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    Amides of pyrrolidinoethylamine which can be used in lung therapy
    1.
    发明授权
    Amides of pyrrolidinoethylamine which can be used in lung therapy 失效
    可用于肺部治疗的吡咯烷基乙胺的酰胺

    公开(公告)号：US4192883A

    公开(公告)日：1980-03-11

    申请号：US931489

    申请日：1978-08-07

    申请人： Henri Cousse ,  Bernard Bonnaud ,  Jean-Pierre Tarayre ,  Silvano Casadio

    发明人： Henri Cousse ,  Bernard Bonnaud ,  Jean-Pierre Tarayre ,  Silvano Casadio

    IPC分类号： C07D279/30 ,  C07D295/13 ,  C07D311/12 ,  C07D311/84 ,  A61K31/40 ,  C07D295/14

    CPC分类号： C07D295/13 ,  C07D279/30 ,  C07D311/12 ,  C07D311/84

    摘要： New chemical compounds, which are pyrrolidinoethylamine amides, in the form of free bases and salts thereof, which are useful as antitussives, pharmaceutical compositions thereof, and method of treating therewith.In the form of their salts, the compounds have the formula: ##STR1## wherein ##STR2## is an acyl radical of a phenylacetic,.alpha.-phenyl-.alpha.-ethylacetic, diphenylacetic, benzilic, .alpha.-lower-alkoxy-.alpha.,.alpha.-diphenylacetic, 10-phenothiazinecarboxylic, benzoic, halobenzoic, 3-coumarincarboxylic, 9-xanthenecarboxylic, salicylic, cresotic, halocresotic, lower-alkoxybenzoic, phenoxyacetic, phenoxyisobutyric, halophenoxyisobutyric, cinnamic, or 9-fluorene carboxylic acid, and wherein R'H represents an inorganic or organic acid, and wherein R may be, for example, a substituted aromatic ring of the formula: ##STR3## wherein R.sub.1 and R.sub.2 may independently be lower-alkyl, lower-alkoxy, hydrogen, lower-alkenyloxy, or lower-alkynyloxy, and X may be hydrogen or halogen.Medicaments containing these active principles may be used, inter alia, in the treatment of coughs and respiratory complaints.

    摘要翻译： 新的化合物，它们是吡咯烷基乙胺酰胺，其形式为游离碱和盐，它们可用作镇咳药，其药物组合物及其处理方法。 以它们的盐的形式，化合物具有下式：其中是苯乙酸，α-苯基-α-乙基乙酸，二苯基乙酸，苯偶酰，α-低级烷氧基-α，α 二苯乙酸，10-吩噻嗪羧酸，苯甲酸，卤代苯甲酸，3-香豆素羧酸，9-呫吨羧酸，水杨酸，间歇，卤代，低级烷氧基苯甲酸，苯氧基乙酸，苯氧基异丁酰，卤代苯氧基异丁酸，肉桂酸或9-芴羧酸，其中R'H代表 无机或有机酸，其中R可以是例如下式的取代芳环：其中R 1和R 2可以独立地为低级烷基，低级烷氧基，氢，低级烯氧基或低级 - 炔氧基，X可以是氢或卤素。 含有这些积极原则的药物，除其他外，可用于治疗咳嗽和呼吸道疾病。

    1-Aryl 2-aminomethyl cyclopropane carboxylates (Z)
    5.
    发明授权
    1-Aryl 2-aminomethyl cyclopropane carboxylates (Z) 失效
    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。

    1-Aryl 2-aminomethyl cyclopropane carboxylates (Z) as drugs in the treatment of pain
    6.
    发明授权
    1-Aryl 2-aminomethyl cyclopropane carboxylates (Z) as drugs in the treatment of pain 失效
    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。

    1-Aryl 2-aminomethyl cyclopropane carboxyamide (Z) derivatives and their use as useful drugs in the treatment of disturbances of the central nervous system
    7.
    发明授权
    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
    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。

    2'-(Orthochlorobenzoyl)-4'-chloroglycylanilides, compositions thereof, and use as medicaments
    10.
    发明授权
    2'-(Orthochlorobenzoyl)-4'-chloroglycylanilides, compositions thereof, and use as medicaments 失效
    2' - （邻氯苯甲酰基）-4'-氯草酰酰苯胺及其组合物，并用作药物

    公开(公告)号：US4382930A

    公开(公告)日：1983-05-10

    申请号：US220514

    申请日：1980-12-29

    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 ,  C07D295/14

    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。