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US 2002/0165252 A1Published application
4-phenyltetrahydrochinoline utilized as an inhibitor of the cholesterol ester transfer protein
AssigneeBayer Aktiengesellschaft
InventorsGunter Schmidt, Jurgen Stoltefuss, Michael Logers, Arndt Brandes, Carsten Schmeck, Klaus-Dieter Bremm, Hilmar Bischoff, Delf Schmidt
Life of this patent
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Abstract
The tetrahydroquinolines can be prepared by condensing appropriately substituted tetrahydroquinoline aldehydes with suitable substances and subsequently varying the substituents present by customary methods. The tetrahydroquinolines are suitable as active compounds in medicaments, in particular in medicaments. for the treatment of arteriosclerosis and dyslipidaemias.
Claims10
Tetrahydroquinolines of the general formula (I)
- 102
- in which
- A represents phenyl which is optionally substituted up to 2 times by identical or different substituents from the group consisting of halogen, trifluoromethyl and straight-chain or branched alkyl or alkoxy having in each case up to 3 carbon atoms,
- D represents a radical of the formula
- 103
- in which
- R5 and R6 together form a carbonyl group (═O), or
- R5 represents hydrogen and
- R6 represents halogen or hydroxyl, or
- R5 and R6 represent hydrogen,
- R7 and R8 are identical or different and represent phenyl, naphthyl, benzothiazolyl, quinolyl, pyrimidyl or pyridyl which are optionally substituted up to 4 times by identical or different substituents from the group consisting of halogen, trifluoromethyl, nitro, cyano, trifluoromethoxy, or by a radical of the formula —SO2—CH3 or —NR9R10,
- in which
- R9 and R10 are identical or different and represent hydrogen or straight-chain or branched alkyl having up to 3 carbon atoms,
- E represents cycloalkyl having 3 to 6 carbon atoms, or represents straight-chain or branched alkyl having up to 8 carbon atoms,
- R1 represents hydroxyl, and
- R2represents hydrogen or represents methyl,
- R3 and R4 are identical or different and represent straight-chain or branched alkyl having up to 3 carbon atoms, or
- R3 and R4 together form a spiro-linked alkyl chain having 2 to 4 carbon atoms,
- and their salts and N-oxides.
16 more elements
Dependencies are inferred from the claim text.