

    CPC分类号： C07K7/06

    摘要： A peptide substrate for myristoylating enzymes is disclosed having an amino acid sequence selected from the group consisting of the following sequences or a physiologically acceptable amide or salt derivative thereof: ##STR1## wherein R=Ala, Asn, Gln or Ser;S=Ala, Arg, Gln, Glu, Phe or Ser;T=Ala or Lys;W=Ala or Ser;X=Ala, Tyr, or Lys;Y=Arg or Pro; andZ=Arg, Leu or Lys.

    摘要翻译： 公开了用于肉豆蔻酰化酶的肽底物，其具有选自以下序列或其生理上可接受的酰胺或盐衍生物的氨基酸序列：其中R = Ala ，Asn，Gln或Ser; S = Ala，Arg，Gln，Glu，Phe或Ser; T = Ala或Lys; W = Ala或Ser; X = Ala，Tyr或Lys; Y = Arg或Pro; Z = Arg，Leu或Lys。

    DNA molecules encoding Macaca mulatta androgen receptor
    5.
    发明授权
    DNA molecules encoding Macaca mulatta androgen receptor 失效
    编码猕猴猕猴雄激素受体的DNA分子

    公开(公告)号：US07060463B2

    公开(公告)日：2006-06-13

    申请号：US10476724

    申请日：2002-05-03

    申请人： Dwight A. Towler ,  Fang Chen

    发明人： Dwight A. Towler ,  Fang Chen

    IPC分类号： C12N15/11 ,  C12N5/10 ,  C12N15/63

    CPC分类号： C07K14/721 ,  C07K2319/00

    摘要： The present invention discloses the isolation and characterization of cDNA molecules encoding novel androgen receptor (AR) protein from Macaca mulatta. Also within the scope of the disclosure are recombinant vectors, recombinant host cells, methods of screening for modulators of Macaca mulatta AR (rhAR) activity, purified proteins and fusion proteins which comprise all or a portion of the rhAR protein, transgenic mice comprising a transgene encoding the rhAR protein, as well as production of antibodies against AR, or epitopes thereof.

    摘要翻译： 本发明公开了从猕猴属（Macaca mulatta）中分离和鉴定编码新型雄激素受体（AR）蛋白的cDNA分子。 也在本公开的范围内的是重组载体，重组宿主细胞，筛选猕猴猕猴AR（rhAR）活性的调节剂的方法，包含全部或部分rhAR蛋白的纯化蛋白质和融合蛋白，包含转基因的转基因小鼠 编码rhAR蛋白，以及产生针对AR的抗体或其表位。