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US 2020/0048258 A1Published application
Kdm5 inhibitors
AssigneeMerck Sharp & Dohme Corp.
InventorsUMAR FARUK MANSOOR, Christian Fischer, Phieng Siliphaivanh, Luis Torres, Hakan Gunaydin, David L. Sloman
Life of this patent
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Abstract
The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors.
Claims9
A compound of formula I
- or a pharmaceutically acceptable salt thereof, wherein
- R1 is
- halogen,
- C1-C6 alkyl, unsubstituted or substituted with CF3,
- C2-C3 alkylene-C(O)—O—C1-C6 alkyl,
- a 3-, 4-, 5- or 6 membered saturated carbocycle, or
- a 6-membered unsaturated carbocycle;
- R2 is
- halogen,
- CF3,
- C1-C6 alkyl,
- C2-C4 alkenylene-O—C1-C3 alkyl,
- C(O)—O—C1-C6 alkyl,
- C(═CH2)C1-C4 alkyl,
- C2-C4 alkenylene C6H5,
- C1-C4 alkylene C6H5,
- a 3-, 4-, 5- or 6 membered saturated carbocycle,
- a 6-membered unsaturated carbocycle, unsubstituted or mono-substituted or independently di-substituted with R3,
- a 6-membered saturated heterocycle, unsubstituted, having 1 heteroatom which is O,
- a 5-membered unsaturated heterocycle having 1 or 2 heteroatoms independently selected from N, O and S, unsubstituted or independently mono- or di-substituted with R5, or
- a 6-membered unsaturated heterocycle, having 1 or 2 heteroatoms independently selected from N and O, unsubstituted or independently mono-, di-, tri- or tetra-substituted with R4, or
- an 8-, 9-, or 10-membered unsaturated bicyclic heterocycle having 1, 2 or 3 heteroatoms independently selected from N or O, unsubstituted or substituted with R6;
- R3 is
- —C1-C3 alkyl, unsubstituted or mono- or independently di-substituted with a 6-membered saturated heterocycle having 1 or 2 heteroatoms independently selected from N and O, —C(O)OC1-C3 alkyl, —OH, —CF3, and CN,
- C1-C3 alkoxy,
- halogen,
- CN,
- OH,
- O—C6H5,
- OC1-C3 alkyl,
- C(O)OC1-C3 alkyl,
- CF3,
- C(O)N(CH3)2,
- NH2,
- NHSO2C1-C3 alkyl,
- NH(C1-C3 alkyl),
- N(C1-C3 alkyl)(C1-C3 alkyl),
- NHSO2 cC3H5,
- a 5- or 6-membered saturated heterocycle having 1 or 2 heteroatoms independently selected from N, O and S, wherein S is a dioxide, unsubstituted or substituted with C1-C3 alkyl, or
- a 5- or 6-membered unsaturated heterocycle, unsubstituted or substituted with C1-C3 alkyl, having 1, 2 or 3 N atoms;
- R4 is
- halogen,
- C1-C3 alkyl, unsubstituted or substituted with —OH,
- CN,
- CF3,
- cC3H5,
- CF2CH2OH,
- a 6-membered saturated heterocycle having 1 or 2 heteroatoms independently selected from N and O, or
- a 5-membered unsaturated heterocycle having 2 N atoms;
- R5 is
- CF3,
- C1-C5 alkyl, unsubstituted or substituted with a 6-membered saturated heterocycle having 1 or 2 heteroatoms independently selected from N and O, a 6-membered unsaturated carbocycle, a 6-membered unsaturated heterocycle having 1 N atom, —OC1-C4 alkyl, —OH, —C(O)OH, a 5-membered unsaturated heterocycle having 1 S atom, cC3H5, —SO2C1-C4 alkyl, —NHC1-C4 alkyl, or a 3-5-membered saturated carbocycle unsubstituted or substituted with F,
- a 3-, 4-, 5- or 6-membered saturated carbocycle,
- a 6-membered unsaturated carbocycle unsubstituted or substituted with halogen,
- a 6-membered saturated heterocycle having 1 or 2 heteroatoms independently selected from N and O, or
- a 5-membered unsaturated unsubstituted heterocycle having 1 or 2 N heteroatoms;
- and
- R6 is C1-C6 alkyl, cyclopropyl or ═O.
55 more elements
(canceled)
Dependencies are inferred from the claim text.