CAS: 183232-66-8; 1-(2,4-Dichlorophenyl)-5-(4-Iodophenyl)-4-Methyl-N-Piperidin-1-Ylpyrazole-3-Carboxamide

该化合物是一种合成有机化合物,其特点是结构复杂,包括一种配有多种芳香和热循环组的聚氨酯核心,以各种芳香和热循环组替代.该化合物的特点是二氯苯基组和一种有助于其潜在生物活动的碘联联苯组.由于存在一种管状动物,表明有可能与生物目标发生相互作用,从而引起对医药化学的兴趣.碳箱胺功能组可能提高溶性性和稳定性,而甲基组则可以影响化合物的脂性.

结构式图片

欧盟法规

C&L通报

上下游产品

1-(2,4-dichlorophenyl)-5-(4-bromophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide H-pyrazole-3-carboxylic acid piperidin-1-ylamide5-(4-amino-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 2,4-dichlorophenyl hydrazine hydr°Chloride 1-phenyl-propan-1-one4-(4-(1-(2,4-dichlorophenyl)-4-methyl-3-(piperidin-1-ylcarbamoyl)-1H-pyrazol-5-yl)phenyl)but-3-yn-1-yl nitrate 1-(2,4-dichlorophenyl)-5-(4-(4-iodobut-1-ynyl)phenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide

合成工艺路线路线简述

    📜5-(4-Bromophenyl)-1-(2,4-Dichlorophenyl)-4-Methyl-1H-Pyrazole-3-Carboxylic Acid置于四(三苯基膦)钯,氯化亚砜,Chloroamine-T,六正丁基二锡,溶剂黄146,三乙胺,Sodium Iodide体系中,用 二氯甲烷,甲苯 用作溶剂,化学反应 35.0H,反应生成1-(2,4-二氯苯基)-5-(4-碘苯基)-4-甲基-N-1-哌啶基-1H-吡唑-3-羧胺
    参考文献:Preparation Of Iodine-123 Labeled Am251: A Potential Spect Radioligand For The Brain Cannabinoid Cb1 Receptor
    标题:Preparation Of Iodine-123 Labeled Am251: A Potential Spect Radioligand For The Brain Cannabinoid Cb1 Receptor
    摘要:
    Doi:10.1002/(Sici)1099-1344(199610)38:10<875::Aid-Jlcr908>3.0.Co;2-G

    海关参考信息

    专利信息


    专利号:US-2022370650-A1
    优先权日:2021-03-26
    标 题 :Formulations and kits for the diagnostic evaluation of infectious diseases and methods thereof
    发明人:BRYANT JR JERRY L
    权利人:VYRIPHARM ENTPR INC
    摘要:Kits for the preparation, synthesis, and delivery of compositions comprising a conjugate of a nucleoside analog, a chelator, and a label for use as imaging and therapeutic agents. The kits, as well as methods for their use, may be used in diagnosing, treating, or monitoring the progression of infectious diseases and/or symptoms or complications resulting from infection.

    专利号:WO-2008084057-A1
    优先权日:2007-01-10
    标题:Compounds with a combination of cannabinoid-cb1 antagonism and serotonin reuptake inhibition
    发明人:LANGE JOSEPHUS H M; KRUSE CORNELIS G
    权利人:SOLVAY PHARM BV; LANGE JOSEPHUS H M; KRUSE CORNELIS G
    摘要:This invention relates to compounds with a combination of cannabinoid-CB1antagonism and serotonin reuptake inhibition to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders. In particular the invention relates to compoundsof the general formula (I): wherein the symbols have the meanings given in the specification.

    专利号:US-8138174-B2
    优先权日:2007-01-10
    标 题:Compounds with a combination of cannabinoid CB1 antagonism and serotonin reuptake inhibition
    发明人:LANGE JOSEPHUS H M; KRUSE CORNELIS G
    权利人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SOLVAY PHARM BV
    摘要:Compounds with a combination of cannabinoid CB 1 antagonism and serotonin reuptake inhibition, pharmaceutical compositions containing these compounds, methods for preparing these compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing these compositions are disclosed. Uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders are disclosed. n In at least one embodiment, the invention relates to compounds of the general formula (1): n nwherein the substitutents have the definitions given in the specification.

    专利号:US-7754188-B2
    优先权日:2003-06-30
    标 题:Radiolabeled cannabinoid-1 receptor modulators
    发明人:BURNS H DONALD; CHEN ALEX M; GIBSON RAYMOND E; GOULET MARK T; HAGMANN WILLIAM K; HAMILL TERENCE G; JEWELL JAMES P; LIN LINUS S; LIU PING; PERESYPKIN ANDREY V
    权利人:MERCK SHARP & DOHME
    摘要:The present invention relates to particular radiolabeled Cannabinoid-1 (CB1) receptor modulators, and methods of using these modulators for labeling and diagnostic imaging of Cannabinoid-1 receptors in mammals, particularly humans. In addition, intermediates useful for the synthesis of the radiolabeled Cannabinoid-1 receptor modulators are also disclosed, as well as the processes for synthesizing the radiolabeled Cannabinoid-1 receptor modulators. Still further, formulations of the radiolabeled Cannabinoid-1 receptor compounds are described.

    专利号:US-2024109830-A1
    优先权日:2020-07-10
    标题:Cannabis extracts and uses thereof
    发明人:LINCIANO PASQUALE; CITTI CINZIA; RUSSO FABIANA; LUONGO LIVIO; IANNOTTA MONICA; BELARDO CARMELA; MAIONE SABATINO; VANDELLI MARIA ANGELA; FORNI FLAVIO; GIGLI GIUSEPPE; LAGANÃ? ALDO; CAPRIOTTI ANNA LAURA; MONTONE CARMELA MARIA; CANNAZZA GIUSEPPE
    权利人:CONSIGLIO NAZIONALE RICERCHE; UNIV DEGLI STUDI DI MODENA E REGGIO EMILIA; SAPIENZA UNIV DI ROMA
    摘要:The present disclosure concerns a group of cannabinoid compounds defined by formulas (I) to (IV), wherein R1 is —H or —COOH, for the first time isolated and fully characterized in structure, absolute stereochemistry by the present applicant. Methods of isolation, characterization, stereoselective synthesis, biological activity, pharmaceutical composition and therapeutic applications of the present compounds as modulators of the cannabinoid CB1 receptor are also object of the disclosure.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Raffa RB, Ward SJ. CB₁-independent mechanisms of Δ⁹-THCV, AM251 and SR141716 (rimonabant). J Clin Pharm Ther. 2012 Jun;37(3):260-5. doi: 10.1111/j.1365-2710.2011.01284.x. Epub 2011 Jul 11. 11(12):e0167848. doi: 10.1371/journal.pone.0167848.
    3: O'Keefe L, Vu T, Simcocks AC, Jenkin KA, Mathai ML, Hryciw DH, Hutchinson DS, McAinch AJ. CB1 Ligand AM251 Induces Weight Loss and Fat Reduction in Addition to Increased Systemic Inflammation in Diet-Induced Obesity. Int J Mol Sci. 2022 Sep 28;23(19):11447. doi: 10.3390/ijms231911447.
    4: Correia-Sá IB, Carvalho CM, Serrão PV, Machado VA, Carvalho SO, Marques M, Vieira-Coelho MA. AM251, a cannabinoid receptor 1 antagonist, prevents human fibroblasts differentiation and collagen deposition induced by TGF-β - An in vitro study. Eur J Pharmacol. 2021 Feb 5;892:173738. doi: 10.1016/j.ejphar.2020.173738. Epub 2020 Nov 19. 26(7):754-62. doi: 10.1097/CAD.0000000000000246. 63(3):670-9. doi: 10.1016/s1734-1140(11)70578-3. 83(1):157-66. doi: 10.1124/mol.112.082651. Epub 2012 Oct 12.

    合成参考文献


    参考文献:10.1186/1471-2210-11-6
    摘要:Hayase T. Differential effects of TRPV1 receptor ligands against nicotine-induced depression-like behaviors. BMC Pharmacol. 2011 Jul 18;11():6.
    参考文献:10.1016/j.ejphar.2011.06.057
    摘要:Curto-Reyes V, Boto T, Hidalgo A, Menéndez L, Baamonde A. Antinociceptive effects induced through the stimulation of spinal cannabinoid type 2 receptors in chronically inflamed mice. Eur J Pharmacol. 2011 Oct 01;668(1-2):184–9. doi: 10.1016/j.ejphar.2011.06.057.
    参考文献:10.1007/s00213-011-2412-3
    摘要:Dasilva MA, Grieve KL, Cudeiro J, Rivadulla C. Endocannabinoid CB1 receptors modulate visual output from the thalamus. Psychopharmacology (Berl). 2012 Feb;219(3):835–45. doi: 10.1007/s00213-011-2412-3.
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