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    PROCESS FOR THE PREPARATION OF PYRIDO[2,1-a] ISOQUINOLINE DERIVATIVES
    2.
    发明申请
    PROCESS FOR THE PREPARATION OF PYRIDO[2,1-a] ISOQUINOLINE DERIVATIVES 失效
    制备吡咯并[2,1-a]异喹啉衍生物的方法

    公开(公告)号：US20120035368A1

    公开(公告)日：2012-02-09

    申请号：US13274523

    申请日：2011-10-17

    申请人： Stefan Abrecht ,  Jean-Michel Adam ,  Alec Fettes

    发明人： Stefan Abrecht ,  Jean-Michel Adam ,  Alec Fettes

    IPC分类号： C07D455/06 ,  C07D401/06 ,  C07D207/27

    CPC分类号： C07D401/06 ,  C07D207/26 ,  C07D471/04

    摘要： The present invention relates to a novel process for the preparation of pyrido[2,1-a]isoquinoline derivatives of the formula wherein R2, R3 and R4 are each independently selected from the group consisting of hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy and lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by a group consisting of lower alkoxycarbonyl, aryl and heterocyclyl, and the pharmaceutically acceptable salts thereof. The pyrido[2,1-a]isoquinoline derivatives of the formula I are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.

    摘要翻译： 本发明涉及制备下式的吡啶并[2,1-a]异喹啉衍生物的新方法：其中R 2，R 3和R 4各自独立地选自氢，卤素，羟基，低级烷基，低级 烷氧基和低级烯基，其中低级烷基，低级烷氧基和低级烯基可以任选被低级烷氧基羰基，芳基和杂环基所组成的基团及其可药用盐。 式I的吡啶并[2,1-a]异喹啉衍生物可用于治疗和/或预防与DPP IV相关的疾病。

    Synthesis of Cyclosporin Analogs
    4.
    发明申请
    Synthesis of Cyclosporin Analogs 审中-公开
    环孢菌素类似物的合成

    公开(公告)号：US20100062976A1

    公开(公告)日：2010-03-11

    申请号：US12555787

    申请日：2009-09-08

    申请人： Selvaraj A. Naicker ,  Randall W. Yatscoff ,  Robert T. Foster ,  Mark Abel ,  Seetharaman Jayaraman ,  Hans-Jurgen Mair ,  Jean-Michel Adam ,  Bruno Lohri

    发明人： Selvaraj A. Naicker ,  Randall W. Yatscoff ,  Robert T. Foster ,  Mark Abel ,  Seetharaman Jayaraman ,  Hans-Jurgen Mair ,  Jean-Michel Adam ,  Bruno Lohri

    IPC分类号： A61K38/13

    CPC分类号： C07K7/645 ,  A61K9/0095 ,  A61K9/1075 ,  A61K9/4858 ,  A61K38/00 ,  A61K38/13 ,  B82Y5/00 ,  C07K7/64 ,  Y10S530/806

    摘要： The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISATX247, and derivatives thereof. ISATX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereoselectivity. Stereoselective pathways may utilize a Wittig reaction, or an organometallic reagent comprising inorganic elements such as boron, silicon, titanium, and lithium. The ratio of isomers in a mixture may range from about 10 to 90 percent by weight of the (E)-isomer to about 90 to 10 percent by weight of the (Z)-isomer, based on the total weight of the mixture.

    摘要翻译： 本发明涉及结构类似于环孢霉素A的环孢菌素类似物的异构体混合物。该混合物具有比单个异构体和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更强的功效和降低的毒性。 本发明的实施方案涉及称为ISATX247的环孢菌素A类似物的顺式和反式异构体及其衍生物。 ISATX247异构体和烷基化，芳基化和氘代衍生物通过立体选择性途径合成，其中反应的特定条件决定了立体选择性的程度。 立体选择性途径可以利用维蒂希反应或包含无机元素如硼，硅，钛和锂的有机金属试剂。 基于混合物的总重量，混合物中异构体的比例可以为（E） - 异构体的约10至90重量％至（Z） - 异构体的约90至10重量％。

    Process for the preparation of pyrido[2,1-a] isoquinoline derivatives
    6.
    发明授权
    Process for the preparation of pyrido[2,1-a] isoquinoline derivatives 失效
    吡啶并[2,1-a]异喹啉衍生物的制备方法

    公开(公告)号：US08420818B2

    公开(公告)日：2013-04-16

    申请号：US13274523

    申请日：2011-10-17

    申请人： Stefan Abrecht ,  Jean-Michel Adam ,  Alec Fettes

    发明人： Stefan Abrecht ,  Jean-Michel Adam ,  Alec Fettes

    IPC分类号： C07D455/06

    CPC分类号： C07D401/06 ,  C07D207/26 ,  C07D471/04

    摘要： The present invention relates to a novel process for the preparation of pyrido[2,1-a]isoquinoline derivatives of the formula wherein R2, R3 and R4 are each independently selected from the group consisting of hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy and lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by a group consisting of lower alkoxycarbonyl, aryl and heterocyclyl, and the pharmaceutically acceptable salts thereof. The pyrido[2,1-a]isoquinoline derivatives of the formula I are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.

    摘要翻译： 本发明涉及制备下式的吡啶并[2,1-a]异喹啉衍生物的新方法：其中R 2，R 3和R 4各自独立地选自氢，卤素，羟基，低级烷基，低级 烷氧基和低级烯基，其中低级烷基，低级烷氧基和低级烯基可以任选被低级烷氧基羰基，芳基和杂环基所组成的基团及其可药用盐。 式I的吡啶并[2,1-a]异喹啉衍生物可用于治疗和/或预防与DPP IV相关的疾病。

    PROCESS FOR THE PREPARATION OF PYRIDO[2,1-a] ISOQUINOLINE DERIVATIVES
    8.
    发明申请
    PROCESS FOR THE PREPARATION OF PYRIDO[2,1-a] ISOQUINOLINE DERIVATIVES 审中-公开
    制备吡咯并[2,1-a]异喹啉衍生物的方法

    公开(公告)号：US20090163718A1

    公开(公告)日：2009-06-25

    申请号：US12326976

    申请日：2008-12-03

    申请人： Stefan Abrecht ,  Jean-Michel Adam ,  Alec Fettes

    发明人： Stefan Abrecht ,  Jean-Michel Adam ,  Alec Fettes

    IPC分类号： C07D471/04 ,  C07D207/27 ,  C07D401/06

    CPC分类号： C07D401/06 ,  C07D207/26 ,  C07D471/04

    摘要： The present invention relates to a novel process for the preparation of pyrido[2,1-a]isoquinoline derivatives of the formula wherein R2, R3 and R4 are each independently selected from the group consisting of hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy and lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by a group consisting of lower alkoxycarbonyl, aryl and heterocyclyl, and the pharmaceutically acceptable salts thereof. The pyrido[2,1-a]isoquinoline derivatives of the formula I are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.

    摘要翻译： 本发明涉及制备下式的吡啶并[2,1-a]异喹啉衍生物的新方法：其中R 2，R 3和R 4各自独立地选自氢，卤素，羟基，低级烷基，低级 烷氧基和低级烯基，其中低级烷基，低级烷氧基和低级烯基可以任选被低级烷氧基羰基，芳基和杂环基所组成的基团及其可药用盐。 式I的吡啶并[2,1-a]异喹啉衍生物可用于治疗和/或预防与DPP IV相关的疾病。