CAS: 151917-39-4; Ethyl 6-Iodonicotinate

相似化合物

13054-02-9 173157-33-0 614-18-6

上下游产品

6-iodo-nicotinic acid chloroformic acid ethyl ester ethanol Triethyl orthoacetate (3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl) (5-carboxypyrid-2-yl)sulfide ethyl 2-ethynylpyridine-5-carboxylate 5-(hydroxymethyl)-2-iodopyridine 4-(8,8-dimethyl-5-oxo-5,6,7,8-tetrahydronaphthalene-2-yl-ethynyl)-benzoic acid ethyl ester

📜6-碘烟酸,氯甲酸乙酯置于4-二甲氨基吡啶,三乙胺体系中,用 二氯甲烷 用作溶剂,化学反应 2.0H,以76%的收率获得6-碘吡啶-3-羧酸乙酯
参考文献:N-(2-二乙基氨基乙基)-4-碘代苯甲酰胺的放射性标记(杂)芳族类似物的评估,用于黑色素瘤的成像和放射性核素治疗.
标题:N-(2-二乙基氨基乙基)-4-碘代苯甲酰胺的放射性标记(杂)芳族类似物的评估,用于黑色素瘤的成像和放射性核素治疗.
摘要:使用对黑素瘤组织具有特定亲和力的放射性碘化化合物的靶向放射性核素治疗是弥散性黑素瘤的一种有前途的治疗方法,但具有理想动力学特征的候选药物仍有待发现.靶向放射性核素疗法集中了对肿瘤细胞的作用,从而提高了疗效并降低了放射疗法的发病率.在这种情况下,N-(2-二乙基氨基乙基)-4-碘代苯甲酰胺(bza)的类似物是令人关注的.合成了多种bza的(杂)芳族类似物5并用(125)i进行了放射性碘标记,并在静脉注射后研究了它们在荷黑素瘤小鼠中的生物分布.大多数[(125)i] 5标记的化合物似乎与黑素瘤肿瘤特异性结合并且具有中到高亲和力.5H和5K这两种化合物,
Doi:10.1021/jm701424G

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