Thienopyridine derivatives useful in treating gastric ulcers
    1.
    发明授权
    Thienopyridine derivatives useful in treating gastric ulcers 失效
    可用于治疗胃溃疡的噻吩并吡啶衍生物

    公开(公告)号:US4839365A

    公开(公告)日:1989-06-13

    申请号:US191057

    申请日:1988-05-06

    IPC分类号: C07D495/04

    CPC分类号: C07D495/04

    摘要: A compound of the formula: ##STR1## (wherein R.sup.1 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkoxycarbonyl, or trifluoromethyl; R.sup.2 is hydrogen, C.sub.1 -C.sub.5 alkoxycarbonyl, C.sub.6 -C.sub.12 aryloxycarbonyl, C.sub.1 -C.sub.5 alkanoyloxy-C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxycarbonyloxy-C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 acylamino-C.sub.1 -C.sub.5 alkyl, 2-hydroxy-1-C.sub.2 -C.sub.5 alkenyl, phthalimido-C.sub.1 -C.sub.5 alkyl, halogeno-C.sub.1 -C.sub.5 alkoxycarbonyl-C.sub.1 -C.sub.5 alkyl, hydroxy-C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkylthio-C.sub.1 -C.sub.5 alkyl, or C.sub.1 -C.sub.5 alkylsulfinyl-C.sub.1 -C.sub.5 alkyl; ##STR2## m is an integer of 0 or 1; R.sup.3 and R.sup.4 each is hydrogen, halogen, cyano, C.sub.1 -C.sub.5 alkyl, amino, C.sub.1 -C.sub.5 alkoxy, C.sub.6 -C.sub.12 aryl-C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkoxycarbonyl, fluoro-C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkanoylamino, or carbamoyl) or its salt, being useful as antiulcer agents, is provided.

    9-(Substituted thio)-4H-pyrido[1,2,-A]pyrimidin-4-one derivatives
    2.
    发明授权
    9-(Substituted thio)-4H-pyrido[1,2,-A]pyrimidin-4-one derivatives 失效
    9-(取代的硫代)-4H-吡啶并[1,2-a]嘧啶-4-酮衍生物

    公开(公告)号:US4840953A

    公开(公告)日:1989-06-20

    申请号:US206665

    申请日:1988-06-15

    IPC分类号: C07D471/04

    CPC分类号: C07D471/04

    摘要: 9-(Substituted thio)-4H-pyrido[1,2-a]pyrimidin-4-one derivatives of the formula: ##STR1## wherein n is 0 or 1, R is --COR.sup.1, --CONR.sup.4 R.sup.5 or --CH.sub.2 R.sup.6, R.sup.1 is C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl, allythio, styryl, phenoxymethyl, thienylmethyl, C.sub.6 -C.sub.10 aryl optionally substituted, benzyl optionally substituted or 5- or 6-membered heterocyclic group optionally substituted, R.sup.2 and R.sup.3 each is hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.5 alkoxycarbonyl or benzyloxycarbonyl optionally substituted, R.sup.4 and R.sup.5 each is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl optionally substituted, and R.sup.8 is pyridyl or phenyl optionally substituted) being useful as antiulcer agents are provided through several routes.

    摘要翻译: 9-(取代的硫代)-4H-吡啶并[1,2-a]嘧啶-4-酮衍生物其中n为0或1,R为-COR 1,-CONR 4 R 5或-CH 2 R 6 R1是C1-C5烷基,C3-C7环烷基,烯硫基,苯乙烯基,苯氧基甲基,噻吩基甲基,任选取代的C 6 -C 10芳基,任选取代的苄基,或任选被取代的5或6元杂环基,R 2和R 3各自是氢, C 1 -C 5烷基,羧基,C 2 -C 5烷氧基羰基或任选取代的苄氧基羰基,R 4和R 5各自为氢,C 1 -C 5烷基,C 3 -C 7环烷基或任选取代的苯基,R 8为任选取代的吡啶基或苯基)可用作抗溃疡剂 代理商通过几条路线提供。

    Thioethylamide derivatives
    4.
    发明授权
    Thioethylamide derivatives 失效
    硫代乙酰胺衍生物

    公开(公告)号:US4318858A

    公开(公告)日:1982-03-09

    申请号:US212222

    申请日:1980-12-02

    摘要: A compound of the formula: ##STR1## [wherein R is dimethylamino or 1-pyrrolidinyl;R.sup.1 and R.sup.2 each is hydrogen or C.sub.1 -C.sub.3 alkyl;R.sup.3 is hydrogen, C.sub.1 -C.sub.3 alkyl (optionally substituted by one member selected from the group consisting of cyano, C.sub.1 -C.sub.3 alkoxy, phenyl, and 5- or 6-membered heterocyclic group), C.sub.3 -C.sub.6 cycloalkyl, C.sub.2 -C.sub.5 alkenyl (optionally substituted by one member selected from the group consisting of C.sub.1 -C.sub.3 alkoxy, phenyl, and phenoxy), C.sub.6 -C.sub.10 aryl (optionally substituted by one or two members selected from the group consisting of hydroxy, halogen, nitro, sulfamoyl, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkanoyl, C.sub.2 -C.sub.4 alkoxycarbonyl, C.sub.2 -C.sub.4 dialkylamino, and C.sub.1 -C.sub.3 alkanesulfonyl), or 5- or 6-membered heterocyclic group (optionally substituted by one member selected from the group consisting of oxo, halogen, C.sub.1 -C.sub.3 alkyl, and C.sub.1 -C.sub.3 alkoxy);and X is oxygen or sulfur]and its pharmaceutically acceptable acid addition salts is useful as histamine H.sub.2 blockers.

    摘要翻译: 下式的化合物:其中R是二甲基氨基或1-吡咯烷基; R1和R2各自为氢或C1-C3烷基; R 3是氢,C 1 -C 3烷基(任选地被选自氰基,C 1 -C 3烷氧基,苯基和5-或6-元杂环基中的一个取代),C 3 -C 6环烷基,C 2 -C 5烯基( 任选地被选自C 1 -C 3烷氧基,苯基和苯氧基的一个取代基取代),C 6 -C 10芳基(任选被一个或两个选自羟基,卤素,硝基,氨磺酰基,C1- C 3烷基,C 1 -C 3烷氧基,C 1 -C 3烷酰基,C 2 -C 4烷氧基羰基,C 2 -C 4二烷基氨基和C 1 -C 3烷磺酰基)或5或6元杂环基(任选被一个选自 的氧代,卤素,C 1 -C 3烷基和C 1 -C 3烷氧基); 并且X是氧或硫],其药学上可接受的酸加成盐可用作组胺H2阻断剂。