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11. 发明授权

US4642308A N-(1,8-naphthyridin-2-yl) amides and their pharmaceutical use 失效
标题翻译： 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。

12. 发明授权

US4753933A Anxiolytic amides derived from certain 1,8-naphthyridine-2-amines 失效
标题翻译：衍生自某些1,8-萘啶-2-胺的溶血性酰胺
公开(公告)号：US4753933A
公开(公告)日：1988-06-28
申请号：US2929
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 , A61P25/08 , A61P25/20 , C07D471/04
CPC分类号： C07D471/04
摘要： The invention provides new substituted amides of formula:R--CONH--Hetin which: either R is cycloalkyl (3 to 6 carbons), cyclohexadienyl, phenyl, substituted phenyl or a heterocyclic systems chosen from 3-pyridyl, alkyloxy-3-pyridyl, thienyl, alkylthienyl, furyl, tetrahydropyridyl, pyridazinyl, and alkylpyridazinyl, and Het is 1,8-naphthyridin-2-yl substituted at the 7-position by alkyloxy, alkylthio or alkylsulphinyl, themselves substituted with alkylamino or dialkylamino (in which the alkyl portions can form, with the nitrogen atom, a 5- or 6-membered heterocyclic system optionally containing another hetero atom chosen from O, S or N, and optionally substituted by alkyl) or by dialkylcarbamoyl or N-alkyl-N-(alkyloxycarbonyl)amino, or substituted at the 7-position by dialkylaminovinyl; or R is 4-(alkylamino)phenyl or 4-(alkyloxycarbonylamino)phenyl and Het is 1,8-naphthyridin-2-yl substituted at the 7-position by alkyloxy or alkylthio, the said alkyl radicals and alkyl portions containing 1 to 4 carbons, their salts, their preparations and pharmaceutical compositions which contain them.These new substituted amides are especially active as anxiolytics, hypnotics, anticonvulsants, antiepileptics 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是环烷基（3-6个碳），环己二烯基，苯基，取代的苯基或选自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，Het是在7位被烷氧基，烷硫基或烷基亚磺酰基取代的1,8-萘啶-2-基，其本身被烷基氨基或二烷基氨基取代（其中烷基部分可以与氮原子一起形成任选地含有另一个选自O，S或N的杂原子，并任选被烷基取代的5-或6-元杂环体系）或二烷基氨基甲酰基或N-烷基-N-（烷氧基羰基）氨基，或在二甲基氨基乙烯基在7-位取代; 或R是4-（烷基氨基）苯基或4-（烷氧基羰基氨基）苯基，Het是在7-位被烷氧基或烷硫基取代的1,8-萘啶-2-基，所述烷基和烷基部分含有1至4个碳，它们的盐，它们的制剂和含有它们的药物组合物。这些新的取代的酰胺作为抗焦虑剂，催眠药，抗惊厥药，抗癫痫剂和肌肉松弛剂是特别活跃的。

13. 发明授权

US4720500A N-1,8-naphthyridin-2-yl amides useful as immunostimulants 失效
标题翻译：可用作免疫刺激剂的N-1,8-萘啶-2-基酰胺
公开(公告)号：US4720500A
公开(公告)日：1988-01-19
申请号：US884212
申请日：1986-07-10
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： C07D471/04 , A61K31/44
CPC分类号： C07D471/04
摘要： Amides of formula ##STR1## in which either R is 2-quinolyl, substituted phenyl (substituted by Br, 3-Cl, CF.sub.3, alkyloxycarbonyl, 4-dialkylamino), dichlorophenyl, trialkyloxyphenyl, benzyl, styryl, benzoyl or anilino and R' is halogen, phenyl or anilino or R' is phenoxy or 4-chlorophenoxy when R is 2-quinolyl, substituted phenyl, trialkyloxyphenyl, benzyl or styryl or R' is 4-fluoro(or alkyloxy)phenyl when R is 4-trifluoromethyl (or dialkylamino)phenyl, or R' is 3-bromophenyl when R is anilino, or R is phenyl or alkyloxyphenyl and R' is phenyl, 4-chlorophenoxy, anilino or 1-pyrrolidinyl or R' is 2-(or 4-)chlorophenyl, 3-(or 4-)bromophenyl, 4-alkyloxyphenyl or 3,4-dichloro(or dibromo)phenyl when R is phenyl or R is 3-halophenyl and R' is 3-(or 4-)fluorophenyl, 3-(or 4-)bromophenyl, 4-chlorophenyl, 2-(or 3-)-alkyloxyphenyl, 3-alkylphenyl or 3,4-difluoro(dichloro or dibromo)phenyl, the straight-chain or branched alkyl radical containing 1 to 4 carbon atoms each, are useful as immunostimulant agents. The invention also provides processes for their preparation and pharmaceutical compositions containing them.
摘要翻译：式（I）的酰胺，其中R是2-喹啉基，取代的苯基（被Br，3-Cl，CF 3，烷氧基羰基，4-二烷基氨基取代），二氯苯基，三烷氧基苯基，苄基，苯乙烯基，苯甲酰基或苯胺基，当R是4-三氟甲基时，当R是2-喹啉基，取代的苯基，三烷氧基苯基，苄基或苯乙烯基或R'是4-氟（或烷氧基）苯基时，R'是卤素，苯基或苯胺基或R'是苯氧基或4-氯苯氧基（或二烷基氨基）苯基，或当R为苯胺基时R'为3-溴苯基，或R为苯基或烷氧基苯基，R'为苯基，4-氯苯氧基，苯胺基或1-吡咯烷基或R'为2-（或4-）当R是苯基或R是3-卤代苯基且R'是3-（或4-）氟苯基，3-（或4-氟苯基），3-（或4-）溴苯基，4-烷氧基苯基或3,4-二氯（或二溴）（或4-）溴苯基，4-氯苯基，2-（或3-） - 烷氧基苯基，3-烷基苯基或3,4-二氟（二氯或二溴）苯基，含有1至4个碳原子的直链或支链烷基各自的原子可用作免疫抑制剂 ant剂。本发明还提供其制备方法和含有它们的药物组合物。

14. 发明授权

US6150387A Heterocyclic carboxamide compounds effective in the treatment of drug abuse 失效
标题翻译：有效治疗药物滥用的杂环羧酰胺化合物
公开(公告)号：US6150387A
公开(公告)日：2000-11-21
申请号：US117931
申请日：1998-08-07
申请人： Andrees Bohme , Marie-Christine Dubroeucq , Walter Fratta , Claude Guyon , Assunta Imperato , Franco Manfre
发明人： Andrees Bohme , Marie-Christine Dubroeucq , Walter Fratta , Claude Guyon , Assunta Imperato , Franco Manfre
IPC分类号： A61K31/40 , A61K31/401 , A61K31/426 , A61K31/425 , A61K31/44 , A61K31/47
CPC分类号： A61K31/426 , A61K31/40 , A61K31/401
摘要： This invention relates to the use of heterocyclic carboxamide compounds for preventing or reducing self-administration, by a human or animal patient, of a drug or a substance capable of giving rise to pharmacomania or to overuse. The preferred types of drugs or substances are nicotine, caffeine, benzodiazepines, narcotics, and hallucinogens.
摘要翻译： PCT No.PCT / FR97 / 00209 Sec。 371日期：1998年8月7日 102（e）1998年8月7日PCT PCT 1997年2月3日PCT公布。公开号WO97 / 28798 日期：1997年8月14日本发明涉及杂环羧酰胺化合物用于预防或减少人或动物患者自身给药药物或能产生药物动力或过度使用的物质的用途。药物或物质的优选类型是尼古丁，咖啡因，苯并二氮杂，麻醉剂和致幻剂。

15. 发明授权

US5321026A Phenothiazine derivatives, their preparation and pharmaceutical compositions containing them 失效
标题翻译：吩噻嗪衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5321026A
公开(公告)日：1994-06-14
申请号：US825753
申请日：1992-01-27
申请人： Claude Garret , Claude Guyon , Bernard Plau , Gerard Taurand
发明人： Claude Garret , Claude Guyon , Bernard Plau , Gerard Taurand
IPC分类号： A61K31/00 , A61K31/54 , A61P25/04 , A61P25/20 , C07D279/28 , C07D417/06
CPC分类号： C07D279/28
摘要： New phenothiazine derivatives of general formula (I) in whichR represents 4- to 6-membered cycloalkyl, or represents --CH.sub.2 R" in which R" is hydrogen, alkyl containing 1 to 5 carbon atoms, alkenyl or alkynyl containing 2 to 4 carbon atoms, cycloalkyl (3- to 6-membered), phenyl, optionally substituted (with 1 or 2 halogen atoms or with a hydroxyl, alkyl, alkyloxy, trifluoromethyl or nitro radical) or heterocyclic selected from furyl, thienyl or pyridyl, andR' either represents a radical of general formula (IIa) in which R.sub.1 and R.sub.2, which may be identical or different, are alkyl, cycloalkylalkyl, hydroxyalkyl or acetyloxyalkyl or, together with the nitrogen atom to which they are attached, form a saturated or partially unsaturated 4- to 7-membered heterocycle optionally substituted with 1 or 2 alkyl, hydroxyalkyl or acetyloxyalkyl radicals, andR.sub.3 is phenethyl or alkyl optionally substituted with cycloalkyl (3 to 6 carbons) or benzoyl, or represents a radical of general formula (IIb) in which R.sub.1 and R.sub.2 are defined as above.The new products are useful as antispasmodics. ##STR1##
摘要翻译：通式（I）的新吩噻嗪衍生物，其中R表示4-至6-元环烷基，或表示其中R“为氢的-CH 2 R”，含有1至5个碳原子的烷基，含有2至4个碳原子的烯基或炔基碳原子，环烷基（3-至6-元），苯基，任选取代的（具有1或2个卤素原子或与羟基，烷基，烷氧基，三氟甲基或硝基）或选自呋喃基，噻吩基或吡啶基的杂环，R “表示通式（IIa）的基团，其中可以相同或不同的R 1和R 2是烷基，环烷基烷基，羟基烷基或乙酰氧基烷基，或者与它们连接的氮原子一起形成饱和或部分任选被1或2个烷基，羟基烷基或乙酰氧基烷基取代的不饱和4-至7-元杂环，R 3为任选被环烷基（3-6个碳）或苯甲酰基取代的苯乙基或烷基，或表示通式（IIb）的基团，在其中R1和R2如上定义。新产品可用作解痉药。（I）（IIa）（IIb）

16. 发明授权

US06699895B2 2-aminothiazoline derivatives and process for preparing the same 失效
标题翻译： 2-氨基噻唑啉衍生物及其制备方法
公开(公告)号：US06699895B2
公开(公告)日：2004-03-02
申请号：US10159498
申请日：2002-05-31
申请人： Jean-Christophe Carry , Dominique Damour , Claude Guyon , Serge Mignani , Antony Bigot , Eric Bacque , Michel Tabart
发明人： Jean-Christophe Carry , Dominique Damour , Claude Guyon , Serge Mignani , Antony Bigot , Eric Bacque , Michel Tabart
IPC分类号： C07D41706
CPC分类号： C07D417/06 , A61K31/426 , A61K31/4439 , C07D277/18
摘要： The present invention relates to a class of 2-aminothiazoline derivatives of formula I: in which either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk-NH2, —CH2—R3, —CH2—S—R4 or phenyl radical substituted with a nitro or —NH—C(═NH)CH3 radical, or R1 is an alkyl radical and R2 is a hydrogen atom, R3 is a (3-6C) cycloalkyl, pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl or phenyl radical or a phenyl radical substituted with a nitro, hydroxy or carboxyl radical, R4 represents a pyridyl or pyridyl N-oxide radical, alk represents an alkylene radical, or pharmaceutically acceptable salts thereof, which are useful as inhibitors of inducible NO-synthase.
摘要翻译：本发明涉及一类式I的2-氨基噻唑啉衍生物：其中R1是氢原子或烷基，R2是烷基，-alk-NH2，-CH2-R3，-CH2-S-R4 或被硝基或-NH-C（= NH）CH 3基团取代的苯基，或R 1是烷基，R 2是氢原子，R 3是（3-6C）环烷基，吡啶基，吡啶基N-氧化物，噻吩基，噻唑基，咪唑基，吡嗪基，三唑基或苯基或被硝基，羟基或羧基取代的苯基，R4表示吡啶基或吡啶基N-氧化物基，alk表示亚烷基或其药学上可接受的盐，它们是可用作诱导型NO合成酶的抑制剂。

17. 发明授权

US5663204A Ureidoacetamide derivatives, their preparation and the medicaments containing them 失效
标题翻译：脲基乙酰胺衍生物，其制备方法和含有它们的药物
公开(公告)号：US5663204A
公开(公告)日：1997-09-02
申请号：US397044
申请日：1995-03-10
申请人： Marie-Christine Dubroeucq , Claude Guyon
发明人： Marie-Christine Dubroeucq , Claude Guyon
IPC分类号： A61K38/00 , A61P21/00 , A61P25/00 , A61P25/20 , A61P25/28 , C07K1/02 , C07K5/06 , C07K5/062 , A61K31/17 , C07C309/02
CPC分类号： C07K5/06026 , A61K38/00
摘要： This invention relates to compounds of formula (I), in which R denotes a hydrogen atom or a methoxy radical. The invention also concerns the salts of said compounds, their racemic forms, their enantiomers, the preparation of said derivatives and drugs containing same.
摘要翻译： PCT No.PCT / FR93 / 00847 Sec。 371 1995年3月10日 102（e）1995年3月10日PCT PCT 1993年9月6日PCT公布。公开号WO94 / 06825 日期：1994年3月31日本发明涉及式（I）化合物，其中R表示氢原子或甲氧基。本发明还涉及所述化合物的盐，其外消旋形式，其对映异构体，所述衍生物的制备和含有它们的药物。

18. 发明授权

US5049669A Analgesic phenothiazine derivatives 失效
标题翻译：镇痛吩噻嗪衍生物
公开(公告)号：US5049669A
公开(公告)日：1991-09-17
申请号：US364155
申请日：1989-06-12
申请人： Claude Garret , Claude Guyon , Bernard Plau , Gerard Taurand
发明人： Claude Garret , Claude Guyon , Bernard Plau , Gerard Taurand
IPC分类号： A61K31/00 , A61K31/54 , A61K31/5415 , A61P7/10 , A61P25/04 , C07D279/28
CPC分类号： C07D279/28
摘要： Phenothiazine derivatives of general formula (I), in which R is a linear or branched (1 to 6 C) alkyl radical and R.sub.1 and R.sub.2, which may be identical or different, are linear or branched (1 to 4 C) alkyl radicals or form, with the nitrogen atom to which they are attached, a 4- to 7-membered heterocycle, their isomeric forms and mixtures thereof as well as their addition salts with acids, possess analgesic and diuretic activity. ##STR1##
摘要翻译：其中R为直链或支链（1至6个C）烷基的通式（I）的吩噻嗪衍生物，R 1和R 2可以相同或不同，为直链或支链（1-4个碳）烷基或与它们所连接的氮原子一起形成4-至7-元杂环，其异构形式及其混合物以及它们与酸的加成盐，具有止痛和利尿活性。（一）

19. 发明授权

US5625066A Optically active hydroquinine (amino-3 phenyl)-1 ethanesulfonate, preparation and use thereof 失效
标题翻译：光学活性氢醌（氨基-3苯基）-1乙磺酸盐，的制备和应用
公开(公告)号：US5625066A
公开(公告)日：1997-04-29
申请号：US397046
申请日：1995-03-10
申请人： Claude Guyon
发明人： Claude Guyon
IPC分类号： A61K38/00 , C07B53/00 , C07C309/24 , C07D20060101 , C07D453/04 , C07K5/078 , C07D403/06
CPC分类号： C07K5/06139 , C07C309/24 , C07D453/04 , A61K38/00
摘要： This invention relates to an optically active hydroquinine (amino-3 phenyl)-1 ethanesulfonate (form A), preparation thereof and its use as an intermediate in the preparation of cholecystokinine and gastrin antagonists.
摘要翻译： PCT No.PCT / FR93 / 00848 Sec。 371 1995年3月10日 102（e）1995年3月10日PCT PCT 1993年9月6日PCT公布。公开号WO94 / 06792 日期：1994年3月31日本发明涉及光学活性氢醌（氨基-3苯基）-1乙烷磺酸盐（A型）及其制备方法及其在制备胆囊收缩素和胃泌素拮抗剂中的应用。

20. 发明授权

US5523469A Optically active alkylammonium 1-(3-aminophenyl)-ethanesulphonate derivatives, their preparation and their use 失效
标题翻译：光学活性的1-（3-氨基苯基） - 乙磺酸铵衍生物，其制备及其应用
公开(公告)号：US5523469A
公开(公告)日：1996-06-04
申请号：US397045
申请日：1995-03-10
申请人： Claude Guyon
发明人： Claude Guyon
IPC分类号： C07D233/60 , A61K38/00 , C07C303/32 , C07C303/44 , C07C309/24 , C07K5/06 , C07C309/29
CPC分类号： C07K5/06026 , C07C309/24 , A61K38/00
摘要： This invention relates to levogyral isomers of alkylammonium (amino-3 phenyl)-1 ethanesulphonate derivatives of formula (I) in which R+ denotes a tetraalkylammonium or trialkylphenylalkylammonium residue. The invention also concerns the preparation and use of said derivatives.
摘要翻译： PCT No.PCT / FR93 / 00849 Sec。 371 1995年3月10日 102（e）1995年3月10日PCT PCT 1993年9月6日PCT公布。出版物WO94 / 06760 本发明涉及式（I）的烷基铵（氨基-3苯基）-1乙磺酸盐衍生物的左旋炔异构体，其中R +表示四烷基铵或三烷基苯基烷基铵残基。本发明还涉及所述衍生物的制备和用途。

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