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1. 发明申请

US20110275816A1 PIPERAZINE SALT AND A PROCESS FOR THE PREPARATION THEREOF 有权
标题翻译：哌嗪盐及其制备方法
公开(公告)号：US20110275816A1
公开(公告)日：2011-11-10
申请号：US13140232
申请日：2009-12-17
申请人： Laszlo Czibula , Eva Againe Csongor , Katalin Nogradi , Balint Juhasz , Ferenc Sebok , Janos Galambos , Istvan Vago
发明人： Laszlo Czibula , Eva Againe Csongor , Katalin Nogradi , Balint Juhasz , Ferenc Sebok , Janos Galambos , Istvan Vago
IPC分类号： C07D241/04
CPC分类号： C07D295/135
摘要： The invention relates to novel trans N-{4-{2-[4-(2, 3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate and a process for the preparation of the trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate, said process comprising the steps a) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl) amino]-cyclohexyl}-acetic acid ester with sodium borohydride and aluminium trichloride to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethanol; b) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]cyclohexyl}-ethanol obtained with methanesulfonic acid chloride in the presence of an acid binding agent to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate; c) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate obtained with 2,3-dichlorophenyl-piperazine in the presence of an acid binding agent to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert-butylester; d) heating trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert-butylester obtained to a temperature between 40-100° C. in a mixture of aqueous hydrochloric acid/methanol to give trans N-{4-{2-[4-(2,3-dichlorophenyl) piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate.
摘要翻译：本发明涉及新的反式N- {4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} - 环己胺二盐酸盐一水合物及其制备方法， 4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} - 环己胺二盐酸盐一水合物，所述方法包括步骤a）使反式2- {1- [4-（N- 叔丁氧羰基）氨基] - 环己基} - 乙酸酯与硼氢化钠和三氯化铝反应，得到反式2- {1- [4-（N-叔丁氧基羰基） - 氨基] - 环己基} - 乙醇; b）使得到的反式2- {1- [4-（N-叔丁氧基羰基） - 氨基]环己基} - 乙醇与甲磺酰氯在酸结合剂存在下反应，得到反式-2- {1- [4- （N-叔丁氧基羰基） - 氨基] - 环己基} - 乙基甲磺酸酯; c）在酸结合剂的存在下，使得到的与2,3-二氯苯基哌嗪的反式2- {1- [4-（N-叔丁氧基羰基） - 氨基] - 环己基} - 乙基甲基磺酸酯反应，得到反式-2- {1- [4-（N-叔丁氧基羰基） - 氨基] - 环己基} - 氨基甲酸叔丁酯; d）将得到的反式2- {1- [4-（N-叔丁氧基羰基） - 氨基] - 环己基} - 氨基甲酸叔丁基酯加热至40-100℃的温度，在盐酸/ 得到反式N- {4- {2- [4-（2,3-二氯苯基）哌嗪-1-基] - 乙基} - 环己胺二盐酸盐一水合物。

2. 发明申请

US20110275804A1 PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF 有权
标题翻译：哌嗪化合物的制备方法及其盐酸盐的制备方法
公开(公告)号：US20110275804A1
公开(公告)日：2011-11-10
申请号：US13140281
申请日：2009-12-18
申请人： Laszlo Czibula , Balint Juhasz , Eva Againe Csongor , Ferenc Sebok , Janos Galambos , Katalin Nogradi
发明人： Laszlo Czibula , Balint Juhasz , Eva Againe Csongor , Ferenc Sebok , Janos Galambos , Katalin Nogradi
IPC分类号： C07D413/12 , C07D241/02
CPC分类号： C07D295/135
摘要： The invention relates to a new process for the preparation of compounds of general formula (I) wherein R1 and R2 represent independently hydrogen or C1-6 alkyl with straight or branched chain optionally substituted with aryl group, or C2-7 alkenyl containing 1-3 double bonds, or monocyclic, bicyclic or tricyclic aryl optionally substituted with one or more C1-6 alkoxy, trifluoro-C1-6 alkoxy, C1-6-alkoxycarbonil, C1-6alkanoyl, aryl, C1-6 alkylthio, halogen or cyano, or optionally substituted monocyclic, bicyclic or tricyclic C3-14 cycloalkyl group, R1 and R2 together with the adjacent nitrogen form a saturated or unsaturated optionally substituted monocyclic or bicyclic heterocyclic ring which may contain further heteroatoms selected from oxygen, nitrogen, or sulphur atoms and hydrochloric acid alts and/or hydrates and/or solvates thereof, by dissolving or suspending trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine of formula (III) or a salt or a hydrate or a solvate thereof in an inert solvent in the presence a base then adding a carbonic acid derivative of general formula (VI) wherein R is alkyl with C 1-6 straight or branched chain or C1-2 fully halogenated alkyl, Z is —O—R or —X, wherein R is as described above, X is halogen, and reacting the compound of general formula (IV) obtained wherein R is as described above, in situ or, optionally in isolated state with an amine of general formula (V) wherein R1 and R2 are as described above to obtain the compound of general formula (I) and then optionally forming the hydrochloride salts and/or hydrates and/or solvates thereof.
摘要翻译：本发明涉及制备通式（I）的化合物的新方法，其中R 1和R 2独立地表示氢或任选被芳基取代的具有直链或支链的C 1-6烷基，或含有1-3个任选被一个或多个C 1-6烷氧基，三氟-C 1-6烷氧基，C 1-6 - 烷氧羰基，C 1-6烷酰基，芳基，C 1-6烷硫基，卤素或氰基取代的单环，双环或三环芳基，或任选取代的单环，双环或三环C 3-14环烷基，R 1和R 2与相邻的氮一起形成饱和或不饱和的任选取代的单环或双环杂环，其可以含有选自氧，氮或硫原子的其它杂原子和盐酸盐和/或水合物和/或溶剂化物，通过溶解或悬浮式（III）的反式4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} - 环己胺或盐或水合物或在惰性溶剂中，在碱的存在下，然后加入通式（VI）的碳酸衍生物，其中R是具有C 1-6直链或支链或C 1-2完全卤代烷基的烷基，Z是-O-R 或-X，其中R如上所述，X是卤素，并使得到的其中R如上所述获得的通式（IV）的化合物原位或任选地在分离状态下与通式（V）的胺反应，其中R1和R2如上所述，以获得通式（I）的化合物，然后任选地形成其盐酸盐和/或水合物和/或溶剂合物。

3. 发明授权

US08569497B2 Process for the preparation of piperazine derivatives 有权
标题翻译：哌嗪衍生物的制备方法
公开(公告)号：US08569497B2
公开(公告)日：2013-10-29
申请号：US13140261
申请日：2009-12-18
申请人： Eva Againe Csongor , Laszlo Czibula , Ferenc Sebok , Balint Juhasz , Janos Galambos , Katalin Nogradi
发明人： Eva Againe Csongor , Laszlo Czibula , Ferenc Sebok , Balint Juhasz , Janos Galambos , Katalin Nogradi
IPC分类号： C07D295/135 , C07D295/14
CPC分类号： C07D295/135
摘要： The invention relates to a process for the preparation of the trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-cyclohexyl}-carbamide derivatives of general formula (I) by reacting the compound of formula (III) with a carbamoylchloride of general formula (II) which comprises carrying out the reaction in a mixture of a solvent and concentrated aqueous solution of an alkali hydroxide at a temperature between 40-100° C. in the presence of a phase transfer catalyst, separating the phases and washing the organic layer then removing the solvent and drying the compound of formula (I) obtained until its weight is constant.
摘要翻译：本发明涉及制备通式（II）的反式N- {4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} - 环己基} - 氨基甲酰胺衍生物的方法 I）化合物与通式（II）的氨基甲酰氯反应，该方法包括在40-100℃的温度下在溶剂和浓氢氧化碱水溶液的混合物中进行反应在相转移催化剂的存在下，分离相并洗涤有机层，然后除去溶剂并干燥获得的式（I）化合物直到其重量不变。

4. 发明申请

US20110269959A1 PROCESS FOR THE PREPARATION OF PIPERAZINE DERIVATIVES 有权
标题翻译：制备哌嗪衍生物的方法
公开(公告)号：US20110269959A1
公开(公告)日：2011-11-03
申请号：US13140261
申请日：2009-12-18
申请人： Eva Againe Csongor , Laszlo Czibula , Ferenc Sebok , Balint Juhasz , Janos Galambos , Katalin Nogradi
发明人： Eva Againe Csongor , Laszlo Czibula , Ferenc Sebok , Balint Juhasz , Janos Galambos , Katalin Nogradi
IPC分类号： C07D413/08 , C07D241/04
CPC分类号： C07D295/135
摘要： The invention relates to a process for the preparation of the trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-cyclohexyl}-carbamide derivatives of general formula (I) by reacting the compound of formula (III) with a carbamoylchloride of general formula (II) which comprises carrying out the reaction in a mixture of a solvent and concentrated aqueous solution of an alkali hydroxide at a temperature between 40-100° C. in the presence of a phase transfer catalyst, separating the phases and washing the organic layer then removing the solvent and drying the compound of formula (I) obtained until its weight is constant.
摘要翻译：本发明涉及制备通式（II）的反式N- {4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} - 环己基} - 氨基甲酰胺衍生物的方法 I）化合物与通式（II）的氨基甲酰氯反应，该方法包括在40-100℃的温度下在溶剂和浓氢氧化碱水溶液的混合物中进行反应在相转移催化剂的存在下，分离相并洗涤有机层，然后除去溶剂并干燥获得的式（I）化合物直到其重量不变。

5. 发明授权

US08569498B2 Process for the preparation of piperazine compounds and hydrochloride salts thereof 有权
标题翻译：制备哌嗪化合物及其盐酸盐的方法
公开(公告)号：US08569498B2
公开(公告)日：2013-10-29
申请号：US13140281
申请日：2009-12-18
申请人： Laszlo Czibula , Balint Juhasz , Eva Againe Csongor , Ferenc Sebok , Janos Galambos , Katalin Nogradi
发明人： Laszlo Czibula , Balint Juhasz , Eva Againe Csongor , Ferenc Sebok , Janos Galambos , Katalin Nogradi
IPC分类号： C07D295/135 , C07D295/14
CPC分类号： C07D295/135
摘要： The invention relates to a new process for the preparation of compounds of general formula (I) whereinR1 and R2 represent independently hydrogen or C1-6 alkyl with straight or branched chain optionally substituted with aryl group, or C2-7 alkenyl containing 1-3 double bonds, or monocyclic, bicyclic or tricyclic aryl optionally substituted with one or more C1-6 alkoxy, trifluoro-C1-6 alkoxy, C1-6-alkoxycarbonil, C1-6alkanoyl, aryl, C1-6 alkylthio, halogen or cyano, or optionally substituted monocyclic, bicyclic or tricyclic C3-14 cycloalkyl group, R1 and R2 together with the adjacent nitrogen form a saturated or unsaturated optionally substituted monocyclic or bicyclic heterocyclic ring which may contain further heteroatoms selected from oxygen, nitrogen, or sulphur atoms and hydrochloric acid alts and/or hydrates and/or solvates thereof, by dissolving or suspending trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine of formula (III) or a salt or a hydrate or a solvate thereof in an inert solvent in the presence a base then adding a carbonic acid derivative of general formula (VI) wherein R is alkyl with C1-6 straight or branched chain or C1-2 fully halogenated alkyl, Z is —O—R or —X, wherein R is as described above, X is halogen, and reacting the compound of general formula (IV) obtained wherein R is as described above, in situ or, optionally in isolated state with an amine of general formula (V) wherein R1 and R2 are as described above to obtain the compound of general formula (I) and then optionally forming the hydrochloride salts and/or hydrates and/or solvates thereof.
摘要翻译：本发明涉及一种制备通式（I）化合物的新方法，其中R 1和R 2独立地表示氢或任选被芳基取代的具有直链或支链的C 1-6烷基，或含有1-3个任选被一个或多个C 1-6烷氧基，三氟-C 1-6烷氧基，C 1-6 - 烷氧羰基，C 1-6烷酰基，芳基，C 1-6烷硫基，卤素或氰基取代的单环，双环或三环芳基，或任选取代的单环，双环或三环C 3-14环烷基，R 1和R 2与相邻的氮一起形成饱和或不饱和的任选取代的单环或双环杂环，其可以含有选自氧，氮或硫原子的其它杂原子和盐酸盐和/或水合物和/或溶剂化物，通过溶解或悬浮式（III）的反式4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} - 环己胺或盐或水合物或在惰性溶剂中，在碱的存在下加入通式（VI）的碳酸衍生物，其中R为烷基，C 1-6直链或支链或C 1-2完全卤代烷基，Z为-OR或-X 其中R如上所述，X是卤素，并且其中R如上所述获得的通式（IV）化合物原位或任选地在分离状态下与通式（Ⅴ）的胺反应，其中R 1和 R2如上所述，得到通式（I）的化合物，然后任选地形成盐酸盐和/或其水合物和/或溶剂化物。

6. 发明授权

US08569496B2 Piperazine salt and a process for the preparation thereof 有权
标题翻译：哌嗪盐及其制备方法
公开(公告)号：US08569496B2
公开(公告)日：2013-10-29
申请号：US13140232
申请日：2009-12-17
申请人： Laszlo Czibula , Eva Againe Csongor , Katalin Nogradi , Balint Juhasz , Ferenc Sebok , Janos Galambos , Istvan Vago
发明人： Laszlo Czibula , Eva Againe Csongor , Katalin Nogradi , Balint Juhasz , Ferenc Sebok , Janos Galambos , Istvan Vago
IPC分类号： C07D295/135
CPC分类号： C07D295/135
摘要： The invention relates to novel trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate and a process for the preparation of the trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate, said process comprising the stepsa) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)amino]-cyclohexyl}-acetic acid ester with sodium borohydride and aluminum trichloride to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethanol;b) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]cyclohexyl}-ethanol obtained with methanesulfonic acid chloride in the presence of an acid binding agent to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate;c) reacting trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate obtained with 2,3-dichlorophenyl-piperazine in the presence of an acid binding agent to give trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert-butylester; d) heating trans 2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert-butylester obtained to a temperature between 40-100° C. in a mixture of aqueous hydrochloric acid/methanol to give trans N-{4-{2-[4-(2,3-dichlorophenyl)piperazine-1-il]-ethyl}-cyclohexylamine dihydrochloride monohydrate.
摘要翻译：本发明涉及新的反式N- {4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} - 环己胺二盐酸盐一水合物及其制备方法， 4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} - 环己胺二盐酸盐一水合物，所述方法包括步骤a）使反式2- {1- [4-（N- 叔丁氧羰基）氨基] - 环己基} - 乙酸酯与硼氢化钠和三氯化铝反应，得到反式2- {1- [4-（N-叔丁氧基羰基） - 氨基] - 环己基} - 乙醇; b）使得到的反式2- {1- [4-（N-叔丁氧基羰基） - 氨基]环己基} - 乙醇与甲磺酰氯在酸结合剂存在下反应，得到反式-2- {1- [4- （N-叔丁氧基羰基） - 氨基] - 环己基} - 乙基甲磺酸酯; c）在酸结合剂的存在下，使得到的与2,3-二氯苯基哌嗪的反式2- {1- [4-（N-叔丁氧基羰基） - 氨基] - 环己基} - 乙基甲基磺酸酯反应，得到反式-2- {1- [4-（N-叔丁氧基羰基） - 氨基] - 环己基} - 氨基甲酸叔丁酯; d）将得到的反式2- {1- [4-（N-叔丁氧基羰基） - 氨基] - 环己基} - 氨基甲酸叔丁基酯加热至40-100℃的温度，在盐酸/ 得到反式N- {4- {2- [4-（2,3-二氯苯基）哌嗪-1-基] - 乙基} - 环己胺二盐酸盐一水合物。

7. 发明授权

US07943621B2 Salts of piperazine compounds as D3/D2 antagonists 有权
标题翻译：哌嗪化合物的盐作为D3 / D2拮抗剂
公开(公告)号：US07943621B2
公开(公告)日：2011-05-17
申请号：US12118437
申请日：2008-05-09
申请人： Laszlo Czibula , Ferenc Sebok , Istvan Greiner , Gyorgy Domany , Eva Againe Csongor
发明人： Laszlo Czibula , Ferenc Sebok , Istvan Greiner , Gyorgy Domany , Eva Againe Csongor
IPC分类号： A61K31/497 , C07D295/00
CPC分类号： C07D241/04
摘要： The present invention relates to novel monohydrochloride, dihydrochloride, monohydrobromide, maleate and methanesulphonate salts of trans 4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-N,N-dimethylcarbamoyl-cyclohexylamine and/or their hydrates and/or solvates. Moreover, the invention relates to the process for preparing the salts and their hydrates and/or solvates, to their use in the treatment and/or prevention of conditions which require modulation of dopamine receptor and to pharmaceutical compositions containing them.
摘要翻译：本发明涉及反式4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} -N，N-二甲基氨基甲酰基 - （C 1 -C 6）烷基的新的一盐酸盐，二盐酸盐，一氢溴酸盐，马来酸盐和甲磺酸盐，环己胺和/或其水合物和/或溶剂合物。此外，本发明涉及制备盐及其水合物和/或溶剂合物的方法，用于治疗和/或预防需要调节多巴胺受体的病症和含有它们的药物组合物。

8. 发明申请

US20090270630A1 PROCESS FOR THE SYNTHESIS OF BENZYLIDENE ROSIGLITAZONE BASE 审中-公开
标题翻译：苯并噻唑基合成方法
公开(公告)号：US20090270630A1
公开(公告)日：2009-10-29
申请号：US12302127
申请日：2007-06-21
申请人： Laszlo Czibula , Ferenc Sebok , Laszlo Dobay , Eva Werkne Papp , Ida Deutschne Juhasz , Judit Nagyne Bagdy , Tamasne Uberhardt
发明人： Laszlo Czibula , Ferenc Sebok , Laszlo Dobay , Eva Werkne Papp , Ida Deutschne Juhasz , Judit Nagyne Bagdy , Tamasne Uberhardt
IPC分类号： C07D417/12
CPC分类号： C07D417/12
摘要： Process for the synthesis of 5-{4-[N-methyl-N-(2-pyridyl)-amino-ethoxy]-benzylidene}-thiazolidine-2,4-dione (INN name: benzylidene-rosiglitazone) of formula (I), which consist of the following steps: Step a) reaction of 2-chloro-pyridine and 2-(N-methylamino)-ethanol Step b) reaction of the obtained compound of formula (III) with 4-fluorobenzaldehyde Step c) reaction of the obtained compound of formula (IV) with thiazolidine-2,4-dione characterized by dissolving 4-{2-[N-methyl-N-(2-pyridyl)amino]-ethanol of formula (III) obtained in Step a) in toluene and using it in Step b) without isolation; reacting the solution of compound of formula (III) in toluene in Step b) with 4-fluorobenzaldehyde in the presence of aqueous alkali hydroxide solution and phase transfer catalyst at 25-50° C.; reacting the solution of the benzaldehyde derivative of formula (IV) obtained in Step b) in toluene in Step c) and isolating the desired product.
摘要翻译：合成式（I）的5- {4- [N-甲基-N-（2-吡啶基） - 氨基 - 乙氧基] - 亚苄基} - 噻唑烷-2,4-二酮（INN名称：亚苄基 - 罗格列酮）），其步骤如下：步骤a）2-氯 - 吡啶和2-（N-甲基氨基） - 乙醇的反应步骤b）将所得到的式（III）化合物与4-氟苯甲醛反应步骤c）反应所得到的式（Ⅳ）化合物与噻唑烷-2,4-二酮的特征在于将步骤a中获得的式（Ⅳ）的4- {2- [N-甲基-N-（2-吡啶基）氨基] - 乙醇）并在步骤b）中使用它而不分离; 使步骤b）中式（III）化合物在甲苯中的溶液与4-氟苯甲醛在碱金属氢氧化物水溶液和相转移催化剂存在下，在25-50℃下反应。使步骤b）中获得的式（IV）的苯甲醛衍生物在步骤c）中的甲苯中的溶液反应，并分离所需产物。

9. 发明授权

US5352790A Process for the preparation of 1.beta.-ethyl-1.alpha.-(hydroxymethyl)-1,2,3,4,6,7,12,12B.alpha.-octahyd ro-indolo[2,3,-A]quinolizine and novel intermediates 失效
标题翻译：制备1β-乙基-1α-（羟甲基）-1,2,3,4,6,7,12,12Bα-八氢 - 吲哚并[2,3-a]喹嗪和新型中间体的方法
公开(公告)号：US5352790A
公开(公告)日：1994-10-04
申请号：US877172
申请日：1992-06-25
申请人： Janos Kreidl , Laszlo Czibula , Gyorgy Visky , Maria F. nee Kirjak , Ida D. nee Juhasz , Judit Brill, deceased , Katalin Nogradi
发明人： Janos Kreidl , Laszlo Czibula , Gyorgy Visky , Maria F. nee Kirjak , Ida D. nee Juhasz , Judit Brill, deceased , Katalin Nogradi
IPC分类号： A61K31/435 , C07D471/14 , C07D459/00
CPC分类号： C07D471/14
摘要： The invention relates to a novel process for the preparation of (-) -1.beta.-ethyl-1.alpha.-(hydroxymethyl) - 1,2,3,4,6,7,12,12b.alpha.-octahydro-indolo[2,3-a]quinolizine of the formula (I) ##STR1## and to novel intermediates obtained in this process. The compound of the formula (I) prepared by the process of the invention possesses a peripheral vasodilator effect.
摘要翻译： PCT No.PCT / HU91 / 00046 Sec。 371日期：1992年6月25日 102（e）日期1992年6月25日PCT 1991年10月30日PCT PCT。公开号WO92 / 07851 本发明涉及一种制备（ - ）-1β-乙基-1α-（羟甲基）-1,2,3,4,6,7,12,12bα- 式（I）的八氢 - 吲哚并[2,3-a]喹嗪和（I）得到的新的中间体。通过本发明方法制备的式（I）化合物具有外周血管扩张作用。

10. 发明授权

US07625935B2 High purity butoconazole nitrate with specified particle size and a process for the preparation thereof 有权
标题翻译：具有规定粒径的高纯度布康康硝酸盐及其制备方法
公开(公告)号：US07625935B2
公开(公告)日：2009-12-01
申请号：US10584662
申请日：2005-01-25
申请人： Laszlo Czibula , Laszlo Dobay , Eva Werkne Papp , Judit Nagyne Bagdy , Ferenc Sebok
发明人： Laszlo Czibula , Laszlo Dobay , Eva Werkne Papp , Judit Nagyne Bagdy , Ferenc Sebok
IPC分类号： A61K31/4174 , C07D233/56
CPC分类号： C07D233/60
摘要： One object of the invention is high purity butoconazole nitrate of the formula (I) (I) containing maximum 0.1 wt % of chemical impurities, wherein at least 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, and process for its preparation. 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.
摘要翻译：本发明的一个目的是含有最多0.1重量％化学杂质的式（I）（I）的高纯度布康唑硝酸盐，其中物质的至少95％的颗粒直径小于75μm，而至少99 颗粒的百分比直径小于250毫米，其制备方法。包含与已知助剂混合的具有特定粒度的高纯度丁苯康唑硝酸盐作为活性成分的药物组合物也在本发明的范围内。

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