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1. 发明授权

US4576954A Anti-rheumatic 5-(substituted amino)-1,2-dithiol-3-one compounds and their use 失效
标题翻译：抗风湿5-（取代氨基）-1,2-二硫酚-3-酮化合物及其用途
公开(公告)号：US4576954A
公开(公告)日：1986-03-18
申请号：US582043
申请日：1984-02-21
申请人： Jean-Dominique Bourzat , Claude Cotrel , Daniel Farge , Jean-Marc Paris , Gerard Taurand
发明人： Jean-Dominique Bourzat , Claude Cotrel , Daniel Farge , Jean-Marc Paris , Gerard Taurand
IPC分类号： C07D339/04 , C07D409/04 , C07D413/04 , A61K31/47 , C07D215/02 , C07D217/02
CPC分类号： C07D409/04 , C07D339/04
摘要： New derivatives of the general formula (I) in which:R=H or Cl and either R.sub.1 and R.sub.2 form a tetrahydroquinoxaline, tetrahydroquinoline, tetrahydroisoquinoline, dihydrobenzoxazine, tetrahydro-1H-benzazepine or isoindoline ring, it being possible for all these rings to be substituted by one or more halogen, carboxyl, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, trifluoromethyl, cyano, nitro, alkoxy, alkylthio or alkyl, substituted by carboxyl, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, hydroxyl, amino, alkylamino or dialkylamino, or R.sub.1 =alkyl and R.sub.2 =alkyl substituted by phenyl which is itself unsubstituted or substituted by one or more halogen, alkyl, alkoxy, alkylthio, hydroxy, amino, alkylamino, dialkylamino, carboxy, alkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, trifluoromethyl, cyano or nitro, all the alkyls having 1 to 4 C in a straight or branched chain.These new products are used as antirheumatics. ##STR1##
摘要翻译：通式（I）的新衍生物，其中：R = H或Cl，R 1和R 2形成四氢喹喔啉，四氢喹啉，四氢异喹啉，二氢苯并恶嗪，四氢-1H-苯并氮杂或异吲哚啉环，所有这些环都是可能的被一个或多个卤素，羧基，烷氧基羰基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，三氟甲基，氰基，硝基，烷氧基，烷硫基或被羧基，烷氧基羰基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，羟基，氨基，烷基氨基或二烷基氨基取代的烷基取代，烷基，烷氧基，烷硫基，羟基，氨基，烷基氨基，二烷基氨基，羧基，烷氧基羰基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，三氟甲基，氰基或硝基，所有烷基在直链或支链上具有1-4个碳原子。这些新产品被用作抗风湿剂。（一）

2. 发明授权

US4407797A 1,2-Dithiol-3-ylideneammonium derivatives, compositions and use 失效
标题翻译： 1,2-二硫醇-3-亚基铵衍生物，组合物和用途
公开(公告)号：US4407797A
公开(公告)日：1983-10-04
申请号：US406980
申请日：1982-08-10
申请人： Claude Cotrel , Daniel Farge , Gerard Taurand
发明人： Claude Cotrel , Daniel Farge , Gerard Taurand
IPC分类号： C07C233/07 , C07D295/185 , C07D339/04 , C07D409/12 , A61K31/535 , A61K31/385 , C07D413/04
CPC分类号： C07D295/185 , C07C233/07 , C07D339/04 , C07D409/12 , Y10S514/926 , Y10S514/927
摘要： New compounds of the formula: ##STR1## wherein X.sup..crclbar. is an anion, R is (C.sub.1-7) alkyl [unsubstituted or substituted by hydroxy, carboxy, alkoxycarbonyl, cyano, dialkylamino, alkylcarbonyl, or benzoyl which is unsubstituted or substituted by one or more halogen atoms or radicals selected from alkyl (optionally substituted by one or more halogens), alkoxy, hydroxy, amino, alkylamino, dialkylamino, cyano and nitro, or by a thenoyl radical (which is unsubstituted or substituted by one or more halogens or radicals selected from alkyl, cyano and nitro), or a pyridinecarbonyl, carbamoyl or dialkylcarbamoyl radical (the alkyl radicals of which can form a 5-membered or 6-membered heterocyclic ring) or a pyridyl radical], dialkylcarbamoyl (the alkyl radicals of which can form a 5-membered or 6-membered heterocyclic ring), (C.sub.2-4) alkenyl, (C.sub.2-4) alkynyl, alkoxycarbonyl or a 2-oxotetrahydrofuran-3-yl or 2-oxotetrahydropyran-3-yl ring, and either R.sub.1 and R.sub.2 are phenyl, cycloalkyl, alkyl or phenylalkyl or together form a 5-membered to 7-membered heterocyclic ring, or R.sub.1 is phenyl optionally substituted by one or more halogen atoms or radicals selected from alkyl optionally substituted by one or more halogens, alkoxy, hydroxy, amino, alkylamino, dialkylamino, cyano and nitro, or alternatively is cycloalkyl, alkyl or phenylalkyl, and R.sub.2 is a hydrogen atom, are useful as cytoprotective anti-ulcer agents.
摘要翻译：新的下式化合物：其中X（ - ）为阴离子，R为未被取代或被羟基，羧基，烷氧基羰基，氰基，二烷基氨基，烷基羰基或未取代或取代的苯甲酰基取代的（C 1-7）烷基烷氧基，羟基，氨基，烷基氨基，二烷基氨基，氰基和硝基，或由过氧酰基（未被取代或被一个或多个取代基取代）的一个或多个卤素原子或基团取代（任选被一个或多个卤素取代）卤素或选自烷基，氰基和硝基的基团）或吡啶羰基，氨基甲酰基或二烷基氨基甲酰基（其烷基可以形成5元或6元杂环）或吡啶基]，二烷基氨基甲酰基其中可以形成5元或6元杂环），（C 2-4）烯基，（C 2-4）炔基，烷氧基羰基或2-氧代四氢呋喃-3-基或2-氧代四氢吡喃-3-基环， R 1和R 2是苯基，环烷基，烷基或苯基烷基 R一起形成5元至7元杂环，或R 1为任选被一个或多个卤素原子取代的苯基或选自任选被一个或多个卤素，烷氧基，羟基，氨基，烷基氨基，二烷基氨基，氰基硝基，或者是环烷基，烷基或苯基烷基，R2是氢原子，可用作细胞保护性抗溃疡剂。

3. 发明授权

US4753941A Amides based on certain 1,8-naphtyridine-2-amines useful as anxiolytics 失效
标题翻译：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。

4. 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。

5. 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。

6. 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。

7. 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）

8. 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）

9. 发明授权

US4985419A 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：US4985419A
公开(公告)日：1991-01-15
申请号：US364465
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 , A61P23/00 , C07D279/28 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D279/28 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
摘要： Phenothiazine derivatives of formula: ##STR1## in which Y is hydrogen or halogen, R.sub.1 and R.sub.2, which may be identical or different, denote alkyl, cycloalkyl-alkyl, hydroxyalkyl or acetyloxyalkyl radicals or form, together with the nitrogen atom to which they are attached, an optionally substituted, saturated or partially unsaturated 4- to 7-membered heterocycle; and either X is oxygen, sulphur or: N-R.sub.4, R is cycloalkyl, phenyl or --CH.sub.2 R.sub.3, R.sub.3 is H, alkyl (1 to 5 C), alkenyl or alkynyl (2 to 4 C), cycloalkyl (3 to 6 C), phenyl, substituted phenyl or a heterocyclic radical, R.sub.4 is H or --CN, except that X is not oxygen if, simultaneously, R.sub.3 is H or alkyl, R.sub.1 and R.sub.2 are alkyl or NR.sub.1 R.sub.2 forms an unsubstituted heterocycle, and Y is H; or X is: N-R.sub.4 and R.sub.4 forms, with R and the neighbouring atoms, an optionally substituted imidazolyl or imidazolinyl radical or a hexahydrobenzimidazolyl radical, in their isomeric forms and mixtures thereof and their acid addition salts are useful as analgesics and diuretics.
摘要翻译：其中Y为氢或卤素的式（Ⅰa）所示的吩噻嗪衍生物，R 1和R 2可以相同或不同，表示烷基，环烷基 - 烷基，羟基烷基或乙酰氧基烷基，或与它们相同的氮原子一起形成任选取代的饱和或部分不饱和的4-至7-元杂环; 并且X是氧，硫或：N-R 4，R是环烷基，苯基或-CH 2 R 3，R 3是H，烷基（1至5 C），烯基或炔基（2至4 C），环烷基（3至6 C ），苯基，取代的苯基或杂环基，R4是H或-CN，除了X不是氧，如果同时R3是H或烷基，则R1和R2是烷基或NR1R2形成未取代的杂环，Y是H ; 或X为：与R和相邻原子形成的任选取代的咪唑基或咪唑啉基或六氢苯并咪唑基，其异构形式及其混合物及其酸加成盐可用作止痛剂和利尿剂。

10. 发明授权

US4912105A Derivatives of phenothiazine and the compositions which contain them 失效
标题翻译：吩噻嗪的衍生物和含有它们的组合物
公开(公告)号：US4912105A
公开(公告)日：1990-03-27
申请号：US364133
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 , A61P1/12 , C07D279/28 , C07D417/06
CPC分类号： C07D279/28
摘要： Phenothiazine derivatives of formula ##STR1## in which R represents --NR.sub.1 R.sub.2 in which R.sub.1 and R.sub.2, which may be identical or different, are alkyl, hydroxyalkyl or acetyloxyalkyl radicals, or form, together with the nitrogen atom to which they are attached, a heterocycle containing 4 to 7 members which may be substituted by 1 or 2 alkyl, hydroxyalkyl or acetyloxyalkyl radicals, or R represents --N.sup.+ R.sub.1 R.sub.2 R.sub.3 in which R.sub.1 and R.sub.2 are as defined above and R.sub.3 is alkyl or phenylalkyl, their isomeric forms and their mixtures, and their salts, are useful in the field of antidiarrhetics.
摘要翻译：式（I）的吩噻嗪衍生物其中R表示-NR1R2，其中R1和R2可以相同或不同，可以是烷基，羟基烷基或乙酰氧基烷基，或与它们所连接的氮原子一起形成可以被1或2个烷基，羟基烷基或乙酰氧基烷基取代的4〜7个成员的杂环，或者R表示-N + R1R2R3，其中R1和R2如上定义，R3是烷基或苯基烷基，它们的异构形式和它们的混合物及其盐可用于抗腹泻领域。

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