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US 2013/0210819 A1Published application
Quinazoline derivatives
AssigneeMerck Patent GmbH
InventorMarkus Klein
Life of this patent
Estimating the term…
Abstract
Compounds of the formula I in which R, X, L2 and A1-A6 have the meanings indicated in Claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours.
Claims14
Compounds of the formula I
- in which
- A1 denotes N or CR1,
- A2 denotes N or CR2,
- A3, A4,
- A5, A6 each, independently of one another, denote N or CR3,
- X is absent or denotes unbranched or branched alkylene having 1-10 C atoms, in which 1-7 H atoms may be replaced by OH, F and/or Cl,
- and/or in which one or two non-adjacent CH and/or CH2 groups may be replaced by O, N, NH, NA′, CO, S, SO, SO2, OCO, NHCONH, NHCO, NHSO2, COO, CONH and/or CH═CH groups,
- or cycloalkylene having 3-7 C atoms,
- L2 is absent or denotes unbranched or branched alkylene having 1-10 C atoms, in which 1-7 H atoms may be replaced by OH, F and/or Cl,
- and/or in which one or two non-adjacent CH and/or CH2 groups may be replaced by O, N, NH, NA′, CO, S, SO, SO2, OCO, NHCONH, NHCO, NHSO2, COO, CONH and/or CH═CH groups,
- or cycloalkylene having 3-7 C atoms,
- with the proviso that X and L2 cannot be absent simultaneously,
- R denotes H or unbranched or branched alkyl having 1-10 C atoms, in which 1-7 H atoms may be replaced by F and/or Cl and/or in which one or two non-adjacent CH and/or CH2 groups may be replaced by O, N, NH, NA′, CO, S, SO, SO2, OCO, NHCONH, NHCO, NHSO2, COO, CONH and/or CH═CH groups,
- or
- cyclic alkyl having 3-7 C atoms,
- R1 denotes H or unbranched or branched alkyl having 1-10 C atoms, in which 1-7 H atoms may be replaced by F and/or Cl and/or in which one or two non-adjacent CH and/or CH2 groups may be replaced by O, N, NH, NA′, CO, S, SO, SO2, OCO, NHCONH, NHCO, NHSO2, COO, CONH and/or CH═CH groups,
- or
- cyclic alkyl having 3-7 C atoms,
- R2 denotes H or unbranched or branched alkyl having 1-10 C atoms, in which 1-7 H atoms may be replaced by F and/or Cl and/or in which one or two non-adjacent CH and/or CH2 groups may be replaced by O, N, NH, NA′, CO, S, SO, SO2, OCO, NHCONH, NHCO, NHSO2, COO, CONH and/or CH═CH groups,
- or
- cyclic alkyl having 3-7 C atoms,
- R3 denotes H or unbranched or branched alkyl having 1-10 C atoms, in which 1-7 H atoms may be replaced by F and/or Cl and/or in which one or two non-adjacent CH and/or CH2 groups may be replaced by O, N, NH, NA′, CO, S, SO, SO2, OCO, NHCONH, NHCO, NHSO2, COO, CONH and/or CH═CH groups,
- or
- cyclic alkyl having 3-7 C atoms,
- A′ in each case, independently of one another, denotes unbranched or branched alkyl having 1-10 C atoms,
- in which 1-7 H atoms may be replaced by F and/or Cl,
- and/or in which one or two non-adjacent CH and/or CH2 groups may be replaced by O, N, NH, NA, S, SO, SO2 and/or CH═CH groups,
- or
- cyclic alkyl having 3-7 C atoms,
- A denotes alkyl having 1, 2, 3 or 4 C atoms,
- and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.
28 more elements
Dependencies are inferred from the claim text.