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    INDOLE-TYPE DERIVATIVES AS INHIBITORS OF p38 KINASE
    63.
    发明申请
    INDOLE-TYPE DERIVATIVES AS INHIBITORS OF p38 KINASE 审中-公开
    作为p38激酶的抑制剂的吲哚型衍生物

    公开(公告)号：US20070161649A1

    公开(公告)日：2007-07-12

    申请号：US11689418

    申请日：2007-03-21

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

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

    IPC: A61K31/496 ,  A61K31/454 ,  C07D403/02

    CPC classification number: C07D209/24 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

    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 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; 1和k中的每一个是0-2的整数，其中1和k之和为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。

    Methods to synthesize indoles as precursors for pharmaceuticals
    64.
    发明申请
    Methods to synthesize indoles as precursors for pharmaceuticals 审中-公开
    合成吲哚作为药物前体的方法

    公开(公告)号：US20070066833A1

    公开(公告)日：2007-03-22

    申请号：US11507869

    申请日：2006-08-21

    Applicant: Sundeep Dugar ,  Peter Giannousis

    Inventor： Sundeep Dugar ,  Peter Giannousis

    IPC: C07D209/04

    CPC classification number: C07D209/08

    Abstract: The invention provides improved methods for the synthesis of indoles, especially useful for making indoles having an ester or amide group at C-5. The methods involve cyclization of a protected ortho-acetylene-substituted aniline derivative to produce an indole.

    Abstract translation: 本发明提供了用于合成吲哚的改进方法，特别可用于在C-5制备具有酯或酰胺基团的吲哚。 所述方法包括环化受保护的邻乙炔取代的苯胺衍生物以产生吲哚。

    Indole-type derivatives as inhibitors of p38 kinase
    69.
    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。

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