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    PIPERAZINE SALT AND A PROCESS FOR THE PREPARATION THEREOF
    1.
    发明申请
    PIPERAZINE SALT AND A PROCESS FOR THE PREPARATION THEREOF 审中-公开
    哌嗪盐及其制备方法

    公开(公告)号：WO2010070369A1

    公开(公告)日：2010-06-24

    申请号：PCT/HU2009/000108

    申请日：2009-12-17

    申请人： RICHTER GEDEON NYRT. ,  CZIBULA, Lászl ,  AGAINE CSONGOR, Eva ,  NOGRADI, Katalin ,  JUHASZ, Bálint ,  SEBOK, Ferenc ,  GALAMBOS, János ,  VAGO, István

    发明人： CZIBULA, Lászl ,  AGAINE CSONGOR, Eva ,  NOGRADI, Katalin ,  JUHASZ, Bálint ,  SEBOK, Ferenc ,  GALAMBOS, János ,  VAGO, István

    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-l-il]-ethyl}- cyclohexylamine dihydrochloride monohydrate and a process for the preparation of the trans N- {4- {2-[4-(2,3-dichlorophenyl)-piperazine-l -il]-ethyl}-cyclohexylamine dihydrochloride monohydrate, said process comprising the steps a) reacting trans 2-{l-[4-(N-tert-butoxycarbonyl)amino]- cyclohexyl} -acetic acid ester with sodium borohydride and aluminium trichloride to give trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethanol; b) reacting trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]cyclohexyl}-ethanol obtained with methanesulfonic acid chloride in the presence of an acid binding agent to give trans 2-{l-[4- (N-tert-butoxycarbonyl)-amino] -cyclohexyl} -ethyl methanesulfonate; c) reacting trans 2-{l-[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-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert-butylester; d) heating trans 2-{l-[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-l-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，以及制备反式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，所述方法包括步骤a）使反式-2- {1- [4-（N- 叔丁氧基羰基）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）将获得的反式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-叔丁氧羰基） - 氨基] - 环己基} - 氨基甲酸叔丁酯加热至40-100℃的温度，在盐酸/甲醇水溶液 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。

    PROCESS FOR THE PREPARATION OF PIPERAZINE DERIVATIVES
    4.
    发明申请
    PROCESS FOR THE PREPARATION OF PIPERAZINE DERIVATIVES 审中-公开
    制备哌嗪衍生物的方法

    公开(公告)号：WO2010070371A1

    公开(公告)日：2010-06-24

    申请号：PCT/HU2009/000110

    申请日：2009-12-18

    申请人： RICHTER GEDEON NYRT. ,  ÁGAINÉ CSONGOR, Éva ,  CZIBULE, László ,  SEBÖK, Ferenc ,  JUHÁSZ, Bálint ,  GALAMBOS, János ,  NÓGRÁDI, Katalin

    发明人： ÁGAINÉ CSONGOR, Éva ,  CZIBULE, László ,  SEBÖK, Ferenc ,  JUHÁSZ, Bálint ,  GALAMBOS, János ,  NÓGRÁDI, Katalin

    IPC分类号： C07D295/135

    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 formula (I) by reacting the compound of formula (III) with a carbamoylchloride of 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： 本发明涉及制备式（I）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 ）通过使式（III）的化合物与式（II）的氨基甲酰氯反应，其包括在存在下在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 的相转移催化剂，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，直到其重量恒定。

    PROCESS FOR THE PREPARATION OF AN ANTIPSORIATIC PHARMACEUTICAL COMPOSITION
    7.
    发明申请
    PROCESS FOR THE PREPARATION OF AN ANTIPSORIATIC PHARMACEUTICAL COMPOSITION 审中-公开
    制备抗药性药物组合物的方法

    公开(公告)号：WO1988009662A1

    公开(公告)日：1988-12-15

    申请号：PCT/HU1988000042

    申请日：1988-06-10

    申请人： RICHTER GEDEON VEGYÉSZETI GYAR RT. ,  KEVE, Tibor ,  SZPORNY, László ,  KIRALY, Arpád ,  FEKETE, György ,  FORGACS, Lilla ,  STEFKO, Béla ,  ZSADON, Béla ,  GALAMBOS, János ,  BALAZSNÉ ZAYER, Mária ,  Hangay, György ,  KELEN, András ,  BUKOVECZNÉ BARTA, Margit ,  KARPATI, Egon ,  KISS, Béla ,  SOS, Gyöngyvér

    发明人： RICHTER GEDEON VEGYÉSZETI GYAR RT.

    IPC分类号： A61K31/475

    CPC分类号： A61K31/475 ,  A61K9/0014 ,  A61K47/10 ,  A61K47/12

    摘要： The invention relates to a process for the preparation of an antipsoriatic pharmaceutical composition containing 17,18-dehydroapovincaminol 3',4',5'-trimethoxybenzoate or its pharmaceutically acceptable acid addition salts, which comprises dissolving one equivalent of 17,18-dehydroapovincaminol 3',4',5'-trimethoxybenzoate or its pharmaceutically acceptable acid addition salt in 1.1 to 50, preferably 5 to 20, equivalents of an organic acid containing no basic group and being soluble in water or in a water-miscible monovalent or polyvalent alcohol or in a mixture thereof, or in a solution prepared from the organic acid with water or with a water-miscible monovalent or polyvalent alcohol or with a mixture thereof, and a) formulating the solution to a pharmaceutical composition as such or, if desired, together with therapeutically active agents showing no synergism with the active ingredient and/or with pharmaceutical auxiliary materials (additives), or b) diluting the solution with 5 to 50 parts by weight of water and formulating the thus-obtained gel, containing the active ingredient in a homogenous molecular distribution, as such or together with therapeutically active agents showing no synergism with the active ingredient and/or with a pharmaceutically acceptable auxiliary materials to a pharmaceutical composition.

    摘要翻译： 本发明涉及一种制备含有17,18-脱氢氨铂醇3'，4'，5'-三甲氧基苯甲酸酯或其药学上可接受的酸加成盐的抗牛皮癣药物组合物的方法，其包括将1当量的17,18-脱氢氨基嘌呤醇3 '，4'，5'-三甲氧基苯甲酸酯或其药学上可接受的酸加成盐在1.1至50，优选5至20当量的不含碱性基团的有机酸中并且可溶于水或水溶性单价或多价醇 或以其混合物，或由有机酸与水或与水混溶的单价或多价醇或其混合物制备的溶液，以及a）将溶液配制成药物组合物，或如果需要， 以及与活性成分和/或与药物辅助材料（添加剂）无协同作用的治疗活性剂，或b）用5至5 将0重量份的水配制成如此获得的含有均匀分子分布的活性成分的凝胶，或与治疗活性成分一起显示与活性成分和/或药学上可接受的辅助材料与 药物组成。

    NOVEL PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF
    8.
    发明申请
    NOVEL PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF 审中-公开
    制备哌嗪化合物及其盐酸盐的新工艺

    公开(公告)号：WO2011073705A1

    公开(公告)日：2011-06-23

    申请号：PCT/HU2010/000144

    申请日：2010-12-17

    申请人： RICHTER GEDEON NYRT. ,  CZIBULA, Lászlό ,  JUHÁSZ, Bálint ,  ÁGAINÉ CSONGOR, Éva ,  SEBŐK, Ferenc ,  GALAMBOS, János ,  NÓGRÁDI, Katalin

    发明人： CZIBULA, Lászlό ,  JUHÁSZ, Bálint ,  ÁGAINÉ CSONGOR, Éva ,  SEBŐK, Ferenc ,  GALAMBOS, János ,  NÓGRÁDI, Katalin

    IPC分类号： C07D295/135

    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 R 1 and R 2 represent independently hydrogen or C 1-6 alkyl with straight or branched chain optionally substituted with aryl group; or C 2-7 alkenyl containing 1-3 double bonds; or monocyclic, bicyclic or tricyclic aryl optionally substituted with one or more C1-6 alkoxy, trifiuoro-C 1-6 alkoxy, C 1-6 -alkoxycarbonil, C 1-6 alkanoyl, aryl, C 1-6 alkylthio, halogen or cyano; or optionally substituted monocyclic, bicyclic or tricyclic C 3-14 cycloalkyl group; R 1 and R 2 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 salts 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 of a base then adding a carbonic acid derivative of general formula (VI) wherein R is alkyl with C 1-6 straight or branched chain, partially or fully halogenated C 1-2 alkyl or phenyl, 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 R 1 and R 2 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）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直链或支链的C 1-6烷基; 或含有1-3个双键的C2-7烯基; 或任选被一个或多个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; R1和R2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/或其水合物和/或溶剂合物，通过溶解 或将式（III）的反式4- {2- [4-（2,3-二氯苯基） - 哌嗪-1-基] - 乙基} - 环己胺或其盐或其水合物或溶剂合物悬浮在惰性溶剂中 碱的存在然后加入通式（VI）的碳酸衍生物，其中R是具有C 1-6直链或支链，部分或完全卤代的C 1-2烷基或苯基的烷基，Z是-OR或-X，其中 R是如上所述，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R 2是 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/或溶剂合物。