Etomidate analogues that do not inhibit adrenocortical steroid synthesis
    1.
    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:US09187421B2

    公开(公告)日:2015-11-17

    申请号:US14281149

    申请日:2014-05-19

    IPC分类号: A61K31/40 C07D207/34

    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。

    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:US20140200251A1

    公开(公告)日:2014-07-17

    申请号:US14026456

    申请日:2013-09-13

    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 with improved pharmacokinetic and pharmacodynamic properties
    3.
    发明授权
    Etomidate analogues with improved pharmacokinetic and pharmacodynamic properties 有权
    具有改善的药代动力学和药效学性质的依托咪酯类似物

    公开(公告)号:US09181197B2

    公开(公告)日:2015-11-10

    申请号:US14026456

    申请日:2013-09-13

    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。