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    MEXILETINE AMINO ACID AND PEPTIDE PRODRUGS AND USES THEREOF
    23.
    发明申请
    MEXILETINE AMINO ACID AND PEPTIDE PRODRUGS AND USES THEREOF 审中-公开
    梅毒素氨基酸和肽类产品及其用途

    公开(公告)号：US20110028552A1

    公开(公告)日：2011-02-03

    申请号：US12823066

    申请日：2010-06-24

    申请人： Richard Franklin ,  Bernard T. Golding ,  Robert G. Tyson

    发明人： Richard Franklin ,  Bernard T. Golding ,  Robert G. Tyson

    IPC分类号： A61K31/197 ,  C07C237/08 ,  A61K31/165 ,  C07C271/54 ,  A61P29/00 ,  A61P9/06

    CPC分类号： C07C381/12 ,  C07C237/08 ,  C07C279/14

    摘要： The present invention concerns prodrugs of mexiletine (and mexiletine's active metabolite) with amino acids or peptides and pharmaceutical compositions containing such prodrugs. Methods for providing pain relief, treating arrhythmia, decreasing the adverse GI side effects associated with mexiletine, increasing the bioavailability of mexiletine, and improving the pharmacokinetic reproducibility of mexiletine with the aforementioned prodrugs are also provided. Oligopeptides incorporating lysine or arginine residues attached directly or indirectly through a glycine residue are also described herein.

    摘要翻译： 本发明涉及美西律（和美西律的活性代谢物）与氨基酸或肽的前药以及含有这些前药的药物组合物。 还提供了提供疼痛缓解，治疗心律失常，减少与美西律相关的不良GI副作用，增加美西律的生物利用度，以及改善美西律与前述药物的药代动力学再现性的方法。 通过甘氨酸残基直接或间接连接的赖氨酸或精氨酸残基的寡肽也在本文中描述。

    Hair cosmetic, aminocarboxylic acid amide and method for producing the same
    26.
    发明申请
    Hair cosmetic, aminocarboxylic acid amide and method for producing the same 失效
    毛发化妆品，氨基羧酸酰胺及其制造方法

    公开(公告)号：US20050091763A1

    公开(公告)日：2005-05-05

    申请号：US10997945

    申请日：2004-11-29

    申请人： Katsuhisa Inoue ,  Takeshi Kaharu ,  Tohru Katoh

    发明人： Katsuhisa Inoue ,  Takeshi Kaharu ,  Tohru Katoh

    IPC分类号： C07C237/08 ,  C07D295/15 ,  A61K7/13

    CPC分类号： C07D295/15 ,  A61K8/42 ,  A61Q5/006 ,  A61Q5/02 ,  A61Q5/06 ,  A61Q5/12 ,  C07C237/08

    摘要： A hair cosmetic which can impart, to hairs, flexibility, smoothness and oily feeling when the hairs are wetted and smoothness, softness and combing easiness after the hairs are dried are provided, the hair cosmetic comprising an amine represented by the formula (I): Formula (I) (wherein R1 represents a C8-40 alkyl group or alkenyl group or a group represented by the formula R5O—(AO)n—CmH2m—(R5 represents a C8-40 alkyl group or alkenyl group having 8 to 40 carbon atoms, A represents a C2-3 alkylene group, n denotes a number from 0 to 30 in average and m denotes an integer of 2 or 3), R2 represents a C1-5 alkylene group, R3 represents H, a C1-24 alkyl group, alkenyl group or hydroxyalkyl group or a C6-28 aryl group or arylalkyl group, R4 represents H, a C1-5 alkyl group, alkylene group or hydroxyalkyl group or a C6-28 aryl group or arylalkyl group, p denotes an integer from 1 to 3, q and r denote integers from 0 to 2 and p+q+r is equal to 3. Also, the amine (I) can be produced with high selectivity and biaghly economically by reacting a primary amine with an aminocarboxylic acid to run amidation. An amine represented by the formula (1), its salt or quaternary ammonium salt are also provided: Formula (1)

    摘要翻译： 本发明提供一种毛发化妆品，其特征在于，含有由式（I）表示的胺类的毛发化妆品，其能够赋予毛发润湿后的毛发，柔软性，平滑性，油性感，柔软性，梳理容易性。 式（I）（其中R 1表示C 8-20烷基或烯基或由式R 5 O表示的基团） - （AO）N 2 -C（O）H 2 - （R 5）表示C 8 - 40个碳原子数为8〜40的烷基或烯基，A表示C 2-3亚烷基，n表示平均为0〜30的数，m表示 2或3），R 2表示C 1-5亚烷基，R 3表示H，C 1-24 烷基，烯基或羟烷基或C 6-28芳基或芳烷基，R 4表示H，C 1〜 5个烷基，亚烷基或羟烷基或C 1 芳基或芳烷基，p表示1〜3的整数，q和r表示0〜2的整数，p + q + r等于3.另外，胺（I ）可以通过使伯胺与氨基羧酸反应进行酰胺化而以高选择性和经济地生产。 还提供了由式（1）表示的胺，其盐或季铵盐：式（1）

    Amino acids peptides or derivatives thereof coupled to fats
    30.
    发明授权
    Amino acids peptides or derivatives thereof coupled to fats 失效
    氨基酸肽或其衍生物与脂肪偶联

    公开(公告)号：US5869606A

    公开(公告)日：1999-02-09

    申请号：US477698

    申请日：1995-06-07

    申请人： Robert George Whittaker

    发明人： Robert George Whittaker

    IPC分类号： C07C237/08 ,  C07C271/22 ,  C07C323/60 ,  C07K1/113 ,  C07K5/06 ,  C07K5/083 ,  C07K5/087

    CPC分类号： C07K5/06043 ,  C07C237/08 ,  C07C271/22 ,  C07C323/60 ,  C07K5/0806 ,  C07K5/0812 ,  Y10S530/812

    摘要： The present invention provides novel compounds in which peptides, amino acids or derivatives thereof are bound to other molecules, in particular fatty acids, which facilitate the use of such peptides, amino acids or derivatives thereof. The basic structure of the compounds of the present invention are an amino acid, peptide or derivative thereof linked to 1 to 3 fatty acid molecules via a tromethamine derivative. Alternatively, the amino acid, peptide or derivative thereof may be linked to a fatty acid by an ethanolamine derivative.

    摘要翻译： 本发明提供了其中肽，氨基酸或其衍生物与其它分子特别是脂肪酸结合的新型化合物，其有利于使用这些肽，氨基酸或其衍生物。 本发明化合物的基本结构是通过氨基丁三醇衍生物与1至3个脂肪酸分子连接的氨基酸，肽或衍生物。 或者，氨基酸，肽或其衍生物可以通过乙醇胺衍生物与脂肪酸连接。