发明申请
US20100081717A1 Chiral Cyclic Beta-Amino Acids and their Derivatives, Pharmaceutical Compositions Containing Them and the Use of Such Compounds
有权
手性环状β-氨基酸及其衍生物，含有这些化合物及其使用的药物组合物
- 专利标题： Chiral Cyclic Beta-Amino Acids and their Derivatives, Pharmaceutical Compositions Containing Them and the Use of Such Compounds
- 专利标题（中）： 手性环状β-氨基酸及其衍生物，含有这些化合物及其使用的药物组合物
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申请号： US12513369申请日： 2007-11-14
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公开(公告)号： US20100081717A1公开(公告)日： 2010-04-01
- 发明人: Ferenc Fulop , Zsolt Szakonyi
- 申请人： Ferenc Fulop , Zsolt Szakonyi
- 申请人地址： HU Budapest
- 专利权人： BIOBLOCKS MAGYARORSZÁG GYÓGYSZERKÉMIAI ÉS FEJLESZTÖ KFT.
- 当前专利权人： BIOBLOCKS MAGYARORSZÁG GYÓGYSZERKÉMIAI ÉS FEJLESZTÖ KFT.
- 当前专利权人地址： HU Budapest
- 优先权： HUP0600847 20061116
- 国际申请： PCT/HU2007/000107 WO 20071114
- 主分类号： A61K31/195
- IPC分类号： A61K31/195 ; C07C229/00
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.
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