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1. 发明授权

US4814336A Method of treating a vascular obstructive lesion resulting from restricted blood circulation 失效
标题翻译：治疗血液循环受限血管阻塞性病变的方法
公开(公告)号：US4814336A
公开(公告)日：1989-03-21
申请号：US937536
申请日：1986-12-03
申请人： Peter Szentmiklosi , Istvan Hermecz , Zoltan Meszaros , Laszo Tardos , Jeno Marton , Lelle Vasvari (nee Debreczy) , Agnes Horvath , Katalin Marmarosi (nee Kellner)
发明人： Peter Szentmiklosi , Istvan Hermecz , Zoltan Meszaros , Laszo Tardos , Jeno Marton , Lelle Vasvari (nee Debreczy) , Agnes Horvath , Katalin Marmarosi (nee Kellner)
IPC分类号： A61K31/485 , A61K31/52 , A61K31/522 , A61P9/00 , C07D473/08 , A61K31/47
CPC分类号： A61K31/52 , A61K31/485
摘要： A new method of treatment is disclosed for a vascular obstructive lesion resulting from restricted blood circulation, characterized by an erythrocyte pathology, in an effected animal subject. The new method involves the administration of 1-(3',4'-diethoxybenzyl)-6,7-diethoxy-3,4-dihydroisoquinolinium-theophylline-7-acetat e, in a dosage and at a rate sufficient to maintain a blood concentration of at least 0.5 to at most 3 .gamma./ml, calculated on the basis of 1-(3',4'-diethoxybenzyl)-6,7-diethoxy-3,4-dihydroisoquinoline.
摘要翻译：公开了一种新的治疗方法，用于在受影响的动物受试者中由特征在于红细胞病理学的限制性血液循环导致的血管阻塞性病变。该新方法涉及以足以维持一个（3'，4'-二乙氧基苄基）-6,7-二乙氧基-3,4-二氢异喹啉鎓-γ-甲基-7-乙酸乙酯的剂量和速率基于1-（3'，4'-二乙氧基苄基）-6,7-二乙氧基-3,4-二氢异喹啉计算血液浓度为至少0.5至3μg/ ml。

2. 发明授权

US4035366A 1-Benzal-1,2,3,4-tetrahydro-isoquinolinium-theophylline-7-acetates 失效
标题翻译： 1-苄基-1,2,3,4-四氢 - 异喹啉 - 茶碱-7-乙酸酯
公开(公告)号：US4035366A
公开(公告)日：1977-07-12
申请号：US435591
申请日：1974-01-22
申请人： Peter Szentmiklosi , Zoltan Meszaros , Laszlo Tardos , Istvan Hermecz , Ilona Erdelyi , Agoston David , Lelle Vasvari nee Debreczy , Agnes Horvath
发明人： Peter Szentmiklosi , Zoltan Meszaros , Laszlo Tardos , Istvan Hermecz , Ilona Erdelyi , Agoston David , Lelle Vasvari nee Debreczy , Agnes Horvath
IPC分类号： C07D217/02 , A61K31/52 , A61K31/522 , A61P1/04 , A61P9/12 , C07D217/00 , C07D217/10 , C07D217/18 , C07D217/20 , C07D473/08
CPC分类号： C07D473/08 , C07D217/10 , C07D217/18 , C07D217/20 , Y10S514/878
摘要： 1-Benzal-1,2,3,4-tetrahydro-isoquinolinium-theophylline-7-acetates are used in the manufacture of geriatric compositions.
摘要翻译： 1-苄基-1,2,3,4-四氢 - 异喹啉 - 茶碱-7-乙酸酯用于制造老年组合物。

3. 发明授权

US4404205A 2-Oxo-2,6,7,8,9,10 hexahydro-pyrimido[1,2-a]azepines and antianginal method of use thereof and of 4-oxo-4,6,7,8,9,10-hexahydropyrimido[1,2-a]azepines 失效
标题翻译： 2-氧代-2,6,7,8,9,10-六氢 - 嘧啶并[1,2-a]吖庚因及其抗肾功能方法和4-氧代-4,6,7,8,9,10- 六氢嘧啶并[1,2-a]吖庚因
公开(公告)号：US4404205A
公开(公告)日：1983-09-13
申请号：US148234
申请日：1980-05-09
申请人： Jozsef Kokosi , Istvan Hermecz , Zoltan Meszaros , Gyorgy Szasz , Lelle Vasvari nee Debreczy , Agnes Horvath , Tibor Breining
发明人： Jozsef Kokosi , Istvan Hermecz , Zoltan Meszaros , Gyorgy Szasz , Lelle Vasvari nee Debreczy , Agnes Horvath , Tibor Breining
IPC分类号： A61K31/55 , A61K31/551 , A61P9/00 , A61P9/04 , C07D487/04 , A61K31/305
CPC分类号： C07D487/04
摘要： 3 Substituted hexahydro-pyrimido[1, 2 a]azepines and quaternary derivatives, useful as antianginals are prepared. Specifically tested are 3 carboxylates and carbo hydrazides. 3 Cyano Carbamonyl and alkyl compounds are also disclosed.
摘要翻译： 3制备用作抗坏血酸的取代的六氢 - 嘧啶并[1,2]吖庚因和季衍生物。具体测试的是3个羧酸酯和碳酰肼。还公开了3种氰基氨基甲酰基和烷基化合物。

4. 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。

5. 发明授权

US4461769A Nitrogen bridgehead compounds having anti-allergic effect 失效
标题翻译：具有抗过敏作用的氮桥头头合成物
公开(公告)号：US4461769A
公开(公告)日：1984-07-24
申请号：US76811
申请日：1979-09-19
申请人： Istvan Hermecz , Zoltan Meszaros , Tibor Breining , Sandor Virag , Lelle Vasvari nee Debreczy , Agnes Horvath , Gabor Nagy , Attila Mandi , Tamas Szucs , Istvan Bitter , Gyula Sebestyen
发明人： Istvan Hermecz , Zoltan Meszaros , Tibor Breining , Sandor Virag , Lelle Vasvari nee Debreczy , Agnes Horvath , Gabor Nagy , Attila Mandi , Tamas Szucs , Istvan Bitter , Gyula Sebestyen
IPC分类号： A61K31/505 , A61K31/519 , A61P1/04 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P25/00 , A61P25/04 , A61P25/20 , A61P29/00 , A61P31/04 , A61P37/08 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04 , Y10S514/826
摘要： Compounds of the formula I ##STR1## or pharmaceutically acceptable salts, hydrates, stereoisomers, optically active isomers, geometrical isomers or tautomeric forms thereof are disclosedwhereinR is hydrogen or lower alkylR.sup.1 is hydrogen, lower alkyl, styryl, or a carboxylic acid; orR and R.sup.1 together form a group of the formula --(CH.dbd.CH).sub.2 -- and in this case the broken line represents a further C--C bond, while in all other cases there is a single bond between positions 6 and 7;R.sup.2 is hydrogen, lower alkyl or hydroxy;R.sup.3 is hydrogen, lower alkyl, aryl, lower alkanoyl, carboxyl or a carboxyl acid derivative or a group of the formula --(CH.sub.2)m--COOH or a derivative thereof formed in the carboxylic group;n=1-3;R.sup.4 is hydrogen, lower alkyl which can be substituted by hydroxy or carboxy; trifluoromethyl, substituted or unsubstituted aryl, phenyl-lower alkyl or substituted or an unsubstituted heterocyclic group;R.sup.5 is hydrogen, lower alkanoyl, substituted or unsubstituted benzoyl or heteroaryl; orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a piperidino, pyrrolidino or morpholino ring; orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a group of the formula ##STR2## wherein R.sup.6 is hydrogen and R.sup.7 is substituted or unsubstituted phenyl; andZ is oxygen. The new compounds are useful for treating asthma.
摘要翻译：公开了式I的化合物或其药学上可接受的盐，水合物，立体异构体，光学活性异构体，几何异构体或互变异构体，其中R是氢或低级烷基R 1是氢，低级烷基，苯乙烯基或羧酸; 或R和R 1一起形成式 - （CH = CH）2 - 的基团，在这种情况下，虚线代表另外的C-C键，而在所有其它情况下，位置6和7之间存在单键; R2是氢，低级烷基或羟基; R3是在羧基中形成的氢，低级烷基，芳基，低级烷酰基，羧基或羧基酸衍生物或式 - （CH2）m-COOH或其衍生物的基团; n = 1-3; R4是氢，可被羟基或羧基取代的低级烷基; 三氟甲基，取代或未取代的芳基，苯基 - 低级烷基或取代或未取代的杂环基; R5是氢，低级烷酰基，取代或未取代的苯甲酰基或杂芳基; 或R4和R5与相邻的氮原子一起形成哌啶子基，吡咯烷子基或吗啉代环; 或R 4和R 5与相邻的氮原子一起形成下式的基团：其中R6是氢，R7是取代或未取代的苯基; Z是氧。新化合物可用于治疗哮喘。

6. 发明授权

US4482557A 3-Substituted-2-oxo-tetrahydro-pyrrol[1,2-a]pyrimidines having digitalis-like activity 失效
标题翻译： 3-取代-2-氧代 - 四氢 - 吡咯并[1,2-a]嘧啶，具有洋地黄样活性
公开(公告)号：US4482557A
公开(公告)日：1984-11-13
申请号：US416130
申请日：1982-09-09
申请人： Jozsef Kokosi , Istvan Hermecz , Zoltan Meszaros , Gyorgy Szasz , Lelle Vasvari nee Debreczy , Agnes Horvath , Tibor Breining
发明人： Jozsef Kokosi , Istvan Hermecz , Zoltan Meszaros , Gyorgy Szasz , Lelle Vasvari nee Debreczy , Agnes Horvath , Tibor Breining
IPC分类号： C07D487/04 , A61K31/505
CPC分类号： C07D487/04
摘要： New 3-substituted-2-oxo-tetrahydro-pyrrolo[1,2-a]pyrimidines of the formula (II) ##STR1## or a pharmaceutically acceptable acid addition or quaternary ammonium salts thereof are disclosed, whereinR is hydrogen or lower alkyl;R.sup.1 is lower alkyl, phenyl, carboxyl, lower alkoxycarbonyl, nitrile, carbamoyl, or carbohydrazido; andR.sup.2 is hydrogen or lower alkyl. The compounds exert a positive inotropic activity on the heart and have digitalis-like activity.
摘要翻译：公开了式（II）的新的3-取代-2-氧代 - 四氢 - 吡咯并[1,2-a]嘧啶或其药学上可接受的酸加成盐或季铵盐，其中R是氢或低级烷基; R 1是低级烷基，苯基，羧基，低级烷氧基羰基，腈，氨基甲酰基或碳酰肼基; 并且R 2是氢或低级烷基。这些化合物对心脏发挥积极的肌力活性，具有洋地黄样活性。

7. 发明授权

US4472399A Indolo[2',3';3,4]pyrido[2,1-b]quinazoline-5-ones, a process for the preparation thereof, and diuretic compositions and methods using them 失效
标题翻译：吲哚并[2'，3'; 3,4]吡啶并[2,1-b]喹唑啉-5-酮，其制备方法和使用它们的利尿剂组合物和方法
公开(公告)号：US4472399A
公开(公告)日：1984-09-18
申请号：US308037
申请日：1981-10-02
申请人： Jozsef Kokosi , Istvan Hermecz , Zoltan Meszaros , Sandor Virag , Lelle Vasvari, nee Debreczy , Gyorgy Szasz , Agnes Horvath , Tibor Breining , Tamas Szuts , Gyula Sebestyen
发明人： Jozsef Kokosi , Istvan Hermecz , Zoltan Meszaros , Sandor Virag , Lelle Vasvari, nee Debreczy , Gyorgy Szasz , Agnes Horvath , Tibor Breining , Tamas Szuts , Gyula Sebestyen
IPC分类号： C07D471/14 , A61K31/505 , C07D487/14
CPC分类号： C07D471/14 , Y10S514/869
摘要： New Rutecarpine analogs are disclosed having Rutecarpine-like activity, especially diuretic activity. Also a novel process for the preparation of the Rutecarpine analogs is disclosed.
摘要翻译：公开了具有罗特金属样活性，特别是利尿活性的新的罗特金属类似物。还公开了用于制备罗非鱼类似物的新方法。

8. 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。

9. 发明授权

US4395549A 6-Hydrazono-pyrido[2,1-b] quinazoline-11 ones 失效
标题翻译： 6-肼基 - 吡啶并[2,1-b]喹唑啉-11
公开(公告)号：US4395549A
公开(公告)日：1983-07-26
申请号：US308038
申请日：1981-10-02
申请人： Istvan Hermecz , Jozsef Kokosi , Agnes Horvath , Zoltan Meszaros , Gyorgy Szasz , Tibor Breining , Lelle Vasvari nee Debreczy
发明人： Istvan Hermecz , Jozsef Kokosi , Agnes Horvath , Zoltan Meszaros , Gyorgy Szasz , Tibor Breining , Lelle Vasvari nee Debreczy
IPC分类号： C07D487/04 , C07D487/14
CPC分类号： C07D487/04
摘要： Intermediates useful in the preparation of Rutecarpine and Rutecarpine derivatives are disclosed as well as a process for the preparation of said intermediates having the following formula: ##STR1## wherein R, R.sup.1 and R.sup.2 are the same or different and stand for hydrogen, halogen, nitro, carboxy, nitrile, alkoxy containing 1 to 4 carbon atoms, alkoxycarbonyl containing 1 to 4 carbon atoms in the alkoxy group, alkyl containing 1 to 4 carbon atoms, amino or hydroxy or R and R.sup.1 together stand for methylenedioxy, R.sup.2 stands for hydrogen, R.sup.3 represents hydrogen or alkyl containing 1 to 4 carbon atoms, R.sup.4 stands for phenyl, phenyl substituted by 1 to 3 same or different substituents selected from the group of halogen(s), alkyl, and alkoxy containing 1 to 4 carbon atoms, phenyloxy, hydroxy, nitro, amino, cyano, carboxy, alkoxycarbonyl having 1 to 4 carbon atoms, alkanoyl having 1 to 4 carbon atoms, methylenedioxy, trifluoromethyl, phenyl and dialkylamino having 1 to 4 carbon atoms in the alkyl part or naphthyl and the dotted line indicated an optional double bond. Also pharmaceutically acceptable acid addition and quaternary ammonium salts are disclosed.
摘要翻译：公开了用于制备罗非鱼和芦丁类衍生物的中间体以及制备具有下式的所述中间体的方法：其中R，R 1和R 2相同或不同并代表氢，卤素，硝基，羧基，腈，含有1至4个碳原子的烷氧基，烷氧基中含有1至4个碳原子的烷氧基羰基，含1至4个碳原子的烷基，氨基或羟基或R和R 1一起代表亚甲二氧基，对于氢，R 3表示氢或含有1至4个碳原子的烷基，R 4代表苯基，被1至3个相同或不同的取代基取代的苯基，所述取代基选自含1至4个碳原子的卤素，烷基和烷氧基，苯氧基，羟基，硝基，氨基，氰基，羧基，具有1至4个碳原子的烷氧基羰基，具有1至4个碳原子的烷酰基，亚甲二氧基，三氟甲基，苯基和在烷基中具有1至4个碳原子的二烷基氨基部分或萘基，虚线表示任选的双键。还公开了药学上可接受的酸加成盐和季铵盐。

10. 发明授权

US4321377A Substituted-4-oxo-1,6,7,8-tetrahydro-4H-pyrido[1,2-a]pyrimidines 失效
标题翻译：取代的-4-氧代-1,6,7,8-四氢-4H-吡啶并[1,2-a]嘧啶
公开(公告)号：US4321377A
公开(公告)日：1982-03-23
申请号：US35279
申请日：1979-05-02
申请人： Istvan Hermecz , Zoltan Meszaros , Istvan Bitter , Agnes Horvath , Lelle Vasvari nee Debreczy
发明人： Istvan Hermecz , Zoltan Meszaros , Istvan Bitter , Agnes Horvath , Lelle Vasvari nee Debreczy
IPC分类号： C07D471/04 , C07D487/04 , A61K31/505
CPC分类号： C07D471/04 , C07D487/04
摘要： Nitrogen bridgehead compounds (pyrido-[1,2-a]-pyrimidine derivatives) which are useful intermediates in the making of known compounds of this class and which themselves possess PG-antagonist, analgesic, antiartheriosclerotic, tranquilizing and like pharmaceutical activity.
摘要翻译：氮桥头钉化合物（吡啶并[1,2-a] - 嘧啶衍生物），它们是制备本类已知化合物的有用中间体，其本身具有PG拮抗剂，止痛剂，抗动物硬化剂，镇静剂和类似的药物活性。

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