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    Inhibiting Eph B-3 kinase
    2.
    发明授权
    Inhibiting Eph B-3 kinase 有权
    抑制Eph B-3激酶

    公开(公告)号：US08927545B2

    公开(公告)日：2015-01-06

    申请号：US13260990

    申请日：2010-03-30

    申请人： Lixin Qiao ,  Marcie Glicksman ,  Thomas Gainer ,  Donald C. Lo ,  Ross L. Stein ,  Sungwoon Choi ,  Gregory D. Cuny

    发明人： Lixin Qiao ,  Marcie Glicksman ,  Thomas Gainer ,  Donald C. Lo ,  Ross L. Stein ,  Sungwoon Choi ,  Gregory D. Cuny

    IPC分类号： A61K31/535 ,  C07D491/02 ,  C07D498/02 ,  C07D513/02 ,  C07D515/02 ,  A61K31/437 ,  A61K31/00

    CPC分类号： A61K31/437 ,  A61K31/00

    摘要： EphB3 kinase inhibitor compounds, including certain pyrazolo[1,5-a]pyridine and imidazo[1,2-a]pyridine compounds, inhibit EphB3 kinase. The EphB3 kinase inhibitor compounds can have greater potency for the inhibition of EphB3 kinase than general kinase inhibitors. Pharmaceutical compositions, such as neuroprotective agents, comprising the EphB3 kinase inhibitor compounds are also provided. The EphB3 kinase inhibitor compounds and pharmaceutical compositions are useful, for example, to provide neuroprotection and/or repair of neuronal tissue damaged during an ischemic event, such as a stroke.

    摘要翻译： 包括某些吡唑并[1,5-a]吡啶和咪唑并[1,2-a]吡啶化合物的EphB3激酶抑制剂化合物抑制EphB3激酶。 与一般激酶抑制剂相比，EphB3激酶抑制剂化合物对EphB3激酶的抑制作用可能更大。 还提供了包含EphB3激酶抑制剂化合物的药物组合物，例如神经保护剂。 EphB3激酶抑制剂化合物和药物组合物可用于例如在缺血事件（例如中风）期间损伤的神经元组织的神经保护和/或修复。

    Etomidate analogues that do not inhibit adrenocortical steroid synthesis
    5.
    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。