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1. 发明授权

US4035491A Pharmaceutical composition having synergistic analgesic activity and containing azidomorphine or azidocodeine 失效
标题翻译：药物组合物具有协同镇痛活性，并含有叠氮吗啡或叠氮基
公开(公告)号：US4035491A
公开(公告)日：1977-07-12
申请号：US700782
申请日：1976-06-29
申请人： Jozsef Knoll , Zsuzsanna Furst , Zoltan Meszaros , Gabor Nagy , Agoston David , Rezso Bognar , Sandor Makleit , Gyula Valovics
发明人： Jozsef Knoll , Zsuzsanna Furst , Zoltan Meszaros , Gabor Nagy , Agoston David , Rezso Bognar , Sandor Makleit , Gyula Valovics
IPC分类号： A61K31/655 , A61K31/485 , A61K31/505
CPC分类号： A61K31/655
摘要： A pharmaceutical composition with synergistic analgesic effect which comprises an effective amount of 6-desoxy-6-azido-14-hydroxy-7,8-dihydro morphine or codeine or an analgesically effective salt thereof and an effective amount of a compound ##STR1## wherein R.sup.1 and R.sup.2 are lower alkyl and R.sup.3 is hydrogen or lower alkyl, and the dotted lines represent hydrogenated or unsaturated bonds or an analgesically effective salt or quaternary compound thereof.
摘要翻译：具有协同镇痛作用的药物组合物，其包含有效量的6-脱氧-6-叠氮基-14-羟基-7,8-二氢吗啡或可待因或其镇痛有效盐和有效量的化合物（IMAGE）（ II）其中R1和R2是低级烷基，R3是氢或低级烷基，虚线代表氢化或不饱和键或其镇痛有效的盐或季铵化合物。

2. 发明授权

US3969519A Pharmaceutical composition having synergistic analgesic activity and containing azidomorphine or azidocodeine 失效
标题翻译：药物组合物具有协同镇痛活性，并含有叠氮吗啡或叠氮基
公开(公告)号：US3969519A
公开(公告)日：1976-07-13
申请号：US536402
申请日：1974-12-26
申请人： Jozsef Knoll , Zsuzsanna Furst , Zoltan Meszaros , Gabor Nagy , Agoston David , Rezso Bognar , Sandor Makleit , Gyula Valovics
发明人： Jozsef Knoll , Zsuzsanna Furst , Zoltan Meszaros , Gabor Nagy , Agoston David , Rezso Bognar , Sandor Makleit , Gyula Valovics
IPC分类号： A61K31/655 , A61K31/505 , A61K31/485
CPC分类号： A61K31/655
摘要： A pharmaceutical composition having synergistic analgesic effect which includes an azido compound of the formula: ##SPC1## namely an azido morphine or an azido codeine, and at least one compound of the formula: ##SPC2##The synergistic composition has been found to have less narcotic side effects than morphine and equal or better analgesic properties.
摘要翻译：一种具有协同止痛效果的药物组合物，其包含下式的叠氮化合物：

3. 发明授权

US4027024A 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：US4027024A
公开(公告)日：1977-05-31
申请号：US649237
申请日：1976-01-15
申请人： Jozsef Knoll , Zsuzsanna Furst , Zoltan Meszaros , Peter Szentmiklosi , Agoston David , Istvan Hermecz , Attila Mandi , Rezso Bognar , Sandor Makleit , Gyula Valovics , Laszlo Szavik , 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 Szavik , Sandor Nagy
IPC分类号： A61K31/655 , A61K31/485 , A61K31/505
CPC分类号： A61K31/655
摘要： Pharmaceutical compositions of synergistic analgesic activity are provided which comprise an azido compound of the following formula: ##STR1## or a salt thereof wherein R is hydrogen, methyl, ethyl, acetyl or morpholino-methyl and a compound of the formula: ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 are hydrogen or lower alkyl and the dotted lines represent hydrogenated bonds or olefinic bonds and pharmaceutically acceptable salts and quaternary salts thereof, in admixture with suitable inert solid or liquid carriers or dilutents.
摘要翻译：提供协同镇痛活性的药物组合物，其包含下式的叠氮化合物：其中R是氢，甲基，乙基，乙酰基或吗啉代甲基的下式的化合物：其中 R1，R2，R3是氢或低级烷基，虚线代表氢化键或烯键及其药学上可接受的盐和季盐，与合适的惰性固体或液体载体或稀释剂混合。

4. 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。

5. 发明授权

US4167636A 7,8-Dihydroisomorphine derivative, namely azidoethylmorphine 失效
标题翻译： 7,8-二氢异吗啡衍生物，即叠氮基乙基吗啡
公开(公告)号：US4167636A
公开(公告)日：1979-09-11
申请号：US891195
申请日：1978-03-29
申请人： Rezso Bognar , Sandor Makleit , Geza Kiss , Sandor Berenyi , Terez Mile , Jozsef Knoll , Sandor Elek , Istvan Gyoker , Attila Zoltai , Gyorgy Toth , Laszlo Litkei
发明人： Rezso Bognar , Sandor Makleit , Geza Kiss , Sandor Berenyi , Terez Mile , Jozsef Knoll , Sandor Elek , Istvan Gyoker , Attila Zoltai , Gyorgy Toth , Laszlo Litkei
IPC分类号： C07D489/00 , C07D489/02 , A61K31/485
CPC分类号： C07D489/02 , C07D489/00 , Y10S514/849
摘要： Azidoethylmorphine, a new 7,8-dihydroisomorphine derivative, has excellent antitussive effects without respiration depression.
摘要翻译：新的7,8-二氢异吗啡衍生物叠氮乙基吗啡具有无呼吸抑制的优异的镇咳作用。

6. 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。

7. 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。

8. 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。

9. 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。

10. 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。

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