CAS: 13735-13-2; 6-Bromothiochroman-4-One

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CAS号3528-17-4 硫代色满-4-酮 | CAS号13735-04-1 3-((4-溴苯基)硫代)丙酸 | CAS号7381-30-8 1,2-双(三甲基硅氧基)乙烷 | CAS号106-53-6 4-溴苯硫酚 | CAS号13457-82-4 sodium 4-bromob...

📜1,2-双(三甲基硅氧基)乙烷置于三氟甲磺酸三甲基硅酯体系中,化学反应生成6-溴硫代苯并二氢吡喃-4-酮
参考文献:Ep1031572
标题:Ep1031572

专利信息

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