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1. 发明授权

US4988730A Diphenkylpropylamines for the therapy of heart disease 失效
标题翻译：用于治疗心脏病的二苯基丙胺
公开(公告)号：US4988730A
公开(公告)日：1991-01-29
申请号：US385539
申请日：1989-07-21
申请人： Dezso Korbonits , Pal Kiss , Laszlo Szekeres , Gyula Papp , Gabor Kovacs , Andrea Santane Csutor , Sandor Virag , Eva Udvari , Imre Bata , Katalin Marmarosi nee Kellner , Laszlo Tardos , Peter Kormoczy , Vera Gergely , Zoltan Vargai
发明人： Dezso Korbonits , Pal Kiss , Laszlo Szekeres , Gyula Papp , Gabor Kovacs , Andrea Santane Csutor , Sandor Virag , Eva Udvari , Imre Bata , Katalin Marmarosi nee Kellner , Laszlo Tardos , Peter Kormoczy , Vera Gergely , Zoltan Vargai
IPC分类号： C07C215/50 , A61K31/13 , A61K31/135 , A61K31/137 , A61K31/16 , A61K31/165 , A61K31/335 , A61K31/36 , A61P3/00 , A61P9/06 , A61P9/08 , A61P9/10 , C07C20060101 , C07C27/00 , C07C67/00 , C07C209/00 , C07C209/08 , C07C209/24 , C07C209/26 , C07C209/62 , C07C209/68 , C07C211/00 , C07C211/03 , C07C211/16 , C07C211/26 , C07C211/27 , C07C211/29 , C07C211/43 , C07C213/00 , C07C217/10 , C07C217/54 , C07C217/56 , C07C217/58 , C07C227/10 , C07C227/16 , C07C229/34 , C07C229/38 , C07C231/00 , C07C231/12 , C07C233/42 , C07C233/43 , C07C233/67 , C07D311/48 , C07D317/00 , C07D317/48 , C07D317/58
CPC分类号： C07D317/58 , C07C211/27 , C07C211/29 , C07C217/58 , C07C233/43
摘要： The invention relates to novel diphenylpropylamine derivatives of the general formula (I). ##STR1## R.sup.1 stands for hydrogen or a methyl group; R.sup.2 stands for hydrogen, a methyl or n-decyl group;Z means a phenyl group substituted by R.sup.3, R.sup.4 and R.sup.5, whereinR.sup.3 means hydrogen, fluorine, chlorine or bromine, or a nitro, C.sub.1-12 alkyl, C.sub.1-4 alkoxy, phenoxy or benzyloxy group;R.sup.4 and R.sup.5 represent hydrogen, chlorine or a hydroxy, alkoxy, benzyloxy, acetamino or carboxy group; orR.sup.4 and R.sup.5 together form a methylendioxy group; orZ may stand for a 4-methoxynaphtyl or 4-ethoxy-naphthyl group; andR.sup.6 stands for hydrogen or fluorine, with the proviso that each of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 cannot simultaneously stand for hydrogen, as well as their physiologically acceptable acid addition salts.The invention also relates to a process for the preparation of these compounds and to the pharmaceutical compositions containing these compounds.The compounds of the general formula (I) can preferably be used for the treatment of cardiovascular diseases.
摘要翻译：本发明涉及通式（I）的新型二苯基丙胺衍生物。（I）R1代表氢或甲基; R2代表氢，甲基或正癸基; Z表示被R 3，R 4和R 5取代的苯基，其中R 3表示氢，氟，氯或溴，或硝基，C 1-12烷基，C 1-4烷氧基，苯氧基或苄氧基; R4和R5代表氢，氯或羟基，烷氧基，苄氧基，乙酰氨基或羧基; 或R4和R5一起形成甲基二氧基; 或Z可以代表4-甲氧基萘基或4-乙氧基 - 萘基; 并且R6代表氢或氟，条件是R1，R2，R3，R4和R6各自不能同时代表氢，以及它们的生理上可接受的酸加成盐。本发明还涉及制备这些化合物的方法和含有这些化合物的药物组合物。通式（I）的化合物可优选用于治疗心血管疾病。

2. 发明授权

US4010193A Basic ester 失效
标题翻译：碱性酯
公开(公告)号：US4010193A
公开(公告)日：1977-03-01
申请号：US354732
申请日：1973-04-26
申请人： Kalman Harsanyi , Laszlo Szekeres , Gergely Heja , Gyula Papp , Dezso Korbonits , Pal Kiss
发明人： Kalman Harsanyi , Laszlo Szekeres , Gergely Heja , Gyula Papp , Dezso Korbonits , Pal Kiss
IPC分类号： C07D233/60 , A61K31/135 , A61K31/138 , A61K31/24 , C07C67/00 , C07C213/00 , C07C213/08 , C07C217/16 , C07C219/14 , C07C219/24 , C07C219/28 , C07C301/00 , C07C303/40 , C07C311/00 , C07C311/29 , C07D213/80 , C07D215/48 , C07D261/18 , C07D307/68 , C07C93/24 , C07C93/20
CPC分类号： C07D213/80 , C07D261/18 , C07D307/68 , Y10S514/818
摘要： A basic ester having the formula ##STR1## wherein Ac is benzoyl substituted by at least two substituents selected from the group which consist of halogen atoms, lower alkyl, lower alkoxy, hydroxy, nitro and sulfamoyl, and A B are hydrogen or lower alkyl or are cycloalkyl together. The compounds are therapeutic for cardic conditions.
摘要翻译：具有式“IMAGE”的碱性酯，其中Ac是被至少两个选自卤素原子，低级烷基，低级烷氧基，羟基，硝基和氨磺酰基的取代基取代的苯甲酰基，AB是氢或低级烷基，或者是环烷基。这些化合物是治疗心脏病症的药物。

3. 发明授权

US4735965A 7-oxo-PGI.sub.2 -ephedrine salts and their pharmaceutical compositions and methods 失效
标题翻译： 7-氧代-PGI2-麻黄碱盐及其药物组合物和方法
公开(公告)号：US4735965A
公开(公告)日：1988-04-05
申请号：US868772
申请日：1986-05-28
申请人： Gabor Kovacs , Geza Galambos , Istvan Tomoskozi , Karoly Kanai , Peter Gyory , Peter Kormoczy , Istvan Stadler , Laszlo Szekeres , Gyula Papp , Eva Udvary , Pal Hadhazy , Jeno Marton , Gyorgy Dorman
发明人： Gabor Kovacs , Geza Galambos , Istvan Tomoskozi , Karoly Kanai , Peter Gyory , Peter Kormoczy , Istvan Stadler , Laszlo Szekeres , Gyula Papp , Eva Udvary , Pal Hadhazy , Jeno Marton , Gyorgy Dorman
IPC分类号： C07C59/90 , A61K31/135 , A61K31/19 , A61K31/34 , A61K31/557 , A61K31/5575 , A61P1/04 , A61P1/16 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P35/00 , A61P43/00 , C07C51/00 , C07C51/41 , C07C67/00 , C07C213/00 , C07C215/40 , C07C405/00 , C07D307/935 , C07D307/937 , C07D521/00
CPC分类号： C07D307/937
摘要： The invention relates to new 7-oxo-PGI.sub.2 -ephedrine salt analogues of the Formula I ##STR1## wherein A stands for --(CH.sub.2).sub.2 --, cis or trans --CH.dbd.CH-- or --C.tbd.C--;R.sup.1 is lower alkyl or hydrogen;B represents a chemical bond, --CH.sub.2 -- or --CR.sup.2 R.sup.3 ;R.sup.2 stands for lower alkyl or hydrogen;R.sup.3 represents lower alkyl or hydrogen;X is a chemical bond, --O-- or --CH.sub.2 --;R.sup.4 stands for C.sub.1-6 alkyl, C.sub.4-7 cycloalkyl, C.sub.1-6 fluoroalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, phenyl, substituted phenyl or heteroaryl.The salts of the Formula I show the same pharmacological profile as the sodium salt of PGI.sub.2, they inhibit blood aggregation and the secretion of gastric acid, are useful in the prevention of anginal attacks. Accordingly the salts of the present invention are useful in the prevention of peripheral vascular diseases, in improving circulation of extremities, in relieving the seriousness of cardiac infarction and also in the treatment and prevention of gastrointestinal ulcer and acute or chronical liver injury.
摘要翻译：本发明涉及式I的新的7-氧代-PGI-麻黄碱盐类似物，其中A代表 - （CH 2）2 - ，顺式或反式-CH = CH-或-C 3位C; R1是低级烷基或氢; B表示化学键，-CH 2 - 或-CR 2 R 3; R2代表低级烷基或氢; R3表示低级烷基或氢; X是化学键，-O-或-CH2-; R4代表C 1-6烷基，C 4-7环烷基，C 1-6氟代烷基，C 2-6烯基，C 2-6炔基，苯基，取代的苯基或杂芳基。式I的盐显示与PGI2的钠盐相同的药理学特征，它们抑制血液聚集和胃酸分泌，可用于预防心绞痛发作。因此，本发明的盐可用于预防周围血管疾病，改善四肢的循环，缓解心肌梗死的严重性，以及治疗和预防胃肠溃疡和急性或慢性肝损伤。

4. 发明授权

US4228164A Condensed purine derivatives useful for improving peripheral circulation 失效
标题翻译：用于改善外周循环的富集嘌呤衍生物
公开(公告)号：US4228164A
公开(公告)日：1980-10-14
申请号：US958526
申请日：1978-11-07
申请人： Rudolf Szebeni , Dezso Korbonits , Kalman Harsanyi , Molnar Leventene , Laszlo Szekeres , Gyula Papp , Gyula Sebestyen
发明人： Rudolf Szebeni , Dezso Korbonits , Kalman Harsanyi , Molnar Leventene , Laszlo Szekeres , Gyula Papp , Gyula Sebestyen
IPC分类号： C07D487/14 , C07D513/14 , A61K31/54 , A61K31/52 , C07D473/08
CPC分类号： C07D487/14 , C07D513/14
摘要： A compound of the formula ##STR1## wherein R is hydroxy, alkoxy or acyloxyQ is sulfur or a .dbd.N--R.sup.1 group, wherein R.sup.1 ishydrogen, C.sub.1-5 alkyl or aralkyl or C.sub.2-4 acyl, or a pharmaceutically acceptable acid addition salt thereof.
摘要翻译：式（I）的化合物其中R是羟基，烷氧基或酰氧基Q是硫或= N-R 1基，其中R 1是氢，C 1-5烷基或芳烷基或C 2-4酰基，或药学上其可接受的酸加成盐。

5. 发明授权

US3979397A Pharmaceutically effective novel 3,4-dihydro-1,2- and 1,3-thiozolo [4,3a] i s 失效
标题翻译：药学有效的新型3,4-二氢-1,2-和1,3-噻唑并{8,43a {9 {0异喹啉及其制备方法
公开(公告)号：US3979397A
公开(公告)日：1976-09-07
申请号：US473918
申请日：1974-05-28
申请人： Kalman Harsanyi , Kalman Takacs , Pal Kiss , Laszlo Szekeres , Gyula Papp , Eva Benedek
发明人： Kalman Harsanyi , Kalman Takacs , Pal Kiss , Laszlo Szekeres , Gyula Papp , Eva Benedek
IPC分类号： A61K31/47 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P11/16 , C07D217/08 , C07D277/60 , C07D513/04
CPC分类号： C07D513/04
摘要： The invention relates to new thiazoloisoquinolines of the general formula (I), or salts thereof, ##SPC1##WhereinA stands for a group of the formula ##EQU1## R.sup.1 stands for hydrogen, hydroxy, alkoxy or aralkoxy, R.sup.2 stands for hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.3 stands for hydrogen, alkyl, aryl, nitro, carboxy or a carboxy derivative, andY stands for oxygen, sulfur, or a group of the formula =N--R.sup.4, wherein R.sup.4 stands for hydrogen, alkyl, aryl, acyl, alkylsulfonyl or arylsulfonyl.These new compounds can be used in practice as heart medicines or respiratory analeptics.The new compounds according to the invention can be prepared as follows: an isoquinoline of the general formula (II) or a salt thereof ##SPC2##WhereinR.sup.5 stands for hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.6 stands for hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.7 stands for hydrogen, alkyl, aryl, carboxy or a carboxy derivative, andX stands for hydrogen, halogen or mercapto,Is reacted with a reactive carbonic acid derivative, provided that at least one of the reactants contains a sulfur atom, and/or an isoquinoline of the general formula (III) ##SPC3##wherein R.sup.5, R.sup.6 and R.sup.7 each have the same meanings as defined above, and Y' stands for oxygen, sulfur or a group of the formula =N--R.sup. 8, wherein R.sup.8 represents hydrogen, alkyl, aryl, acyl, arylsulfonyl or alkylsulfonyl, is oxidized, and/or substituents A', R.sup.5, R.sup.6 and R.sup.7 of the obtained thiazoloisoquinoline of the general formula (IA) ##SPC4##wherein A' stands for a group of the formula ##EQU2## and R.sup.5, R.sup.6, R.sup.7 and Y' each have the same meanings as defined above, are converted into those required in the end-products.
摘要翻译：本发明涉及通式（I）的新的噻唑并喹啉或其盐，其中A代表式-SC-基团，PARALLEL Y R1代表氢，羟基，烷氧基或芳烷氧基，R2代表氢，羟基，烷氧基或芳烷氧基，R3代表氢，烷基，芳基，硝基，羧基或羧基衍生物，Y代表氧，硫或式= N-R4的基团，其中R4代表氢，烷基，芳基，酰基，烷基磺酰基或芳基磺酰基。

6. 发明授权

US4163786A Thiazoloisoquinolines with coronary and respiratory effects 失效
标题翻译：具有冠状动脉和呼吸道作用的噻唑并喹啉
公开(公告)号：US4163786A
公开(公告)日：1979-08-07
申请号：US869791
申请日：1978-01-16
申请人： Kalman Harsanyi , Kalman Takacs , Pal Kiss , Laszlo Szekeres , Gyula Papp , Eva Benedek
发明人： Kalman Harsanyi , Kalman Takacs , Pal Kiss , Laszlo Szekeres , Gyula Papp , Eva Benedek
IPC分类号： C07D513/04 , A61K31/47
CPC分类号： C07D513/04
摘要： The invention relates to new thiazoloisoquinolines of the formula (I), or pharmaceutically acceptable salts thereof, ##STR1## wherein R.sup.1 is hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.2 is hydrogen, hydroxy, alkoxy or aralkoxy,R.sup.3 is hydrogen, cyano, alkyl, aryl, nitro, carboxy, carboalkoxy or carboxamido, andY is oxygen, sulfur, or a group of the formula .dbd.N--R.sup.4, wherein R.sup.4 stands for hydrogen, alkyl, aryl, acyl, alkyl-sulfonyl or arysulfonyl.These new compounds can be used in practice as heart medicines or respiratory analeptics.
摘要翻译：本发明涉及式（I）的新型噻唑并喹啉或其药学上可接受的盐，其中R 1是氢，羟基，烷氧基或芳烷氧基，R 2是氢，羟基，烷氧基或芳烷氧基，R 3是氢，氰基，烷基，芳基，硝基，羧基，烷氧基或甲酰胺基，Y是氧，硫或式= N-R4的基团，其中R4代表氢，烷基，芳基，酰基，烷基磺酰基或芳磺酰基。

7. 发明授权

US4062850A Thiazoloisoquinolines with coronary and respiratory effects 失效
标题翻译：具有冠状动脉和呼吸道作用的噻唑并喹啉
公开(公告)号：US4062850A
公开(公告)日：1977-12-13
申请号：US701130
申请日：1976-06-30
申请人： Kalman Harsanyi , Kalman Takacs , Pal Kiss , Laszlo Szekeres , Gyula Papp , Eva Benedek
发明人： Kalman Harsanyi , Kalman Takacs , Pal Kiss , Laszlo Szekeres , Gyula Papp , Eva Benedek
IPC分类号： C07D513/04 , A61K31/47
CPC分类号： C07D513/04
摘要： 1-Cyano-2-imino-2H,4H-5,6-dihydro-8,9-dimethoxy-1,2-thiazolo(3,2a)isoquinoline or 2-imino-2H,4H-5,6-dihydro-8,9-dimethoxy-1,2-thiazolo(3,2a)isoquinoline or a pharmaceutically acceptable salt thereof. These compounds are effective as heart medicines and respiratory analeptics.
摘要翻译： 1-氰基-2-亚氨基-2H，4H-5,6-二氢-8,9-二甲氧基-1,2-噻唑并（3,2a）异喹啉或2-亚氨基-2H，4H-5,6-二氢 -8,9-二甲氧基-1,2-噻唑并（3,2a）异喹啉或其药学上可接受的盐。这些化合物作为心脏药物和呼吸消毒剂是有效的。

8. 发明授权

US4530923A N-acetamilide, N-(phenoxy-2-propanol)- and N-(phenylamino-2-propanol)-cyclicamines 失效
标题翻译： N-乙酰苯胺，N-（苯氧基-2-丙醇）和N-（苯基氨基-2-丙醇） - 环胺
公开(公告)号：US4530923A
公开(公告)日：1985-07-23
申请号：US435493
申请日：1982-10-20
申请人： Jozsef Rakoczi , Edit Berenyi nee Poldermann , Bela Fekete , Laszlo Szekeres , Gyula Papp , Eva Keszthelyi nee Udvary
发明人： Jozsef Rakoczi , Edit Berenyi nee Poldermann , Bela Fekete , Laszlo Szekeres , Gyula Papp , Eva Keszthelyi nee Udvary
IPC分类号： C07D295/08 , A61K31/395 , A61K31/55 , A61P9/06 , C07D295/088 , C07D295/092 , C07D295/10 , C07D295/13 , C07D295/15 , C07D223/02 , A61K31/33
CPC分类号： C07D295/088 , C07D295/13 , C07D295/15
摘要： The invention relates to new cyclic imines of the general formula (I), ##STR1## wherein A represents carbonyl or hydroxymethylene,B is oxygen or imino,R stands for hydrogen or lower alkyl,X.sub.1 and X.sub.2 may be the same or different and represent hydrogen, halogen, lower alkyl or alkoxy, amino or nitro,n is 6 or 7, andm is 0 or 1,and pharmaceutically acceptable acid addition salts and quaternary salts thereof. The invention relates further to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds as the active ingredient and to a process for the preparation of said pharmaceutical compositions.The cyclic imine derivatives of the invention possess valuable antiarrhythmic properties and can be used to advantage in the treatment of cardiovascular diseases.
摘要翻译：本发明涉及通式（I）的新型环状亚胺，其中A代表羰基或羟基亚甲基，B是氧或亚氨基，R代表氢或低级烷基，X 1和X 2可以相同或不同，代表氢，卤素，低级烷基或烷氧基，氨基或硝基，n为6或7，m为0或1，以及其药学上可接受的酸加成盐和季盐。本发明进一步涉及制备所述化合物的方法，含有所述化合物作为活性成分的药物组合物和制备所述药物组合物的方法。本发明的环状亚胺衍生物具有有价值的抗心律失常性质，可用于治疗心血管疾病。

9. 发明授权

US4365064A 1,2,4-Oxadiazolin-5-one derivatives, process for their preparation and pharmaceutical compositions containing them 失效
标题翻译： 1,2,4-恶二唑啉-5-酮衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4365064A
公开(公告)日：1982-12-21
申请号：US196583
申请日：1980-10-14
申请人： Kalman Takacs , Ilona Kiss nee Ajzert , Antal Simay , Peter Literati Nagy , Maria Hetyey nee Papp , Marian Ecsery nee Puskas , Laszlo Szekeres , Gyula Papp , Sandor Viragh , Eva Udvardy
发明人： Kalman Takacs , Ilona Kiss nee Ajzert , Antal Simay , Peter Literati Nagy , Maria Hetyey nee Papp , Marian Ecsery nee Puskas , Laszlo Szekeres , Gyula Papp , Sandor Viragh , Eva Udvardy
IPC分类号： C07D413/06 , A61K20060101 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/435 , A61K31/47 , A61K31/475 , A61P9/08 , C07D20060101 , C07D217/00 , C07D217/04 , C07D217/16 , C07D271/00 , C07D271/06 , C07D273/04 , C07D401/06
CPC分类号： A61K31/41 , A61K31/415 , A61K31/42 , A61K31/435 , A61K31/47 , A61K31/475 , C07D217/00 , C07D217/04 , C07D217/16 , C07D271/00 , C07D271/06 , C07D273/04 , C07D401/06 , C07D413/06 , Y10S514/929 , Y10S514/96 , Y10S514/962
摘要： The invention concerns new compounds of the formula (I) ##STR1## wherein R.sup.1 is hydrogen, phenyl or phenyl substituted with at least one alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro;R.sup.2 is alkyl having 1 to 4 carbon atoms, cycloalkyl having 5 to 7 carbon atoms, phenyl, or phenyl substituted with at least one alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro;R.sup.3 is alkoxy having 1 to 4 carbon atoms or hydrogen,R.sup.4 is hydrogen, alkyl having 1 to 4 carbon atoms unsubstituted or substituted with alkoxy having 1 to 4 carbon atoms, benzyloxy or cyano, phenyl, or phenyl substituted with at least one alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro, or phenyl-(C.sub.1-4 alkyl)-alkyl, in which the phenyl moiety may bear an alkoxy substituent having 1 to 4 carbon atoms or a halogen;m and n are each 0, 1 or 2 or a pharmaceutically acceptable acid addition or quaternary salt thereof.The compounds are potent vasodilators and exert a favorable influence on the extremital blood flow. They also show a heart function influencing activity.Methods for the preparation of said compounds and pharmaceutical compositions containing them are also the subject of the invention.
摘要翻译：本发明涉及新的式（I）化合物，其中R 1是氢，苯基或被至少一个具有1-4个碳原子的烷基取代的苯基，卤素，具有1-4个碳原子的烷氧基或硝基; R2是具有1至4个碳原子的烷基，具有5至7个碳原子的环烷基，苯基或被至少一个具有1至4个碳原子的烷基取代的苯基，卤素，具有1至4个碳原子的烷氧基或硝基; R3为具有1-4个碳原子的烷氧基或氢，R4为氢，未取代或未被取代或未被取代或未被取代的具有1-4个碳原子的烷氧基的烷基，苄氧基或氰基，苯基或被至少一个具有至少一个烷基 1至4个碳原子，卤素，具有1至4个碳原子的烷氧基或硝基，或苯基 - （C 1-4烷基） - 烷基，其中苯基部分可以带有具有1至4个碳原子的烷氧基取代基或卤素; m和n各自为0,1或2，或其药学上可接受的酸加成盐或季盐。这些化合物是有效的血管扩张剂，对前列腺血流量有很好的影响。它们也显示出影响活动的心脏功能。制备所述化合物的方法和含有它们的药物组合物也是本发明的主题。

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