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1. 发明授权

US4622327A 2H-azeto[2,1-a]-isoquinoline derivatives and pharmaceutical compositions containing them 失效
标题翻译： 2H-azeto [2,1-a] - 异喹啉衍生物和含有它们的药物组合物
公开(公告)号：US4622327A
公开(公告)日：1986-11-11
申请号：US664786
申请日：1984-10-25
申请人： Gabor Bernath , Jeno Kobor , Alajos Kalman , Pal Sohar , Ferenc Fulop , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
发明人： Gabor Bernath , Jeno Kobor , Alajos Kalman , Pal Sohar , Ferenc Fulop , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
IPC分类号： A61K31/435 , A61P1/04 , A61P25/04 , A61P29/00 , A61P37/08 , C07D463/00 , A61K31/40 , C07D455/08
CPC分类号： C07D463/00
摘要： The invention relates to new 2H-azeto[2,1-a]isoquinoline derivatives of formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is hydroxyl, halogen or an ##STR2## group, whereinX is oxygen or sulfur,R.sup.4 is optionally substituted phenyl,and acid addition, metal and quaternary salts thereof.According to the invention the new compounds are prepared by cyclization of the corresponding compounds of formula (II), ##STR3## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, and Hal is halogen.Compounds of formula (I) are pharmaceutically active, in particular are potent analgesic and antipyretic agents.
摘要翻译：本发明涉及式（I）的新的2H-azeto [2,1-a]异喹啉衍生物其中R 1和R 2表示羟基或具有1至6个碳原子的烷氧基，R 3是羟基，卤素或其中X是氧或硫，R4是任选取代的苯基，和其酸加成物，金属和季盐。根据本发明，通过相应的式（II）化合物，其中R 1，R 2和R 3如上定义，Hal是卤素，通过环化相应的式（II）化合物制备新化合物。式（I）的化合物是药学活性的，特别是有效的镇痛和解热剂。

2. 发明授权

US4623647A [1,3]oxazino[4,3-a]-isoquinoline derivatives and pharmaceutical compositions containing them 失效
标题翻译： [1,3]恶嗪并[4,3-a] - 异喹啉衍生物和含有它们的药物组合物
公开(公告)号：US4623647A
公开(公告)日：1986-11-18
申请号：US664844
申请日：1984-10-25
申请人： Gabor Bernath , Jeno Kobor , Ferenc Folop , Pal Sohar , Pal Perjesi , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
发明人： Gabor Bernath , Jeno Kobor , Ferenc Folop , Pal Sohar , Pal Perjesi , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
IPC分类号： A61K31/535 , A61P1/04 , A61P25/04 , A61P25/24 , A61P25/26 , A61P29/00 , A61P37/06 , C07D498/04 , C07D498/10 , C07D265/34
CPC分类号： C07D498/04 , C07D498/10
摘要： The invention relates to new [1,3]oxazino[4,3-a]-isoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is hydrogen, alkyl having from 1 to 8 carbon atoms, cycloakyl or cycloalkenyl having from 3 to 6 carbon atoms, optionally substituted phenyl, aralkyl having from 1 to 4 carbon atoms in the alkyl moiety or heteroaryl,R.sup.4 is hydrogen or alkyl having from 1 to 4 carbon atoms, orR.sup.3 and R.sup.4 together form a --(CH.sub.2).sub.n -- group, in which n is an integer from 3 to 7,R.sup.5 is hydroxyl, halogen or an ##STR2## group, in which R.sup.6 is optionally substituted phenyl,X is oxygen or sulfur,and salts thereof.According to another aspect of the invention there is provided a process for the preparation of these compounds. Compounds of formula (I) are pharmaceutically active. Pharmaceutical compositions containing them are also within the scope of the invention.
摘要翻译：本发明涉及式（I）的新的[1,3]恶嗪并[4,3-a] - 异喹啉衍生物其中R 1和R 2表示羟基或具有1至6个碳原子的烷氧基，R 3 是氢，具有1至8个碳原子的烷基，具有3至6个碳原子的环烷基或环烯基，任选取代的苯基，在烷基部分或杂芳基具有1至4个碳原子的芳烷基，R 4是氢或具有1 至4个碳原子，或者R 3和R 4一起形成 - （CH 2）n - 基团，其中n为3-7的整数，R 5为羟基，卤素或基团，其中R 6为任选取代的苯基 X是氧或硫，及其盐。根据本发明的另一方面，提供了一种制备这些化合物的方法。式（I）的化合物是药学活性的。含有它们的药物组合物也在本发明的范围内。

3. 发明授权

US4605653A 1-(hydroxymethyl)-1,6,7,11b-tetrahydro-2H,4H-[1,3]oxazino- or -thiazino-[4,3-a]isoquinoline derivatives and pharmaceutical compositions containing them 失效
标题翻译： 1-（羟基甲基）-1,6,7,11b-四氢-2H- 2H- [1,3]恶嗪基 - 或噻嗪并[4,3-a]异喹啉衍生物和含有它们的药物组合物
公开(公告)号：US4605653A
公开(公告)日：1986-08-12
申请号：US713533
申请日：1985-03-19
申请人： Gabor Bernath , Jeno Kobor , Ferenc Folop , Attila Sohajda , Alajos Kalman , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
发明人： Gabor Bernath , Jeno Kobor , Ferenc Folop , Attila Sohajda , Alajos Kalman , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
IPC分类号： A61K31/535 , A61K31/54 , A61P1/12 , A61P9/08 , A61P25/08 , C07D498/04 , C07D513/04
CPC分类号： C07D513/04
摘要： The invention relates to 1-(hydroxymethyl)-1,6,7,11b-tetrahydro-2H,4H-[1,3]oxazino- or -thiazino-[4,3-a]isoquinoline derivatives of the formula (I), ##STR1## wherein R.sup.1 and R.sup.2 are alkoxy having from 1 to 6 carbon atoms,X is oxygen or sulfur,Y is .dbd.O, .dbd.S or an .dbd.NR.sup.3 group, whereinR.sup.3 is hydrogen, alkyl having from 1 to 6 carbon atoms, cycloalkyl having from 3 to 8 carbon atoms or optionally substituted phenyl,and acid addition and quaternary salts thereof.
摘要翻译：本发明涉及式（I）的1-（羟甲基）-1,6,7,11b-四氢-2H，4H- [1,3]恶嗪基 - 或噻唑并〔4,3-a〕异喹啉衍生物，，其中R 1和R 2是具有1至6个碳原子的烷氧基，X是氧或硫，Y是= O，= S或= NR 3基团，其中R 3是氢，具有1至 6个碳原子，具有3至8个碳原子的环烷基或任选取代的苯基，及其酸加成盐和季盐。

4. 发明授权

US4656179A Isoquinoline derivatives, and pharmaceutical compositions containing them 失效
标题翻译：异喹啉衍生物和含有它们的药物组合物
公开(公告)号：US4656179A
公开(公告)日：1987-04-07
申请号：US664842
申请日：1984-10-25
申请人： Gabor Bernath , Jeno Kobor , Ferenc Fulop , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
发明人： Gabor Bernath , Jeno Kobor , Ferenc Fulop , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
IPC分类号： A61K31/47 , A61K31/472 , A61P1/04 , A61P25/04 , A61P25/24 , A61P25/26 , A61P29/00 , A61P37/06 , C07D217/16
CPC分类号： B82Y10/00 , C07D217/16
摘要： The invention relates to new 1-[bis(hydroxymethyl)-methyl]-3,4-dihydro- or -1,2,3,4-tetrahydroisoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is hydrogen or a single electron pair,and the dotted line represents an optional double bond,and salts thereof.The new compounds are useful intermediates in the preparation of other, pharmaceutically active isoquinoline derivatives or are pharmaceutically active themselves.
摘要翻译：本发明涉及式（I）的新的1- [双（羟甲基） - 甲基] -3,4-二氢或-1,2,3,4-四氢异喹啉衍生物其中R1和R2 表示具有1至6个碳原子的羟基或烷氧基，R 3是氢或单个电子对，虚线表示任选的双键及其盐。新化合物是制备其它药学活性异喹啉衍生物的有用的中间体或其本身是药物活性的。

5. 发明授权

US4668688A N-substituted isoquinoline derivatives and pharmaceutical compositions containing them 失效
标题翻译： N-取代的异喹啉衍生物和含有它们的药物组合物
公开(公告)号：US4668688A
公开(公告)日：1987-05-26
申请号：US664770
申请日：1984-10-25
申请人： Gabor Bernath , Jeno Kobor , Ferenc Fulop , Pal Perjesi , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
发明人： Gabor Bernath , Jeno Kobor , Ferenc Fulop , Pal Perjesi , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
IPC分类号： A61K31/47 , A61K31/472 , A61P1/04 , A61P25/04 , A61P29/00 , A61P37/06 , C07D217/16
CPC分类号： C07D217/16
摘要： The invention relates to new N-substituted bis(hydroxymethyl)-methyl-isoquinoline derivatives of the formula (I), ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,the dotted line is an optional double bond in the 1,2-position,R.sup.3 is alkyl having from 1 to 6 carbon atoms or aralkyl containing from 1 to 4 carbon atoms in the alkyl moiety, or--if there is a single bond in the 1,2-position--represents a group of the formula ##STR2## in which X is oxygen ifR.sup.4 is alkyl having from 1 to 5 carbon atoms, alkoxy having from 1 to 4 carbon atoms, hydroxyl, phenyl or substituted phenyl; orX is oxygen or sulfur ifR.sup.4 is an --NH.sub.2, --NH--C.sub.1-4 -alkyl, --NH--C.sub.3-6 -cycloalkyl, --NH-phenyl or --NH--C.sub.1-4 -alkyl-phenyl group; andR.sup.5 and R.sup.6 independently stand for hydrogen, alkyl having from 1 to 4 carbon atoms or phenyl, with the proviso that at least one of them is other than phenyl,and salts thereof. Processes for the preparation of these compounds and pharmaceutical compositions are also within the scope of the invention.
摘要翻译：本发明涉及式（I）的新的N-取代双（羟甲基） - 甲基 - 异喹啉衍生物，其中R1和R2代表羟基或具有1-6个碳原子的烷氧基，虚线是在1,2-位上的任选的双键，R3是具有1至6个碳原子的烷基或在烷基部分含有1至4个碳原子的芳烷基，或 - 如果1,2-二烷基中存在单键，位置 - 表示如果R 4是具有1至5个碳原子的烷基，具有1至4个碳原子的烷氧基，羟基，苯基或取代的苯基，其中X是氧的式“IMAGE”的基团; 如果R 4是-NH 2，-NH-C 1-4 - 烷基，-NH-C 3-6 - 环烷基，-NH-苯基或-NH-C 1-4 - 烷基 - 苯基，则X是氧或硫; 并且R 5和R 6独立地代表氢，具有1至4个碳原子的烷基或苯基，条件是它们中的至少一个不是苯基，及其盐。用于制备这些化合物和药物组合物的方法也在本发明的范围内。

6. 发明授权

US4654351A Bis(substituted methyl)-methyl-isoquinoline derivatives and pharmaceutical compositions containing them 失效
标题翻译：双（取代的甲基） - 甲基 - 异喹啉衍生物和含有它们的药物组合物
公开(公告)号：US4654351A
公开(公告)日：1987-03-31
申请号：US664849
申请日：1984-10-25
申请人： Gabor Bernath , Jeno Kobor , Ferenc Fulop , Gabor Motika , Attila Sohajda , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
发明人： Gabor Bernath , Jeno Kobor , Ferenc Fulop , Gabor Motika , Attila Sohajda , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
IPC分类号： A61K31/47 , A61K31/472 , A61P1/04 , A61P9/00 , A61P25/04 , A61P25/24 , A61P25/26 , A61P29/00 , A61P37/06 , C07D217/14 , C07D217/16
CPC分类号： C07D217/16 , C07D217/14
摘要： The invention relates to new bis(substituted methyl)-methyl-isoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is hydrogen, aralkyl having from 1 to 4 carbon atoms in the alkyl moiety or a ##STR2## group, in which R.sup.4 is alkyl having from 1 to 5 carbon atoms, phenyl, substituted phenyl or --NH--phenyl,X is oxygen or sulfur,R.sup.7 is hydroxyl, halogen or an ##STR3## group, R.sup.8 is halogen, alkoxy from 1 to 4 carbon atoms or an ##STR4## group, in which X has the same meaning as defined above, andR.sup.9 independently from R.sup.4 may have the same meanings as defined for R.sup.4, or is an --NH(C.sub.1-4 -alkyl) or C.sub.3-6 -cycloalkyl group,and salts thereof. According to another aspect of the invention there are provided processes for the preparation of these compounds and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式（I）的新的双（取代的甲基） - 甲基 - 异喹啉衍生物，其中R 1和R 2表示羟基或具有1至6个碳原子的烷氧基，R 3是氢，具有烷基部分或其中R 4为具有1至5个碳原子的烷基，苯基，取代的苯基或-NH-苯基，X为氧或硫，R 7为羟基，卤素或一个基团，R 8为卤素，1至4个碳原子的烷氧基或一个基团，其中X具有与上述相同的含义，并且独立地为R 4的R 9可具有与R 4所定义相同的含义，或是-NH（C 1-4 - 烷基）或C 3-6 - 环烷基，及其盐。根据本发明的另一方面，提供了制备这些化合物的方法和含有它们的药物组合物。

7. 发明授权

US4677109A 1-(6-(2'-substiuted-5', 6', 7', 8'-tetrahydro-4',-oxo-quinazolino))-3-4-dihydro-6,7-disubstituted-isoqui noline derivatives and pharmaceutical compostions containing them 失效
标题翻译： 1-（6-（2'-取代 - 5'，6'，7'，8'-四氢-4' - 氧代 - 喹唑啉））-3,4-二氢-6,7-二取代 - 异喹啉衍生物和含有它们的药物组合物
公开(公告)号：US4677109A
公开(公告)日：1987-06-30
申请号：US721807
申请日：1985-04-10
申请人： Gabor Bernath , Jeno Kobor , Janos Lazar , Gabor Motika , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
发明人： Gabor Bernath , Jeno Kobor , Janos Lazar , Gabor Motika , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
IPC分类号： A61K31/505 , A61K31/535 , A61P25/04 , A61P25/08 , A61P29/00 , A61P39/02 , C07D401/04 , C07D401/14
CPC分类号： C07D401/04 , C07D401/14
摘要： The invention relates to new 1-[6-(2'-substituted-5', 6', 7', 8'-tetrahydro-4'-oxo-quinazolino)]-3,4-dihydro-6,7-disubstituted-isoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 each independently represents hdyroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is alky having from 1 to 6 carbon atoms, optionally substituted phenyl, optionally substituted alkylphenyl having from 1 to 4 carbon atoms in the alkyl moiety or an optionally substiutted heterocyclic group,and acid addition and quaternary salts thereof.Compounds of the formula (I) are pharmaceutically active, in particular show spasmolytic, analgesic, antipyretic activity and have a protecting effect in acute alcoholic intoxication.
摘要翻译：本发明涉及新的1- [6-（2'-取代-5'，6'，7'，8'-四氢-4'-氧代 - 喹唑啉基）] - 3,4-二氢-6,7-二取代（I）的异喹啉衍生物其中R 1和R 2各自独立地表示具有1至6个碳原子的羟基或烷氧基，R 3是具有1至6个碳原子的烷基，任选取代的苯基，任选地在烷基部分或任选取代的杂环基中具有1至4个碳原子的取代烷基苯基，及其酸加成和季盐。式（I）的化合物是药学活性的，特别是显示解痉，镇痛，解热活性，并且在急性酒精中毒中具有保护作用。

8. 发明授权

US4622329A 1-cyclohexyl-3,4-dihydroisoquinoline derivatives and pharmaceutical compositions containing them 失效
标题翻译： 1-环己基-3,4-二氢异喹啉衍生物和含有它们的药物组合物
公开(公告)号：US4622329A
公开(公告)日：1986-11-11
申请号：US721880
申请日：1985-04-10
申请人： Gabor Bernath , Jeno Kobor , Janos Lazar , Gabor Motika , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
发明人： Gabor Bernath , Jeno Kobor , Janos Lazar , Gabor Motika , Elemer Ezer , Gyorgy Hajos , Eva Palosi , Laszlo Denes , Laszlo Szporny
IPC分类号： C07D217/16 , A61K31/47 , A61K31/472 , A61P1/04 , A61P25/04 , A61P25/08 , A61P25/20 , A61P25/30 , A61P39/02 , C07D217/14
CPC分类号： C07D217/14
摘要： The invention relates to new 1-cyclohexyl-3,4-dihydroisoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 each independently represents hydrogen, hydroxyl or alkoxy having from 1 to 6 carbon atoms,X is oxygen andZ is a .dbd.CH.sub.2 or .dbd.CH--COOR.sup.3 group, in which R.sup.3 is hydrogen or alkyl having from 1 to 6 carbon atoms; orX represents an .dbd.NR.sup.4 group, in which R.sup.4 is hydrogen or hydroxyl, andZ is a .dbd.CH--CN, .dbd.CH.sub.2 or .dbd.CH--COOR.sup.3 group, in which R.sup.3 is as defined above,and acid addition salts thereof.The compounds of formula (I) are pharmaceutically active, in particular show antispasm, analgesic, gastric acid secretion inhibiting, sedative and hypnotic activity and effectively reduce the alcoholic narcosis time. According to a further aspect of the invention there is provided a process for the preparation of these compounds. The invention further relates to pharmaceutical compositions containing them as active ingredient.
摘要翻译：本发明涉及式（I）的新的1-环己基-3,4-二氢异喹啉衍生物其中R 1和R 2各自独立地表示氢，羟基或具有1至6个碳原子的烷氧基，X是氧 Z为a = CH 2或= CH-COOR 3基团，其中R 3为氢或具有1至6个碳原子的烷基; 或X表示= NR4基团，其中R4为氢或羟基，Z为a = CH-CN，= CH2或= CH-COOR3基团，其中R3如上定义，及其酸加成盐。式（I）的化合物是药学活性的，特别是表现出痉挛，镇痛，胃酸分泌抑制，镇静和催眠活性，并有效降低酒精性麻醉时间。根据本发明的另一方面，提供了制备这些化合物的方法。本发明还涉及含有它们作为活性成分的药物组合物。

9. 发明授权

US4200631A Treating mammalian subject sensitive to indomethacin ulcerogenisis 失效
标题翻译：治疗对吲哚美辛溃疡发生敏感的哺乳动物受试者
公开(公告)号：US4200631A
公开(公告)日：1980-04-29
申请号：US931910
申请日：1978-08-08
申请人： Elemer Ezer , Laszlo Szporny , Lilla Forgach , Eva Palosi , Eszter Cholnoky , Egon Karpati , Gyorgy Hajos , Gyozo Hortobagyi , Katalin Gidai
发明人： Elemer Ezer , Laszlo Szporny , Lilla Forgach , Eva Palosi , Eszter Cholnoky , Egon Karpati , Gyorgy Hajos , Gyozo Hortobagyi , Katalin Gidai
IPC分类号： A61K31/405 , A61K31/62
CPC分类号： A61K31/60
摘要： Ulcer production in animals is prevented during prolonged antiphlogistic treatment with ulcerogenic quantities of indomethacin by using it in a composition of 1 part of indomethacin to 7.5 to 25 parts, preferably 10 parts by weight of a salicylate. Indomethacin is the most potent ulcerating compound among approved non-steroid antiinflammatory agents.
摘要翻译：通过将其用于1份吲哚美辛组合物中的7.5〜25份，优选10份重量的水杨酸酯，在用溃疡性量的吲哚美辛进行长时间的消炎治疗期间，能够预防动物的溃疡生产。吲哚美辛是经批准的非类固醇抗炎药物中最有效的溃疡化合物。

10. 发明授权

US5155123A Pyridine derivatives and pharmaceutical compositions containing them 失效
标题翻译：吡啶衍生物和含有它们的药物组合物
公开(公告)号：US5155123A
公开(公告)日：1992-10-13
申请号：US607153
申请日：1990-10-31
申请人： Gyorgy Domany , Elemer Ezer , Istvan Schon , Judit Matuz , Katalin Saghy , Laszlo Szporny , Gyorgy Hajos , Marta Renyei
发明人： Gyorgy Domany , Elemer Ezer , Istvan Schon , Judit Matuz , Katalin Saghy , Laszlo Szporny , Gyorgy Hajos , Marta Renyei
IPC分类号： A61K31/44 , A61K31/4425 , A61P1/00 , A61P1/04 , A61P25/04 , A61P29/00 , C07D213/72 , C07D213/77
CPC分类号： C07D213/77 , C07D213/72
摘要： The invention relates to novel pyridine derivatives of formula (I), ##STR1## wherein Q stand for a nitro or cyano group; andX.sup.1 and X.sup.2, independently from each other, represent hydrogen or halogen or a trifluoromethyl, a lower alkyl or alkoxy or nitro group bound to any of the carbon atoms of the phenyl ring.The invention further relates to pharmaceutical compositions containing these compounds and a process for their preparation.The compounds of formula (I) possess gastric acid secretion inhibiting, tissue-protecting, analgetic and mild antiinflammatory effects and are useful for therapeutical purposes.

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