Azole derivatives and anti-ulcerative composition containing same
    2.
    发明授权
    Azole derivatives and anti-ulcerative composition containing same 失效
    唑衍生物和含有其的抗溃疡组合物

    公开(公告)号:US5141946A

    公开(公告)日:1992-08-25

    申请号:US716622

    申请日:1991-06-14

    CPC分类号: C07D471/04 C07D513/04

    摘要: Compounds of the general formula (I): ##STR1## and pharmaceutically acceptable salts thereof, in whichA, B, C and D each represent --CH.dbd. or --N.dbd., with the proviso that at least one of them is --N.dbd.;X represents --NH--, --O-- or --S--;Y represents --(CH.sub.2).sub.p -- wherein p is an integer from 0 to 4, --C(CH.sub.3).sub.2 --, --CH.sub.2 CH.dbd.CH--, --CH.sub.2 CO--, --CF.sub.2 -- or --CH.sub.2 COCH.sub.2 --;R.sup.1 represents a hydrogen atom, a C.sub.1-4 alkyl group, a halogen atom or a C.sub.1-4 alkoxy group;R.sup.2 represnts a hydrogen atom, a hydroxyl group, a saturated or unsaturated C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a carboxyl group, a saturated or unsaturated C.sub.1-12 alkoxycarbonyl group which may be optionally substituted, a cycloalkoxycarbonyl group, a saturated or unsaturated five- or six-memebered heterocyclic group containing at least one nitrogen atom optionally with one or more nitrogen and/or oxygen atoms, which may be optionally condensed and/or substituted, --CONR.sup.3 R.sup.4, --NR.sup.3 R.sup.4, --OCOR.sup.3 or --NHCONHR.sup.3 wherein R.sup.3 and R.sup.4, which may be the same or different, represent a C.sub.1-6 alkyl group which may be optionally substituted or a cycloalkyl group, andm and n each represent an integrer from 0 to 2.The compounds are useful in treating ulcers.

    摘要翻译: 通式(I)的化合物:其中A,B,C和D各自表示-CH =或-N =,条件是其中至少一个为 -N =; X表示-NH-,-O-或-S-; Y表示 - (CH 2)p - ,其中p是0至4的整数,-C(CH 3)2 - , - CH 2 CH = CH - , - CH 2 CO - , - CF 2 - 或-CH 2 COCH 2 - R1表示氢原子,C1-4烷基,卤素原子或C1-4烷氧基; R2表示氢原子,羟基,饱和或不饱和的C1-6烷基,C1-6烷氧基,羧基,可以任意取代的饱和或不饱和的C 1-12烷氧基羰基,环烷氧基羰基, 含有至少一个氮原子的饱和或不饱和五元或六元杂环基团,任选具有一个或多个氮原子和/或氧原子,其可以任选地被缩合和/或取代,-CONR 3 R 4,-NR 3 R 4,-OCOR 3或 - NHCONHR 3其中R3和R4可以相同或不同,表示可以任选被取代的C 1-6烷基或环烷基,m和n各自表示0至2的整数。该化合物可用于处理 溃疡

    Azole derivatives and anti-ulcerative composition containing same
    3.
    发明授权
    Azole derivatives and anti-ulcerative composition containing same 失效
    唑衍生物和含有其的抗溃疡组合物

    公开(公告)号:US5200407A

    公开(公告)日:1993-04-06

    申请号:US716621

    申请日:1991-06-14

    CPC分类号: C07D471/04 C07D513/04

    摘要: Compounds of the general formula (I): ##STR1## and pharmaceutically acceptable salts thereof, in which A, B, C and D each represent --CH.dbd. or --N.dbd., with the proviso that at least one of them is --N.dbd.;X represents --NH--, --O-- or --S--;Y represents --(CH.sub.2).sub.p -- wherein p is an integer from 0 to 4, --C(CH.sub.3).sub.2 --, --CH.sub.2 CH.dbd.CH--, --CH.sub.2 CO--, --CF.sub.2 -- or --CH.sub.2 COCH.sub.2 --;R.sup.1 represents a hydrogen atom, a C.sub.1-4 alkyl group, a halogen atom or a C.sub.1-4 alkoxy group;R.sup.2 represents a hydrogen atom, a hydroxyl group, a saturated or unsaturated C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a carboxyl group, a saturated or unsaturated C.sub.1-12 alkoxycarbonyl group which may be optionally substituted, a cycloalkoxycarbonyl group, a saturated or unsaturated five- or six-membered heterocyclic group containing at least one nitrogen atom optionally with one or more nitrogen and/or oxygen atoms, which may be optionally condensed and/or substituted, --CONR.sup.3 R.sup.4, --NR.sup.3 R.sup.4, --OCOR.sup.3 or --NHCONHR.sup.3 wherein R.sup.3 and R.sup.4, which may be the same or different, represent a C.sub.1-6 alkyl group which may be optionally substituted or a cycloalkyl group, andm and n each represent an integer from 0 to 2.

    摘要翻译: 通式(I)的化合物:其中A,B,C和D各自表示-CH =或-N =,条件是其中至少一个为 -N =; X表示-NH-,-O-或-S-; Y表示 - (CH 2)p - ,其中p是0至4的整数,-C(CH 3)2 - , - CH 2 CH = CH - , - CH 2 CO - , - CF 2 - 或-CH 2 COCH 2 - R1表示氢原子,C1-4烷基,卤素原子或C1-4烷氧基; R2表示氢原子,羟基,饱和或不饱和的C1-6烷基,C1-6烷氧基,羧基,可以任意取代的饱和或不饱和的C 1-12烷氧基羰基,环烷氧基羰基, 含有至少一个氮原子的饱和或不饱和五元或六元杂环基,任选具有一个或多个氮和/或氧原子,其可以任选地被缩合和/或取代,-CONR 3 R 4,-NR 3 R 4,-OCOR 3或 - NHCONHR 3其中R3和R4可以相同或不同,表示可以被任意取代的C 1-6烷基或环烷基,m和n各自表示0〜2的整数。

    Cephalosporin derivatives
    6.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号:US4785090A

    公开(公告)日:1988-11-15

    申请号:US704077

    申请日:1985-02-21

    摘要: This is a class of antibacterial compounds of the formula: ##STR1## wherein Y is straight or branched alkyl or alkenyl chain, cycloalkanomethyl of 3-6 carbon atoms, each group being optionally substituted by halogen, or a group ##STR2## wherein n is 0 or an integer of 1-3, A is a group --COR.sup.3 wherein R.sup.3 is hydroxy, a group ##STR3## wherein R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or alkyl of 1-5 carbon atoms, a group ##STR4## or a 5- or 6-membered heterocyclic group containing nitrogen and/or sulfur, and R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, alkyl of 1-5 carbon atoms, or R.sup.1 and R.sup.2 may be combined together to form cycloalkylidene of 3-5 carbon atoms, and Z is a group of the formula: ##STR5## wherein m is 0 or an integer of 3-5, R.sup.6 is hydrogen or alkyl of 1-3 carbon atoms, and R.sup.7, when m is an integer of 3-5, is alkyl of 1-5 carbon atoms, alkenyl, cyclopropyl, a group --(CH.sub.2).sub.p B wherein p is 0 or an integer of 1-3 and B is amino, alkyl-substituted amino, hydroxy, carboxy, carbamoyl, trifluoromethyl, sulfonic acid, sulfonic acid amide, alkylthio or cyano or, when m is 0, is alkyl of 1-5 carbon atoms, which may optionally be substituted by halogen, alkenyl, a group ##STR6## wherein R.sup.8 is hydrogen, alkyl of 1-4 carbon atoms or phenyl, or cyclopropyl, and a salt thereof.

    摘要翻译: 这是一类具有下式的抗菌化合物:其中Y是直链或支链烷基或烯基链,3-6个碳原子的环烷基甲基,每个基团任选被卤素取代,或基团< 其中n为0或1-3的整数,A为基团-COR 3,其中R 3为羟基,其中R 4和R 5可以相同或不同,为氢或1-5碳的烷基 原子,基团或含有氮和/或硫的5-或6-元杂环基,R 1和R 2可以相同或不同,为氢,1-5个碳原子的烷基或R1 并且R 2可以组合在一起形成3-5个碳原子的亚烷基,Z是下式的基团:其中m是0或3-5的整数,R6是氢或1-3个碳的烷基 原子和R 7,当m是3-5的整数时,是1-5个碳原子的烷基,烯基,环丙基,基团 - (CH 2)pB,其中p是0或1-3的整数,B是氨基 ,烷基取代的氨基 羟基,羧基,氨基甲酰基,三氟甲基,磺酸,磺酸酰胺,烷硫基或氰基,或当m为0时,其为1-5个碳原子的烷基,其可任选被卤素,链烯基,基团 其中R8是氢,1-4个碳原子的烷基或苯基,或环丙基及其盐。