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29 条记录 (耗时 0.047 秒)

    Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors
    1.
    发明授权
    Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors 失效
    用作PDE4抑制剂的取代的2-喹啉基 - 恶唑

    公开(公告)号：US07511062B2

    公开(公告)日：2009-03-31

    申请号：US11130359

    申请日：2005-05-16

    申请人： Rongze Kuang ,  David Blythin ,  Neng-Yang Shih ,  Ho-Jane Shue ,  Xiao Chen ,  Jianhua Cao ,  Danlin Gu ,  Ying Huang ,  John H. Schwerdt ,  Pauline C. Ting ,  Shing-Chun Wong ,  Li Xiao

    发明人： Rongze Kuang ,  David Blythin ,  Neng-Yang Shih ,  Ho-Jane Shue ,  Xiao Chen ,  Jianhua Cao ,  Danlin Gu ,  Ying Huang ,  John H. Schwerdt ,  Pauline C. Ting ,  Shing-Chun Wong ,  Li Xiao

    IPC分类号： C07D215/38 ,  A61K31/44

    CPC分类号： C07D405/14 ,  C07D401/04 ,  C07D405/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

    摘要： The invention claims compounds of the formula wherein is a 5-membered heteroaryl; X is S or O; R1 is H, alkyl, cycloalkyl, cylcoalkylalkyl-, —CH2F, —CHF2, —CF3, —C(O)alkyl or —C(O)NR18R19; R3 and R4 H, alkyl, hydroxyalkyl or —C(O)Oalkyl; R5 and R6 are H, alkyl, hydroxyalkyl, alkoxyalkyl, mercaptoalkyl, —CH2F, —CHF2, —CF3, —C(O)OH or —C(O)Oalkyl; R7 is H, alkyl, alkenyl, hydroxyalkyl, cycloalkyl, alkoxyalkyl, aminoalkyl, (R17-phenyl)alkyl or —CH2—C(O)—O-alkyl; and R8 comprises alkyl, heteroaryl, phenyl or cycloalkyl, or heterocycloalkyl, all optionally substituted, or a cycloalkyl- or heterocycloalkyl-substituted amide; or R7 and R8 and the nitrogen to which they are attached together form an optionally substituted ring; and the remaining variables are as defined in the specification. Also claimed are pharmaceutical compositions, the use of the compounds as PDE4 inhibitors, and combinations with other actives.

    摘要翻译： 本发明要求具有下式的化合物其中是5元杂芳基; X是S或O; R 1是H，烷基，环烷基，环烷基烷基 - ， - CH 2 F，-CHF 2，-CF 3，-C（O）烷基或-C（O）NR 18 R 19; R 3和R 4 H，烷基，羟基烷基或-C（O）O烷基; R5和R6是H，烷基，羟基烷基，烷氧基烷基，巯基烷基，-CH2F，-CHF2，-CF3，-C（O）OH或-C（O） R 7是H，烷基，烯基，羟基烷基，环烷基，烷氧基烷基，氨基烷基，（R 17 - 苯基）烷基或-CH 2 -C（O）-O-烷基; 和R8包括烷基，杂芳基，苯基或环烷基，或杂环烷基，全部任意取代，或环烷基 - 或杂环烷基取代的酰胺; 或R 7和R 8，并且与它们相连的氮一起形成任选取代的环; 其余变量如本说明书中所定义。 还要求保护的是药物组合物，化合物作为PDE4抑制剂的用途，以及与其它活性物质的组合。

    Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors
    2.
    发明申请
    Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors 失效
    用作PDE4抑制剂的取代的2-喹啉基 - 恶唑

    公开(公告)号：US20060106062A1

    公开(公告)日：2006-05-18

    申请号：US11130359

    申请日：2005-05-16

    申请人： Rongze Kuang ,  David Blythin ,  Neng-Yang Shih ,  Ho-Jane Shue ,  Xiao Chen ,  Jianhua Cao ,  Danlin Gu ,  Ying Huang ,  John Schwerdt ,  Pauline Ting ,  Shing-Chun Wong ,  Li Xiao

    发明人： Rongze Kuang ,  David Blythin ,  Neng-Yang Shih ,  Ho-Jane Shue ,  Xiao Chen ,  Jianhua Cao ,  Danlin Gu ,  Ying Huang ,  John Schwerdt ,  Pauline Ting ,  Shing-Chun Wong ,  Li Xiao

    IPC分类号： A61K31/4709 ,  C07D417/02 ,  C07D413/02 ,  C07D43/02

    CPC分类号： C07D405/14 ,  C07D401/04 ,  C07D405/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

    摘要： The invention claims compounds of the formula wherein is a 5-membered heteroaryl; X is S or O; R1 is H, alkyl, cycloalkyl, cylcoalkylalkyl-, —CH2F, —CHF2, —CF3, —C(O)alkyl or —C(O)NR18R19; R3 and R4H, alkyl, hydroxyalkyl or —C(O)Oalkyl; R5 and R6 are H, alkyl, hydroxyalkyl, alkoxyalkyl, mercaptoalkyl, —CH2F, —CHF2, —CF3, —C(O)OH or —C(O)Oalkyl; R7 is H, alkyl, alkenyl, hydroxyalkyl, cycloalkyl, alkoxyalkyl, aminoalkyl, (R17-phenyl)alkyl or —CH2—C(O)—O-alkyl; and R8 comprises alkyl, heteroaryl, phenyl or cycloalkyl, or heterocycloalkyl, all optionally substituted, or a cycloalkyl- or heterocycloalkyl-substituted amide; or R7 and R8 and the nitrogen to which they are attached together form an optionally substituted ring; and the remaining variables are as defined in the specification. Also claimed are pharmaceutical compositions, the use of the compounds as PDE4 inhibitors, and combinations with other actives.

    摘要翻译： 本发明要求具有下式的化合物其中是5元杂芳基; X是S或O; R 1是H，烷基，环烷基，环烷基烷基 - ，-CH 2 F，-CHF 2，-CF 3， -C（O）烷基或-C（O）NR 18 R 19; R 3和R 4 H，烷基，羟烷基或-C（O）O烷基; R 5和R 6是H，烷基，羟基烷基，烷氧基烷基，巯基烷基，-CH 2 F 2，-CHF 2， -CF 3，-C（O）OH或-C（O）O烷基; R 7是H，烷基，烯基，羟基烷基，环烷基，烷氧基烷基，氨基烷基，（R 17 - 苯基）烷基或-CH 2 - C（O）-O-烷基; 和R 8包括烷基，杂芳基，苯基或环烷基，或杂环烷基，全部被取代，或环烷基 - 或杂环烷基取代的酰胺; 或R 7和R 8和它们所连接的氮一起形成任选取代的环; 其余变量如本说明书中所定义。 还要求保护的是药物组合物，化合物作为PDE4抑制剂的用途，以及与其它活性物质的组合。

    Selective neurokinin antagonists
    8.
    发明授权
    Selective neurokinin antagonists 失效
    选择性神经激肽拮抗剂

    公开(公告)号：US06635630B2

    公开(公告)日：2003-10-21

    申请号：US10163663

    申请日：2002-06-06

    申请人： Neng-Yang Shih ,  Ho-Jane Shue ,  Gregory A. Reichard ,  Sunil Paliwal ,  David J. Blythin ,  John J. Piwinski ,  Dong Xiao ,  Xiao Chen

    发明人： Neng-Yang Shih ,  Ho-Jane Shue ,  Gregory A. Reichard ,  Sunil Paliwal ,  David J. Blythin ,  John J. Piwinski ,  Dong Xiao ,  Xiao Chen

    IPC分类号： A61K31330

    CPC分类号： C07D239/10 ,  C07C45/71 ,  C07C217/48 ,  C07D211/58 ,  C07D233/14 ,  C07D233/16 ,  C07D233/22 ,  C07D233/30 ,  C07D233/32 ,  C07D233/42 ,  C07D233/46 ,  C07D233/48 ,  C07D233/78 ,  C07D285/10 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D409/06 ,  C07D413/04 ,  C07D413/06 ,  C07D413/10 ,  C07F9/6506 ,  C07C47/575

    摘要： Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl; X1 is —O—, —S—, —SO—, —SO2—, —NR12—, —NCOR12— or —NR12SO2R15;  is selected from the group consisting of X2 is —O—, —S— or —NR5—; Y is ═O, ═S or ═NR11; Y1 is H, C1-C6 alkyl, —NR17R13, —SCH3, R19-aryl(CH2)n6—, R19-heteroaryl-(CH2)n6—, —(CH2)n6—heterocycloalkyl, —(C1-C3)alkyl-NH—C(O)O(C1-C6)alkyl or —NHC(O)R15; R5 is H or —(CH2)n1—G, wherein n1 is 0-5, G is H, —CF3, —CHF2, —CH2F, —OH, —O—(C1-C6 alkyl), —SO2R13, —O—(C3-C8 cycloalkyl), —NR13R14, —SO2NR13R14, —NR13SO2R15, —NR13COR12, —NR12(CONR13R14), —CONR13R14, —COOR12, C3-C8 cycloalkyl, R19-aryl, R19-heteroaryl, and provided when n1=0, G is not H; R1, R2, R3 and R7 are H, alkyl, cycloalkyl, —CHF2, —CH2F or —CF3; or R1 and R2, together with the carbon to which they are attached, form an alkylene ring; or R1 and R2 together are ═O; R6 is R7 or —OH; and the remaining variables are as defined in the specification, methods of treating diseases susceptible to treatment with neurokinin antagonists with said compounds, and pharmaceutical compositions comprising said compounds are disclosed. Also disclosed are pharmaceutical compositions comprising an effective amount of a compound of claim 1, at least one pharmaceutically acceptable carrier, and in combination with an effective amount of a selective serotonin reuptake inhibitor.

    摘要翻译： 由结构式表示的化合物或其药学上可接受的盐，其中Ar 1和Ar 2是任选取代的杂芳基或任选取代的苯基; X 1是-O - ， - S - ， - SO-，-SO 2 - ，-NR 12 - ， - NR C 12 - 或-NR 12 SO 2 R 15选自X 2是-O - ， - S-或-NR 5 - ; Y是= O，= S或= NR 11; Y 1是H，C 1 -C 6烷基，-NR 17 R 13，-SCH 3，R 19 - 芳基（CH 2）n6 - （CH 2）n6 - ， - （CH 2）n 6-杂环烷基， - （C 1 -C 3）烷基-NH-C（O）O（C 1 -C 6）烷基或-NHC（O） R 15; R 5是H或 - （CH 2）n1-G，其中n1是0-5，G是H，-CF 3，-CHF 2，-CH 2 F，-OH，-O-（C 1 -C 6 烷基），-SO 2 R 13，-O-（C 3 -C 8环烷基），-NR 13 R 14，-SO 2 NR 13 R 14，-NR 13 SO 2 R 15， NR 13 R 12，-NR 12（CONR 13 R 14），-CONR 13 R 14，-COOR 12，C 3 -C 8环烷基，R 19 芳基，R 19 - 杂芳基，并且当n 1 = 0时，G不为H; R 1，R 2，R 3和R 7为H，烷基，环烷基，-CHF 2 ，-CH2F或-CF3; 或R 1和R 2与它们所连接的碳一起形成亚烷基环; 或R 1和R 2一起为= O; R 6为R 7或-OH;其余变量如本说明书中所定义，治疗易受神经激肽拮抗剂治疗的疾病的方法， 所述化合物和包含所述化合物的药物组合物。还公开了药物组合物，其包含有效量的权利要求1的化合物，至少一种药学上可接受的载体，并与有效量的选择性5-羟色胺再摄取抑制剂组合。