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    Methods of use and combinations
    15.
    发明授权
    Methods of use and combinations 有权

    公开(公告)号：US10328082B2

    公开(公告)日：2019-06-25

    申请号：US15314574

    申请日：2015-05-18

    Applicant: Pfizer Inc.

    Inventor： Eugene Lvovich Piatnitski Chekler ,  Adam Matthew Gilbert ,  Rayomand Jal Unwalla ,  Patrick Robert Verhoest ,  James Thomas Anderson

    IPC: A61K31/549 ,  A61K45/06 ,  A61K31/277 ,  A61K31/397 ,  A61K31/402 ,  A61K31/433 ,  A61K31/451 ,  A61K31/472 ,  A61K31/4725

    Abstract: The present invention relates to a compound of Formula 1, 2 or 3: wherein A is N or —CR0—, where R0 is hydrogen, C1-C6 linear or branched chain alkyl, etc., Z is —CRe—, or, —N—, where Re is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R1 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R2 are independently hydrogen or C1-C6 linear or branched chain alkyl; R3 and R4 are independently hydrogen, C1-C6 linear or branched chain alkyl, etc.; R5 and R6 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; R8 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R9 and R10 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; Q is —CO—, —(CH2)q—, —(CHRs)q—, or —(CRsRt)q—, where Rs and Rt are independently C1-C6 linear or branched chain alkyl, aryl, alkylaryl, heteroaryl or alkylheteroaryl; where q is 0, 1, 2, or 3; and, where n is 0, 1, 2, 3, 4 or 5; or, a pharmaceutically acceptable salt thereof, for the treatment of certain diseases, particularly those affected or mediated by the androgen receptor; to combinations comprising such compounds with a second pharmaceutically active ingredient; to compositions containing such combinations; and to such combinations for the treatment of various diseases, particularly, those affected or mediated by the androgen receptor.

    NOVEL SELECTIVE ANDROGEN RECEPTOR MODULATORS
    18.
    发明申请
    NOVEL SELECTIVE ANDROGEN RECEPTOR MODULATORS 审中-公开
    新型选择性雄激素受体调节剂

    公开(公告)号：US20140155390A1

    公开(公告)日：2014-06-05

    申请号：US14093812

    申请日：2013-12-02

    Applicant: Pfizer Inc.

    Inventor： James Thomas Anderson ,  Eugene Lvovich Piatnitski Chekler ,  Edmund L. Ellsworth ,  Bruce Kipp Erickson ,  Adam Matthew Gilbert ,  Anthony P. Ricketts ,  David P. Thompson ,  Rayomand Jal Unwalla ,  Patrick Robert Verhoest

    IPC: C07D417/04 ,  C07C255/59

    CPC classification number: C07D417/04 ,  C07C255/58 ,  C07C255/59 ,  C07D205/04 ,  C07D207/08 ,  C07D211/22 ,  C07D217/26 ,  C07D285/10 ,  C07D401/04

    Abstract: The present invention relates to a compound of Formula 1, 2 or 3: wherein A is N or —CR0—, where R0 is hydrogen, C1-C6 linear or branched chain alkyl, etc., Z is —CRe—, or, —N—, where Re is hydrogen, C1-C6 linear or branched chain alkyl,etc.; R1 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R2 are independently hydrogen or C1-C6 linear or branched chain alkyl; R3 and R4 are independently hydrogen, C1-C6 linear or branched chain alkyl, etc.;. R5 and R6 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; R8 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R9 and R10 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; Q is —CO—, —(CH2)q—, —(CHRs)q—, or (CRsRt)q—, where Rs and Rt are independently C1-C6 linear or branched chain alkyl, aryl, alkylaryl, heteroaryl or alkylheteroaryl; where q is 0, 1, 2, or 3; and, where n is 0, 1, 2, 3, 4 or 5; or, a pharmaceutically acceptable salt thereof, to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly, those affected or mediated by the androgen receptor.

    Abstract translation: 本发明涉及式1,2或3的化合物：其中A是N或-CR 0-，其中R 0是氢，C 1 -C 6直链或支链烷基等，Z是-CRe-或 - N-，其中Re为氢，C1-C6直链或支链烷基等; R1是氢，C1-C6直链或支链烷基等; R2独立地为氢或C1-C6直链或支链烷基; R3和R4独立地是氢，C1-C6直链或支链烷基等。 R5和R6独立地是氢或C1-C6直链或支链烷基等; R8是氢，C1-C6直链或支链烷基等; R9和R10独立地为氢或C1-C6直链或支链烷基等; Q是-CO-， - （CH 2）q - ， - （CHRs）q-或（CRsRt）q-，其中R 5和R 5独立地是C 1 -C 6直链或支链烷基，芳基，烷基芳基，杂芳基或烷基杂芳基; 其中q是0,1,2或3; 并且其中n为0,1,2,3,4或5; 或其药学上可接受的盐包含含有这些化合物的组合物; 以及这些化合物在治疗各种疾病，特别是受雄激素受体影响或介导的疾病的用途。

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