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    Deuterated Cyclosporine Analogs and Methods of Making the Same
    1.
    发明申请
    Deuterated Cyclosporine Analogs and Methods of Making the Same 审中-公开
    氘代环孢霉素类似物及其制备方法

    公开(公告)号：US20120214745A1

    公开(公告)日：2012-08-23

    申请号：US13402370

    申请日：2012-02-22

    申请人： Salvaraj Naicker ,  Randall W. Yatscoff ,  Robert T. Foster

    发明人： Salvaraj Naicker ,  Randall W. Yatscoff ,  Robert T. Foster

    IPC分类号： A61K38/13 ,  A61P37/06 ,  C07K7/64

    CPC分类号： C07K7/645 ,  A61K38/00 ,  C07B59/008 ,  C07K1/13 ,  C07K7/64 ,  Y10S530/806 ,  Y10S530/807

    摘要： Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporin and cyclosporine derivatives. The cyclosporine derivatives of the present invention are produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by: (1) Chemical substitution and optionally deuterium substitution of amino acid 1; and (2) deuterium substitution at key sites of metabolism of the cyclosporine A molecule such as amino acids 1, 4, 9. Also disclosed are methods of producing the cyclosporine derivatives and method of producing immunosuppression with reduced toxicity with the disclosed cyclosporine derivatives.

    摘要翻译： 公开了与天然存在的和其它目前已知的环孢菌素和环孢菌素衍生物相比具有增强的功效和降低的毒性的环孢菌素衍生物。 本发明的环孢菌素衍生物通过以下方式通过环孢菌素A（CsA）分子的化学和同位素取代产生：（1）氨基酸1的化学取代和任选的氘取代; 和（2）在环孢菌素A分子的代谢关键位置的氘代替，例如氨基酸1,4,9。还公开了产生环孢菌素衍生物的方法和与所公开的环孢菌素衍生物一起产生具有降低的毒性的免疫抑制的方法。

    DEUTERATED CYCLOSPORINE ANALOGS AND METHODS OF MAKING THE SAME
    2.
    发明申请
    DEUTERATED CYCLOSPORINE ANALOGS AND METHODS OF MAKING THE SAME 审中-公开
    去除环孢霉素类似物及其制备方法

    公开(公告)号：US20110166080A1

    公开(公告)日：2011-07-07

    申请号：US13048258

    申请日：2011-03-15

    申请人： Salvaraj Naicker ,  Randall W. Yatscoff ,  Robert T. Foster

    发明人： Salvaraj Naicker ,  Randall W. Yatscoff ,  Robert T. Foster

    IPC分类号： A61K38/13 ,  C07K7/64 ,  A61P37/06

    CPC分类号： C07K7/645 ,  A61K38/00 ,  C07B59/008 ,  C07K1/13 ,  C07K7/64 ,  Y10S530/806 ,  Y10S530/807

    摘要： Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporin and cyclosporine derivatives. The cyclosporine derivatives of the present invention are produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by: (1) Chemical substitution and optionally deuterium substitution of amino acid 1; and (2) deuterium substitution at key sites of metabolism of the cyclosporine A molecule such as amino acids 1, 4, 9. Also disclosed are methods of producing the cyclosporine derivatives and method of producing immunosuppression with reduced toxicity with the disclosed cyclosporine derivatives.

    摘要翻译： 公开了与天然存在的和其它目前已知的环孢菌素和环孢菌素衍生物相比具有增强的功效和降低的毒性的环孢菌素衍生物。 本发明的环孢菌素衍生物通过以下方式通过环孢菌素A（CsA）分子的化学和同位素取代产生：（1）氨基酸1的化学取代和任选的氘取代; 和（2）在环孢菌素A分子的代谢关键位置的氘代替，例如氨基酸1,4,9。还公开了产生环孢菌素衍生物的方法和与所公开的环孢菌素衍生物一起产生具有降低的毒性的免疫抑制的方法。

    Deuterated cyclosporin analogs and their use as immunomodulating agents
    4.
    发明申请
    Deuterated cyclosporin analogs and their use as immunomodulating agents 有权
    氘代环孢菌素类似物及其作为免疫调节剂的用途

    公开(公告)号：US20060052290A1

    公开(公告)日：2006-03-09

    申请号：US11245775

    申请日：2005-10-06

    申请人： Salvaraj Naicker ,  Randall Yatscoff ,  Robert Foster

    发明人： Salvaraj Naicker ,  Randall Yatscoff ,  Robert Foster

    IPC分类号： A61K38/13 ,  C07K7/64

    CPC分类号： C07K7/645 ,  A61K38/00 ,  C07B59/008 ,  C07K1/13 ,  C07K7/64 ,  Y10S530/806 ,  Y10S530/807

    摘要： Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins and cyclosporine derivatives. The cyclosporine derivatives of the present invention are produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by: (1) Chemical substitution and optionally deuterium substitution of amino acid 1; and (2) deuterium substitution at key sites of metabolism of the cyclosporine A molecule such as amino acids 1, 4, 9. Also disclosed are methods of producing the cyclosporine derivatives and method of producing immunosuppression with reduced toxicity with the disclosed cyclosporine derivatives.

    摘要翻译： 公开了与天然存在的和其他目前已知的环孢菌素和环孢菌素衍生物相比具有增强的功效和降低的毒性的环孢菌素衍生物。 本发明的环孢菌素衍生物通过以下方式通过环孢菌素A（CsA）分子的化学和同位素取代产生：（1）氨基酸1的化学取代和任选的氘取代; 和（2）在环孢菌素A分子的代谢关键位置的氘代替，例如氨基酸1,4,9。还公开了产生环孢菌素衍生物的方法和与所公开的环孢菌素衍生物一起产生具有降低的毒性的免疫抑制的方法。