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    N.sup.6 -(benzothien-3-yl)ethyl adenosine; N.sup.6 -(benzothien-3-yl)ethyl adenosine, S-oxide; and N.sup.6 -(benzothien-3-yl)ethyl S,S-dioxide adenosine
    6.
    发明授权
    N.sup.6 -(benzothien-3-yl)ethyl adenosine; N.sup.6 -(benzothien-3-yl)ethyl adenosine, S-oxide; and N.sup.6 -(benzothien-3-yl)ethyl S,S-dioxide adenosine 失效
    N6-（苯并噻吩-3-基）乙基腺苷; N6-（苯并噻吩-3-基）乙基腺苷，S-氧化物; 和N6-（苯并噻吩-3-基）乙基S，S-二氧化物腺苷

    公开(公告)号：US4764506A

    公开(公告)日：1988-08-16

    申请号：US853536

    申请日：1986-04-18

    申请人： William Patt

    发明人： William Patt

    IPC分类号： C07H19/16 ,  A61K31/70

    CPC分类号： C07H19/16

    摘要： Benzothien-3-yl adenosine; benzothien-3-yl adenosine, S-oxide; and benzothien-3-yl adenosine, S,S-dioxide compounds or pharmaceutically acceptable acid addition salts having highly desirable central nervous system and antihypertensive properties, processes for their manufacture and pharmaceutical compositions and methods for using said compounds and compositions are described.

    摘要翻译： 苯并噻吩-3-基腺苷; 苯并噻吩-3-基腺苷，S-氧化物; 和苯并噻吩-3-基腺苷，S，S-二氧化物化合物或具有高度期望的中枢神经系统和抗高血压性质的药学上可接受的酸加成盐，其制备方法和药物组合物以及使用所述化合物和组合物的方法。

    Kinase inhibitors useful for the treatment of proliferative diseases
    7.
    发明申请
    Kinase inhibitors useful for the treatment of proliferative diseases 失效
    可用于治疗增殖性疾病的激酶抑制剂

    公开(公告)号：US20080114006A1

    公开(公告)日：2008-05-15

    申请号：US11854354

    申请日：2007-09-12

    申请人： Daniel Flynn ,  Peter Petillo ,  Michael Kaufman ,  William Patt

    发明人： Daniel Flynn ,  Peter Petillo ,  Michael Kaufman ,  William Patt

    IPC分类号： A61K31/519 ,  A61K31/4375 ,  A61P1/00 ,  A61P11/00 ,  A61P17/06 ,  A61P19/02 ,  A61P35/00 ,  A61P37/00 ,  A61P9/00 ,  C07D401/04 ,  C07D471/04 ,  C12N9/12

    CPC分类号： A61K31/4375 ,  A61K31/519 ,  C07D471/04

    摘要： The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

    摘要翻译： 本发明涉及可用于治疗各种疾病的新型激酶抑制剂和调节剂化合物。 更具体地，本发明涉及这些化合物，激酶/化合物加合物，治疗疾病的方法和化合物的合成方法。 优选地，所述化合物可用于调节Raf激酶及其疾病多形体的激酶活性。 本发明的化合物可用于治疗哺乳动物癌症，特别是人类癌症，包括但不限于恶性黑素瘤，结肠直肠癌，卵巢癌，甲状腺乳头状癌，非小细胞肺癌和间皮瘤。 本发明的化合物还可用于治疗类风湿性关节炎和视网膜病变，包括糖尿病性视网膜神经病变和黄斑变性。

    Benzothien-3-yl adenosine; benzothien-3-yl adenosine, S-oxide; and benzothien-3-yl, S,S-dioxide adenosine compounds
    8.
    发明授权
    Benzothien-3-yl adenosine; benzothien-3-yl adenosine, S-oxide; and benzothien-3-yl, S,S-dioxide adenosine compounds 失效
    苯并噻吩-3-基腺苷; 苯并噻吩-3-基腺苷，S-氧化物; 和苯并噻吩-3-基，S，S-二氧化物腺苷化合物

    公开(公告)号：US4636493A

    公开(公告)日：1987-01-13

    申请号：US853581

    申请日：1986-04-18

    申请人： William Patt

    发明人： William Patt

    IPC分类号： C07H19/16 ,  A61K31/70

    CPC分类号： C07H19/16

    摘要： Benzothien-3-yl adenosine; benzothien-3-yl adenosine, S-oxide; and benzothien-3-yl adenosine, S,S-dioxide compounds or pharmaceutically acceptable acid addition salts having highly desirable central nervous system and antihypertensive properties, processes for their manufacture and pharmaceutical compositions and methods for using said compounds and compositions are described.

    摘要翻译： 苯并噻吩-3-基腺苷; 苯并噻吩-3-基腺苷，S-氧化物; 和苯并噻吩-3-基腺苷，S，S-二氧化物化合物或具有高度期望的中枢神经系统和抗高血压性质的药学上可接受的酸加成盐，其制备方法和药物组合物以及使用所述化合物和组合物的方法。

    Isophthalic acid derivatives as matrix metalloproteinase inhibitors
    9.
    发明申请
    Isophthalic acid derivatives as matrix metalloproteinase inhibitors 失效
    间苯二甲酸衍生物作为基质金属蛋白酶抑制剂

    公开(公告)号：US20060025396A1

    公开(公告)日：2006-02-02

    申请号：US11238502

    申请日：2005-09-29

    申请人： Nicole Barvian ,  David Connor ,  Richard Dyer ,  Adam Johnson ,  William Patt

    发明人： Nicole Barvian ,  David Connor ,  Richard Dyer ,  Adam Johnson ,  William Patt

    IPC分类号： A61K31/455 ,  A61K31/195 ,  A61K31/192 ,  C07C235/78

    CPC分类号： C07D213/30 ,  C07C69/80 ,  C07C69/90 ,  C07C69/92 ,  C07C229/60 ,  C07C233/66 ,  C07C233/69 ,  C07C233/73 ,  C07C233/75 ,  C07C233/78 ,  C07C235/60 ,  C07D285/14 ,  C07D317/54 ,  C40B50/14

    摘要： Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula wherein: R1, R2, and R3 independently are hydrogen, halo, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; each R4 and R5 independently are H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring, optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.

    摘要翻译： 选择性MMP-13抑制剂是下式的间苯二甲酸衍生物，其中：R 1，R 2和R 3独立地是氢，卤素， 羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 2 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， C 1 -C 6亚烷基，C 2 -C 6炔基，NO 2，NR 2， 4，R 5，CN或CF 3; E独立地为O或S; A和B独立地为OR 4或NR 4 R 5; 每个R 4和R 5独立地是H，C 1 -C 6烷基，C 2 C 1 -C 6亚烷基，C 2 -C 6炔基，（CH 2 2） （CH 2）2芳基，（CH 2）2芳基，（CH 2 CH 2）n个杂芳基， 或R 4和R 5与它们所连接的氮原子一起形成3至8元环，任选含有选自O，S的杂原子 ，或NH，并且任选取代或未取代; n为0〜6; 或其药学上可接受的盐。 该化合物可用于治疗由MMP酶介导的哺乳动物中的疾病。