公开(公告)号：US20100081717A1

公开(公告)日：2010-04-01

申请号：US12513369

申请日：2007-11-14

申请人： Ferenc Fulop ,  Zsolt Szakonyi

发明人： Ferenc Fulop ,  Zsolt Szakonyi

IPC分类号： A61K31/195 ,  C07C229/00

CPC分类号： C07C335/18 ,  C07B2200/07 ,  C07C215/42 ,  C07C229/50 ,  C07C271/24 ,  C07C275/30 ,  C07C275/34 ,  C07C335/14 ,  C07C2602/42 ,  C07C2603/18 ,  C07D205/12

摘要： The invention relates to chiral cyclic β-amino acids of Formula (I) and their salts formed with pharmaceutically acceptable acids or bases, wherein the main meanings of the substituents are as follows: R stands for C1-4 Alk; X stands for —COOH, —CONH2, —CONH(C1-4 Alk), —CON(C1-4 Alk)2, —COO(C1-4 Alk), —COPhe-O-(C1-4 Alk) or —CH2OH; Y stands for —NH2, —NHBoc, —NHFmoc, —NH(C1-4 Alk), —N(C1-4 Alk)2, —NHCH2Ph, or Ar—NH—C(=X0)—N(R0)— wherein Ar stands for a phenyl group substituted by C1-4 alkoxy or halogen, X0 stands for O or S, and R0 stands for hydrogen or benzyl; and X+Y stands for —CONH— vagy —CON(Boc)-; with the proviso that when X stands for —COOH, then Y may be only different from —NH2. The invention also relates to pharmaceutical compositions having multidrug-resistance reversing effect that contain one or more compound(s) of Formula (I) or a salt thereof and inert pharmaceutical carriers and/or auxiliary agents. The invention also relates to carboxylic acids of Formula (XX) and their salts.

摘要翻译： 本发明涉及式（I）的手性环状 - 氨基酸及其与药学上可接受的酸或碱形成的盐，其中取代基的主要含义如下：R代表C1-4烷基; X代表-COOH，-CONH 2，-CONH（C 1-4 Alk），-CON（C 1-4 Alk）2，-COO（C 1-4 Alk），-C OPhe-O-（C 1-4 Alk）或 - CH2OH; Y代表-NH2，-NHBoc，-NHFmoc，-NH（C1-4 Alk），-N（C1-4 Alk）2，-NHCH2Ph或Ar-NH-C（= X0）-N（R0） - 其中Ar表示被C 1-4烷氧基或卤素取代的苯基，X 0表示O或S，R 0表示氢或苄基; 而X + Y代表-CON​​H- vagy -CON（Boc） - ; 条件是当X代表-COOH时，则Y可以仅与-NH 2不同。 本发明还涉及含有一种或多种式（I）化合物或其盐和惰性药物载体和/或辅助剂的具有多重耐药性逆转作用的药物组合物。 本发明还涉及式（XX）的羧酸及其盐。