专利号:US-6818773-B2 优先权日:2001-10-15 标题:Synthesis of 4-[(Z)-4-bromophenyl)(ethoxyimino) methyl]-1'-[(2,4-dimethyl-1-oxido-3-pyridinyl)carbony)]-4'-methyl-1,4-′bipiperidine 发明人:CHEN MINZHANG; D SA BOSCO ANTHONY; LEONG WILLIAM W; GAN TONG; WONG GEORGE S K; TANG SUHAN; NIELSEN CHRISTOPHER MICHAEL 权利人:SCHERING CORP 摘要:In one embodiment, the present invention describes the synthesis of 4-[(Z)-(4-bromophenyl)(ethoxyimino)methyl]-1'-[(2,4-dimethyl-1-oxido-3-pyridinyl)carbonyl]-4'-methyl-1,4'-bipiperidine, and intermediates therefor from easily available starting materials by a simple route.
专利号:US-7947701-B2 优先权日:2003-11-14 标题:Dual molecules containing peroxy derivative, the synthesis and therapeutic applications thereof 发明人:CAZELLES JEROME; COSLEDAN FREDERIC; MEUNIER BERNARD; PELLET ALAIN 权利人:SANOFI AVENTIS 摘要:The invention relates to dual molecule compounds containing a peroxide derivative, to processes for the synthesis of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment and prevention of malaria comprising administering such compounds and such pharmaceutical compositions.
专利号:US-6326372-B1 优先权日:1999-09-30 标 题:Lactam and cyclic urea derivatives useful as alpha 1a adrenoceptor antagonists 发明人:EVANS BEN E; GILBERT KEVIN F 权利人:MERCK & CO INC 摘要:Lactam and cyclic urea derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
专利号:US-7361765-B2 优先权日:2003-10-27 标 题:Process for the preparation of CCR-2 antagonists 发明人:CAI DONGWEI; FLEITZ FRED; GE MIN; HOERRNER SCOTT; JAVADI GARY; JENSEN MARK; LARSEN ROBERT; LI WENJIE; NELSON DORIAN; SZUMIGALA ELIZABETH; YANG LIHU; ZHOU CHANGYOU 权利人:MERCK & CO INC 摘要:The present invention provides an efficient synthesis for the preparation of ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-m ethoxytetrahydro-2H-pyran-4-yl]amine and its succinate salt. The present invention additionally provides an efficient syntheses for the preparation of intermediates (3R)-3-methoxytetrahydro-4H-pyran-4-one; (1S,4S)-4-(2,5-dimethyl-1H-pyrrol-1-yl)-1-isopropylcyclopent-2-ene-1-carboxylic acid; and 3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,6-naphthyridine; and for the preparation of the precursor (3S,4S)-N-((1S,4S)-4-isopropyl-4-{[3-(tri-fluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopent-2-en-1-yl)-3-methoxytetrahydro-2H-pyran-4-amine. The invention additionally resides in the superior properties of the succinate salt of ((1R,3S)-3-isopropyl-3-1{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-methoxytetrahydro-2H-pyran-4-yl]amine
专利号:US-2003105131-A1 优先权日:2001-10-15 标题:Synthesis of 4-[(Z)-4-bromophenyl)(ethoxyimino) methyl]-1'-[(2,4-dimethyl-1-oxido-3-pyridinyl)carbonyl]-4'-methyl-1,4-'bipiperidine
专利号:US-6316437-B1 优先权日:1999-09-30 标题:Spirohydantoin compounds and uses thereof 发明人:HOFFMAN JACOB M 权利人:MERCK & CO INC 摘要:Spirohydantoin compounds and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
参考文献:10.1007/s10895-011-0915-2 摘要:Patil SR, Shelar DP, Rote RV, Jachak MN. A fluorescence study of new angular polycyclic blue light-emitting pyrazolo[3,4-h][1,6]naphthyridine and their interaction with bovine serum albumin (BSA). J Fluoresc. 2011 Nov;21(6):2037–52. doi: 10.1007/s10895-011-0915-2.