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US 11,026,936 B2Granted
Piperidinyl-propanone derivatives
AssigneeMerck Patent GmbH
InventorHans-Peter Buchstaller
Life of this patent
Estimating the term…
Abstract
Compounds of the formula I in which X, Q, R1 and R2 have the meanings indicated in Claim 1, are inhibitors of pyruvate dehydrogenase kinase (PDHK), and can be employed, inter alia, for the treatment of diseases such as cancer.
Claims17
A compound of the formula I
- in which
- X denotes NH or O,
- Q denotes C(CH3)2 or 1,1-cyclopropylene,
- R1 denotes H, A, Cyc, Ar or Het,
- R2 denotes H or CH3,
- R3 denotes H or A′,
- 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 and/or NR3CON(R3)2,
- Het denotes a mono- or bicyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which is unsubstituted or mono- or disubstituted by Hal, NO2, CN, A, OR3, S(O)mR3, N(R3)2, COA, COOR3, CON(R3)2, SO2N(R3)2, NR3COR3, NR3SO2A and/or NR3CON(R3)2,
- A denotes unbranched or branched alkyl with 1-10 C-atoms, wherein one or two non-adjacent CH- and/or CH2-groups may be replaced by N-, O- and/or S-atoms and/or wherein 1-7 H-atoms may be replaced by R4,
- R4 denotes F, Cl or OH,
- A′ denotes unbranched or branched alkyl with 1-6 C-atoms, wherein 1-5 H-atoms may be replaced by F,
- Cyc denotes cyclic alkyl with 3, 4, 5, 6 or 7 C-atoms, which is unsubstituted or monosubstituted by OH,
- Hal denotes F, Cl, Br or I,
- m denotes 0, 1 or 2,
- and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.
12 more elements
Dependencies are inferred from the claim text.