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    2-amino naphthyridine derivative, its preparation and its use
    1.
    发明授权
    2-amino naphthyridine derivative, its preparation and its use 失效
    2-氨基萘啶衍生物，其制备及其用途

    公开(公告)号：US5498716A

    公开(公告)日：1996-03-12

    申请号：US181641

    申请日：1994-01-12

    申请人： Marie-Therese David-Comte ,  Gerard Roussel

    发明人： Marie-Therese David-Comte ,  Gerard Roussel

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04

    摘要： The present invention relates to a novel 2-aminonaphthyridine compounds that are useful in preparing a 2-isoindolinyl napthyridine compound that exhibits remarkable anxiolytic, hypnotic, anticonvulsant, antiepileptic and muscle-relaxant properties. The invention is also directed to the optical isomers of the 2-amino napthyridine compounds and salts thereof, their preparation and the use of the 2-amino napthyridine compounds for preparing the 2-isoindolinyl napthyridine compound.

    摘要翻译： 本发明涉及一种新的2-氨基萘啶化合物，其可用于制备显示出显着的抗焦虑，催眠，抗惊厥，抗癫痫和肌肉松弛性质的2-异吲哚啉基萘啶化合物。 本发明还涉及2-氨基萘啶化合物及其盐的光学异构体，其制备方法和2-氨基萘啶化合物用于制备2-异吲哚啉基萘啶化合物的用途。

    Amides based on certain 1,8-naphtyridine-2-amines useful as anxiolytics
    3.
    发明授权
    Amides based on certain 1,8-naphtyridine-2-amines useful as anxiolytics 失效
    基于某些可用作抗焦虑药的1,8-萘啶-2-胺的酰胺

    公开(公告)号：US4753941A

    公开(公告)日：1988-06-28

    申请号：US2996

    申请日：1987-01-13

    申请人： Claude Cotrel ,  Claude Guyon ,  Gerard Roussel ,  Gerard Taurand

    发明人： Claude Cotrel ,  Claude Guyon ,  Gerard Roussel ,  Gerard Taurand

    IPC分类号： A61K31/435 ,  A61P21/02 ,  A61P25/20 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The invention provides new substituted amides of formulaR--CONH--Hetin which:either R is phenyl substituted by acyloxy, alkylthio or alkyloxycarbonylamino, or by chloro at the 2- or 4-position, or by two alkyloxy radicals, or R is 2- or 4-pyridyl, pyrazinyl, 5,6-dihydrodithiin-2-yl, 5,6-dihydrooxathiin-2-yl, 1,3-dithiolyl, thiazolyl or substituted thienyl or furyl, or R is alkenyl (of 2 to 4 carbons) unsaturated in the .alpha.-position to the amide carbonyl, and Het is 1,8-naphthyridin-2-yl substituted at the 7-position by halogen, alkyloxy, phenoxy, 3-chloro- or dichlorophenoxy, hydroxy or cyano,or R is methoxyphenyl and Het is 1,8-naphthyridin-2-yl substituted in the 7-position by 3-chloro- or dichlorophenoxy, hydroxy or cyano, or R is methoxy-3-pyridazinyl and Het is 1,8-naphthyridin-2-yl substituted at the 7-position by phenoxy, the said alkyl and acyl radicals containing 1 to 4 carbon atoms in a linear or branched chain, their preparation and the pharmaceutical compositions which contain them.These new amides are useful as anxiolytics, hypnotics and muscle relaxants.

    摘要翻译： 本发明提供新的式R-CONH-Het取代的酰胺，其中R是被酰氧基，烷硫基或烷氧基羰基氨基取代的苯基，或在2-或4-位被氯取代，或被两个烷氧基取代，或者R 2是 - 或4-吡啶基，吡嗪基，5,6-二氢二硫杂环戊烯-2-基，5,6-二羟基硫蛋白-2-基，1,3-二硫基，噻唑基或取代的噻吩基或呋喃基，或R为烯基（2至4个 碳原子）与酰胺羰基的α-位不饱和，Het是在7-位被卤素，烷氧基，苯氧基，3-氯 - 或二氯苯氧基，羟基或氰基取代的1,8-萘啶-2-基，或 R是甲氧基苯基，Het是在3-位被3-氯 - 或二氯苯氧基，羟基或氰基取代的1,8-萘啶-2-基，或R是甲氧基-3-哒嗪基，Het是1,8-萘啶-2-酮， 在7-位被苯氧基取代的2-取代基，所述烷基和酰基在直链或支链中含有1至4个碳原子，其制备和药物组合物 包含它们 这些新型酰胺可用作抗焦虑药，催眠药和肌肉松弛剂。

    N-(1,8-naphthyridin-2-yl) amides and their pharmaceutical use
    4.
    发明授权
    N-(1,8-naphthyridin-2-yl) amides and their pharmaceutical use 失效
    N-（1,8-萘啶-2-基）酰胺及其药物用途

    公开(公告)号：US4642308A

    公开(公告)日：1987-02-10

    申请号：US755896

    申请日：1985-07-17

    申请人： Claude Cotrel ,  Claude Guyon ,  Gerard Roussel ,  Gerard Taurand

    发明人： Claude Cotrel ,  Claude Guyon ,  Gerard Roussel ,  Gerard Taurand

    IPC分类号： C07D215/08 ,  A61K31/435 ,  A61K31/47 ,  A61K31/4709 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  A61P25/22 ,  A61P39/02 ,  C07D213/80 ,  C07D215/38 ,  C07D471/04 ,  A61K31/50 ,  A61K31/44 ,  C07D237/24

    CPC分类号： C07D213/80 ,  C07D215/38 ,  C07D471/04

    摘要： The invention provides novel substituted amides of formula:R--CONH--Hetin which R is cycloalkyl, cyclohexadienyl, phenyl optionally substituted with one or 2 fluorine atoms or with a hydroxy radical, or substituted at position 3- or 4- with an alkyl or alkyloxy radical, or with a methylenedioxy radical at positions 3- and 4-, or at position 2- or 3- with a dialkylamino radical, or is 3-pyridyl, alkyloxy-3-pyridyl, thienyl, alkylthienyl, furyl, tetrahydropyridyl, pyridazinyl and alkylpyridazinyl, and Het is 2-quinolyl or 1,8-naphthyridin-2-yl, both optionally substituted at position 7- with a halogen atom or a hydroxymethyl, alkyl, alkyloxy, alkyloxyalkyloxy, alkenyloxy or alkynyloxy radical (of 3 or 4 carbon atoms), an alkylthio or benzylthio radical, a phenoxy radical which is optionally substituted (with fluorine, with chlorine or bromine at position 2-, or with an alkyloxy radical or 1 or 2 alkyl radicals) or with pyridyloxy or alkylpiperidyloxy, provided that, when Het is 2-quinolyl, R is other than phenyl, and that the radicals and alkyl portions contain 1 to 4 carbon atoms each in a linear or branched chain.The new products are useful as anxiolytics, hypnotics, anticonvulsants, antiepileptics and muscle relaxants. The invention also provides a process for the preparation of, and pharmaceutical compositions containing, the new compounds.

    摘要翻译： 本发明提供新的式R-CONH-Het的取代酰胺，其中R是环烷基，环己二烯基，任选被一个或两个氟原子或羟基取代的苯基，或在3-或4-位被烷基取代或 或在3-位和4-位的亚甲二氧基或与2-烷基氨基的位置2-或3-一起形成亚甲二氧基，或3-吡啶基，烷氧基-3-吡啶基，噻吩基，烷基噻吩基，呋喃基，四氢吡啶基，哒嗪基 和烷基哒嗪基，和Het是2-喹啉基或1,8-萘啶-2-基，它们任选地在7-位被卤素原子或羟甲基，烷基，烷氧基，烷氧基氧基，烯氧基或炔氧基（3或4个 碳原子），烷硫基或苄硫基，苯氧基，其任选地被取代（氟，与氯或溴在位置2-，或与烷氧基或1或2个烷基基团）或与吡啶氧基或烷基哌啶氧基取代，条件是 当Het是2-quinoly时 l，R不是苯基，并且基团和烷基部分各自含有1-4个碳原子的直链或支链。 新产品可用作抗焦虑药，催眠药，抗惊厥药，抗癫痫剂和肌肉松弛剂。 本发明还提供了制备含有新化合物的药物组合物的方法。

    Process for preparing pyrrolo(1,2-A)azepinone derivatives
    6.
    发明授权
    Process for preparing pyrrolo(1,2-A)azepinone derivatives 失效
    制备吡咯（1,2-A）氮杂酮衍生物的方法

    公开(公告)号：US4826974A

    公开(公告)日：1989-05-02

    申请号：US116725

    申请日：1987-11-04

    申请人： Michel Barreau ,  Marie-Therese Comte ,  Daniel Farge ,  Jean-Luc Malleron ,  Gerard Ponsinet ,  Gerard Roussel

    发明人： Michel Barreau ,  Marie-Therese Comte ,  Daniel Farge ,  Jean-Luc Malleron ,  Gerard Ponsinet ,  Gerard Roussel

    IPC分类号： A61K31/55 ,  A61P25/18 ,  C07D487/04 ,  C07D487/06 ,  C07D403/14 ,  C07D413/14

    CPC分类号： C07D487/04

    摘要： Pyrrolo[1,2-a]azepinone derivatives of formula: ##STR1## in which R.sub.3 is H or halogen and either (A) R is benzyl or phenylthio in which the phenyls are optionally substituted by one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals, R.sub.1 and R.sub.2, which may be identical or different, denote alkyl optionally substituted by dialkylamino in which the alkyls are optionally joined to form a 1-pyrrolidinyl, piperidino, morpholino or 1-piperazinyl ring substituted by alkyl, or alternatively R.sub.1 and R.sub.2 form a heterocyclic ring chosen from pyrrolidine, piperidine, morpholine and piperazine, substituted by alkyl, alkenyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C, or (B) R is phenyl optionally substituted with one or more halogens or hydroxy, alkyl, alkyloxy or alkylthio radicals and R.sub.1 and R.sub.2 together form a piperazine or homopiperazine ring substituted by hydroxyalkyl (2 to 4 C), alkenyl (2 to 4 C), alkynyl (2 to 4 C), benzyl or phenethyl optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CN, CF.sub.3, COOH, carboxyalkyl, alkyloxycarbonyl, alkyloxycarbonylalkyl, hydroxyalkyl, or alkylcarbonyloxyalkyl in which the alkylcarbonyl has 2 to 18 C, the said alkyls containing, except where otherwise stated, 1 to 4 C in a straight or branched chain, and the pharmaceutically acceptable salts thereof, are useful as antipsychotics.

    摘要翻译： 吡咯并[1,2-a]吖庚因酮衍生物，其中R 3为H或卤素，（A）R为苄基或苯硫基，其中苯基任选被一个或多个卤素或羟基取代 ，烷基，烷氧基或烷硫基，R 1和R 2可以相同或不同，表示任选被二烷基氨基取代的烷基，其中烷基任选地连接以形成被烷基取代的1-吡咯烷基，哌啶子基，吗啉代或1-哌嗪基环 或者R1和R2形成选自吡咯烷，哌啶，吗啉和哌嗪的杂环，被烷基，烯基（2至4 C），任选被卤素，烷基，烷氧基，烷硫基，CF 3，COOH取代的苄基或苯乙基取代， 羧基烷基，烷氧基羰基，烷氧基羰基烷基，羟基烷基或烷基羰氧基烷基，其中烷基羰基具有2至18个C，或（B）R是任选被一个或多个卤素或羟基，烷基，烷氧基或烷硫基取代的苯基， 和R2一起形成被羟烷基（2〜4 C），烯基（2〜4 C），炔基（2〜4 C），任选被卤素，烷基，烷氧基，烷硫基，CN取代的苄基或苯乙基取代的哌嗪或高哌嗪环 ，CF 3，COOH，羧基烷基，烷氧基羰基，烷氧基羰基烷基，羟基烷基或其中烷基羰基具有2〜18个碳原子的烷基羰氧基烷基，所述烷基除了另外说明的含有1〜4个C的直链或支链， 其盐可用作抗精神病药。

    Pyrrole derivatives, their preparation and pharmaceutical compositions which contain them
    8.
    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
    10.
    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。