New tetrahydroquinoline compounds are cholesterol ester transfer protein inhibitors useful for primary and/or secondary prevention of coronary heart disease; and for treatment and/or prevention of e.g. hypolipoproteinemia and dyslipidemia

摘要

Tetrahydroquinoline compounds (I), (Ia) or (Ib) and their salts and solvates, are new. Tetrahydroquinoline compounds of formula (I), specifically (Ia) or (Ib), and their salts and solvates, are new. R : cyclopentyl or iso-propyl. Independent claims are also included for: (1) a medicament (A) comprising (I), (Ia) or (Ib) in combination with an inert and non-toxic auxiliary material; and (2) the preparations of (I), (Ia) and (Ib). [Image] ACTIVITY : Cardiant; Vasotropic; Antilipemic; Antiarteriosclerotic; Anorectic; Antidiabetic; Cerebroprotective; Neuroprotective; Nootropic. MECHANISM OF ACTION : Cholesterol ester transfer protein inhibitor. The ability of (I) to inhibit cholesterol ester transfer protein was tested using biological assays. The results showed that (5S)-4-cyclopentyl-3-{(S)-fluoro-[4-(trifluoromethyl)phenyl]methyl}-2-isopropyl-7,7-dimethyl-5,6,7,8-tetrahydrochinolin-5-ol exhibited a median inhibitory concentration (IC 50) value of 25 nM.