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42 条记录 (耗时 0.033 秒)

    (2-oxo-1,2,3,5-tetrahydroimidazo[2,1-b]quinoazolinyl)oxyalkylamides, compositions and the use thereof
    1.
    发明授权
    (2-oxo-1,2,3,5-tetrahydroimidazo[2,1-b]quinoazolinyl)oxyalkylamides, compositions and the use thereof 失效

    公开(公告)号：US4663320A

    公开(公告)日：1987-05-05

    申请号：US744100

    申请日：1985-06-11

    申请人： Gordon H. Jones ,  Michael C. Venuti ,  Robert Alvarez ,  John J. Bruno ,  Jurg R. Pfister

    发明人： Gordon H. Jones ,  Michael C. Venuti ,  Robert Alvarez ,  John J. Bruno ,  Jurg R. Pfister

    IPC分类号： C07C205/37 ,  C07C205/44 ,  C07C205/56 ,  C07D209/08 ,  C07D215/08 ,  C07D217/06 ,  C07D295/185 ,  C07D487/04 ,  A61K31/55 ,  A61K31/505 ,  C07D213/08 ,  C07D213/14

    CPC分类号： C07D295/185 ,  C07C205/37 ,  C07C205/44 ,  C07C205/56 ,  C07D209/08 ,  C07D215/08 ,  C07D217/06 ,  C07D487/04

    摘要： Compounds according to the formula ##STR1## an optical isomer thereof, or a pharmaceutically acceptable acid addition salt thereof wherein:n is an integer of 1 to 6;R.sub.1 is hydrogen or alkyl of 1 to 4 carbons;R.sub.2 is hydrogen or R.sub.1 and R.sub.2 are combined to form an oxo group;R.sub.3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl, hydroxy lower alkyl or an aliphatic acylate thereof of 1 to 6 carbon atoms or an aryl acylate thereof of 7 to 12 carbon atoms, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl of an .alpha.-amino acid side chain;R.sub.4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl;Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy;A is NR.sub.5 R.sub.6 wherein R.sub.5 and R.sub.6 are independently selected from the group consisting of: hydrogen; alkyl of 1 to 6 carbon atoms; hydroxyalkyl of 1 to 6 carbon atoms or an aliphatic acylate thereof of 1 to 6 carbon atoms or an aryl acrylate thereof of 7 to 12 carbon atoms; cycloalkyl of 3 to 8 carbon atoms or cycloalkyl lower alkyl of 4 to 12 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, --OH, --OCOR.sub.7, halo, --NH.sub.2, --N(R.sub.7).sub.2, --NHCOR.sub.7, --COOH, or --COO(R.sub.7) group wherein R.sub.5 is lower alkyl; and phenyl or phenyl lower alkyl wherein phenyl is unsubstituted or substituted with at least one lower alkyl, halo or lower alkoxy group or an --NH.sub.2, --N(R.sub.7).sub.2, --NHCOR.sub.7, --COOH, or --COOR.sub.7 group wherein R.sub.7 is lower alkyl; or wherein R.sub.5 and R.sub.6 are combined to form a compound selected from the group consisting of: morpholinyl; piperidinyl; perhexylenyl; N-loweralkylpiperazinyl; pyrrolidinyl; tetrahydroquinolinyl; tetrahydroisoquinolinyl; (.+-.)-decahydroquinolinyl and indolinyl. These compounds are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic agents and the like in mammals. The compounds also have inotropic and anti-metastatic activities.

    Anticholinergic bronchodilators
    5.
    发明授权
    Anticholinergic bronchodilators 失效
    抗胆碱能支气管扩张剂

    公开(公告)号：US4353922A

    公开(公告)日：1982-10-12

    申请号：US243674

    申请日：1981-03-13

    申请人： Jurg R. Pfister

    发明人： Jurg R. Pfister

    IPC分类号： C07D303/36 ,  C07D487/08 ,  A61K31/40

    CPC分类号： C07D487/08 ,  C07D303/36 ,  Y10S514/826

    摘要： Compounds of the formula ##STR1## wherein the serrated lines denote both endo and exo forms; R.sub.1 and R.sub.2 are the same or different and are C.sub.1 to C.sub.6 alkyl, C.sub.5 or C.sub.6 cycloalkyl, C.sub.5 or C.sub.6 cycloalkenyl, phenyl optionally substituted with C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy or halo, or 5 or 6 membered heterocyclic aryl wherein the heteroatom is oxygen, nitrogen or sulfur; R.sub.3 is a C.sub.1 to C.sub.6 alkyl radical; R.sub.4 and X are optionally present, and when present R.sub.4 is a C.sub.1 to C.sub.6 alkyl radical or hydrogen and X is an inorganic or organic anion which forms a pharmaceutically acceptable salt. Methods for preparing these compounds are also disclosed. The compounds of the present invention are useful as anticholinergic agents.

    摘要翻译： 式“IMAGE”的化合物，其中锯齿状线表示内部和外部形式; R1和R2相同或不同，为C1至C6烷基，C5或C6环烷基，C5或C6环烯基，任选被C1至C6烷基取代的苯基，C1至C6烷氧基或卤素，或5或6元杂环芳基，其中 杂原子是氧，氮或硫; R3是C1-C6烷基; R4和X任选存在，当存在时R4是C1-C6烷基或氢，X是形成药学上可接受的盐的无机或有机阴离子。 还公开了制备这些化合物的方法。 本发明的化合物可用作抗胆碱剂。

    Disubstituted xanthone-2-carboxylic acid antiallergy agents
    6.
    发明授权
    Disubstituted xanthone-2-carboxylic acid antiallergy agents 失效
    二取代的呫吨酮-2-羧酸抗过敏剂

    公开(公告)号：US4217361A

    公开(公告)日：1980-08-12

    申请号：US908312

    申请日：1978-05-22

    申请人： Jurg R. Pfister

    发明人： Jurg R. Pfister

    IPC分类号： C07D311/86 ,  A61K31/35

    CPC分类号： C07D311/86

    摘要： Compositions containing and methods employing, as the essential ingredient, novel substituted xanthone-2-carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed.

    摘要翻译： 含有可用于治疗过敏症状的新型取代的呫吨酮-2-羧酸化合物作为必需成分的组合物和方法。 还公开了制备这些化合物及其组合物和中间体的方法。

    Method of use of, and compositions containing, disubstituted xanthone carboxylic acid compounds
    7.
    发明授权
    Method of use of, and compositions containing, disubstituted xanthone carboxylic acid compounds 失效
    使用方法和含有二取代的呫吨酮羧酸化合物的组合物

    公开(公告)号：US3951618A

    公开(公告)日：1976-04-20

    申请号：US542477

    申请日：1975-01-20

    申请人： Jurg R. Pfister ,  Ian T. Harrison ,  John H. Fried

    发明人： Jurg R. Pfister ,  Ian T. Harrison ,  John H. Fried

    IPC分类号： C07D311/86 ,  A61K31/35

    CPC分类号： C07D311/86

    摘要： Compositions containing and methods employing, as the essential ingredient, novel disubstituted xanthone carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed. 5-Methylthio-7-isopropoxyxanthone-2-carboxylic acid and 5,7-di-(methylthio)xanthone-2-carboxylic acid are illustrated as representative compounds.

    摘要翻译： 含有可用于治疗过敏症状的新型二取代呫吨酮羧酸化合物作为必需成分的组合物和方法。 还公开了制备这些化合物及其组合物和中间体的方法。 5-甲硫基-7-异丙氧基呫吨酮-2-羧酸和5,7-二（甲硫基）呫吨酮-2-羧酸作为代表性化合物。

    10, 11-methanodibenzosuberane derivatives
    10.
    发明授权
    10, 11-methanodibenzosuberane derivatives 失效
    10,11-甲烷二苯并三唑衍生物

    公开(公告)号：US5889007A

    公开(公告)日：1999-03-30

    申请号：US436992

    申请日：1995-05-08

    申请人： Jurg R. Pfister ,  Doris L. Slate

    发明人： Jurg R. Pfister ,  Doris L. Slate

    IPC分类号： C07D295/08 ,  A61K31/495 ,  A61P33/02 ,  A61P35/00 ,  C07D213/65 ,  C07D215/20 ,  C07D215/26 ,  C07D271/12 ,  C07D295/092 ,  C07D401/12 ,  C07D413/12 ,  A61K31/50

    CPC分类号： C07D295/088 ,  C07D213/65 ,  C07D215/20 ,  C07D215/26 ,  C07C2103/40

    摘要： 10,11-Methanodibenzosuberane derivatives, i.e., the compounds of Formula I: ##STR1## wherein: A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHR.sup.a --CH.sub.2 --, or --CH.sub.2 --CHR.sup.a --CHR.sup.b --CH.sub.2 --, where one of R.sup.a or R.sup.b is H, OH, or lower acyloxy, and the other is H;R.sup.1 is H, P, Cl or Br;R.sup.2 is H, F, Cl or Br; andR.sup.3 is heteroaryl or phenyl optionally substuted with F, Cl, Br, CF.sub.3, CN, NO.sub.2 or OCHF.sub.2 ;and the pharmaceutically acceptable salts thereof, are useful chemosensitizing agents, e.g., for cancer chemotherapy, particularly for treating multidrug resistance.

    摘要翻译： 10,11-甲烷二苯并环烷衍生物，即式I的化合物：其中：A是-CH 2 -CH 2 - ， - CH 2 -CHR a -CH 2 - 或-CH 2 -CHR a -CHR b -CH 2 - ，其中 Ra或Rb之一是H，OH或低级酰氧基，另一个是H; R1是H，P，Cl或Br; R2是H，F，Cl或Br; 并且R 3是杂芳基或任选被F，Cl，Br，CF 3，CN，NO 2或OCHF 2取代的苯基; 和其药学上可接受的盐是有用的化学敏化剂，例如用于癌症化疗，特别是用于治疗多药耐药性。