PYRIDO[3,4-B]INDOLES AND METHODS OF USE
    33.
    发明申请

    公开(公告)号:US20130137705A1

    公开(公告)日:2013-05-30

    申请号:US13498099

    申请日:2010-09-23

    CPC classification number: C07D471/04

    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

    PYRIDO[4,3-B]INDOLES AND METHODS OF USE
    36.
    发明申请
    PYRIDO[4,3-B]INDOLES AND METHODS OF USE 失效
    吡咯并[4,3-B]吲哚和使用方法

    公开(公告)号:US20120172377A1

    公开(公告)日:2012-07-05

    申请号:US13318124

    申请日:2010-04-29

    CPC classification number: C07D471/04

    Abstract: New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

    Abstract translation: 描述了可用于调节个体中组胺受体的新杂环化合物。 描述了吡啶并[4,3-b]吲哚,以及包含化合物的药物组合物以及在各种治疗应用中使用该化合物的方法,包括治疗认知障碍,精神病性障碍,神经递质介导的病症和/或 神经元紊乱。

    Indole-type derivatives as inhibitors of p38 kinase
    39.
    发明授权
    Indole-type derivatives as inhibitors of p38 kinase 有权
    吲哚型衍生物作为p38激酶的抑制剂

    公开(公告)号:US07238712B2

    公开(公告)日:2007-07-03

    申请号:US10156997

    申请日:2002-05-28

    Abstract: The invention is directed to methods to inhibit p38-α kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein represents a single or double bond; one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent; A is —Wi—COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2–6 Å, and each of i and j is independently 0 or 1; Z3 is NR7 or O; each R3 is independently a noninterfering substituent; n is 0–3; each of L1 and L2 is a linker; each R4 is independently a noninterfering substituent; m is 0–4; Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent; each of l and k is an integer from 0–2 wherein the sum of l and k is 0–3; Ar is an aryl group substituted with 0–5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; and the distance between the atom of Ar linked to L2 and the center of the α ring is 4.5–24 Å.

    Abstract translation: 本发明涉及使用下式的化合物及其药学上可接受的盐或其药物组合物来抑制p38-α激酶的方法,其中表示单键或双键; 一个Z 2是CA或CR 8 A,另一个是CR 1,CR 1,2, 其中每个R 1,R 6和R 8独立为氢,NR 6,N 6, 或非干扰取代基; A是其中Y是COR 2或其等同体和R 2的-Wi-i-X 氢或非干扰取代基,W和X各自为2-6的间隔基,i和j各自独立地为0或1; Z 3是NR 7或O; 每个R 3独立地是非干扰取代基; n为0-3; L 1和L 2各自为连接体; 每个R 4独立地是非干扰取代基; m为0-4; Z 1是CR 5或N,其中R 5是氢或非干扰取代基; l和k中的每一个是0-2的整数,其中l和k的和为0-3; Ar是被0-5个非直链取代基取代的芳基,其中两个非干扰取代基可以形成稠环; 并且与L 2连接的Ar原子和α环的中心之间的距离为4.5-24埃。

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