专利号:US-6867202-B1 优先权日:1997-06-25 标 题 :Treatment of insulin resistance 发明人:CARPINO PHILIP ALBERT; CHIU CHARLES KWOK-FUNG; PAN LYDIA CODETTA; LEFKER BRUCE ALLEN; TREADWAY JUDITH LEE; ZAWISTOSKI MICHAEL PAUL 权利人:PFIZER 摘要:This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, n n nwhere the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.
专利号:US-8575331-B2 优先权日:2003-01-15 标题:Synthesis and use of 2′-substituted-N6-modified nucleosides 发明人:AN HAOYUN; RAMASAMY KANDA; SHAW STEPHANIE 权利人:AN HAOYUN; RAMASAMY KANDA; SHAW STEPHANIE; VALEANT PHARMACEUTICALS NORTH AMERICA 摘要:An improved method of preparing a sugar modified nucleoside analog includes a protocol in which a hydroxy group of a sugar is selectively deprotected and oxidized prior to nucleophilic modification of the corresponding carbonyl group. The modified sugar is then coupled to a heterocyclic base that is modified with a dual nucleophilic reagent in a further step that provides N6-modified adenosine analogs with high stereoselectivity.
专利号:US-2006135465-A1 优先权日:2003-01-15 标题:Synthesis and use of 2'-substituted-n6-modified nucleosides
专利号:US-2011196144-A1 优先权日:2003-01-15 标题 :Synthesis and use of 2'-substituted-n6-modified nucleosides
专利号:US-7799908-B2 优先权日:2003-01-15 标题:Synthesis and use of 2′-substituted-N6 -modified nucleosides
专利号:WO-2004065398-A2 优先权日:2003-01-15 标 题:Synthesis and use of 2'-substituted-n6-modified nucleosides
参考文献:10.1134/s0036024407030168 摘要:Rodin IA, Smolenkov AD, Shpak AV, Shpigun OA. Ion-chromatographic determination of the constant of ion exchange of aliphatic hydrazines and amines on silica-gel-based sulfocationites. Russian Journal of Physical Chemistry A. 2007 Mar;81(3):390–5. doi: 10.1134/s0036024407030168.