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US 9,809,598 B2Granted
Heterocyclyl-butanamide derivatives
AssigneeMerck Patent GmbH
InventorsHans-Peter Buchstaller, Dieter Dorsch
Life of this patent
Estimating the term…
Abstract
Compounds of the formula I in which W, X and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
Claims20
A compound of formula I
- in which
- W denotes
- wherein * indicates the point of attachment to the propylene moiety,
- X denotes O, CO or is absent,
- Y denotes Ar or Het1,
- R1 denotes H, F, Cl, CN, CH3, CF3, CHF2, CH2OH or OCH3,
- R2 denotes H or CH3,
- Ar denotes phenyl, which is unsubstituted, or mono-, di- or trisubstituted by Hal, NO2, CN, A, OR3, S(O)mR3, N(R3)2, COA, COOR3, CON(R3)2, SO2N(R3)2, NR3COR3, NR3SO2A, NR3CON(R3)2 and/or Het2,
- Het1 denotes furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, triazolyl, tetrazolyl, pyridyl, pyrimidyl or pyridazinyl, each of which is unsubstituted or mono- or disubstituted by Hal, NO2, Ar1, CN, A, OR3, N(R3)2, CON(R3)2, Het2 and/or ═O,
- Het2 denotes furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, triazolyl, tetrazolyl, pyridyl, pyrimidyl or pyridazinyl, each of which is unsubstituted or mono- or disubstituted by Hal, NO2, Ar1, CN, A, OR3, N(R3)2, CON(R3)2 and/or ═O,
- Ar1 denotes phenyl, which is unsubstituted, or mono-, di- or trisubstituted by Hal, NO2, CN, A, OR3, S(O)mR3, N(R3)2, COA, COOR3, CON(R3)2, NR3COR3 and/or NR3SO2A,
- A denotes unbranched or branched alkyl with 1-8 C-Atoms, wherein one or two non-adjacent CH- and/or CH2-groups may each be replaced by N- or O-atoms and wherein 1-7 H-atoms may each be replaced by F, Cl or OH,
- R3 denotes H or unbranched or branched alkyl with 1, 2, 3 or 4 C-Atoms,
- Hal denotes F, Cl, Br or I,
- m denotes 0, 1 or 2,
- n denotes 1 or 2,
- and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.
14 more elements
The compound 3-{4-[3-(4-Methoxy-benzoyl)-azetidin-1-yl]-4-oxo-butyl}-2H-pyrrolo[1,2-a]pyrazin-1-one (“D1”)
- and pharmaceutically acceptable solvates, salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.
Dependencies are inferred from the claim text.