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1. 发明授权

US4434152A Time-release 失效
标题翻译：时间释放
公开(公告)号：US4434152A
公开(公告)日：1984-02-28
申请号：US372049
申请日：1982-04-26
申请人： Tibor Horvath , Agnes Udvardy , Agoston David , Katalin Marmarosi nee Kellner
发明人： Tibor Horvath , Agnes Udvardy , Agoston David , Katalin Marmarosi nee Kellner
IPC分类号： A61K9/20 , A61K9/22 , A61K31/495 , A61K9/24
CPC分类号： A61K31/495 , A61K9/2004
摘要： Time-release pharmaceutical compositions, suitable for oral administration, are disclosed, which comprise as active ingredient 50 to 70% by weight of a compound of the formula (I) ##STR1## or the formula (Ia) ##STR2## wherein R is hydrogen or --CH.sub.2 COOH,R.sup.1 is hydrogen or alkyl having 1 to 4 carbon atoms,R.sup.2 is alkyl having 1 to 4 carbon atoms, alkoxycarbonyl having 2 to 5 carbon atoms, carbamoly or ureido,R.sup.3 is hydrogen or methyl, and the dotted line stands for two hydrogens or another bond, or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof, and which further include 4 to 8% by weight of a hydrophobic substance with a great specific surface;7 to 12% by weight of a lipoid;8 to 12% by weight of a polyoxy compound;4 to 9% by weight of a binding agent; and0.5 to 4% by weight of an acid stabilizer.
摘要翻译：公开了适用于口服给药的时间释放药物组合物，其包含作为活性成分的50至70重量％的式（I）化合物（I）或式（Ia）的化合物，其中 R是氢或-CH 2 COOH，R 1是氢或具有1至4个碳原子的烷基，R 2是具有1至4个碳原子的烷基，具有2至5个碳原子的烷氧基羰基，氨基甲酰基或脲基，R 3是氢或甲基，线代表两个氢或另一个键，或其药学上可接受的酸加成盐或季铵盐，并且还包括4至8重量％的具有大比表面积的疏水性物质; 7至12重量％的脂质; 8〜12重量％的聚氧化合物; 4〜9重量％的粘合剂; 和0.5〜4重量％的酸稳定剂。

2. 发明授权

US4335097A Stabilized, prostaglandin-containing tablets with controlled rate of solubility, for local use and process for the preparation thereof 失效
标题翻译：稳定的含前列腺素的片剂，具有控制的溶解度，用于局部使用，并且其制备方法
公开(公告)号：US4335097A
公开(公告)日：1982-06-15
申请号：US225361
申请日：1981-01-15
申请人： Agoston David , Tibor Horvath , Csaba Kiss , Gabor Nagy , Kalman Simon , Ilona Simonidesz nee Vermes , Agnes Udvardi , Sandor Virag
发明人： Agoston David , Tibor Horvath , Csaba Kiss , Gabor Nagy , Kalman Simon , Ilona Simonidesz nee Vermes , Agnes Udvardi , Sandor Virag
IPC分类号： A61K9/00 , A61K9/20 , A61K31/557 , A61K31/19 , A61K31/215
CPC分类号： A61K9/0034 , A61K31/557 , A61K9/006 , A61K9/2004
摘要： The invention relates to stabilized, prostaglandin-containing tablets with controlled rate of solubility, for local use and a process for the preparation thereof. The tablets according to the invention comprise 0.2 to 20% by weight of one or more natural or synthetic prostaglandins, 0.4 to 40% by weight of a non-toxic buffer, which adjusts the pH of the liquid film formed on the surface of the solid phase due to air humidity, to 3 to 5, 1 to 50% by weight of stearic acid, 0 to 15% by weight of an alkali earth metal stearate, 10 to 95% by weight of lactose and/or mannite, 0 to 15% by weight of a further granulation aid, 1 to 30% by weight of a disintegrating agent and optionally 0.5 to 10% by weight of a flavoring and aroma substance and are prepared under a pressure of 500 to 2000 kp./cm.sup.2. (49.03 to 196.13 MPa).
摘要翻译：本发明涉及稳定的含前列腺素的片剂，其具有受控的溶解度，用于局部使用及其制备方法。根据本发明的片剂包含0.2至20重量％的一种或多种天然或合成前列腺素，0.4至40重量％的无毒性缓冲液，其调节在固体表面上形成的液膜的pH 相对于空气湿度为3〜5重量％，1〜50重量％的硬脂酸，0〜15重量％的碱土金属硬脂酸酯，10〜95重量％的乳糖和/或甘露醇，0〜15 重量％的另外的造粒助剂，1至30重量％的崩解剂和任选的0.5至10重量％的调味香料，并在500至2000kp. / cm 2的压力下制备。（49.03〜196.13MPa）。

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

US4404189A Synergistic antimicrobial compositions 失效
标题翻译：协同抗菌组合物
公开(公告)号：US4404189A
公开(公告)日：1983-09-13
申请号：US226615
申请日：1981-01-21
申请人： Gabor Kulcsar , Gyula Sebestyen , Agoston David , Tibor Zilahi
发明人： Gabor Kulcsar , Gyula Sebestyen , Agoston David , Tibor Zilahi
IPC分类号： A61K31/65 , A61K35/00
CPC分类号： A61K31/70 , A61K31/65
摘要： A synergistic antimicrobial active ingredient for a pharmaceutical or veterinary composition comprises 5 to 50 percent by weight of a primycin component which consists of a primycin fermentation product of Thermonospora galeriensis and 95 to 50 percent by weight of at least one other component selected from the group which consists of doxycyline compounds and sisomicin compounds. The doxycycline compounds are selected from the group which consists of doxycycline, salts thereof with mineral acids, and doxycycline tryclate. The sisomicin compounds are selected from the group which consists of sisomicin, substituted sisomicins with substitution at the N atom by lower alkyl, hydroxyl lower alkyl, lower aminoalkyl and lower alkanoyl, and sisomicin acid salts.
摘要翻译：用于药物或兽医组合物的协同抗微生物活性成分包含5-50重量％的伯霉素组分，所述伯霉素组分由热霉菌属（Thermomonospora galeriensis）的伯霉素发酵产物和95至50重量％的至少一种选自以下的组中由多西环素化合物和西索米星化合物组成。多西环素化合物选自由多西环素，其与无机酸的盐和多西环素三环酸组成的组。西索米星化合物选自西索霉素，在N原子被低级烷基取代的取代的西索米星，羟基低级烷基，低级氨基烷基和低级烷酰基以及西索米星酸盐组成的组。

5. 发明授权

US4102886A Process for the preparation of benzo(a)quinolizidine derivatives 失效
标题翻译：苯并（a）喹嗪衍生物的制备方法
公开(公告)号：US4102886A
公开(公告)日：1978-07-25
申请号：US624470
申请日：1975-10-21
申请人： Csaba Szantay , Lajos Szabo , Laszlo Toke , Istvan Toth , Sandor Virag , Erzsebet Kanyo , Agoston David
发明人： Csaba Szantay , Lajos Szabo , Laszlo Toke , Istvan Toth , Sandor Virag , Erzsebet Kanyo , Agoston David
IPC分类号： C07D455/06 , C07D491/056 , C07D491/14
CPC分类号： C07D491/14 , C07D455/06
摘要： A process for the preparation of a compound of the formula I or a salt thereof ##STR1## wherein R.sup.1 and R.sup.2 each represent hydrogen or a C.sub.1-4 alkoxy group, or together form a methylenedioxy group;R.sup.3, r.sup.4, r.sup.5 and R.sup.6 are the same or different and are hydrogen or a group of the formula --CH.sub.2 --(CH.sub.2).sub.n --R.sup.7 with the proviso that at least one of the members R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is other than hydrogen; R.sup.7 is carboxyl or a carboxylic acid derivative group;N = 0.1 or 2 which comprises reacting a compound of the formula II ##STR2## with an organic secondary amine and reacting the N-amine of the formula III ##STR3## thus obtained wherein R.sup.8 and R.sup.9 each represent a C.sub.1-5 alkyl group, or together with the adjacent nitrogen atom form a 5- or 6-membered heterocyclic ring which can contain a further heteroatom, with a compound of the formula IVch.sub.2 .dbd. ch -- (ch.sub.2).sub.n -- R.sup.10 (IV)wherein R.sup.10 is a cyano or alkoxycarbonyl group.
摘要翻译：一种制备式I化合物或其盐的方法，其中R 1和R 2各自代表氢或C 1-4烷氧基，或一起形成亚甲二氧基; R 3，R 4，R 5和R 6相同或不同，为氢或式-CH 2 - （CH 2）n -R 7的基团，条件是至少有一个R 3，R 4，R 5和R 6不是氢; R7是羧基或羧酸衍生物基团; N = 0.1或2，其包含用有机仲胺反应式II化合物，并使由此得到的式III的N-胺反应，其中R 8和R 9各自表示C 1-5烷基，或者与相邻的氮原子一起形成可以含有另外的杂原子的5或6元杂环与式IV的化合物CH2 = CH-（CH2）n-R10（IV），其中R10是氰基或烷氧基羰基。

6. 发明授权

US3954986A Pharmaceutical composition having synergistic analgesic activity 失效
标题翻译：具有协同止痛活性的药物组合物
公开(公告)号：US3954986A
公开(公告)日：1976-05-04
申请号：US415749
申请日：1973-11-14
申请人： Jozsef Knoll , Zsuzsanna Furst , Zoltan Meszaros , Peter Szentmiklosi , Agoston David , Istvan Hermecz , Attila Mandi , Rezso Bognar , Sandor Makleit , Gyula Valovics , Laszlo Szlavik , Sandor Nagy
发明人： Jozsef Knoll , Zsuzsanna Furst , Zoltan Meszaros , Peter Szentmiklosi , Agoston David , Istvan Hermecz , Attila Mandi , Rezso Bognar , Sandor Makleit , Gyula Valovics , Laszlo Szlavik , Sandor Nagy
IPC分类号： A61K31/655 , A61K31/505 , A61K31/485
CPC分类号： A61K31/655
摘要： An analgesic substitute for morphine comprising the synergistic combination of azidomorphine or azidocodeine with a pyrimidazolium.
摘要翻译：吗啡的止痛剂替代物，其包含叠氮吗啡或叠氮基与佐剂的协同组合。

7. 发明授权

US4342871A Benzo(a)quinolizidine derivatives 失效
标题翻译：苯并（a）喹嗪啶衍生物
公开(公告)号：US4342871A
公开(公告)日：1982-08-03
申请号：US744608
申请日：1976-11-24
申请人： Csaba Szantay , Lajos Szabo , Laszlo Toke , Istvan Toth , Sandor Virag , Erzsebet Kanyo , Agoston David
发明人： Csaba Szantay , Lajos Szabo , Laszlo Toke , Istvan Toth , Sandor Virag , Erzsebet Kanyo , Agoston David
IPC分类号： C07D455/06 , C07D491/056 , C07D491/14 , C07D455/03 , A61K31/47
CPC分类号： C07D491/14 , C07D455/06
摘要： An antiphlogistic compound of the formula (I) ##STR1## or a pharmaceutically effective salt thereof wherein R.sup.1 and R.sup.2 are hydrogen or C.sub.1-4 alkoxy or together form a methylenedioxy group;R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are hydrogen or a group of the formula --CH.sub.2 --(CH.sub.2).sub.n -R.sup.7 with the proviso that at least one of R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is other than hydrogen;R.sup.7 is a carboxylic group or a carboxylic acid derivative group; n=0, 1 or 2, provided that if R.sup.3, R.sup.4 and R.sup.5 are hydrogen and R.sup.7 in the group R.sup.6 is cyano or alkoxycarbonyl, and n=1, then R.sup.1 and R.sup.2 are hydrogen, C.sub.2-4 alkoxy, or together form a methylenedioxy group.
摘要翻译：式（I）的消炎化合物（I）或其药学上有效的盐，其中R 1和R 2是氢或C 1-4烷氧基或一起形成亚甲二氧基; R3，R4，R5和R6是氢或式-CH2-（CH2）n-R7的基团，条件是R3，R4，R5和R6中的至少一个不是氢; R7是羧基或羧酸衍生物基团; n = 0,1或2，条件是如果R3，R4和R5是氢，R6中的R7是氰基或烷氧基羰基，n = 1，则R1和R2是氢，C2-4烷氧基或一起形成亚甲二氧基。

8. 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。

9. 发明授权

US4049639A 5-Amido imido triazene triazoles and pyrazoles with photographic and antimycotic utility 失效
标题翻译： 5-酰氨基亚氨基三氮烯三唑和具有照相和抗霉菌作用的吡唑
公开(公告)号：US4049639A
公开(公告)日：1977-09-20
申请号：US549761
申请日：1975-02-13
申请人： Jozsef Schawartz , Maria Hornyak , Eva Majorszki , Agoston David , Gabor Horvath
发明人： Jozsef Schawartz , Maria Hornyak , Eva Majorszki , Agoston David , Gabor Horvath
IPC分类号： C07D231/38 , C07D233/90 , C07D249/04 , G03C1/35 , C07C107/00 , C07C107/04 , G03C5/30
CPC分类号： C07D231/38 , C07D233/90 , C07D249/04 , G03C1/35
摘要： Triazene derivatives of the formula ##STR1## wherein X is = CH-- or nitrogen,Y is --CH = or nitrogen,R and R' are substituted or unsubstituted alkyl, aryl, arakyl or cycloarkyl. The compounds are effective as photographic toners and additives to photographic developers and as antimycotic agents in animal therapy.
摘要翻译：其中X为= CH-或氮，Y为-CH =或氮，R和R'为取代或未取代的烷基，芳基，芳烷基或环烷基。这些化合物作为照相调色剂和添加剂作为动物疗法中的照相显影剂和抗真菌剂是有效的。

10. 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。

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