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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。

    P38 kinase inhibiting agents
    4.
    发明授权
    P38 kinase inhibiting agents 有权
    P38激酶抑制剂

    公开(公告)号：US08513289B2

    公开(公告)日：2013-08-20

    申请号：US13266043

    申请日：2010-04-26

    申请人： Hiroo Koyama ,  Soumya P. Sahoo ,  Ginger Xu-Qiang Yang ,  Daniel J. Miller

    发明人： Hiroo Koyama ,  Soumya P. Sahoo ,  Ginger Xu-Qiang Yang ,  Daniel J. Miller

    IPC分类号： A61K31/4245 ,  A61K31/433 ,  C07D285/08 ,  C07D207/333

    CPC分类号： C07D417/12 ,  C07D417/14

    摘要： Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: Formula (I); are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.

    摘要翻译： 由化学式（I）或其药学上可接受的盐描述的化合物：式（I）; 是p38的抑制剂，可用于治疗炎症，例如治疗哮喘，COPD，ARDS，类风湿性关节炎，类风湿性脊椎炎，骨关节炎，痛风性关节炎和其他关节炎病症; 发炎关节，湿疹，牛皮癣或其他炎症皮肤病如晒伤; 炎症性眼病，包括结膜炎; 皮肤炎，疼痛等与炎症有关的病症。

    P38 KINASE INHIBITING AGENTS
    5.
    发明申请
    P38 KINASE INHIBITING AGENTS 有权
    P38激酶抑制剂

    公开(公告)号：US20120040999A1

    公开(公告)日：2012-02-16

    申请号：US13266043

    申请日：2010-04-26

    申请人： Hiroo Koyama ,  Soumya P. Sahoo ,  Ginger Xu-Qiang Yang ,  Daniel J. Miller

    发明人： Hiroo Koyama ,  Soumya P. Sahoo ,  Ginger Xu-Qiang Yang ,  Daniel J. Miller

    IPC分类号： A61K31/433 ,  C07D417/14 ,  A61K31/4439 ,  A61P19/10 ,  C07D487/04 ,  A61K31/519 ,  A61P29/00 ,  A61P11/00 ,  C07D417/12 ,  A61K31/497

    CPC分类号： C07D417/12 ,  C07D417/14

    摘要： Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: Formula (I); are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.

    摘要翻译： 由化学式（I）或其药学上可接受的盐描述的化合物：式（I）; 是p38的抑制剂，可用于治疗炎症，例如治疗哮喘，COPD，ARDS，类风湿性关节炎，类风湿性脊椎炎，骨关节炎，痛风性关节炎和其他关节炎病症; 发炎关节，湿疹，牛皮癣或其他炎症皮肤病如晒伤; 炎症性眼病，包括结膜炎; 皮肤炎，疼痛等与炎症有关的病症。

    17-alkyl-7-substituted-4-aza steroid derivatives as 5-.alpha.-reductase inhibitors
    8.
    发明授权
    17-alkyl-7-substituted-4-aza steroid derivatives as 5-.alpha.-reductase inhibitors 失效
    17-烷基-7-取代-4-氮杂类固醇衍生物作为5-α-还原酶抑制剂

    公开(公告)号：US5763361A

    公开(公告)日：1998-06-09

    申请号：US734705

    申请日：1996-10-21

    申请人： Georgianna Harris ,  Richard L. Tolman ,  Soumya P. Sahoo

    发明人： Georgianna Harris ,  Richard L. Tolman ,  Soumya P. Sahoo

    IPC分类号： C07J73/00 ,  A61K31/58

    CPC分类号： C07J73/005

    摘要： The novel compounds of the present invention are those of structural formula I: ##STR1## or a pharmaceutically acceptable salt, or stereoisomer thereof, which are inhibitors of 5.alpha.-reductase, particularly 5.alpha.-reductase type 1. The compounds of formula I are useful in the systemic, including oral, or parenteral or topical treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia which includes female and male pattern baldness, female hirsutism, benign prostafic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as in the treatment of prostatitis. Methods of using the compounds of formula I for the treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia, male pattern baldness, female hirsutism, benign prostatic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as the treatment of prostatitis are provided, as well as pharmaceutical compositions for the compounds of formula I. The use of compounds of formula I in combination with other, active agents, for example with a 5.alpha.-reductase type 2 inhibitor such as finasteride or epristeride, or a potassium channel opener, such as minoxidil, or a retinoic acid or a derivative thereof is also taught, wherein such combinations would be useful in one or more of the above-mentioned methods of treatment or pharmaceutical compositions.

    摘要翻译： 本发明的新化合物是结构式I的化合物：其中（I）化合物或其药学上可接受的盐或立体异构体，其为5α-还原酶，特别是5型α-还原酶1型的抑制剂。 式I可用于全身，包括口服或肠胃外或局部治疗高雄性性疾病，如寻常痤疮，皮脂溢，雄激素性脱发，包括女性和男性型秃发，女性多毛症，良性前列腺增生，以及预防和治疗前列腺 癌，以及前列腺炎的治疗。 使用式I化合物治疗高雄激素病症如寻常痤疮，皮脂溢，雄激素性脱发，男性型秃发，女性多毛症，良性前列腺增生以及预防和治疗前列腺癌的方法，以及治疗 提供前列腺炎，以及用于式I化合物的药物组合物。式I化合物与其它活性剂，例如5α-还原酶2抑制剂如非那雄胺或艾美他啶的组合或 钾通道开放剂如米诺地尔或视黄酸或其衍生物也被教导，其中这些组合可用于一种或多种上述治疗方法或药物组合物。

    P38 kinase inhibiting agents
    10.
    发明授权
    P38 kinase inhibiting agents 有权
    P38激酶抑制剂

    公开(公告)号：US07879875B2

    公开(公告)日：2011-02-01

    申请号：US11990050

    申请日：2006-08-08

    申请人： Meng-Hsin Chen ,  James B. Doherty ,  Robert Tynebor ,  Swaminathan R. Natarajan ,  Zhen Li ,  Soumya P. Sahoo

    发明人： Meng-Hsin Chen ,  James B. Doherty ,  Robert Tynebor ,  Swaminathan R. Natarajan ,  Zhen Li ,  Soumya P. Sahoo

    IPC分类号： A61K31/4375 ,  C07D455/02

    CPC分类号： C07D471/04

    摘要： Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: (I) are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.

    摘要翻译： 由化学式（I）或其药学上可接受的盐描述的化合物：（I）是p38的抑制剂，可用于治疗炎症，例如治疗类风湿性关节炎，类风湿性脊椎炎，骨关节炎，痛风性关节炎和其他关节炎病症 ; 发炎关节，湿疹，牛皮癣或其他炎症皮肤病如晒伤; 炎症性眼病，包括结膜炎; 皮肤炎，疼痛等与炎症有关的病症。