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1. 发明申请

WO2005073235A3 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[1,5-a]嘧啶-7-基） - 苯基] -N-乙基 - 乙酰胺的方法
公开(公告)号：WO2005073235A3
公开(公告)日：2005-10-06
申请号：PCT/HU2005000008
申请日：2005-01-31
申请人： RICHTER GEDEON VEGYESZET , CZIBULA LASZLO , DOBAY LASZLO , SZOKE KATALIN , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , TARKANYI GABOR
发明人： CZIBULA LASZLO , DOBAY LASZLO , SZOKE KATALIN , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , TARKANYI GABOR
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：本发明涉及含有少于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，用于治疗应用。此外，本发明涉及一种通过使新的中间体N- {3- [3-（二甲基氨基）-1-氧代-2-丙烯基] -1,3,5-三嗪与式（IV）化合物反应合成含有少于0.2％苯基} -N-乙基乙酰胺盐酸盐和式（III）的3-氨基-4-吡唑甲腈碱在无酸介质中反应。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 - 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％收率形成的分离的新杂质。

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

BG65699B1 PROCESS FOR THE SYNTHESIS OF A TETRAZOL DERIVATIVE 未知
公开(公告)号：BG65699B1
公开(公告)日：2009-07-31
申请号：BG10703102
申请日：2002-08-23
申请人： RICHTER GEDEON VEGYESZET
发明人： FISCHER JANOS , BALLO ILDIKO , PATENYI ENDRENE , KREIDL JANOS , CZBULA LASZLO , NEMES ANDRAS , DEUTSCHNE JUHASZ IDA , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , HEGEDUS ISTVAN , FARKAS JENONE
IPC分类号： C07D403/10 , A61K31/41 , A61P9/12
摘要： The invention relates to a process for the synthesis of losartan potassium of formula in particular potassium salt of 2-n-butyl-4-chloro-1[(2'-(tetrazol-5-yl)-1,1'-biphenyl-4-yl)-methyl]imidazol-5-methanol. The yield of the end product is increased. According to the process initial compound is used of 2-n-butyl-4-chloro-1[2'-(2-triphenylmethyl-2H-tetrazol-5-yl)-1,1'-biphenyl-4-yl)-methyl]-1H-imidazol-4-methonol with the formula which reacts in alcohol with formula wherein R means C1-C4 alkyl group with a strain chain, with 0.1-1 equivalent of potassium hydroxide. The final product with formula (I) is isolated after crystallizing out by changing the solvent to an aprotic or weakly protic solvent.

4. 发明专利

RS20060427A POSTUPAK ZA DOBIJANJE N-/3(3-CIJANOPIRAZOLO/1,5a/PIRIMIDIN-7- IL)-FENIL/-N-ETIL-ACETAMIDA 未知
公开(公告)号：RS20060427A
公开(公告)日：2008-08-07
申请号：RSP20060427
申请日：2005-01-31
申请人： RICHTER GEDEON VEGYESZET
发明人： CZIBULA LASZLO , DOBAY LASZLO , SZOKE KATALIN , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , TARKANYI GABOR
IPC分类号： C07D487/04
摘要： Postupak se odnosi na N-[3- (3-cijanopirazolo [1,5a] pirimidin -7-il) -fenil]-N-etilacetamid formule (IV) koji sadrži manje od 0,2% nečistoće, koji je pogodan za terapijsko davanje. Osim toga postupak se odnosi na sintezu terapijski prihvatljivih jedinjenja formule (IV) koje sadrže manje od 0,2% nečistoće reagujući sa novim intermedijerom N-{3-[3(dimetilamino )-1-okso-2-propenil]fenil} -N -etil-acetamid hidrohloridom formule (II) i 3-amino-4-pirazol-karbonitril bazom formule (III) u ne kiseloj sredini. Postupak se takodje odnosi na novi N-{3-[3-( dimetilamino )-1-okso-2-propenil]fenil}- N-etil- acetamid hidrohlorid formule (II). Osim toga postupak se odnosi na sintezu novog N-{3-[3(dimetilamino )-1-okso-2-propenil]fenil }-N-etil- acetamid .hidrohlorida formule (II) koji ima čistoću veću od 99.5%. Dalje se pronalazak odnosi na N-{3-[3-cijanopirazolo (l,5-a) pirimidin]-6-il-3-[(3-N-etil-acetamido-fenil)- 3- okso- propen-l- il]- (pirimidin- 7- il)- fenil}N- etil- acetamid formule (V), koji je izolovan kao nova primesa u količini od 0,07% u toku sinteze jedinjenja formule (IV).

5. 发明专利

HU221922B1 PROCESS FOR PRODUCING PAROXETIN SALTS AND THEIR HYDRATES 未知
公开(公告)号：HU221922B1
公开(公告)日：2003-02-28
申请号：HU9601858
申请日：1996-07-08
申请人： RICHTER GEDEON VEGYESZET
发明人： KREIDL JANOS DR , CZIBULA LASZLO DR , NEMES ANDRAS DR , HARSANYI KALMAN DR , DEUTSCHNE JUHASZ IDA DR , CSUTORAS LASZLO DR , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , BORZA ISTVAN , HEGEDUES ISTVAN
IPC分类号： C07D405/12

6. 发明专利

DE69709938T2 未知
公开(公告)号：DE69709938T2
公开(公告)日：2002-08-29
申请号：DE69709938
申请日：1997-07-07
申请人： RICHTER GEDEON VEGYESZET
发明人： KREIDL JANOS , CZIBULA LASZLO , NEMES ANDRAS , DEUTSCHNE JUHASZ IDA , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , DOBAY LASZLO , HEGEDUES ISTVAN , HARSANYI KALMAN , BORZA ISTVAN
IPC分类号： C07D211/22 , C07D211/70 , C07D405/12 , C07D211/30 , C07D211/18
摘要： A process is disclosed for the preparation of compounds of the formula (I),which compounds are useful as intermediates for the preparation of paroxetine of formula(V).

7. 发明专利

HU0001414A2 NEW PAROXETIN SALT AND MEDICAMENT CONTAINING IT 未知
公开(公告)号：HU0001414A2
公开(公告)日：2002-05-29
申请号：HU0001414
申请日：2000-04-07
申请人： RICHTER GEDEON VEGYESZET
发明人： DR CZIBULA LASZLO , DR NEMES ANDRAS , DR KREIDL JANOS , DR BALINT SANDORNE , DR DEUTSCHNE JUHASZ IDA , DOBAY LASZLO , NAGYNE BAGDY JUDIT , WERKNE PAPP EVA , HEGEDUES ISTVAN , SEBOEK FERENC , TERDY LASZLO
IPC分类号： C07D405/12

8. 发明专利

AT211732T 未知
公开(公告)号：AT211732T
公开(公告)日：2002-01-15
申请号：AT97932953
申请日：1997-07-07
申请人： RICHTER GEDEON VEGYESZET
发明人： KREIDL JANOS , CZIBULA LASZLO , NEMES ANDRAS , DEUTSCHNE JUHASZ IDA , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , DOBAY LASZLO , HEGEDUES ISTVAN , HARSANYI KALMAN , BORZA ISTVAN
IPC分类号： C07D211/22 , C07D211/70 , C07D405/12 , C07D211/30 , C07D211/18
摘要： A process is disclosed for the preparation of compounds of the formula (I),which compounds are useful as intermediates for the preparation of paroxetine of formula(V).

9. 发明专利

HU0400270A2 HIGH PURITY BUTOCONAZOLE NITRATE HAVING A PREDETERMINED PARTICLE SIZE AND PROCESS FOR THE PRODUCTION OF THE SAME 未知
公开(公告)号：HU0400270A2
公开(公告)日：2005-12-28
申请号：HU0400270
申请日：2004-01-27
申请人： RICHTER GEDEON VEGYESZET
发明人： CZIBULA LASZLO DR , DOBAY LASZLO , WERKNE PAPP EVA , NAGYNE BAGDY JUDIT , SEBOK FERENC
IPC分类号： C07D233/54 , C07D233/60
摘要： One object of the invention is high purity butoconazole nitrate of the formula (I) (chemical name: 1-[4-(4-chlorophenyl)-2-(2,6-dichlorophenylthio)-n-butyl]-imidazole nitrate) containing maximum 0.1 wt % of chemical impurities, wherein at last 95 % of the particles of the substance are below 75 µm by diameter, whereas at least 99 % of the particles are below 250 µm by diameter. Another object of the invention is a process for the preparation of butoconazole nitrate starting from 1-chloro-4-chlorophenyl-2-butanol and imidazole to yield a compound of the formula (IV), reacting said compound of formula (IV) with thionyl chloride to give a compound of the formula (V) and reacting the obtained compound of the formula (V) with 2,6-dichlorothiophenol, performing said reaction steps in such a manner that the first step is carried out in a mixture of a water immiscible solvent and an aqueous solution of an alkali metal hydroxide or carbonate in the presence a phase transfer catalyst; the second step is accomplished in 1,2-dichloroethane solvent in the presence of dimethylformamide, whereas 1-1.2 mol of thionyl chloride reactant is used based on the amount of the compound of the formula (IV); and the third steps is performed without isolation of the product (VI) from the solution obtained, but to said solution nitric acid is added to give the butoconazole nitrate salt. Still another object of the invention is a process for the preparation of the compound with the above specified particle size starting from crude butoconazole nitrate in such a manner that the starting material is dissolved in a mixture of methanol and methyl isobutyl ketone of 1 - 1.5 : 1 ratio (v/v), this solution is then added to methyl isobutyl ketone cooled to a temperature between 5 °C and -15 °C and the product obtained is isolated. A pharmaceutical composition comprising as active ingredient high purity butoconazole nitrate of specified particle size in admixture with known auxiliaries is also within the scope of the invention.

10. 发明专利

AT309226T 未知
公开(公告)号：AT309226T
公开(公告)日：2005-11-15
申请号：AT01921683
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

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