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。

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。

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。