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1. 发明公开

EP1345897A1 CHEMICAL PROCESS AND NEW INTERMEDIATES 审中-公开
标题翻译： CHEMISCHES VERFAHREN UNDER NEUE ZWISCHENPRODUKTE
公开(公告)号：EP1345897A1
公开(公告)日：2003-09-24
申请号：EP01998539.9
申请日：2001-11-27
申请人： SANOFI-SYNTHELABO
发明人： BOKOTEY, Sándor , GALAMBOS, Gézáné , HAJDU, Félix , HERMECZ, István , HORVATH, Agnes , IVANICS, Józsefné , KISS, Gyuláné , NAGY, Lajos , PODANYI, Benjámin , SIMON, Attila , SIPOS, Judit , SMELKONE ESEK, Agota , SZAB , Anna , VASVARI, Arpádné
IPC分类号： C07D209/42 , C07D417/12 , C07C49/84 , C07C323/22
CPC分类号： C07D417/12 , C07C45/46 , C07C45/63 , C07C49/84 , C07C323/22 , C07C2601/14 , C07D209/42
摘要： Process for the preparation of a compound of the general formula (I) and pharmaceutically acceptable salts and solvates thereof, (I) characterised by reacting an N-(amino-tioxo-methyl)-1H-indole-2-carboxamide of the general formula (II), with an α-halogen-ketone of the general formula (III), wherein X stands for halogen.
摘要翻译：制备通式（I）化合物及其药学上可接受的盐和溶剂化物的方法，（I）的特征在于使通式（I）的N-（氨基 - 氧代 - 甲基）-1H-吲哚-2-甲酰胺与通式（II）与通式（III）的α-卤代酮反应，其中X代表卤素。

2. 发明公开

EP1337519A1 PROCESS FOR THE PREPARATION OF 1,5-DISUBSTITUATED-3-AMINO-1,2,4-TRIAZOLES AND SUBSTITUTED AMINOGUANIDINES AS INTERMEDIATE COMPOUNDS 审中-公开
标题翻译：用于生产1,5-二取代的3-氨基-1,2,4-三唑和取代的氨基胍中间产品
公开(公告)号：EP1337519A1
公开(公告)日：2003-08-27
申请号：EP01982628.8
申请日：2001-10-25
申请人： SANOFI-SYNTHELABO
发明人： BOKOTEY, Sándor , CSIKOS, Eva , GöNCZI, Csaba , HAJDU, Félix , HERMECZ, István , HEJA, Gergely , PODANYI, Benjámin , SANTANE, Csutor, Andrea , SZOMOR, Tiborné , SZVOBODA, Györgyné
IPC分类号： C07D249/14 , C07C281/16 , C07D295/12
CPC分类号： C07D295/13 , C07C281/16 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D249/14
摘要： New process for the preparation of 1,5-disubstituted-3-amino-1,2,4-triazoles of the general formula (I), wherein the meaning of R is C1-5alkyl group; C3-13cycloalkyl-C0-4alkyl group, optionally substituted by one or more C1-3alkyl group; phenyl-C0-2alkyl-, (CH2)n-morpholino-, piperidino-, pyrrolidino- or piperazino-group, optionally substituted by one or more halogen atom, C1-3alkyl group, C1-3alkoxy group, n is 1-5, R?1, R2, R3, and R4¿ stand independently for hydrogen, halogen, C¿1-6?alkyl group, C1-3alkoxy group or trifuluoromethyl group, with the proviso that of the substituents R?1, R2, R3, and R4¿ at least one stands for hydrogen.
摘要翻译：为1,5-二取代的3-氨基-1,2,4-三唑通式（I），worin R的含义是C 1-5烷基基团的制备新方法; C3-13cycloalkyl-C 0-4烷基基团，被一个或多个C 1-3烷基，任选地substituiertem; 苯基C0-2alkyl-，（CH2）N-吗啉代，哌啶子基，吡咯烷基或哌嗪基团，任选地被一个或多个卤原子，C 1-3烷基，C 1-3烷氧基的基团取代，n为1-5， [R <1>，R <2> [R <3>，和R <4>是unabhängig为氢，卤素，C 1-6烷基，C 1-3烷氧基团或trifuluoromethyl基，其条件没有取代基R <1 >，R <2> [R <3>，和R <4>的至少一个代表氢。

3. 发明公开

EP1202960A1 METHOD FOR THE PREPARATION OF 2-METHOXY-4-(N-T-BUTYLAMINO-CARBONYL)-BENZENESULFONYL CHLORIDE 有权
标题翻译： PROCESS FOR 2-甲氧基-4-（N-叔丁基氨基羰基）的制备-BENZOLSULFONSAÜRECHLORID
公开(公告)号：EP1202960A1
公开(公告)日：2002-05-08
申请号：EP00949824.7
申请日：2000-07-13
申请人： SANOFI-SYNTHELABO
发明人： GÖNCZI, Csaba , CSIKOS, Eva, , HAJDU, Félix , HERMECZ, István , HEJA, Gergelyné , HEJA, Gergelyné , NAGY, Lajos , SANTANE CSUTOR, Andrea , SIMON, Kálmán , SMELKONE ESEK, Agota , SZOMOR, Tiborné , SZVOBODA, Györgyné
IPC分类号： C07C303/06 , C07C303/22 , C07C309/60 , C07C309/89
CPC分类号： C07C303/32 , C07C303/06 , C07C303/22 , C07C309/60 , C07C309/89
摘要： The invention relates to a process for the preparation of 2-methoxy-4-(N-t-butylaminocarbonyl) benzenesulfonyl chloride by sulfonating m-hydroxybenzoic acid, methylating the hydroxy group of the resulting sulfonic acid or its salt, transforming the carboxylic acid group and the sulfonic acid group to acid chloride groups and reacting the 4-chlorosulfonyl-3-methoxy-benzoyl chloride with t-butylamine, which comprises carrying out the sulfonation of the 3-methoxy-benzoic acid of general formula (II) with 96 % sulfuric acid, separating the resulting 3-hydroxy-4-sulfobenzoic acid of general formula (III) in the form of its salt of general formula (IV), wherein Z stands for alkali metal or ammonium group, methylating the compound of general formula (IV) in the presence of a phase transfer catalyst at a pH value of about 11.5, transforming the 3-methoxy-4-sulfobenzoic acid mono salt of general formula (V), wherein the meaning of Z is as defined above, to the acid chloride of general formula (VI), and reacting the compound of genneral formula (VI) with t-butylamine used in equimolar amount or in a small excess, in the presence of an acid binding agent, in aprotic solvent, at low temperature.

4. 发明授权

EP1202960B1 METHOD FOR THE PREPARATION OF 2-METHOXY-4-(N-T-BUTYLAMINO-CARBONYL)-BENZENESULFONYL CHLORIDE 有权
标题翻译： PROCESS FOR 2-甲氧基-4-（N-叔丁基氨基羰基）的制备-BENZOLSULFONSAÜRECHLORID
公开(公告)号：EP1202960B1
公开(公告)日：2004-03-10
申请号：EP00949824.7
申请日：2000-07-13
申请人： SANOFI-SYNTHELABO
发明人： GÖNCZI, Csaba , CSIKOS, Eva, , HAJDU, Félix , HERMECZ, István , HEJA, Gergely , HEJA, Gergelyné , NAGY, Lajos , SANTANE CSUTOR, Andrea , SIMON, Kálmán , SMELKONE ESEK, Agota , SZOMOR, Tiborné , SZVOBODA, Györgyné
IPC分类号： C07C303/06 , C07C303/22 , C07C309/60 , C07C309/89
CPC分类号： C07C303/32 , C07C303/06 , C07C303/22 , C07C309/60 , C07C309/89
摘要： The invention relates to a process for the preparation of 2-methoxy-4-(N-t-butylaminocarbonyl) benzenesulfonyl chloride by sulfonating m-hydroxybenzoic acid, methylating the hydroxy group of the resulting sulfonic acid or its salt, transforming the carboxylic acid group and the sulfonic acid group to acid chloride groups and reacting the 4-chlorosulfonyl-3-methoxy-benzoyl chloride with t-butylamine, which comprises carrying out the sulfonation of the 3-methoxy-benzoic acid of general formula (II) with 96 % sulfuric acid, separating the resulting 3-hydroxy-4-sulfobenzoic acid of general formula (III) in the form of its salt of general formula (IV), wherein Z stands for alkali metal or ammonium group, methylating the compound of general formula (IV) in the presence of a phase transfer catalyst at a pH value of about 11.5, transforming the 3-methoxy-4-sulfobenzoic acid mono salt of general formula (V), wherein the meaning of Z is as defined above, to the acid chloride of general formula (VI), and reacting the compound of genneral formula (VI) with t-butylamine used in equimolar amount or in a small excess, in the presence of an acid binding agent, in aprotic solvent, at low temperature.

5. 发明公开

EP1456204A1 TRIAZOLO-QUINOLIN DERIVATIVES USEFUL AS ADENOSINE RECEPTOR LIGANDS 审中-公开
标题翻译：三唑醇 - 喹诺酮衍生物维生素ALS ADENOSINREZEPTORLIGANDEN
公开(公告)号：EP1456204A1
公开(公告)日：2004-09-15
申请号：EP02788260.4
申请日：2002-12-17
申请人： SANOFI-SYNTHELABO
发明人： ARANYI, Péter , BALAZS, Lászlo , BATORI, Sándor , BENCE, Judit , BOER, Kinga , HAJDU, Félix , KAPUI, Zoltán , MIKUS, Endre , SZABO, Tibor , T. NAGY, Lajos , TIMARI, Géza , URBAN-SZABO, Katalin , WALCZ, Erzsébet
IPC分类号： C07D471/04 , C07D213/89 , C07D405/12 , A61K31/506
CPC分类号： C07D471/04 , C07D215/54 , C07D215/56
摘要： The present invention relates to adenosine A3 receptor ligands of the general formula (I), within those preferably antagonists, as well as their salts, solvates and isomers, and the pharmaceutical compositions containing them, to the use of the compounds of the general formula (I), as well as their salts, solvates and isomers, to the preparation of the compounds of the general formula (I) and theirs salts, solvates and isomers, furthermore to the new intermediates of the general formulae (II) and to the preparation thereof.
摘要翻译：三唑并喹啉衍生物是新的。式（I）的三唑并喹啉衍生物，其盐，溶剂合物和旋光异构体及其盐或溶剂合物是新的。 R 1> R 2> H或直链或支链的1-4C烷基; R 3>直链或支链的1-4C烷基，苯基，噻吩基，呋喃基（任选被至少一个直链或支链的1-4C烷基，直链或支链的1-4C烷氧基或卤素取代），H，5-6元杂芳环含有1-3个氮原子或5元杂芳环，其含有一个氮原子和一个氧原子或一个氮原子和一个硫原子（任选地被至少一个直链或支链的1-4C烷基，直链或支链的1-4C烷氧基或卤素）; R 4>和R 5> H; R 4> + R 5> 1,3-丁二烯基（任选被亚甲二氧基或至少一个直链或支链的1-4C烷基，直链或支链的1-4C烷氧基，OH或卤素取代）; R 6> H，氰基，氨基羰基，1-4C烷氧基羰基或羧基; R 7>苯基，苄基，噻吩基，呋喃基（全部由亚甲二氧基或至少一个直链或支链的1-4C烷基，直链或支链的1-4C烷氧基，OH，三氟甲基，氰基或卤素取代），H，直链或支链 1-4C烷基或1-4C亚烷基（任选被苯基取代），氨基，一或二烷基氨基，含有1-3个N原子的5-6元杂芳环或含有一个氮原子和一个氧原子的5元杂芳环或一个氮原子和一个硫原子（任选地被至少一个直链或支链的1-4C烷基，直链或支链的1-4C烷氧基或卤素取代）; X：-CH 2 - ， - NH - ， - NR 1 - ， - S，O，磺基或磺氧基; R 1> 2>直链或支链的1-4C烷基或3-6C环烷基; 和n：0 - 2.还包括：（1）（I）的制备; 和（2）式（II）的新的中间体1,2-二氨基吡啶盐。活动： Nephrotropic; 抗过敏; 抗炎; 皮肤; 银屑病; 低血压; 眼科; 降血糖; 平喘; 免疫抑制; 抗风湿; 抑制细胞生长; Vasotropic; 抗心律不整。作用机制：腺苷A 3受体拮抗剂。使用HEK-293细胞测试化合物的腺苷A 3受体拮抗活性。描述测试细节，但没有给出具体化合物的结果。通常化合物（I）显示K i为3.5和0.78nM。

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