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1. 发明申请

WO2004026845A1 NEW PROCESS FOR THE SYNTHESIS OF HIGH PURITY 3,5-DIAMINO-6-(2, 3-DICHLOROPHENYL)-1,2,4-TRIAZINE 审中-公开
标题翻译：合成高纯度3,5-二氨基-6-（2,3-二氯苯基）-1,2,4-三嗪的新工艺
公开(公告)号：WO2004026845A1
公开(公告)日：2004-04-01
申请号：PCT/HU2003/000072
申请日：2003-09-18
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , NEU, József , GIZUR, Tibor , TÖRLEY, József , CSABAI, János , VÉGH, Ferenc , KÁLVIN, Péter , TÁRKÁNYI, Gábor
发明人： NEU, József , GIZUR, Tibor , TÖRLEY, József , CSABAI, János , VÉGH, Ferenc , KÁLVIN, Péter , TÁRKÁNYI, Gábor
IPC分类号： C07D253/06
CPC分类号： C07D253/075 , C07C281/16
摘要： The present invention relates to a new process for the synthesis of high purity 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine of formula (I) using 2,3-dichlorobenzoyl cyanide and an aminoguanidine salt as starting materials. 2,3-dichlorobenzoyl cyanide is reacted with 1-2 mol equivalent of aminoguanidine salt in 3-6 mol equivalent of methanesulfonic acid, then the obtained adduct of formula (IV) is transformed without isolation into the product with magnesium oxide. In given case the obtained crude product can be recrystallized from a proper organic solvent.
摘要翻译：本发明涉及使用2,3-二氯苯甲酰氰合成式（I）的高纯度3,5-二氨基-6-（2,3-二氯苯基）-1,2,4-三嗪的新方法，氨基胍盐为起始原料。将2,3-二氯苯甲酰氰与1-2摩尔当量的氨基胍盐在3-6摩尔当量甲磺酸中反应，然后将得到的式（Ⅳ）加合物转化为不含氧化镁的产物。在给定情况下，所得粗产物可以从合适的有机溶剂中重结晶。

2. 发明申请

WO2005005373A1 A PROCESS FOR THE PREPARATION OF CHIRALLY PURE N-(TRANS-4-ISOPROPYL-CYCLOHEXYLCARBONYL)-D-PHENYLALANINE AND CRYSTALLINE MODIFICATIONS THEREOF 审中-公开
标题翻译：制备纯化N-（反式-4-异丙基 - 环己基甲基）-D-苯并噻喃的方法及其结晶改性方法
公开(公告)号：WO2005005373A1
公开(公告)日：2005-01-20
申请号：PCT/HU2004/000073
申请日：2004-07-08
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , GAZDAG, Mária , GIZUR, Tibor , HEGEDÛS, Béla , SZEMZÕ, Attila , TÁRKÁNYI, Gábor , TÖRLEY, József , BABJÁK, Mónika
发明人： GAZDAG, Mária , GIZUR, Tibor , HEGEDÛS, Béla , SZEMZÕ, Attila , TÁRKÁNYI, Gábor , TÖRLEY, József , BABJÁK, Mónika
IPC分类号： C07C231/12
CPC分类号： C07C233/63 , C07C231/12 , C07C231/24
摘要： The invention relates to N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine (nateglinide) in the novel crystalline form “G” and a process for the preparation thereof. A process for the preparation of chirally pure nateglinide by treating a lower alkyl ester thereof with a base to yield an alkali salt and liberating the product from said salt by proper addition of an acid, is also provided. Still another aspect of the invention is a process for the preparation of nateglinide in the crystalline form “H” from other crystalline modifications of nateglinide.
摘要翻译：本发明涉及新型晶型“G”中的N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸（那格列奈）及其制备方法。还提供了通过用碱处理其低级烷基酯以产生碱金属盐并通过适当添加酸从所述盐释放产物来制备手性纯奈格列奈的方法。本发明的另一方面是从那格列奈的其他结晶修饰物制备结晶形式“H”的那格列奈的方法。

3. 发明申请

WO2003028725A1 4-(1-PIPERIDINY)-BUTYLCARBOXAMIDE AS D3 DOPAMINE RECEPTOR SUBTYPE SELECTIVE LIGANDS 审中-公开
标题翻译： 4-（1-哌啶基） - 丁酰胺作为D3多巴胺受体亚型选择性配体
公开(公告)号：WO2003028725A1
公开(公告)日：2003-04-10
申请号：PCT/HU2002/000094
申请日：2002-09-25
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , ÁCS, Tibor , ÁGAINÉ CSONGOR, Éva , BARTÁNÉ SZALAI, Gizella , MAGDÓ, Ildikó , TÁRKÁNYI, Gábor , DOMÁNY, György , KISS, Béla , GYERTYÁN, István , LASZLOVSZKY, István , GÁL, Krisztina
发明人： ÁCS, Tibor , ÁGAINÉ CSONGOR, Éva , BARTÁNÉ SZALAI, Gizella , MAGDÓ, Ildikó , TÁRKÁNYI, Gábor , DOMÁNY, György , KISS, Béla , GYERTYÁN, István , LASZLOVSZKY, István , GÁL, Krisztina
IPC分类号： A61K31/4468
CPC分类号： C07D401/06 , A61K31/445 , A61K31/4468 , A61K31/4523 , A61K31/4535 , A61K31/4545 , A61K31/4709 , A61K31/519 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/34 , C07D211/46 , C07D211/58 , C07D401/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention relates to new D 3 dopamine receptor subtype selective ligands of Formula (I), wherein R 1 and R 2 represent independently a substituent selected from hydrogen, halogen, C 1-6 alkyl, C¿1-6 ?alkoxy, cyano, hydroxy, trifluoromethyl, C 1-6 alkylsulfonyloxy, trifluoromethanesulfonyloxy, optionally substituted C 1-6 alkanoyloxy, amino, aminoalkyl, carboxy, aminocarbonyl, N-hydroxycarbamimidoyl, carbamimidoyl, hydroxycarbamoyl, thiocarbamoyl, sulfamoyl or mono or bicyclic heterocyclic group; Y represents an oxygen atom or NH or CH 2 or OCH 2 group; Q represents an optionally substituted C 1-6 alkyl, aryl, heteroaryl, heteroaralkyl or heteroaralkenyl group, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or the salts and/or hydrates and/or solvates thereof, to the process for producing the same, to pharmacological compositions containing the same and to their use in therapy and/or prevention of psychoses (e.g. schizophrenia, schizo-affective disorders, etc.), drug (e.g. alcohol, cocaine and nicotine, opioids, etc.) abuse, cognitive impairment accompanying schizophrenia, mild-to-moderate cognitive deficits, amnesia, eating disorders (e.g. bulimia nervosa, etc.), attention deficit/hyperactivity disorder in children, psychotic depression, mania, paranoid and delusional disorders, dyskinetic disorders (e.g. Parkinson's disease, neuroleptic induced parkinsonism, tardive dyskinesias) anxiety, sexual disorders, sleep disorders, emesis, aggression, autism, pain, ophthalmological diseases (e.g. glaucoma, etc.).
摘要翻译：本发明涉及式（I）的新的D3多巴胺受体亚型选择性配体，其中R 1和R 2分别独立地表示选自氢，卤素，C 1-6烷基，C 1-6烷氧基，氰基，羟基，三氟甲基，C 1-6烷基磺酰氧基三氟甲磺酰氧基，任选取代的C 1-6烷酰氧基，氨基，氨基烷基，羧基，氨基羰基，N-羟基甲脒基，氨基甲酰基，羟基氨基甲酰基，硫代氨基甲酰基，氨磺酰基或单或双环杂环基。 Y表示氧原子或NH或CH 2或OCH 2基团; Q表示任选取代的C 1-6烷基，芳基，杂芳基，杂芳烷基或杂链烯基，和/或几何异构体和/或立体异构体和/或非对映异构体和/或其盐和/或水合物和/或溶剂化物制备相同的药物组合物，以及其用于治疗和/或预防精神病（例如精神分裂症，分裂症情感障碍等），药物（例如酒精，可卡因和尼古丁，阿片样物质等）滥用中的用途伴随精神分裂症的认知障碍，轻度至中度的认知缺陷，健忘症，进食障碍（例如神经性贪食症等），儿童注意力缺陷/多动障碍，精神抑郁症，躁狂症，偏执狂和妄想症，运动障碍（如帕金森病焦虑症，性障碍，睡眠障碍，呕吐，侵略，自闭症，疼痛，眼科疾病（如青光眼等））。

4. 发明申请

WO2005073235A2 PROCESS FOR THE SYNTHESIS OF N- [3-(3-CYANOPYRAZOLO [1,5A] PYRIMIDIN-7-YL)-PHENYL]-N-ETHYL-ACETAMIDE 审中-公开
标题翻译：合成N- [3-（3-氰基吡唑并[1,5A]吡啶基-7-YL） - 苯基] -N-乙基 - 乙酰胺的方法
公开(公告)号：WO2005073235A2
公开(公告)日：2005-08-11
申请号：PCT/HU2005/000008
申请日：2005-01-31
申请人： RICHTER GEDEON VEGYÉSZETI GYÁR RT. , CZIBULA, László , DOBAY, László , SZÕKE, Katalin , WERKNÉ PAPP, Éva , NAGYNÉ BAGDY, Judit , TÁRKÁNYI, Gábor
发明人： CZIBULA, László , DOBAY, László , SZÕKE, Katalin , WERKNÉ PAPP, Éva , NAGYNÉ BAGDY, Judit , TÁRKÁNYI, Gábor
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07C233/43
摘要： The invention relates to N- [3- (3-cyanopyrazolo [1,5-a] pyrimidin-7-yl) - phenyl]-N-ethyl-acetamide of formula (IV) containing less than 0.2 % impurities, which is suitable for therapeutic application. Furthermore the invention relates to a process for the synthesis of therapeutically applicable compound of formula (IV) containing less than 0.2 % impurities by reacting the new intermediate N-{3-[3-(dimethylamino)-1-oxo-2-propenyl]phenyl}-N-ethylacetamide hydrochloride of formula (II) and 3-amino-4-pyrazol-carbonitrile base of formula (III) in an acid free medium. The invention also relates to the new N- {3- [3- (dimethylamino) -1- oxo -2- propenyl]phenyl } -N-ethyl-acetamide hydrochloride of formula (II). The invention also relates to a process for the synthesis of the new N- [3- [3, (dimethylamino)-1-oxo-2-propenyl]phenyl}-N-ethyl-acetamide hydrochloride of formula (II) having a purity of more than 99.5 %. Furthermore the invention relates to N-{3-[3-cyanopyrazolo (1,5-a) pyrimidin]6 -yl-3- [ (3-N-ethyl-acetamido-phenyl) -3-oxo-propen-1-yl] - (pyrimidin-7-yl) -phenyl} - N-ethyl-acet-amide of formula (V), which is an isolated new impurity formed in 0.07 % yield during the synthesis of compound of formula (IV).
摘要翻译：本发明涉及含有小于0.2％杂质的式（IV）的N- [3-（3-氰基吡唑并[1,5-a]嘧啶-7-基） - 苯基] -N-乙基 - 乙酰胺，其是合适的用于治疗应用。此外，本发明涉及通过使新的中间体N- {3- [3-（二甲基氨基）-1-氧代-2-丙烯基] -1-哌嗪基] 苯基} -N-乙基乙酰胺盐酸盐和式（III）的3-氨基-4-吡唑基 - 腈基的无酸介质中。本发明还涉及式（II）的新的N- {3- [3-（二甲基氨基）-1-氧代-2-丙烯基]苯基} -N-乙基 - 乙酰胺盐酸盐。本发明还涉及合成具有纯度的式（II）的新的N- [3- [3，（二甲基氨基）-1-氧代-2-丙烯基]苯基} -N-乙基 - 乙酰胺盐酸盐的方法超过99.5％。此外，本发明涉及N- {3- [3-氰基吡唑并（1,5-a）嘧啶] -6-基-3 - [（3-N-乙基 - 乙酰氨基 - 苯基）-3-氧代 - 吡啶-2-基] - （嘧啶-7-基） - 苯基} -N-乙基 - 乙酰胺，其是在合成式（IV）化合物期间以0.07％产率形成的分离的新杂质。

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