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21 条记录 (耗时 0.04 秒)

    Substituted N-carboxyalkylpeptidyl derivatives as antidegenerative active agents
    5.
    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。

    Glycopeptide antibacterial compounds, compositions containing same and methods of using same
    6.
    发明授权
    Glycopeptide antibacterial compounds, compositions containing same and methods of using same 失效
    糖肽抗菌化合物，含有它们的组合物和使用它们的方法

    公开(公告)号：US06498238B1

    公开(公告)日：2002-12-24

    申请号：US09574225

    申请日：2000-05-19

    申请人： Ronald M. Kim ,  Daniel E. Kahne ,  Kevin T. Chapman

    发明人： Ronald M. Kim ,  Daniel E. Kahne ,  Kevin T. Chapman

    IPC分类号： C07G1100

    CPC分类号： C07K9/008 ,  A61K38/00

    摘要： The present invention relates to vancomycin analogs in which the vancosamine residue is substituted with a lipid-like substituent that includes a first aryl moiety and a second aryl moiety joined together by a flexible linker moiety, that is not a single bond directly joining the first aryl moiety and the second aryl moiety, and a glucose C-6 substituent modified to be other than the naturally occurring hydroxyl group, or pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及万古霉素类似物，其中万花胺残基被脂质取代基取代，该类脂质取代基包括通过柔性接头部分连接在一起的第一芳基部分和第二芳基部分，其不是直接连接第一芳基的单键 部分和第二芳基部分，以及被修饰为不是天然存在的羟基的葡萄糖C-6取代基或其药学上可接受的盐。

    Peptidyl derivatives as inhibitors of interleukin-1.beta. converting enzyme
    8.
    发明授权
    Peptidyl derivatives as inhibitors of interleukin-1.beta. converting enzyme 失效
    肽基衍生物作为白细胞介素-1β转换酶的抑制剂

    公开(公告)号：US5430128A

    公开(公告)日：1995-07-04

    申请号：US342991

    申请日：1994-11-21

    申请人： Kevin T. Chapman ,  Malcolm MacCoss ,  Adnan Mjalli

    发明人： Kevin T. Chapman ,  Malcolm MacCoss ,  Adnan Mjalli

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/08 ,  C07K5/00 ,  C07K7/00 ,  C07K17/00

    CPC分类号： C07K5/0202 ,  A61K38/00

    摘要： Novel peptidyl derivatives of formula I are found to be potent inhibitors of interleukin-1.beta. converting enzyme (ICE). Compounds of formula I may be useful in the treatment of inflammatory or immune-based diseases of the lung and airways; central nervous system and surrounding membranes; the eyes and ears; joints, bones, and connective tissues; cardiovascular system including the pericardium; the gastrointestinal and urogenital systems; the skin and mucosal membranes. Compounds of formula I are also useful in treating the complications of infection (e.g., gram negative shock) and tumors in which IL 1 functions as an autocrine growth factor or as a mediator of cachexia. ##STR1##

    摘要翻译： 发现式I的新型肽基衍生物是白细胞介素-1β转换酶（ICE）的有效抑制剂。 式I化合物可用于治疗肺和气道炎性或免疫性疾病; 中枢神经系统和周围膜; 眼睛和耳朵 关节，骨骼和结缔组织; 包括心包的心血管系统; 胃肠道和泌尿生殖系统; 皮肤和粘膜。 式I化合物也可用于治疗感染（例如，革兰氏阴性休克）的并发症和其中IL1作为自分泌生长因子或作为恶病质介质的肿瘤。