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91. 发明授权

US4451473A 3,7-Diazabicyclo [3.3.1] nonanes having anti-arrhythmic activity 失效
标题翻译：具有抗心律不齐活性的3,7-二氮杂双环[3.3.1]壬烷
公开(公告)号：US4451473A
公开(公告)日：1984-05-29
申请号：US398801
申请日：1982-07-16
申请人： Karoly Nador , Gabor Kraiss , Katalin Sinko , Margit Paroczai , Egon Karpati , Laszlo Szporny
发明人： Karoly Nador , Gabor Kraiss , Katalin Sinko , Margit Paroczai , Egon Karpati , Laszlo Szporny
IPC分类号： A61K31/395 , A61K31/435 , A61K31/48 , A61K31/4995 , A61P9/06 , C07D451/14 , C07D471/08 , A61K31/44
CPC分类号： C07D471/08 , Y10S514/821
摘要： New bicyclic compounds of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each represent a C.sub.1-6 alkyl group, andR.sup.3 is an etherified hydroxy group of the formula --CR.sup.4, wherein R.sup.4 is benzyl group, benzhydryl group or a phenyl group bearing optionally a phenyl or a trihalomethyl substituent or one or more halogen substituent(s), orR.sup.3 is an esterified hydroxy group of the formula --OCO--R.sup.5, which representsa phenyl-(C.sub.1-5 alkyl)-carbonyloxy group,a cinnamoyloxy group having optionally a halogen or one or more C.sub.1-4 alkoxy substituent(s),a benzoyloxy group having optionally a C.sub.1-4 alkyl, phenyl or trihalomethyl substituent or one or more C.sub.1-4 alkoxy substituent(s), one or more halo substituent(s) and/or nitro substituent,a benzyloyloxy group,a xanthene-9-carbonyloxy group,an optionally substituted naphthoyloxy group, oran acyloxy group derived from a five- or six-membered heterocyclic carboxylic acid bearing optionally a halo substituent on the ring,are prepared by etherifying or esterifying a bicyclic compound of the general formula (II), ##STR2## wherein R.sup.1 and R.sup.2 are as defined above. The new compounds according to the invention possess anti-arrhythmic effects and can be applied to advantage in the therapy of cardiac rhythm disorders.
摘要翻译：通式（I）的新的双环化合物，其中R 1和R 2各自表示C 1-6烷基，R 3是式-CR 4的醚化羟基，其中R 4是苄基，二苯甲基基团或任选带有苯基或三卤甲基取代基或一个或多个卤素取代基的苯基，或R3是式-OCO-R5的酯化羟基，其代表苯基 - （C 1-5烷基） - 具有任选卤素或一个或多个C 1-4烷氧基取代基的肉桂酰氧基，任选具有C 1-4烷基的苯甲酰氧基，苯基或三卤甲基取代基或一个或多个C 1-4烷氧基取代基，，一个或多个卤素取代基和/或硝基取代基，苯甲酰氧基，呫吨-9-羰氧基，任选取代的萘氧基或衍生自五元或六元杂环羧酸的酰氧基任选地，环上的卤素取代基通过醚化制备或酯化通式（II）的双环化合物，其中R 1和R 2如上所定义。根据本发明的新化合物具有抗心律失常作用，可用于治疗心律失常的优点。

92. 发明授权

US4329350A 1,1-Disubstituted octahydro-indolo[2,3-a]quinolizines, process for the preparation thereof and compositions containing same 失效
标题翻译： 1,1-二取代八氢 - 吲哚并[2,3-a]喹嗪，其制备方法和含有它们的组合物
公开(公告)号：US4329350A
公开(公告)日：1982-05-11
申请号：US41192
申请日：1979-05-21
申请人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/04 , A61K31/435 , A61K31/437 , A61K31/4375 , A61P9/08 , C07D471/14 , A61K31/40 , C07D455/02
CPC分类号： C07D471/14 , Y10S514/929
摘要： Compounds of the formula: ##STR1## wherein R is alkyl having 1 to 6 carbon atoms;A is substituted or unsubstituted alkyl having 1 to 6 carbon atoms, aralkyl having 7 to 16 carbon atoms wherein the alkyl or aralkyl groups are unbranched in the 1-position or an acyl group derived from an aliphatic or aromatic carboxylic acid;B is hydrogen; orA and B together form an optionally substituted alkylidene having 2 to 8 carbon atoms or an aralkylidene group having 7 to 18 carbon atoms where the alkylidene and aralkylidene groups are unbranched in the 1-position or pharmaceutically acceptable salts thereof are disclosed. The compounds have vasodilating properties.
摘要翻译：下式的化合物：其中R是具有1至6个碳原子的烷基; A是取代或未取代的具有1至6个碳原子的烷基，具有7至16个碳原子的芳烷基，其中烷基或芳烷基在1-位是非支链的，或由脂族或芳族羧酸衍生的酰基; B是氢; 或A和B一起形成任选取代的具有2至8个碳原子的亚烷基或具有7至18个碳原子的芳烷叉基，其中亚烷基和亚烷叉基在1-位或其药学上可接受的盐中是无支链的。该化合物具有血管扩张性质。

93. 发明授权

US4315011A 1-Alkyl-9-bromohexahydroindolo quinolizium salts and use thereof to increase blood flow 失效
标题翻译： 1-烷基-9-溴六氢吲哚喹啉盐及其用于增加血流量的用途
公开(公告)号：US4315011A
公开(公告)日：1982-02-09
申请号：US56395
申请日：1979-07-10
申请人： Csaba Szantay , Lajos Szabo , Gyoorgy Kalaus , Lajos Dancsi , Tibor Keve , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajos Szabo , Gyoorgy Kalaus , Lajos Dancsi , Tibor Keve , Egon Karpati , Laszlo Szporny
IPC分类号： C07D209/16 , C07D209/42 , C07D461/00 , C07D471/14 , C07D471/22 , A61K31/475 , C07D459/00
CPC分类号： C07D471/14 , C07D209/16 , C07D209/42 , C07D461/00
摘要： The invention is directed to 1-alkyl-9-bromohexagydro indoloquinolizium salts and a method for their use to increase blood circulation and decrease in blood vessel resistance.
摘要翻译：本发明涉及1-烷基-9-溴六氢吲哚喹啉鎓盐及其用于增加血液循环和降低血管阻力的方法。

94. 发明授权

US4221739A Amino-substituted nitrobenzophenone derivatives with alkyl, phenyl, phenyl alkyl or cycloalkyl amino-substituting groups 失效
标题翻译：具有烷基，苯基，苯基烷基或环烷基氨基取代基的氨基取代的硝基二苯甲酮衍生物
公开(公告)号：US4221739A
公开(公告)日：1980-09-09
申请号：US603853
申请日：1975-08-12
申请人： Edit Toth , Jozsef Torley , Eva Palosi , Szabolos Szeberenyi , Laszlo Szporny , Sandor Gorog , Csilla Meszaros
发明人： Edit Toth , Jozsef Torley , Eva Palosi , Szabolos Szeberenyi , Laszlo Szporny , Sandor Gorog , Csilla Meszaros
IPC分类号： C07D295/10 , A61K31/135 , A61K31/395 , A61P43/00 , C07C225/22 , C07D207/06 , C07D233/60 , C07D295/112 , C07C97/10
CPC分类号： C07D295/112 , Y10S514/916
摘要： Compounds of the formula (I), ##STR1## wherein R.sub.1 and R.sub.2 each is saturated or unsaturated, straight-chained or branched alkyl phenyl, alkylphenyl or saturated or unsaturated cycloalkyl;but when R.sub.1 is methyl, R.sub.2 is a group other than methyl, are prepared by reacting a compound of the formula (II), ##STR2## wherein X is halogen, with a secondary amine of the formula (III),R.sub.1 --NH--R.sub.2 (III)The new compounds of the formula (I), as well as their pharmaceutically acceptable acid addition salts are active primarily in the induction of liver microsomal enzyme, but also possess antipyretic activity.
摘要翻译：式（I）化合物，其中R 1和R 2各自为饱和或不饱和的直链或支链烷基苯基，烷基苯基或饱和或不饱和环烷基; 但是当R 1为甲基时，R 2为除甲基以外的基团，其通过使式（II）化合物，其中X为卤素的式（II）与式（III）的仲胺反应，R1 -NH-R2（III）式（I）的新化合物及其药学上可接受的酸加成盐主要在肝微粒体酶的诱导中起主要作用，但也具有解热活性。

95. 发明授权

US4200650A 2-Amino-cyclopent-1-ene-1-thiocarboxylic acid-disulfides to treat noradrenergic malfunctions 失效
标题翻译： 2-氨基 - 环戊-1-烯-1-硫代羧酸 - 二硫化物，用于治疗去甲肾上腺素能异常
公开(公告)号：US4200650A
公开(公告)日：1980-04-29
申请号：US6523
申请日：1979-01-25
申请人： Gyorgy Matolcsy , Piroska Bartok nee Berencsy , Bela Kiss , Eva Palosi , Egon Karpati , Laszlo Szporny
发明人： Gyorgy Matolcsy , Piroska Bartok nee Berencsy , Bela Kiss , Eva Palosi , Egon Karpati , Laszlo Szporny
IPC分类号： A61K31/195
CPC分类号： A61K31/195
摘要： New 2-amino-cyclopent-1-ene-thiocarboxylic acid-disulfides of the general formula (I), ##STR1## wherein R is hydrogen, a C.sub.1-6 alkyl group having optionally a C.sub.1-4 alkoxy, hydroxy, carboxy and/or amino substituent, a C.sub.2-4 alkenyl group, a C.sub.3-8 cycloalkyl group or phenyl group, are prepared by oxidizing the respective 2-amino-cyclopent-1-ene-dithiocarboxylic acids of the general formula (II), ##STR2## wherein R is as defined above. The new compounds of the general formula (I) and their salts exert dopamine-.beta.-hydroxylase inhibiting effects and can be applied in the therapy.
摘要翻译：通式（I）的新的2-氨基 - 环戊-1-烯 - 硫代羧酸 - 二硫化物，其中R是氢，任选具有C1-4烷氧基的C1-6烷基，羟基，羧基和/或氨基取代基，C2-4烯基，C3-8环烷基或苯基，通过将通式（II）的各个2-氨基 - 环戊-1-烯 - 二硫代羧酸氧化，（II）其中R如上定义。通式（I）的新化合物及其盐可发挥多巴胺-β-羟化酶的抑制作用，可用于治疗。

96. 发明授权

US4140790A 3-(4-Substituted piperazino)-1-xanthene-9-carbonyloxy-propanes 失效
标题翻译： 3-（4-取代的哌嗪子基）-1-呫吨-9-羰基氧基 - 丙烷
公开(公告)号：US4140790A
公开(公告)日：1979-02-20
申请号：US859928
申请日：1977-12-12
申请人： Karoly Felfoldi , Jozsef Apjok , Mihaly Bartok , Jozsef Czombos , Arpad Molnar , Ferenc Noteisz , Egon Karpati , Laszlo Szporny
发明人： Karoly Felfoldi , Jozsef Apjok , Mihaly Bartok , Jozsef Czombos , Arpad Molnar , Ferenc Noteisz , Egon Karpati , Laszlo Szporny
IPC分类号： C07D243/26 , A61K31/495 , A61K31/55 , A61K31/551 , A61P3/00 , A61P9/06 , A61P9/08 , A61P25/20 , C07D241/04 , C07D243/16 , C07D243/18 , C07D243/24 , C07D295/08 , C07D295/088 , C07D295/096 , C07D307/68 , C07D311/82 , C07D311/84 , C07D405/12 , C07D295/14 , C07D241/06 , C07D241/10
CPC分类号： C07D295/088 , C07D307/68 , C07D311/84 , Y10S514/821
摘要： The invention relates to novel piperazine derivatives having the formula (I), ##STR1## wherein R.sub.1 represents a C.sub.1-5 alkyl group having optionally a phenyl, trimethoxyphenyl, phenoxy, methoxy-cyclohexyl or heptamethyleneimino substituent on the terminal carbon atom, allyl group, a phenyl group having optionally one or more halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trihalomethyl or allyl substituent(s), or a C.sub.2-5 alkoxycarbonyl group,R.sub.2 represents hydrogen or a C.sub.1-4 alkyl group, andR.sub.3 represents furyl group, 9-xanthenyl group or a C.sub.5-6 cycloalkyl group having a C.sub.1-4 alkoxy substituent,Or acid addition salts or quaternary salts thereof.The invention also relates to pharmaceutical compositions containing the above compounds, furthermore to a process for the preparation of the novel compounds and pharmaceutical compositions.The novel compounds according to the invention possess anti-arrhythmic and coronary dilatating effects.The novel compounds can be prepared by reacting a compound of the formula (II) ##STR2## with a compound of the formula (III),R.sup.3 --COOH (III)or a reactive derivative thereof.
摘要翻译：本发明涉及具有式（I）的新型哌嗪衍生物，其中R 1表示在末端碳原子上具有任选的苯基，三甲氧基苯基，苯氧基，甲氧基 - 环己基或七亚甲基亚氨基取代基的C 1-5烷基，烯丙基，任选具有一个或多个卤素的苯基，C 1-4烷基，C 1-4烷氧基，三卤代甲基或烯丙基取代基，或C 2-5烷氧基羰基，R 2表示氢或C 1-4烷基， R3表示呋喃基，9-呫吨基或具有C1-4烷氧基取代基的C5-6环烷基，或其酸加成盐或季铵盐。

97. 发明授权

US4075249A 3,4,5-Trimethoxy-.alpha.-ethynyl-benzhydrol as a fungicidally effective compound 失效
标题翻译： 3,4,5-三甲氧基 - {60-乙炔基 - 二苯甲醇作为杀真菌有效的化合物
公开(公告)号：US4075249A
公开(公告)日：1978-02-21
申请号：US630510
申请日：1975-11-10
申请人： Edit Toth , Jozsef Torley , Sandor Gorog , Laszlo Szporny , Eva Palosi , Szabolcz Szeberenyi
发明人： Edit Toth , Jozsef Torley , Sandor Gorog , Laszlo Szporny , Eva Palosi , Szabolcz Szeberenyi
IPC分类号： C07C29/42 , C07C33/06
CPC分类号： C07C29/42
摘要： The new compound 3,4,5-trimethoxy-.alpha.-ethynyl benzhydrol which has been found to be an effective fungicide.
摘要翻译：已被发现是一种有效的杀真菌剂的新化合物3,4,5-三甲氧基-α-乙炔基二苯甲醇。

98. 发明授权

US4054571A Nitrogen-containing polycyclic compounds and a process for the preparation thereof 失效
标题翻译：含氮多环化合物及其制备方法
公开(公告)号：US4054571A
公开(公告)日：1977-10-18
申请号：US614151
申请日：1975-09-17
申请人： Csaba Szantay , Lajor Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
发明人： Csaba Szantay , Lajor Szabo , Gyorgy Kalaus , Egon Karpati , Laszlo Szporny
IPC分类号： C07D471/06 , A61K31/4375 , A61K31/4745 , C07D461/00 , C07D471/04
CPC分类号： C07D461/00
摘要： The invention relates to new eburnamenine derivatives of the general formula (I), ##STR1## wherein R.sub.1 stands for an alkyl group,R.sub.2 stands for a carboxy group, a functional carboxy derivative (preferably an ester group) or a group convertable into carboxy group or a functional derivative thereof (preferably cyano group), andX.sup.- is an anion derived from an acid,And the corresponding free bases.These compounds are valuable intermediates of the preparation of eburnamenine derivatives with advantageous therapeutical effects.The above compounds are prepared as follows: a compound of the general formula (II), ##STR2## wherein R.sub.1 has the same meanings as defined above, is reacted with a compound of the general formula (III), ##STR3## wherein R.sub.2 has the same meanings as defined above and Y is halogen, and, if desired, a thus-obtained compound of the general formula (I), wherein R.sub.1 and R.sub.2 each have the same meanings as defined above and X.sup.- is a halide ion, is reacted with an acid, and/or, if desired, a compound of the general formula (I), wherein R.sub.1 and X.sup.- each have the same meanings as defined above and R.sub.2 is cyano or an ester group, is subjected to hydrolysis, and/or, if desired, a compound of the general formula (I), wherein R.sub.1, R.sub.2 and X.sup.- each have the same meanings as defined above, is treated with a base.
摘要翻译：本发明涉及通式（I），其中R1代表烷基，R2代表羧基，官能羧基衍生物（优选酯基）或可转化基团的新颖的本本母胺衍生物羧基或其功能性衍生物（优选氰基），X是衍生自酸的阴离子，和相应的无碱基。

99. 发明授权

US3975390A N-methyl substituted piperazino nitrobenzophenones and a process for the preparation thereof 失效
标题翻译： N-甲基取代的哌嗪子基硝基二苯甲酮及其制备方法
公开(公告)号：US3975390A
公开(公告)日：1976-08-17
申请号：US603854
申请日：1975-08-12
申请人： Edit Toth , Jozsef Torley , Eva Palosi , Szaholes Szeberenyi , Laszlo Szporny , Sandor Gorog , Csilla Meszaros
发明人： Edit Toth , Jozsef Torley , Eva Palosi , Szaholes Szeberenyi , Laszlo Szporny , Sandor Gorog , Csilla Meszaros
IPC分类号： C07D295/10 , C07D295/06
CPC分类号： C07D295/10 , Y10S514/916
摘要： New compounds of the general formula (I), ##SPC1##whereinR.sub.1 and R.sub.2 each stand for a saturated or unsaturated, straight-chained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom may form an optionally substituted heterocyclic group optionally containing a further oxygen or nitrogen hetero atom,But if R.sub.1 stands for methyl, R.sub.2 may only stand for a group other than methyl,Are prepared by reacting a compound of the general formula (II), ##SPC2##wherein X stands for halogen, with a secondary amine of the general formula (III),r.sub.1 --nh--r.sub.2 (iii)wherein R.sub.1 and R.sub.2 each have the same meanings as defined above.The new compounds of the general formula (I), as well as their pharmaceutical acceptable acid addition salts or quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess antipyretic activity.
摘要翻译：通式（I）的新化合物，其中R 1和R 2各自表示饱和或不饱和的直链或支链烷基，芳烷基，饱和或不饱和环烷基或芳基，或R 1和R 2一起相邻的氮原子可以形成任选地含有另外的氧或氮杂原子的任选取代的杂环基团，但是，R 1代表甲基，R 2可以仅代表甲基以外的基团，ARE通过反应通用化合物（II），其中X代表卤素，具有通式（III）的仲胺，R1-NH-R2（III）其中R1和R2各自具有与上述相同的含义。

100. 发明授权

US06656921B1 Use of zinc hyaluronate against peptic ulcer 有权
标题翻译：使用透明质酸锌对消化性溃疡
公开(公告)号：US06656921B1
公开(公告)日：2003-12-02
申请号：US09403714
申请日：2000-09-21
申请人： Janos Illes , Judit Matuz , Erzsabet Neszmelyi , Gaborne Forrai , Bela Stefko , Katalin Saghy , Laszlo Szporny
发明人： Janos Illes , Judit Matuz , Erzsabet Neszmelyi , Gaborne Forrai , Bela Stefko , Katalin Saghy , Laszlo Szporny
IPC分类号： A61K31715
CPC分类号： A61K31/728 , A61K47/61
摘要： The invention relates to pharmaceutical compositions against peptic ulcer as well as to a method of treating peptic ulcer. The compositions contain and the method of treatment employs zinc hyaluronate as an active ingredient having a molecular weight in the range of 500,000 to 1,200,000 daltons.
摘要翻译：本发明涉及消化性溃疡的药物组合物以及治疗消化性溃疡的方法。组合物含有和治疗方法使用透明质酸锌作为分子量在500,000至1,200,000道尔顿范围内的活性成分。

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