Imidazoisoquinoline compounds useful as anti-ulcerative agents
    3.
    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
    4.
    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。

    Chromone derivatives
    6.
    发明授权
    Chromone derivatives 失效
    色酮衍生物

    公开(公告)号:US4001280A

    公开(公告)日:1977-01-04

    申请号:US371852

    申请日:1973-06-20

    IPC分类号: C07D311/24

    CPC分类号: C07D311/24

    摘要: Chromone derivatives of the formula: ##STR1## wherein R.sup.1 is alkoxy, an N,S-containing heterocyclic group or aryloxy in which heterocyclic group may be substituted with halogen or acyl, and aryl may be substituted with amino, alkylamino, acylamino, nitro or alkylenedioxy; R.sup.2 is alkylene; R.sup.3 is hydroxy, alkoxy or a group of the formula ##STR2## in which R.sup.4 is hydrogen, R.sup.5 is hydroxy or amino or R.sup.4 and R.sup.5 means taken together with the adjacent nitrogen atom, piperazinyl substituted with alkyl or hydroxyalkyl; provided that when R.sup.3 is hydroxy or alkoxy, R.sup.1 is an N,S-containing heterocyclic group or aryloxy in which heterocyclic group is substituted with halogen or acyl, and aryl is substituted with amino, alkylamino, acylamino, nitro or alkylenedioxy, and nontoxic, pharmaceutically acceptable salt thereof. These compounds are useful as anti-allergic agents.

    Chromone compounds and preparation thereof
    7.
    发明授权
    Chromone compounds and preparation thereof 失效
    色酮化合物及其制备方法

    公开(公告)号:US3965122A

    公开(公告)日:1976-06-22

    申请号:US213180

    申请日:1971-12-28

    摘要: Chromone compounds having the structure ##SPC1##Wherein R is aryl, substituted aryl, thienyl, furyl or pyridyl, Y is hydroxy(lower)alkylene, R.sub.1 is hydrogen, lower alkyl, aryl, substituted aryl or a heterocyclic group, R.sub.2 is hydrogen or lower alkoxy, Y.sub.1 is lower alkylene or hydroxyl(lower)alkylene, Z is oxygen or sulfur and R.sub.3 is hydrogen, lower alkyl, aryl, substituted aryl, or ar(lower)alkyl have anti-allergic activity and are useful in the treatment of asthma. Compounds of the structure [I] are prepared by reacting ##SPC2##Wherein Y' is hydroxy(lower)alkylene whose hydroxy group is optimally protected or a reactive derivative of [II] with a carboxylic acid of the formula R--COOH in the presence of a basic catalyst. The resulting compound is then reacted with an acid. Compounds of the structure [I'] are prepared by reacting the compound ##SPC3##With the compound X--Y.sub.1 '--Z--R.sub.3 ' wherein X is an acid residue, Y' is lower alkylene or hydroxy(lower)alkylene whose hydroxy group is optionally protected by a protective group, R.sub.3 ' is hydrogen, lower alkyl, aryl, substituted aryl, or ar(lower)alkyl and Z is as defined above. When R.sub.3 ' is hydrogen, --Z--R.sub.3 ' is optionally protected by a protective group. The resultant compound is subjected to an elimination reaction when Y' is a protected group or when --Z--R.sub.3 ' is protected to split off the protective group.

    摘要翻译: 具有下式结构的色酮化合物是芳基,取代的芳基,噻吩基,呋喃基或吡啶基,Y是羟基(低级)亚烷基,R1是氢,低级烷基,芳基,取代的芳基或杂环基,R2是氢或低级烷氧基, Y1是低级亚烷基或羟基(低级)亚烷基,Z是氧或硫,R3是氢,低级烷基,芳基,取代芳基或芳(低级)烷基具有抗过敏活性,可用于治疗哮喘。 结构[I]的化合物通过在碱存在下使WHEREIN Y'为羟基被最佳保护的羟基(低级)亚烷基或[II]的反应性衍生物与式R-COOH的羧酸反应来制备 催化剂。 然后将所得化合物与酸反应。 通过使化合物与化合物X-Y1'-Z-R3'反应制备化合物,其中X是酸残基,Y'是羟基被任选保护的低级亚烷基或羟基(低级)亚烷基 通过保护基团,R 3'是氢,低级烷基,芳基,取代的芳基或芳(低级)烷基,Z如上所定义。 当R3'为氢时,-Z-R3'任选被保护基保护。 当Y'为受保护基团时或当-Z-R3'被保护以分离保护基团时,所得化合物进行消除反应。

    Cephem compounds
    9.
    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。