ETOMIDATE ANALOGUES WITH IMPROVED PHARMACOKINETIC AND PHARMACODYNAMIC PROPERTIES
    1.
    发明申请
    ETOMIDATE ANALOGUES WITH IMPROVED PHARMACOKINETIC AND PHARMACODYNAMIC PROPERTIES 审中-公开
    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:WO2009146024A1

    公开(公告)日:2009-12-03

    申请号:PCT/US2009/038872

    申请日:2009-03-31

    CPC classification number: C07D233/90 A61K31/4174 A61K45/06

    Abstract: The invention is directed to compounds according to formula (I): where R 1 is L 1 C(O)OT or L 1 C(O)OL 2 C(O)OT; R 2 is a substituted or unsubstituted C 1 -C 10 alkyl, C 2 -C 10 alkenyl, or C 2 -C 10 alkynyl, or R 1 ; n is an integer from 0 to 5; each R 3 is independently halogen or R 2 ; L 1 and L 2 are each independently a bond, a substituted or unsubstituted C 1 -C 10 alkylene, C 2 -C 10 alkenylene, or C 2 -C 10 alkynylene; and T is H, a substituted or unsubstituted C 1 -C 10 alkyl, C 2 -C 10 alkenyl, or C 2 -C 10 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.

    Abstract translation: 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 WITH IMPROVED PHARMACOKINETIC AND PHARMACODYNAMIC PROPERTIES
    3.
    发明申请
    ETOMIDATE ANALOGUES WITH IMPROVED PHARMACOKINETIC AND PHARMACODYNAMIC PROPERTIES 审中-公开
    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:WO2009146024A8

    公开(公告)日:2010-04-08

    申请号:PCT/US2009038872

    申请日:2009-03-31

    CPC classification number: C07D233/90 A61K31/4174 A61K45/06

    Abstract: 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.

    Abstract translation: 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.
    发明申请
    ETOMIDATE ANALOGUES THAT DO NOT INHIBIT ADRENOCORTICAL STEROID SYNTHESIS 审中-公开
    不抑制ADRENOCORTICAL STEROID合成的ETOMIDATE模拟物

    公开(公告)号:WO2011005969A2

    公开(公告)日:2011-01-13

    申请号:PCT/US2010041379

    申请日:2010-07-08

    CPC classification number: C07D207/34 A61K31/40

    Abstract: 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.

    Abstract translation: 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。

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