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    PIPERAZINE SALT AND A PROCESS FOR THE PREPARATION THEREOF
    3.
    发明申请
    PIPERAZINE SALT AND A PROCESS FOR THE PREPARATION THEREOF 有权
    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。

    PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF
    4.
    发明申请
    PROCESS FOR THE PREPARATION OF PIPERAZINE COMPOUNDS AND HYDROCHLORIDE SALTS THEREOF 有权
    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。

    Process for the preparation of piperazine compounds and hydrochloride salts thereof
    5.
    发明授权
    Process for the preparation of piperazine compounds and hydrochloride salts thereof 有权
    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。

    Process for the preparation of piperazine derivatives
    6.
    发明授权
    Process for the preparation of piperazine derivatives 有权
    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。

    PROCESS FOR THE PREPARATION OF PIPERAZINE DERIVATIVES
    7.
    发明申请
    PROCESS FOR THE PREPARATION OF PIPERAZINE DERIVATIVES 有权
    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。

    Piperazine salt and a process for the preparation thereof
    8.
    发明授权
    Piperazine salt and a process for the preparation thereof 有权
    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。

    COMPOUNDS
    10.
    发明申请
    COMPOUNDS 审中-公开
    化合物

    公开(公告)号：US20100022521A1

    公开(公告)日：2010-01-28

    申请号：US12158568

    申请日：2006-12-19

    申请人： Katalin Nogradi ,  Gabor Wagner ,  Gyorgy Keseru ,  Attila Bielik ,  Tamas Gati ,  Viktor Hada ,  Janos Koti ,  Krisztina Gal ,  Monika Vastag ,  Amrita Agnes Bobok

    发明人： Katalin Nogradi ,  Gabor Wagner ,  Gyorgy Keseru ,  Attila Bielik ,  Tamas Gati ,  Viktor Hada ,  Janos Koti ,  Krisztina Gal ,  Monika Vastag ,  Amrita Agnes Bobok

    IPC分类号： A61K31/541 ,  C07D471/04 ,  C07D279/12 ,  C07D413/14 ,  C07D417/14 ,  A61K31/4365 ,  A61K31/5377 ,  A61K31/497 ,  A61P25/00 ,  A61P25/04

    CPC分类号： C07D495/04

    摘要： The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I) wherein X represents a group selected from SO, SO2; Y represents a group selected from (CH2)n, NH, NHCH2; n is an integer of 0 to 1; Z is H or monosubstituted by alkyl, nitro, halogen, alkoxy, trifluoromethyl, cyano, amino, alkylamino, dialkylamino, aminomethyl, e alkylaminomethyl, dialkylaminomethyl, hydroxyl, alkylsulfonylamino; R1 is an optionally substituted alkyl, cycloalkyl, phenyl, biphenyl, heterocyclyl; R2 is an optionally substituted phenyl, heterocyclyl, or NR3R4 group wherein R3 and R4 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R3 and R4 together with the N atom to which they are attached form an optionally substituted C5-7 heterocyclyl group, containing one or more heteroatom(s), or NH—CO—NR5R6 group, wherein R5 and R6 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R5 and R6 together with the N atom to which they are attached form an optionally substituted C5-7 heterocyclyl group, containing one or more heteroatom(s); and/or hydrates and/or solvates and/or pharmaceutically acceptable salts thereof formed with acids or bases, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluR1 and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain, neuromuscular dysfunctions of the lower urinary tract and gastrointestinal disorders.

    摘要翻译： 本发明涉及新的mGluR1和mGluR5受体亚型优选式（I）的配体，其中X表示选自SO，SO 2的基团; Y表示选自（CH 2）n，NH，NHCH 2; n为0〜1的整数; 卤素，烷氧基，三氟甲基，氰基，氨基，烷基氨基，二烷基氨基，氨基甲基，e烷基氨基甲基，二烷基氨基甲基，羟基，烷基磺酰基氨基; R 1是任选取代的烷基，环烷基，苯基，联苯基，杂环基; R 2是任选取代的苯基，杂环基或NR 3 R 4基团，其中R 3和R 4独立地选自氢和任选取代的烷基，或者R 3和R 4与它们所连接的N原子一起形成任选取代的C 5 - 7杂环基，其含有一个或多个杂原子或NH-CO-NR 5 R 6基团，其中R 5和R 6独立地选自氢和任选取代的烷基，或者R 5和R 6与其中的N原子一起 它们连接形成任选取代的含有一个或多个杂原子的C 5-7杂环基; 和/或与酸或碱形成的水合物和/或其溶剂合物和/或其药学上可接受的盐与其制备方法相关的药物组合物及其在治疗和/或预防需要的病理状况中的用途 mGluR1和mGluR5受体的调节，例如神经障碍，精神疾病，急性和慢性疼痛，下尿路神经肌肉功能障碍和胃肠道疾病。