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1. 发明申请

WO2004085391B1 PROCESS FOR THE SYNTHESIS OF AMORPHOUS ATORVASTATIN CALCIUM 审中-公开
标题翻译：合成非晶态阿托伐他汀钙的方法
公开(公告)号：WO2004085391B1
公开(公告)日：2004-11-18
申请号：PCT/HU2004000026
申请日：2004-03-23
申请人： RICHTER GEDEON VEGYESZET , CZIBULA LASZLO , DOBAY LASZLO , WERKNE PAPP EVA , DEUTSCHNE JUHASZ IDA , BALINT SANDORNE
发明人： CZIBULA LASZLO , DOBAY LASZLO , WERKNE PAPP EVA , DEUTSCHNE JUHASZ IDA , BALINT SANDORNE
IPC分类号： A61P3/06 , C07D207/34 , A61K31/00
CPC分类号： C07D207/34
摘要： The invention relates to a new process for the synthesis of amorphous atorvastatin calcium, which consists of dissolving the salt of the formula (I) of atorvastatin acid formed with a basic amino acid (I); in a mixture of water and a water miscible organic solvent, adding an aqueous solution of a water soluble calcium salt to the solution and isolating the so obtained entirely amorphous atorvastatin calcium of high purity by filtration.
摘要翻译：本发明涉及一种合成无定形阿托伐他汀钙的新方法，其由溶解由碱性氨基酸（I）形成的阿托伐他汀酸的式（I）的盐; 在水和可与水混溶的有机溶剂的混合物中，向溶液中加入水溶性钙盐水溶液，并通过过滤分离如此获得的完全无定形的高纯度阿托伐他汀钙。

2. 发明申请

WO0181336A8 PROCESS FOR THE SYNTHESIS OF A KNOWN TETRAZOL DERIVATIVE 审中-公开
标题翻译：合成已知的四氮唑衍生物的方法
公开(公告)号：WO0181336A8
公开(公告)日：2002-08-29
申请号：PCT/HU0100047
申请日：2001-04-20
申请人： RICHTER GEDEON VEGYESZET , FISCHER JANOS , BALLO ILDIKO , PETENYI ENDRENE , KREIDL JANOS , CZIBULA LASZLO , NEMES ANDRAS , DEUTSCHNE JUHASZ IDA , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , HEGEDUS ISTVAN , FARKAS JEN ODBLAC
发明人： FISCHER JANOS , BALLO ILDIKO , PETENYI ENDRENE , KREIDL JANOS , CZIBULA LASZLO , NEMES ANDRAS , DEUTSCHNE JUHASZ IDA , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , HEGEDUS ISTVAN , FARKAS JEN ODBLAC
IPC分类号： A61P9/12 , C07D403/10 , A61K31/41
CPC分类号： C07D403/10
摘要： The invention relates to a process for the synthesis of losartan potassium of formula (I), chemical name: 2-n-butyl-4-chloro-1-[(2'-(tetrazol-5-yl)-1,1'biphenyl-4-yl)-methyl]-imidazol-5-methanol potassium, starting from 2-n-butyl-4-chloro-1-[(2'-(2-triphenylmetyl-2H-tetrazol-5-yl)-1,1'-biphenyl-4-yl)-methyl]-1H-imidazol-4-methanol of formula (III). According to the process the compound of formula (III) is reacted in an alcohol of formula (VI), - wherein the meaning of R is C1-C4 straight chain alkyl group -with 0.1-1 equivalent of potassium hydroxide. The final product of formula (I) is isolated after crystallizing out by changing the solvent to an aprotic or weakly protic solvent (I).
摘要翻译：本发明涉及一种合成式（I）的氯沙坦钾的方法，化学名称为：2-正丁基-4-氯-1 - [（2' - （四唑-5-基）-1,1' 联苯-4-基） - 甲基] - 咪唑-5-甲醇钾，由2-正丁基-4-氯-1 - [（2' - （2-三苯基甲基-2H-四唑-5-基） - 1,1'-联苯-4-基） - 甲基] -1H-咪唑-4-甲醇。根据该方法，式（Ⅳ）的化合物在式（Ⅵ）的醇中反应，其中R的含义是C 1 -C 4直链烷基 - 与0.1-1当量的氢氧化钾。通过将溶剂改变为非质子或弱质子性溶剂（I），结晶后分离出式（I）的最终产物。

3. 发明专利

BG66152B1 МЕТОД ЗА ПОЛУЧАВАНЕ НА ФЛУКОНАЗОЛ И НЕГОВИТЕ КРИСТАЛНИ МОДИФИКАЦИИ 未知
公开(公告)号：BG66152B1
公开(公告)日：2011-08-31
申请号：BG10817203
申请日：2003-09-11
申请人： RICHTER GEDEON VEGYESZET
发明人： KREIDL JANOS , CZIBULA LASZLO , SZANTAY CSABA , FARKAS JENONE , DEUTSCHNE JUHASZ IDA , HEGEDUS ISTVAN , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , PILLER AGNES
IPC分类号： C07D249/08
摘要： Изобретениетосеотнасядометодзаполучаваненафлуконазолс формула@@инеговитекристалнимодификации. Методътвключва: а) хидролизираненасилилетернопроизводнос формула@@вкоято R2 означававодородилиС1-С10 алкилнаилифенилнагрупа, R3 и R4 независимоединотдругсаС1-С10 алкилилифенилнигрупи- прирНкактопод 3, такаи над 8 въвводенразтвор, охлажданенаполученатареакционнасмеси изолираненапреципитиралияфлуконазолмонохидрат, разтваряненафлуконазолмонохидратав С1-С4 алкохолс праваилиразклоненаверигапритемпературанакипенеи охлажданенаразтвора, бавно, запредпочитанесъсскоростот 5 до 15 градусаС/h, заполучаваненакристалнатамодификация II нафлуконазола, илибързо, запредпочитанесъсскорост 35-65 градусаС/h заполучаваненакристалнатамодификация I нафлуконазола, ив дватаслучаяизолираненапреципитиралитекристалив разтвор, или b) разтваряненафлуконазолмонохидратав С1-С4 алкохолс праваилиразклоненаверигапритемпературанакипенеи охлажданенаразтворасъсскоростот 5 до 15 градусаС/h, заполучаваненакристалнатамодификация II нафлуконазола, илибързо, запредпочитанесъсскорост 35-65 градусаС/h, заполучаваненакристалнатамодификация I нафлуконазола, ив дватаслучаяизолираненапреципитиралитекристалив разтвори изсушаване, илис) изсушаванебавнонафлуконазолмонохидратаследпосяване, запредпочитанес кристализанарастванес кристалнамодификация II при 30 и 70 градуса

4. 发明专利

CA2439310C PROCESS FOR PREPARING FLUCONAZOLE AND ITS CRYSTAL MODIFICATIONS 未知
公开(公告)号：CA2439310C
公开(公告)日：2009-09-29
申请号：CA2439310
申请日：2001-03-23
申请人： RICHTER GEDEON VEGYESZET
发明人： WERKNE PAPP EVA , SZANTAY CSABA , CZIBULA LASZLO , PILLER AGNES , FARKAS JENONE , HEGEDUS ISTVAN , KREIDL JANOS , DEUTSCHNE JUHASZ IDA , NAGYNE BAGDY JUDIT
IPC分类号： C07D249/08
摘要： The invention relates to a process for preparing of fluoconazole of formula (I) and its crystal modifications. The process is as follows; a) hydrolyzing a silyl ether derivative of formula (II) wherein the meaning of R2 is hydrogen , or a C1-C10 alkyl or phenyl group, R3 and R4 independently of each other are a C1-C10alkyl or phenyl group -at a pH preferably either below 3 or above 8 in an aqueous solution, cooling the obtained reaction mixture and isolating the precipitated fluconazole monohydrate, dissolving the fluconazole monohydrate in a C1-C4 straight or branched chain alcohol at boiling temperature and cooling the solution slowly, preferably with a speed of 5-15 ~C/h to obtain the crystal modification II of fluconazole, or fast, preferably with a speed of 35-65 ~C/h to obtain the crystal modification I of fluconazole and in bot h cases isolating the precipitated crystals and rying, or b) dissolving fluconazole monohydrate in C1-C4 straigth or branched chain alcohol at boili ng temperature and cooling the solution slowly, preferably with a speed of 5-15 ~C/h to obtain the crystal modification II of fluconazole, or fast, preferab ly with a speed of 35-65 ~C/h to obtain the crystal modification I of fluconazo le and in both cases isolating the precipitated crystals and drying, or c) dryi ngslowly fluconazole monohydrate after seeding preferably with seeding cryst als of crystal modification II at 30-70 ~C, preferably in vacuum to obtain the crystal modification II of fluconazole, or d) drying fast fluconazole monohydrate after seeding preferably with seeding crystals of crystal modification I at 80 ~C, to obtain the crystal modification I of fluconazole .

5. 发明专利

DE60114889T2 未知
公开(公告)号：DE60114889T2
公开(公告)日：2006-07-20
申请号：DE60114889
申请日：2001-03-23
申请人： RICHTER GEDEON VEGYESZET
发明人： KREIDL JANOS , CZIBULA LASZLO , SZANTAY CSABA , FARKAS JENONE , DEUTSCHNE JUHASZ IDA , HEGEDUS ISTVAN , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , PILLER AGNES
IPC分类号： C07D249/08

6. 发明专利

DE60114889D1 未知
公开(公告)号：DE60114889D1
公开(公告)日：2005-12-15
申请号：DE60114889
申请日：2001-03-23
申请人： RICHTER GEDEON VEGYESZET
发明人： KREIDL JANOS , CZIBULA LASZLO , SZANTAY CSABA , FARKAS JENONE , DEUTSCHNE JUHASZ IDA , HEGEDUS ISTVAN , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , PILLER AGNES
IPC分类号： C07D249/08

7. 发明专利

PL363756A1 PROCESS FOR PREPARING FLUCONAZOLE AND ITS CRYSTAL MODIFICATIONS 未知
公开(公告)号：PL363756A1
公开(公告)日：2004-11-29
申请号：PL36375601
申请日：2001-03-23
申请人： RICHTER GEDEON VEGYESZET
发明人： KREIDL JANOS , CZIBULA LASZLO , SZANTAY CSABA , FARKAS JENONE , DEUTSCHNE JUHASZ IDA , HEGEDUS ISTVAN , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , PILLER AGNES
IPC分类号： C07D249/08

8. 发明专利

PL186626B1 ESTER-TYPE DERIVATIVES OF TRANSAPOVINCAMINIC ACID AS DRUGS 未知
公开(公告)号：PL186626B1
公开(公告)日：2004-02-27
申请号：PL32817096
申请日：1996-12-13
申请人： RICHTER GEDEON VEGYESZET
发明人： SZANTAY CSABA , MOLDVAI ISTVAN , VEDRES ANDRAS , INCZE MARIA , KREIDL JANOS , CZIBULA LASZLO , FARKAS JENONE , DEUTSCHNE JUHASZ IDA , GERE ANIKO , PELLIONISZNE PAROCZAI MARGIT , LAPIS ERZSEBET , SZEKERES ANDRAS , ZAJERNE BALAZS MARIA , SARKADI ADAM , AUTH FERENC , KISS BELA , KARPATI EGON , FARKAS SANDOR
IPC分类号： A61K31/00 , A61K31/395 , A61K31/435 , A61K31/4353 , A61K31/4375 , A61P9/00 , A61P9/10 , A61P25/28 , C07D461/00
摘要： PCT No. PCT/HU96/00075 Sec. 371 Date Jun. 9, 1998 Sec. 102(e) Date Jun. 9, 1998 PCT Filed Dec. 13, 1996 PCT Pub. No. WO97/23481 PCT Pub. Date Jul. 3, 1997The invention relates to novel racemic and optically active trans apovincaminic acid ester derivatives of formula (I), wherein R means hydrogen or a group (a), wherein Z stands for C1-4 alkyl, optionally substituted aryl, aralkyl, heteroaryl or 14-eburnameninyl group; and n is an integer of 2, 3 or 4, as well as therapeutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing these compounds as well as a process for the preparation of the above compounds and compositions, and in addition, to a method of treatment. The novel compounds of Formula (I) exhibit particularly antioxidant, antiischemic as well as antiamnesic effects and are useful for inhibiting lipid peroxidation and for protection from or treatment of ischemia and amnesia as well as for treating various degenerative neurological diseases, e.g. Alzheimer's disease.

9. 发明专利

SK12892002A3 PROCESS FOR THE SYNTHESIS OF A KNOWN TETRAZOL DERIVATIVE 未知
公开(公告)号：SK12892002A3
公开(公告)日：2002-12-03
申请号：SK12892002
申请日：2001-04-20
申请人： RICHTER GEDEON VEGYESZET
发明人： FISCHER JANOS , BALLO ILDIKO , PETENYI ENDRENE , KREIDL JANOS , CZIBULA LASZLO , NEMES ANDRAS , DEUTSCHNE JUHASZ IDA , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , HEGEDUS ISTVAN , FARKAS JENONE
IPC分类号： A61P9/12 , C07D403/10 , A61K31/41
摘要： A Process is disclosed for preparing a compound of the Formula (I)which comprises the steps of:(a) detritylating a compound of the Formula (III)with 0.1 to 1 equivalent of potassium hydroxide in a C1 to C4 straight chain alcohol solvent to obtain a reaction mixture containing the compound of the Formula (I),(b) changing the C1 to C4 straight chain alcohol solvent in the reaction mixture to an aprotic solvent or a weakly protic solvent, and(c) following step (b) crystallizing out the compound of the Formula (I) from the reaction mixture.

10. 发明专利

CA2238635A1 TRANS APOVINCAMINIC ACID ESTER DERIVATIVES AS DRUGS 未知
公开(公告)号：CA2238635A1
公开(公告)日：1997-07-03
申请号：CA2238635
申请日：1996-12-13
申请人： RICHTER GEDEON VEGYESZET
发明人： LAPIS ERZSEBET , FARKAS SANDOR , PELLIONISZNE PAROCZAI MARGIT , KARPATI EGON , MOLDVAI ISTVAN , SZEKERES ANDRAS , SARKADI ADAM , KISS BELA , AUTH FERENC , SZANTAY CSABA , DEUTSCHNE JUHASZ IDA , GERE ANIKO , ZAJERNE BALAZS MARIA , CZIBULA LASZLO , FARKAS JENONE KIRJAK MARIA , KREIDL JANOS , INCZE MARIA , VEDRES ANDRAS
IPC分类号： A61K31/00 , A61K31/395 , A61K31/435 , A61K31/4353 , A61K31/4375 , A61P9/00 , A61P9/10 , A61P25/28 , C07D461/00 , A61K31/505 , A61K31/535
摘要： The invention relates to novel racemic and optically active trans apovincaminic acid ester derivatives of formula (I), wherein R means hydrogen or a group (a), wherein Z stands for C1-4 alkyl, optionally substituted aryl, aralkyl, heteroaryl or 14-eburnameninyl group; and n is an integer of 2, 3 or 4, as well as therapeutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing these compounds as well as a process for the preparation of the above compounds and compositions, and in addition, to a method of treatment. The novel compounds of formula (I) exhibit particularly antioxidant, antiischemic as well as antiamnesic effects and are useful for inhibiting lipid peroxidation and for protection from or treatment of ischemia and amnesia as well as for treating various degenerative neurological diseases, e.g. Alzheimer's disease.

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