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    N-phenylglycinamide CCK antagonists and pharmaceutical compositions containing them
    4.
    发明授权
    N-phenylglycinamide CCK antagonists and pharmaceutical compositions containing them 失效
    N-苯基甘氨酰胺CCK拮抗剂和含有它们的药物组合物

    公开(公告)号：US5475106A

    公开(公告)日：1995-12-12

    申请号：US924065

    申请日：1992-10-08

    申请人： Jean-Dominique Bourzat ,  Marc Capet ,  Claude Cotrel ,  Claude Guyon ,  Franco Manfre ,  Gerard Roussel

    发明人： Jean-Dominique Bourzat ,  Marc Capet ,  Claude Cotrel ,  Claude Guyon ,  Franco Manfre ,  Gerard Roussel

    IPC分类号： A61K38/00 ,  A61K38/05 ,  A61P1/00 ,  A61P3/04 ,  A61P21/00 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  A61P35/00 ,  C07K1/02 ,  C07K1/113 ,  C07K5/00 ,  C07K5/06 ,  C07K5/065 ,  A61K31/325 ,  C07C205/00 ,  C07C229/00

    CPC分类号： C07K5/06026 ,  A61K38/00

    摘要： Compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom, an alkyl or alkoxycarbonyl radical or a phenyl radical, optionally substituted,R.sub.2 represents an alkoxy, optionally substituted cycloalkyloxy, cycloalkylalkyloxy, phenylalkyloxy, polyfluoroalkyloxy or cinnamyloxy radical or a radical --NR.sub.5 R.sub.6,R.sub.3 represents a phenylamino radical in which the phenyl ring is optionally substituted, an optionally substituted phenyl radical or a naphthyl, indolyl or quinolyl radical,R.sub.4 represents a substituted phenyl radical,R.sub.5 and R.sub.6, which may be identical or different, represent a hydrogen atom or an alkyl, optionally substituted phenyl, indanyl, cycloalkylalkyl, cycloalkyl or phenylalkyl radical, or alternatively R.sub.5 and R.sub.6, together with the nitrogen atom to which they are attached, form a heterocycle, their preparation and medicinal products containing them.

    摘要翻译： PCT No.PCT / FR91 / 00174 Sec。 371日期：1992年10月8日 102（e）日期1992年10月8日PCT 1991年3月5日PCT公布。 第WO91 / 13907号公报 1991年9月19日，化学式：其中R 1表示氢原子，烷基或烷氧基羰基或苯基，任意取代的式（I）化合物：R 2表示烷氧基，任选取代的环烷氧基，环烷基烷氧基，苯基烷氧基 ，多氟烷氧基或肉桂氧基或自由基-NR5R6，R3表示苯基氨基，其中苯环任选被取代，任选取代的苯基或萘基，吲哚基或喹啉基，R4表示取代的苯基，R5和R6， 其可以相同或不同，表示氢原子或烷基，任选取代的苯基，二氢化茚基，环烷基烷基，环烷基或苯基烷基，或者R5和R6与它们所连接的氮原子一起形成杂环，它们 制剂和含有它们的药用产品。

    Pyrrole derivatives, and pharmaceutical compositions which contain them and pharmacological methods of use
    6.
    发明授权
    Pyrrole derivatives, and pharmaceutical compositions which contain them and pharmacological methods of use 失效
    吡咯衍生物和含有它们的药物组合物和药理学方法

    公开(公告)号：US4960779A

    公开(公告)日：1990-10-02

    申请号：US360122

    申请日：1989-06-01

    申请人： Jean-Dominique Bourzat ,  Marc Capet ,  Claude Cotrel ,  Richard Labaudiniere ,  Philippe Pitchen ,  Gerard Roussel

    发明人： Jean-Dominique Bourzat ,  Marc Capet ,  Claude Cotrel ,  Richard Labaudiniere ,  Philippe Pitchen ,  Gerard Roussel

    IPC分类号： C07D209/46 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61K31/495 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  C07D221/12 ,  C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D519/00

    CPC分类号： C07D401/04 ,  C07D471/04

    摘要： Pyrrole derivatives of formula (I): ##STR1## in which A forms with the pyrrole ring an isoindoline, 6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, 2,3,6,7-tetrahydro-5H-[1,4]oxathiino[2,3-c]pyrrole or 2,3,6,7-tetrahydro-5H-[1,4]dithiino[2,3-c]pyrrole ring-system, Het.dbd.naphthyridinyl, pyridyl or quinolyl which are unsubstituted or substituted with halogen, (1 to 4 C) alkyl, (1 to 4 C) alkyloxy, (1 to 4 C) alkylthio or CF.sub.3, Y.dbd.CO, C.dbd.NOH or CHOH and R.dbd.(3 to 10 C) alkenyl, alkyl which is unsubstituted or substituted with OH, alkyloxy, alkylthio, (3 to 6 C) cycloalkyl, NH.sub.2, alkylamino, dialkylamino, alkylcarbonylamino, piperazinyl, piperidyl, 1-azetidinyl, morpholino, pyrrolidinyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, (1-piperazinyl)carbonyl, piperidinocarbonyl, pyrrolidinocarbonyl, phenyl, pyridyl, 1-imidazolyl or alternatively R.dbd.2- or 3-pyrrolididnyl, 2-, 3- or 4-piperidyl, (3 to 6 C) cycloalkyl or phenyl which is unsubstituted or substituted with halogen, (1 to 4 C) alkyl, (1 to 4 C) alkyloxy, (1 to 4 C) alkylthio, the said alkyl radicals and portions containing, except where specifically stated, 1 to 10 C, and the piperazinyl, piperidino, piperidyl, pyrrolidinyl, azetidinyl radicals being unsubstituted or substituted at any position by alkyl, alkylcarbonyl, benzyl or hydroxyalkyl, or can alternatively form a lactam group with the nitrogen atom of the ring, and their salts and optical isomers are useful as anxiolytics.

    摘要翻译： 式（I）的吡咯衍生物：其中A与吡咯环形成异吲哚啉，6,7-二氢-5H-吡咯并[3,4-b]吡嗪，2,3,6,7 - 四氢-5H- [1,4]氧硫杂环[2,3-c]吡咯或2,3,6,7-四氢-5H- [1,4]二噻唑并[2,3-c]吡咯环体系， Het =未被取代或被卤素取代的（1-4C）烷基，（1-4C）烷氧基，（1-4C）烷硫基或CF3，Y = CO，C = NOH或CHOH的萘啶基，吡啶基或喹啉 （3〜6）环烷基，NH 2，烷基氨基，二烷基氨基，烷基羰基氨基，哌嗪基，哌啶基，1-氮杂环丁烷基，吗啉代，吗啉代， 吡咯烷基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，（1-哌嗪基）羰基，哌啶子基羰基，吡咯烷基羰基，苯基，吡啶基，1-咪唑基或R = 2-或3-吡咯烷二基，2-，3-或4-哌啶基 6 C）未被取代或被卤素取代的环烷基或苯基，（1-4C）烷基，（1-4C） 烷氧基，（1〜4个C）烷硫基，所述烷基及其部分除特别说明为1-10个以外，其中哌嗪基，哌啶子基，哌啶基，吡咯烷基，氮杂环丁烷基在任意位置未被取代或被烷基取代， 烷基羰基，苄基或羟基烷基，或者可以与环的氮原子形成内酰胺基，其盐和旋光异构体可用作抗焦虑剂。

    Pyrrole derivatives, their preparation and pharmaceutical compositions which contain them
    7.
    发明授权
    Pyrrole derivatives, their preparation and pharmaceutical compositions which contain them 失效
    吡咯衍生物，它们的制备和含有它们的药物组合物

    公开(公告)号：US5102890A

    公开(公告)日：1992-04-07

    申请号：US402457

    申请日：1989-09-05

    申请人： Jean-Dominique Bourzat ,  Marc Capet ,  Claude Cotrel ,  Richard Labaudiniere ,  Philippe Pitchen ,  Gerard Roussel

    发明人： Jean-Dominique Bourzat ,  Marc Capet ,  Claude Cotrel ,  Richard Labaudiniere ,  Philippe Pitchen ,  Gerard Roussel

    IPC分类号： C07D471/04 ,  C07D519/00

    CPC分类号： C07D471/04

    摘要： This invention relates to pyrrole derivatives of formula: ##STR1## in which A forms with the pyrrole ring an isoindoline, 6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, 2,3,6,7-tetrahydro-5H-[1,4]oxathiino[2,3-c]pyrrole or 2,3,6,7-tetrahydro-5H-[1,4]dithiino[2,3-c]pyrrole ring-system and Hetis naphthyridinyl, pyridyl or quinolyl which is unsubstituted or substituted with halogen, (1 to 4 C) alkyl, (1 to 4 C) alkyloxy, (1 to 4 C) alkylthio or CF.sub.3 and R=(3 to 10 C) straight- or branched-chain alkenyl or alkyl which is unsubstituted or substituted with alkyloxy, alkylthio, (3 to 6 C) cycloalkyl, NH.sub.2, alkylamino, dialkylamino, alkylcarbonylamino, (in which the amino portion is optionally substituted with alkyl), 1- or 2-piperazinyl, piperidyl, piperidino, morpholino, pyrrolidinyl, 1-azetidinyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, (1-piperazinyl)carbonyl, piperidinocarbonyl, (1-pyrrolidinyl)carbonyl, phenyl, pyridyl, 1-imidazolyl, or alternatively R=2- or 3-pyrrolidinyl, 2-, 3- or 4-piperidyl, on the understanding that the alkyl radicals are straight- or branched-chain radicals and contain, except where specifically stated, 1 to 10 C, and that the piperazinyl, piperidino, piperidyl, pyrrolidinyl and azetidinyl radicals can be unsubstituted or substituted at any position with alkyl, alkylcarbonyl, benzyl or hydroxyalkyl, or can alternatively form a lactam group with the nitrogen atom of the ring, and, where they exist, their pharmaceutically acceptable salts and optical isomers, are useful as anxiolytics.

    摘要翻译： 本发明涉及下式的吡咯衍生物：其中A与吡咯环形成异吲哚啉，6,7-二氢-5H-吡咯并[3,4-b]吡嗪，2,3,6， -7- [1,4]恶二唑并[2,3-c]吡咯或2,3,6,7-四氢-5H- [1,4]二硫杂环[2,3-c]吡咯环体系 和未取代的或被卤素取代的吡啶基或喹啉基，（1-4C）烷基，（1-4C）烷氧基，（1-4C）烷硫基或CF3和R =（3-10C）直链 - 或支链烯基或烷基，其未被取代或被烷氧基，烷硫基，（3至6 C）环烷基，NH 2，烷基氨基，二烷基氨基，烷基羰基氨基（其中氨基部分任选被烷基取代）取代， 2-哌嗪基，哌啶基，哌啶子基，吗啉代，吡咯烷基，1-氮杂环丁烷基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，（1-哌嗪基）羰基，哌啶子基羰基，（1-吡咯烷基）羰基，苯基，吡啶基，1-咪唑基， 2-或3-吡咯烷基，2-，3-或4-哌啶基 基于这样的理解，烷基是直链或支链基，并含有，除非特别说明为1-10个碳原子，并且哌嗪基，哌啶子基，哌啶基，吡咯烷基和氮杂环丁烷基可以是未取代的或任何取代的 与烷基，烷基羰基，苄基或羟基烷基的位置，或者可选择地与环的氮原子形成内酰胺基，并且如果它们存在，其药学上可接受的盐和旋光异构体可用作抗焦虑剂。

    Pyrrole derivatives and pharmaceutical compositions which contain them as hypnotics and anticonvulsants
    8.
    发明授权
    Pyrrole derivatives and pharmaceutical compositions which contain them as hypnotics and anticonvulsants 失效
    含有它们作为催眠剂和抗惊厥药的吡咯衍生物和药物组合物

    公开(公告)号：US4898871A

    公开(公告)日：1990-02-06

    申请号：US126352

    申请日：1987-11-30

    申请人： Jean-Dominique Bourzat ,  Marc Capet ,  Claude Cotrel ,  Richard Labaudiniere ,  Philippe Pitchen ,  Gerard Roussel

    发明人： Jean-Dominique Bourzat ,  Marc Capet ,  Claude Cotrel ,  Richard Labaudiniere ,  Philippe Pitchen ,  Gerard Roussel

    IPC分类号： C07D209/46 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61K31/495 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D519/00

    CPC分类号： C07D401/04 ,  C07D471/04

    摘要： Pyrrole derivatives of formula ##STR1## in which A forms with the pyrrole ring an isoindoline, 6,7-dihydro-5H-pyrrolo-[3,4-b]pyrazine, 2,3,6,7-tetrahydro-5H-[1,4]-oxathiino-[2,3-c]pyrrole or 2,3,6,7-tetrahydro-5H-[1,4]dithiino-[2,3-c]pyrrole ring-system, Y+0, S or NH, Het=naphthyridinyl or quinolyl which are unsubstituted or substituted with halogen, (1 to 4 C) alkyl, (1 to 4 C) alkyloxy, (1 to 4 C) alkylthio, CN or CF.sub.3 and R=(3 to 10 C) alkenyl or alkyl which is unsubstituted or substituted with alkyloxy, alkylthio, cycloalkyl, alkylcarbonyl, cycloalkylcarbonyl or cycloalkylcarbamoyl in which the cycloalkyl portions contain 3 to 6 C, NH.sub.2, alkylamino, dialkylamino, alkylcarbonylamino, 1- or 2-piperazinyl, piperidyl, piperidino, morpholino, 1-azetidinyl, pyrrolidinyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, (1-piperazinyl)carbonyl, piperidinocarbonyl, piperidylcarbonyl, (1-pyrrolidinyl)carbonyl, morpholinocarbonyl, aminoalkylcarbamoyl, alkylaminoalkylcarbamoyl, dialkylaminoalkylcarbamoyl, alkyloxyalkylcarbamoyl, phenyl, pyridyl, or 1-imidazolyl, or R=2- or 3-pyrrolidinyl, or 1-imidazolyl, or 2-, 3- or 4-piperidyl, the aforesaid piperazinyl, piperidino, piperidyl, pyrrolidinyl, and azetidinyl radicals being unsubstituted or substituted at any position by alkyl, OH, alkylcarbonyl, benzyl, or hydroxyalkyl, or can form (i) a lactam group with the nitrogen atom of the ring or (ii) a 2-spirodioxolane residue with a carbon of the ring, and the said alkyl radicals containing 1 to 10 C except where specifically stated, are useful as anxiolytics.

    摘要翻译： 其中A与吡咯环形成异构吲哚，6,7-二氢-5H-吡咯并 - [3,4-b]吡嗪，2,3,6,7-四氢-5H- [ 1,4] - 氧硫杂环丁烷并[2,3-c]吡咯或2,3,6,7-四氢-5H- [1,4]二硫基 - [2,3-c]吡咯环系统，Y + （1-4C）烷基，（1-4C）烷氧基，（1-4C）烷硫基，CN或CF3和R =（3）中的任意一个或多个取代或未取代或被卤素取代的苯甲酰基， 未取代或被烷氧基，烷硫基，环烷基，烷基羰基，环烷基羰基或环烷基氨基甲酰基取代的烯基或烷基，其中环烷基部分含有3至6个C，NH 2，烷基氨基，二烷基氨基，烷基羰基氨基，1-或2-哌嗪基， 哌啶基羰基，（1-吡咯烷基）羰基，吗啉代羰基，氨基烷基氨基甲酰基，烷基氨基烷基氨基甲酰基，二烷基氨基烷基氨基 酰基，烷氧基烷基氨基甲酰基，苯基，吡啶基或1-咪唑基，或R = 2-或3-吡咯烷基或1-咪唑基，或2-，3-或4-哌啶基，上述哌嗪基，哌啶子基，哌啶基，吡咯烷基和 氮杂环丁烷基是未取代的或在任何位置被烷基，OH，烷基羰基，苄基或羟基烷基取代，或可以形成（i）具有环的氮原子的内酰胺基团或（ii）2-螺 环和所述含有1至10个C的烷基，除非特别说明，可用作抗焦虑剂。