公开(公告)号：US4223041A

公开(公告)日：1980-09-16

申请号：US844618

申请日：1977-10-25

申请人： Charles Pigerol ,  Pierre Eymard ,  Jean-Claude Vernieres ,  Madeleine Combet epse Broll ,  Jean-Yves Lacolle

发明人： Charles Pigerol ,  Pierre Eymard ,  Jean-Claude Vernieres ,  Madeleine Combet epse Broll ,  Jean-Yves Lacolle

IPC分类号： A61K31/17 ,  A61P25/00 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07C275/04 ,  C07C275/06 ,  C07C275/20

CPC分类号： C07C275/06 ,  C07C275/20

摘要： Urea derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3, which are the same or different, each represent a straight- or branched-chain alkyl, alkenyl or alkynyl radical having from 1 to 5 carbon atoms, R.sub.4 and R.sub.5, which are the same or different, each represent a hydrogen atom or a straight- or branched-chain alkyl, alkenyl or alkynyl radical having from 1 to 5 carbon atoms, R.sub.1, R.sub.2 and R.sub.3 being such that:(a) only one of these radicals can represent an alkenyl or alkynyl group having an unsaturated bond in the .alpha.,.beta.-position with respect to the methylurea radical, in this case, each of the other two substituents represents an alkyl radical,(b) the sum of their carbon atoms is never inferior to 4.They are useful as anxiolytic and antiagressive agents.

摘要翻译： 下式的脲衍生物：其中R1，R2和R3相同或不同，分别表示具有1至5个碳原子的直链或支链烷基，烯基或炔基，R4和R5， 它们相同或不同，各自表示氢原子或具有1至5个碳原子的直链或支链烷基，烯基或炔基，R1，R2和R3使得：（a）这些中仅有一个 基团可以表示相对于甲基脲基团在α，β-位上具有不饱和键的烯基或炔基，在这种情况下，其它两个取代基各自表示烷基，（b）它们的碳原子之和 它们不会劣于4.它们作为抗焦虑药和抗抑郁药有用。

公开(公告)号：US4048334A

公开(公告)日：1977-09-13

申请号：US606880

申请日：1975-08-22

申请人： Charles Pigerol ,  Pierre Eymard ,  Jean-Claude Vernieres ,  Jean-Pierre Werbenec

发明人： Charles Pigerol ,  Pierre Eymard ,  Jean-Claude Vernieres ,  Jean-Pierre Werbenec

IPC分类号： A61K31/13

CPC分类号： A61K31/13

摘要： Methylamine derivatives of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein R.sub.1 and R.sub.3 each represent a hydrogen atom or a straight- or branched-chain alkyl, alkenyl or alkynyl radical containing from 1 to 6 carbon atoms, R.sub.2 represents a straight- or branched-chain alkyl, alkenyl or alkynyl radical containing from 2 to 7 carbon atoms with the proviso that when R.sub.2 represents an alkenyl radical of the formula CH.tbd.CH--R.sub.4 or an alkynyl radical of the formula C=C--R.sub.4, in which R.sub.4 represents a hydrogen atom or a straight- or branched-chain alkyl radical of 1 to 5 carbon atoms, R.sub.1 and R.sub.3 each represent an atom of hydrogen or an alkyl radical, R.sub.1, R.sub.2 and R.sub.3 being such that no compound of formula I possesses more than 13 carbon atoms.They are useful for treating Parkinson's disease and for correcting extra-pyramidal disturbances provoked by neuroleptics.

摘要翻译： 下式的甲胺衍生物及其药学上可接受的酸加成盐，其中R 1和R 3各自表示氢原子或含有1至6个碳原子的直链或支链烷基，烯基或炔基，R 2表示 含有2至7个碳原子的直链或支链烷基，烯基或炔基，条件是当R 2表示式CH 3 CH 2 R 4或式C = C-R 4的炔基时， ，其中R 4表示氢原子或1至5个碳原子的直链或支链烷基，R 1和R 3各自表示氢原子或烷基，R 1，R 2和R 3不使化合物 式I具有多于13个碳原子。

公开(公告)号：US4283420A

公开(公告)日：1981-08-11

申请号：US31165

申请日：1979-04-18

申请人： Charles Pigerol ,  Jean-Claude Vernieres ,  Pierre Eymard ,  Jacques Simiand ,  Madeleine Broll ,  Jean-Yves Lacolle

发明人： Charles Pigerol ,  Jean-Claude Vernieres ,  Pierre Eymard ,  Jacques Simiand ,  Madeleine Broll ,  Jean-Yves Lacolle

IPC分类号： A61K31/16 ,  A61K31/165 ,  A61K31/19 ,  A61P25/00 ,  A61P25/08 ,  A61P25/18 ,  A61P25/28 ,  C07C51/00 ,  C07C51/08 ,  C07C51/09 ,  C07C51/27 ,  C07C51/353 ,  C07C51/367 ,  C07C51/377 ,  C07C51/41 ,  C07C51/60 ,  C07C61/08 ,  C07C61/10 ,  C07C61/15 ,  C07C61/16 ,  C07C61/20 ,  C07C61/22 ,  C07C61/35 ,  C07C61/39 ,  C07C61/40 ,  C07C62/04 ,  C07C62/10 ,  C07C62/20 ,  C07C62/34 ,  C07C67/00 ,  C07C231/00 ,  C07C233/00 ,  C07C233/58 ,  C07C235/40 ,  C07C235/82

CPC分类号： C07C62/34 ,  C07C51/08 ,  C07C51/09 ,  C07C51/27 ,  C07C51/353 ,  C07C51/367 ,  C07C51/377 ,  C07C51/412 ,  C07C51/60 ,  C07C61/08 ,  C07C61/15 ,  C07C61/35 ,  C07C61/39 ,  C07C61/40 ,  C07C62/04 ,  C07C62/10 ,  C07C62/20

摘要： The chemical compounds of the invention are useful as the active compound in drugs because of their anticonvulsant and/or antianoxic activity. They have the general formula ##STR1## wherein Z is a hydroxyl group; a group--OM wherein M is an alkali metal atom or an equivalent atom fraction of an alkaline-earth metal or an amino group such as --NH.sub.2, and R is a linear or branched alkyl group containing from 1 to 9 carbon atoms, and optionally substituted by one or more halogen atoms; a linear or branched alkenyl or alkynyl, alkoxyalkyl, or acylalkyl group containing from 2 to 9 carbon atoms and optionally substituted by one or more halogen atoms; an aryl or arylalkyl or aryloxyalkyl group comprising at least one aromatic radical and an alkyl chain having from 1 to 4 carbon atoms.

摘要翻译： 本发明的化合物由于其抗惊厥和/或抗氧化活性而可用作药物中的活性化合物。 它们具有通式，其中Z是羟基; 基团-M OM，其中M是碱金属原子或碱土金属或氨基的等价原子级分，例如-NH 2，R是含有1至9个碳原子的直链或支链烷基，并且任选地 被一个或多个卤素原子取代; 含有2至9个碳原子并且任选被一个或多个卤素原子取代的直链或支链烯基或炔基，烷氧基烷基或酰基烷基; 包含至少一个芳族基团和具有1至4个碳原子的烷基链的芳基或芳基烷基或芳氧基烷基。

公开(公告)号：US4057644A

公开(公告)日：1977-11-08

申请号：US707897

申请日：1976-07-22

申请人： Charles Pigerol ,  Pierre Eymard ,  Jean-Claude Vernieres ,  Jean-Pierre Werbenec ,  Madeleine Broll

发明人： Charles Pigerol ,  Pierre Eymard ,  Jean-Claude Vernieres ,  Jean-Pierre Werbenec ,  Madeleine Broll

IPC分类号： A61K31/13 ,  A61K31/395 ,  A61K31/535 ,  C07D203/08 ,  C07D205/04 ,  C07D295/15

CPC分类号： C07D203/08 ,  A61K31/13 ,  A61K31/395 ,  A61K31/535 ,  C07D205/04 ,  C07D295/15

摘要： Methylamine derivatives of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein R.sub.1 and R.sub.3 each represent a hydrogen atom or a straight- or branched-chain alkyl, alkenyl or alkynyl radical containing from 1 to 6 carbon atoms, R.sub.2 represents a straight- or branched-chain alkyl, alkenyl or alkynyl radical containing from 2 to 7 carbon atoms with the proviso that when R.sub.2 represents an alkenyl radical of the formula CH.dbd.CH--R.sub.6 or an alkynyl radical of the formula C.tbd.C--R.sub.6, in which R.sub.6 represents a hydrogen atom or a straight- or branched-chain alkyl radical of 1 to 5 carbon atoms, R.sub.1 and R.sub.3 each represent an atom of hydrogen or an alkyl radical, R.sub.4 and R.sub.5, which are the same or different, each represent a hydrogen atom, a straight- or branched-chain alkyl, alkenyl or alkynyl radical containing from 1 to 5 carbon atoms or an .omega.-hydroxyalkyl radical containing from 2 to 5 carbon atoms or R.sub.4 and R.sub.5, when they are taken together represent an alkylene radical containing from 2 to 6 carbon atoms, an alkylidene radical containing from 1 to 5 carbon atoms or the radical --CH.sub.2 --CH.sub.2 --O--CH.sub.2 --CH.sub.2 --, R.sub.1, R.sub.2 and R.sub.3 being such that the trisubstituted methylamine radical possesses no more than 13 carbon atoms.They are useful for treating Parkinson's disease and for correcting extra-pyramidal disturbances provoked by neuroleptics.

摘要翻译： 下式的甲胺衍生物及其药学上可接受的酸加成盐，其中R 1和R 3各自表示氢原子或含有1至6个碳原子的直链或支链烷基，烯基或炔基，R 2表示 含有2至7个碳原子的直链或支链烷基，烯基或炔基，条件是当R 2表示式CH = CH-R 6的烯基或式C的炔基时， ，其中R 6表示氢原子或1至5个碳原子的直链或支链烷基，R 1和R 3各自表示氢或烷基的原子，R 4和R 5相同或不同， 各自表示氢原子，含有1至5个碳原子的直链或支链烷基，烯基或炔基或含有2至5个碳原子的ω-羟基烷基或R 4和R 5，当它们一起表示时 亚烷基 含有2至6个碳原子的二烷基，含有1至5个碳原子的亚烷基或基团-CH 2 -CH 2 -O-CH 2 -CH 2 - ，R 1，R 2和R 3使得三取代的甲基胺基不超过 13个碳原子。

公开(公告)号：US4026925A

公开(公告)日：1977-05-31

申请号：US577732

申请日：1975-05-15

申请人： Charles Pigerol ,  Pierre Eymard ,  Jean-Claude Vernieres ,  Jean-Pierre Werbenec

发明人： Charles Pigerol ,  Pierre Eymard ,  Jean-Claude Vernieres ,  Jean-Pierre Werbenec

IPC分类号： A61K31/13 ,  C07C87/06 ,  C07C87/24

CPC分类号： A61K31/13

摘要： Methylamine derivatives of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein R.sub.1 and R.sub.3 each represent a hydrogen atom or a straight- or branched-chain alkyl, alkenyl or alkynyl radical containing from 1 to 6 carbon atoms, R.sub.2 represents a straight- or branched-chain alkyl, alkenyl or alkynyl radical containing from 2 to 7 carbon atoms with the proviso that when R.sub.2 represents an alkenyl radical of the formula CH=CH--R.sub.4 or an alkynyl radical of the formula C.tbd.C--R.sub.4, in which R.sub.4 represents a hydrogen atom or a straight- or branched-chain alkyl radical of 1 to 5 carbon atoms, R.sub.1 and R.sub.3 each represent an atom of hydrogen or an alkyl radical, R.sub.1, R.sub.2 and R.sub.3 being such that no compound of formula I possesses more than 13 carbon atoms.They are useful for treating Parkinson's disease and for correcting extra-pyramidal disturbances provoked by neuroleptics.

摘要翻译： 下式的甲胺衍生物及其药学上可接受的酸加成盐，其中R 1和R 3各自表示氢原子或含有1至6个碳原子的直链或支链烷基，烯基或炔基，R 2表示 含有2至7个碳原子的直链或支链烷基，烯基或炔基，条件是当R 2表示式CH = CH-R 4的烯基或式C的炔基时， ，其中R 4表示氢原子或1至5个碳原子的直链或支链烷基，R 1和R 3各自表示氢原子或烷基，R 1，R 2和R 3不使化合物 式I具有多于13个碳原子。

公开(公告)号：US4158862A

公开(公告)日：1979-06-19

申请号：US846088

申请日：1977-10-27

申请人： Andre Michaud ,  Pierre Eymard

发明人： Andre Michaud ,  Pierre Eymard

IPC分类号： G11B5/02 ,  G06K1/12 ,  G06K19/02 ,  G06K19/06 ,  G11B5/845 ,  G11B13/04 ,  G03G19/00

CPC分类号： G11B5/845 ,  G06K1/125 ,  G06K19/022 ,  G06K19/06196

摘要： Permanent magnetic recordings are made by orienting the magnetic particlesf a polymerizable ink in a first direction, then selectively polymerizing the ink to fix some of the particles in the first direction. The remaining particles are then oriented in a second direction and the previously unpolymerized portions of the ink are polymerized, while the ink is kept in a magnetic field tending to orient the particles in the second direction to prevent the particles fixed in the first direction from blurring the magnetic pattern before the polymerization is effective to lock it in completely. Such recordings are particularly useful for ID cards.

摘要翻译： 通过使可聚合油墨的磁性颗粒沿第一方向定向，然后选择性聚合油墨以使一些颗粒沿第一方向固定来制备永久磁记录。 然后剩余的颗粒在第二方向上定向，并且油墨的预先未聚合的部分聚合，同时油墨保持在倾向于使颗粒沿第二方向定向的磁场中，以防止沿第一方向固定的颗粒模糊 聚合前的磁性图案有效地将其完全锁定。 这样的记录对于身份证特别有用。

公开(公告)号：US4139634A

公开(公告)日：1979-02-13

申请号：US798802

申请日：1977-05-20

申请人： Charles Pigerol ,  Paul DE Cointet de Fillain ,  Pierre Eymard ,  Jean-Pierre Werbenec ,  Madeleine Broll

发明人： Charles Pigerol ,  Paul DE Cointet de Fillain ,  Pierre Eymard ,  Jean-Pierre Werbenec ,  Madeleine Broll

IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D209/08 ,  C07D209/12 ,  C07D209/30 ,  C07D401/06

CPC分类号： C07D209/12 ,  C07D209/08 ,  C07D209/30

摘要： Indole derivatives of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl radical, R.sub.2 and R.sub.3, which are the same or different, each represent a hydrogen atom, a methyl or ethyl radical, a benzyl radical or represent together a pentamethylene, hexamethylene, oxydiethylene or N-methylaminodiethylene chain, forming thus a cycle with the nitrogen atom, R.sub.4 represents a phenyl, 2', 4'-dimethyl-phenyl, isopropyl, cyclopropyl, 1-methyl-cyclopropyl, cyclopentyl or cyclohexyl radical, R.sub.5 represents a hydrogen atom, a branched- or straight-chain alkyl radical containing from 1 to 3 carbon atoms, a methylthio or ethylthio radical or a straight-chain acyl radical containing from 2 to 6 carbon atoms, R.sub.6 represents a hydrogen atom or a halogen atom, a methyl, methoxy, hydroxy, carboxy, nitro, amino, methylamino or dimethylamino radical, R.sub.7 represents a hydrogen atom or a halogen atom and n is 1 or 2, with the proviso that two at least of the groups R.sub.5, R.sub.6 and R.sub.7 represent a hydrogen atom and that, when n is 2, one at least of the groups R.sub.2 and R.sub.3 is not a hydrogen atom, and their pharmaceutically acceptable acid addition salts.The derivatives of the invention are useful as antidepressant and/or antiaggressive agents.

摘要翻译： 下式的吲哚衍生物：其中R 1表示氢原子或甲基，R 2和R 3相同或不同，各自表示氢原子，甲基或乙基，苄基或一起代表 五亚甲基，六亚甲基，氧联二乙烯或N-甲基氨基二亚乙基链，由此形成与氮原子的循环，R4代表苯基，2'，4'-二甲基 - 苯基，异丙基，环丙基，1-甲基 - 环丙基，环戊基或环己基 R 5表示氢原子，含有1〜3个碳原子的支链或直链烷基，甲硫基或乙硫基或含有2-6个碳原子的直链酰基，R6表示氢原子或 卤素原子，甲基，甲氧基，羟基，羧基，硝基，氨基，甲基氨基或二甲基氨基，R7表示氢原子或卤素原子，n为1或2，条件是两个至少R5， R6和R7表示氢 并且当n为2时，基团R 2和R 3中的至少一个不是氢原子，以及它们的药学上可接受的酸加成盐。

公开(公告)号：US4423071A

公开(公告)日：1983-12-27

申请号：US126191

申请日：1980-03-03

申请人： Michel Chignac ,  Claude Grain ,  Fernand Jammot ,  Charles Pigerol ,  Pierre Eymard ,  Bernard Ferrandes

发明人： Michel Chignac ,  Claude Grain ,  Fernand Jammot ,  Charles Pigerol ,  Pierre Eymard ,  Bernard Ferrandes

IPC分类号： C07C69/003 ,  A61K31/215 ,  A61K31/22 ,  A61K31/335 ,  A61K31/357 ,  A61P25/08 ,  A61P25/24 ,  C07C67/00 ,  C07C67/10 ,  C07C67/28 ,  C07C69/007 ,  C07C69/013 ,  C07C69/18 ,  C07C69/28 ,  C07C69/30 ,  C07C69/708 ,  C07C69/75 ,  C07C219/06 ,  C07C233/18 ,  C07C233/19 ,  C07C235/08 ,  C07C313/00 ,  C07C323/12 ,  C07D303/16 ,  C07D317/12 ,  C07D317/18 ,  C07D317/20 ,  C07D317/22 ,  C07D317/24 ,  C07D317/72 ,  C07D319/06

CPC分类号： C07D317/72 ,  C07C327/00 ,  C07D303/16 ,  C07D317/12 ,  C07D317/20 ,  C07D317/24 ,  C07D319/06

摘要： Mono-, di-, tri- and tetra-esters derived from an acid of the general formula:R--OHin which R represents an acyl radical of the general formula: ##STR1## in which n represents 0 or 1, m represents 0, 1, 2, 3 or 4, R.sub.1 and R.sub.2 each represent a straight- or branched-chain alkyl radical having from 1 to 5 carbon atoms, R.sub.3 represents hydrogen or a straight- or branched-chain alkyl radical having from 1 to 5 carbon atoms, the sum of the carbon atoms in R.sub.1 and R.sub.2 being from 4 to 10 when R.sub.3 represents hydrogen and the sum of the carbon atoms in R.sub.1, R.sub.2 and R.sub.3 being from 6 to 15 when R.sub.3 is different from hydrogen, or R.sub.1 and R.sub.2 when they are taken together represent a tetramethylene, pentamethylene or hexamethylene radical and R.sub.3 represents a straight-chain alkyl radical and an alcohol selected from the group consisting of glycerol, 2,3-epoxy-propanol, 1,2-propanediol, 1,3-propanediol, 1,2-butanediol, 1,3-butanediol, 1,4-butanediol, 1,2,3-butanetriol, 1,2,4-butanetriol, 1,2,3,4-butanetetrol, 2-buten-1,4-diol, 2-butyn-1,4-diol, diethyleneglycol, a cyclohexanediol preferably 1,2-cyclohexanediol, thiodiglycol, diethanolamine, N-R-substituted-diethanolamine, trimethylolpropane, pentaerythritol and an alcohol of the general formula: ##STR2## in which p represents 0 or 1, R.sub.4 represents methyl, R.sub.5 represents methyl, ethyl, 2-methyl-butyl or R.sub.4 and R.sub.5, when they are taken together represent a pentamethylene radical, with the exception of glyceryl tri-(di-n-propylacetate).These esters are useful in the treatment of central nervous system disorders and including, in particular, convulsive states and seizures, and disorders relating to the field of neuropsychiatry.

摘要翻译： 衍生自以下通式的酸的单 - ，二 - ，三 - 和四 - 酯：其中R表示通式如下的酰基：其中n表示0或1，m表示0 ，1,2,3或4，R 1和R 2各自表示具有1至5个碳原子的直链或支链烷基，R 3表示氢或具有1至5个碳的直链或支链烷基 原子时，R 3和R 2中的碳原子的总和为4至10，当R 3表示氢时，当R 3不同于氢时，R 1，R 2和R 3中的碳原子之和为6至15，或R 1和R 2 当它们一起表示四亚甲基，五亚甲基或六亚甲基时，R 3表示直链烷基和选自甘油，2,3-环氧丙醇，1,2-丙二醇，1,3 丙二醇，1,2-丁二醇，1,3-丁二醇，1,4-丁二醇，1,2,3-丁三醇，1,2,4-丁三醇，1,2,3,4-丁酮，2-丁醇 1,4-丁二醇，2-丁炔-1,4-二醇，二甘醇，环己二醇优选1,2-环己二醇，硫二甘醇，二乙醇胺，NR-取代二乙醇胺，三羟甲基丙烷，季戊四醇和通式如下的醇： 其中p表示0或1，R4表示甲基，R5表示甲基，乙基，2-甲基 - 丁基或R4和R5，当它们一起表示五亚甲基时，除三 乙酸二正丙酯）。 这些酯可用于治疗中枢神经系统疾病，特别是包括惊厥状态和癫痫发作以及与神经精神病学领域有关的疾病。

公开(公告)号：US4115401A

公开(公告)日：1978-09-19

申请号：US783284

申请日：1977-03-31

申请人： Souli Nanthavong ,  Charles Pigerol ,  Pierre Eymard ,  Jacques Simiand

发明人： Souli Nanthavong ,  Charles Pigerol ,  Pierre Eymard ,  Jacques Simiand

IPC分类号： C07D207/27 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/5575 ,  A61K31/559 ,  A61P43/00 ,  C07C53/128 ,  C07C405/00 ,  C07D207/26 ,  C07F9/40 ,  C07D207/12

CPC分类号： C07D207/26 ,  C07C53/128 ,  C07F9/4006 ,  Y10S514/826 ,  Y10S514/927 ,  Y10S514/929

摘要： Prostaglandin derivatives corresponding to the general formula: ##STR1## wherein R.sub.1 represents hydrogen, methyl or ethyl, R.sub.2, R.sub.3 and R.sub.4, which are the same or different, each represent hydrogen or methyl and R is selected from the groups consisting of: ##STR2## in which R.sub.5 represents hydrogen, methyl or ethyl, R.sub.6 represents methyl, ethyl or acetyl and R.sub.7 and R.sub.8, when they are different, each represent hydrogen or a branched- or straight-chain alkyl group having from 1 to 7 carbon atoms or R.sub.7 and R.sub.8, when they are identical, each represent hydrogen or a straight-chain alkyl group having from 1 to 3 carbon atoms with the provisos that:When both R.sub.7 and R.sub.8 represent hydrogen, R.sub.5 is methyl or ethyl,When R.sub.5 represents methyl and R.sub.2, R.sub.3, R.sub.4, R.sub.7 and R.sub.8 all represent hydrogen then R.sub.1 is ethyl,The said prostaglandin derivatives being in the form of a mixture of isomers or of an individual isomer. They are useful in the treatment of pathological states which affect the respiratory system.

摘要翻译： 对应于以下通式的前列腺素衍生物：其中R 1表示氢，甲基或乙基，R 2，R 3和R 4相同或不同，各自表示氢或甲基，R选自由以下组成的组：其中R 5表示氢，甲基或乙基，R 6表示甲基，乙基或乙酰基，且R 7和R 8不同时，分别代表氢或具有1至7个碳的支链或直链烷基 原子或R 7和R 8，当它们相同时，各自表示氢或具有1至3个碳原子的直链烷基，条件是：

公开(公告)号：US4201725A

公开(公告)日：1980-05-06

申请号：US888187

申请日：1978-03-20

申请人： Charles Pigerol ,  Pierre Eymard ,  Jean-Claude Vernieres ,  Jean-Pierre Werbenec ,  Madeleine C. Epse Broll

发明人： Charles Pigerol ,  Pierre Eymard ,  Jean-Claude Vernieres ,  Jean-Pierre Werbenec ,  Madeleine C. Epse Broll

IPC分类号： A61K31/13 ,  C07C87/08

CPC分类号： A61K31/13

摘要： Methylamine derivatives of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein R.sub.1 and R.sub.3 each represent a hydrogen atom or a straight- or branched-chain alkyl, alkenyl or alkynyl radical containing from 1 to 6 carbon atoms, R.sub.2 represents a straight- or branched-chain alkyl, alkenyl or alkynyl radical containing from 2 to 7 carbon atoms with the proviso that when R.sub.2 represents an alkenyl radical of the formula CH.dbd.CH--R.sub.6 or an alkynyl radical of the formula C.tbd.C--R.sub.6, in which R.sub.6 represents a hydrogen atom or a straight- or branched-chain alkyl radical of 1 to 5 carbon atoms, R.sub.1 and R.sub.3 each represent an atom of hydrogen or an alkyl radical, R.sub.4 and R.sub.5, which are the same or different, each respresent a hydrogen atom, a straight- or branched-chain alkyl, alkenyl or alkynyl radical containing from 1 to 5 carbon atoms or an .omega.-hydroxyalkyl radical containing from 2 to 5 carbon atoms or R.sub.4 and R.sub.5, when they are taken together represent an alkylene radical containing from 2 to 6 carbon atoms, an alkylidene radical containing from 1 to 5 carbon atoms or the radical --CH.sub.2 --CH.sub.2 --O--CH.sub.2 --CH.sub.2 --, R.sub.1, R.sub.2 and R.sub.3 being such that the trisubstituted methylamine radical possesses no more than 13 carbon atoms.They are useful for treating Parkinson's disease and for correcting extra-pyramidal disturbances provoked by neuroleptics.

摘要翻译： 下式的甲胺衍生物及其药学上可接受的酸加成盐，其中R 1和R 3各自表示氢原子或含有1至6个碳原子的直链或支链烷基，烯基或炔基，R 2表示 含有2至7个碳原子的直链或支链烷基，烯基或炔基，条件是当R 2表示式CH = CH-R 6的烯基或式C的炔基时， ，其中R 6表示氢原子或1至5个碳原子的直链或支链烷基，R 1和R 3各自表示氢或烷基的原子，R 4和R 5相同或不同， 各自表示氢原子，含有1至5个碳原子的直链或支链烷基，烯基或炔基或含有2至5个碳原子的ω-羟基烷基或R 4和R 5一起代表 亚烷基 含有2至6个碳原子的烷基，含有1至5个碳原子的亚烷基或基团-CH 2 -CH 2 -O-CH 2 -CH 2 - ，R 1，R 2和R 3使得三取代的甲基胺基团不超过 13个碳原子。 它们可用于治疗帕金森病和矫正精神安定药引起的金字塔外的紊乱。