CONTROLLED RELEASES OF ACTIVES IN SKIN
    43.
    发明申请
    CONTROLLED RELEASES OF ACTIVES IN SKIN 有权
    控制释放皮肤活动

    公开(公告)号:US20090317472A1

    公开(公告)日:2009-12-24

    申请号:US12525529

    申请日:2008-01-31

    Abstract: Topical compositions are provided in which active compounds for topical delivery through the stratum corneum are complexed with nanospheres of a triblock copolymer having an A-B-A structure wherein each A end block is a water-soluble, hydrophilic and non-toxic polymer or oligomer; and the hydrophobic middle B block is a hydrophobic polymer or oligomer with the same or different repeating units having the structure according to formula:(I) wherein X is —C —R—C— or —C—; Z is between 2 and about 100, inclusive; R1 is CH═CH or (CH2), wherein n is from 0 to 18, inclusive; R2 is selected from hydrogen and straight and branched alkyl, alkoxy, alkylaryl and alkoxyaryl groups containing up to 18 carbon atoms; and R is selected from a bond or straight and branched alkyl, alkoxy, alkylaryl and alkoxyaryl groups containing up to 18 carbon atoms.

    Abstract translation: 提供了局部组合物,其中通过角质层局部递送的活性化合物与具有A-B-A结构的三嵌段共聚物的纳米球络合,其中每个A端嵌段是水溶性的,亲水的和无毒的聚合物或低聚物; 并且疏水性中间B嵌段是具有相同或不同重复单元的疏水性聚合物或低聚物,其具有根据下式的结构:(I)其中X是-C-C-C或-C-; Z在2至约100之间(含); R1为CH-CH或(CH2),其中n为0至18,包括端值; R2选自氢和含有至多18个碳原子的直链和支链烷基,烷氧基,烷基芳基和烷氧基芳基; 并且R选自含有至多18个碳原子的键或直链和支链烷基,烷氧基,烷基芳基和烷氧基芳基。

    PHARMACEUTICAL FORMULATION COMPOSED OF A POLYMER BLEND AND AN ACTIVE COMPOUND FOR TIME-CONTROLLED RELEASE
    44.
    发明申请
    PHARMACEUTICAL FORMULATION COMPOSED OF A POLYMER BLEND AND AN ACTIVE COMPOUND FOR TIME-CONTROLLED RELEASE 有权
    用于时间控制释放的聚合物混合物和活性化合物组成的药物制剂

    公开(公告)号:US20080194469A1

    公开(公告)日:2008-08-14

    申请号:US11970028

    申请日:2008-01-07

    Abstract: A formulation containing a biologically active compound having a chemical structure with hydrogen bonding sites, a first biocompatible, hydrolytically degrading polycarbonate with hydrogen bonding sites and tyrosine-derived diphenol monomer units, and a second biocompatible hydrolytically degrading polymer that is less hydrophobic than the polycarbonate, wherein the second polymer degrades hydrolytically to form acidic degradation products that promote the release of the active compound. Methods for active compound delivery are also disclosed.

    Abstract translation: 包含具有氢键结合位点的化学结构的生物活性化合物,具有氢键位点的第一生物相容性,水解降解性聚碳酸酯和酪氨酸衍生的二酚单体单元的制剂,以及比聚碳酸酯疏水性低的第二生物相容性水解降解聚合物, 其中第二聚合物水解降解以形成促进活性化合物释放的酸性降解产物。 还公开了活性化合物递送的方法。

    Polymeric drug formulations
    45.
    发明授权
    Polymeric drug formulations 失效
    聚合药物制剂

    公开(公告)号:US07005454B2

    公开(公告)日:2006-02-28

    申请号:US09257145

    申请日:1999-02-24

    CPC classification number: A61K9/146 A61K9/2031 A61K9/204 A61K9/7007

    Abstract: 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.

    Abstract translation: 含水溶性药物的非释放单相分散体在水不溶性组织相容的聚合物基质中的聚合药物制剂。 还公开了含有水溶性药物和水不溶性组织相容聚合物基质的单相分散体的聚合药物制剂,以及与组织相容的聚合物不可混溶的第二种相位破坏性聚合物,并且是 存在的量足以在组织相容性聚合物基质中形成第二聚合物的相分离微区,使得来自组织相容性聚合物基质的水溶性药物的释放速率与第二聚合物的量相关 。 还描述了制备聚合物药物制剂的方法,以及利用聚合物药物制剂的用于位点特异性药物递送的方法。

    Synthesis of tyrosine-derived diphenol monomers
    46.
    再颁专利
    Synthesis of tyrosine-derived diphenol monomers 有权
    酪氨酸衍生的二酚单体的合成

    公开(公告)号:USRE37795E1

    公开(公告)日:2002-07-16

    申请号:US09358015

    申请日:1999-07-21

    Abstract: 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 discussed.

    Abstract translation: 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。 还讨论了新的二酚单体和从其聚合的聚合物。

    Synthesis of amino acid-derived bioerodible polymers
    47.
    发明授权
    Synthesis of amino acid-derived bioerodible polymers 失效
    氨基酸衍生的生物可腐蚀聚合物的合成

    公开(公告)号:US5198507A

    公开(公告)日:1993-03-30

    申请号:US804767

    申请日:1991-12-09

    CPC classification number: C07C235/34 C08G64/12 C08G69/44

    Abstract: Novel amino acid-derived polycarbonates and amino acid-derived diphenol compound starting materials from which the polycarbonates are polymerized. Polymer blends of the amino acid-derived polycarbonates with polyiminocarbonates prepared from identical amino acid-derived diphenol starting materials.

    Abstract translation: 来自聚碳酸酯的新型氨基酸衍生的聚碳酸酯和氨基酸衍生的二酚化合物原料聚合。 氨基酸衍生的聚碳酸酯与由相同的氨基酸衍生的二酚起始原料制备的聚亚碳酸酯的聚合物共混物。

    Bioresorbable polymers synthesized from monomer analogs of natural metabolites
    49.
    发明授权
    Bioresorbable polymers synthesized from monomer analogs of natural metabolites 有权
    由天然代谢物的单体类似物合成的生物可吸收聚合物

    公开(公告)号:US08415449B2

    公开(公告)日:2013-04-09

    申请号:US13387798

    申请日:2010-07-31

    CPC classification number: C08G79/02 A61K47/59 A61K47/60 C08G79/025

    Abstract: This invention discloses biocompatible polymers prepared from monomers (IV), and (IVa), or derivatives thereof, for which the variables are described in the claims and specification. These polymers may be bioresorbable and thus useful for manufacture of medical devices. Therefore, methods for preparing these polymers and medical devices prepared therefrom are also encompassed by this disclosure.

    Abstract translation: 本发明公开了由权利要求和说明书中描述的变体描述的由单体(IV)和(IVa)或其衍生物制备的生物相容性聚合物。 这些聚合物可以是生物可再吸收的,因此可用于制造医疗器械。 因此,制备这些聚合物的方法和由其制备的医疗装置也包括在本公开中。

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