公开(公告)号：US5118687A

公开(公告)日：1992-06-02

申请号：US566275

申请日：1990-08-10

申请人： Edit Toth ,  Jozsef Torley ,  Laszlo Szporny ,  Bela Kiss ,  Egon Karpati ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Zsolt Szombathelyi ,  Adam Sarkadi ,  Aniko Gere ,  Katalin Csomor ,  Mihaly Bodo ,  Judit Laszy ,  Zsolt Szentirmay

发明人： Edit Toth ,  Jozsef Torley ,  Laszlo Szporny ,  Bela Kiss ,  Egon Karpati ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Zsolt Szombathelyi ,  Adam Sarkadi ,  Aniko Gere ,  Katalin Csomor ,  Mihaly Bodo ,  Judit Laszy ,  Zsolt Szentirmay

IPC分类号： A61K31/33 ,  A61K31/335 ,  A61K31/42 ,  A61K31/435 ,  A61K31/445 ,  A61P3/00 ,  A61P9/00 ,  A61P9/10 ,  A61P25/28 ,  C07D221/00 ,  C07D263/00 ,  C07D317/00 ,  C07D491/10 ,  C07D491/107 ,  C07D491/113 ,  C07D493/10 ,  C07D498/10

CPC分类号： C07D491/10

摘要： The invention relates to novel compounds 1-oxa-2-oxo-8- of the formula (I), ##STR1## wherein X means oxygen or an >NR group, whereinR stands for hydrogen, a C.sub.1-12 alkyl, C.sub.3-6 cycloalkyl, carbocyclic C.sub.6-10 aryl or carbocyclic C.sub.6-10 aryl-C.sub.10-4 alkyl group, the latter two groups are optionally substituted on their aromatic moiety by one or more, same or different halogen(s), one or more C.sub.1-4 alkyl or C.sub.1-4 alkoxy group(s);R.sup.1 and R.sup.2 together represent a methylene group or, when X stands for an >NR group, wherein R is as defined above, one of R.sup.1 and R.sup.2 may represent a hydroxyl group whereas the other is a methyl group;R.sup.3 stands for hydrogen or a phenyl group optionally substituted by one or more halogen(s), one or more C.sub.1-4 alkyl or C.sub.1-4 alkoxy or hydroxyl group(s);R.sup.4 means hydrogen, one or more halogen(s), C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxyl or trihalomethyl group(s); andn is 1, 2 or 3as well as their acid addition and quaternary ammonium salts.

公开(公告)号：US5157038A

公开(公告)日：1992-10-20

申请号：US566274

申请日：1990-08-10

申请人： Edit Toth ,  Jozsef Torley ,  Bela Hegedus ,  Laszlo Szporny ,  Bela Kiss ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Erzsebet Lapis ,  Ferenc Auth ,  Laszlo Gaal

发明人： Edit Toth ,  Jozsef Torley ,  Bela Hegedus ,  Laszlo Szporny ,  Bela Kiss ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Erzsebet Lapis ,  Ferenc Auth ,  Laszlo Gaal

IPC分类号： A61K31/42 ,  A61K31/445 ,  A61K31/4465 ,  A61P3/00 ,  A61P25/00 ,  A61P43/00 ,  C07D211/48 ,  C07D491/10 ,  C07D491/107 ,  C07D491/113 ,  C07D493/10 ,  C07D498/10

CPC分类号： C07D491/10

摘要： The invention relates to novel 2-oxo-1-oxa-8-azaspiro[4,5]decane derivatives of the formula (I), ##STR1## wherein X means oxygen or an >NR group, whereinR stands for hydrogen; a C.sub.1-12 alkyl; C.sub.3-6 cycloalkyl; carbocyclic C.sub.6-10 aryl or carbocyclic C.sub.6-10 aryl-C.sub.1-4 alkyl group, the two latter two substituents optionally substituted on their aromatic moiety by one or more, same or different halogen, one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trihalomethyl group; or a tosyl group;R.sup.1 and R.sup.2 together represent a methylene group or, when X stands for an >NR group wherein R is as defined above, one of R.sup.1 and R.sup.2 m may represent a hydroxyl group and the other one is a methyl group; andR.sup.3 means hydrogen, benzyl, (C.sub.1-4 alkoxy)carbonyl, phenoxycarbonyl, benzyloxycarbonyl, formyl, piperidin-1-ylcarbonyl, morpholin-4-ylcarbonyl, 4-methylpiperazin-1-ylcarbonyl, 4-(2-hydroxethyl)piperazin-1-ylcarbonyl, 2-chloro-3-nicotinoylcarbamoyl or C.sub.1-6 alkylcarbamoyl group,as well as their acid addition and quaternary ammonium salts.

公开(公告)号：US5132303A

公开(公告)日：1992-07-21

申请号：US566278

申请日：1990-08-10

申请人： Edit Toth ,  Jozsef Torley ,  Sandor Gorog ,  Laszlo Szporny ,  Bela Kiss ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Erzsebet Lapis ,  Ferenc Auth ,  Laszlo Gaal

发明人： Edit Toth ,  Jozsef Torley ,  Sandor Gorog ,  Laszlo Szporny ,  Bela Kiss ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Erzsebet Lapis ,  Ferenc Auth ,  Laszlo Gaal

IPC分类号： A61K31/42 ,  A61K31/445 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D211/22 ,  C07D491/10 ,  C07D491/113 ,  C07D498/10

CPC分类号： C07D491/10

摘要： The invention relates to novel, therapeutically active 4-methylene-2-oxo-8-azaspiro[4,5]decane derivatives of the compound, ##STR1## wherein X means oxygen or an >NR group, whereinR stands for hydrogen, C.sub.1-12 alkyl, C.sub.3-6 cycloalkyl, carbocyclic C.sub.6-10 aryl or carbocyclic C.sub.6-10 arylC.sub.1-4 alkyl group, the latter two being optionally substituted on their aromatic moiety by one or more, same or different halogen(s) or one or more C.sub.1-4 alkyl group(s) or by one or more C.sub.1-4 alkoxy group(s);R.sup.3 and R.sup.4, which are the same or different, represent hydrogen, one or more halogen(s), C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trihalomethyl group or hydroxyl group optionally esterified by a C.sub.1-4 alkanoic acid; andis 1 or 2,their isomers, solvates, hydrates, acid addition and quaternary ammonium salts.

公开(公告)号：US5132309A

公开(公告)日：1992-07-21

申请号：US566279

申请日：1990-08-10

申请人： Edit Toth ,  Jozsef Torley ,  Sandor Gorog ,  Laszlo Szporny ,  Bela Kiss ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Erzsebet Lapis ,  Ferenc Auth ,  Laszlo Haal

发明人： Edit Toth ,  Jozsef Torley ,  Sandor Gorog ,  Laszlo Szporny ,  Bela Kiss ,  Eva Palosi ,  Dora Groo ,  Istvan Laszlovszky ,  Erzsebet Lapis ,  Ferenc Auth ,  Laszlo Haal

IPC分类号： A61K31/42 ,  A61K31/445 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D211/22 ,  C07D491/10 ,  C07D491/113 ,  C07D498/10

CPC分类号： C07D491/10

摘要： The invention relates to, therapeutically active 2-oxo-3,8-diazaspiro[4,5]decane derivatives (I), ##STR1## wherein R means hydrogen, a C.sub.1-12 alkyl, C.sub.3-6 cycloalkyl, carbocyclic C.sub.6-10 aryl or carbocyclic C.sub.6-10 aryl-C.sub.1-4 alkyl group, the latter two optionally being substituted on their aromatic moiety by one or more, same or different halogen(s) or one or more C.sub.1-4 alkyl or C.sub.1-4 alkoxy group(s);one of R.sup.1 and R.sup.2 stands for a hydroxyl group whereas the other means a methyl gorup;R.sup.3 and R.sup.4, which are the same or different, represent hydrogen, one or more halogen(s), C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trihalomethyl group or a hydroxyl group optionally esterified by a C.sub.1-4 alkanoic acid; andn is 1 or 2,their isomers, solvates, hydrates, acid addition and quaternary ammonium salts.

公开(公告)号：US4874765A

公开(公告)日：1989-10-17

申请号：US41206

申请日：1987-04-22

申请人： Erzsebet Lapis ,  Edit Toth ,  Bela Kiss ,  Jozsef Torley ,  Eva Palosi ,  Istvan Hajdu ,  Laszlo Szporny ,  Dora Groo ,  Istvan Laszlovszky

发明人： Erzsebet Lapis ,  Edit Toth ,  Bela Kiss ,  Jozsef Torley ,  Eva Palosi ,  Istvan Hajdu ,  Laszlo Szporny ,  Dora Groo ,  Istvan Laszlovszky

IPC分类号： C07D295/08 ,  A61K31/495 ,  A61P25/00 ,  A61P25/24 ,  A61P25/26 ,  C07D295/088 ,  C07D295/18 ,  C07D295/185 ,  C07D295/10

CPC分类号： C07D295/185 ,  C07D295/088

摘要： The invention relates to novel 1,4-disubstituted piperazine derivatives of the general formula (I), pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and stand for hydrogen or halogen or a trihalomethyl, lower alkyl, lower alkoxy, nitro, hydroxyl, aralkyloxy or an 1-(2-propenyl-4-piperazinyl) group;R.sub.5 stands for hydrogen or a C.sub.1-4 alkyl group;R.sub.6 represents a C.sub.3-6 alkyl, alkenyl, alkynyl group or a ##STR2## group, wherein R.sub.7 means a C.sub.2-5 alkyl, alkenyl or alkinyl group; andis 2 or 3,with the provisos that:R.sub.6 is different from isopropyl, n-butyl and isobutyl group when R.sub.2, R.sub.3, R.sub.4 and R.sub.5 stand for hydrogen, R.sub.1 means 2-chloro and n is 2;R.sub.6 is different from isopropyl group when R.sub.2, R.sub.3, R.sub.4 and R.sub.5 stand for hydrogen, R.sub.1 means 2-chloro and n is 2; or when R.sub.2, R.sub.3, R.sub.4 and R.sub.5 stand for hydrogen, R.sub.1 means 2-methyl group and n is 2; andR.sub.6 is different from propionyl group when R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are hydrogen and n means 2.The compounds of the general formula (I) are therapeutically useful for the treatment of diseases arising from a hypofunction of the dopaminergic system.

摘要翻译： 本发明涉及通式（I）的新的1,4-二取代哌嗪衍生物，其药学上可接受的酸加成盐和季铵盐，含有它们的药物组合物及其制备方法。 在通式（I）中，R 1，R 2，R 3和R 4相同或不同，代表氢或卤素或三卤代甲基，低级烷基，低级烷氧基，硝基，羟基，芳烷氧基或1- （2-丙烯基-4-哌嗪基）基团; R5代表氢或C1-4烷基; R6表示C3-6烷基，烯基，炔基或者IMAGE基团，其中R7表示C2-5烷基，烯基或炔基; 并且为2或3，条件是：当R 2，R 3，R 4和R 5代表氢时，R 6不同于异丙基，正丁基和异丁基，R 1表示2-氯且n为2; 当R2，R3，R4和R5代表氢时，R6不同于异丙基，R1表示2-氯，n是2; 或当R2，R3，R4和R5代表氢时，R1表示2-甲基，n表示2; 当R 1，R 2，R 3，R 4和R 5为氢且n表示2时，R 6与丙酰基不同。通式（I）的化合物可治疗用于治疗多巴胺能系统功能低下的疾病。

公开(公告)号：US4868184A

公开(公告)日：1989-09-19

申请号：US41233

申请日：1987-04-22

申请人： Edith Toth ,  Bela Kiss ,  Jozsef Torley ,  Eva Palosi ,  Istvan Hajdu ,  Laszlo Szporny ,  Dora Groo ,  Erzsebet Lapis ,  Istvan Laszlovszky

发明人： Edith Toth ,  Bela Kiss ,  Jozsef Torley ,  Eva Palosi ,  Istvan Hajdu ,  Laszlo Szporny ,  Dora Groo ,  Erzsebet Lapis ,  Istvan Laszlovszky

IPC分类号： C07D295/08 ,  A61K31/495 ,  A61P25/00 ,  A61P25/24 ,  A61P25/26 ,  C07D295/088

CPC分类号： C07D295/088

摘要： The invention relates to novel benzhydryl-piperazine derivatives of the general formula (I) and the acid addition and quaternary ammonium salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and stand for hydrogen or halogen, or a trihalomethyl, C.sub.1-4 alkyl or C.sub.1-4 alkoxy group;R.sub.6 means hydrogen or a C.sub.1-4 alkyl group; andn is 2 or 3.The compounds of the general formula (I) are useful for treating diseases arising from a decrease in the dopamine level, i.e. from a hypofunction of the dopaminergic system, and have low toxicity.

摘要翻译： 本发明涉及通式（I）的新型二苯甲基 - 哌嗪衍生物及其酸加成盐和季铵盐，含有它们的药物组合物及其制备方法。 在通式（I）中，R 1，R 2，R 3，R 4和R 5相同或不同，代表氢或卤素，或三卤甲基，C 1-4烷基或C 1-4烷氧基; R6表示氢或C1-4烷基; n为2或3.通式（I）的化合物可用于治疗多巴胺水平降低引起的疾病，即多巴胺能系统的功能低下，毒性低。

公开(公告)号：US4082813A

公开(公告)日：1978-04-04

申请号：US630512

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： C07C33/486 ,  C07C29/42

摘要： The invention is directed to a new substituted derivative of .alpha.-ethylnyl-benzophenone, namely, the 3-iodo-.alpha.-ethynyl-benzhydrol which has high antifungal activity.

公开(公告)号：US4645774A

公开(公告)日：1987-02-24

申请号：US803792

申请日：1985-12-02

申请人： Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szabolcs Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Istvan Hajdu

发明人： Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szabolcs Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Istvan Hajdu

IPC分类号： A61K31/135 ,  A61K31/40 ,  A61K31/445 ,  A61K31/535 ,  A61K31/5375 ,  A61P43/00 ,  C07C67/00 ,  C07C213/00 ,  C07C217/18 ,  C07D207/20 ,  C07D295/08 ,  C07D295/092 ,  C12N9/02

CPC分类号： C07D295/088

摘要： The invention relates to new aminoethoxybenzylalcohol derivatives of the formula (I) ##STR1## wherein R.sub.1 is hydrogen, halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms;R.sub.2 is halogen, trihalomethyl, or alkoxy having from one to 4 carbon atoms;R.sub.3 and R.sub.4 stand for methyl or together with the adjacent nitrogen form an up to 8-membered ring optionally containing oxygen,and acid addition or quaternary ammonium salts thereof.The compounds of formula (I) are pharmacologically active, thus show enzyme-inducing effect. The pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.

摘要翻译： 本发明涉及式（I）的新的氨基乙氧基苄醇衍生物：其中R 1是氢，卤素，三卤代甲基，具有1至4个碳原子的烷基或具有1至4个碳原子的烷氧基; R2是卤素，三卤甲基或具有1至4个碳原子的烷氧基; R3和R4代表甲基或与相邻的氮一起形成任选含有氧的至多8元环，及其酸加成或季铵盐。 式（I）化合物具有药理活性，因此显示出酶诱导作用。 含有它们作为活性成分的药物组合物也在本发明的范围内。

公开(公告)号：US4618611A

公开(公告)日：1986-10-21

申请号：US565901

申请日：1983-12-27

申请人： Edit Toth ,  Jozsef Torley ,  Gyorgy Fekete ,  Laszlo Szporny ,  Laszlo Vereczkey ,  Eva Palosi ,  Imre Klebovich ,  Pal Vittay ,  Sandor Gorog ,  Istvan Hajdu

发明人： Edit Toth ,  Jozsef Torley ,  Gyorgy Fekete ,  Laszlo Szporny ,  Laszlo Vereczkey ,  Eva Palosi ,  Imre Klebovich ,  Pal Vittay ,  Sandor Gorog ,  Istvan Hajdu

IPC分类号： A61K31/135 ,  A61K31/415 ,  A61K31/495 ,  A61K31/53 ,  A61P25/30 ,  C07C67/00 ,  C07C213/00 ,  C07C217/18 ,  C07D233/60 ,  C07D295/08 ,  C07D295/092 ,  C07C149/32 ,  C07D295/02

CPC分类号： C07D295/088

摘要： The invention relates to new aminopropanol derivatives of the formula (I) ##STR1## wherein R.sub.1 is halogen, trihalomethyl, alkoxy having from one to 3 carbon atoms or alkyl having from one to 3 carbon atoms,R.sub.2 is alkyl having from one to 3 carbon atoms, andR.sub.3 is cycloalkyl having from 3 to 6 carbon atoms, orR.sub.2 and R.sub.3 together with the nitrogen they are attached to form an up to 8 membered ring optionally containing oxygen or a further nitrogen as an additional hetero atom, and optionally substituted with alkyl having from one to 4 carbon atoms or benzyl,and acid addition and quaternary ammonium salts thereof.According to another aspect of the invention there are provided processes for the preparation of these compounds.The new compounds are suitable for the treatment of acute ethanolic intoxication. Pharmaceutical compositions containing them are also within the scope of the invention.

摘要翻译： 本发明涉及式（I）的新的氨基丙醇衍生物其中R 1为卤素，三卤代甲基，具有1至3个碳原子的烷氧基或具有1至3个碳原子的烷基，R 2为具有一个 3个碳原子，R3是具有3至6个碳原子的环烷基，或者R 2和R 3与它们连接的氮一起形成任选含有氧或另外的氮作为另外的杂原子的至多8元环，以及 任选被具有1至4个碳原子的烷基取代或苄基，及其酸加成盐和季铵盐。 根据本发明的另一方面，提供了这些化合物的制备方法。 新化合物适用于急性乙醇中毒治疗。 含有它们的药物组合物也在本发明的范围内。

公开(公告)号：US4064121A

公开(公告)日：1977-12-20

申请号：US603855

申请日：1975-08-12

申请人： Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szaboles Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Csilla Meszaros

发明人： Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szaboles Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Csilla Meszaros

IPC分类号： C07D295/10 ,  C07D225/02 ,  C07D211/14

CPC分类号： C07D295/10

摘要： New compounds of the general formula (I), ##STR1## wherein R.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 ##STR2## 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R1和R2与相邻的氮原子一起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表示甲基，R 2可以仅代表甲基以外的基团，其通过使 通式（II）的化合物，其中X表示卤素，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 。