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    Amides of creatine, method of their preparation, and remedy possessing a neuroprotective activity
    35.
    发明授权
    Amides of creatine, method of their preparation, and remedy possessing a neuroprotective activity 有权
    肌酸酰胺，其制备方法以及具有神经保护活性的补救剂

    公开(公告)号：US08350077B2

    公开(公告)日：2013-01-08

    申请号：US12734183

    申请日：2008-12-24

    申请人： Sergej Vladimirovich Burov ,  Natalia Vasilyevna Khromova ,  Anna Alexandrovna Khromova ,  Petr Alekseevich Khromov

    发明人： Sergej Vladimirovich Burov ,  Natalia Vasilyevna Khromova ,  Anna Alexandrovna Khromova ,  Petr Alekseevich Khromov

    IPC分类号： C07C229/26 ,  C07C231/00 ,  C07C237/20

    CPC分类号： A61K31/16 ,  C07C279/14

    摘要： The invention relates to pharmaceutical chemistry notably to new biologically active substances (BAS) and their properties. In particular, the invention relates to Creatine derivatives having a general formula: NH═C(NH2)—N(CH3)—CH2—CO—NH—R*X, wherein R—amino acid residue of aliphatic, aromatic or heteroaromatic L-amino acid or its derivative representing a salts of amino acid, amino acid esters, amino acid amides or peptides; X—lower organic or mineral acid or water. New substances are prepared by interaction of aforesaid amides of sarcosine having a general formula of HN(CH3)—CH2—CO—NH—R*X, wherein: R is amino acid residue or substituted amino acid residue; X is low-molecular-weight organic acid or mineral acid or water, with a guanidinylating agents with the in organic solvents at temperature not exceeding 50° C. New chemical compounds can be used as a remedy possessing a neuroprotective activity.

    摘要翻译： 本发明涉及药物化学，特别涉及新的生物活性物质（BAS）及其性质。 特别地，本发明涉及具有以下通式的肌酸衍生物：NH = C（NH 2）-N（CH 3）-CH 2 -CO-NH-R * X，其中脂族，芳族或杂芳族L- 代表氨基酸，氨基酸酯，氨基酸酰胺或肽的氨基酸或其衍生物; X-有机或无机酸或水。 新物质通过上述具有通式HN（CH 3）-CH 2 -CO-NH-R * X的肌氨酸酰胺的相互作用制备，其中：R是氨基酸残基或取代的氨基酸残基; X是低分子量有机酸或无机酸或水，在有机溶剂中的胍基化剂温度不超过50℃。新化合物可用作具有神经保护活性的补救剂。

    PROCESS FOR PREPARING OPTICALLY PURE MILNACIPRAN AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS
    36.
    发明申请
    PROCESS FOR PREPARING OPTICALLY PURE MILNACIPRAN AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS 审中-公开
    制备光敏米拉宁药物及其药物接受口服的方法

    公开(公告)号：US20120289744A1

    公开(公告)日：2012-11-15

    申请号：US13574775

    申请日：2010-12-20

    申请人： Ganesh Gurpur Pai ,  Arun Kanti Mandal ,  Kamlesh Jayantilal Ranbhan ,  Vikram Sarjerao Jagtap ,  Dayaghan Gangadhar Patil ,  Yuvraj Kashinath Zunjarrao

    发明人： Ganesh Gurpur Pai ,  Arun Kanti Mandal ,  Kamlesh Jayantilal Ranbhan ,  Vikram Sarjerao Jagtap ,  Dayaghan Gangadhar Patil ,  Yuvraj Kashinath Zunjarrao

    IPC分类号： C07C231/16 ,  C07C237/20

    CPC分类号： C07C231/20 ,  C07B2200/07 ,  C07C59/50 ,  C07C237/20 ,  C07C2601/02

    摘要： The present invention relates to an improved and commercially, viable process for the resolution of racemic cis milnacipran of formula I and its pharmaceutically acceptable salts of formula II. The present invention comprises using racemic cis milnacipran or its pharmaceutically acceptable salts as starting material, a low cost and commercially available resolving agent of formula III and industrially safe and economically low cost material such as water as a solvent. The said process results into optical isomers of racemic cis milnacipran having excellent optical purity without involving multiple crystallization steps. The present invention also comprises the concept of green chemistry as the invention works well with water as a solvent thereby minimizing the use of any other solvent. (Formular I and II should be inserted here) Wherein X is anion selected from Cl, Br, I, HSO4, Phosphate or organic acid (Formular III should be inserted here) *represent asymmetric centre Compound of formula III represent mandelic acid and its derivatives.

    摘要翻译： 本发明涉及用于拆分式I的外消旋顺式米那普仑及其药学上可接受的式II的盐的改进且商业上可行的方法。 本发明包括使用外消旋的顺式米那普仑或其药学上可接受的盐作为起始原料，低成本和市售的式III拆分剂和工业上安全和经济低成本的材料如水作为溶剂。 所述方法产生具有优异光学纯度的外消旋顺式米那普仑的光学异构体，而不涉及多个结晶步骤。 本发明还包括绿色化学的概念，因为本发明与水作为溶剂良好地工作，从而最小化任何其它溶剂的用途。 （此处应插入式I和II）其中X为选自Cl，Br，I，HSO4，磷酸盐或有机酸的阴离子（此处应插入式III）*表示式III的不对称中心化合物，表示扁桃酸及其衍生物 。

    Ethoxy Diphenyl Ethane Derivatives, Preparation Processes and Uses Thereof
    39.
    发明申请
    Ethoxy Diphenyl Ethane Derivatives, Preparation Processes and Uses Thereof 有权
    乙氧基二苯基乙烷衍生物，其制备方法及用途

    公开(公告)号：US20120046492A1

    公开(公告)日：2012-02-23

    申请号：US13124504

    申请日：2009-10-15

    申请人： Fanhong Wu ,  Fanhua Xiao ,  Weiguo Zhou ,  Fangming Xu

    发明人： Fanhong Wu ,  Fanhua Xiao ,  Weiguo Zhou ,  Fangming Xu

    IPC分类号： C07C43/23 ,  C07F9/12 ,  C07C231/08 ,  C07C41/30 ,  C07C213/02 ,  C07C217/84 ,  C07C237/20

    CPC分类号： A61K31/09 ,  A61K31/165 ,  A61K31/661 ,  C07C217/84 ,  C07C237/04 ,  C07F9/12

    摘要： The invention discloses an ethoxydiphenylethane derivative and a synthetic method and uses thereof 4′ position of phenylethane B aromatic ring is chemically modified by ethoxy and hydroxy at position 3′ thereof is simultaneously modified to water soluble prodrug such as phosphate, and similarly, amino acid side chain is introduced to amino at position 3′ to form amino acid amide water soluble prodrug having the structure shown as formula (I) the ethoxydiphenylethane derivative and the prodrug thereof include strong tubulin aggregation inhibiting ability and obvious target damage effect for tumor vessels, selectively cause dysfunction and structural damage of tumor vessels and induce apoptosis of vascular endothelial cells in order to play the role of killing tumor cells or inhibiting tumor metastasis in case that the tumor cells are free from the support of nutrition and oxygen.

    摘要翻译： 本发明公开了一种乙氧基二苯乙烷衍生物及其合成方法和用途苯乙醚B芳环的4'位通过乙氧基化学改性，3'位的羟基同时修饰为水溶性前药，如磷酸盐，类似地，氨基酸侧 链引入3'位的氨基，形成具有式（I）结构的氨基酰胺水溶性前药，乙氧基二苯乙烷衍生物及其前药包括强大的微管蛋白聚集抑制能力和对肿瘤血管具有明显的靶损伤作用，有选择地引起 功能障碍和肿瘤血管结构损伤，并诱导血管内皮细胞凋亡，以发挥肿瘤细胞杀伤作用或抑制肿瘤转移的作用，以免肿瘤细胞不受营养和氧气的支持。