CAS: 184036-34-8; N-(4-Chloro-3-Methylisoxazol-5-yl)-2-(2-(6-Methylbenzo[d][1,3]Dioxol-5-yl)Acetyl)Thiophene-3-Sulfonamide

该化合物是一种选择性内分泌素受体,主要用于治疗肺动脉高血压(PAH),它的作用是阻止内分泌-1的动作,一种强大的血管收缩器,从而在肺动脉中促进血管变异和减少血压. 静脉动的化学配方是C21H26N2O3S, 它的特点是一种有助于其药理活动的磺酰胺组. 静脉活性一般是口服的,半衰期相对较长,允许每天做一次. 临床试验表明,静脉动能在提高运动能力以及推迟PAHA病人临床恶化方面的效力. 但是,必须指出,静脉活性与肝毒性有关,导致它退出某些地区的市场. 任何药物,副作用和反作用的监测在临床实践中都至关重要. 总的来说,静脉活性反应是肺动脉动脉压管理的重大进步,尽管其安全性考虑是必要的.

结构式图片

上下游产品

CAS号210421-71-9 3-(N-(4-氯-3-甲基异... | CAS号117661-72-0 5-(氯甲基)-6-甲基-1,... | CAS号20850-43-5 5-氯甲基-1,3-苯并二氧杂环戊烯 | CAS号184040-74-2 3-(N-(4-氯-3-甲基异...

合成工艺路线路线简述

  • 合成目标产物 N- (4- Chloro- 3- Methyl- Oxazol- 5- Yl)- 2- [2- (6- Methylbenzo[1,3]Dioxol- 5- Yl)Acetyl]- Thiophene- 3- Sulfonamide 主要起始原料 3,4-Methylenedioxy-6-Methylbenzyl Chloride
  • (文献来源)合成步骤主要原料 3,4-Methylenedioxy-6-Methylbenzyl Chloride
📜(3,4-亚甲基二氧基)-6-甲基苄氯 以71%的收率获得n-(4-氯-3-甲基-5-异恶唑基)-2-[(2-甲基-4,5-亚甲二氧基苯基)乙酰]噻吩-3-磺酰胺
参考文献:Formulation Of Sulfonamides For Treatment Of Endothelin-Mediated Disorders
标题:Formulation Of Sulfonamides For Treatment Of Endothelin-Mediated Disorders
摘要:提供了药物可接受的噻吩基,呋喃基和吡咯基磺酰胺的制剂以及使用这些制剂调节或改变内皮素肽家族活性的方法.特别是,提供了n-(异恶唑基)噻吩磺酰胺,N-(异恶唑基)呋喃磺酰胺和n-(异恶唑基)吡咯磺酰胺的钠盐的制剂以及使用这些磺酰胺盐通过将受体与磺酰胺盐接触来抑制内皮素肽与内皮素受体结合的方法.还提供了通过施用有效量的一个或多个这些磺酰胺盐或抑制或增加内皮素活性的前药来治疗内皮素介导的疾病的方法.

海关参考信息

专利信息


专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:US-5705629-A
优先权日:1995-10-20
标 题:Methods for H-phosphonate synthesis of mono- and oligonucleotides
发明人:BHONGLE NANDKUMAR
权利人:HYBRIDON INC
摘要:New methods of synthesizing mono- and oligo- nucleotide H-phosphonates are disclosed. The methods comprise contacting a mononucleoside with phosphonic acid and benzoyl anyhydride to yield the corresponding mononucleoside H-phosphonate. Preferrably a catalytic amount of triphosgene is also used. A similar procedure can be used to couple a first mononucleoside to a second mononucleoside or to an oligonucleotide, the method comprising contacting, in the presence of benzoic anhydride and, preferrably, a catalytic amount of triphosgene, a mononucleotide or oligonucleotide having a free 5' hydroxyl with a mononucleoside having a 3' hydroxyl-bearing phosphorous moiety (preferably H-phosphonate).

专利号:WO-9817675-A1
优先权日:1996-10-18
标 题:Improved methods for h-phosphonate synthesis of mono- and oligonucleotides
发明人:BHONGLE NANDKUMAR
权利人:HYBRIDON INC
摘要:New methods of synthesizing mono- and oligo- nucleotide H-phosphonates are disclosed. The methods comprise contacting a mononucleoside with phosphonic acid and benzoyl anhydride to yield the corresponding mononucleoside H-phosphonate. Preferably, a catalytic amount of triphosgene is also used. A similar procedure can be used to couple a first mononucleoside to a second mononucleoside or to an oligonucleotide, the method comprising contacting, in the presence of benzoic anhydride and, preferably, a catalytic amount of triphosgene, a mononucleotide or oligonucleotide having a free 5'hydroxyl with a mononucleoside having a 3'hydroxyl-bearing phosphorous moiety (preferably H-phosphonate).

专利号:US-10906888-B2
优先权日:2016-07-14
标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
权利人:PFIZER
摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-10308615-B2
优先权日:2015-05-29
标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme
发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN
权利人:PFIZER
摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-2013345311-A1
优先权日:2004-07-19
标 题 :Synthesis Of Triethylenetetramines

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

合成参考文献


参考文献:10.1097/01.hco.0000231410.07426.9b|10.1097/01.hco.0000240593.52580.5c
摘要:Archer SL, Michelakis ED. An evidence-based approach to the management of pulmonary arterial hypertension. Curr Opin Cardiol. 2006 Jul;21(4):385–92. doi: 10.1097/01.hco.0000231410.07426.9b.
参考文献:10.1097/ccm.0b013e318120b7437
摘要:Stafford-Smith M. Pharmacologic renoprotection: are the stars finally moving into alignment Crit Care Med. 2011 Apr;39(4):906–7. doi: 10.1097/ccm.0b013e318120b7437.
参考文献:10.1681/asn.2012040355
摘要:Dhaun N, Melville V, Blackwell S, Talwar DK, Johnston NR, Goddard J, Webb DJ. Endothelin-A receptor antagonism modifies cardiovascular risk factors in CKD. J Am Soc Nephrol. 2013 Jan;24(1):31–6.
参考文献:10.1111/imj.12007
摘要:Don GW, Joseph F, Celermajer DS, Corte TJ. Ironic case of hepatic dysfunction following the global withdrawal of sitaxentan. Intern Med J. 2012 Dec;42(12):1351–4. doi: 10.1111/imj.12007.
参考文献:10.4081/reumatismo.2012.326
摘要:Soldano S, Montagna P, Brizzolara R, Ferrone C, Parodio A, Sulli A, Seriolo B, Villaggio B, Cutolo M. Endothelin receptor antagonists: effects on extracellular matrix synthesis in primary cultures of skin fibroblasts from systemic sclerosis patients. Reumatismo. 2012 Dec 11;64(5):326–34. doi: 10.4081/reumatismo.2012.326.
📝 需求与反馈
尽可能描述清楚需求与问题信息
×

通知