知搜-全球专利检索

  1. 登录
  2. 注册

搜索结果

29 条记录 (耗时 0.039 秒)

    Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors
    2.
    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。

    Cyclic diesters of 4-hydroxy-1,3-benzenedimethanol and compositions and methods employing such compounds
    5.
    发明授权
    Cyclic diesters of 4-hydroxy-1,3-benzenedimethanol and compositions and methods employing such compounds 失效
    4-羟基-1,3-苯二甲醇的环状二酯和使用这些化合物的组合物和方法

    公开(公告)号：US5011845A

    公开(公告)日：1991-04-30

    申请号：US537385

    申请日：1990-06-13

    申请人： David J. Blythin ,  Ho-Jane Shue ,  Ashit K. Ganguly

    发明人： David J. Blythin ,  Ho-Jane Shue ,  Ashit K. Ganguly

    IPC分类号： C07D321/00 ,  C07D491/04 ,  C07D493/04 ,  C07D495/04

    CPC分类号： C07D491/04 ,  C07D321/00 ,  C07D493/04 ,  C07D495/04 ,  Y10S514/826

    摘要： Compounds of the formula ##STR1## wherein R.sup.5 represents C.sub.1 to C.sub.6 -alkyl or the group--(CH.sub.2).sub.n --Z--(CH.sub.2).sub.m --Ar wherein Z represents O, S or --CH.sub.2 --and Ar is phenyl, optionally substituted by one or two groups selected from the group consisting of hydrogen, C.sub.1 to C.sub.6 -alkyl, C.sub.1 to C.sub.6 -alkoxy, Cl,F,Br,I,NO.sub.2, CF.sub.3, CN, R.sup.6 -S(O).sub.x, R.sup.7 --CO--,(R.sup.8 R.sup.9)NCO-and phenyl, wherein x is 0, 1 or 2, and each R.sup.6, R.sup.7, R.sup.8 and R.sup.9 is independently C.sub.1 to C.sub.6 alkyl or two adjacent groups on Ar may form together an additional fused benzenoid ring; n and m independently represent integers of from 1 to 8; and ring Q represents one of the rings Q.sub.1, Q.sub.2, Q.sub.3 or Q.sub.4 below: ##STR2## X is N or C--R.sup.1 ; Y is N or C--R.sup.4 ;W represents O or S;each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently selected from hydrogen, C.sub.1 to C.sub.6 -alkyl, C.sub.1 to C.sub.6 -alkoxy, Cl,F,Br,I,NO.sub.2,CF.sub.3,CN, R.sup.10 -S(O).sub.y --, R.sup.11 --CO--, (R.sup.12 R.sup.13)N--CO--or phenyl, wherein y is 0, 1 or 2 and each of SR.sup.10, R.sup.11, R.sup.12 and R.sup.13 is independently C.sub.1 to C.sub.6 -alkyl, or, in the ring Q.sub.1, two adjacent groups, i.e. R.sup.1 R.sup.2, R.sup.2 R.sup.3 or R.sup.3 R.sup.4, may form together an additional fused benzenoid ring; and pharmaceutically acceptable acid addition salts of such compounds are described.These compounds provide favorable properties for the treatment of asthma and all types of chronic, obstructionary bronchopulmonary diseases.

    摘要翻译： 其中R 5表示C 1 -C 6 - 烷基或基团 - （CH 2）n Z-（CH 2）m-Ar的化合物，其中Z表示O，S或-CH 2 - ，Ar是任选被一个 或选自氢，C1至C6-烷基，C1至C6-烷氧基，C1，F，Br，I，NO2，CF3，CN，R6-S（O）x，R7-CO-， （R8R9）NCO-和苯基，其中x为0,1或2，并且每个R 6，R 7，R 8和R 9独立地为C 1 -C 6烷基或Ar上的两个相邻基团可以一起形成另外的稠合苯环; n和m独立地表示1至8的整数; 环Q表示下面的环Q1，Q2，Q3或Q4中的一个：X是N或C-R1; Y是N或C-R4; W表示O或S; R 1，R 2，R 3和R 4各自独立地选自氢，C 1至C 6 - 烷基，C 1至C 6 - 烷氧基，Cl，F，Br，I，NO 2，CF 3，CN，R 10 -S（O） R11-CO-，（R12R13）N-CO-或苯基，其中y为0,1或2，SR10，R11，R12和R13各自独立地为C1至C6-烷基，或在环Q1中，两个相邻 基团，即R1R2，R2R3或R3R4，可以一起形成另外的稠合苯环; 和这些化合物的药学上可接受的酸加成盐。 这些化合物为治疗哮喘和所有类型的慢性阻塞性支气管肺疾病提供了有利的特性。

    (17R)-Spiro-[androstane-17,1'-cyclobutan]-2'-ones, methods for their manufacture and intermediates useful therein
    8.
    发明授权
    (17R)-Spiro-[androstane-17,1'-cyclobutan]-2'-ones, methods for their manufacture and intermediates useful therein 失效
    （17R）-Siro- {8雄甾烷-17,1 {40-环丁烷{9-2 {40-酮，其制造方法和其中有用的中间体

    公开(公告)号：US3968132A

    公开(公告)日：1976-07-06

    申请号：US535387

    申请日：1974-12-23

    申请人： Michael J. Green ,  Ho-Jane Shue

    发明人： Michael J. Green ,  Ho-Jane Shue

    IPC分类号： C07J1/00 ,  C07J21/00 ,  C07J53/00 ,  C07J5/00

    CPC分类号： C07J53/001 ,  C07J1/0011 ,  C07J21/003 ,  C07J53/007

    摘要： (17R)-Spiro-[androstane-17,1'-cyclobutan]-2'-ones are prepared by the reaction of a 17-oxo androstane, wherein all other ketones are blocked, with a cyclopropylarylsulfide or with a cyclopropylarylsulfonium salt having a non-nucleophilic anion, in an organic solvent together with a strong base, followed by reaction in situ of the intermediate thereby formed with aqueous acid or water.Some (17R)-spiro-[androstan-17,1'-cyclobutan]-2'-ones are useful as intermediates in preparing (17R)-spiro-[3-oxo-4-androstene-17,1'-cyclobutan]-2'-ones which are aldosterone antagonists. Additionally, (17R)-spiro-[androstane-17,1'-cyclobutan]-2'-ones are useful as intermediates in preparing known 17.alpha.-pregnane-21,17.beta.-carbolactones, valuable aldosterone blocking agents.

    摘要翻译： （17R）-Siro- [雄甾烷-17,1'-环丁烷] -2'-酮通过与环丙基芳基硫醚或具有环丙基芳基锍盐的17-氧代雄甾烷（其中所有其它酮被封闭）的反应制备， 非亲核阴离子，在有机溶剂中与强碱一起，随后由中间体原位反应，由此与酸或水的水溶液形成。