Sodium salt of
4-oxo-10-(2,3-dimethylpentanamido)-4H-pyrimido[1,2-c]quinozoline-3-carbo
xylic acid
    2.
    发明授权
    Sodium salt of 4-oxo-10-(2,3-dimethylpentanamido)-4H-pyrimido[1,2-c]quinozoline-3-carbo xylic acid 失效
    4-氧代-10-(2,3-二甲基戊酰氨基)-4H-嘧啶并[1,2-c]喹唑啉-3-羧酸钠盐

    公开(公告)号:US4429126A

    公开(公告)日:1984-01-31

    申请号:US384998

    申请日:1982-06-04

    摘要: Quinazoline derivatives of the formulae: ##STR1## wherein A.sup.1 is ##STR2## A.sup.2 is ##STR3## R.sup.1 is hydrogen, carboxy or esterified carboxy, R.sub.a.sup.1 and R.sub.b.sup.1 are esterified carboxy,R.sup.2 and R.sup.3 are hydrogen, alkyl, halogen, nitro, amino, alkoxy, aryloxy, alkylthio, alkylpiperazinyl, acylamino or dialkylamino which may be substituted with hydroxy,R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy, dialkylamino or 2,2-dialkoxycarbonylvinylaminoR.sub.a.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy or dialkylamino,R.sup.5 is alkyl or alkenyl, andR.sup.6 is carboxy or esterified carboxy.

    摘要翻译: 喹啉衍生物,其结构式如下:其中A1是甲基,R1是氢,羧基或酯化的羧基,Ra1和Rb1是酯化的羧基,R2和R3是氢,烷基,卤素,硝基 ,可以被羟基取代的氨基,烷氧基,芳氧基,烷硫基,烷基哌嗪基,酰基氨基或二烷基氨基,R 4是氢,烷基,羟基,烷氧基,烯氧基,二烷基氨基或2,2-二烷氧基羰基乙烯基氨基R 4a是氢,烷基,羟基,烷氧基, 烯氧基或二烷基氨基,R 5是烷基或烯基,R 6是羧基或酯化的羧基。

    Quinazoline derivatives
    3.
    发明授权
    Quinazoline derivatives 失效
    喹唑啉衍生物

    公开(公告)号:US4543356A

    公开(公告)日:1985-09-24

    申请号:US455411

    申请日:1983-01-03

    摘要: This invention is directed to new quinazoline derivatives of the following formula having use in the treatment of symptoms associated with allergic manifestations. ##STR1## wherein R.sub.a.sup.1 and R.sub.b.sup.1 are C.sub.2 -C.sub.7 alkoxycarbonyl or R.sub.a.sup.1 and R.sub.b.sup.1 is linked together to form a group of the formula: ##STR2## R.sup.2 and R.sup.3 are hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, amino, C.sub.1 -C.sub.6 alkoxy, phenoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylpiperazinyl, C.sub.1 -C.sub.18 alkanoylamino, di(C.sub.1 -C.sub.6)alkanoylamino, C.sub.3 -C.sub.9 alkoxalylamino, C.sub.4 -C.sub.8 cycloalkylcarbonylamino, C.sub.3 -C.sub.7 cycloalkyl(C.sub.1 -C.sub.6)alkanoylamino, benzamido, phenyl(C.sub.1 -C.sub.6)alkanoylamino, C.sub.1 -C.sub.6 alkylsulfonylamino or di(C.sub.1 -C.sub.6)alkylamino which may be substituted with hydroxy,A.sup.1 is a group of the formula: ##STR3## in which R.sup.4 is hydrogen C.sub.1 -C.sub.6 alkyl, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkenyloxy, di(C.sub.1 -C.sub.6)alkylamino or 2,2-di(C.sub.1 -C.sub.6)alkoxycarbonylvinylamino, andR.sup.5 is C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkenyl,or pharmaceutically acceptable salt thereof.

    Tricyclic quinazoline derivatives
    4.
    发明授权
    Tricyclic quinazoline derivatives 失效
    三环喹唑啉衍生物

    公开(公告)号:US4377580A

    公开(公告)日:1983-03-22

    申请号:US210340

    申请日:1980-11-25

    摘要: Quinazoline derivatives of the formulae: ##STR1## wherein A.sup.1 is ##STR2## A.sup.2 is ##STR3## R.sup.1 is hydrogen, carboxy or esterified carboxy, R.sub.a.sup.1 and R.sub.b.sup.1 are esterified carboxy,R.sup.2 and R.sup.3 are hydrogen, alkyl, halogen, nitro, amino, alkoxy, aryloxy, alkylthio, alkylpiperazinyl, acylamino or dialkylamino which may be substituted with hydroxy,R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy, dialkylamino or 2,2-dialkoxycarbonylvinylaminoR.sub.a.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, alkenyloxy or dialkylamino,R.sup.5 is alkyl or alkenyl, andR.sup.6 is carboxy or esterified carboxy.

    摘要翻译: 下式的喹唑啉衍生物:其中A 1是A,其中R 1是氢,羧基或酯化的羧基,R 1a和R b1是酯化的羧基,R 2和R 3是氢,烷基,卤素,硝基,氨基, 烷氧基,芳氧基,烷硫基,烷基哌嗪基,酰氨基或可被羟基取代的二烷基氨基,R 4是氢,烷基,羟基,烷氧基,烯氧基,二烷基氨基或2,2-二烷氧基羰基乙烯基氨基R 4a是氢,烷基,羟基,烷氧基,烯氧基或二烷基氨基 R 5为烷基或烯基,R 6为羧基或酯化羧基。

    Imidazoisoquinoline compounds useful as anti-ulcerative agents
    5.
    发明授权
    Imidazoisoquinoline compounds useful as anti-ulcerative agents 失效
    咪唑并异喹啉化合物可用作抗溃疡剂

    公开(公告)号:US4738967A

    公开(公告)日:1988-04-19

    申请号:US945788

    申请日:1986-12-23

    CPC分类号: C07D487/04

    摘要: A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl,R.sup.3 is hydrogen, halogen or ar(lower)alkoxy, andR is lower alkanoyl, nitroso, amino, carboxy, esterified carboxy, carbamoyl, hydroxycarbamoyl, haloformyl, aminomethyleneamino which may be substituted with cyano or lower alkyl, iminomethylamino which may be substituted with cyano or lower alkyl, or a group of the formula: --A--R.sup.2 in which A is lower alkylene andR.sup.2 is di(lower) alkylamino, cyano, lower alkoxy, N-containing heterocyclic group which may have suitable substituent(s), lower alkynyloxy, lower alkenyloxy, lower alkylthio, amino(lower)alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, carboxy, esterified carboxy, carbamoyl, hydroxycarbamoyl, hydroxy, lower alkanoyloxy, heterocyclicamino(lower)alkylthio having two oxo groups, hydrogen or a group of the formula: ##STR2## in which R.sup.4, R.sup.5 and R.sup.6 are each lower alkyl andX is an acid residue,and pharmaceutically acceptable salts thereof. pa The compounds are useful as anti ulcer agents.

    Imidazoisoquinoline compounds useful as anti-ulcerative agents
    6.
    发明授权
    Imidazoisoquinoline compounds useful as anti-ulcerative agents 失效
    咪唑并异喹啉化合物可用作抗溃疡剂

    公开(公告)号:US4686227A

    公开(公告)日:1987-08-11

    申请号:US745638

    申请日:1985-06-17

    CPC分类号: C07D487/04

    摘要: A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl,R.sup.3 is hydrogen, halogen or ar(lower)alkoxy, andR is lower alkanoyl, nitroso, amino, carboxy, esterified carboxy, carbamoyl, hydroxycarbamoyl, haloformyl, aminomethyleneamino which may be substituted with cyano or lower alkyl, iminomethylamino which may be substituted with cyano or lower alkyl, or a group of the formula: --A--R.sup.2 in whichA is lower alkylene andR.sup.2 is di(lower)alkylamino, cyano, lower alkoxy, N-containing heterocyclic group which may have suitable substituent(s), lower alkynyloxy, lower alkenyloxy, lower alkylthio, amino(lower)alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, carboxy, esterified carboxy, carbamoyl, hydroxycarbamoyl, hydroxy, lower alkanoyloxy, heterocyclicamino (lower)alkylthio having two oxo groups, hydrogen or a group of the formula: ##STR2## in which R.sup.4, R.sup.5 and R.sup.6 are each lower alkyl andX is an acid residue,and pharmaceutically acceptable salts thereof.The compounds are useful as anti ulcer agents.

    摘要翻译: 下式的化合物,其中R 1为低级烷基,R 3为氢,卤素或芳(低级)烷氧基,R为低级烷酰基,亚硝基,氨基,羧基,酯化羧基,氨基甲酰基,羟基氨基甲酰基,卤代甲酰基,氨基亚甲基氨基 可以被氰基或低级烷基取代,可以被氰基或低级烷基取代的亚氨基甲基氨基,或下列基团:其中A是低级亚烷基,R2是二(低级)烷基氨基,氰基,低级烷氧基 ,可具有适当取代基的含N杂环基,低级炔氧基,低级烯氧基,低级烷硫基,氨基(低级)烷硫基,低级烷基亚磺酰基,低级烷基磺酰基,羧基,酯化羧基,氨基甲酰基,羟基氨基甲酰基,羟基,低级烷酰氧基, 具有两个氧代基的杂环氨基(低级)烷硫基,氢或下式的基团:其中R 4,R 5和R 6各自为低级烷基,X为酸残基,及其药学上可接受的盐。 该化合物可用作抗溃疡剂。

    Cephem compounds
    7.
    发明授权
    Cephem compounds 失效
    头孢烯化合物

    公开(公告)号:US4443443A

    公开(公告)日:1984-04-17

    申请号:US213232

    申请日:1980-12-05

    摘要: This invention relates to novel cephem compounds of high antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is carboxy or a protected carboxy group;A is lower alkylene which may have an oxo group;R.sup.3 is carboxy, a protected carboxy group, lower alkyl, lower alkenyl, hydroxy (lower) alkyl, phenyl (lower) alkyl, phenyl, tolyl, xylyl, cumenyl, or naphthyl; andR.sup.4 is hydrogen or lower alkoxy, and pharmaceutically acceptable salts thereof.

    摘要翻译: 本发明涉及高抗微生物活性的新型头孢烯化合物,其具有下式:其中R 1是氨基或被保护的氨基; R2是羧基或被保护的羧基; A是可以具有氧代基的低级亚烷基; R3是羧基,被保护的羧基,低级烷基,低级烯基,羟基(低级)烷基,苯基(低级)烷基,苯基,甲苯基,二甲苯基,枯烯基或萘基; 和R4是氢或低级烷氧基,及其药学上可接受的盐。