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1. 发明授权

US4113868A 5,6-Dihydropyrimidin-4(3H)one derivatives, and antiedema compositions and methods employing them 失效
标题翻译： 5,6-DIHYDROPYRIMIDIN-4（3H）一种衍生物，抗微生物组合物及其使用方法
公开(公告)号：US4113868A
公开(公告)日：1978-09-12
申请号：US728459
申请日：1976-09-29
申请人： Gabor Bernath , Lajos Gera , Gyorgy Gondos , Zoltan Ecsery , Judit Hermann nee Voros , Matyas Szentivanyi , Erzsebet Janvari, nee Kanyo
发明人： Gabor Bernath , Lajos Gera , Gyorgy Gondos , Zoltan Ecsery , Judit Hermann nee Voros , Matyas Szentivanyi , Erzsebet Janvari, nee Kanyo
IPC分类号： C07D239/60 , A61K31/505 , A61K31/517 , A61P23/00 , A61P25/04 , A61P29/00 , C07D221/26 , C07D239/70 , C07D239/88 , C07D239/90 , C07D239/91
CPC分类号： C07D239/91 , C07D239/70 , C07D239/88 , C07D239/90
摘要： An antiedema compound of the formula: ##STR1## in which R.sup.1 is methyl, ethyl, cyclohexyl, phenyl, m-tolyl, p-tolyl, p-tert-butylphenyl, m-trifluoromethylphenyl, m-fluorophenyl, p-fluorophenyl, m-chlorophenyl, p-chlorophenyl, m-bromophenyl, p-bromophenyl, o-hydroxyphenyl, p-methoxyphenyl, p-nitrophenyl, benzyl, p-chlorobenzyl, m,p-dimethoxybenzyl, and o-pyridyl;R.sup.2 is hydrogen, p-tolyl, p-ethoxyphenyl, m-pyridyl, methyl or phenyl; andn is 1, 2 or 3And a process for the preparation thereof are disclosed.

2. 发明授权

US4162327A N,N-Disubstituted-2-furylethyl amines 失效
标题翻译： N，N-二取代-2-呋喃乙基胺
公开(公告)号：US4162327A
公开(公告)日：1979-07-24
申请号：US754278
申请日：1976-12-27
申请人： Jozsef Knoll , Zoltan Ecsery , Judit Hermann nee Voros , Zoltan Torok , Eva Somfai , Gabor Bernath
发明人： Jozsef Knoll , Zoltan Ecsery , Judit Hermann nee Voros , Zoltan Torok , Eva Somfai , Gabor Bernath
IPC分类号： C07D307/52 , A61K31/34
CPC分类号： C07D307/52
摘要： A compound of the formula ##STR1## or a pharmaceutically effective salt thereof in which R.sup.1 and R.sup.2 are hydrogen or lower alkyl and R.sup.3 is halogenoalkenyl or propinyl. The compounds have pharmacological effects similar to those of phenylethylamine but are free from the amphetamine effect with an excellent therapeutic index and selectivity especially with respect to inhibition of monoaminooxidase.
摘要翻译：其中R 1和R 2为氢或低级烷基且R 3为卤代烯基或丙烯基的式IMA化合物或其药学上有效的盐。该化合物具有与苯乙胺类似的药理作用，但是没有苯丙胺作用，具有优异的治疗指数和选择性，特别是在抑制单氨基氧化酶方面。

3. 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。

4. 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。

5. 发明授权

US4220771A 2,3-Polymethylene-4-oxo-4H-pyrido[1,2-a]pyrimidines 失效
标题翻译： 2,3-二亚甲基-4-氧代-4H-吡啶并[1,2-a]嘧啶
公开(公告)号：US4220771A
公开(公告)日：1980-09-02
申请号：US935071
申请日：1978-08-18
申请人： Istvan Hermecz , Ferenc Fulop , Zoltan Meszaros , Gabor Bernath , Jozsef Knoll
发明人： Istvan Hermecz , Ferenc Fulop , Zoltan Meszaros , Gabor Bernath , Jozsef Knoll
IPC分类号： A61K31/505 , A61K31/517 , A61K31/55 , A61P7/02 , A61P9/10 , A61P11/00 , A61P25/04 , A61P29/00 , A61P31/04 , A61P43/00 , C07D471/04 , C07D487/04 , C07D487/14
CPC分类号： C07D471/04 , C07D487/04
摘要： Pharmaceutical intermediates, morphine potentiators and other compounds have the formula ##STR1## wherein R is hydrogen, halogen, C.sub.1-4 alkyl, hydroxy, nitro, amino, carboxy or a carboxylic acid derivate radical, R.sup.1 is hydrogen or a C.sub.1-4 alkyl, R.sup.2 is hydrogen or C.sub.1-4 alkyl, R.sup.3 is hydrogen, R.sup.4 is hydrogen or C.sub.1-4 alkyl, R.sup.5 is hydrogen R.sup.6 is hydrogen or R.sup.3 and R.sup.4 and/or R.sup.5 and R.sup.6 form a chemical bond, X is oxygen or imino, m is 1, 2, 3 or 4, n is 0, 1, 2 or 3, and if n is 1, then the dotted lines can stand for bonds, with the proviso that if m=1 and n=1 and if in the 2,3-, 6,7-, 8,9- and 1,10-positions double bonds are present, and R.sup.1 and R.sup.2 are hydrogen, then R is other than 9-hydroxy or 9-methyl; if m=2 and n=1 and R.sup.2 is hydrogen, then at least one of R and R.sup.1 is other than hydrogen; and if m=2 and n=2 and R.sup.2 is hydrogen and the molecule is a 2,3,4,6,7,8,9,10-octahydro derivative, then at least one of R and R.sup.1 is other than hydrogen or an acid-addition or quaternary salt thereof.
摘要翻译：药物中间体，吗啡增效剂和其它化合物具有式“IMAGE”，其中R是氢，卤素，C 1-4烷基，羟基，硝基，氨基，羧基或羧酸衍生物基团，R 1是氢或C 1-4烷基， R2是氢或C1-4烷基，R3是氢，R4是氢或C1-4烷基，R5是氢R6是氢或R3和R4和/或R5和R6形成化学键，X是氧或亚氨基，m 是1,2,3或4，n是0,1,2或3，如果n是1，则虚线可以代表键，条件是如果m = 1且n = 1，如果在存在2,3,6,7,8,9和1,10-位双键，R1和R2是氢，则R不是9-羟基或9-甲基; 如果m = 2且n = 1且R2是氢，则R和R1中的至少一个不是氢; 并且如果m = 2且n = 2且R 2是氢并且该分子是2,3,4,6,7,8,9,10-八氢衍生物，则R和R 1中的至少一个不是氢或其加酸或季盐。

6. 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。

7. 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。

8. 发明授权

US5494909A Substituted oxazinoisoquinoline derivatives, pharmaceutical compositions containing them and process for preparing same 失效
标题翻译：取代的恶嗪基异喹啉衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：US5494909A
公开(公告)日：1996-02-27
申请号：US244736
申请日：1994-07-20
申请人： Jen Kobor , Laszlo Lazar , Imre Huber , Judit Arva , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Zsolt Szombathelyi , Adam Sarkadi , Aniko Gere , Mihaly Bodo , Katalin Csomor , Judit Laszy , Zsolt Szentirmai , Erzsebet Lapis , Sandor Szabo , Gabor Bernath , Ferenc Fulop
发明人： Jen Kobor , Laszlo Lazar , Imre Huber , Judit Arva , Laszlo Szporny , Bela Kiss , Egon Karpati , Eva Palosi , Zsolt Szombathelyi , Adam Sarkadi , Aniko Gere , Mihaly Bodo , Katalin Csomor , Judit Laszy , Zsolt Szentirmai , Erzsebet Lapis , Sandor Szabo , Gabor Bernath , Ferenc Fulop
IPC分类号： A61K31/535 , A61P3/00 , A61P9/08 , A61P9/10 , A61P25/28 , C07D217/06 , C07D498/04 , A61K31/47 , C07D265/14
CPC分类号： C07D498/04
摘要： New compounds with the ability to inhibit calcium uptake in the brains of mammals are disclosed of the Formula (I) ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 to C.sub.4 alkyl, phenyl, or phenyl-C.sub.1 to C.sub.4 alkyl;one of R.sup.2 and R.sup.3 is C.sub.1 to C.sub.4 alkoxy and the other one is phenyl-C.sub.1 to C.sub.4 alkoxy optionally substituted by C.sub.1 to C.sub.4 alkyl in the aromatic nucleus; andR.sup.4 is phenyl optionally substituted by C.sub.1 to C.sub.4 alkyl in the aromatic nucleus, or their solvates, individual optically active and geometric isomers, mixtures of such isomers, as well as pharmaceutically acceptable acid addition salts thereof. The compounds of the Formula (I) are capable of inhibiting calcium uptake to brain cells and have a protective effect on hypobaric hypoxia.
摘要翻译： PCT No.PCT / HU92 / 00053 Sec。 371日期：1994年7月20日 102（e）日期1994年7月20日PCT提交1992年12月11日PCT公布。公开号WO93 / 12118 （I）其中R 1是氢，C 1至C 4烷基，苯基或苯基的式（I）公开了具有抑制哺乳动物脑中钙摄取的能力的新化合物。 C1至C4烷基; R2和R3中的一个是C1-C4烷氧基，另一个是在芳核中被C1-C4烷基任选取代的苯基-C 1至C 4烷氧基; 并且R 4是任选地被芳族核中的C 1 -C 4烷基取代的苯基，或它们的溶剂化物，单独的光学活性和几何异构体，这些异构体的混合物，以及其药学上可接受的酸加成盐。式（I）的化合物能够抑制钙对脑细胞的吸收并对低压缺氧具有保护作用。

9. 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。

10. 发明授权

US4219649A Pyrido[1,2-a]pyrimidine derivatives 失效
标题翻译：吡啶并[1,2-a]嘧啶衍生物
公开(公告)号：US4219649A
公开(公告)日：1980-08-26
申请号：US934801
申请日：1978-08-17
申请人： Josef Knoll , Zoltan Meszaros , Istvan Hermecz , Ferenc Fulop , Gabor Bernath , Sandor Virag , Gabor Nagy , Peter Szentmiklosi
发明人： Josef 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 quaternary ammonium salts thereofwhereinR.sup.2 is C.sub.1 to C.sub.6 alkyl:R.sup.3 is C.sub.1 to C.sub.6 alkyl;R.sup.4 is a single electron pair, hydrogen or lower alkyl; and the dotted lines indicate saturated or unsaturated bonds, are disclosed with analgesic properties.
摘要翻译：下式的化合物或其药学上可接受的酸加成盐或季铵盐，其中R 2为C 1至C 6烷基：R 3为C 1至C 6烷基; R4是单电子对，氢或低级烷基; 虚线表示饱和或不饱和键，具有镇痛特性。

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