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24 条记录 (耗时 0.023 秒)

    Thiophenopyrimidines
    1.
    发明授权
    Thiophenopyrimidines 有权
    噻吩并嘧啶

    公开(公告)号：US06469166B2

    公开(公告)日：2002-10-22

    申请号：US09896250

    申请日：2001-06-29

    申请人： Thomas R. Webb ,  Chen Chen ,  James R. McCarthy ,  Terence J. Moran

    发明人： Thomas R. Webb ,  Chen Chen ,  James R. McCarthy ,  Terence J. Moran

    IPC分类号： C07D49504

    CPC分类号： C07D495/04

    摘要： This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein X is S, SO or SO2; R1 is NR4R5 or OR5; R2 is C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R4 is hydrogen, C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl or C1-6alkyloxyC1-6alkyl; R5 is C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar1CH2, C1-6alkyloxy-C1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkyl substituted with imidazolyl; or a radical of formula -Alk-O—CO-Ar1; or R4 and R5 taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; Ar is phenyl, substituted phenyl, pyridinyl or substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

    摘要翻译： 本发明涉及包括立体异构体及其药学上可接受的酸加成盐形式的化合物，其中X是S，SO或SO 2; R1是NR4R5或OR5; R2是C1-6烷基，C1-6烷氧基或C1-6烷硫基; R3是氢，C1-6烷基，C1-6烷基磺酰基，C1-6烷基亚磺酰基或C1-6烷硫基; R4是氢，C1-6烷基，一或二（C3-6环烷基）甲基，C3-6环烷基，C3-6烯基，羟基C1-6烷基，C1-6烷基羰基氧基C 1-6烷基或C 1-6烷氧基C 1-6烷基; R5是C1-6烷基，单或二（C3-6环烷基）甲基，Ar1CH2，C1-6烷氧基-C 1-6烷基，羟基C 1-6烷基，C 3-6烯基，噻吩基甲基，呋喃基甲基，C 1-6烷硫基C 1-6烷基，吗啉基，单或 二（C 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基）氨基，C 1-6烷基羰基C 1-6烷基，被咪唑基取代的C 1-6烷基; 或式-Alk-O-CO-Ar1基团; 或R 4和R 5与它们所连接的氮原子一起可以形成任选取代的吡咯烷基，哌啶基，高哌啶基或吗啉基; Ar是苯基，取代的苯基，吡啶基或取代的吡啶基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合物; 通过施用有效量的式（I）化合物来治疗与CRF过度分泌有关的疾病的方法，例如抑郁症，焦虑症，药物滥用。

    Anticancer compounds and methods of making and using same
    6.
    发明授权
    Anticancer compounds and methods of making and using same 有权
    抗癌化合物及其制备和使用方法

    公开(公告)号：US08969405B2

    公开(公告)日：2015-03-03

    申请号：US12999218

    申请日：2009-06-22

    申请人： Thomas R. Webb ,  Chandraiah Lagisetti

    发明人： Thomas R. Webb ,  Chandraiah Lagisetti

    IPC分类号： C07D493/10 ,  C07D319/06 ,  A61K31/351 ,  A61K31/357

    CPC分类号： C07D493/10 ,  A61K31/351 ,  A61K31/357 ,  C07D319/06

    摘要： In one aspect, the invention relates to compounds having anticancer activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with uncontrolled cellular proliferation using the compounds and compositions. This abstract is intended to be used as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

    摘要翻译： 一方面，本发明涉及具有抗癌活性的化合物; 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用所述化合物和组合物治疗与不受控制的细胞增殖相关的疾病的方法。 该摘要旨在用作扫描工具，用于在特定技术中进行搜索，而不意在限制本发明。