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    Polymer Conjugates of K-252A and Derivatives Thereof
    4.
    发明申请
    Polymer Conjugates of K-252A and Derivatives Thereof 有权
    K-252A及其衍生物的聚合物共轭物

    公开(公告)号：US20080193517A1

    公开(公告)日：2008-08-14

    申请号：US12064461

    申请日：2006-08-25

    申请人： Silvio Traversa ,  Raffaella Bagnod ,  Domenico Barone ,  Luisa Bertarione Rava Rossa ,  Silvano Fumero ,  Valentina Mainero ,  Alessandra Marconi ,  Cecilia Oderda ,  Carlo Pincelli ,  Chiara Lorenzetto ,  Luca Beccaria

    发明人： Silvio Traversa ,  Raffaella Bagnod ,  Domenico Barone ,  Luisa Bertarione Rava Rossa ,  Silvano Fumero ,  Valentina Mainero ,  Alessandra Marconi ,  Cecilia Oderda ,  Carlo Pincelli ,  Chiara Lorenzetto ,  Luca Beccaria

    IPC分类号： A61K31/787 ,  C08G73/06 ,  A61K9/127 ,  A61P35/00 ,  A61P17/00 ,  A61P19/00 ,  A61P25/00

    CPC分类号： C08G73/0672 ,  A61K47/60 ,  C08G61/124

    摘要： The present invention relates to novel polymer conjugates of K-252a and derivatives thereof and to their use for the preparation of a pharmaceutical composition useful for the prevention, alleviation and treatment of kinase-associated pathologies. In particular, the present invention relates to the prevention, alleviation and treatment of HMGB1-associated pathologies. In a particular aspect, the invention relates to the use of the novel polymer conjugates of K-252a and derivatives thereof in the preparation of a pharmaceutical composition useful for the prevention, alleviation and treatment of neurological disorders, neuropathies and neurodegenerative disorders of the central and peripheral nervous system. In a further preferred aspect, the invention relates to the use of the polymer conjugates in the preparation of a pharmaceutical composition useful for the prevention, alleviation and treatment of dermal pathologies, in particular dermal pathologies associated with an excessive keratinocyte proliferation, in particular psoriasis. In a still further aspect, the invention relates to the use of the polymer conjugates in the prevention, alleviation and treatment of NGF-related pain. More specifically, the present invention relates to a polymer conjugate of K-252a and derivatives thereof, wherein the polymer is polyethylene glycol or methoxy-polyethylene glycol formula (I).

    摘要翻译： 本发明涉及K-252a及其衍生物的新型聚合物缀合物及其用于制备可用于预防，缓解和治疗激酶相关病理学的药物组合物的用途。 特别地，本发明涉及HMGB1相关病变的预防，缓解和治疗。 在一个特定方面，本发明涉及K-252a及其衍生物的新型聚合物缀合物在制备药物组合物中的用途，所述药物组合物可用于预防，缓解和治疗中枢神经系统疾病，神经病和神经变性疾病 外周神经系统。 在另一优选方面，本发明涉及聚合物缀合物在制备用于预防，减轻和治疗真皮病理学，特别是与过度角质形成细胞增殖相关的皮肤病理学，特别是牛皮癣的药物组合物中的用途。 在另一方面，本发明涉及聚合物缀合物在预防，减轻和治疗NGF相关疼痛中的用途。 更具体地说，本发明涉及K-252a及其衍生物的聚合物缀合物，其中聚合物是聚乙二醇或甲氧基 - 聚乙二醇配方（I）。