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    • 9. 发明申请
    • NONEL 1,2,3,4-TETRAHYDROQUINOLINE DERIVATIVES
    • NONEL 1,2,3,4-四氢喹啉衍生物
    • WO2007120621A2
    • 2007-10-25
    • PCT/US2007008781
    • 2007-04-11
    • CONCERT PHARMACEUTICALS INCTUNG ROGERZELLE ROBERT
    • TUNG ROGERZELLE ROBERT
    • A61K31/4706
    • C07D215/42Y10T436/10
    • The present invention relates to a novel derivative of Compound 1 selectively substituted with fluorine and/or deuterium and optionally further substituted with deuterium and 13 C elsewhere in the molecule. The compounds of this invention are cholesterol esterase transfer protein inhibitors and possess unique biopharmaceutical and pharmacokinetic properties compared to Compound 1. They may also be used to accurately determine the concentration of Compound 1 in biological fluids and tissues and to determine metabolic patterns of Compound 1 and its isotopologues. The invention further provides compositions comprising these compounds and methods of treating diseases and conditions that are responsive to inhibition of cholesterol esterase transfer protein, alone and in combination with additional agents.
    • 本发明涉及化合物1的新型衍生物,其选择性地被氟和/或氘取代并任选进一步被分子中其他地方的氘和13 C取代。 本发明的化合物是胆固醇酯酶转移蛋白抑制剂,与化合物1相比具有独特的生物药物和药代动力学特性。它们还可用于准确测定化合物1在生物流体和组织中的浓度,并确定化合物1和 其同位素学。 本发明进一步提供了包含这些化合物的组合物以及治疗单独和与其它试剂组合对胆固醇酯酶转移蛋白的抑制有反应的疾病和病症的方法。