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    METHOD FOR PREPARING (2S,3S)-3-AMINO-BICYCLO[2.2.2]OCTANE-2-CARBOXYLATE
    1.
    发明公开
    METHOD FOR PREPARING (2S,3S)-3-AMINO-BICYCLO[2.2.2]OCTANE-2-CARBOXYLATE 审中-公开

    公开(公告)号：EP3904333A1

    公开(公告)日：2021-11-03

    申请号：EP20911028.7

    申请日：2020-06-30

    申请人： Guangdong Raffles Pharmatech Co., Ltd

    发明人： ZHOU, Zhangtao ,  HUANG, Zhining ,  YE, Weiping ,  PHILLIS, Andrew Toroa

    IPC分类号： C07C227/18 ,  C07C229/50 ,  C07C227/32

    摘要： The present disclosure relates to a method for preparing (2S,3S)-3-amino-bicyclo[2.2.2]octane-2-carboxylate; it belongs to the field of pharmaceutical intermediate synthesis. The purpose of the present disclosure is to solve the problems of high preparation cost and low material safety of (2S,3S)-3-amino-bicyclo[2.2.2]octane-2-carboxylate, to further increase the production capacity and to reduce the production cost. The method of the present invention takes 3-carbonyl-bicyclo[2.2.2]octane-2-carboxylate as the starting material and performs reductive amination, alkalinity configuration flip, and hydrogenation to remove the protecting group in sequence to obtain the target product. The synthesis of (2S,3S)-3-amino-bicyclo[2.2.2]octane-2-carboxylate according the present invention is characterized by a novel route, mild reaction conditions and low cost, with a yield of more than 65%.

    HYDRATED N-FULLERENE AMINO ACIDS, METHOD FOR PRODUCING THE LATTER, AND PHARMACEUTICAL COMPOSITIONS ON THE BASIS THEREOF
    2.
    发明授权
    HYDRATED N-FULLERENE AMINO ACIDS, METHOD FOR PRODUCING THE LATTER, AND PHARMACEUTICAL COMPOSITIONS ON THE BASIS THEREOF 有权
    水合N-富勒烯氨基酸，其制备方法以及基于其的药物组合物

    公开(公告)号：EP2679574B1

    公开(公告)日：2018-05-09

    申请号：EP12742445.5

    申请日：2012-02-06

    申请人： Rasnetsov, Lev Davidovich

    发明人： SHVARTSMAN, lakov Yudelevich ,  SUVOROVA, Olga Nikolaevna ,  RASNETSOV, Lev Davidovich

    IPC分类号： C07C229/50 ,  C07C227/14 ,  A61K31/197 ,  A61P31/16 ,  A61P31/18 ,  A61P31/22 ,  A61P35/00 ,  A61P17/06 ,  C07C229/14 ,  C07C227/18

    CPC分类号： C07C229/12 ,  C07C227/14 ,  C07C227/18 ,  C07C229/14 ,  C07C229/50

    摘要： The invention relates to the pharmaceutical industry and to medicine, specifically to novel hydrated amino-acid derivatives of fullerene C 60 of general formula C 60 (H) 3 {NH(CH 2 ) n COOH} 3 ·xH 2 O, where C 60 - fullerene, n = 5, 6, 7, x = 8 - 10, and also to a method for producing said derivatives, and to the production of pharmaceutical compositions on the basis thereof. Hydrated N-fullerene amino acids are formed in the interaction of fullerene with 15 times the molar excess of anhydrous potassium salts of amino acids in a medium of organic aromatic solvent with slow addition to the resultant suspension of an interphase catalyst and with mixing and heating to a temperature not exceeding 60°C until the solution is completely decolorized and a solid residue formed, after which the latter is separated out, and then 0.8 M of aqueous solutions of potassium salts of fullerene amino-acid derivatives is treated with a solution of organic or mineral acids, followed by centrifugation, rinsing and drying of the residue. A pharmaceutical composition which exhibits activity against the herpes virus, flu viruses of various origin and HIV, and also anti-tumor and anti-psoriatic activity, comprising, as active substance, an effective quantity of hydrated N-fullerene amino acids.

    HYDRATED N-FULLERENE AMINO ACIDS, METHOD FOR PRODUCING THE LATTER, AND PHARMACEUTICAL COMPOSITIONS ON THE BASIS THEREOF
    3.
    发明公开
    HYDRATED N-FULLERENE AMINO ACIDS, METHOD FOR PRODUCING THE LATTER, AND PHARMACEUTICAL COMPOSITIONS ON THE BASIS THEREOF 有权
    氢化n FULLEREN氨基酸，PROCESS FOR THEIR和药物成分，以便

    公开(公告)号：EP2679574A1

    公开(公告)日：2014-01-01

    申请号：EP12742445.5

    申请日：2012-02-06

    申请人： Rasnetsov, Lev Davidovich

    发明人： SHVARTSMAN, lakov Yudelevich ,  SUVOROVA, Olga Nikolaevna ,  RASNETSOV, Lev Davidovich

    IPC分类号： C07C229/50 ,  C07C227/14 ,  A61K31/197 ,  A61P31/16 ,  A61P31/18 ,  A61P31/22 ,  A61P35/00 ,  A61P17/06

    CPC分类号： C07C229/12 ,  C07C227/14 ,  C07C227/18 ,  C07C229/14 ,  C07C229/50

    摘要： The invention relates to the pharmaceutical industry and to medicine, specifically to novel hydrated amino-acid derivatives of fullerene C 60 of general formula C 60 (H) 3 {NH(CH 2 ) n COOH} 3 ·xH 2 O, where C 60 - fullerene, n = 5, 6, 7, x = 8 - 10, and also to a method for producing said derivatives, and to the production of pharmaceutical compositions on the basis thereof. Hydrated N-fullerene amino acids are formed in the interaction of fullerene with 15 times the molar excess of anhydrous potassium salts of amino acids in a medium of organic aromatic solvent with slow addition to the resultant suspension of an interphase catalyst and with mixing and heating to a temperature not exceeding 60°C until the solution is completely decolorized and a solid residue formed, after which the latter is separated out, and then 0.8 M of aqueous solutions of potassium salts of fullerene amino-acid derivatives is treated with a solution of organic or mineral acids, followed by centrifugation, rinsing and drying of the residue. A pharmaceutical composition which exhibits activity against the herpes virus, flu viruses of various origin and HIV, and also anti-tumor and anti-psoriatic activity, comprising, as active substance, an effective quantity of hydrated N-fullerene amino acids.

    摘要翻译： 本发明涉及制药工业和医学，特别涉及通式C 60（H）3 {NH（CH 2）n的COOH}的富勒烯C 60的新颖水合氨基酸衍生物3·XH 2 O，其中C 60 - 富勒烯中，n = 5，6，7中，x = 8 - 10，从而用于产生所述衍生物的方法，并且涉及其的基础上生产的药物组合物。 水合N-富勒烯氨基酸形成在富勒烯的相互作用与15倍摩尔过量的氨基酸无水钾盐与缓慢加入到相间催化剂的所得悬浮液的有机芳族溶剂的介质，并在混合和加热至 不超过60℃，直至溶液被完全呼叫脱色和固体残余物形成的温度，afterwhich后者分离出来，然后在0.8M富勒烯氨基酸衍生物的钾盐的wässrige解决方案是治疗具有的有机溶液 或无机酸，通过离心其次，漂洗和残留物的干燥。 其表现出活性对疱疹病毒的药物组合物，各种起源和HIV，因此抗肿瘤和抗牛皮癣活性，包含作为活性物质，在水合的富勒烯的N-氨基酸有效量的流感病毒。

    MONOVERETHERTE DIOLE DER DIAMANTOIDEN
    4.
    发明公开
    MONOVERETHERTE DIOLE DER DIAMANTOIDEN 审中-公开

    公开(公告)号：EP2285764A2

    公开(公告)日：2011-02-23

    申请号：EP09757522.9

    申请日：2009-06-02

    申请人： Justus-Liebig-Universität Gießen

    发明人： SCHREINER, Peter R. ,  SCHWERTFEGER, Hartmut

    IPC分类号： C07C41/09 ,  C07C43/196 ,  C07C205/18 ,  C07C213/02 ,  C07C215/42 ,  C07C217/52 ,  C07C227/02 ,  C07C229/50 ,  C07C231/06 ,  C07C233/23

    CPC分类号： C07C41/09 ,  C07C43/196 ,  C07C215/44 ,  C07C217/52 ,  C07C229/50 ,  C07C233/23 ,  C07C2603/90 ,  Y02P20/55

    摘要： The invention at hand describes functionalized diols of diamondoids, in which one of the two hydroxy groups is masked by a protective group, as well as methods for producing these functionalized diols. The protective group is a group —CHR1R2, wherein R1 and R2 stand for alkyl groups and the protective group comprises at least one halogen atom. The monoethers of the diamondoid diols according to the present invention are produced by reacting the diamondoid diol with a halogenated alcohol CHOHR1R2 in the presence of a catalyst acid. The monoetherified diols allow for the targeted production of derivatives of diamondoids, for example, of the corresponding aminoalcohols and aminocarboxylic acids. For that purpose, the diamondoid monoether is reacted in a first step with a halogen nitrile in a Ritter reaction to the corresponding monoether amide. From this monoether amide, the corresponding aminoalcohol can be produced by reacting the protective group —CHR1R2 first with trifluoroacetic acid to the alkanoyloxy group and by subsequently obtaining the aminoalcohol by reaction with thiourea, ethanol and glacial acetic acid. The aminoalcohol can be reacted with a sulfuric acid/formic acid or oleum/formic acid to the corresponding aminocarboxylic acid. The amino, hydroxy and carboxylic groups of the diamondoids can be converted into many other functional groups.

    摘要翻译： 本发明描述了金刚石的官能化二醇，其中两个羟基中的一个被保护基掩蔽，以及制备这些官能化二醇的方法。 保护基是基团-CHR1R2，其中R1和R2代表烷基，保护基包括至少一个卤素原子。 根据本发明的金刚石二醇的单醚通过在催化剂酸存在下使类金刚石二醇与卤代醇CHOHR1R2反应来制备。 单醚化二醇允许目标生成类金刚石衍生物，例如相应的氨基醇和氨基羧酸。 为此，金刚石单醚在第一步中与Ritter反应中的卤素腈与相应的单醚酰胺反应。 从该单醚酰胺可以通过使保护基-CHR1R2与三氟乙酸首先与烷酰氧基反应，然后通过与硫脲，乙醇和冰醋酸反应获得氨基醇来制备相应的氨基醇。 氨基醇可与硫酸/甲酸或发烟硫酸/甲酸反应至相应的氨基羧酸。 金刚石的氨基，羟基和羧基可以转化为许多其他官能团。

    2-AMINOBICYCLO 3.1.0 HEXANE-2,6-DICARBOXYLIC ESTER DERIVATIVE
    7.
    发明公开
    2-AMINOBICYCLO 3.1.0 HEXANE-2,6-DICARBOXYLIC ESTER DERIVATIVE 有权
    2AMINOBICYCLO¬3.1.0|己基-2,6-DICARBONSÄUREESTERDERIVAT

    公开(公告)号：EP1637517A4

    公开(公告)日：2007-05-23

    申请号：EP04746867

    申请日：2004-06-25

    申请人： TAISHO PHARMA CO LTD

    发明人： YASUHARA AKITO ,  SAKAGAMI KAZUNARI ,  OHTA HIROSHI ,  NAKAZATO ATSURO

    IPC分类号： C07C229/50 ,  A61K31/216 ,  A61K31/357 ,  A61K31/365 ,  A61P9/10 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07C235/06 ,  C07C247/04 ,  C07C323/61 ,  C07D307/88 ,  C07D317/34

    CPC分类号： C07C229/50 ,  C07D307/88

    摘要： A drug which is effective in treatments for and prevention of schizophrenia, anxiety, and diseases related to these, i.e., psychiatrical disorders such as depression, bipolar disorder, and epilepsy. The drug has high activity in oral administration and has an antagonistic effect on a Group II metabotropic glutamate receptor. It is a 2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by the formula [I]: [I] [wherein R1 and R2 are the same or different and each represents hydrogen, C1-10 alkyl, etc.; X represents hydrogen or fluorine; and Y represents, e.g., -OCHR3R4 (wherein R3 and R4 are the same or different and each represents hydrogen, C1-10 alkyl, etc. and n is an integer of 1 or 2)], a pharmaceutically acceptable salt of the derivative, or a hydrate of either.

    摘要翻译： 对治疗和预防精神分裂症，焦虑症和与这些有关的疾病，即抑郁症，双相性精神障碍和癫痫等精神病症有效的药物。 该药在口服给药中具有高活性，并对II组代谢型谷氨酸受体具有拮抗作用。 它是由式[I]表示的2-氨基二环[3.1.0]己烷-2,6-二羧酸酯衍生物：[I] [其中R1和R2相同或不同，各代表氢，C1-10烷基 等; X代表氢或氟; Y表示例如-OCHR 3 R 4（其中R 3和R 4相同或不同，并且各自表示氢，C 1-10烷基等，并且n是1或2的整数）]，衍生物的药学上可接受的盐， 或任一种的水合物。