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1. 发明授权

US4980356A 2-imino-6-polyfluoroalkoxybenzothiazole derivatives, and pharamaceutical compositions containing them and their treatment of medical conditions associated with the effects of glutamate 失效
标题翻译： 2-亚氨基-6-多氟烷氧基苯并噻唑衍生物和含有它们的药物组合物及其与谷氨酸的作用相关的医学病症的治疗
公开(公告)号：US4980356A
公开(公告)日：1990-12-25
申请号：US449810
申请日：1989-12-13
申请人： Francois Audiau , Claude Gueremy , Patrick Jimonet , Serge Mignani
发明人： Francois Audiau , Claude Gueremy , Patrick Jimonet , Serge Mignani
IPC分类号： A61K31/425 , A61K31/428 , A61K31/44 , A61K31/505 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/28 , C07D277/82 , C07D417/12
CPC分类号： C07D417/12 , C07D277/82
摘要： Compounds of formula: ##STR1## and their salts, in which R.sub.1 represents polyfluoroalkoxy, and R.sub.2 represents alkyl, alkenyl (3-6 C), [cycloalkyl (3-6 C)]-alkyl, carbamoylalkyl, dialkylcarbamoylalkyl, acylaminoalkyl, phenylthioalkyl, hydroxyalkyl, cyanoalkyl, sulphamoylethyl, N-alkylsulphamoylethyl, pyridylthioalkyl, pyridiylalkylthioalkyl, pyridylsulphinylalkyl, alkynyl (3-6 C), phenylsulphinylalkyl, halophenylthioalkyl, (2,2,2-trifluoroethylthio)alkyl, 2-dialkylaminopropyl, pyrimidinylsulphinylalkyl, pyridylalkylsulphinylalkyl, halophenylsulphinylalkyl or (2,2,2-trifluoroethylsulphinyl)alkyl are useful in the treatment of medical conditions associated with the effects of glutamate.
摘要翻译：式（Ⅰ）化合物及其盐，其中R1代表多氟烷氧基，R2代表烷基，烯基（3-6C），[环烷基（3-6C）] - 烷基，氨基甲酰基烷基，二烷基氨基甲酰基烷基，酰基氨基烷基苯基亚磺酰基烷基，卤代苯硫基烷基，（2,2,2-三氟乙硫基）烷基，2-二烷基氨基丙基，嘧啶基亚磺酰基烷基，吡啶基烷基亚磺酰基烷基，吡啶基亚磺酰基烷基，卤代苯基亚磺酰基烷基或（2,2,2-三氟乙基亚磺酰基）烷基可用于治疗与谷氨酸的作用相关的医学病症。

2. 发明授权

US5026717A 2-imino-6-polyfluoroalkoxybenzothiazole derivatives, and pharmaceutical compositions containing them 失效
标题翻译： 2-亚氨基-6-多氟烷氧基苯并噻唑衍生物和含有它们的药物组合物
公开(公告)号：US5026717A
公开(公告)日：1991-06-25
申请号：US543418
申请日：1990-06-26
申请人： Francois Audiau , Claude Gueremy , Patrick Jimonet , Serge Mignani
发明人： Francois Audiau , Claude Gueremy , Patrick Jimonet , Serge Mignani
IPC分类号： A61K31/425 , A61K31/428 , A61K31/44 , A61K31/505 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/28 , C07D277/82 , C07D417/12
CPC分类号： C07D417/12 , C07D277/82
摘要： Compounds of formula: ##STR1## and their salts, in which R.sub.1 represents polyfluoroalkoxy, and R.sub.2 represents alkyl, alkenyl (3-6 C), [cycloalkyl (3-6 C)]-alkyl, carbamoylalkyl, dialkylcarbamoylalkyl, acylaminoalkyl, phenylthioalkyl, hydroxyalkyl, cyanoalkyl, sulphamoylethyl, N-alkylsulphamoylethyl, pyridylthioalkyl, pyridiylalkylthioalkyl, pyridylsulphinylalkyl, alkynyl (3-6 C), phenylsulphinylalkyl, halophenylthioalkyl, (2,2,2-trifluoroethylthio)alkyl, 2-dialkylaminopropyl, pyrimidinylsulphinylalkyl, pyridylalkylsulphinylalkyl, halophenylsulphinylalkyl or (2,2,2-trifluoroethylsulphinyl)alkyl are useful in the treatment of medical conditions associated with the effects of glutamate.

3. 发明授权

US5008280A 2-iminobenzothiazoline derivatives, their preparation and pharmaceutical compositions containing them 失效
标题翻译： 2-亚氨基苯并噻唑啉衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5008280A
公开(公告)日：1991-04-16
申请号：US450231
申请日：1989-12-13
申请人： Claude Gueremy , Patrick Jimonet , Serge Mignani
发明人： Claude Gueremy , Patrick Jimonet , Serge Mignani
IPC分类号： A61K31/425 , A61K31/428 , A61K31/445 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/28 , C07D277/68 , C07D277/82 , C07D417/06
CPC分类号： C07D277/82
摘要： Compounds of the formula: ##STR1## in which - R.sub.1 denotes a polyfluoroalkoxy or polyfluoroalkyl radical, and - R.sub.2 denoteseither a chain --CH.sub.2 --(CH(R.sub.4)).sub.n --R.sub.3, in which R.sub.3 denotes a dialkylamino, piperidino, 1-pyrrolidinyl, mercapto, acylthio, alkylthio, alkylsulphinyl or alkylsulphonyl radical, R.sub.4 denotes a hydrogen atom or an alkyl radical and n is equal to 0 or 1,or a residue of formula: ##STR2## the said alkyl and alkoxy radicals and portions containing 1 to 4 carbon atoms each in a straight or branched chain and said the acyl portions containing 2 to 4 carbon atoms each, and the salts of these compounds, are useful in the treatment of diseases in which glutamate is implicated.
摘要翻译：下式的化合物：其中-R 1表示多氟烷氧基或多氟烷基，-R 2表示链-CH 2 - （CH（R 4））n -R 3，其中R 3表示二烷基氨基，哌啶子基，1-吡咯烷基，巯基，酰硫基，烷硫基，烷基亚磺酰基或烷基磺酰基，R4表示氢原子或烷基，n等于0或1，或下式的残基：所述烷基和烷氧基，各直链或支链含有1至4个碳原子的部分和所述酰基部分各自含有2至4个碳原子，并且这些化合物的盐可用于治疗涉及谷氨酸的疾病。

4. 发明授权

US5340824A Benzothiazole derivatives and medicinal products containing them 失效
标题翻译：苯并噻唑衍生物和含有它们的药用产品
公开(公告)号：US5340824A
公开(公告)日：1994-08-23
申请号：US938153
申请日：1992-12-02
申请人： Claude Gueremy , Patrick Jimonet , Serge Mignani
发明人： Claude Gueremy , Patrick Jimonet , Serge Mignani
IPC分类号： A61K31/445 , A61P25/28 , C07D277/82 , C07D417/12 , A61K31/44
CPC分类号： C07D277/82
摘要： ##STR1## Compounds of formula (I), in which R
1 is a polyfluoralkoxy, R
2 is a sulphur or nitrogen atom substituted by an alkyl radical or a sulfonyl or sulfinyl radical, R
3 is a phenyl, benzoyl, --NR
4 R
5 or piperidinyl-4radical substituted in position 1 by a phenylalkyl radical, R
4 is an alkyl radical, R
5 is a phenylalkyl radical, n is equal to 1, 2 or 3, m is equal to 0, 1, 2 or 3. The present invention also relates to the salts of said compounds, processes for the preparation of the latter and drugs containing them.
摘要翻译： PCT No.PCT / FR91 / 00437 Sec。 371日期1992年12月2日 102（e）日期1992年12月2日PCT提交1991年5月31日PCT公布。 WO91 / 18892 PCT出版物（I）式（I）化合物，其中R 1是多氟烷氧基，R 2是被烷基或磺酰基或亚磺酰基取代的硫或氮原子，R 3是苯基，苯甲酰基，-NR4R5或哌啶基-4-取代的苯基烷基，R4为烷基，R5为苯基烷基，n等于1,2或3，m等于0,1,2或本发明还涉及所述化合物的盐，其制备方法和含有它们的药物。

5. 发明授权

US5114949A Heterocyclic derivatives, their preparation and medicinal products containing them 失效
标题翻译：杂环衍生物，其制备和含有它们的药物
公开(公告)号：US5114949A
公开(公告)日：1992-05-19
申请号：US615670
申请日：1990-11-19
申请人： Claude Gueremy , Jean-Luc Malleron , Serge Mignani
发明人： Claude Gueremy , Jean-Luc Malleron , Serge Mignani
IPC分类号： C07D209/46 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/415 , A61K31/4184 , A61K31/425 , A61K31/428 , A61K31/47 , A61K31/495 , A61K31/496 , A61P3/04 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D209/92 , C07D235/26 , C07D275/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D513/04 , C07D513/06
CPC分类号： C07D403/06 , C07D403/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/06 , C07D513/04
摘要： Compounds are disclosed of formula:R.sub.1 --(CH.sub.2).sub.n --Hetin which R.sub.1 represents a residue of formula ##STR1## X represents a hydrogen atom or an alkyl radical, Y represents a hydrogen atom or an alkyl or alkoxy radical,Z represents an alkyl radical,n is equal to 2 or 3,Het represents a substituted piperidino (substituted at the 4-position with a 1-indenylidene, 1-indenyl or 1-indanyl radical or with a chain --(CH.sub.2).sub.m --R.sub.2 or .dbd.CH--R.sub.2), substituted 1,2,3,6-tetrahydro-1-pyridyl (substituted at the 4-position with a chain --(CH.sub.2).sub.m --R.sub.2),m is equal to 1 or 2, andR.sub.2 represents an optionally substituted 2- or 3-indolyl radical, a 1- or 2-indanyl, 1- or 2-indenyl, an optionally substituted 1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-2-yl radical, a 1,2,3,4-tetrahydro-3-quinolyl radical, an optionally substituted 1,2,3,4-tetrahydro-2-naphthyl radical or a 1-indolyl radical, their preparation and medicinal products containing them.
摘要翻译：（C）＆gt;（C）＆lt; IMAGE＆gt;（D）＆lt; IMAGE＆gt;（D）＆lt; IMAGE＆gt; J）X表示氢原子或烷基，Y表示氢原子或烷基或烷氧基，Z表示烷基，n表示2或3，Het表示取代的哌啶子基（在4-位取代具有1-茚基，1-茚基或1-茚满基或与链 - （CH 2）m -R 2或= CH-R 2）取代的1,2,3,6-四氢-1-吡啶基（在具有链 - （CH 2）m -R 2）的4-位，m等于1或2，并且R 2表示任选取代的2-或3-吲哚基，1-或2-二氢茚基，1-或2- 茚基，任选取代的1,2,3,4-四氢-5H-吡啶并[4,3-b]吲哚-2-基，1,2,3,4-四氢-3-喹啉基，任选地取代的1,2,3,4-四氢-2-萘基或1-吲哚基，它们的制备方法和含有它们的药用产品。

6. 发明授权

US5036075A Derivatives of (AZA) naphthalensultam, their preparation and compositions containing them 失效
标题翻译：（AZA）萘磺酸的衍生物，它们的制备和含有它们的组合物
公开(公告)号：US5036075A
公开(公告)日：1991-07-30
申请号：US609506
申请日：1990-11-06
申请人： Marie-Therese Comte , Claude Gueremy , Jean-Luc Malleron , Serge Mignani , Jean-Francois Peyronel , Alain Truchon
发明人： Marie-Therese Comte , Claude Gueremy , Jean-Luc Malleron , Serge Mignani , Jean-Francois Peyronel , Alain Truchon
IPC分类号： A61K31/425 , A61K31/428 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/54 , A61P9/00 , A61P11/00 , A61P25/00 , A61P43/00 , C07D275/06 , C07D417/00 , C07D417/06 , C07D417/14 , C07D513/06
CPC分类号： C07D275/06 , C07D417/06 , C07D417/14 , C07D513/06
摘要： This invention relates to a compound of the formula: ##STR1## in which R.sub.1 representsa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position.a 1-piperazinyl radical substituted in the 4-position.a piperidino radical substituted in the 4-positioneither:R.sub.2 and R.sub.3, which are identical, represent a hydrogen or halogen atom and R.sub.4 represents a hydrogen atom orR.sub.2 and R.sub.4 represent a hydrogen atom and R.sub.3 represents a halogen atom or an acetylamino radical orR.sub.2 and R.sub.3 represent a hydrogen atom and R.sub.4 represents a halogen atom and R.sub.5 represents a --CH.dbd. group.or R.sub.2, R.sub.3 and R.sub.4 represent a hydrogen atom and R.sub.5 represents a nitrogen atom.R.sub.6 represents an alkylene chain containing 2 to 4 carbon atoms or a propylene chain substituted in the 1- or 3-position by an alkyl radical or in the 2-position by an alkyl, alkoxy, hydroxy, dialkylamino, piperidino, morpholino or thiomorpholino radical, and their salts, are useful in therapy for their ability to block serotonin receptors.

7. 发明授权

US5260297A 2-imino-3-alkylbenzothiazoline derivatives bearing a heterocyclic substituent on the alkyl group, their preparation and medicinal products containing them. 失效
标题翻译：在烷基上带有杂环取代基的2-亚氨基-3-烷基苯并噻唑啉衍生物及其制备物和含有它们的药用产品。
公开(公告)号：US5260297A
公开(公告)日：1993-11-09
申请号：US815220
申请日：1991-12-31
申请人： Patrick Jimonet , Claude Gueremy , Joseph Le Blevec , Conception Nemecek
发明人： Patrick Jimonet , Claude Gueremy , Joseph Le Blevec , Conception Nemecek
IPC分类号： C07D277/82 , C07D417/06 , C07D417/12 , A61K31/44 , A61K31/445 , A61K31/495
CPC分类号： C07D417/06 , C07D277/82 , C07D417/12
摘要： Compounds of formula: ##STR1## in which R.sub.1 represents a substituted 1-piperazinyl, substituted 1,2,3,6-tetrahydro-1-pyridyl or substituted piperidino radical, R.sub.2 represents a polyfluoroalkoxy or a polyfluoroalkyl radical and n is equal to 2 or 3, the salts of these compounds with an acid, processes for preparing them and medicinal products containing them.
摘要翻译：其中R1表示取代的1-哌嗪基，取代的1,2,3,6-四氢-1-吡啶基或取代的哌啶子基的式：其中R 2表示多氟烷氧基或多氟烷基，n等于2 或3，这些化合物与酸的盐，其制备方法和含有它们的药用产品。

8. 发明授权

US5021420A Derivatives of (AZA)naphthalenesultam, their preparation and compositions containing them 失效
公开(公告)号：US5021420A
公开(公告)日：1991-06-04
申请号：US375934
申请日：1989-07-06
申请人： Marie-Iherese Comte , Claude Gueremy , Jean-Luc Malleron , Serge Mignani , Jean-Francois Peyronel , Alain Truchon
发明人： Marie-Iherese Comte , Claude Gueremy , Jean-Luc Malleron , Serge Mignani , Jean-Francois Peyronel , Alain Truchon
IPC分类号： A61K31/425 , A61K31/428 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/54 , A61P9/00 , A61P11/00 , A61P25/00 , A61P43/00 , C07D275/06 , C07D417/00 , C07D417/06 , C07D417/14 , C07D513/06
CPC分类号： C07D275/06 , C07D417/06 , C07D417/14 , C07D513/06
摘要： This invention relates to a compound ##STR1## in which R.sub.1 representsa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or an alkyl, hydroxy or alkoxy radical, (c) a 3-indolyl radical, (d) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (e) a 3-(5-hydroxyindolyl) radical.a 1-piperazinyl radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by an alkoxy, alkyl, hydroxy, nitro or amino radical or a halogen atom, (c) a 1,2-benzisothiazol-3-yl radical, (d) a 1,2-benzisoxazol-3-yl radical or (e) a 2-pyridyl radical.a piperidino radical substituted in the 4-position by (a) a phenyl radical, (b) a phenyl radical substituted by a halogen atom or a hydroxy, alkyl or alkoxy radical, (c) two phenyl radicals, (d) a bis(4-fluorophenyl)methylene radical, (e) a 4-fluorobenzoyl radical, (f) a 2-oxo-1-benzimidazolinyl radical, (g) a 2-oxo-1-benzimidazolinyl radical substituted in the 3-position by an alkylcarbonyl or benzoyl radical, (b) a hydroxy radical and a phenyl radical optionally substituted with an alkyl, alkoxy or hydroxy radical or a halogen atom, (i) a 3-indolyl radical, (j) a 3-indolyl radical substituted on the nitrogen atom by an alkyl or alkylcarbonyl radical and/or in the 5-position by a halogen atom or (k) a 3-(5-hydroxyindolyl) radical.either:R.sub.2 and R.sub.3, which are identical, represent a hydrogen or halogen atom and R.sub.4 represents a hydrogen atom orR.sub.2 and R.sub.4 represent a hydrogen atom and R.sub.3 represents a halogen atom or an acetylamino radical orR.sub.2 and R.sub.3 represent a hydrogen atom and R.sub.4 represents a halogen atom and R.sub.5 represents a --CH.dbd. group.or R.sub.2, R.sub.3 and R.sub.4 represent a hydrogen atom and R.sub.5 represents a nitrogen atom.R.sub.6 represents an alkylene chain containing 2 to 4 carbon atoms or a propylene chain substituted in the 1- or 3-position by an alkyl radical or in the 2-position by an alkyl, alkoxy, hydroxy, dialkylamino, piperidino, morpholino or thiomorpholino radical,with the reservation that when R.sub.6 represents a propylene radical substituted in the 2-position by a dialkylamino, piperidino, morpholino or thiomorpholino radical, R.sub.1 cannot be a radical containing a hydroxy radical, and their salts, are useful in therapy for their ability to block serotonin receptors.

9. 发明授权

US5240948A 3-(3-alkylthiopropyl)benzothiazoline derivatives, their preparation and the medicament containing them 失效
标题翻译： 3-（3-烷硫基丙基）苯并噻唑啉衍生物，其制备方法和含有它们的药物
公开(公告)号：US5240948A
公开(公告)日：1993-08-31
申请号：US647395
申请日：1991-01-29
申请人： Claude Gueremy , Patrick Jimonet
发明人： Claude Gueremy , Patrick Jimonet
IPC分类号： C07D277/82
CPC分类号： C07D277/82
摘要： Compounds of formula: ##STR1## in which R.sub.1 represents a polyfluoroalkoxy radical and R.sub.2 represents an alkylthio, alkylsulphinyl or alkylsulphonyl radical, their salts, their preparation and the medicaments containing them.
摘要翻译：其中R 1表示多氟烷氧基，R 2表示烷硫基，烷基亚磺酰基或烷基磺酰基，它们的盐，它们的制备方法和含有它们的药物。

10. 发明授权

US4999355A Isoindolinone derivatives, processes for preparing them and medicines containing them 失效
标题翻译：异吲哚啉酮衍生物，其制备方法和含有它们的药物
公开(公告)号：US4999355A
公开(公告)日：1991-03-12
申请号：US319302
申请日：1989-03-06
申请人： Marie-Therese Comte , Claude Gueremy , Gerard Ponsinet
发明人： Marie-Therese Comte , Claude Gueremy , Gerard Ponsinet
IPC分类号： C07D209/46 , A61K31/44 , A61K31/4427 , A61K31/495 , A61P43/00 , C07D209/48 , C07D209/50 , C07D401/06 , C07D401/12 , C07D401/14
CPC分类号： C07D209/48 , C07D401/06 , C07D401/14
摘要： Compounds of formula: ##STR1## in which: either R.sub.1 represents 4-phenyl-1,2,3,6-tetrahydro-1-pyridyl or 4-(4-fluorophenyl)-1,2,3,6-tetrahydro-1-pyridyl, R.sub.2 represents hydrogen, alkoxy of 1 or 2 carbon atoms, hydroxyl, alkyl, alkylthio, alkylcarbonyloxy, phenylalkylcarbonyloxy, phenylalkyl or --NR.sub.4 R.sub.5 in which R.sub.4 represents hydrogen or alkyl and R.sub.5 represents alkyl, phenyl, monohalogenated phenyl or pyridyl, and R.sub.3 represents a hydrogen atom, or else R.sub.2 represent phenyl and R.sub.3 represents hydrogen or hydroxyl;or R.sub.1 represnets 4-phenyl-1-piperazinyl whose phenyl nucleus has a substituent halogen atom or hydroxyl radical in the 4-position, R.sub.2 represents alkoxy and R.sub.3 represents hydrogen;it being understood that when R.sub.1 represents the 4-phenyl-1,2,3,6-tetrahydro-1-pyridyl radical, R.sub.2 is not hydroxyl and that, unless otherwise stated, the alkyl and alkoxy radicals and the alkyl and alkoxy portions contain 1 to 4 carbon atoms each in a straight or branched chain, and addition salts thereof with an inorganic or organic acid, are useful in therapy for their serotonin antagonist properties.
摘要翻译：式（I）的化合物，其中：R 1表示4-苯基-1,2,3,6-四氢-1-吡啶基或4-（4-氟苯基）四氢-1-吡啶基，R 2表示氢，1或2个碳原子的烷氧基，羟基，烷基，烷硫基，烷基羰基氧基，苯基烷基羰氧基，苯基烷基或-NR4R5，其中R4表示氢或烷基，R5表示烷基，苯基，单卤代苯基或吡啶基，R 3表示氢原子，或者R 2表示苯基，R 3表示氢或羟基; 或R 1表示4-苯基-1-哌嗪基，其苯基在4-位上具有取代基的卤原子或羟基，R2表示烷氧基，R3表示氢; 应当理解，当R 1表示4-苯基-1,2,3,6-四氢-1-吡啶基时，R 2不是羟基，除非另有说明，烷基和烷氧基以及烷基和烷氧基部分含有每个直链或支链的碳原子数为1至4个碳原子，和其与无机或有机酸的加成盐可用于治疗其5-羟色胺拮抗剂性质。

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