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    • 113. 发明授权
    • Pure polyanhydride from dicarboxylic acid and coupling agent
    • 来自二羧酸和偶联剂的纯聚酐
    • US4916204A
    • 1990-04-10
    • US80332
    • 1987-07-31
    • Abraham J. DombRobert S. LangerEyal RonSteven GiannosRohit KothariEdith Mathiowitz
    • Abraham J. DombRobert S. LangerEyal RonSteven GiannosRohit KothariEdith Mathiowitz
    • A61K31/335A61K31/365A61K31/39C08G67/04C08G69/08C08G69/10
    • A61K31/335A61K31/365A61K31/39C08G67/04C08G69/08C08G69/10Y10S514/863
    • A method for synthesizing polyanhydrides in solution using coupling agents and a removable acid acceptor to effect a one-step polymerization of dicarboxylic acids. As used in the method, these coupling agents include phosgene, diphosgene, and acid chlorides. Insoluble acid acceptors include insoluble polyamines and crosslinked polyamines such as polyethyleneimine and polyvinylpyridine and inorganic bases such as K.sub.2 CO.sub.3, Na.sub.2 CO.sub.3, NaHCO.sub.3, and CaCO.sub.3. The only byproduct formed is a removable hydrochloric acid-acid acceptor.Examples are provided of the polymerization of highly pure polyanhydrides using phosgene, diphosgene or an acid chloride as the coupling agent, in combination with either an insoluble acid acceptor or a soluble acid acceptor in a solvent wherein the polymerization byproduct or polymer is insoluble.A particularly important application of these polyanhydrides is in the formation of drug delivery devices containing bioactive compounds. The method is also useful in the polymerization of dicarboxylic acids including heat liable dipeptides of glutamic or aspartic acid.
    • 使用偶联剂和可除去的酸受体在溶液中合成聚酐以进行二羧酸的一步聚合的方法。 如该方法所用,这些偶联剂包括光气,双光气和酰氯。 不溶性酸受体包括不溶性多胺和交联聚胺如聚乙烯亚胺和聚乙烯吡啶以及无机碱如K 2 CO 3,Na 2 CO 3,NaHCO 3和CaCO 3。 形成的唯一副产物是可除去的盐酸酸受体。 提供了使用光气,双极光或酰氯作为偶联剂的高纯度聚酐与在溶剂中的不溶性酸受体或可溶性酸受体组合的聚合反应,其中聚合副产物或聚合物是不溶的。 这些多酸酐的特别重要的应用是形成含有生物活性化合物的药物递送装置。 该方法也可用于二羧酸的聚合,包括谷氨酸或天冬氨酸的热应答二肽。
    • 119. 发明授权
    • Novel polyamides from ketene-aminals
    • 来自乙烯酮的新型聚酰胺
    • US4338428A
    • 1982-07-06
    • US292872
    • 1981-08-14
    • Louis M. AlberinoDale F. Regelman
    • Louis M. AlberinoDale F. Regelman
    • C08G18/67C08G18/32C08G18/38C08G69/08
    • C08G18/678C08G2120/00
    • Novel polyketene-aminal polyamides are disclosed which have the following recurring unit ##STR1## wherein R is a divalent hydrocarbon radical, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 when taken separately are independently selected from the group consisting of lower alkyl, aralkyl, and cycloalkyl, and when taken together as R.sub.1 with R.sub.2 and R.sub.3 with R.sub.4 with the respective nitrogen atoms to which they are attached represent independently a heterocyclic group having from 5 to 7 ring atoms.The polyamides are prepared by reacting together the appropriate diisocyanate [R(NCO).sub.2 ] and appropriate ketene-aminal to form the polymer directly without the evolution of any by-products or volatiles.The novel polymers are thermoplastic and can be formed or shaped using any of the techniques known to those skilled in the thermoplastic polymer art.
    • 公开了具有以下重复单元的新型聚烯酮 - 酰胺聚酰胺,其中R是二价烃基,R 1,R 2,R 3和R 4分开独立地选自低级烷基,芳烷基和环烷基 并且当R 1和R 3与R 4与它们所连接的相应氮原子一起作为R 1独立地表示具有5至7个环原子的杂环基时。 聚酰胺通过使合适的二异氰酸酯[R(NCO)2]和适当的乙烯酮 - 胺反应而直接形成聚合物而制备,而不会产生任何副产物或挥发物。 新型聚合物是热塑性的并且可以使用热塑性聚合物领域的技术人员已知的任何技术形成或成型。