CAS: 158876-82-5; 8-Chloro-11-(1-((5-Methylpyridin-3-yl)Methyl)Piperidin-4-Ylidene)-6,11-Dihydro-5H-Benzo[5,6]Cyclohepta[1,2-B]Pyridine

上下游产品

CAS号120276-47-3 3-溴甲基-5-甲基吡啶 | CAS号100643-71-8 地氯雷他定 | CAS号591-22-0 3,5-二甲基吡啶 | CAS号3222-49-9 5-甲基烟酸

3,5-二甲基吡啶置于sodium Tetrahydroborate,Potassium Permanganate,1-羟基苯并三唑,N,N'-二环己基碳二亚胺,三氯氧磷体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 43.5H,反应生成卢帕他定
参考文献:[(3-吡啶基烷基)哌啶]苯并环庚吡啶衍生物作为paf和组胺的双重拮抗剂.
标题:[(3-吡啶基烷基)哌啶]苯并环庚吡啶衍生物作为paf和组胺的双重拮抗剂.
摘要:制备了一系列的[(3-吡啶基烷基)哌啶基]-和(烟酰基哌啶基)苯并环庚吡啶衍生物ia,B,并评价了paf拮抗剂和h1抗组胺活性.通过体外paf诱导的血小板聚集测定(ppa)和体内paf诱导的大鼠低血压测试(ph)和小鼠的死亡率测试(pm),研究了paf拮抗剂的活性.为了评估h1抗组胺药的活性,在血压正常的大鼠中使用了体外组胺引起的豚鼠回肠试验(hc)收缩和体内组胺引起的低血压试验(hh).使用活性过敏性休克试验在小鼠中评估了化合物的潜在抗过敏活性.这些化合物在结构上与氯雷他定(1)有关,是通过用取代的3-吡啶基甲基和烟酰基部分取代1的乙氧羰基而生成的.抗paf和h1抗组胺活性均显示出对吡啶环中取代基的确切性质和位置的高度依赖性.结合有(5-甲基-3-吡啶基)甲基的最佳结构19(ur-12592)表现出独特的双重活性,可抑制两种paf诱导的作用(ppa,Ic50 = 3.7 Microm; Ph,Id50
Doi:10.1021/jm00043A009

专利信息

专利号:US-6803468-B2
优先权日:2000-08-29
标 题 :Process for the synthesis of n-(5-methylnicontinoyl)-4 hydroxypiperidine, a key intermediate of rupatadine
发明人：KUMAR YATENDRA; PRASAD MOHAN; SINGH SHAILENDRA KUMAR
权利人:RANBAXY LAB LTD
摘要:The present invention relates to an improved and industrially advantageous process for the preparation of N-(5-methylnicotinoyl)-4-hydroxypiperidine of Formula I, as shown in the accompanied drawings. This compound is a key intermediate for the synthesis of rupatadine, a potent dual antagonist of histamine and platelet-activating factor (PAF).

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.

专利号:US-2004044216-A1
优先权日:2000-08-29
标题 :Process for the synthesis of n-(5-methylnicotinoyl)-4 hydroxypiperidine, a key intermediate of rupatadine

专利号:AU-2001284320-A1
优先权日:2000-08-29
标题:Process for the synthesis of n-(5-methylnicotinoyl)-4-hydroxypiperidine, a key intermediate of rupatadine

专利号:WO-0218366-A1
优先权日:2000-08-29
标题 :Process for the synthesis of n-(5-methylnicotinoyl)-4-hydroxypiperidine, a key intermediate of rupatadine

专利号:US-2014315720-A1
优先权日:2012-10-24
标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
发明人：FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
权利人:CELANESE ACETATE LLC
摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.