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    Process for the preparation of piperazine compounds and hydrochloride salts thereof
    1.
    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。

    Cyclohexylamides as Dopamine D3, D2 and 5Ht1a Antagonists
    3.
    发明申请
    Cyclohexylamides as Dopamine D3, D2 and 5Ht1a Antagonists 失效
    环己基酰胺作为多巴胺D3，D2和5Ht1a拮抗剂

    公开(公告)号：US20080103140A1

    公开(公告)日：2008-05-01

    申请号：US11814874

    申请日：2006-02-02

    申请人： Eva Againe Csongor ,  Gyorgy Domany ,  Janos Galambos ,  Istvan Gyertyan ,  Bela Kiss ,  Katalin Saghy ,  Eva Schmidt

    发明人： Eva Againe Csongor ,  Gyorgy Domany ,  Janos Galambos ,  Istvan Gyertyan ,  Bela Kiss ,  Katalin Saghy ,  Eva Schmidt

    IPC分类号： A61K31/495 ,  A61K31/5377 ,  A61P43/00 ,  C07D295/155 ,  C07D413/02

    CPC分类号： C07D295/135

    摘要： The present invention relates to new dopamine D3 and D2 and serotonin 5-HT1A receptor subtype preferring ligands of formula (I); wherein A represents alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or a group of formula —NR1R2, wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, alkenyl, aryl, heteroaryl or cycloalkyl or R1 and R2 form with the adjacent nitrogen atom and optionally with further heteroatom(s) a heterocyclic ring; m is an integer of 0 to 1; n is an integer of 1 to 2, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmacological compositions containing the same and to their use in therapy and/or prevention of a condition which requires modulation of dopamine and/or 5-HT1A receptors.

    摘要翻译： 本发明涉及新的多巴胺D 3和D 2和5-羟色胺5-HT 1A受体亚型优选式（I）的配体; 其中A表示烷基，烯基，芳基，杂芳基，环烷基或式-NR 1 R 2的基团，其中R 1和R 2， 取代基独立地表示选自氢，烷基，链烯基，芳基，杂芳基或环烷基的取代基或R 1和R 2，以及相邻的氮原子 和任选地带有杂原子的杂环; m为0〜1的整数; n是1至2的整数，和/或几何异构体和/或立体异构体和/或非对映异构体和/或其盐和/或水合物和/或溶剂化物，其制备方法，含有其相同的药物组合物 以及它们在治疗和/或预防需要调节多巴胺和/或5-HT 1A受体的病症中的用途。

    Process for the preparation of an apovincaminol derivative
    4.
    发明授权
    Process for the preparation of an apovincaminol derivative 失效
    阿朴菌素衍生物的制备方法

    公开(公告)号：US4758666A

    公开(公告)日：1988-07-19

    申请号：US861550

    申请日：1986-05-09

    申请人： Janos Galambos ,  Tibor Keve ,  Bela Stefko ,  Gyorgy Fekete ,  Bela Zsadon ,  Anna Kassai nee Zieger ,  Klara Horvath nee Otta

    发明人： Janos Galambos ,  Tibor Keve ,  Bela Stefko ,  Gyorgy Fekete ,  Bela Zsadon ,  Anna Kassai nee Zieger ,  Klara Horvath nee Otta

    IPC分类号： C07D461/00

    CPC分类号： C07D461/00

    摘要： The invention relates to a new process for the preparation of 17,18-dehydro-apovincaminol-trimethoxy-benzoate of the formula (I) ##STR1## and acid addition salts thereof. According to the invention compound of the formula (I) is prepared starting from 17,18-dehydrovincamine of the formula (IIa) ##STR2## and/or 17,18-dehydro-epivincamine of formula (IIb) ##STR3## by reducing with a complex metal hydride, acylating the new hydroxy-vincaminol derivative obtained selectively with 3,4,5-trimethoxy-benzoic acid or a derivative thereof capable of acylation, optionally in the presence of a catalyst and/or an acid binding agent, and treating the corresponding acylated hydroxylderivative obtained with formic acid, in the presence of an acid chloride, and, if desired, converting the compound of formula (I) obtained into an acid addition salt thereof.

    摘要翻译： 本发明涉及一种制备式（I）所示的17,18-脱氢 - 氨基亚氨基三醇 - 苯甲酸酯（I）的新方法及其酸加成盐。 根据本发明，式（I）化合物是从式（IIa）（IIa）的17,18-脱氢丁胺和/或式（IIb）的17,18-脱氢 - 亚氨基胺开始制备的。 （IIb），通过用复合金属氢化物还原，任选地在催化剂和/或催化剂存在下酰化用3,4,5-三甲氧基 - 苯甲酸或其能够酰化的衍生物选择性地得到的新的羟基 - 长春花母醇衍生物 并且在酰氯存在下处理由甲酸获得的相应的酰化羟基衍生物，如果需要，将得到的式（I）化合物转化为其酸加成盐。

    Apovincaminol derivative
    5.
    发明授权
    Apovincaminol derivative 失效
    亚氨基酚衍生物

    公开(公告)号：US4680397A

    公开(公告)日：1987-07-14

    申请号：US727130

    申请日：1985-04-25

    申请人： Tibor Keve ,  Bela Zsadon ,  Gyorgy Fekete ,  Janos Galambos ,  Margit Barta nee Bukovecz ,  Laszlo Szporny ,  Lilla Forgacs ,  Arpad Kiraly ,  Gyongyver Soos ,  Bela Kiss ,  Maria Zajer nee Balazs

    发明人： Tibor Keve ,  Bela Zsadon ,  Gyorgy Fekete ,  Janos Galambos ,  Margit Barta nee Bukovecz ,  Laszlo Szporny ,  Lilla Forgacs ,  Arpad Kiraly ,  Gyongyver Soos ,  Bela Kiss ,  Maria Zajer nee Balazs

    IPC分类号： A61K31/475 ,  A61P17/00 ,  A61P43/00 ,  C07D461/00

    CPC分类号： C07D461/00

    摘要： The invention relates to new apovincaminol derivatives of the formula /I/ ##STR1## wherein R.sub.1 is hydrogen, nitro or halogen,R.sub.2 is a substituted or unsubstituted alkyl or phenyl group,R.sub.3 and R.sub.4 together form a valency bond or each independently represents hydrogen, hydroxyl or an --OR.sub.5 group, in whichR.sub.5 is substituted or unsubstituted alkanoyl or benzoyl group,with the proviso that if R.sub.2 stands for a 3,4,5-trimethoxyphenyl group and R.sub.1 is hydrogen, R.sub.3 and R.sub.4 together do not form a valency bond, or if R.sub.2 is a 3,4,5-trimethoxyphenyl group and R.sub.3 and R.sub.4 both are hydrogen, R.sub.1 is other than hydrogen, nitro or bromine, and acid addition salts thereof.The compounds may be used in the therapy of various skin diseases accompanied by a pathological cell proliferation, preferably psoriasis.

    摘要翻译： 本发明涉及式I /（I）的新的氨基嘌呤醇衍生物，其中R1是氢，硝基或卤素，R2是取代或未取代的烷基或苯基，R3和R4一起形成价键或各自独立地 表示氢，羟基或-OR 5基团，其中R 5为取代或未取代的烷酰基或苯甲酰基，条件是如果R 2表示3,4,5-三甲氧基苯基且R 1为氢，则R 3和R 4一起不为 形成价键，或者如果R2是3,4,5-三甲氧基苯基，且R3和R4都是氢，R1不是氢，硝基或溴，以及其酸加成盐。 该化合物可用于治疗伴随病理细胞增殖的各种皮肤疾病，优选牛皮癣。

    Process for the preparation of piperazine derivatives
    7.
    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
    9.
    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。