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    Composition for Long-Acting Peptide Analogs
    1.
    发明申请
    Composition for Long-Acting Peptide Analogs 有权
    长效肽类似物的组成

    公开(公告)号：US20110207662A1

    公开(公告)日：2011-08-25

    申请号：US13095753

    申请日：2011-04-27

    Applicant: Gerardo M. Castillo ,  Elijah M. Bolotin

    Inventor： Gerardo M. Castillo ,  Elijah M. Bolotin

    IPC: A61K38/28 ,  C07K14/00 ,  A61K38/16 ,  A61K38/18 ,  A61K38/22 ,  A61K38/24 ,  A61K38/26 ,  A61K38/27 ,  A61K38/29 ,  A61K38/30 ,  A61K38/31 ,  C07K14/635 ,  C07K14/62 ,  C07K14/61 ,  C07K14/605 ,  C07K14/60 ,  C07K14/595 ,  C07K14/575 ,  C07K14/58 ,  C07K14/65 ,  C07K14/655 ,  C07K14/475 ,  C07K14/485 ,  C07K14/495 ,  A61P3/10

    CPC classification number: C07K14/57563 ,  A61K38/00 ,  A61K47/542 ,  C07K7/16 ,  C07K14/485 ,  C07K14/575

    Abstract: The invention describes compositions of peptide analogs that are active in blood or cleavable in blood to release an active peptide. The peptide analogs have a general formula: A-(Cm)x-Peptide (SEQ ID NO: 76), wherein A is hydrophobic moiety or a metal binding moiety, e.g., a chemical group or moiety containing 1) an alkyl group having 6 to 36 carbon units, 2) a nitrilotriacetic acid group, 3) an imidodiacetic acid group, or 4) a moiety of formula (ZyHisw)p (SEQ ID NO: 50), wherein Z is any amino acid residue other than histidine, His is histidine, y is an integer from 0-6; w is an integer from 1-6; and p is an integer from 1-6; wherein if A has alkyl group with 6 to 36 carbon units x is greater than 0; and Cm is a cleavable moiety consisting of glycine or alanine or lysine or arginine or N-Arginine or N-lysine, wherein x is an integer between 0-6 and N may be any amino acid or none. The peptide analogs are complexed with polymeric carrier to provide enhanced half-life.

    Abstract translation: 本发明描述了在血液中有活性的或可裂解的血液中释放活性肽的肽类似物的组合物。 肽类似物具有以下通式：A-（Cm）x-肽（SEQ ID NO：76），其中A是疏水部分或金属结合部分，例如化学基团或部分，其含有1）具有6个 至36个碳单元，2）次氮基三乙酸基团，3）亚氨基二乙酸基团，或4）式（ZyHisw）p（SEQ ID NO：50）的部分，其中Z是组氨酸以外的任何氨基酸残基，His 是组氨酸，y是0-6的整数; w是1-6的整数; p为1-6的整数; 其中如果A具有6至36个碳单元的烷基，x大于0; 和Cm是由甘氨酸或丙氨酸或赖氨酸或精氨酸或N-精氨酸或N-赖氨酸组成的可切割部分，其中x是0-6之间的整数，N可以是任何氨基酸或没有氨基酸。 肽类似物与聚合物载体复合以提供增强的半衰期。

    Soluble Hydrophobic Core Carrier Compositions for Delivery of Therapeutic Agents, Methods of Making and Using the Same
    2.
    发明申请
    Soluble Hydrophobic Core Carrier Compositions for Delivery of Therapeutic Agents, Methods of Making and Using the Same 有权
    用于递送治疗剂的可溶性疏水性核心载体组合物，其制备和使用方法

    公开(公告)号：US20100234279A1

    公开(公告)日：2010-09-16

    申请号：US12711564

    申请日：2010-02-24

    Applicant: Gerardo M. Castillo ,  Elijah M. Bolotin

    Inventor： Gerardo M. Castillo ,  Elijah M. Bolotin

    IPC: A61K38/22 ,  C07K17/02 ,  A61P3/10

    CPC classification number: C07K17/02 ,  A61K38/00 ,  A61K47/42 ,  A61K47/542 ,  A61K47/60 ,  A61K47/645

    Abstract: The present invention relates to a soluble hydrophobic-core carrier composition comprising (i) a linear polymeric backbone; (ii) a plurality of hydrophilic polymeric protective chains covalently linked and pendant to the polymeric backbone and (iii) at least one hydrophobic moiety covalently linked and pendant to the polymeric backbone. In certain embodiments, the weight ratio of hydrophilic protective chains to hydrophobic moieties in the carrier is at least 15:1. In other embodiments, at least 90% of the residues of the polymeric backbone are coupled to a hydrophilic polymeric protective chain or a hydrophobic moiety. In other embodiments, the composition further comprises (iv) a hydrophobic load molecule dissociably linked to the hydrophobic moiety of the carrier.

    Abstract translation: 本发明涉及一种可溶性疏水核心载体组合物，其包含（i）直链聚合物骨架; （ii）多个亲水聚合保护链共价连接并悬挂于聚合物主链，和（iii）至少一个共价连接并垂饰于聚合物主链的疏水部分。 在某些实施方案中，载体中亲水性保护链与疏水部分的重量比为至少15:1。 在其它实施方案中，聚合物主链的至少90％的残基与亲水聚合物保护链或疏水部分偶联。 在其它实施方案中，组合物还包含（iv）与载体的疏水部分可离解连接的疏水负载分子。

    Soluble hydrophobic core carrier compositions for delivery of therapeutic agents, methods of making and using the same
    7.
    发明授权
    Soluble hydrophobic core carrier compositions for delivery of therapeutic agents, methods of making and using the same 有权
    用于递送治疗剂的可溶性疏水性核心载体组合物，制备和使用它们的方法

    公开(公告)号：US08999930B2

    公开(公告)日：2015-04-07

    申请号：US12711564

    申请日：2010-02-24

    Applicant: Gerardo M. Castillo ,  Elijah M. Bolotin

    Inventor： Gerardo M. Castillo ,  Elijah M. Bolotin

    IPC: A61K38/00 ,  A61K38/22 ,  A61K38/26 ,  A61K47/48 ,  A61K47/42

    CPC classification number: C07K17/02 ,  A61K38/00 ,  A61K47/42 ,  A61K47/542 ,  A61K47/60 ,  A61K47/645

    Abstract: The present invention relates to a soluble hydrophobic-core carrier composition comprising (i) a linear polymeric backbone; (ii) a plurality of hydrophilic polymeric protective chains covalently linked and pendant to the polymeric backbone and (iii) at least one hydrophobic moiety covalently linked and pendant to the polymeric backbone. In certain embodiments, the weight ratio of hydrophilic protective chains to hydrophobic moieties in the carrier is at least 15:1. In other embodiments, at least 90% of the residues of the polymeric backbone are coupled to a hydrophilic polymeric protective chain or a hydrophobic moiety. In other embodiments, the composition further comprises (iv) a hydrophobic load molecule dissociably linked to the hydrophobic moiety of the carrier.

    Abstract translation: 本发明涉及一种可溶性疏水核心载体组合物，其包含（i）直链聚合物骨架; （ii）多个亲水聚合保护链共价连接并悬挂于聚合物主链，和（iii）至少一个共价连接并垂饰于聚合物主链的疏水部分。 在某些实施方案中，载体中亲水性保护链与疏水部分的重量比为至少15:1。 在其它实施方案中，聚合物主链的至少90％的残基与亲水聚合物保护链或疏水部分偶联。 在其它实施方案中，组合物还包含（iv）与载体的疏水部分可离解连接的疏水负载分子。

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