893407-10-8

Upstream product

• 202263-72-7 3-amino-3-cyclopentyl-1-(4-trifluoromethylphenyl)-propenone 
• 872-53-7 cyclopentanealdehyde 
• 126-81-8 dimedone 

Downstream Products

• 893407-12-0 2,4-dicyclopentyl-7,7-dimethyl-3-(4-trifluoromethylbenzoyl)-7,8-dihydro-6H-quinolin-5-one 

Relevant academic research and scientific papers

Novel tetrahydrochinoline derived CETP inhibitors

In the course of our efforts to identify orally active cholesteryl ester transfer protein (CETP) inhibitors, we have continued to explore tetrahydrochinoline derivatives. Based on BAY 19-4789 structural modifications led to the discovery of novel cycloalkyl substituted compounds. Thus, example 11b is a highly potent CETP inhibitor both in vitro and in vivo in transgenic mice with favourable pharmacokinetic properties for clinical development.

(5S) -3-[(S)-FLUORO (4-TRIFLUOROMETHYLPHENYL) METHYL]-5,6,7,8-TETRAHYDROQUINOLINE-5-OL DERIVATIVES AND USE THEREOF AS CETP INHIBITORS

The invention relates to novel tetrahydroquinoline derivatives of formula (I), wherein R1 represents cyclohexyl or cyclopentyl, R2 and R3 each represent methyl or jointly form a cyclobutane, and R4 represents cyclopentyl or isopropyl, the salts and solvates thereof, and the solvates of said salts. Also disclosed are a method for the production thereof, the use thereof on its own or in combinations for the treatment and/or prevention of diseases, and the use thereof for producing medicaments, particularly as a cholesterol ester transfer protein (CETP) inhibitor in order to treat and/or prevent cardiovascular diseases, especially hypolipoproteinemia, dyslipidemia, hypertriglyceridemia, hyperlipidemia, hypercholesterolemia, and arteriosclerosis.