公开(公告)号：US4593047A

公开(公告)日：1986-06-03

申请号：US565835

申请日：1983-12-27

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

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

IPC: A61K31/05 ,  A61K31/047 ,  A61P25/30 ,  C07C27/00 ,  C07C29/143 ,  C07C37/055 ,  C07C37/20 ,  C07C39/12 ,  C07C39/24 ,  C07C39/367 ,  C07C67/00 ,  A61K31/065

CPC classification number: C07C37/055 ,  C07C37/20 ,  C07C39/12 ,  C07C39/367 ,  Y10S514/811

Abstract: The invention relates to the preparation of 3-trifluoromethyl- and 2,5-dimethyl-4'-hydroxy-.alpha.-ethyl-benzhydrol. Both compounds have so far been described only as metabolites of corresponding benzhydrol derivatives containing no hydroxyl group. Neither their physico-chemical characteristics nor their manufacturing processes have been disclosed in the known publications.3-Trifluoromethyl- and 2,5-dimethyl-4'-hydroxy-.alpha.-ethyl-benzhydrol are suitable for the treatment of acute ethanolic intoxication. Accordingly, another aspect of the invention is a pharmaceutical composition containing one of these compounds as active ingredient.

Abstract translation: 本发明涉及3-三氟甲基 - 和2,5-二甲基-4'-羟基-α-乙基 - 二苯甲醛的制备。 迄今为止，两种化合物仅被描述为不含羟基的相应二苯甲醇衍生物的代谢物。 他们的物理化学特性及其制造方法都没有在已知的出版物中公开。 3-三氟甲基 - 和2,5-二甲基-4'-羟基-α-乙基 - 二苯甲醇适用于治疗急性乙醇中毒。 因此，本发明的另一方面是含有这些化合物之一作为活性成分的药物组合物。

公开(公告)号：US4551465A

公开(公告)日：1985-11-05

申请号：US565902

申请日：1983-12-27

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

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

IPC: C07D295/08 ,  A61K31/445 ,  A61P1/16 ,  A61P39/02 ,  A61P43/00 ,  C07D211/14 ,  C07D295/092 ,  C12N9/99

CPC classification number: C07D295/088

Abstract: The invention relates to new piperidine derivatives of the formula (I) ##STR1## wherein R.sub.1 is halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms; andR.sub.2 is hydrogen or alkyl having from one to 4 carbon atoms, 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 compounds of the formula (I) are pharmacologically active. In particular, they inhibit the microsomal monooxigenase enzyme system of the liver. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.

Abstract translation: 本发明涉及式（I）的新的哌啶衍生物：其中R 1是卤素，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; 并且R 2为氢或具有1至4个碳原子的烷基，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。 式（I）的化合物具有药理活性。 特别地，它们抑制肝脏的微粒体单致原子酶系统。 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：US4504481A

公开(公告)日：1985-03-12

申请号：US565923

申请日：1983-12-27

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

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

IPC: C12N9/99 ,  A61K31/495 ,  A61P1/16 ,  A61P43/00 ,  C07D295/08 ,  C07D295/092 ,  C07D295/02

CPC classification number: C07D295/088

Abstract: The invention relates to new benzhydrylpiperazine derivatives of the formula (I) ##STR1## wherein n is 2 or 3, and acid addition salts thereof. According to another aspect of the invention there are provided processes for the preparation of these compounds.The compounds of the formula (I) are pharmacologically active. More particularly, they inhibit the microsomal monooxigenase enzyme system of liver. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.

Abstract translation: 本发明涉及式（I）的新的二苯甲基哌嗪衍生物，其中n为2或3，及其酸加成盐。 根据本发明的另一方面，提供了这些化合物的制备方法。 式（I）的化合物具有药理活性。 更具体地说，它们抑制肝脏的微粒体单致原子酶系统。 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：US4221739A

公开(公告)日：1980-09-09

申请号：US603853

申请日：1975-08-12

Applicant: Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szabolos Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Csilla Meszaros

Inventor： Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szabolos Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Csilla Meszaros

IPC: C07D295/10 ,  A61K31/135 ,  A61K31/395 ,  A61P43/00 ,  C07C225/22 ,  C07D207/06 ,  C07D233/60 ,  C07D295/112 ,  C07C97/10

CPC classification number: C07D295/112 ,  Y10S514/916

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US4075249A

公开(公告)日：1978-02-21

申请号：US630510

申请日：1975-11-10

Applicant: Edit Toth ,  Jozsef Torley ,  Sandor Gorog ,  Laszlo Szporny ,  Eva Palosi ,  Szabolcz Szeberenyi

Inventor： Edit Toth ,  Jozsef Torley ,  Sandor Gorog ,  Laszlo Szporny ,  Eva Palosi ,  Szabolcz Szeberenyi

IPC: C07C29/42 ,  C07C33/06

CPC classification number: C07C29/42

Abstract: The new compound 3,4,5-trimethoxy-.alpha.-ethynyl benzhydrol which has been found to be an effective fungicide.

Abstract translation: 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。

公开(公告)号：US4066709A

公开(公告)日：1978-01-03

申请号：US630511

申请日：1975-11-10

Applicant: Edit Toth ,  Jozsef Torley ,  Sandor Gorog ,  Laszlo Szporny ,  Eva Palosi ,  Szabolcs Szeberenyi

Inventor： Edit Toth ,  Jozsef Torley ,  Sandor Gorog ,  Laszlo Szporny ,  Eva Palosi ,  Szabolcs Szeberenyi

IPC: C07C29/42 ,  C07C31/16

CPC classification number: C07C29/42

Abstract: .alpha.-ethynyl-benzhydrols, namely 2,5-dimethyl-.alpha.-ethynyl and 4-n-butyl-.alpha.-ethynyl benzhydrol, are made by reacting the starting benzophenone with acetylene in a solvent delivering no protons, in the presence of an alkali metal tertiary alcoholate, preferably potassium-ter.-butylate or potassium-tert.-amylate.

公开(公告)号：US3975390A

公开(公告)日：1976-08-17

申请号：US603854

申请日：1975-08-12

Applicant: Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szaholes Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Csilla Meszaros

Inventor： Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szaholes Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Csilla Meszaros

IPC: C07D295/10 ,  C07D295/06

CPC classification number: C07D295/10 ,  Y10S514/916

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5132309A

公开(公告)日：1992-07-21

申请号：US566279

申请日：1990-08-10

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

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

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

CPC classification number: C07D491/10

Abstract: 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：US5118693A

公开(公告)日：1992-06-02

申请号：US566273

申请日：1990-08-10

Applicant: Edit Toth ,  Jozef Torley ,  Sandor Gorog ,  Laszlo Szporny ,  Bela Kiss ,  Eva Palosi ,  Groo ,  Istvan Laszlovszky ,  Erzsebet Lapis ,  Ferenc Auth ,  Laszlo Gaal

Inventor： Edit Toth ,  Jozef Torley ,  Sandor Gorog ,  Laszlo Szporny ,  Bela Kiss ,  Eva Palosi ,  Groo ,  Istvan Laszlovszky ,  Erzsebet Lapis ,  Ferenc Auth ,  Laszlo Gaal

IPC: A61K31/445 ,  A61K31/4465 ,  A61P1/08 ,  A61P25/04 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D211/48 ,  C07D211/74 ,  C07D491/10 ,  C07D498/10

CPC classification number: C07D491/10 ,  C07D211/48

Abstract: The invention relates to novel, therapeutically active 4,4-disubstituted piperidine derivatives of the formula (I), ##STR1## wherein R.sup.1 means hydrogen or --CONHR 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 aryl-C.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 of more C.sub.1-4 alkyl or C.sub.1-4 alkoxy group(s);R.sup.2 stands for an ethynyl or acetyl group;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; andn is 1 or 2,as well as their pharmaceutically acceptable 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

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

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

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

CPC classification number: C07D295/185 ,  C07D295/088

Abstract: 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.

Abstract translation: 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。