CAS: 107753-78-6; Cyclopentyl (3-(2-Methoxy-4-((O-Tolylsulfonyl)Carbamoyl)Benzyl)-1-Methyl-1H-Indol-5-yl)Carbamate

上下游产品

CAS号88-19-7 邻甲苯磺酰胺 | CAS号107754-20-1 4-(5-环戊酰基氨基-1-甲... | CAS号70264-94-7 3-甲氧基-4-溴甲基苯甲酸甲酯 | CAS号107786-36-7 4-[5-nitro-1H-i... | CAS号107754-15-4 Methyl-Benzoate... | CAS号6146-52-7 5-硝基吲哚 | CAS号50715-28-1 氯甲酸环戊酯 | CAS号107754-14-3 4-(5-Amino-1-me... | CAS号107754-19-8 4-[[5-[[(Cyclop... | CAS号29906-67-0 1-甲基-5-硝基吲哚

4-溴甲基-3-甲氧基苯甲酸甲酯置于palladium On Activated Charcoal N-甲基吗啉,4-二甲氨基吡啶,Lithium Hydroxide,氢气,Sodium Hydride,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,Silver(L) Oxide体系中,用 四氢呋喃,1,4-二氧六环,甲醇,二氯甲烷,水 用作溶剂,60.0 °C,345.0 Kpa 条件下,反应 62.67H,反应生成扎鲁司特
参考文献:一系列肽白三烯拮抗剂的演变:1,3,5-取代的吲哚和吲唑的合成及结构/活性关系.
标题:一系列肽白三烯拮抗剂的演变:1,3,5-取代的吲哚和吲唑的合成及结构/活性关系.
摘要:研发了1,3,5-取代的吲哚和吲唑作为肽白三烯的受体拮抗剂.这些化合物中最好的化合物通常在n1位具有甲基,在c-5位具有[(环戊氧基)羰基]氨基或2-环戊基乙酰氨基或n'-环戊基脲基,而芳基磺酰基酰胺基则是酸性的一部分.链在环的c-3位置.此类化合物在豚鼠气管上对lte4的激动剂的离解常数(kb)在10(-9)-10(-11)m范围内,抑制常数(ki)小于或等于10(-9)m豚鼠薄壁膜对[3H] Ltd4的影响.许多化合物以小于或等于1 Mg / Kg的剂量对豚鼠阻断ltd4诱导的"呼吸困难"有效.化合物45 [n-[4-[[5-[[(环戊氧基氧基)羰基]-氨基]-1-甲基吲哚-3-基]甲基]-3-甲氧基苯甲酰基]-2-甲基苯磺酰胺,Ici 204,219;化合物45.目前正在对哮喘进行pkb = 9.67 +/-0.13,Ki = 0.3 +/-0.03 Nm,Po Ed50
Doi:10.1021/jm00168A037

专利信息

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-9051302-B2
优先权日:2008-01-15
标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents
发明人：WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN
权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG
摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.

专利号:US-7919505-B2
优先权日:2006-07-11
标题 :Xinafoate salt of a substituted 5-oxazol-2-yl-quinoline compound
发明人：TING PAULINE C; LEE JOE F; FENG KUNG-I; REEDER MICHAEL R; TRZASKA SCOTT T; ZHU MAN; MAO CHEN; FILIPOV DIMITAR L; ZARKADAS DIMITRIOS N
权利人:SCHERING CORP
摘要:The present invention relates to the compound of the formula n nTo methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to polymorphs and processes of synthesis of the polymorphic forms.

专利号:US-2011003780-A1
优先权日:2007-07-10
标题:Hydrogen chloride salt of a substituted 5-oxazol-2-yl-quinoline compound and a process for the production thereof
发明人：ZHU MAN
权利人:SCHERING CORP
摘要:The present invention relates to the compound of the Formula I: n n n n n n n n n n and to methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to a particular crystalline form and processes of synthesis of the crystalline form. n IM=105109

专利号:WO-9964032-A1
优先权日:1998-06-08
标题 :Combinatorial synthesis of multibinding libraries
发明人：CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN
权利人:ADVANCED MEDICINE INC; CHRISTENSEN BURTON G; GRIFFIN JOHN H; JENKINS THOMAS E; JUDICE J KEVIN
摘要:Disclosed are methods for synthesizing large collections of diverse multimeric compounds as well as iterative processes for evaluating key molecular constraints imparting multibinding properties to multimeric compounds. Also disclosed are libraries of multimeric compounds which can be evaluated for imparting multibinding properties.

专利号:US-9949934-B1
优先权日:2016-10-20
标题:Device and method of treating conditions associated with neuroinflammation
发明人：ZERBE HORST G; OBEID RODOLPHE; CONWAY JUSTIN W; PAIEMENT NADINE; AIGNER LUDWIG
权利人:INTELGENX CORP
摘要:Disclosed is a device and method for treating a neurodegenerative disease or condition associated with neuroinflammation induced by a leukotriene. The device is a film unit dosage form having a film layer and a safe and effective amount of a leukotriene receptor antagonist or leukotriene synthesis inhibitor. The device is configured and formulated to achieve transmucosal and/or enteral delivery of the leukotriene receptor antagonist or leukotriene synthesis inhibitor. The method includes transmucosally and/or enterally delivering to an animal in need of treatment, a safe and effective amount of a leukotriene blocker capable of crossing the blood-brain barrier.