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    Pyridopyrimidine derivatives, pharmaceutical compositions containing them and process for preparing same
    1.
    发明授权
    Pyridopyrimidine derivatives, pharmaceutical compositions containing them and process for preparing same 失效
    吡啶并嘧啶衍生物，含有它们的药物组合物及其制备方法

    公开(公告)号：US5252572A

    公开(公告)日：1993-10-12

    申请号：US903246

    申请日：1992-06-23

    申请人： Istvan Hermecz ,  Jozsef Knoll ,  Lelle Vasvari nee Debreczy ,  Klara Gyires ,  Judit Sipos ,  Agnes Horvath ,  Laszlo Tardos ,  Maria Blaogh

    发明人： Istvan Hermecz ,  Jozsef Knoll ,  Lelle Vasvari nee Debreczy ,  Klara Gyires ,  Judit Sipos ,  Agnes Horvath ,  Laszlo Tardos ,  Maria Blaogh

    IPC分类号： C07D471/04 ,  A61K31/505

    CPC分类号： C07D471/04

    摘要： The present invention relates to novel 4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxamide derivatives of the general formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R stands for a C.sub.1-12 alkyl group optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a C.sub.3-9 cycloalkyl, adamantyl or optionally substituted phenyl group;R.sup.1 means hydrogen or a C.sub.1-4 alkyl group; orR and R.sup.1 together form a --(CH.sub.2).sub.n -- chain, wherein n is 4, 5 or 6;R.sup.2 stands for hydrogen, a C.sub.1-4 alkyl group or halogen;R.sup.3 represents hydrogen or a C.sub.1-4 alkyl group; andm is 0 or 1.The compounds of the general formula (I) possess a gastroprotective effect and are useful for the prevention and therapy of ulcers of the stomach and the small intestine.

    摘要翻译： 本发明涉及通式（I）的新型4-氧代-4H-吡啶并[1,2-a]嘧啶-3-甲酰胺衍生物及其酸加成盐，含有它们的药物组合物及其制备方法 。 在通式（I）中，R 1表示任选被C 1-4烷氧基羰基取代的C 1-12烷基; C3-9环烷基，金刚烷基或任选取代的苯基; R1表示氢或C1-4烷基; 或R和R 1一起形成 - （CH 2）n - 链，其中n为4,5或6; R2代表氢，C1-4烷基或卤素; R3表示氢或C1-4烷基; m为0或1.通式（I）的化合物具有胃保护作用，可用于预防和治疗胃和小肠溃疡。

    Pyridopyrimidine derivatives useful in treatment of ulcers
    2.
    发明授权
    Pyridopyrimidine derivatives useful in treatment of ulcers 失效
    用于治疗溃疡的吡啶并嘧啶衍生物

    公开(公告)号：US5158951A

    公开(公告)日：1992-10-27

    申请号：US307665

    申请日：1989-02-06

    申请人： Istvan Hermecz ,  Jozsef Knoll ,  Lelle Vasvari nee Debreczy ,  Klara Gyires ,  Judit Sipos ,  Agnes Horvath ,  Laszlo Tardos ,  Maria Blaogh

    发明人： Istvan Hermecz ,  Jozsef Knoll ,  Lelle Vasvari nee Debreczy ,  Klara Gyires ,  Judit Sipos ,  Agnes Horvath ,  Laszlo Tardos ,  Maria Blaogh

    IPC分类号： A61K31/505 ,  A61K31/513 ,  A61K31/519 ,  A61P1/04 ,  C07D221/00 ,  C07D239/26 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The present invention relates to novel 4-oxo-4H-pyrido[1,2-a]pyrimidine -3-carbonamide derivatives of the general formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## wherein: R stands for a C.sub.1-12 alkyl group optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a C.sub.3-9 cycloalkyl, adamantyl or optionally substituted phenyl group;R.sup.1 means hydrogen or a C.sub.1-4 alkyl group; orR and R.sup.1 together form a --(CH.sub.2).sub.n -- chain, wherein n is 4, 5 or 6;R.sup.2 stands for hydrogen, a C.sub.1-4 alkyl group or halogen;R.sup.3 repesents hydrogen or a C.sub.1-4 alkyl group; andm is 0 or 1.The compounds of the general formula (I) possess a gastroprotective effect and are useful for the prevention and therapy of ulcers of the stomach and the small intestine.

    摘要翻译： 本发明涉及通式（I）的新型4-氧代-4H-吡啶并[1,2-a]嘧啶-3-甲酰胺衍生物及其酸加成盐，含有它们的药物组合物及其制备方法 。 通式（I）其中：R表示任选被C 1-4烷氧基羰基取代的C 1-12烷基; C3-9环烷基，金刚烷基或任选取代的苯基; R1表示氢或C1-4烷基; 或R和R 1一起形成 - （CH 2）n - 链，其中n为4,5或6; R2代表氢，C1-4烷基或卤素; R3代表氢或C1-4烷基; m为0或1.通式（I）的化合物具有胃保护作用，可用于预防和治疗胃和小肠溃疡。

    Pyridopyrimidine derivatives, pharmaceutical compositions containing them and process for preparing same
    3.
    发明授权
    Pyridopyrimidine derivatives, pharmaceutical compositions containing them and process for preparing same 失效
    吡啶并嘧啶衍生物，含有它们的药物组合物及其制备方法

    公开(公告)号：US5387588A

    公开(公告)日：1995-02-07

    申请号：US80402

    申请日：1993-06-21

    申请人： Istvan Hermecz ,  Jozsef Knoll ,  Lelle Vasvari nee Debreczy ,  Klara Gyires ,  Judit Sipos ,  Agnes Horvath ,  Laszlo Tardos ,  Maria Blaogh

    发明人： Istvan Hermecz ,  Jozsef Knoll ,  Lelle Vasvari nee Debreczy ,  Klara Gyires ,  Judit Sipos ,  Agnes Horvath ,  Laszlo Tardos ,  Maria Blaogh

    IPC分类号： C07D471/04 ,  A61K31/505

    CPC分类号： C07D471/04

    摘要： The present invention relates to novel 4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxamide derivatives of the general formula (I) and the acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R stands for a C.sub.1-12 alkyl group optionally substituted by a C.sub.1-4 alkoxycarbonyl group; a C.sub.3-9 cycloalkyl, adamantyl or optionally substituted phenyl group;R.sup.1 means hydrogen or a C.sub.1-4 alkyl group; orR and R.sup.1 together form a --(CH.sub.2).sub.n -- chain, wherein n is 4, 5 or 6;R.sup.2 stands for hydrogen, a C.sub.1-4 alkyl group or halogen;R.sup.3 represents hydrogen or a C.sub.1-4 alkyl group; andm is 0 or 1.The compounds of the general formula (I) possess a gastroprotective effect and are useful for the prevention and therapy of ulcers of the stomach and the small intestine.

    摘要翻译： 本发明涉及通式（I）的新型4-氧代-4H-吡啶并[1,2-a]嘧啶-3-甲酰胺衍生物及其酸加成盐，含有它们的药物组合物及其制备方法 。 在通式（I）中，R 1表示任选被C 1-4烷氧基羰基取代的C 1-12烷基; C3-9环烷基，金刚烷基或任选取代的苯基; R1表示氢或C1-4烷基; 或R和R 1一起形成 - （CH 2）n - 链，其中n为4,5或6; R2代表氢，C1-4烷基或卤素; R3表示氢或C1-4烷基; m为0或1.通式（I）的化合物具有胃保护作用，可用于预防和治疗胃和小肠溃疡。

    Triazole substituted quinoline derivatives for gastrointestinal treat-treatment
    6.
    发明授权
    Triazole substituted quinoline derivatives for gastrointestinal treat-treatment 失效
    用于胃肠道治疗的三唑取代喹啉衍生物

    公开(公告)号：US5830903A

    公开(公告)日：1998-11-03

    申请号：US343576

    申请日：1996-01-29

    申请人： Laszlo Frank ,  Klara Gyires ,  Andras Bilkei-Gorzo ,  Ferenc Korodi ,  Vilmos Galamb

    发明人： Laszlo Frank ,  Klara Gyires ,  Andras Bilkei-Gorzo ,  Ferenc Korodi ,  Vilmos Galamb

    IPC分类号： C07D401/06 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61P1/00 ,  C07D401/04 ,  C07D401/12 ,  C07D521/00

    CPC分类号： C07D231/12 ,  A61K31/47 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12

    摘要： The invention relates to pharmaceutical compositions for the treatment or prevention of lesions of gastrointestinal mucous membranes and having secretion inhibiting, cytoprotective activities. The compositions contain in a biologically effective quantity a triazole-group-substituted quinoline derivative of general formula (I) R.sup.1 stands for a 1-triazolyl-group in position 2 or 4 or a 3-triazolyl-thio or a 5-/C.sub.1-4 -alkyl/-3-triazolyl-thio-group, R.sup.2 stands for a hydrogen atom in position 3 or optionally in position 2, or for a C.sub.1-4 -alkyl-group, R.sup.3 stands for a hydrogen atom or for a C.sub.1-4 -alkyl-group, X stands for a hydrogen or halogen-atom or for a C.sub.1-4 -alkyl-group or its salts. The invention includes processes for the preparation of the above compositions, and methods for treatment of patients in need of such treatment by administering the substance or the composition. The prefered substance of formula (IV) is also subject of the invention.

    摘要翻译： PCT No.PCT / HU94 / 00008 Sec。 371日期1996年1月29日 102（e）日期1996年1月29日PCT 1994年3月31日PCT公布。 公开号WO94 / 22413 日期：1994年10月13日本发明涉及用于治疗或预防胃肠粘膜病变并具有分泌抑制，细胞保护活性的药物组合物。 组合物含有生物有效量的通式（I）的三唑基取代喹啉衍生物R1代表位置2或4或3-三唑基硫基或5- / C1- 4-烷基-3-三唑基硫基，R 2表示3位或任选位置2的氢原子，或表示C 1-4 - 烷基，R 3表示氢原子或C1- 4-烷基，X代表氢或卤素原子或C1-4烷基或其盐。 本发明包括制备上述组合物的方法，以及通过施用该物质或组合物来治疗需要这种治疗的患者的方法。 式（IV）的优选物质也是本发明的主题。