CAS: 701977-09-5; [14C]-Taranabant

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    📜3-{(1S,2S)-1-(4-Chlorobenzyl)-2-[(2-Methyl-2-{[5-(Trifluoromethyl)Pyridin-2-Yl]Oxy}Propanoyl)Amino]Propyl}Benzamide 以99.2% Ee; 90的收率获得产物n-[(1S,2S)-3-(4-氯苯基)-2-(3-氰基苯基)-1-甲基丙基]-2-甲基-2-[(5-(三氟甲基)吡啶-2-基)氧基]丙酰胺
    参考文献: Formation Of Tetra-Substituted Enamides And Stereoselective Reduction Thereof[fr] Formation D'Enamides Tetra-Substitues Et Reduction Stereoselective De Ces Derniers
    标题: Formation Of Tetra-Substituted Enamides And Stereoselective Reduction Thereof[fr] Formation D'Enamides Tetra-Substitues Et Reduction Stereoselective De Ces Derniers
    摘要:本发明涉及一种实用的过程,通过钯催化偶联结构式(iii)的化合物与一级酰胺(iv)进行偶联反应,制备出烯酰胺(II).此外,本发明还涉及通过该过程制备的化合物的晶体形式,特别是无水晶体形式b和分别属于三种模式的晶体溶剂,即第一型,第二型和第三型,以及在该过程中产生的晶体中间体化合物.此外,本发明还涉及四取代烯酰胺(II)的立体选择性还原,得到相应的酰胺(i).

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    专利信息


    专利号:US-10005720-B2
    优先权日:2013-04-05
    标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
    发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
    权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
    摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

    专利号:US-8063062-B2
    优先权日:2006-12-20
    标 题 :Compounds with a combination of cannabinoid-CB1 antagonism and acetylcholinesterase inhibition
    发明人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SHADID BELAL
    权利人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SHADID BELAL; SOLVAY PHARM BV
    摘要:Embodiments of this invention relate to compounds having a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition, to pharmaceutical compositions comprising these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions comprising these compounds. The invention also relates to methods of treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficit disorder, traumatic brain injury, drug dependence, addiction or substance abuse by administering a pharmaceutical composition comprising these compounds to a patient in need thereof. A compound with a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition is a compound of formula (1) n nwherein the symbols have the meanings given in the specification.

    专利号:US-2018370905-A1
    优先权日:2013-04-05
    标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same

    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-2011301143-A1
    优先权日:2009-02-23
    标题 :Heterocyclic derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
    发明人:ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN
    权利人:ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN
    摘要:Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1— substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N—CR5R6, Câ• CR5 or CR13—CR5R6, Y is a bond or —C(O)—, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis, obesity, diabetes, neurological disease, Metabolic Syndrome, insulin resistance, cancer, liver steatosis, and non-alcoholic steatohepatitis.

    专利号:US-2012010186-A1
    优先权日:2009-03-23
    标题:Heterocyclic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
    发明人:LACHANCE NICOLAS; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; TRANMER GEOFFREY K; MARTINS EVELYN; GAREAU YVES
    权利人:LACHANCE NICOLAS; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; TRANMER GEOFFREY K; MARTINS EVELYN; GAREAU YVES; MERCK FROSST CANADA LTD
    摘要:Heterocyclic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer, liver steatosis; and non-alcoholic steatohepatitis.

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    📌 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: Fichna J, Sibaev A, Sałaga M, Sobczak M, Storr M. The cannabinoid-1 receptor inverse agonist taranabant reduces abdominal pain and increases intestinal transit in mice. Neurogastroenterol Motil. 2013 Aug;25(8):e550-9. doi: 10.1111/nmo.12158. Epub 2013 May 21. doi: 10.1097/JCP.0b013e31825d380d. doi: 10.3109/00498254.2010.509820. doi: 10.1016/j.bmcl.2010.06.127. Epub 2010 Jul 1. doi: 10.3109/00498254.2010.501117. doi: 10.1208/s12248-010-9212-2. Epub 2010 Jun 26.
    7: Kipnes MS, Hollander P, Fujioka K, Gantz I, Seck T, Erondu N, Shentu Y, Lu K, Suryawanshi S, Chou M, Johnson-Levonas AO, Heymsfield SB, Shapiro D, Kaufman KD, Amatruda JM. A one-year study to assess the safety and efficacy of the CB1R inverse agonist taranabant in overweight and obese patients with type 2 diabetes. Diabetes Obes Metab. 2010 Jun;12(6):517-31. doi: 10.1111/j.1463-1326.2009.01188.x. doi: 10.1038/nrendo.2010.56. doi: 10.1038/oby.2010.67. Epub 2010 Apr 8. doi: 10.1038/ijo.2010.38. Epub 2010 Mar 9. doi: 10.1007/s00213-010-1790-2. Epub 2010 Feb 27. doi: 10.1038/ijo.2010.21. Epub 2010 Feb 16. doi: 10.1111/j.1471-4159.2009.06549.x. Epub 2009 Dec 17. doi: 10.1177/0091270009341651. doi: 10.1007/s12325-009-0003-z. Epub 2009 Feb 14. doi: 10.1016/j.jpba.2009.01.003. Epub 2009 Jan 9. doi: 10.1007/s12325-008-0116-9. doi: 10.1177/0091270008325930. Epub 2008 Oct 20. Review. doi: 10.1002/ardp.200700255. Review.

    合成参考文献


    参考文献:10.1038/ijo.2010.21
    摘要:Aronne LJ, Tonstad S, Moreno M, Gantz I, Erondu N, Suryawanshi S, Molony C, Sieberts S, Nayee J, Meehan AG, Shapiro D, Heymsfield SB, Kaufman KD, Amatruda JM. A clinical trial assessing the safety and efficacy of taranabant, a CB1R inverse agonist, in obese and overweight patients: a high-dose study. International Journal of Obesity. 2010 Feb 16;34(5):919–35. doi: 10.1038/ijo.2010.21.
    参考文献:10.2165/11592040-000000000-00000
    摘要:Cheung BM. Drug treatment for obesity in the post-sibutramine era. Drug Saf. 2011 Aug 01;34(8):641–50. doi: 10.2165/11592040-000000000-00000.
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