专利号:US-6906046-B2 优先权日:2000-12-22 标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes 发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY 权利人:CELLTECH R & D INC 摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
专利号:US-7186709-B2 优先权日:2002-08-27 标 题:Dihydropyrancarboxamides and uses thereof 发明人:SCHREIBER STUART L; STAVENGER ROBERT A; MITCHISON TIMOTHY J; MALIGA ZOLTAN 权利人:HARVARD COLLEGE 摘要:The present invention provides novel dihydropyrancarboxamide compounds of formula (I): n nand collections of these compounds, and provides methods for the synthesis of these compounds; wherein R 1 –R 6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.
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-7829699-B2 优先权日:2006-04-10 标题:Process for the preparation of CGRP antagonist 发明人:BELYK KEVIN; RIVERA NELO 权利人:MERCK SHARP & DOHME 摘要:An efficient synthesis for the preparation of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1 -carboxamide, by coupling (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride with 1,1′-carbonyldiimidazole (“CDIâ€?) as carbonyl source; and an efficient preparation of the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide.
专利号:US-2003069305-A1 优先权日:2000-12-22 标题:Pharmaceutical uses and synthesis of benzobicyclooctanes
专利号:US-6096763-A 优先权日:1995-02-23 标题 :α1a adrenergic receptor antagonists 发明人:HOFFMAN JACOB M; CHANG RAYMOND S L 权利人:MERCK & CO INC 摘要:This invention relates to novel compounds, their synthesis and use as selective α 1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The compounds are selective in their ability to relax smooth muscle tissue enriched in the α 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 are achieved.
参考文献:10.1111/j.1476-5381.1996.tb15631.x 摘要:Candura SM, Messori E, Franceschetti GP, D'Agostino T, Vicini D, Tagliani M, Tonini M. Neural 5‐HT4receptors in the human isolated detrusor muscle: effects of indole, benzimidazolone and substituted benzamide agonists and antagonists. British J Pharmacology. 1996 Aug;118(8):1965–70. doi: 10.1111/j.1476-5381.1996.tb15631.x. 参考文献:10.1016/j.neo.2015.08.009 摘要:Bilsland AE, Pugliese A, Liu Y, Revie J, Burns S, McCormick C, Cairney CJ, Bower J, Drysdale M, Narita M, Sadaie M, Keith WN. Identification of a Selective G1-Phase Benzimidazolone Inhibitor by a Senescence-Targeted Virtual Screen Using Artificial Neural Networks. Neoplasia. 2015 Sep;17(9):704–15. 参考文献:10.1016/j.bmcl.2006.08.010 摘要:Finley DR, Bell MG, Borel AG, Bloomquist WE, Cohen ML, Heiman ML, Kriauciunas A, Matthews DP, Miles T, Neel DA, Rito CJ, Sall DJ, Shuker AJ, Stephens TW, Tinsley FC, Winter MA, Jesudason CD. Potent benzimidazolone based human beta(3)-adrenergic receptor agonists. Bioorg Med Chem Lett. 2006 Nov 01;16(21):5691–4. doi: 10.1016/j.bmcl.2006.08.010.