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42 条记录 (耗时 0.018 秒)

    10, 11-methanodibenzosuberane derivatives
    3.
    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。

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

    Disubstituted xanthone carboxylic acid compounds
    6.
    发明授权
    Disubstituted xanthone carboxylic acid compounds 失效
    二取代的呫吨酮羧酸化合物

    公开(公告)号：US3963753A

    公开(公告)日：1976-06-15

    申请号：US558023

    申请日：1975-03-13

    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

    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-Methyl-sulfinyl-7-isopropoxyxanthone-2-carboxylic acid and 5,7-di(methylsulfinyl)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-甲基亚磺酰基-7-异丙氧基呫吨酮-2-羧酸和5,7-二（甲基亚磺酰基）呫吨酮-2-羧酸作为代表性化合物。

    Novel substituted xanthone carboxylic acid compounds
    7.
    发明授权
    Novel substituted xanthone carboxylic acid compounds 失效
    新型取代的呫吨酮羧酸化合物

    公开(公告)号：US3949084A

    公开(公告)日：1976-04-06

    申请号：US543390

    申请日：1975-01-23

    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： C07C65/24 ,  C07D311/86 ,  A61K31/35

    CPC分类号： C07C65/24 ,  C07D311/86

    摘要： Compositions containing and methods employing, as the essential ingredient, novel substituted 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. 6-Acetylxanthone-2-carboxylic acid is illustrated as a representative compound.

    摘要翻译： 含有可用于治疗过敏症状的新型取代的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。 6-乙酰呫吨酮-2-羧酸被示为代表性化合物。