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    3-Cyano-quinoline derivatives
    1.
    发明申请
    3-Cyano-quinoline derivatives 失效
    3-氰基 - 喹啉衍生物

    公开(公告)号：US20050282856A1

    公开(公告)日：2005-12-22

    申请号：US10532958

    申请日：2003-10-28

    Applicant: Laurent Hennequin

    Inventor： Laurent Hennequin

    IPC: A61P35/00 ,  C07D405/12 ,  A61K31/4709 ,  C07D45/02

    CPC classification number: C07D405/12

    Abstract: The invention concerns quinoline derivatives of Formula (I) wherein each of Z1, m, R1, n, R3, Z2 and R14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive or anti-proliferative agent in the containment and/or treatment of solid tumour disease.

    Abstract translation: 本发明涉及式（I）的喹啉衍生物，其中Z 1，m，R 1，n，R 3，Z， > 2 和R 14具有上文在描述中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于在实体瘤疾病的遏制和/或治疗中作为抗侵袭性或抗增殖剂的药物的用途。

    Neurotrophin antagonist compositions
    2.
    发明申请
    Neurotrophin antagonist compositions 失效
    神经营养因子拮抗剂组合物

    公开(公告)号：US20050250807A1

    公开(公告)日：2005-11-10

    申请号：US11179610

    申请日：2005-07-13

    Applicant: Ashok Tehim ,  Xiannong Chen

    Inventor： Ashok Tehim ,  Xiannong Chen

    IPC: A61K31/435 ,  A61K31/473 ,  A61K31/4738 ,  A61K31/5377 ,  A61P25/28 ,  C07D221/14 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D405/06 ,  C07D471/06 ,  C07D45/02

    CPC classification number: C07D221/14 ,  A61K31/473 ,  A61K31/4738 ,  C07D401/04 ,  C07D401/06 ,  C07D405/06

    Abstract: A pharmaceutical composition comprising a compound of Formula I wherein R1 is selected from, inter alia, alkyl, aryl-loweralkyl, heterocycle-loweralkyl, loweralkyl-carbonate; optionally substituted amino; benzimidaz-2-yl; optionally substituted phenyl; loweralkyl-(R5)(R6) wherein one of R5 and R6 is selected from H and and the other is selected from carboxy, carboxy-loweralkyl and lower alkoxycarbonyl; NHCH2CH2OX wherein X represents an in vivo hydrolyzable ester; and R2 and R3 are independently selected from H, NO2, halo, di(loweralkyl)amino, cyano, C(O)OH, phenyl-S—, loweralkyl, and Z(O)OR7 wherein Z is selected from C and S and R7 is selected from H, lower alkylamino and arylamino; or pharmaceutically acceptable salts or certain in vivo hydrolyzable esters or amides thereof, in an amount effective to inhibit neurotrophin-mediated activity, and a suitable carrier, is described. The compositions are useful to inhibit undesirable neurotrophin-mediated activity such as the neurite outgrowth that occurs in some neurodegenerative disease states.

    Abstract translation: 一种药物组合物，其包含式I化合物，其中R 1选自烷基，芳基 - 低级烷基，杂环 - 低级烷基，低级烷基 - 碳酸酯; 任选取代的氨基; 苯并咪唑-2-基; 任选取代的苯基; 低级烷基 - （R 5）（R 6）其中R 5和R 6中的一个选自H 并且另一个选自羧基，羧基 - 低级烷基和低级烷氧基羰基; NHCH 2 CH 2 OX其中X表示体内可水解的酯; R 2和R 3独立地选自H，NO 2，卤素，二（低级烷基）氨基，氰基，C（O） OH，苯基-S-，低级烷基和Z（O）OR 7其中Z选自C和S，R 7选自H，低级烷基氨基和芳基氨基 ; 或其药学上可接受的盐或某些体内可水解的酯或酰胺，以有效抑制神经营养因子介导的活性的量和合适的载体。 该组合物可用于抑制不期望的神经营养因子介导的活性，例如在一些神经变性疾病状态中发生的神经突生长。

    Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof
    7.
    发明申请
    Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof 有权
    糖皮质激素模拟物，其制备方法，药物组合物及其用途

    公开(公告)号：US20050203128A1

    公开(公告)日：2005-09-15

    申请号：US11072797

    申请日：2005-03-04

    Applicant: Thomas Kirrane ,  Daniel Kuzmich ,  John Proudfoot

    Inventor： Thomas Kirrane ,  Daniel Kuzmich ,  John Proudfoot

    IPC: A61K31/405 ,  A61K31/47 ,  C07D215/14 ,  C07D311/58 ,  C07D405/06 ,  C07D471/04 ,  C07D45/02

    CPC classification number: C07D471/04 ,  C07D215/14 ,  C07D311/58 ,  C07D405/06

    Abstract: Compounds of Formula (IA) and Formula (IB) where in R1 stands for the following group (the dashed line indicates the point of attachment) and R2, R3, R4, R5, R6, Y, Z, X1 and X2 are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

    Abstract translation: 其中在R 1中的式（IA）和式（IB）的化合物代表下列基团（虚线表示连接点），R 2，R 2， R 4，R 4，R 5，R 6，Y，Z，X 1，O 2， （IA）和式（IB）或其互变异构体，前药，溶剂合物或其盐如本文所定义; 含有这些化合物的药物组合物，以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法，或其特征在于使用这些化合物的患者的炎症，过敏或增殖过程。

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