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1. 发明授权

US4123533A Fused pyrimidine derivatives and compositions for treating atherosclerosis containing them 失效
标题翻译：融合的嘧啶衍生物和用于治疗含有它们的动脉粥样硬化的组合物
公开(公告)号：US4123533A
公开(公告)日：1978-10-31
申请号：US765595
申请日：1977-02-04
申请人： Istvan Hermecz , Zoltan Meszaros , Sandor Virag , Lelle Vasvari nee Debreczy , Agnes Horvath , Jozsef Knoll , Gyula Sebestyen , Agoston David
发明人： Istvan Hermecz , Zoltan Meszaros , Sandor Virag , Lelle Vasvari nee Debreczy , Agnes Horvath , Jozsef Knoll , Gyula Sebestyen , Agoston David
IPC分类号： C07D487/04 , A61K31/505 , A61K31/519 , A61P3/06 , A61P9/10 , A61P25/28 , C07D471/04
CPC分类号： C07D471/04 , Y10S514/824 , Y10S514/826 , Y10S514/893 , Y10S514/916 , Y10S514/924
摘要： Compounds of the formula: ##STR1## or pharmaceutically acceptable salts thereof are disclosed wherein R is hydrogen or C.sub.1 to C.sub.6 alkyl;R.sup.2 and R.sup.3 are each hydrogen or together form a valency bond;R.sup.6 is carboxy or C.sub.1 to C.sub.6 alkoxycarbonyl;R.sup.7 and R.sup.8 are each hydrogen or together form a valency bond;R.sup.10 is carboxy or C.sub.1 to C.sub.6 alkoxycarbonyl and the dotted line represents two hydrogen atoms or a valency bond. The compounds are useful in the treatment of atherosclerosis.
摘要翻译：公开了下式的化合物：其中R是氢或C1-C6烷基; R2和R3各自为氢或一起形成价键; R6是羧基或C1-C6烷氧基羰基; R7和R8各自为氢或一起形成价键; R 10是羧基或C 1至C 6烷氧基羰基，虚线表示两个氢原子或价键。该化合物可用于治疗动脉粥样硬化。

2. 发明授权

US4472398A Condensed pyrimidines 失效
标题翻译：浓缩嘧啶
公开(公告)号：US4472398A
公开(公告)日：1984-09-18
申请号：US14689
申请日：1979-02-23
申请人： Zoltan Meszaros , Jozsef Knoll , Istvan Hermecz , Agnes Horvath , Sandor Virag , Lelle Vasvari, nee Debreczy , Agoston David
发明人： Zoltan Meszaros , Jozsef Knoll , Istvan Hermecz , Agnes Horvath , Sandor Virag , Lelle Vasvari, nee Debreczy , Agoston David
IPC分类号： A61K31/505 , A61K31/519 , A61P7/02 , A61P25/04 , A61P29/00 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： Antiphlogistic and anticoagulant compounds of the formula: ##STR1## wherein m is 0, 1 or 2,n is 0, 1 or 2,R is C.sub.1 to C.sub.6 alkyl,R.sub.1 is hydrogen, or C.sub.1 to C.sub.6 alkyl,R.sub.2 is hydrogen, C.sub.1 to C.sub.6 alkyl, substituted or unsubstituted amino, substituted or unsubstituted hydroxy, carboxy or a group derived from a carboxylic acid orR.sub.1 and R.sub.2 together form a --(CH.dbd.CH).sub.2 --group andR.sub.5 is 0 or imino or substituted imino.
摘要翻译：其中m为0,1或2，n为0,1或2，R为C 1至C 6烷基，R 1为氢或C 1至C 6烷基，R 2为氢，C 1 -C 6烷基，取代或未取代的氨基，取代或未取代的羟基，羧基或衍生自羧酸的基团，或R 1和R 2一起形成 - （CH = CH）2 - 基，R 5为0或亚氨基或取代的亚氨基。

3. 发明授权

US4460771A Antiphlogistic and anticoagulant condensed pyrimidine derivatives 失效
标题翻译：消炎和抗凝血嘧啶衍生物
公开(公告)号：US4460771A
公开(公告)日：1984-07-17
申请号：US742464
申请日：1976-11-17
申请人： Zoltan Meszaros , Jozsef Knoll , Peter Szentmiklosi , Istvan Hermes , Agnes Horvath , Sandor Virag , Lelle Vasvari nee Debreczy , Agoston David
发明人： Zoltan Meszaros , Jozsef Knoll , Peter Szentmiklosi , Istvan Hermes , Agnes Horvath , Sandor Virag , Lelle Vasvari nee Debreczy , Agoston David
IPC分类号： A61K31/505 , A61K31/519 , A61P7/02 , A61P25/04 , A61P29/00 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： New optionally racemic or optically active pyrimido(1,2a) heterocyclic compounds of the formula ##STR1## wherein m is 0, 1 or 2,n is 0, 1 or 2,R is an alkyl group containing one to six carbon atoms,R.sup.1 is hydrogen, alkyl containing one to six carbon atoms,R.sup.2 is hydrogen, alkyl containing one to six carbon atoms, optionally substituted amino, optionally substituted hydroxy, carboxy or a group derived from a carboxylic acid orR.sup.1 and R.sup.2 together form a --(CH.dbd.CH).sub.2 -- group attached to the two adjacent carbon atoms of the ring A and the broken line represents a chemical bond,R.sup.3 is hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycle, optionally substituted cycloalkyl, optionally substituted acyl or optionally substituted hydroxy,R.sup.4 is hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocycle, optionally substituted cycloalkyl, optionally substituted acyl orR.sup.3 and R.sup.4 together with the nitrogen can form an optionally substituted five-, six- or seven-membered ring, which can contain a further heteroatom or heteroatoms,R.sup.5 is oxygen or an optionally substituted imino group are disclosed as well as a process for the preparation thereof.
摘要翻译：新的任选的外消旋或光学活性嘧啶（1,2a）杂环化合物，其中m为0,1或2，n为0,1或2，R为含有1至6个碳原子的烷基，R 1为是氢，含有1至6个碳原子的烷基，R 2是氢，含1至6个碳原子的烷基，任选取代的氨基，任选取代的羟基，羧基或衍生自羧酸的基团或R 1和R 2一起形成 - （CH = CH）连接到环A的两个相邻碳原子上的2-基团，虚线表示化学键，R 3是氢，任选取代的烷基，任选取代的芳基，任选取代的芳烷基，任选取代的杂环，任选取代的环烷基，任选取代的酰基或任选取代的羟基，R 4是氢，任选取代的烷基，任选取代的芳基，任选取代的芳烷基，任选取代的杂环，任选取代的环烷基，选择可以将氮取代的酰基或R3和R4与氮一起形成任选取代的五元，六元或七元环，其可以含有另外的杂原子或杂原子，R5是氧或任选取代的亚氨基，其制备方法。

4. 发明授权

US4252807A Fused pyrimidine derivatives and antiatherosclerotic methods of treatment with them 失效
标题翻译：融合嘧啶衍生物和抗动脉粥样硬化治疗方法
公开(公告)号：US4252807A
公开(公告)日：1981-02-24
申请号：US931908
申请日：1978-08-08
申请人： Istvan Hermecz , Zoltan Meszaros , Sandor Virag , Lelle Vasvari , Agnes Horvath , Jozsef Knoll , Gyula Sebestyen , Agoston David
发明人： Istvan Hermecz , Zoltan Meszaros , Sandor Virag , Lelle Vasvari , Agnes Horvath , Jozsef Knoll , Gyula Sebestyen , Agoston David
IPC分类号： C07D487/04 , A61K31/505 , A61K31/519 , A61P3/06 , A61P9/10 , A61P25/28 , C07D471/04
CPC分类号： C07D471/04 , Y10S514/824 , Y10S514/826 , Y10S514/893 , Y10S514/916 , Y10S514/924
摘要： An optically active or racemic fused pyrimidine derivative of the formula I ##STR1## has pharmaceutical activity in decreasing serum lipids, cholesterol deposits and, in general, against atherosclerosis.
摘要翻译：式I（I）的光学活性或外消旋的稠合嘧啶衍生物具有降低血清脂质，胆固醇沉积物和一般抗动脉粥样硬化的药物活性。

5. 发明授权

US4495189A Condensed pyrimidines 失效
标题翻译：浓缩嘧啶
公开(公告)号：US4495189A
公开(公告)日：1985-01-22
申请号：US364753
申请日：1982-04-02
申请人： Zoltan Meszaros , Jozsef Knoll , Peter Szentmiklosi , Istvan Hermecz , Agnes Horvath , Sandor Virag , Lelle Vasvari , Agoston David
发明人： Zoltan Meszaros , Jozsef Knoll , Peter Szentmiklosi , Istvan Hermecz , Agnes Horvath , Sandor Virag , Lelle Vasvari , Agoston David
IPC分类号： C07D471/04 , A61K31/505
CPC分类号： C07D471/04
摘要： New compounds of the following formula are disclosed:1,6-dimethyl-3-carbamoyl-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)-pyrimidine;1,6-dimethyl-3-(N-tertiary-butyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine;1,6-dimethyl-3-(N-2-phenethyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine;1,6-dimethyl-3-[N-(3,3-diphenyl-propyl)-carbamoyl]-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine;1,6-dimethyl-3-(N-phenyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine; and1,6-dimethyl-3-(N-methyl-carbamoyl)-4-oxo-1,6,7,8-tetrahydro-4H-pyrido(1,2-a)pyrimidine, as well as pharmaceutical compositions containing these compounds and a method of inhibiting thrombocyte aggregation in mammals employing a pharmaceutically effective amount of at least one of these compounds.
摘要翻译：公开了下式的新化合物：1,6-二甲基-3-氨基甲酰基-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a） - 吡啶亚胺; 1,6-二甲基-3-（N-叔丁基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶; 1,1-二甲基-3-（N-2-苯乙基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-哒嗪（1,2-a）嘧啶; 1,6-二甲基-3- [N-（3,3-二苯基 - 丙基） - 氨基甲酰基] -4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶 ; 1,6-二甲基-3-（N-苯基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶; 和1,6-二甲基-3-（N-甲基 - 氨基甲酰基）-4-氧代-1,6,7,8-四氢-4H-吡啶并（1,2-a）嘧啶，以及含有这些的药物组合物化合物和使用药学上有效量的这些化合物中的至少一种来抑制哺乳动物血小板聚集的方法。

6. 发明授权

US5252572A Pyridopyrimidine derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：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。

7. 发明授权

US5158951A Pyridopyrimidine derivatives useful in treatment of ulcers 失效
标题翻译：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。

8. 发明授权

US5387588A Pyridopyrimidine derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：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。

9. 发明授权

US4291036A Pyrido[1,2-A]pyrimidine derivatives and method of analgesic treatment 失效
标题翻译：吡啶并[1,2-A]嘧啶衍生物和镇痛治疗方法
公开(公告)号：US4291036A
公开(公告)日：1981-09-22
申请号：US130371
申请日：1980-03-14
申请人： Jozsef Knoll , Zoltan Meszaros , Istvan Hermecz , Ferenc Fulop , Gabor Bernath , Sandor Virag , Gabor Nagy , Peter Szentmiklosi
发明人： Jozsef Knoll , Zoltan Meszaros , Istvan Hermecz , Ferenc Fulop , Gabor Bernath , Sandor Virag , Gabor Nagy , Peter Szentmiklosi
IPC分类号： A61K31/505 , A61K31/519 , A61P25/04 , A61P29/00 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04
摘要： Compounds of the formula ##STR1## or pharmaceutically acceptable acid-addition or quaternart ammonium salts thereofwhereinR is hydroxy, carboxy, lower alkoxycarbonyl, benzyloxycarbonyl, phenoxycarbonyl, carbamoyl, N-loweralkyl-carbamoyl, N,N-dilower-alkyl-carbamoyl, carboazido, carbohydrazido or cyano;R.sup.2 is C.sub.1 to C.sub.6 alkyl;R.sup.3 is C.sub.1 to C.sub.6 alkyl or benzyl; andR.sup.4 is a single electron pair, hydrogen or lower alkyl; and the dotted lines represent saturated or unsaturated bonds, are disclosed with analgesic properties.
摘要翻译：其中R是羟基，羧基，低级烷氧基羰基，苄氧基羰基，苯氧基羰基，氨基甲酰基，N-低级烷基 - 氨基甲酰基，N，N-二 - 低级烷基 - 氨基甲酰基，碳氮杂，碳酰肼基或氰基; R2是C1-C6烷基; R3是C1-C6烷基或苄基; R4是单电子对，氢或低级烷基; 并且虚线表示饱和或不饱和键，其具有镇痛特性。

10. 发明授权

US4089858A Heterocyclic-amino-acrylic acid derivatives 失效
标题翻译：杂环氨基 - 丙烯酸衍生物
公开(公告)号：US4089858A
公开(公告)日：1978-05-16
申请号：US614208
申请日：1975-09-17
申请人： Zoltan Meszaros , Jozsef Knoll , Istvan Hermecz , Piroska Simon , Peter Szentmiklosy , Lelle Vasvari , Agnes Horvath , Gabor Horvath , Peter Dvortsak
发明人： Zoltan Meszaros , Jozsef Knoll , Istvan Hermecz , Piroska Simon , Peter Szentmiklosy , Lelle Vasvari , Agnes Horvath , Gabor Horvath , Peter Dvortsak
IPC分类号： C07D213/74 , C07D215/38 , C07D239/42 , C07D239/84 , C07D239/94 , C07D213/02
CPC分类号： C07D213/74 , C07D215/38 , C07D239/42 , C07D239/84 , C07D239/94
摘要： The present invention is concerned with the preparation of chemical intermediates, namely, beta-amino-acrylic acid ester derivatives of nitrogen heterocycles, i.e. pyridine, quinoline, quinoxaline, pyrazine, pyrimidine and the like. Said intermediates are cyclized to form pyrido-pyrimidine type final products possessing analgesic activity.
摘要翻译：本发明涉及化学中间体的制备，即氮杂环的β-氨基 - 丙烯酸酯衍生物，即吡啶，喹啉，喹喔啉，吡嗪，嘧啶等。所述中间体环化形成具有止痛活性的吡啶并嘧啶型终产物。

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