CAS: 87848-99-5; (E)-3-(6-((E)-3-(Pyrrolidin-1-yl)-1-(P-Tolyl)Prop-1-En-1-yl)Pyridin-2-yl)Acrylic Acid

上下游产品

-2-pyridinyl>propeboateethyl (E)-3-6-(4-methylphenyl)carbonyl-2-pyridinylpropeboate 2,6-Dibromopyridine 2-bromo-6-(4-toluoyl)pyridine 6-(2-p-Tolyl-[1,3]dioxolan-2-yl)-pyridine-2-carbaldehyde (E)-3-[6-(3-pyrrolidino-1-(4-tolyl)prop-1E-enyl)-2-pyridyl]acrylohydroxamic acid

2-溴-6-[2-(4-甲基苯基)-1,3-二氧戊环-2-基]吡啶置于盐酸,Sodium Hydroxide,正丁基锂,Sodium Hydride体系中,用 乙醚,正己烷 作为反应溶剂,化学反应 8.33H,反应生成 阿伐斯汀
参考文献:Triprolidine放射免疫分析:在动物和人类中的配置.
标题:Triprolidine放射免疫分析:在动物和人类中的配置.
摘要:合成了三吡咯烷的半抗原衍生物,其在吡啶环氮原子旁带有丙烯酸侧链,并与牛血清白蛋白偶联.用所得的药物-蛋白质缀合物免疫新西兰白兔导致产生抗血清,该抗血清能够以高抗血清稀释度(1:70,000-1:150,000)结合雷公藤半抗原衍生物的放射性碘化酪胺缀合物.这些抗血清用于开发人类血浆中曲普利定的放射免疫分析(ria),灵敏度极限为0.1 Ng / Ml(实际质量为0.01 Ng).已知的三氢吡啶的羟甲基和羧基代谢产物与该抗血清的交叉反应较弱(分别小于2%和小于0.05%).ria可以用于人和兔血浆中曲普利定的直接分析,但不适用于大鼠或狗血浆,大概是由于存在其他干扰物质(可能是代谢物).通过定量tlc(r = 0.985,斜率= 1.076)对许多样品进行比较分析,证明了ria方法在人血浆中的有效性.该测定法用于描述曲普利定在兔中的药代动力学(t 1/2,β= 1.7 H).该测定具有足够的灵
DOI:10.1002/jps.2600731003

专利信息

专利号:US-8653238-B2
优先权日:2006-02-27
标题:Compositions and methods for transport of molecules with enhanced release properties across biological barriers
发明人：WENDER PAUL A; GOUN ELENA A; JONES LISA R
权利人:WENDER PAUL A; GOUN ELENA A; JONES LISA R; UNIV LELAND STANFORD JUNIOR
摘要:Conjugates of a cargo molecule with a transporter molecule are disclosed, where the cargo molecule and the transporter molecule are linked covalently by a releasable linker. The cargo of the conjugate can be a biologically active agent or a reporter molecule. The transporter modulates the transport of the cargo across a biological barrier (e.g., a cell membrane) compared to the transport of the unconjugated cargo. Releasable linkers suitable for rapid and facile conjugation to various types of cargo and transporters are also disclosed, along with methods for using the linkers in the synthesis of conjugates.

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:US-12295961-B2
优先权日:2009-12-31
标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
发明人：DHINGRA OM
权利人:MARIUS PHARMACEUTICALS INC
摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:US-5426196-A
优先权日:1993-12-22
标题 :Synthesis of diaryl methanes
发明人：FANG FRANCIS G
权利人:GLAXO INC
摘要:The present Invention includes synthetic steps and intermediates involved in the following reaction scheme a of converting compounds of Formula (II) to the diarylmethanes of Formula (I): ##STR1## wherein: Y is oxygen or sulfur; n A, B, C, D, and E are carbon or 1, 2 or 3 of A, B, C, D, and E are independently nitrogen, and the others are carbon; and n wherein n R 1 through R 10 are selected independently from the group consisting of: hydrogen, hydroxy, alkyl, C 3 -C 8 cycloalkyl, C 3 -C 8 cycloalkyl alkyl, alkenyl, hydroxy alkyl, alkoxy alkyl, perhalo-alkyl, amino, nitro, nitrile, halo, carboxyl, sulfonyl, acyl, formyl, carbamoyl, trifluoromethyl, aminomethyl, azido, amido, hydrazino, aryl, aryloxy, heteroaryl, or aryl or heteroaryl, mono, di, or tri substituted with one or more hydrogen, hydroxy, alkyl, C 3 -C 8 cycloalkyl, C 3 -C 8 cycloalkyl alkyl, alkenyl, hydroxy alkyl, alkoxy alkyl, perhaloalkyl, amino, nitro, nitrile, halo, carboxyl, sulfonyl, acyl, formyl, carbamoyl, trifluoromethyl, aminomethyl, azido, amido, hydrazino, aryl, aryloxy, or heteroaryl groups and; n the pharmaceutically acceptable salts and solvates thereof.

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.