CAS: 58581-89-8; 4-(4-Chlorobenzyl)-2-(1-Methylazepan-4-yl)Phthalazin-1(2H)-One

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CAS号1878-66-6 4-氯苯乙酸 | CAS号85-44-9 苯酐 | CAS号1859-33-2 1-甲基六氢-4H-氮杂卓-4-酮 | CAS号53242-76-5 2-(4-氯苯乙酰基)苯甲酸

1-甲基六氢-4H-氮杂卓-4-酮置于盐酸,氢氧化钾,Sodium Tetrahydroborate体系中,化学反应 5.0H,反应生成 氮卓斯汀
参考文献:氮卓斯汀的合成及晶体结构分析
标题:氮卓斯汀的合成及晶体结构分析
摘要:氮卓斯汀盐酸盐(asta A 5610),4-(对氯苄基)-2-(六氢-1-甲基-1H-Azepin-4-Yl)-1(2H)-酞嗪酮盐酸盐(2)是一种新型口服溶液长-持久的抗过敏和预防哮喘.从邻苯二甲酸酐开始,描述了盐酸氮卓斯汀的两种替代合成路线.氮卓斯汀一水合物的 X 射线结构分析显示两个独立的分子 A 和 B,具有显着的构象差异.根据结构-活性关系讨论结构差异.
DOI:10.1002/ardp.19883210406

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-5760221-A
优先权日:1993-12-18
标 题:Method for the preparation of hexahydroazepinones and hexahydroazepinoles
发明人：OLBRICH ALFRED; ENGEL JUERGEN; KUTSCHER BERNHARD; MOELLER ROLAND
权利人:ASTA MEDICA AG
摘要:This disclosure describes two technical procedures for the high-yield synthesis of heterocyclic seven-membered ring-systems by Dieckmann-condensation avoiding usual dilution techniques and long reaction times. Thus, it significantly increases the overall yields of the pharmaceutically active ingredients azelastine and flezelastine, whose synthesis, starting from these seven-membered heterocyclic rings, is reported elsewhere. Yields range from 80-89%, avoiding waste and increasing economics of the synthesis.

专利号:US-8734846-B2
优先权日:2008-06-16
标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
发明人：ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
权利人:BIND BIOSCIENCES INC
摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

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-2023075715-A1
优先权日:2021-10-26
标题 :A pharmaceutical formulation including leukotriene receptor antagonists and/or leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (nsaids)
发明人：OYTUN FARUK; CAN EFE
权利人:VSY BIYOTEKNOLOJI VE ILAC SANAYI ANONIM SIRKETI
摘要:This invention is related to a pharmaceutical formulation including Leukotriene receptor antagonists and/or Leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (NSAIDs) and antihistamines in ocular diseases and in inflammatory and allergic diseases for systemic and topical use. The objective of this invention is to create a novel formulation to be effective as much as steroids while having significantly less side effects for long-term use in treating ocular diseases, inflammatory and allergic diseases. In other words our aim is to achieve the inhibition of pro-inflammatory mediators (prostaglandins, thromboxane, histamine and leukotrienes) as much as steroids do with a safer combination.