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    3-Ureidobenzodiazepinones useful as antagonists of CCK or of gastrin
    23.
    发明授权
    3-Ureidobenzodiazepinones useful as antagonists of CCK or of gastrin 失效
    可用作CCK或胃泌素的拮抗剂的3-尿嘧啶并二氮杂酮

    公开(公告)号：US5563136A

    公开(公告)日：1996-10-08

    申请号：US211323

    申请日：1994-04-06

    Applicant: Marc Capet ,  Claude Cotrel ,  Marie-Christine Dubroeuco ,  Claude Guyon ,  Jean-Paul Martin

    Inventor： Marc Capet ,  Claude Cotrel ,  Marie-Christine Dubroeuco ,  Claude Guyon ,  Jean-Paul Martin

    IPC: A61K31/55 ,  A61K31/551 ,  A61K31/675 ,  A61P25/00 ,  A61P25/04 ,  A61P25/20 ,  C07D243/24 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

    CPC classification number: C07D401/04 ,  C07D243/24 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

    Abstract: This invention relates to compounds having formula (I), ##STR1## wherein R.sub.1 is a hydrogen or halogen atom or an alkyl, alkoxy, alkylthio, nitro, hydroxy or cyano radical; R.sub.2 is an alkyl radical or a chain --CH(R.sub.5)--CO--R.sub.6 ; R.sub.3 is (a) a phenyl radical substituted by one or a plurality of substituents selected amongst the radicals -alk-SO.sub.3 H, -alk-PO.sub.3 H.sub.2, --CH.dbd.NOH, --CH--NO-alk-COOX, --S-alk-COOX, --SO-alk-COOX, --SO.sub.2 -alk-COOX, --CH.dbd.CH--COOX, -alk-CO--NHOH, --C(.dbd.NOH)--COOX, -alk-N(OH)--CO-alk,-alk-SO.sub.2 H, --CH.dbd.CH--SO.sub.3 H, --C(COOX).dbd.N--O-alk-COOX, tetrazolyalkyle or a group having a formula (I) or (b) a ring having the formula (A) ##STR2## wherein R.sub.9 is a radical .dbd.NOX, .dbd.NO-alk-COOX, .dbd.CH--COOX, -alk-COOX, -alk-SO.sub.2 H or -alk-S).sub.3 H, R.sub.10 is an oxygen or sulfur atom or a methylene or alkylimino radical and R.sub.11 is a methylene or ethylene radical, R.sub.4 is a pyridyle or phenyl radical optionally substituted by one or a plurality of substituents selected amongst halogen atoms or the alkyl, alkoxy, hydroxy, carboxy, nitro and --CO--NR.sub.6 radicals, alk is an alkyl or alkylene radical and X is a hydrogen atom or an alkyl radical. The invention also discloses the salts thereof, their preparation and medicaments containing them.

    Abstract translation: PCT No.PCT / FR92 / 00935 Sec。 371日期1994年4月6日 102（e）日期1994年4月6日PCT提交1992年10月8日PCT公布。 出版物WO93 / 07130 日本公开号为1993年4月15日本发明涉及具有式（I），其中R 1为氢或卤素原子或烷基，烷氧基，烷硫基，硝基，羟基或氰基的式（I） R2是烷基或链-CH（R5）-CO-R6; R3是（a）被一个或多个取代基取代的苯基，所述取代基选自基团-SO 3 H，-alk-PO 3 H 2，-CH = NOH，-CH-NO-烷基-COOX，-S-烷基-COOX ，-SO-烷基-COOX，-SO 2 - 烷基-COOX，-CH = CH-COOX，-alk-CO-NHOH，-C（= NOH）-COOX，-alk-N（OH） -alk-SO 2 H，-CH = CH-SO 3 H，-C（COOX）= NO-alk-COOX，四唑烷基或具有式（I）或（b）具有式（A）的环的基团 A）其中R9是基团= NOX，= NO-alk-COOX，= CH-COOX，-alk-COOX，-alk-SO2H或-alk-S）3H，R10是氧或硫原子或亚甲基或 烷基亚氨基，R 11是亚甲基或亚乙基，R 4是任选被一个或多个选自卤素原子或烷基，烷氧基，羟基，羧基，硝基和-CO-NR 6基团中的一个或多个取代基取代的吡啶基或苯基 是烷基或亚烷基，X是氢原子或烷基。 本发明还公开了其盐，它们的制备方法和含有它们的药物。

    Pyrrole derivatives, their preparation and pharmaceutical compositions which contain them
    25.
    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

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

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

    IPC: C07D471/04 ,  C07D519/00

    CPC classification number: C07D471/04

    Abstract: 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.

    Abstract translation: 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
    26.
    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

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

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

    IPC: 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 classification number: C07D401/04 ,  C07D471/04

    Abstract: 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.

    Abstract translation: 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。

    Arylvinylazacycloalkane Compounds and Methods of Preparation and Use Thereof
    28.
    发明申请
    Arylvinylazacycloalkane Compounds and Methods of Preparation and Use Thereof 有权
    芳基乙烯基氮杂环烷烃化合物及其制备和使用方法

    公开(公告)号：US20080293778A1

    公开(公告)日：2008-11-27

    申请号：US12187584

    申请日：2008-08-07

    Applicant: Jeffrey Daniel Schmitt ,  Gary Maurice Dull ,  Arielle Genevois-Borella ,  Marc Capet ,  Michel Cheve

    Inventor： Jeffrey Daniel Schmitt ,  Gary Maurice Dull ,  Arielle Genevois-Borella ,  Marc Capet ,  Michel Cheve

    IPC: A61K31/4439 ,  C07D401/14 ,  A61P25/00

    CPC classification number: A61K31/506 ,  C07D405/14

    Abstract: Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.

    Abstract translation: 公开了式（I）的新型乙烯基氮杂环烷化合物。 这些化合物是各种nAChR的配体。 化合物及其药学上可接受的盐可用于制备旨在预防或治疗与nAChR功能障碍相关的疾病，特别是在中枢神经系统或胃肠系统内的药物组合物和/或药物。 可以治疗的疾病类型的实例包括神经变性疾病，包括中枢神经系统疾病如阿尔茨海默病，认知障碍，运动障碍如帕金森病，药物成瘾，行为障碍和胃肠系统内的炎性疾病。 化合物也可用作治疗急性，慢性或复发性疼痛的镇痛药。

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