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-7468375-B2 优先权日:2004-04-26 标题:Inhibitors of the HIV integrase enzyme 发明人:DRESS KLAUS RUPRECHT; HU QIYUE; JOHNSON TED WILLIAM; PLEWE MICHAEL BRUNO; TANIS STEVEN PAUL; WANG HAI; YANG ANLE; YIN CHUNFENG; ZHANG JUNHU 权利人:PFIZER 摘要:The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIVâ€?) integrase enzyme.
专利号:US-9018203-B2 优先权日:2012-04-18 标题 :Pharmaceutical composition of salicylanilide-derived small molecules and preparation and application thereof 发明人:CHANG DEH-MING; HUANG HSU-SHAN; CHEN CHUN-LIANG; LEE CHIA-CHUNG 权利人:CHANG DEH-MING; HUANG HSU-SHAN; CHEN CHUN-LIANG; LEE CHIA-CHUNG; NAT DEFENSE MEDICAL CT 摘要:The present invention provides a pharmaceutical composition of salicylanilide-derived small molecules include:n (a) a compound which structure is selected from formula I or formula II: nn n n n n n n n n n n n (b) a pharmaceutically acceptable salt and excipient. The present invention also provides the synthesis method of the pharmaceutical composition and the application thereof.
专利号:PL-240596-B1 优先权日:2018-12-06 标 题 :Synthesis of pyridin-2-yl-vinylpyridinyl (PvP) derivatives
专利号:US-6861523-B2 优先权日:2002-02-08 标 题 :1,3,5- trisubstituted-1,3,5-triazine-2,4,6-trione compounds and libraries 发明人:YU YONGPING; OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TORREY PINES INST 摘要:The solid-phase synthesis of individual 1,3-disubstituted and 1,3,5-trisubstituted-1,3,5-triazine-2,4,6-triones and libraries thereof from a resin is described. Reaction of resin-bound amino acids with isocyanates yields resin-bound ureas, which further react with chlorocarbonyl isocyanate to selectively afford the resin-bound 1,3-disubstituted-1,3,5-triazine-2,4,6-triones. Selective alkylation at the N-5 position of the resin-bound 1,3-disubstituted-1,3,5-triazine-2,4,6-triones produces a trisubstituted triazinetrione. The products are cleaved from their solid support and obtained in good yield and purity.
专利号:US-2005113397-A1 优先权日:2002-01-31 标题:Imidazo[1,2-a]pyridine derivative 发明人:TAKEMURA MAKOTO; TAKAHASHI HISASHI; KAWAKAMI KATSUHIRO; TAKESHITA HIROSHI; KIMURA YOUICHI; WATANABE JUN; SUGIMOTO YUICHI; KITAMURA AKIHIRO; NAKAJIMA RYOHEI; KANAI KAZUO; FUJISAWA TETSUNORI 摘要:A compound reprsented by the following formula (I), its salts or nsolvates thereof capable of specifically or selectively expressig an antifungal activity in a broad spectrum based on the novel mechanism thereof of 1,6-β-glucan synthesis inhibition, and an antifungal agent containing any of them.
[参考文献]: Yan Luo, Et Al. Synthesis, Antibacterial And Antifungal Activities Of Novel 1,2,4-Triazolium Derivatives. Arch Pharm (Weinheim). 2009 Jul;342(7):386-93.
合成参考文献
摘要:Ulrich, H., Science of Synthesis, (2004) 17, 149.