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    Substituted N-carboxyalkylpeptidyl derivatives as antidegenerative active agents
    7.
    发明授权
    Substituted N-carboxyalkylpeptidyl derivatives as antidegenerative active agents 失效
    取代的N-羧基烷基肽基衍生物作为抗再生活性剂

    公开(公告)号：US5932551A

    公开(公告)日：1999-08-03

    申请号：US848766

    申请日：1997-05-01

    申请人： Charles G. Caldwell ,  Kevin T. Chapman ,  Craig K. Esser ,  William K. Hagmann ,  Ihor E. Kopka ,  Scott A. Polo ,  Soumya P. Sahoo ,  Philippe L. Durette

    发明人： Charles G. Caldwell ,  Kevin T. Chapman ,  Craig K. Esser ,  William K. Hagmann ,  Ihor E. Kopka ,  Scott A. Polo ,  Soumya P. Sahoo ,  Philippe L. Durette

    IPC分类号： A61K38/00 ,  C07K5/02 ,  A61K38/05

    CPC分类号： C07K5/022 ,  A61K38/00

    摘要： Novel N-carboxyalkylpeptidyl compounds of formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. The matrix metalloendoproteinases are a family of zinc-containing proteinases including but not limited to stromelysin, collagenase, and gelatinase, that are capable of degrading the major components of articular cartilage and basement membranes. The inhibitors claimed herein may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to a permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation. ##STR1##

    摘要翻译： 发现式I的新型N-羧基烷基肽基化合物是有用的基质金属蛋白酶介导的疾病的抑制剂，包括骨关节炎，类风湿性关节炎，脓毒性关节炎，某些癌症中的肿瘤侵袭，牙周病，角膜溃疡，蛋白尿，疏水性表皮松解性大疱性和冠状动脉血栓形成 与动脉粥样硬化斑块破裂有关。 基质金属蛋白酶是含有蛋白酶的家族，其包括但不限于基质溶素，胶原酶和明胶酶，其能够降解关节软骨和基底膜的主要成分。 本文所要求的抑制剂也可用于预防可能导致永久性残疾的外伤性损伤后的病理后遗症。 这些化合物也可以通过预防排卵或植入作为避孕的手段。

    15-substituted 4-azasteroids
    9.
    发明授权
    15-substituted 4-azasteroids 失效
    15-取代的4-azasteroids

    公开(公告)号：US5359071A

    公开(公告)日：1994-10-25

    申请号：US30508

    申请日：1993-03-12

    申请人： Philippe L. Durette ,  Craig K. Esser ,  William Hagmann ,  Ihor E. Kopka

    发明人： Philippe L. Durette ,  Craig K. Esser ,  William Hagmann ,  Ihor E. Kopka

    IPC分类号： C07J41/00 ,  A61K31/58 ,  A61P5/28 ,  C07J1/00 ,  C07J21/00 ,  C07J51/00 ,  C07J73/00 ,  A61K31/535

    CPC分类号： C07J73/005 ,  C07J1/0011 ,  C07J21/003 ,  C07J51/00

    摘要： Compounds of the formula ##STR1## or a pharmaceutically acceptable salt or ester thereof, wherein R.sup.1 is selected from the group consisting of hydrogen and C.sub.1-10 alkyl;R.sup.2 is selected from the group consisting of hydrogen and C.sub.1-10 alkyl;R.sup.3 is selected from the group consisting of C.sub.1-10 alkoxyl, C.sub.1-10 alkyl and cyano;R.sup.4 is selected from the group consisting of C.sub.1-10 alkenyloxyl, C.sub.1-10 alkoxyl, C.sub.1-10 alkyl, C.sub.1-10 alkylcarbamic, C.sub.1-10 alkylcarbonyloxyl, carbonyl, hydroxyl, and --NHR.sup.5, andR.sup.5 is selected from the group consisting of hydrogen and C.sub.1-10 alkylcarbonyl. Such compounds are useful as selective antagonists of testosterone 5.alpha.-reductase 1.

    摘要翻译： 式IMA的化合物或其药学上可接受的盐或酯，其中R 1选自氢和C 1-10烷基; R2选自氢和C 1-10烷基; R3选自C1-10烷氧基，C1-10烷基和氰基; R4选自C1-10烯氧基，C1-10烷氧基，C1-10烷基，C1-10烷基氨基甲酸，C1-10烷基羰基氧基，羰基，羟基和-NHR5，R5选自 氢和C 1-10烷基羰基。 这些化合物可用作睾酮5α-还原酶1的选择性拮抗剂。