CAS: 87051-43-2; Ritanserin

该化合物是一种选择性的血清素受体激素激素对抗剂,主要针对5-HT2A和5-HT2C子型,显示这些受体具有高度亲近性和特殊性,使其成为研究血清素介质途径的药理研究的宝贵工具;Ritanserin因其对血清素信号的调制作用,在...

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6-(2-氯乙基)-7-甲基-[1,3]噻唑并[3,2-A]嘧啶-5-酮 6-(2-Chloroethyl)-7-Methyl-5H-[1,3]Thiazolo[3,2-A]Pyrimidin-5-One 86488-00-8

合成工艺路线路线简述

  • 58113-36-3 + 86488-00-8 = 87051-43-2 [标题:Reaction Conditions
    标题:[bis(Aryl)Methylene]-1-Piperidinyl)Alkyl Pyrimidinones
    参考文献:European Patent Organization]

    93076-09-6 = 87051-43-2 [标题:Reaction Conditions
    标题:[bis(Aryl)Methylene]-1-Piperidinyl)Alkyl Pyrimidinones
    参考文献:European Patent Organization]

    111627-25-9 = 87051-43-2 [标题:Reaction Conditions
    标题:[bis(Aryl)Methylene]-1-Piperidinyl)Alkyl Pyrimidinones
    参考文献:European Patent Organization
6-(2-氯乙基)-7-甲基-[1,3]噻唑并[3,2-A]嘧啶-5-酮,4-(双(4-氟苯基)亚甲基)哌啶 反应生成 利坦色林
参考文献:Kennis,L. E. J.;Vandenberk,J.;Mertens,J. C.
标题:Kennis,L. E. J.;Vandenberk,J.;Mertens,J. C.

海关参考信息

专利信息


专利号:US-9315483-B2
优先权日:2007-09-13
标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
权利人:CONCERT PHARMACEUTICALS INC
摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

专利号:US-2008214827-A1
优先权日:2004-02-03
标 题:Synthesis of Cyanoimino-Benzoimidazoles
发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
权利人:EURO CELTIQUE SA
摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

专利号:US-8815883-B2
优先权日:2009-11-02
标 题 :Compounds and methods for inhibiting serotonin synthesis
发明人:LANDRY DONALD; DENG SHI-XIAN
权利人:LANDRY DONALD; DENG SHI-XIAN; TRUSTEES OF COLUMBIA UNVIERSITY IN THE CITY OF NEW YORK
摘要:Compounds having the structures below that are TPH1 inhibitors are provided: The compounds are useful of, e.g., to increase bone mass. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis.

专利号:US-7309799-B2
优先权日:2004-06-01
标 题:Methods for the synthesis of milnacipran and congeners thereof
发明人:BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V
权利人:COLLEGIUM PHARMACEUTICAL INC
摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.

专利号:US-2012282255-A1
优先权日:2011-04-07
标题 :Methods and compositions for the treatment of alcoholism and alcohol dependence
发明人:PLUCINSKI GREG
权利人:PLUCINSKI GREG
摘要:The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated. Accordingly, the methods and compositions of the invention are useful for preventing, treating, diagnosing, or monitoring the progression various alcohol and drug dependency diseases disclosed herein.

专利号:US-7749985-B2
优先权日:2006-09-15
标 题 :Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
发明人:GALLOP MARK A; XU FENG; PHAN THU; DILIP USHA; PENG GE
权利人:XENOPORT INC
摘要:Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of making acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of using acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, and pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs 3-aminopropylphosphinic acid and analogs thereof for treating diseases or disorders such as mild cognitive impairment, cognitive impairment associated with Alzheimer's disease Alzheimer's disease, depression, anxiety, and epilepsy are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, which are suitable for oral administration and sustained release oral dosage forms are also disclosed.
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CAS号:87051-43-2
中文名:利坦丝林
英文名:Ritanserin
纯度:99% HPLC1G/5G/1KG
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主要参考文献


1: Tan J, Zhong M, Hu Y, Pan G, Yao J, Tang Y, Duan H, Jiang Y, Shan W, Lin J, Liu Y, Huang J, Zheng H, Zhou Y, Fu G, Li Z, Xu B, Zha J. Ritanserin suppresses acute myeloid leukemia by inhibiting DGKα to downregulate phospholipase D and the Jak-Stat/MAPK pathway. Discov Oncol. 2023 Jul 1;14(1):118. doi: 10.1007/s12672-023-00737-9.
2: Zhou D, Liu T, Rao X, Jie X, Chen Y, Wu Z, Deng H, Zhang D, Wang J, Wu G. Targeting diacylglycerol kinase α impairs lung tumorigenesis by inhibiting cyclin D3. Thorac Cancer. 2023 May;14(13):1179-1191. doi: 10.1111/1759-7714.14851. Epub 2023 Mar 25.
3: Jiang SS, Gong MN, Rao W, Chai W, Chen WZ, Zhang X, Nie HB, Xu RS. 5-Hydroxytryptamine: a potential therapeutic target in amyotrophic lateral sclerosis. Neural Regen Res. 2023 Sep;18(9):2047-2055. doi: 10.4103/1673-5374.367929.

合成参考文献


参考文献:10.1186/2047-783x-14-s4-32
摘要:Budzinska K. Serotoninergic modulation of cortical and respiratory responses to episodic hypoxia. European Journal of Medical Research. 2009 Dec 07;14(Suppl 4):32. doi: 10.1186/2047-783x-14-s4-32.
参考文献:10.1017/s146114571000009x
摘要:Bortolozzi A, Masana M, Díaz-Mataix L, Cortés R, Scorza MC, Gingrich JA, Toth M, Artigas F. Dopamine release induced by atypical antipsychotics in prefrontal cortex requires 5-HT(1A) receptors but not 5-HT(2A) receptors. Int J Neuropsychopharmacol. 2010 Nov;13(10):1299–314.
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