专利号:US-7108846-B1 优先权日:1999-08-11 标题 :Methods for preparing perfluorinated [18f]-radiolabelled nitroimidazole derivatives for cellular hypoxia detection 发明人:MARCHAND JACQUELINE; GREGOIRE VINCENT 权利人:UNIV CATHOLIQUE LOUVAIN 摘要:The present invention relates to chemical synthesis of radiolabelled perfluorinated bioactive compounds. More particularly, the present invention relates to radiolabelled compounds to be used as indicators for tissue hypoxia. More particularly, the present invention relates to the synthesis and the use of [ 18 F] labelled perfluorinated nitroimidazole compounds having an incorporation of [ 18 F] atoms characterized by a specific radioactivity of the compound comprised between 1 and 30 Ci/mmol, preferably between 1 and 20 Ci/mmol, preferably 1 and 10 Ci/mmol. More particularly to [ 18 F] labelled EF3 or [ 18 F] labelled EF5. The present invention also relates to a method for the detection of tissue hypoxia in a patient comprising introducing an [ 18 F] labelled nitroimidazole compound into said patient, imaging tissue hypoxia in said patient, and, quantifying tissue hypoxia in said patient.
专利号:US-2006122240-A1 优先权日:2002-11-05 标题 :Benzotriazoles and methods of prophylaxis or treatment of metabolic-related disorders thereof 发明人:SEMPLE GRAEME; SKINNER PHILIP J; CHERRIER MARTIN C; WEBB PETER; TAMURA SUSAN Y 权利人:ARENA PHARM INC 摘要:The present invention relates to certain benzotriazole carboxylic acid or ester derivatives of Formula (I), pharmaceutically acceptable salts and solvates thereof, which exhibit useful pharmaceutical properties, for example, as agonists for the GPCR referred to as hRUP38. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the prophylaxis or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of -glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.
专利号:US-7169932-B2 优先权日:2001-06-11 标题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses, material for their synthesis 发明人:KUCERA DAVID JOHN; SCOTT ROBERT WILLIAM 权利人:PFIZER 摘要:Compounds of the formula: n nwhere the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.
专利号:US-2008176865-A1 优先权日:2005-06-15 标 题:Substituted arylpyrazoles 发明人:BILLEN DENIS; BOYLE JESSICA; CRITCHER DOUGLAS JAMES; GETHIN DAVID MORRIS; HALL KIM THOMAS; KYNE GRAHAM MICHAEL 权利人:PFIZER LTD 摘要:This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.
专利号:US-9192612-B2 优先权日:2013-02-13 标题:Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds 发明人:BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; BECK ELIZABETH MARY; DAVOREN JENNIFER ELIZABETH; LACHAPELLE ERIK ALPHIE; O'NEILL BRIAN THOMAS 权利人:PFIZER 摘要:The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, n nand the variables R 1 and R 2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-7968584-B2 优先权日:2005-06-15 标 题:Substituted arylpyrazoles 发明人:BILLEN DENIS; BOYLE JESSICA; CRITCHER DOUGLAS JAMES; GETHIN DAVID MORRIS; HALL KIM THOMAS; KYNE GRAHAM MICHAEL 权利人:PFIZER; PFIZER PROD INC 摘要:This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.
摘要:Toxicometric Parameters of Industrial Toxic Chemicals Under Single Exposure, Izmerov, N.F., et al., Moscow, Centre of International Projects, GKNT, 1982, -(116), 1982