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US 8,912,216 B2Granted
Hetaryl-[1,8]naphthyridine derivatives
AssigneeMerck Patent GmbH
InventorsAlfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
Life of this patent
Estimating the term…
Abstract
Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
Claims15
Compounds of formula (I)
- wherein
- W1, W3 denote CR3;
- W5, denotes N;
- W6 denotes CR4;
- R1 denotes a monocyclic carboaryl having 5-8 C atoms, Het1 or a monocyclic heteroaryl having 2-7 C atoms and 1-4 N, O and/or S atoms, each of which can be substituted by at least one substituent selected from the group of Y, Hal, CN, OY;
- R2 denotes Ar, Het1 or Het2, each of which can be substituted by R5;
- R3, R4 denotes independently from one another H, NYY, —NY—COY, A, OY or COOA;
- R2, R3 together also denote Alk under the proviso that R2 and at most one R2-adjacent R3 are together;
- R5 denotes Hal, A, —(CYY)n—OY, —(CYY)n—NYY, (CYY)n-Het3, SY, NO2, CN, COOY, —CO—NYY, —NY—COA, —NY—SO2A, —SO2—NYY, S(O)mA, —CO-Het3, —O(CYY)n—NYY, —O(CYY)n-Het3, —NH—COOA, —NH—CO—NYY, —NH—COO—(CYY)n—NYY, —NH—COO—(CYY)n-Het3, —NH—CO—NH—(CYY)n—NYY, —NH—CO—NH(CYY)n-Het3, —OCO—NH—(CYY)n—NYY, —OCO—NH—(CYY)n-Het3, CHO, COA, ═S, ═NY, ═O, Alk-OH, —CO—NY—(CYY)n—NYY, —CO—NY-Het3 or —SO2-Het3;
- Y denotes H or A;
- A denotes unbranched or branched alkyl having 1-10 C atoms,
- in which 1-7 H atoms can be replaced independently from one another by Hal and/or in which one or two adjacent CH2 groups can be replaced independently of one another by a O, S, SO, SO2, a —CY═CY— group and/or a —C≡C— group;
- Alk denotes unbranched alkylene, alkenyl or alkynyl having 2-5 C atoms, in which 1-2 H atoms can be replaced independently from one another by R5 and/or in which 1-4 C atoms can be replaced independently from one another by N, O and/or S;
- Ar denotes a saturated, unsaturated or aromatic, mono- or bicyclic carbocycle having 6-10 C atoms;
- Het1 denotes a saturated or unsaturated, mono, bi- or tricyclic heterocycle having 2-19 C atoms and 1-5 N, O and/or S atoms;
- Het2 denotes a mono, bi- or tricyclic heteroaryl having 2-19 C atoms and 1-5 N, O and/or S atoms;
- Het3 denotes a saturated, unsaturated or aromatic, mono-, bi- or tricyclic heterocycle having 2-19 C atoms and 1-5 N, O and/or S atoms, which can be substituted by at least one substituent selected from the group of Hal, A, —(CYY)n—OY, —(CYY)n—NYY, SY, NO2, CN, COOY, —CO—NYY, —NY—COA, —NY—SO2A, —SO2—NYY, S(O)mA, —NH—COOA, —NH—CO—NYY, CHO, COA, ═S, ═NY, ═O;
- Hal denotes F, Cl, Br or I;
- m denotes 0, 1 or 2;
- and
- n denotes 0, 1, 2, 3 or 4;
- and/or physiologically acceptable salts thereof.
19 more elements
Dependencies are inferred from the claim text.