CAS: 5817-39-0; L-3,3',5'-Triiodothyronine

上下游产品

3',5'-Diiodothyronine 3-Monoiodothyronine L-thyroxine N-acetyl-3-iodo-L-tyrosine3'-Iodothyronine 3-Monoiodothyronine L-3,3'-Diiodothyronine 3',5'-Diiodothyronine

甲状腺素置于naphthalene-1,8-Diselenol,1,4-二巯基-2,3-丁二醇体系中,化学反应生成 碘塞罗宁
参考文献:碘甲状腺原氨酸脱碘酶模拟物对甲状腺激素的脱碘:反应性的增加是否会改变区域选择性
标题:碘甲状腺原氨酸脱碘酶模拟物对甲状腺激素的脱碘:反应性的增加是否会改变区域选择性
摘要:描述了作为碘甲状腺原氨酸脱碘酶功能模拟物的有机硒化合物.具有两个硒醇基团的萘基化合物在甲状腺素的内环脱碘中非常有效.在硒醇部分之一附近引入碱性氨基可增强脱碘作用.该研究表明,脱碘酶活性位点上保守的 Cys 残基亲核反应性的增加对于有效脱碘非常重要.
DOI:10.1021/ja201657S

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-2003186847-A1
优先权日:2000-07-10
标题 :Insulin derivatives and synthesis thereof
发明人：JONES RICHARD HENRY; SHOJAEE-MORADI FARIBA; BRANDENBURG DIETRICH; SUNDERMANN ERIK
摘要:Derivatives of insulin are described which are conjugated to thyroid hormones. The thyroid hormone is, for instance, D-thyroxine (3,3′,5,5′-tetraiodo-D-thyronine). Other analogues are described in which a spacer having a alkanediyl chain at least eleven carbon atoms long is included. Binding studies show useful binding characteristics to thyroid binding proteins. New synthetic methods in which racemisation of the thyroxin is minimised, are described.

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-5169984-A
优先权日:1990-09-10
标题:Synthesis and characterization of N-bromoacetyl-3,3'5-triiodo-L-thyronine using high speed countercurrent chromatography
发明人：CAHNMANN HANS J; ITO YOICHIRO
权利人:US HEALTH
摘要:A method for synthesizing N-bromoacetyl-3,3',5-triiodo-L-thyronine which involves subjecting 3,3', 5-triiodo-L-thyronine to a one-step bromacetylation reaction wherein 3,3', 5-triiodo-L-thyronine and bromoacetyl bromide are refluxed together in a solution of ethyl acetate. After formation the N-bromoacetyl-3,3'-triiodo-L-thyronine is purified by fractionation utilizing high speed countercurrent chromatography. Labeled N-bromoacetyl-3,3'-5-triiodo-L-thryonine may be made by a one-step bromacetylation reaction by reducing either [ 125 I]T 3 or [ 14 C]T 3 with bromoacetyl bromide.