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21 条记录 (耗时 0.025 秒)

    Substituted aryl hydroxamic acids as metalloproteinase inhibitors
    2.
    发明授权
    Substituted aryl hydroxamic acids as metalloproteinase inhibitors 有权
    取代的芳基异羟肟酸作为金属蛋白酶抑制剂

    公开(公告)号：US06268379B1

    公开(公告)日：2001-07-31

    申请号：US09311168

    申请日：1999-05-13

    申请人： Chu-Biao Xue ,  Carl P. Decicco ,  Ruth R. Wexler

    发明人： Chu-Biao Xue ,  Carl P. Decicco ,  Ruth R. Wexler

    IPC分类号： C07D21700

    CPC分类号： C07D401/12 ,  C07D405/12

    摘要： The present application describes novel substituted aryl hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from 0-2 heteroatoms selected from N, 0, and S, which are useful as metalloprotease inhibitors.

    摘要翻译： 本申请描述了式I的新型取代的芳基异羟肟酸：或其药学上可接受的盐形式，其中环A是含有0-2个选自N，O和S的杂原子的5-8元环，其可用作金属蛋白酶 抑制剂。

    Antihypertensive 4,5-diaryl-1H-imidazole-2-methanol derivatives
    7.
    发明授权
    Antihypertensive 4,5-diaryl-1H-imidazole-2-methanol derivatives 失效
    抗高血压4,5-二芳基-1H-咪唑-2-甲醇衍生物

    公开(公告)号：US4576958A

    公开(公告)日：1986-03-18

    申请号：US573214

    申请日：1984-01-23

    申请人： Ruth R. Wexler

    发明人： Ruth R. Wexler

    IPC分类号： C07D233/54 ,  C07D233/64 ,  A61K31/415

    CPC分类号： C07D233/64

    摘要： Antihypertensive 4-phenyl-5-(4-methylsulfonylphenyl)-.alpha.,.alpha.-bis(trifluoromethyl)-1H-imidazole-2-methanol derivatives are useful in the treatment of hypertension.

    摘要翻译： 抗高血压4-苯基-5-（4-甲基磺酰基苯基）-α，α-双（三氟甲基）-1H-咪唑-2-甲醇衍生物可用于治疗高血压。

    Substituted tricyclic gamma-carbolines as serotonin receptor agonists and antagonists
    8.
    发明授权
    Substituted tricyclic gamma-carbolines as serotonin receptor agonists and antagonists 有权
    取代三环γ-咔啉作为血清素受体激动剂和拮抗剂

    公开(公告)号：US07109339B2

    公开(公告)日：2006-09-19

    申请号：US10743449

    申请日：2003-12-19

    申请人： Taekyu Lee ,  Wenting Chen ,  Wei Deng ,  Albert J. Robichaud ,  Ruth R. Wexler

    发明人： Taekyu Lee ,  Wenting Chen ,  Wei Deng ,  Albert J. Robichaud ,  Ruth R. Wexler

    IPC分类号： C07D417/00 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The present invention is directed to novel compounds represented by structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R4a, R5, R6, R7, R8, R9,and m, are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain central nervous system disorders. The compounds of this invention are serotonin receptor modulators, in particular 5HT2C receptor agonists and antagonists, and are useful in the control or prevention of central nervous system disorders including obesity, anorexia, bulemia, depression, anxiety, psychosis, schizophrenia, migraine, addictive behavior, obsessive-compulsive disorder, and sexual disorders.

    摘要翻译： 本发明涉及由结构式（I）表示的新化合物或其药学上可接受的盐，其中R 1，R 4a，R 5， R 6，R 6，R 7，R 8，R 9和M如本文所定义 。 本发明还涉及包含这些新化合物作为活性成分的药物制剂以及新型化合物及其制剂在治疗某些中枢神经系统疾病中的用途。 本发明的化合物是5-羟色胺受体调节剂，特别是5HT 2C受体激动剂和拮抗剂，并且可用于控制或预防中枢神经系统疾病，包括肥胖症，厌食症，血症，抑郁症，焦虑症， 精神病，精神分裂症，偏头痛，成瘾行为，强迫症和性功能障碍。

    Fused-ring heterocycles for the treatment of atherosclerosis
    10.
    发明授权
    Fused-ring heterocycles for the treatment of atherosclerosis 失效
    用于治疗动脉粥样硬化的融合环杂环

    公开(公告)号：US5478830A

    公开(公告)日：1995-12-26

    申请号：US889892

    申请日：1992-05-29

    申请人： C. Anne Higley ,  Ruth R. Wexler ,  Richard G. Wilde

    发明人： C. Anne Higley ,  Ruth R. Wexler ,  Richard G. Wilde

    IPC分类号： C07D487/04 ,  A61K31/44 ,  A61K31/505 ,  A61K31/52

    CPC分类号： C07D487/04

    摘要： This invention relates to pyrazolo pyrimidines for the treatment of atherosclerosis as inhibitors of acyl--CoA, cholesterol acyetransferase (ACAT), and their use as antihypercholesterolemic agents, pharmaceutical compositions and preparation, and having the formula (I): ##STR1## wherein: A and Q are selected independently from CH or N with no more than two nitrogens per ring:D, E, and G are selected independently from CR.sup.1 or N with no more than two nitrogens per ring;X is S(O).sub.r, O, NR.sup.4 or CH.sup.2 ;J is C.sub.2 -C.sub.10 alkyl, C.sub.3 -C.sub.10 branched alkyl, C.sub.3 -C.sub.10 alkenyl or C.sub.3 -C.sub.10 alkynyl;Y is O, S, H.sub.2 or NH:Z is NHR.sup.3, OR.sup.3 or R.sup.3 :R.sup.1 is selected independently from H, NO.sub.2, Br, Cl, F, CF.sub.3, CN, CH.sub.3 S(O).sub.r, C.sub.1 -C.sub.8 alkyl or alloxy, C.sub.3 -C.sub.8, branched alkyl, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.5 R.sup.6 or NR.sup.5 COR.sup.6 ;R.sup.2 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.8 alkenyl or alkynyl, C.sub.7 -C.sub.14 araalkyl where the aryl group is optionally substituted; phenyl optionally substituted benzyl optionally substituted 2-, 3-, or 4- pyridinyl, pyrimidinyl: or biphenyl:R.sup.3 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.4 -C.sub.10 cycloallylalkyl, C.sub.3 -C.sub.6 alkenyl or alkynyl, C.sub.1 -C.sub.3 perfluoroalkyl, C.sub.7 -C.sub.14 araalkyl where the aryl group is optionally substituted phenyl optionally substituted benzyl optionally substituted 2-, 3-, or 4- pyridinyl, pyrimidinyl; or biphenyl:R.sup.4 is H, C.sub.1 -C.sub.6 alkyl or benzyl;R.sup.5 and R.sup.6 are selected independently from H or C.sub.1 -C.sub.4 alkyl;r is 0 to 2:or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及用于治疗动脉粥样硬化的吡唑并嘧啶作为酰基辅酶A，胆固醇转氨酶（ACAT）的抑制剂及其作为抗高胆固醇血症药物，药物组合物和制剂的用途，并具有式（I）：其中： A和Q独立地选自CH或N，每个环不多于两个氮：D，E和G独立地选自CR1或N，每个环不多于两个氮; X是S（O）r，O，NR 4或CH 2; J是C 2 -C 10烷基，C 3 -C 10支链烷基，C 3 -C 10链烯基或C 3 -C 10炔基; Y是O，S，H2或NH：Z是NHR3，OR3或R3：R1独立地选自H，NO2，Br，Cl，F，CF3，CN，CH3S（O）r，C1-C8烷基或烯氧基， C3-C8，支链烷基，C1-C4烷氧羰基，NR5R6或NR5COR6; R2是C1-C8烷基，C3-C8支链烷基，C3-C7环烷基，C3-C8链烯基或炔基，其中芳基任选被取代的C7-C14芳烷基; 苯基任选取代的苄基任选取代的2-，3-或4-吡啶基，嘧啶基或联苯基：R3是C1-C8烷基，C3-C8支链烷基，C3-C7环烷基，C4-C10环烯基烷基，C3-C6烯基或 炔基，C1-C3全氟烷基，C7-C14芳烷基，其中芳基是任选取代的苯基任选取代的苄基任选取代的2-，3-或4-吡啶基，嘧啶基; 或联苯基：R 4是H，C 1 -C 6烷基或苄基; R 5和R 6独立地选自H或C 1 -C 4烷基; r为0〜2：或其药学上可接受的盐。