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    Biphasic polymerization process
    55.
    发明授权
    Biphasic polymerization process 失效
    双相聚合工艺

    公开(公告)号：US06359102B1

    公开(公告)日：2002-03-19

    申请号：US09107753

    申请日：1998-06-29

    申请人： John E. Kemnitzer ,  George L. Brode ,  Joachim B. Kohn

    发明人： John E. Kemnitzer ,  George L. Brode ,  Joachim B. Kohn

    IPC分类号： C08G6424

    CPC分类号： C08G64/24 ,  C08G63/6856 ,  C08G63/79 ,  C08G63/87 ,  C08G64/12

    摘要： Improvements are disclosed for biphasic polymerization processes in which an aqueous solution of a first monomer that is hydrolytically unstable below a pH of about six or above a pH of about eight is admixed with a water-immiscible organic solvent and there is added to the admixture a catalyst selected from tertiary amine, quaternary amine and phosphonium catalysts, an acid-forming co-monomer for the first monomer, an acid scavenger, after which the resulting polymer is recovered, wherein the improvement includes providing the aqueous solution at a pH between about si and about eight, and adding to the admixture the acid-forming co-monomer and the acid scavenger at relative rates effective to maintain the pH of the admixture between about six and about eight. The catalyst may be added in a molar ratio to the first monomer effective to provide a predetermined weight-average or number-average molecular weight for the resulting polymer. Biphasic polymerization processes for monomers that are not pH sensitive are also disclosed.

    摘要翻译： 对于双相聚合方法公开了改进，其中将水解稳定性低于约6或大于约pH 8的水解不稳定的第一单体的水溶液与水不混溶的有机溶剂混合并加入到混合物a 选自叔胺，季胺和鏻催化剂的催化剂，用于第一单体的酸形成共聚单体，酸清除剂，之后回收所得聚合物，其中改进包括将水溶液提供在约si 和约8，并且以相对速率加入酸形成共聚单体和酸清除剂，以有效地将混合物的pH保持在约6至约8之间。 催化剂可以与第一单体的摩尔比加入，有效地为所得聚合物提供预定的重均分子量或数均分子量。 还公开了对不敏感的单体的双相聚合方法。

    Polymeric drug formulations
    59.
    发明授权
    Polymeric drug formulations 失效

    公开(公告)号：US5877224A

    公开(公告)日：1999-03-02

    申请号：US508577

    申请日：1995-07-28

    申请人： Stephen Brocchini ,  Stephen R. Hanson ,  Joachim B. Kohn

    发明人： Stephen Brocchini ,  Stephen R. Hanson ,  Joachim B. Kohn

    IPC分类号： A61K9/10 ,  A61K9/14 ,  A61K9/20 ,  A61K9/70 ,  A61K47/30 ,  A61K47/32 ,  A61K47/34

    CPC分类号： A61K9/146 ,  A61K9/2031 ,  A61K9/204 ,  A61K9/7007

    摘要： Polymeric drug formulations containing a non-releasing single-phase dispersion of a water-soluble drug in a water-insoluble tissue-compatible polymer matrix. Polymeric drug formulations are also disclosed containing a single-phase dispersion of a water-soluble drug and a water-insoluble tissue-compatible polymer matrix, and a second, phase-disrupting polymer that is non-miscible with the tissue-compatible polymer and is present in an amount sufficient to form phase-separated microdomains of the second polymer in the tissue-compatible polymer matrix, so that the release rate of the water-soluble drug from the tissue-compatible polymer matrix is related to the amount of the second polymer. Methods of preparing the polymeric drug formulations are also described, as well as methods for site-specific drug delivery utilizing the polymeric drug formulations.

    Synthesis of tyrosine-derived diphenol monomers
    60.
    发明授权
    Synthesis of tyrosine-derived diphenol monomers 失效
    酪氨酸衍生的二酚单体的合成

    公开(公告)号：US5670602A

    公开(公告)日：1997-09-23

    申请号：US625763

    申请日：1996-03-29

    申请人： Joachim B. Kohn ,  Stephen J. Brocchini ,  Arthur L. Schwartz

    发明人： Joachim B. Kohn ,  Stephen J. Brocchini ,  Arthur L. Schwartz

    IPC分类号： C07C231/02 ,  C07C235/34 ,  C08G63/685 ,  C08G64/12 ,  C08G69/44 ,  C08G63/00 ,  C07C229/00

    CPC分类号： C08G69/44 ,  C07C231/02 ,  C07C235/34 ,  C08G63/6856 ,  C08G64/12

    摘要： A method for preparing diphenol compounds, which method includes the steps of coupling a hydroxyphenyl carboxylic acid with a L-tyrosine ester in a water-miscible organic reaction solvent containing a carbodiimide capable of forming a water-soluble urea by-product, thereby forming a diphenol reaction product; and combining the reaction mixture with an amount of water effective to precipitate the diphenol as a water-immiscible organic phase, so that a water-immiscible organic phase is formed containing the diphenol reaction product. New diphenol monomers and polymers polymerized therefrom are also disclosed.

    摘要翻译： 一种制备二酚化合物的方法，该方法包括将羟基苯基羧酸与L-酪氨酸酯偶联在含有可形成水溶性尿素副产物的碳二亚胺的水混溶性有机反应溶剂中，由此形成 二酚反应产物; 并将反应混合物与一定量的水组合，将水作为与水不混溶的有机相沉淀，使得形成含有二酚反应产物的与水不混溶的有机相。 还公开了新的二酚单体和从其聚合的聚合物。