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    ETOMIDATE ANALOGUES WITH IMPROVED PHARMACOKINETIC AND PHARMACODYNAMIC PROPERTIES
    2.
    发明申请
    ETOMIDATE ANALOGUES WITH IMPROVED PHARMACOKINETIC AND PHARMACODYNAMIC PROPERTIES 有权
    具有改善药物动力学和药物动力学特性的ETOMIDATE模拟物

    公开(公告)号：US20110053998A1

    公开(公告)日：2011-03-03

    申请号：US12935086

    申请日：2009-03-31

    申请人： Douglas E. Raines ,  Stuart A. Forman ,  Keith W. Miller ,  Syed Shaukat Husain ,  Joseph F. Cotten

    发明人： Douglas E. Raines ,  Stuart A. Forman ,  Keith W. Miller ,  Syed Shaukat Husain ,  Joseph F. Cotten

    IPC分类号： A61K31/4174 ,  C07D233/90 ,  A61P23/00

    CPC分类号： C07D233/90 ,  A61K31/4174 ,  A61K45/06

    摘要： The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.

    摘要翻译： 本发明涉及式（I）化合物：其中R1是L1C（O）OT或L1C（O）OL2C（O）OT; R2是取代或未取代的C1-C10烷基，C2-C10烯基或C2-C10炔基，或R1; n为0〜5的整数， 每个R 3独立地是卤素或R 2; L1和L2各自独立地为键，取代或未取代的C1-C10亚烷基，C2-C10亚烯基或C2-C10亚炔基; 和T是H，取代或未取代的C 1 -C 10烷基，C 2 -C 10烯基或C 2 -C 10炔基，硝基苯酚或环丙基。 本发明还涉及包含根据式（I）的化合物和药学上可接受的载体的药物组合物，以及通过施用这种药物组合物在哺乳动物中提供麻醉的方法。

    Etomidate analogues that do not inhibit adrenocortical steroid synthesis
    4.
    发明授权
    Etomidate analogues that do not inhibit adrenocortical steroid synthesis 有权
    不抑制肾上腺皮质类固醇合成的依托咪酯类似物

    公开(公告)号：US08765973B2

    公开(公告)日：2014-07-01

    申请号：US13382544

    申请日：2010-07-08

    申请人： Douglas E. Raines ,  Joseph F. Cotten ,  Stuart A. Forman ,  Keith W. Miller ,  Syed S. Husain ,  Gregory D. Cuny

    发明人： Douglas E. Raines ,  Joseph F. Cotten ,  Stuart A. Forman ,  Keith W. Miller ,  Syed S. Husain ,  Gregory D. Cuny

    IPC分类号： C07D207/337 ,  A61K31/40

    CPC分类号： C07D207/34 ,  A61K31/40

    摘要： The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; R4 and R5 are independently H, halogen, CN or CF3; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.

    摘要翻译： 本发明涉及式（I）化合物：其中R1是L1C（O）OT或L1C（O）OL2C（O）OT; R2是取代或未取代的C1-C10烷基，C2-C10烯基或C2-C10炔基，或R1; n为0〜5的整数， 每个R 3独立地是卤素或R 2; R4和R5独立地为H，卤素，CN或CF3; L1和L2各自独立地为键，取代或未取代的C1-C10亚烷基，C2-C10亚烯基或C2-C10亚炔基; 和T是H，取代或未取代的C 1 -C 10烷基，C 2 -C 10烯基或C 2 -C 10炔基，硝基苯酚或环丙基。 本发明还涉及包含根据式（I）的化合物和药学上可接受的载体的药物组合物，以及通过施用这种药物组合物在哺乳动物中提供麻醉的方法。