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US 8,569,295 B2Granted
Bicyclic urea compounds
AssigneeMerck Patent GmbH
InventorsXiaoling Chen, Srinivasa R. Karra, Bayard R. Huck, Ruoxi Lan, Amanda E. Sutton, Andreas Goutopoulos, Brian L. Hodous, Reinaldo Jones
Life of this patent
Estimating the term…
Abstract
The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Claims60
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- X is a bond, NH, O, S, or CH2NH or CH2O, wherein NH or O moieties are connected to the 2-oxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine moiety,
- Q is a 5- or 6-membered monocyclic, or 9- or 10-membered bycyclic, aromatic, homo- or heterocycle having 1 or 2 N, O and/or S atoms, which may be unsubstituted or, independently of one another, mono- or disubstituted by Hal, LA, C(Hal)3, OC(Hal)3, OH, SH, O(LA), NH2, NH(LA), N(LA)2, NO2, CN, OCN, 4-fluorophenyl, oxo or SCN,
- M is a bond, CH2, CO, SO2, CONH, NHCO, NHCONH, SO2NH, NHSO2, NHSO2NH or CH2NHCO, wherein the CO moiety is connected to Q,
- R1 is H, A, Ar or Ar-A,
- R2 is H, or
- R1 and R2 together with the N and C atoms to which they are attached, may form a 5- or 6-membered aliphatic heterocycle having 1 or 2 N, O and/or S atoms, which may be unsubstituted or substituted by Hal, A, OH, NH2 or CN,
- R3 is A or Q, or
- R3-M may be absent,
- Ar is a mono- or bicyclic aromatic homo- or heterocycle having 1 to 4 N, O and/or S atoms and 5to 10 skeleton atoms, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by Hal, A, OH, SH, OA, NH2, NHA, NA2, NO2, CN, OCN, SCN, COOH, COOA, CONH2, CONHA, CONH(LAr), CONA2, NHCOA, NHCO(LAr), NHCONHA, NHCONH2, NHSO2A, CHO, COA, SO2NH2, SO2A and/or SO2Hal,
- A is unbranched or branched, linear or cyclic alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 C atoms, in which one or two CH2 groups may be replaced by an O or S atom and/or by an NH, CO, N(LA), SO2, CONH, NHCO or —CH═CH—group, and in which 1-3 H atoms may be replaced by Hal, and in which one or two CH3 groups may be replaced by OH, SH, NH2, NH(LA), N(LA)2, NHCOOH, NHCONH2, N3, NO2 or CN,
- LA is unbranched or branched, linear alkyl having 1, 2, 3 or 4 C atoms,
- Hal is F, Cl, Br or I.
10 more elements
Dependencies are inferred from the claim text.