CAS: 211513-37-0; S-(2-(1-(2-Ethylbutyl)Cyclohexane-1-Carboxamido)Phenyl) 2-Methylpropanethioate
该化合物是一种合成小分子,主要作为胆固醇基转移蛋白抑制剂(CETP),其开发目的是提高高密度脂蛋白胆固醇水平,改善心血管结果;甲虫菌的特征是其独特的化学结构,其中包括一个苯基组和一个环状动物,有助于其生物活动;该化合物已经研究过其调整脂质剖面和降低肾脏硬化风险的潜力;在临床试验中,甲虫菌菌表现出一种有利的安全特征,但减少心血管事件的效果一直是辩论的主题,导致各种研究的结果参差不齐;该化合物在有机溶剂中溶解,并表现出特定的致癌性,包括主要通过肝道的代谢性.
- 英文名称S-(2-(1-(2-Ethylbutyl)Cyclohexane-1-Carboxamido)Phenyl) 2-Methylpropanethioate
- 中文名称达塞曲匹
- IUPAC名称S-(2-(1-(2-ethylbutyl)cyclohexane-1-carboxamido)phenyl) 2-methylpropanethioate
- 其它别名Dalcetrapib
- CAS编号211513-37-0
- MFCD编号:MFCD06407886
- EINECS号:816-493-8
- FDA UNII编号:3D050LIQ3H
- 分子式:C23H35NO2S分子量:389.61
- 产品CID: 1093674
- 产品分类生物化工 → 抑制剂 → 代谢(Metabolism)
物理性质
MSDS等安全信息
欧盟法规
C&L通报上下游产品
isobutyryl chloride Dalcetrapib 1-(2-ethyl-butyl)-cyclohexanecarboxylic acid 2-ethyl-1-bromobutane合成工艺路线路线简述
📜2-乙基溴代丁烷置于吡啶,草酰氯,水,三苯基膦,Lithium Diisopropyl Amide体系中,用 四氢呋喃,1,4-二氧六环,二氯甲烷 用作溶剂,化学反应 4.5H,反应生成达塞曲匹
参考文献:Bis(2-(Acylamino)Phenyl) Disulfides,2-(Acylamino)Benzenethiols,And S-(2-(Acylamino)Phenyl) Alkanethioates As Novel Inhibitors Of Cholesteryl Ester Transfer Protein
标题:Bis(2-(Acylamino)Phenyl) Disulfides,2-(Acylamino)Benzenethiols,And S-(2-(Acylamino)Phenyl) Alkanethioates As Novel Inhibitors Of Cholesteryl Ester Transfer Protein
摘要:A Series Of Bis(2-(Acylamino)Phenyl) Disulfides,2-(Acylamino)Benzenethiols,S-(2-(Acylamino)Phenyl) Alkanethioates,And Related Compounds Were Synthesized,And Their Inhibitory Effect On Cholesteryl Ester Transfer Protein Activity In Human Plasma Was Evaluated. This Study Elucidated The Structural Requirements For Inhibitory Activity And Determined That The Optimum Compound Was S-(2-((1-(2-Ethylbutyl)Cyclohexane)Carbonylamino)Phenyl) 2-Methylpropanethioate (27) (Jtt-705). This Compound Achieved 50% Inhibition Of Cetp Activity In Human Plasma At A Concentration Of 9 Mu M And 95% Inhibition Of Cetp Activity In Male Japanese White Rabbits At An Oral Dose Of 30 Mg/kg. It Increased The Plasma Hdl Cholesterol Level By 27% And 54%,Respectively,When Given At Oral Doses Of 30 Or 100 Mg/kg Once A Day For 3 Days To Male Japanese White Rabbits.
Doi:10.1021/jm000224S
海关参考信息
- 2912110000-甲醛
2912120000-乙醛
2924199090-其他无环酰胺
2901100000-饱和无环烃 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
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-7612106-B2
优先权日:2004-12-23
标题 :Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof
发明人：BOATMAN P DOUGLAS; SCHRADER THOMAS O; SEMPLE GRAEME; SKINNER PHILIP J; JUNG JAE-KYU
权利人:ARENA PHARM INC
摘要:The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. n nAlso provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.
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:US-8637555-B2
优先权日:2003-10-31
标题:Tetrazole derivatives and methods of treatment of metabolic-related disorders thereof
发明人：SEMPLE GRAEME; SCHRADER THOMAS; SKINNER PHILIP J; COLLETTI STEVEN L; GHARBAOUI TAWFIK; IMBRIGLIO JASON E; JUNG JAE-KYU; LIANG RUI; RAGHAVAN SUBHAREKHA; SCHMIDT DARBY; TATA JAMES R
权利人:SEMPLE GRAEME; SCHRADER THOMAS; SKINNER PHILIP J; COLLETTI STEVEN L; GHARBAOUI TAWFIK; IMBRIGLIO JASON E; JUNG JAE-KYU; LIANG RUI; RAGHAVAN SUBHAREKHA; SCHMIDT DARBY; TATA JAMES R; ARENA PHARM INC; MERCK & CO INC
摘要:The present invention relates to certain tetrazole derivatives of Formula (I), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. n nAlso provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.
专利号:EP-1551403-B1
优先权日:2002-10-10
标 题 :5-substituted 2h-pyrazone-3-carboxylic acid derivatives as antilipolytic agents for the treatment of metabolic-related disorders such as dyslipidemia
发明人：SEMPLE GRAEME; AVERBUJ CLAUDIA; SKINNER PHILIP; GHARBAOUI TAWFIK; SHIN YOUNG-JUN
权利人:ARENA PHARM INC
摘要:The present invention relates to certain pyrazole carboxylic acid derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, as antilipolytic agents and against for the receptor RUP25, wherein: R2 is H, halogen, C1-12 alkyl or C1-12 haloalkyl; and R3 is C3-6 cycloalkyl, C1-12 alkyl, C1-12 haloalkyl, C3-6 cycloalkyl-C1-4-alkylene, aryl-C1-4-alkylene or heteroaryl-C1-4-alkylene, wherein said aryl-C1-4-alkylene and heteroaryl-C1-4-alkylene can be optionally substituted 1 to 5 substituents selected from the substituents listed in the claims. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for pharmaceutical compositions in combination with other active agents, for example, those agents belonging to the class of alpha-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, thiazolidinedione and the like.
专利号:US-2016046560-A1
优先权日:2013-04-05
标题 :Compounds useful for the treatment of metabolic disorders and synthesis of the same
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品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Johns DG, Chen Y, Wang SP, Castro-Perez J, Previs SF, Roddy TP. Inhibition of cholesteryl ester transfer protein increases cholesteryl ester content of large HDL independently of HDL-to-HDL homotypic transfer: in vitro vs in vivo comparison using anacetrapib and dalcetrapib. Eur J Pharmacol. 2015 Sep 5;762:256-62. doi: 10.1016/j.ejphar.2015.05.061. Epub 2015 Jun 3. doi: 10.1161/CIRCGENETICS.114.000663. Epub 2015 Jan 11. doi: 10.1007/s11745-014-3956-x. Epub 2014 Oct 4. doi: 10.1016/j.ejphar.2014.06.022. Epub 2014 Jul 5. doi: 10.3109/00498254.2014.932471. Epub 2014 Jun 23. doi: 10.1056/NEJMc1300057#SA1. doi: 10.1056/NEJMc1300057. doi: 10.1007/s40262-013-0035-z. doi: 10.5414/CP201766. doi: 10.1038/nrcardio.2012.171. Epub 2012 Nov 20. Effects of dalcetrapib in patients with a recent acute coronary syndrome. N Engl J Med. 2012 Nov 29;367(22):2089-99. doi: 10.1056/NEJMoa1206797. Epub 2012 Nov 5. doi: 10.2147/DDDT.S34976. Epub 2012 Sep 24. Review.
13: Gross G, Tardio J, Kuhlmann O. Solubility and stability of dalcetrapib in vehicles and biological media. Int J Pharm. 2012 Nov 1;437(1-2):103-9. doi: 10.1016/j.ijpharm.2012.07.071. Epub 2012 Aug 4. doi: 10.2217/fca.12.25. Review. doi: 10.1517/13543784.2012.699040. Epub 2012 Jun 24. doi: 10.1016/j.jpba.2012.03.056. Epub 2012 Apr 6. e1-3. doi: 10.1016/j.ahj.2011.11.017. doi: 10.1038/nrcardio.2012.31. Vascular effects and safety of dalcetrapib in patients with or at risk of coronary heart disease: the dal-VESSEL randomized clinical trial. Eur Heart J. 2012 Apr;33(7):857-65. doi: 10.1093/eurheartj/ehs019. Epub 2012 Feb 16.
合成参考文献
参考文献:10.1016/s0021-9150(01)00705-5
摘要:Kobayashi J, Okamoto H, Otabe M, Bujo H, Saito Y. Effect of HDL, from Japanese white rabbit administered a new cholesteryl ester transfer protein inhibitor JTT-705, on cholesteryl ester accumulation induced by acetylated low density lipoprotein in J774 macrophage. Atherosclerosis. 2002 May;162(1):131–5. doi: 10.1016/s0021-9150(01)00705-5.
参考文献:10.2165/00003495-200464110-00003
摘要:Evans M, Roberts A, Davies S, Rees A. Medical lipid-regulating therapy: current evidence, ongoing trials and future developments. Drugs. 2004;64(11):1181–96. doi: 10.2165/00003495-200464110-00003.
参考文献:10.1517/13543784.17.4.445
摘要:Athyros VG, Kakafika A, Tziomalos K, Karagiannis A, Mikhailidis DP. Cholesteryl ester transfer protein inhibition and HDL increase: has the dream ended Expert Opinion on Investigational Drugs. 2008 Mar 25;17(4):445–9. doi: 10.1517/13543784.17.4.445.
参考文献:10.1007/s11883-007-0055-y
摘要:Oram JF, Heinecke JW. When good cholesterol turns bad: the evolving saga of CETP inhibitors and clinical strategies to elevate high-density lipoprotein. Curr Atheroscler Rep. 2007 Dec;9(6):425–7. doi: 10.1007/s11883-007-0055-y.
参考文献:10.1097/mol.0b013e3283475e00
摘要:Niesor EJ. Different effects of compounds decreasing cholesteryl ester transfer protein activity on lipoprotein metabolism. Curr Opin Lipidol. 2011 Aug;22(4):288–95. doi: 10.1097/mol.0b013e3283475e00.
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