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    Indole-type derivatives as inhibitors of p38 kinase
    23.
    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：US06867209B1

    公开(公告)日：2005-03-15

    申请号：US09575060

    申请日：2000-05-19

    Applicant: Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

    Inventor： Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

    IPC: C07D209/08 ,  C07D209/24 ,  C07D235/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D471/04 ,  A61K31/495 ,  C07D241/04

    CPC classification number: C07D235/06 ,  C07D209/08 ,  C07D209/24 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D471/04

    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; as 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 1 and k is an integer from 0-2 wherein the sum of 1 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抑制p38-α激酶的方法，其中表示单键或双键;一个Z 2为CA或CR <8> A，另一个为CR <1> ，CR 1，NR 6或N，其中每个R 1，R 6和R 8独立地是氢或非干扰取代基; A是-Wi-COX j Y，其中Y是COR 2或 其等同基团和R 2是氢或非干扰取代基，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为NR 7 >或O;每个R 3独立地为非干扰取代基; n为0-3; L 1和L 2各自为连接基;每个R 4独立地为非干扰取代基; m为0 -4; Z 1是CR 5或N，其中R 5是氢或非干扰取代基; 1和k各自是整数fr om 0-2其中1和k的和为0-3; Ar是被0-5个非干扰取代基取代的芳基，其中两个非干扰取代基可以形成稠环; 并且连接到L 2的Ar原子与α环的中心之间的距离为4.5-24。

    Pyrido[4,3-B]indoles and methods of use
    25.
    发明授权
    Pyrido[4,3-B]indoles and methods of use 有权
    吡啶并[4,3-B]吲哚和使用方法

    公开(公告)号：US09255094B2

    公开(公告)日：2016-02-09

    申请号：US13318123

    申请日：2010-04-29

    Applicant: Rajendra Parasmal Jain ,  Sarvajit Chakravarty

    Inventor： Rajendra Parasmal Jain ,  Sarvajit Chakravarty

    IPC: A61K31/437 ,  C07D417/04 ,  C07D471/04

    CPC classification number: C07D471/04

    Abstract: Provided are new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Also provided are pyrido[4,3-b]indoles, 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: 提供了可用于调节个体中组胺受体的新的杂环化合物。 还提供了吡啶并[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。

    PYRIDO[4,3-b]INDOLE AND PYRIDO[3,4-b]INDOLE DERIVATIVES AND METHODS OF USE
    27.
    发明申请
    PYRIDO[4,3-b]INDOLE AND PYRIDO[3,4-b]INDOLE DERIVATIVES AND METHODS OF USE 有权
    吡咯并[4,3-b]吲哚和吡咯并[3,4-b]吲哚衍生物及其使用方法

    公开(公告)号：US20140206711A1

    公开(公告)日：2014-07-24

    申请号：US14000179

    申请日：2012-02-17

    Applicant: Sarvajit Chakravarty ,  Barry Patrick Hart ,  Rajendra Parasmal Jain

    Inventor： Sarvajit Chakravarty ,  Barry Patrick Hart ,  Rajendra Parasmal Jain

    IPC: C07D471/04

    CPC classification number: A61K31/437 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  A61K2300/00

    Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are 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. The compounds may bind to and antagonize receptor α2B, α1B or α2A. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption, or to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. The compounds may also be used to treat diseases or conditions that are expected to be responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular, renal disorders or type 2 diabetes is particularly described.

    Abstract translation: 本公开涉及吡啶并[4,3-b]吲哚和吡啶并[3,4-b]吲哚衍生物。 还提供了包含化合物的药物组合物，以及在多种治疗应用中使用化合物的方法，包括治疗认知障碍，精神病性障碍，神经递质介导的病症和/或神经元病症。 该化合物可以结合并拮抗受体α2B，α1B或α2A。 这些化合物可用于治疗，例如（i）降低血压和/或（ii）促进肾血流量和/或（iii）降低或抑制钠再吸收，或调节血糖水平，增加胰岛素分泌和 治疗或预期对胰岛素生产增加有反应的疾病或病症。 所述化合物也可用于治疗预期对血压降低有反应的疾病或病症。 具体描述了使用该化合物治疗心血管，肾脏疾病或2型糖尿病。

    Pyrido[4,3-B]indoles and methods of use
    29.
    发明授权
    Pyrido[4,3-B]indoles and methods of use 失效
    吡啶并[4,3-B]吲哚和使用方法

    公开(公告)号：US08741919B2

    公开(公告)日：2014-06-03

    申请号：US13318124

    申请日：2010-04-29

    Applicant: Rajendra Parasmal Jain ,  Sarvajit Chakravarty

    Inventor： Rajendra Parasmal Jain ,  Sarvajit Chakravarty

    IPC: A61K31/04 ,  C07D215/38

    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。

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