公开(公告)号：US5157038A

公开(公告)日：1992-10-20

申请号：US566274

申请日：1990-08-10

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

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

IPC: 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 classification number: C07D491/10

Abstract: 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：US5118687A

公开(公告)日：1992-06-02

申请号：US566275

申请日：1990-08-10

Applicant: 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

Inventor： 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: 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 classification number: C07D491/10

Abstract: 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：US4082813A

公开(公告)日：1978-04-04

申请号：US630512

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: C07C33/486 ,  C07C29/42

Abstract: 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

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: 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 classification number: C07D295/088

Abstract: 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.

Abstract translation: 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

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: A61K31/135 ,  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 classification number: C07D295/088

Abstract: 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.

Abstract translation: 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：US4564630A

公开(公告)日：1986-01-14

申请号：US565922

申请日：1983-12-27

Applicant: Edit Toth ,  Jozsef Torley ,  Istvan Hajdu ,  Sander Gorog ,  Andrea Maderspach ,  Gyorgy Hajos ,  Laszlo Szporny ,  Andras Javor

Inventor： Edit Toth ,  Jozsef Torley ,  Istvan Hajdu ,  Sander Gorog ,  Andrea Maderspach ,  Gyorgy Hajos ,  Laszlo Szporny ,  Andras Javor

IPC: A61K31/27 ,  A61K31/325 ,  A61P3/06 ,  C07C67/00 ,  C07C239/00 ,  C07C271/08 ,  C07C271/44 ,  C07C271/46 ,  C07C271/56 ,  C07C271/58 ,  C07C125/067 ,  C07C125/075

CPC classification number: A61K31/325

Abstract: The invention relates to new carbamyloxybenzhydrol 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 hydrogen or an R.sub.3 --NH--COO-- group;R.sub.3 is alkyl having from one to 6 carbon atoms, cycloalkyl having up to 7 carbon atoms, or phenyl, optionally substituted with one or more halogen(s).The compounds of the formula (I) show antilipaemic activity and can therefore be used in therapy for treating hyperlipaemia and coronary diseases. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.

Abstract translation: 本发明涉及式（I）的新的氨基甲酰氧基二苯甲醇衍生物其中R 1是氢，卤素，三卤甲基，具有1至4个碳原子的烷基或具有1至4个碳原子的烷氧基的式（I） R2是氢或R3-NH-COO-基团; R3是具有1至6个碳原子的烷基，具有至多7个碳原子的环烷基，或任选被一个或多个卤素取代的苯基。 式（I）的化合物显示抗血脂活性，因此可用于治疗高脂血症和冠状动脉疾病。 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：US4064121A

公开(公告)日：1977-12-20

申请号：US603855

申请日：1975-08-12

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

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

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

CPC classification number: C07D295/10

Abstract: 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.

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 。

公开(公告)号：US3957777A

公开(公告)日：1976-05-18

申请号：US485701

申请日：1974-07-03

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

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

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

CPC classification number: C07D295/112 ,  Y10S514/916

Abstract: New compounds of the formula (I), ##SPC1##whereinR.sub.1 and R.sub.2 each stand for a saturated or unsaturated, straightchained 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 form a substituted or unsubstituted heterocyclic group which can contain a further oxygen or nitrogen hetero atom,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), ##SPC2##wherein X stands for halogen, with a secondary amine of the general formula (III),r.sub.1 --nh--r.sub.2. (iii)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.

公开(公告)号：US4605785A

公开(公告)日：1986-08-12

申请号：US565838

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: C07C69/708 ,  A61K31/085 ,  A61K31/135 ,  A61K31/16 ,  A61K31/165 ,  A61K31/19 ,  A61K31/22 ,  A61K31/275 ,  A61P1/16 ,  A61P39/02 ,  A61P43/00 ,  C07C41/00 ,  C07C41/16 ,  C07C41/18 ,  C07C41/30 ,  C07C43/23 ,  C07C67/00 ,  C07C201/00 ,  C07C205/30 ,  C07C217/18 ,  C07C235/06 ,  C07C235/20 ,  C07C253/00 ,  C07C255/54 ,  C07C43/20

CPC classification number: C07C43/23

Abstract: The invention relates to new 1,1-diphenylpropan-1-ol derivatives of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms,R.sub.3 is halogen, trihalomethyl, alkyl having from one to 5 carbon atoms or alkoxy having from one to 5 carbon atoms,R.sub.4 is phenyl optionally substituted by one or more identical or different substituents selected from the group of halogen, trihalomethyl, alkyl, alkoxy, cyano, nitro, amino, alkylamino, dialkylamino, hydroxyl, carboxyl or substituted carboxyl; dialkylaminocarbonyl or alkoxycarbonyl containing from one to 4 carbon atoms in the alkyl and alkoxy moieties, respectively,n is 1, 2, 3, 4, or 5.According to another aspect of the invention there are provided processes for the preparation of the compounds of formula (I).The new compounds induce the polysubstrate monooxigenase enzyme system of liver and are devoid from other pharmacodinamic effects. Pharmaceutical compositions containing compounds of the formula (I) as active ingredient are also within the scope of the invention.

Abstract translation: 本发明涉及式（I）的新的1,1-二苯基丙-1-醇衍生物其中R 1和R 2独立地表示氢，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，R 3是卤素，三卤甲基，具有1至5个碳原子的烷基或具有1至5个碳原子的烷氧基，R 4是任选地被一个或多个相同或不同的选自卤素 ，三卤代甲基，烷基，烷氧基，氰基，硝基，氨基，烷基氨基，二烷基氨基，羟基，羧基或取代的羧基; 在烷基和烷氧基部分中分别含有1至4个碳原子的二烷基氨基羰基或烷氧基羰基，n分别为1,2,3,4或5.根据本发明的另一方面，提供了制备 式（I）。 新化合物诱导肝脏的多底物一氧化酶基因系统，缺乏其他药物作用。 含有式（I）化合物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：US4605672A

公开(公告)日：1986-08-12

申请号：US565912

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: A61K31/135 ,  A61K31/13 ,  A61K31/205 ,  A61K31/40 ,  A61K31/445 ,  A61P25/24 ,  A61P25/26 ,  A61P25/30 ,  C07C20060101 ,  C07C67/00 ,  C07C213/00 ,  C07C217/18 ,  C07C217/20 ,  C07D295/08

CPC classification number: C07C217/18

Abstract: The invention relates to the preparation of new diethylaminoalkoxybenzhydrol 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, andn is 1, 2, 3 or 4,and acid addition and quaternary ammonium salts thereof.According to another aspect of the invention, there are provided new compounds of the formula (I), and acid addition and quaternary salts thereof. The compounds can be used for the treatment of acute ethanolic intoxication and depression syndromes. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.

Abstract translation: 本发明涉及制备式（I）的新的二乙氨基烷氧基二氢化茚醇衍生物其中R1是氢，卤素，三卤代甲基，具有1-4个碳原子的烷基或具有1-4个碳原子的烷氧基，R2 是卤素，三卤代甲基或具有1至4个碳原子的烷氧基，n为1,2,3或4，以及其酸加成盐和季铵盐。 根据本发明的另一方面，提供了新的式（I）化合物及其酸加成盐和季盐。 该化合物可用于治疗急性乙醇中毒和抑郁综合征。 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。