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1. 发明授权

US08674120B2 Process for manufacturing zeranol 有权
标题翻译：制造Zeranol的方法
公开(公告)号：US08674120B2
公开(公告)日：2014-03-18
申请号：US13127392
申请日：2009-11-03
申请人： John Richard Bethell , Gary Robert Reid , Krista Marie Affleck , Tibor Breining
发明人： John Richard Bethell , Gary Robert Reid , Krista Marie Affleck , Tibor Breining
IPC分类号： C07D493/00
CPC分类号： C07D313/00
摘要： This invention is directed generally to a process for producing Zeranol that eliminates high pressure and high temperature hydrogenations and provides high selectivity for Zeranol at improved yields.
摘要翻译：本发明一般涉及消除高压和高温氢化的Zeranol生产方法，并以提高的产率为Zeranol提供高选择性。

2. 发明授权

US4452982A Process for the preparation of nitrogen-bridgehead condensed pyrimidine compounds, and pharmaceutical compositions containing them 失效
标题翻译：氮桥头浓缩嘧啶化合物的制备方法和含有它们的药物组合物
公开(公告)号：US4452982A
公开(公告)日：1984-06-05
申请号：US148238
申请日：1980-05-09
申请人： Istvan Hermecz , Tibor Breining , Lelle Vasvari nee Debreczy , Agnes Horvath , Jozsef Kokosi
发明人： Istvan Hermecz , Tibor Breining , Lelle Vasvari nee Debreczy , Agnes Horvath , Jozsef Kokosi
IPC分类号： A61K31/505 , A61K31/519 , A61P11/00 , A61P37/08 , C07D471/04 , C07D239/70
CPC分类号： C07D471/04
摘要： A process is disclosed for the preparation of compounds of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen or lower alkyl;R.sup.3 is carboxy, lower alkoxycarbonyl, carbamoyl, carbamoyl substituted by one or two lower alkyl groups, or cyano;R.sup.4 is hydrogen, lower alkyl, phenyl, naphthyl, phenyl or naphthyl substituted by at least one fluoro, chloro, bromo, iodo, lower alkyl, lower alkoxy, hydroxy, carboxy, or phenyl, pyridyl or tetrazolyl; andR.sup.5 is hydrogen or lower alkyl; or a pharmaceutically acceptable salt, hydrate, stereoisomer, optically active isomer, geometric isomer, or tautomer thereof, which comprises the step of aminating a racemic or optically active compound of the formula (II) ##STR2## wherein X is halogen with a compound of the formula (III) ##STR3## or a pharmaceutically acceptable acid addition salt thereof. The compound of formula (II) possess antiallergic, especially antiasthma, activity.
摘要翻译：公开了制备式（I）化合物的方法，其中R 1和R 2各自为氢或低级烷基; R3是羧基，低级烷氧基羰基，氨基甲酰基，被一个或两个低级烷基取代的氨基甲酰基，或氰基; R4是氢，低级烷基，苯基，萘基，苯基或被至少一个氟，氯，溴，碘，低级烷基，低级烷氧基，羟基，羧基或苯基，吡啶基或四唑基取代的萘基。 R5是氢或低级烷基; 或其药学上可接受的盐，水合物，立体异构体，旋光异构体，几何异构体或其互变异构体，其包括将式（II）的外消旋或旋光活性化合物胺化的步骤，其中X是卤素，式（III）或其药学上可接受的酸加成盐。式（II）化合物具有抗过敏，特别是抗哮喘作用。

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

US5606037A Processes antineoplastic heteronaphthoquinones 失效
标题翻译：处理抗肿瘤异黄酮
公开(公告)号：US5606037A
公开(公告)日：1997-02-25
申请号：US401492
申请日：1995-03-10
申请人： Giorgio Attardo , Tibor Breining , Marc Courchesne , Serge Lamothe , Jean-Fran.cedilla.ois Lavall ee , Dieu Nguyen , Rabindra Rej , Yves St-Denis , Wuyi Wang , Yao-Chang Xu , France Barbeau , Elaine Lebeau , Jean L. Kraus
发明人： Giorgio Attardo , Tibor Breining , Marc Courchesne , Serge Lamothe , Jean-Fran.cedilla.ois Lavall ee , Dieu Nguyen , Rabindra Rej , Yves St-Denis , Wuyi Wang , Yao-Chang Xu , France Barbeau , Elaine Lebeau , Jean L. Kraus
IPC分类号： C07D311/76 , C07D311/92 , C07D335/08 , C07D493/04 , C07H15/252 , C07H17/00 , C07H17/04 , C07H17/08 , C07H1/00 , C07C50/22
CPC分类号： C07D311/76 , C07D311/92 , C07D335/08 , C07D493/04 , C07H15/252 , C07H17/00 , C07H17/04 , C07H17/08
摘要： This invention relates to a naphthoquinone derivatives, to processes and to intermediates for preparing these derivatives, to pharmaceutical composition and to the use of these derivatives as antitumor agents in mammals.
摘要翻译：本发明涉及萘醌衍生物，制备这些衍生物的方法和中间体，以及这些衍生物作为哺乳动物抗肿瘤剂的用途。

5. 发明授权

US4588526A Bronchodilatory azepino(1,2-A)pyrimidine derivatives and acid addition salts thereof and bronchodilating pharmaceutical compositions containing same 失效
标题翻译：支气管佐剂（1,2-A）嘧啶衍生物及其酸加成盐和含有其的支气管扩张药物组合物
公开(公告)号：US4588526A
公开(公告)日：1986-05-13
申请号：US550937
申请日：1983-11-10
申请人： Istvan Hermecz , Lelle Vasvari nee Debreczy , Agnes Horvath , Jozsef Kokosi , Sandor Virag , Tibor Breining
发明人： Istvan Hermecz , Lelle Vasvari nee Debreczy , Agnes Horvath , Jozsef Kokosi , Sandor Virag , Tibor Breining
IPC分类号： A61K31/519 , A61K31/55 , A61P11/08 , C07D487/04 , A61K31/505
CPC分类号： C07D487/04
摘要： The invention relates to new azepino[1,2-a]pyrimidine derivatives--of the general formula ##STR1## wherein p=1, 2 and acid addition salts thereof which can be prepared by(a) reacting a compound of the formula ##STR2## with a compound of the general formula ##STR3## wherein p is as defined above and R.sup.7 is alkoxycarbonyl containing 2 to 5 carbon atoms or carboxamido or(b) reacting a compound of the general formula ##STR4## wherein R.sup.8 is alkyl containing 1 to 4 carbon atoms with a compound of the general formula ##STR5## wherein R.sup.7 is as defined above and if desired converting a compound of the general formula I to acid addition salt thereof or setting it free from the salt thereof.The new compounds show bronchodilatory activity.
摘要翻译：本发明涉及通式为其中p = 1,2及其酸加成盐的通式为其中的氮杂[1,2-a]嘧啶衍生物及其酸加成盐，其可通过（a）使式图像II与具有通式III的化合物，其中p如上所定义，R 7是含有2至5个碳原子的烷氧基羰基或甲酰胺基，或（b）使通式为IV的化合物其中R8为含有1至4个碳原子的烷基与通式为其中R 7如上所定义的化合物反应，如果需要，将通式I的化合物转化为其酸加成盐或使其不含盐。新化合物显示支气管扩张活性。

6. 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。

7. 发明授权

US5736523A Antineoplastic heteronapthoquinones 失效
标题翻译：抗肿瘤异二氢醌
公开(公告)号：US5736523A
公开(公告)日：1998-04-07
申请号：US401493
申请日：1995-03-10
申请人： Giorgio Attardo , Tibor Breining , Marc Courchesne , Serge Lamothe , Jean-Fran.cedilla.ois Lavallee , Dieu Nguyen , Rabindra Rej , Yves St-Denis , Wuyi Wang , Yao-Chang Xu , France Barbeau , Elaine Lebeau , Jean Louis Kraus
发明人： Giorgio Attardo , Tibor Breining , Marc Courchesne , Serge Lamothe , Jean-Fran.cedilla.ois Lavallee , Dieu Nguyen , Rabindra Rej , Yves St-Denis , Wuyi Wang , Yao-Chang Xu , France Barbeau , Elaine Lebeau , Jean Louis Kraus
IPC分类号： C07D311/76 , C07D311/92 , C07D335/08 , C07D493/04 , C07H15/252 , C07H17/00 , C07H17/04 , C07H17/08 , A61K31/70 , C07H15/24
CPC分类号： C07D311/76 , C07D311/92 , C07D335/08 , C07D493/04 , C07H15/252 , C07H17/00 , C07H17/04 , C07H17/08
摘要： This invention relates to a naphthoquinone derivatives, to processes and to intermediates for preparing these derivatives, to pharmaceutical composition and to the use of these derivatives as antitumor agents in mammals.
摘要翻译：本发明涉及萘醌衍生物，制备这些衍生物的方法和中间体，以及这些衍生物作为哺乳动物抗肿瘤剂的用途。

8. 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。

9. 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。

10. 发明授权

US4367229A 3-Substituted-tetrahydro-pyrrolo[1,2-a]pyrimidines and pharmaceutical compositions 失效
标题翻译： 3-取代的四氢 - 吡咯并[1,2-a]嘧啶和药物组合物
公开(公告)号：US4367229A
公开(公告)日：1983-01-04
申请号：US148239
申请日：1980-05-09
申请人： Jozsef Kokosi , Istvan Hermecz , Zoltan Meszaros , Gyorgy Szasz , Lelle Vasuarl nee Debreczy , Agnes Horvath , Tibor Breining
发明人： Jozsef Kokosi , Istvan Hermecz , Zoltan Meszaros , Gyorgy Szasz , Lelle Vasuarl nee Debreczy , Agnes Horvath , Tibor Breining
IPC分类号： A61K31/505 , A61P9/08 , A61P9/10 , C07D487/04
CPC分类号： C07D487/04
摘要： Chemical compounds having an effect on the circulatory system have the formulas ##STR1## or a mixture thereof, or a pharmaceutically suitable acid-addition salt or quaternary salt thereof, whereinR is hydrogen or lower alkyl,R.sup.1 is lower alkyl, phenyl, carboxyl, lower alkoxycarbonyl, nitrile, carbamoyl or carbohydrazido,R.sup.2 is hydrogen or lower alkyl,and wherein the formula I R.sup.2 is hydrogen then R.sup.1 is other than nitrile, alkoxycarbonyl or propyl.
摘要翻译：对循环系统具有影响的化合物具有式（I）或（II）或其混合物或其药学上合适的酸加成盐或季盐，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，R 2是氢或低级烷基，其中式I R 2是氢，R 1不是腈，烷氧基羰基或丙基。

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