专利号:US-6770763-B2 优先权日:2002-06-11 标题 :Asymmetric synthesis of amino-pyrrolidinones 发明人:MAGNUS NICHOLAS A; CONFALONE PASQUALE N; SAVAGE SCOTT A; YATES MATTHEW; WALTERMIRE ROBERT E; MELONI DAVID J; CAMPAGNA SILVIO 权利人:BRISTOL MYERS SQUIBB CO 摘要:A novel process for the asymmetric synthesis of an amino-pyrrolidinone of the type shown below from appropriate pyrrolidinones is described.These compounds are useful as intermediates for MMP and TACE inhibitors.
专利号:US-2008287407-A1 优先权日:2003-12-10 标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use 发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.
专利号:US-7148362-B2 优先权日:2003-09-18 标题:Process for the preparation of enantiopure pyrrolidin-2-one derivatives 发明人:IDING HANS; KRUMMENACHER DANIELA; WIRZ BEAT; WOSTL WOLFGANG 权利人:HOFFMANN LA ROCHE 摘要:The present invention relates to a process for the preparation of enantiopure intermediates useful in the synthesis of valuable pharmaceutically active compounds, e.g. MAOB inhibitors, and to novel intermediates of formulae I and II n nwherein R 21 , R 22 , R 23 and R 24 are as defined in the description and claims.
专利号:US-7612106-B2 优先权日:2004-12-23 标题 :Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof 发明人:BOATMAN P DOUGLAS; SCHRADER THOMAS O; SEMPLE GRAEME; SKINNER PHILIP J; JUNG JAE-KYU 权利人:ARENA PHARM INC 摘要:The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. n nAlso 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 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 α-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, DP receptor antagonists, and the like.
专利号:US-2003236401-A1 优先权日:2002-06-11 标 题:Asymmetric synthesis of amino-pyrrolidinones
专利号:US-6004965-A 优先权日:1994-12-20 标题 :Sulfonamides 发明人:BREU VOLKER; BURRI KASPAR; CASSAL JEAN-MARIE; CLOZEL MARTINE; HIRTH GEORGES; LOEFFLER BERND-MICHAEL; MUELLER MARCEL; NEIDHART WERNER; RAMUZ HENRI 权利人:HOFFMANN LA ROCHE 摘要:Compounds of the formula: ##STR1## where A, B, R 1 -R 8 are as described herein are endothelin inhibitors that can be used in treating diseases associated with endothelin, such as high blood pressure. Chemical synthesis of these compounds and pharmaceutical compositions containing these compounds are also useful.
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