CAS: 68302-57-8; 2-Amino-7-Isopropyl-5-Oxo-5H-Chromeno[2,3-B]Pyridine-3-Carboxylic Acid

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CAS号68301-99-5 2-氨基-7-异丙基-5-氧代... | CAS号50743-32-3 6-异丙基色酮-3-甲腈

6-异丙基-4-氧代-4H-1-苯并吡喃-3-甲腈置于哌啶,硫酸,溶剂黄146体系中,用 乙醇 作为反应溶剂,化学反应 8.0H,反应生成 氨来诺
参考文献:抗过敏药的研究.7.合成抗过敏的5-氧代-5H-[1]苯并吡喃并[2,3-B]吡啶.
标题:抗过敏药的研究.7.合成抗过敏的5-氧代-5H-[1]苯并吡喃并[2,3-B]吡啶.
摘要:由4-氧代-4H-1-苯并吡喃-3-甲腈3或2-氨基合成5-氧代-5H-[1]苯并吡喃并[2,3-B]吡啶-3-羧酸23及其四唑类似物24.-4-氧代-4H-1-苯并吡喃-3-甲醛4.静脉内给药时,它们在大鼠的pca试验中表现出抗过敏活性.在羧酸系列中,活性受2-位取代基的影响,并按以下顺序显着增加:Me,Ome小于nh2小于oh,H小于nhome.另一方面,在四唑系列中,2-未取代的衍生物显示出最高的活性.不管位置2和3上的取代基种类如何,带有烷基,尤其是7位上的异丙基的化合物的活性均优于相应的未取代的化合物.在这些烷基衍生物中,3-羧酸衍生物,即23C(7-乙基),23G(2-氨基-7-异丙基),23R [2-(甲氧基氨基)-7-异丙基]和3-四唑衍生物. 24C(7-异丙基)的效力是色甘氨酸二钠的41-184倍.口服时它们还表现出显着的活性.23G(aa-673)的临床研究正在进行中.
DOI:10.1021/jm50001A005

专利信息

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-2003138490-A1
优先权日:2001-09-08
标 题 :Synthesis and uses of polymer gel nanoparticle networks
发明人：HU ZHIBING; LU XIHUA; GAO JUN; PONDER BILL C; JOHN JOHN ST; MORO DANIEL G
摘要:Disclosed is a new class of nanostructured polymeric materials comprising polymer gel nanoparticles that are covalently bonded through functional groups on the surfaces of neighboring particles. These nanoparticles may be prepared as suspensions in an aqueous or, non-aqueous environment. These gels have two unique and different structural networks; the primary network comprises crosslinked polymer chains in each individual particle, while the secondary network is a system of crosslinked nanoparticles. Particular polymer gel nanoparticle network compositions disclosed herein may function as carriers for controlled delivery of pharmaceuticals or other chemical agents, gel sensors and other commercial applications.

专利号:US-9359376-B2
优先权日:2011-04-08
标题:Substituted methylformyl reagents and method of using same to modify physicochemical and/or pharmacokinetic properties of compounds
发明人：DUGAR SUNDEEP; MAHAJAN DINESH; HOLLINGER FRANK PETER
权利人:DUGAR SUNDEEP; MAHAJAN DINESH; HOLLINGER FRANK PETER; SPHAERA PHARMA PTE LTD
摘要:The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.

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 %.

专利号:WO-03022910-A1
优先权日:2001-09-08
标题:Synthesis and uses of polymer gel nanoparticle networks