专利号:US-8835476-B2 优先权日:2005-03-04 标 题:Synthesis of novel antimicrobials 发明人:WU FAN; WEAVER DONALD; BARDEN CHRIS; MCMASTER CHRISTOPHER; BYERS DAVID; HENNEBERRY ANNETTE; BAN FUQIANG 权利人:WU FAN; WEAVER DONALD; BARDEN CHRIS; MCMASTER CHRISTOPHER; BYERS DAVID; HENNEBERRY ANNETTE; BAN FUQIANG 摘要:The synthesis and activity of novel LpxA inhibitors is described, these inhibitors present antibacterial activity. The compounds were designed based on a receptor model developed using the crystal structure of LpxA and are arranged to have a favorable binding interaction at the active site of the enzyme. In particular, the compounds present the following formula (I) where V, W, X, Y and Z can be independently C, S, N or O and P1, P2 and P3 are ligands to bind to the three points of the proposed pharmacophore model. They can be chosen from a variety of groups.
专利号:US-2006069260-A1 优先权日:2004-09-28 标 题:Preparation of N-aryl pyridones 发明人:ZHANG HUIPING; CHEN BANG-CHI; ZHAO RULIN 权利人:ZHANG HUIPING; CHEN BANG-CHI; ZHAO RULIN 摘要:A novel process and intermediates thereof for making N-aryl pyridones of the type shown below from appropriate pyridinolates is described. n nThese compounds are useful as intermediates for the synthesis of clinical candidates.
专利号:US-7582771-B2 优先权日:2003-09-03 标题:Process for the synthesis of cPLA2 inhibitors 发明人:DEHNHARDT CHRISTOPH M; MEGATI SREENIVASULU; MICHALAK RONALD S; RAVEENDRANATH PANOLIL; REN JIANXIN; WU CHARLES C; WU YANGZHONG 权利人:WYETH CORP 摘要:A process for making the compound of formula (I) n nwherein Ac represents acetate; X represents O or CH 2 ; Y represents C 1 -C 6 alkyl; and Z is selected from the group consisting of H, halogen, CN, CHO, CF 3 , OCF 3 , OH, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 thioalkyl, NH 2 , N(C 1 -C 6 alkyl) 2 , NH(C 1 -C 6 alkyl), NC(O)—(C 1 C 6 alkyl), and NO 2 . In his process, a compound of formula (II)n n nis reacted with hydrazine to form a primary alkylamine, and then the primary alkylamine is reacted with acetic anhydride, to produce the compound of formula (I).
专利号:US-10647688-B2 优先权日:2014-12-19 标题:Compounds, synthesis method thereof and use of same in medicine and in cosmetics 发明人:PORTAL THIBAUD 权利人:GALDERMA RES & DEV 摘要:Novel compounds, synthesis methods and use of the same in medicine and in cosmetics are disclosed. Also disclosed, are novel compounds and ligands that modulate RARs.
专利号:US-6090810-A 优先权日:1995-09-01 标题:Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities 发明人:KLEIN ELLIOTT S; JOHNSON ALAN T; STANDEVEN ANDREW M; BEARD RICHARD L; GILLETT SAMUEL J; DUONG TIEN T; NAGPAL SUNIL; VULIGONDA VIDYASAGAR; TENG MIN; CHANDRARATNA ROSHANTHA A 权利人:ALLERGAN SALES INC 摘要:Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.
专利号:US-5877207-A 优先权日:1996-03-11 标 题:Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities 发明人:KLEIN ELLIOTT S; JOHNSON ALAN T; STANDEVEN ANDREW M; BEARD RICHARD L; GILLETT SAMUEL J; DUONG TIEN T; NAGPAL SUNIL; VULIGONDA VIDYASAGAR; TENG MIN; CHANDRARATNA ROSHANTHA A 权利人:ALLERGAN SALES INC 摘要:Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.
摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 591. 摘要:Stará, I. G.; Starý, I., Science of Synthesis, (2010) 45, 902. 摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 599. 摘要:Alonso, D. A.; Nájera, C., Science of Synthesis, (2010) 47, 473. 摘要:Sartori, G.; Maggi, R., Science of Synthesis, (2010) 47, 520.