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US 2005/0239780 A1Published application
Tetrahydropyran derivative
OwnerAkira Suga, Hideki Kubota +3inventors
InventorsAkira Suga, Hideki Kubota, Masanori Miura, Daisuke Sasuga, Hiroshi Moritani
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Abstract
The invention has succeeded in settling the aforementioned problems by finding that a novel tetrahydropyran derivative has excellent apo B-related lipoprotein secretion-inhibiting activity.
Claims9
A tetrahydropyran derivative represented by the following general formula (I) or a salt thereof
- (symbols in the formula mean as follows;
- R1 and R3:
- the same or different and each represents H or lower alkyl,
- R2:
- H, halogen, Ra-lower alkyl-, or R20O—CO—,
- Ra:
- H, R21O—CO—, R22R23N—, R24R2N—CO—, R26O—, cyano, or optionally-substituted hetero ring-,
- R4, R5, R6 and R7:
- the same or different and each represents H, halogen, haloalkyl, cyano, lower alkyl, lower alkyl-O—, R21O—CO-lower alkyl-, R27—CO—, or R2R29N—S(O)2
- R8 and R9:
- the same or different and each represents H, lower alkyl, R30-lower alkyl-, R31R32N—, optionally-substituted hetero ring-, or R33R34R35C—, with the proviso that R8 and R9 may together form a optionally-substituted hetero ring
- X:
- N, or CR36,
- R20, R22 to R26, R28, R29, R32, R35 and R36:
- the same or different and each represents H, or lower alkyl,
- R21:
- H, lower alkyl, or aryl-lower alkyl-,
- R27:
- HO—, lower alkyl-O—, or optionally-substituted hetero ring-,
- R30:
- optionally-substituted aryl, optionally-substituted hetero ring-, or lower alkyl-O—,
- R31:
- optionally-substituted aryl, or optionally-substituted hetero ring-,
- R33:
- HO-lower alkyl-, or optionally-substituted hetero ring-lower alkyl-, and
- R34:
- optionally-substituted aryl).
24 more elements
A compound selected from 3-(2,4-dimethyl-9-{4-[(S)-2-oxo-2-(4-pyridin-2-ylpiperazin-1-yl)-1-(tetrahydro-2H-pyran-4-yl)ethyl]benzyl}-9H-pyrido[2,3-b]indol-3-yl)propanoic acid;
- 3-(2,4-dimethyl-9-{4-[(S)-2-oxo-2-(4-propylpiperazin-1-yl)-1-(tetrahydro-2H-pyran-4-yl)ethyl]benzyl}-9H-pyrido[2,3-b]indol-3-yl)propanoic acid;
- 3-(9-{4-[(S)-(benzylcarbamoyl)(tetrahydro-2H-pyran-4-yl)methyl]benzyl}-2,4-dimethyl-9H-pyrido[2,3-b]indol-3-yl)propanoic acid;
- 3-(2,4-dimethyl-9-{4-[(S)-(dimethylcarbamoyl)(tetrahydro-2H-pyran-4-yl)methyl]benzyl}-9H-pyrido[2,3-b]indol-3-yl)propanoic acid;
- 3-(2,4-dimethyl-9-{4-[(S)-2-morpholin-4-yl-2-oxo-1-(tetrahydro-2H-pyran-4-yl)ethyl]benzyl}-9H-pyrido[2,3-b]indol-3-yl)propanoic acid;
- 3-(2,4-dimethyl-9-{4-[(S)-2-(4-isobutylpiperazin-1-yl)-2-oxo-1-(tetrahydro-2H-pyran-4-yl)ethyl]benzyl}-9H-pyrido[2,3-b]indol-3-yl)propanoic acid;
- 3-9-{4-[(S)-2-(4-cyclobutylpiperazin-1-yl)-2-oxo-1-(tetrahydro-2H-pyran-4-yl)ethyl]benzyl}-2,4-dimethyl-9H-pyrido[2,3-b]indol-3-yl)propanoic acid;
- 3-9-{4-[(S)-2-(4-cyclopentylpiperazin-1-yl)-2-oxo-1-(tetrahydro-2H-pyran-4-yl)ethyl]benzyl}-2,4-dimethyl-9H-pyrido[2,3-b]indol-3-yl)propanoic acid;
- and their salts.
5 more elements
Dependencies are inferred from the claim text.