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11. 发明授权

US5441980A Potentialization of pyrethroid by crotamiton which is useful in the treatment of pediculosis 失效
标题翻译：拟除虫菊酯通过克罗他米通的潜力，其可用于治疗pediculosis
公开(公告)号：US5441980A
公开(公告)日：1995-08-15
申请号：US46797
申请日：1993-04-16
申请人： Pierre Fabre , Gilbert Mouzin , Michel JeanJean , Nicole Monteny , Henri Cousse
发明人： Pierre Fabre , Gilbert Mouzin , Michel JeanJean , Nicole Monteny , Henri Cousse
IPC分类号： A01N37/24 , A01N53/00 , A01N53/08 , A61K8/37 , A61K8/42 , A61K31/215 , A61K31/275 , A61K31/40 , A61Q17/02 , C09D5/22
CPC分类号： A61K31/215 , A01N53/00 , A61K31/275 , A61K31/40 , A61K8/37 , A61K8/42 , A61Q17/02
摘要： The present invention relates to a dermatological and/or cosmetological composition which is useful in the treatment of pediculosis, characterized in that it contains a synergic combination of a pyrethroid and of crotamiton.The pyrethroids which are the subject of this composition are more particularly permethrin, bioallethrin, resmethrin, tetramethrin and deltamethrin.
摘要翻译：本发明涉及可用于治疗pediculosis的皮肤病学和/或美容组合物，其特征在于其含有拟除虫菊酯和克罗他米通的协同组合。作为该组合物的主题的拟除虫菊酯更特别是氯菊酯，生物菊酯，氯菊酯，溴氰菊酯和溴氰菊酯。

12. 发明授权

US4476061A 2'-(Orthochlorobenzoyl)-4'-chloroglycylanilides 失效
标题翻译： 2' - （邻氯苯甲酰基）-4'-氯草酰苯胺
公开(公告)号：US4476061A
公开(公告)日：1984-10-09
申请号：US409320
申请日：1982-08-18
申请人： Gilbert Mouzin , Henri Cousse , Antoine Stenger
发明人： Gilbert Mouzin , Henri Cousse , Antoine Stenger
IPC分类号： A61K31/165 , A61K31/535 , A61P21/02 , A61P25/18 , A61P25/20 , C07C231/12 , C07C237/04 , C07C237/06 , C07C275/38 , C07D295/15 , C07C103/737
CPC分类号： C07D295/15 , Y10S514/96 , Y10S514/962 , Y10S514/966
摘要： The present invention relates to 2'-(ortho-chlorobenzoyl)-4'-chloroglycylanilides, compositions thereof, and their use as medicaments, e.g., as anxiolytic agents.The compounds of the invention have the general formula I ##STR1## in which R represents hydrogen or alkyl,R.sub.1 and R.sub.2 may be identical or different and are selected from hydrogen, alkyl, hydroxyalkyl, alkenyl, and alkynyl, possibly substituted by alkyl, and cycloalkyl having three to six members, possibly substituted by alkyl, with the proviso that, when one of R.sub.1 and R.sub.2 represents hydrogen, the other is not lower alkyl or hydroxyalkyl; and with the further proviso that R.sub.1 and R.sub.2 may not simultaneously represent either hydrogen or lower-alkyl. R.sub.1 and R.sub.2 may furthermore form, with the nitrogen atom to which they are connected, a nitrogen heterocycle possibly containing a second heteroatom selected from oxygen and nitrogen.
摘要翻译：本发明涉及2' - （邻氯苯甲酰基）-4'-氯草酰苯胺，其组合物及其作为药物的用途，例如作为抗焦虑剂。本发明的化合物具有通式I（I）其中R表示氢或烷基，R 1和R 2可以相同或不同，并且选自氢，烷基，羟基烷基，烯基和炔基，可能被烷基和具有3至6个成员的环烷基，可能被烷基取代，条件是当R 1和R 2之一表示氢时，另一个不是低级烷基或羟烷基; 并且进一步的条件是R 1和R 2可以不同时表示氢或低级烷基。 R1和R2可以与它们所连接的氮原子形成可能含有选自氧和氮的第二杂原子的氮杂环。

13. 再颁专利

USRE31237E 2-Benzoyl-4-nitroanilides and their use as medicaments 失效
标题翻译： 2-苯甲酰基-4-硝基酰苯胺及其作为药物的用途
公开(公告)号：USRE31237E
公开(公告)日：1983-05-10
申请号：US350233
申请日：1982-02-19
申请人： Henri Cousse , Gilbert Mouzin
发明人： Henri Cousse , Gilbert Mouzin
IPC分类号： A61K31/165 , A61K31/535 , A61P25/20 , C07C237/04 , C07C237/06 , C07D295/15
CPC分类号： C07D295/15
摘要： New derivatives of 2-benzoyl-4-nitro anilides, their preparation and their use as medicaments.The new chemical derivatives of the invention have the general formula ##STR1## in which R represents a linear or branched alkyl group, an alkenyl group, a cycloalkyl group or a benzyl group,R.sub.1 represents a hydrogen atom, an alkyl group or a hydroxy alkyl group,R.sub.2 represents a hydroxy-alkyl, alkenyl or alkynyl group, possibly substituted one or more times by an alkyl radical, or a cycloalkyl group having three to six carbon atoms;R.sub.1 and R.sub.2 may furthermore form, with the nitrogen atom to which they are attached, a nitrogen heterocycle containing possibly a second heteroatom selected from among oxygen and nitrogen;under the condition, however, that when R.sub.2 represents a hydroxy-alkyl group R.sub.1 may not be a hydrogen atom.Use as hypnotic agents for the treatment of insomnia.

14. 发明授权

US4188387A Amino-aryl 1,24-triazines useful in the treatment of diverse pain 失效
标题翻译：氨基 - 芳基1,24-三嗪可用于治疗多种疼痛
公开(公告)号：US4188387A
公开(公告)日：1980-02-12
申请号：US884732
申请日：1978-03-09
申请人： Guy Pitet , Henri Cousse , Gilbert Mouzin , Antoine Stenger
发明人： Guy Pitet , Henri Cousse , Gilbert Mouzin , Antoine Stenger
IPC分类号： C07D253/06 , A61K31/53 , A61K31/535 , A61P29/00 , C07D253/07 , C07D413/10
CPC分类号： C07D253/065 , C07D253/07 , Y10S514/825
摘要： The invention relates to new chemical compounds which can be used as analgesic drugs and their preparation.The new chemical compounds have the general formula: ##STR1## in which: R is a lower alkylR.sub.1, which is always other than H, is a linear or branched lower alkyl, an allyl, amino alkyl of type ##STR2## in which n=2 to 4, R.sub.2 R.sub.3 represent a lower alkyl; they may also form a heterocycle with the nitrogen atom.Y is a hydrogen, halogen, lower alkyl, alkoxy, ##STR3## R being a lower alkyl. The position of Y is variable on the ring.X=oxygen or sulfur atom.The drugs containing these active principles may be used in the treatment of rheumatismal disturbances and various pains.
摘要翻译：本发明涉及可用作止痛药及其制剂的新化合物。新的化合物具有以下通式：其中：R为低级烷基，其总是不是H，是直链或支链的低级烷基，类型为“IMAGE”的烯丙基，氨基烷基，其中n = 2〜4，R2R3表示低级烷基; 它们也可以与氮原子形成杂环。 Y是氢，卤素，低级烷基，烷氧基，R是低级烷基。 Y的位置在环上是可变的。 X =氧或硫原子。含有这些活性成分的药物可用于治疗风湿性疾病和各种疼痛。

15. 发明授权

US4167566A Antithrombotic 2-prenyl-3-oxo-5,6-diaryl-as-triazenes 失效
标题翻译：抗血栓2-异戊烯基-3-氧代-5,6-二芳基 - 三氮烯
公开(公告)号：US4167566A
公开(公告)日：1979-09-11
申请号：US884733
申请日：1978-03-09
申请人： Guy Pitet , Henri Cousse , Gilbert Mouzin , Andre Delhon
发明人： Guy Pitet , Henri Cousse , Gilbert Mouzin , Andre Delhon
IPC分类号： C07D253/07 , C07D253/06 , A61K31/53
CPC分类号： C07D253/065 , C07D253/07 , Y10S514/822
摘要： The invention relates to compounds of the formula ##STR1## in which R and R' are identical or different and may be a hydrogen, an alkyl, a dialkylamino, an alkoxy, a halogen, or a hydroxy. These compounds are useful as drugs in the control of thromboses.
摘要翻译：本发明涉及式（I）的化合物，其中R和R'相同或不同并且可以是氢，烷基，二烷基氨基，烷氧基，卤素或羟基。这些化合物可用作控制血栓形成的药物。

16. 发明授权

US4567288A 1-Aryl 2-aminomethyl cyclopropane carboxylates (Z) 失效
标题翻译： 2-芳基2-氨基甲基环丙烷羧酸酯（Z）
公开(公告)号：US4567288A
公开(公告)日：1986-01-28
申请号：US656443
申请日：1984-10-01
申请人： Henri Cousse , Gilbert Mouzin , Bernard Bonnaud , Marie Charveron , Francois Fauran
发明人： Henri Cousse , Gilbert Mouzin , Bernard Bonnaud , Marie Charveron , Francois Fauran
IPC分类号： A61K31/445 , A61K31/451 , A61P25/04 , C07C67/00 , C07C229/46 , C07C301/00 , C07C303/40 , C07C311/39 , C07D211/14 , C07D295/155 , C07D307/14 , C07C79/46 , C07C101/02 , C07C101/30
CPC分类号： C07D295/155 , C07D211/14 , C07D307/14
摘要： The present invention concerns new derivatives of 1-aryl 2-aminomethyl cyclopropane carboxylates (Z), their preparation and their use as useful drugs for the treatment of various pains.The new derivatives of the present invention have the general formula I ##STR1## in which: R represents a hydrogen or halogen atom, a C.sub.1 to C.sub.4 lower alkyl group, a C.sub.1 to C.sub.4 lower alkoxy group, or a nitro, amino, sulfamoyl or hydroxy group;n represents the values 1, 2 or 3;(R).sub.n may together with the benzene ring also form the naphthyl group;R.sub.1 represents a linear or branched C.sub.1 to C.sub.5 alkyl or alkenyl group or an aryl or benzyl group;R.sub.2 and R.sub.3 represent a hydrogen atom, a linear or branched C.sub.1 to C.sub.5 alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl or dialkylaminoalkyl group or an aryl, arylalkyl or cycloalkyl group;R.sub.2 and R.sub.3 possibly also forming a heterocycle of 5 or 6 members with the adjacent nitrogen atom,provided however that when R.sub.1 represents the ethyl radical and R represents a hydrogen atom, R.sub.2 and R.sub.3 cannot simultaneously represent a methyl radical.
摘要翻译：本发明涉及1-芳基2-氨基甲基环丙烷羧酸酯（Z）的新衍生物，其制备及其作为治疗各种疼痛的有用药物的用途。本发明的新衍生物具有通式I（I），其中：R表示氢或卤素原子，C1至C4低级烷基，C1至C4低级烷氧基或硝基，氨基，氨磺酰基或羟基; n表示值1,2或3; （R）n可以与苯环一起形成萘基; R1表示直链或支链C1至C5烷基或烯基或芳基或苄基; R2和R3表示氢原子，直链或支链C1至C5烷基，烯基，炔基，羟基烷基，烷氧基烷基，羧基烷基或二烷基氨基烷基或芳基，芳烷基或环烷基; R2和R3也可能与相邻的氮原子形成5或6个成员的杂环，但是当R1表示乙基且R表示氢原子时，R2和R3不能同时代表甲基。

17. 发明授权

US4539413A Preparation of 3-amino-1-[(1,4-benzodioxan)-2-yl-methoxy]-2-propanols 失效
标题翻译：制备3-氨基-1 - [（1,4-苯并二恶烷）-2-基 - 甲氧基] -2-丙醇
公开(公告)号：US4539413A
公开(公告)日：1985-09-03
申请号：US455125
申请日：1983-01-03
申请人： Gilbert Mouzin , Henri Cousse , Pol Vilain
发明人： Gilbert Mouzin , Henri Cousse , Pol Vilain
IPC分类号： A61K31/335 , A61K31/357 , A61P9/06 , A61P9/12 , C07D319/20 , C07D319/14
CPC分类号： C07D319/20 , Y10S514/821
摘要： The present invention concerns a novel process for the production of new chemical compounds of the general formula: ##STR1## in which: R.sub.1 and R.sub.2 may be identical or different and represent a hydrogen or halogen atom or else a lower alkyl, lower alkoxy, nitro or acetyl group andR represents a lower alkyl or lower aralkyl group, such as benzyl.These compounds are useful in therapy for the treatment of hypertension and cardiac arrhythmia.The novel process involves reaction of a 2-hydroxymethyl-1,4-benzodioxan with epichlorohydrin to produce an intermediate glycidyl ether, which is then reacted with a primary amine to produce the final 3-amino-1-[(1,4-benzodioxan)-2-yl-methoxy]-2-propanol or an acid addition salt thereof.
摘要翻译：本发明涉及一种制备通式如下的新化合物的新方法：其中：R 1和R 2可以相同或不同，表示氢或卤素原子，或低级烷基，低级烷氧基，硝基或乙酰基，R表示低级烷基或低级芳烷基，例如苄基。这些化合物可用于治疗高血压和心律失常的治疗。该新方法涉及2-羟甲基-1,4-苯并二恶烷与表氯醇的反应以产生中间体缩水甘油醚，然后将其与伯胺反应以产生最终的3-氨基-1 - [（1,4-苯并二恶烷））-2-基 - 甲氧基] -2-丙醇或其酸加成盐。

18. 发明授权

US4511566A 2-N-Cycloalkylmethyl 3-oxo 5,6-diaryl-as-triazines 失效
标题翻译： 2-N-环烷基甲基3-氧代5,6-二芳基 - 三嗪
公开(公告)号：US4511566A
公开(公告)日：1985-04-16
申请号：US600473
申请日：1984-04-16
申请人： Guy Pitet , Henri Cousse , Gilbert Mouzin
发明人： Guy Pitet , Henri Cousse , Gilbert Mouzin
IPC分类号： C07D253/06 , A61K31/53 , A61P7/02 , A61P25/04 , C07C17/16 , C07D253/07 , C07D401/14 , C07D405/14 , C07D409/14 , C07D401/04
CPC分类号： C07D409/14 , C07C17/16 , C07D253/07 , C07D401/14 , C07D405/14
摘要： The present invention concerns new 2-N-cycloalkylmethyl 3-oxo 5,6-diaryl as-triazines, their method of production, pharmaceutical compositions thereof, and their use as medicaments, for treating pain.The derivatives of 2-N-cycloalkylmethyl 3-oxo 5,6-diaryl as-triazine according to the invention have the general formula I ##STR1## in which Ar represents a phenyl, furyl, thienyl, or pyridyl group, which group may possibly be substituted by a lower C.sub.1 to C.sub.4 alkoxy radical, in particular by the methoxy radical, andn is a whole number having a value of 1 to 4.
摘要翻译：本发明涉及新的2-N-环烷基甲基3-氧代5,6-二芳基三嗪，它们的制备方法，其药物组合物及其作为药物的用途，用于治疗疼痛。根据本发明的2-N-环烷基甲基3-氧代5,6-二芳基 - 三嗪的衍生物具有通式I（I），其中Ar表示苯基，呋喃基，噻吩基或吡啶基，其中基团可能被低级C1至C4烷氧基取代，特别是被甲氧基取代，n为整数，其值为1至4。

19. 发明授权

US4507318A 1-Aryl 2-aminomethyl cyclopropane carboxylates (Z) as drugs in the treatment of pain 失效
标题翻译： 1-芳基2-氨基甲基环丙烷羧酸盐（Z）作为药物治疗疼痛
公开(公告)号：US4507318A
公开(公告)日：1985-03-26
申请号：US390811
申请日：1982-06-22
申请人： Henri Cousse , Gilbert Mouzin , Bernard Bonnaud , Marie Charveron , Francois Fauran
发明人： Henri Cousse , Gilbert Mouzin , Bernard Bonnaud , Marie Charveron , Francois Fauran
IPC分类号： A61K31/445 , A61K31/451 , A61P25/04 , C07C67/00 , C07C229/46 , C07C301/00 , C07C303/40 , C07C311/39 , C07D211/14 , C07D295/155 , C07D307/14 , A61K31/34 , A61K31/215 , A61K31/395 , C07C93/24
CPC分类号： C07D295/155 , C07D211/14 , C07D307/14
摘要： The present invention concerns new derivatives of 1-aryl 2-aminomethyl cyclopropane carboxylates (Z), their preparation and their use as useful drugs for the treatment of various pains.The new derivatives of the present invention have the general formula I ##STR1## in which: R represents a hydrogen or halogen atom, a C.sub.1 to C.sub.4 lower alkyl group, a C.sub.1 to C.sub.4 lower alkoxy group, or a nitro, amino, sulfamoyl or hydroxy group;n represents the values 1, 2 or 3;(R).sub.n may together with the benzene ring also form the naphthyl group;R.sub.1 represents a linear or branched C.sub.1 to C.sub.5 alkyl or alkenyl group or an aryl or benzyl group;R.sub.2 and R.sub.3 represent a hydrogen atom, a linear or branched C.sub.1 to C.sub.5 alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl or dialkylaminoalkyl group or an aryl, arylalkyl or cycloalkyl group;R.sub.2 and R.sub.3 possibly also forming a heterocycle of 5 or 6 members with the adjacent nitrogen atom,provided however that when R.sub.1 represents the ethyl radical and R represents a hydrogen atom, R.sub.2 and R.sub.3 cannot simultaneously represent a methyl radical.
摘要翻译：本发明涉及1-芳基2-氨基甲基环丙烷羧酸酯（Z）的新衍生物，其制备及其作为治疗各种疼痛的有用药物的用途。本发明的新衍生物具有通式I（I），其中：R表示氢或卤素原子，C1至C4低级烷基，C1至C4低级烷氧基或硝基，氨基，氨磺酰基或羟基; n表示值1,2或3; （R）n可以与苯环一起形成萘基; R1表示直链或支链C1至C5烷基或烯基或芳基或苄基; R2和R3表示氢原子，直链或支链C1至C5烷基，烯基，炔基，羟基烷基，烷氧基烷基，羧基烷基或二烷基氨基烷基或芳基，芳烷基或环烷基; R2和R3也可能与相邻的氮原子形成5或6个成员的杂环，但是当R1表示乙基且R表示氢原子时，R2和R3不能同时代表甲基。

20. 发明授权

US4478836A 1-Aryl 2-aminomethyl cyclopropane carboxyamide (Z) derivatives and their use as useful drugs in the treatment of disturbances of the central nervous system 失效
标题翻译： 2-芳基2-氨基甲基环丙烷羧酰胺（Z）衍生物及其作为治疗中枢神经系统紊乱的有用药物
公开(公告)号：US4478836A
公开(公告)日：1984-10-23
申请号：US390810
申请日：1982-06-22
申请人： Gilbert Mouzin , Henri Cousse , Bernard Bonnaud , Michel Morre , Antoine Stenger
发明人： Gilbert Mouzin , Henri Cousse , Bernard Bonnaud , Michel Morre , Antoine Stenger
IPC分类号： A61K31/165 , A61K31/40 , A61K31/535 , A61K31/5375 , A61P25/24 , A61P25/26 , C07C67/00 , C07C231/00 , C07C231/02 , C07C237/24 , C07D295/18 , C07D295/185
CPC分类号： C07D295/185
摘要： The present invention concerns new derivatives of 1-aryl 2-aminomethyl cyclopropane carboxamides (Z) of general formula I: ##STR1## in which: R represents a hydrogen or halogen atom, a lower alkyl group, a lower alkoxy group, or a hydroxy. nitro or amino group;n represents the value 1 or 2;R.sub.1 and R.sub.2 represent a hydrogen atom, a lower alkyl group, an aryl or lower alkaryl group, possibly substituted, preferably in para position, by a halogen atom, preferably a chlorine atom;R.sub.1 and R.sub.2 may also form a heterocycle having 5 or 6 members with the adjacent nitrogen atom;R.sub.3 and R.sub.4 represent a hydrogen atom or a lower alkyl group;R.sub.3 and R.sub.4 may also form with the adjacent nitrogen atom a heterocycle having 5 or 6 members, possibly containing an additional heteroatom selected from among nitrogen and oxygen,as well as their salts with therapeutically acceptable inorganic or organic acids, and their pharmaceutical compositions and use in the treatment of central nervous system disturbances, e.g., depression.
摘要翻译：本发明涉及通式I的1-芳基2-氨基甲基环丙烷甲酰胺（Z）的新衍生物：其中：R表示氢或卤素原子，低级烷基，低级烷氧基，或羟基。硝基或氨基; n表示值1或2; R 1和R 2表示氢原子，低级烷基，芳基或低级烷芳基，可能被卤素原子，优选氯原子取代，优选在对位。 R1和R2也可以与相邻的氮原子形成具有5或6个成员的杂环; R3和R4表示氢原子或低级烷基; R3和R4还可以与相邻的氮原子一起形成具有5或6个成员的杂环，可能含有另外的选自氮和氧的杂原子，以及它们与治疗上可接受的无机或有机酸的盐，以及它们的药物组合物和用途在治疗中枢神经系统紊乱时，例如抑郁症。

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