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107 条记录 (耗时 0.026 秒)

    HYDROLASE BINDING ASSAY
    45.
    发明公开
    HYDROLASE BINDING ASSAY 失效
    水解酶结合试验

    公开(公告)号：EP0937157A1

    公开(公告)日：1999-08-25

    申请号：EP97911090.0

    申请日：1997-11-03

    申请人： Merck Frosst Canada & Co.

    发明人： DESMARAIS, Sylvie ,  FRIESEN, Richard ,  GRESSER, Michael ,  KENNEDY, Brian ,  NICHOLSON, Don ,  RAMACHANDRAN, Chidambaran ,  SKOREY, Kathryn ,  FORD-HUTCHINSON, Anthony

    IPC分类号： G01N33 ,  C07K5 ,  C12N11 ,  C12N15 ,  C12Q1

    CPC分类号： G01N33/573 ,  C07K5/0827 ,  C12Q1/34 ,  C12Q1/37 ,  C12Q1/42 ,  G01N2333/96466

    摘要： Disclosed is a binding assay for proteases and phosphatases, which contain cysteine in their binding sites or as a necessary structural component for enzymatic binding. The sulfhydryl group of cysteine is the nucleophilic group in the enzyme's mechanistic proteolytic and hydrolytic properties. The assay can be used to determine the ability of new, unknown ligands and mixtures of compounds to competitively bind with the enzyme versus a known binding agent for the enzyme, e.g., a known enzyme inhibitor. By the use of a mutant form of the natural or native wild-type enzyme, in which serine, or another amino acid, e.g., alanine, replaces cysteine, the problem of interference from extraneous oxidizing and alkylating agents in the assay procedure is overcome. The interference arises because of oxidation or alkylation of the sulfhydryl, -SH (or -S-), in the cysteine, which then adversely affects the binding ability of the enzyme. Specifically disclosed is an assay for tyrosine phosphatases and cysteine proteases, including capsases and cathepsins, e.g., Cathepsin K(O2), utilizing scintillation proximity assay (SPA) technology. The assay has important applications in the discovery of compouds for the treatment and study of, for example, diabetes, immunosuppression, cancer, Alzheimer's disease and osteoporosis. The novel feature of the use of a mutant enzyme can be extended to its use in a wide variety of conventional colorimetric, photometric, spectrophotometric, radioimmunoassay and ligand-binding competitive assays.

    NITRIC OXIDE RELEASING SELECTIVE CYCLOOXYGENASE-2 INHIBITORS
    46.
    发明公开
    NITRIC OXIDE RELEASING SELECTIVE CYCLOOXYGENASE-2 INHIBITORS 审中-公开
    选择性环氧化酶-2抑制剂FREE寓氮氧化物

    公开(公告)号：EP1562914A1

    公开(公告)日：2005-08-17

    申请号：EP03769122.7

    申请日：2003-10-21

    申请人： MERCK FROSST CANADA & CO.

    发明人： WANG, Zhaoyin ,  YOUNG, Robert, N. ,  ZAMBONI, Robert

    IPC分类号： C07D261/08 ,  C07D231/12 ,  A61K31/415 ,  A61K31/42

    CPC分类号： C07D231/12 ,  C07D261/08

    摘要： The invention encompasses novel compounds of Formula (I) and Formula (II), which are nitric oxide-releasing prodrugs useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions and methods for treatment of cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula (I) or Formula (II). The above compounds may be used as a combination therapy with low-dose aspirin to treat chronic cyclooxygenase-2 mediated diseases or conditions while simultaneously reducing the risk of thrombotic cardiovascular events.

    DI-ARYL-SUBSTITUTED ETHANE PYRIDONE PDE4 INHIBITORS
    50.
    发明公开
    DI-ARYL-SUBSTITUTED ETHANE PYRIDONE PDE4 INHIBITORS 审中-公开
    二芳基取代的ETHANPYRIDONE作为PDE4抑制剂的

    公开(公告)号：EP1519922A1

    公开(公告)日：2005-04-06

    申请号：EP03739922.7

    申请日：2003-07-02

    申请人： MERCK FROSST CANADA & CO.

    发明人： COTE, Bernard ,  MARTINS, Evelyn

    IPC分类号： C07D213/64 ,  C07D417/06 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/444 ,  A61P11/06 ,  A61P29/00

    CPC分类号： C07D213/64 ,  C07D417/06

    摘要： Di-aryl substituted ethane pyridones, particularly ethane pyridones substituted with i) a phenyl, ii) a pyridyl, iii) a thiazole, iv) a pyrimidinyl, v) a pyridazinyl, vi) a furyl, vii) a thienyl, viii) an oxazolyl, ix) an isoxazolyl, or x) an isothiazolyl moiety are phosphodiesterase-4 inhibitors useful in the treatment or prevention of asthma; chronic bronchitis; chronic obstructive pulmonary disease; adult respiratory distress syndrome; infant respiratory distress syndrome; cough; chronic obstructive pulmonary disease in animals; adult respiratory distress syndrome; ulcerative colitis; Crohn's disease; hypersecretion of gastric acid; bacterial, fungal or viral induced sepsis or septic shock; endotoxic shock; laminitis or colic in horses; spinal cord trauma; head injury; neurogenic inflammation; pain; reperfusion injury of the brain; psoriatic arthritis; rheumatoid arthritis; ankylosing spondylitis; osteoarthritis; inflammation; or cytokine-mediated chronic tissue degeneration. Formula (I) wherein X is phenyl, pyridinyl, thiazolyl, pyrimidinyl, pyridazinyl, furyl, thienyl, oxazolyl, isoxazolyl, isothiazolyl.