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    • 5. 发明公开
    • Derivatives of Alpha-alkyl polyolefinic compounds useful in the treatment of psoriasis
    • 用于治疗PSORIASIS的ALPHA-ALKYL POLYOLEFINIC化合物的衍生物
    • EP0137155A3
    • 1985-12-18
    • EP84108432
    • 1984-07-17
    • USV PHARMACEUTICAL CORPORATION
    • Loev, BernardJones, HowardChan, Wan-kit
    • C07C175/00A61K31/07
    • C07C403/16C07C43/23C07C403/02C07C403/08C07C403/10C07C403/12C07C403/18C07C403/22C07C2601/16
    • The present invention relates to novel a-alkyl polyolefinic compounds and to pharmaceuticals containing said compounds. The pharmaceuticals are useful for the treatment of psoriasis. The a-alkyl polyolefinic compounds have the structure
      wherein
      n is 0 to 3; R, and R 4 are each independently hydrogen or an alkyl group of from 1 to 5 carbon atoms; R 2 is an alkyl group of from 1 to 5 carbon atoms; R 3 is H, C 1 -C 5 alkyl, cyclo C 3 -C 7 alkyl, C 2 -C 5 alkenyl, cyclo C 3 -C 7 alkenyl, aryl, hydroxy, C 1 -C 5 alkoxy, aryloxy, arylalkoxy, formyl, C 1 -C 6 alkylcarbonyl, C 2 -C 5 alkenylcarbonyl, arylcarbonyl, aryl C 1 -C 5 alkylcarbonyl, aryl C 2 -C 5 alkenylcarbonyl, NR 6 R 5 , SR 5 ,
      retinyloxy, retinoyl, retinoyloxy, or
      R 6 is H, C 1 -C 20 alkyl, aryl, aralkyl; and Z is a cycloalkyl, cycloalkenyl or cycloalkadienyl group substituted with from 0 to 5 alkyl groups, a keto group or a hydroxyl group, or a phenyl group substituted with from 0 to 4 hydroxy, alkoxy, alkyl or trifluoromethyl groups or halogen atoms or combinations thereof; and the pharmaceutically- acceptable salts thereof.
    • 本发明涉及新的α-烷基聚烯烃化合物和含有所述化合物的药物。 这些药物可用于治疗牛皮癣。 α-烷基聚烯烃化合物具有以下结构:其中... n为0至3; R 1至R 4各自独立地为氢或1至5个碳原子的烷基; R 2为 1至5个碳原子; R3是H,C1-C5烷基,环C3-C7烷基,C2-C5烯基,环C3-C7链烯基,芳基,羟基,C1-C5烷氧基,芳氧基,芳基烷氧基,甲酰基,C1- C6烷基羰基,C2-C5烯基羰基,芳基羰基,芳基C1-C5烷基羰基,芳基C2-C5烯基羰基,NR5R5,SR5,...... -O-@-R5,...视黄酰基,视黄酰氧基或... H,C 1 -C 20烷基,芳基,芳烷基; Z是被0-5个烷基,酮基或羟基取代的环烷基,环烯基或环二烯基,或被0至4个羟基,烷氧基,烷基或三氟甲基或卤素原子取代的苯基或 其组合; 及其药学上可接受的盐。
    • 6. 发明公开
    • Benzoxazole and benzothiazole derivatives with anti-allergic activity
    • 苯并恶唑和苯并噻唑衍生物抗逆转录酶Wirkung。
    • EP0039919A1
    • 1981-11-18
    • EP81103497.4
    • 1981-05-07
    • USV PHARMACEUTICAL CORPORATION
    • Brown, Richard E.Georgiev, Vasil St.Loev, Bernard
    • A61K31/42A61K31/425C07D263/58C07D277/68C07D413/12C07D498/04C07D513/04
    • C07D263/58C07D265/36C07D277/68
    • An anti-allergic compound of the formula:
      wherein,

      X is S or O R 1 and R 2 are each H, R 3 , OR 4 , halogen, cyano, COOR 4 , methanesulfonyl, nitro, trifluoromethyl or taken together, methylenedioxy, wherein R 3 is loweralkyl orcycloalkyl of 3 to 7 carbon atoms and R 4 is hydrogen or lower alkyl; and
      R is -Z-O-R 3 ; -Z-N(R 5 R 6 ); Z 1 -O-Z 2 -N(R 5 R 6 ); -Z- heterocycle; -Z 1 -O-Z 2 -heterocycle; or-Z-O-C 6 H 4 R 1 wherein each of R 5 and R 6 are hydrogen or lower alkyl, or when taken together with the nitrogen to which they are attached R 5 and R 6 form a nitrogen-heterocyclic ring, R 1 and R 3 have the meaning hereinbefore described, and Z,Z 1 and Z 2 are each branched or unbranched alkylene chain containing from 2 to about 6 carbon atoms in the principal chain and a total of up to about 12 carbon atoms; Z 1 and Z 2 when taken together with a hetero atom form a saturated heterocyclic ring; and heterocycle represents a heterocyclic ring containing one or more of the hetero atoms, oxygen, nitrogen and sulfur and acid addition and conjugate salts thereof.
    • 一种下式的抗过敏化合物:其中,... X为S或O ... R 1和R 2各自为H,R 3,OR 4,卤素,氰基,COOR 4,甲磺酰基,硝基,三氟甲基或一起取代亚甲二氧基 其中R3是3-7个碳原子的低级烷基或环烷基,R4是氢或低级烷基; 和... R是-Z-O-R3; -Z-N(R 5 R 6); ž<1> -O-Z <2> -N(R 5 R 6); -Z-杂环; -Z <1> -O-Z <2> - 杂环; 或-ZO-C 6 H 4 R 1,其中R 5和R 6各自为氢或低级烷基,或者当与其连接的氮一起连接时,R 5和R 6形成氮杂环,R 1和R 3具有上述含义,Z Z 1和Z 2分别是在主链中含有2至约6个碳原子且总共至多约12个碳原子的支链或非支链亚烷基链; Z 1和Z 2与杂原子一起形成饱和杂环; 杂环表示含有一个或多个杂原子,氧,氮和硫及其酸加成和共轭盐的杂环。
    • 9. 发明公开
    • Derivatives of Alpha-alkyl polyolefinic compounds useful in the treatment of psoriasis
    • α-烷基 - 聚烯烃衍生的银屑病银屑病。
    • EP0137155A2
    • 1985-04-17
    • EP84108432.0
    • 1984-07-17
    • USV PHARMACEUTICAL CORPORATION
    • Loev, BernardJones, HowardChan, Wan-kit
    • C07C175/00A61K31/07
    • C07C403/16C07C43/23C07C403/02C07C403/08C07C403/10C07C403/12C07C403/18C07C403/22C07C2601/16
    • The present invention relates to novel a-alkyl polyolefinic compounds and to pharmaceuticals containing said compounds. The pharmaceuticals are useful for the treatment of psoriasis. The a-alkyl polyolefinic compounds have the structure
      wherein

      n is 0 to 3;
      R, and R 4 are each independently hydrogen or an alkyl group of from 1 to 5 carbon atoms;
      R 2 is an alkyl group of from 1 to 5 carbon atoms;
      R 3 is H, C 1 -C 5 alkyl, cyclo C 3 -C 7 alkyl, C 2 -C 5 alkenyl, cyclo C 3 -C 7 alkenyl, aryl, hydroxy, C 1 -C 5 alkoxy, aryloxy, arylalkoxy, formyl, C 1 -C 6 alkylcarbonyl, C 2 -C 5 alkenylcarbonyl, arylcarbonyl, aryl C 1 -C 5 alkylcarbonyl, aryl C 2 -C 5 alkenylcarbonyl, NR 6 R 5 , SR 5 ,
      retinyloxy, retinoyl, retinoyloxy, or

      R 6 is H, C 1 -C 20 alkyl, aryl, aralkyl; and
      Z is a cycloalkyl, cycloalkenyl or cycloalkadienyl group substituted with from 0 to 5 alkyl groups, a keto group or a hydroxyl group, or a phenyl group substituted with from 0 to 4 hydroxy, alkoxy, alkyl or trifluoromethyl groups or halogen atoms or combinations thereof; and the pharmaceutically- acceptable salts thereof.
    • 本发明涉及新的α-烷基聚烯烃化合物和含有所述化合物的药物。 这些药物可用于治疗牛皮癣。 α-烷基聚烯烃化合物具有以下结构:其中... n为0至3; R 1至R 4各自独立地为氢或1至5个碳原子的烷基; R 2为 1至5个碳原子; R3是H,C1-C5烷基,环C3-C7烷基,C2-C5烯基,环C3-C7链烯基,芳基,羟基,C1-C5烷氧基,芳氧基,芳基烷氧基,甲酰基,C1- C6烷基羰基,C2-C5烯基羰基,芳基羰基,芳基C1-C5烷基羰基,芳基C2-C5烯基羰基,NR5R5,SR5,...... -O-@-R5,...视黄酰基,视黄酰氧基或... H,C 1 -C 20烷基,芳基,芳烷基; Z为被0-5个烷基,酮基或羟基取代的环烷基,环烯基或环二烯基,或被0至4个羟基,烷氧基,烷基或三氟甲基或卤素原子取代的苯基或 其组合; 及其药学上可接受的盐。