合成目标产物 6-Bromo-2-Naphthoic Acid 主要起始原料 6-Bromo-2-Naphthol And Acetic Acid
(文献来源)合成步骤主要原料 6-Bromo-2-Naphthol 和 Acetic Acid
Alkaline Earth Salt Of/the/ Methylsulfuric Acid置于硝酸体系中,化学反应生成 6-溴-2-萘甲酸 参考文献:Dziewonski; Sternbach,Bulletin De L'Academie Polonaise Des Sciences,Serie Des Sciences Chimiques,1931,Vol.,P. 59,65 标题:Dziewonski; Sternbach,Bulletin De L'Academie Polonaise Des Sciences,Serie Des Sciences Chimiques,1931,Vol.,P. 59,65
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.
专利号:US-2003219832-A1 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; STANDEVEN ANDREW M; NAGPAL SUNIL; CHANDRARATNA ROSHANTHA A 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-6469028-B1 优先权日:1995-09-01 标题:Synthesis and use of retinoid compounds having negative hormone and/or anatgonist 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 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-5958954-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:2,2-Dialkyl-4-aryl-substituted benzopyran and benzothiopyran derivatives of the formula where the symbols have the meaning described in the specification, 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.
专利号:US-2002156054-A1 优先权日:1995-09-01 标题:Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
参考文献:10.1007/s00044-024-03245-9 摘要:Zhang Y, Dai L, Tan Y, Yu Y, Xing J, Yang F, Ren B, Xu Y, Li Q. Design and synthesis of novel factor XIa Inhibitors with bicyclic isoquinoline and naphthalene fragments. Med Chem Res. 2024 May 30;33(6):1003–23. doi: 10.1007/s00044-024-03245-9.