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US 8,946,247 B2Granted
Quinazoline carboxamide azetidines
AssigneeMerck Patent GmbH
InventorsBayard R. Huck, Reinaldo Jones, Yufang Xiao, Constantin Neagu, Donald Bankston, Andreas Goutopoulos
Life of this patent
Estimating the term…
Abstract
The invention provides novel quinazoline carboxamide azetidine compounds according to Formula (I) and use for the treatment of hyperproliferative diseases, such as cancer.
Claims12
A compound of Formula (II′)
- and/or its stereoisomers or tautomers, or pharmaceutically acceptable salts of each of the foregoing, including mixtures thereof in all ratios, wherein:
- R1, R2 are H,
- R3′, R3″ independently are H, LA or Hal,
- R4, R5, R6, R7, R8, independently are H, Hal, LA, OH, SH, O(LA), NH2, NH(LA), N(LA)2, NO2, CN, OCN, SCN, COOH, COO(LA), CONH2, CONH(LA), CON(LA)2, NHCO(LA), NHCONH(LA), NHCONH2, NHSO2(LA), CO(LA), SO2NH2, SO2(LA) or SO2Hal,
- or
- R5, R6 together with the phenyl group they are attached to, may form a 9 or 10 membered bicyclic ring system, in which 1 or 2 of the non-phenyl carbon atoms may be independently replaced by NH, O or S, in which the cycle formed by R5 and R6 may be unsubstituted or mono- or disubstituted by Hal or LA,
- or
- one of R5, R6, R7
- may be Ar1, O(Ar1), NH(Ar1), CONH(Ar1), NHCO(Ar1), NHCONH(Ar1), NHSO2(Ar1), CO(Ar1) or SO2(Ar1),
- while the other two of R5, R6, R7 are not Ar1, O(Ar1), NH(Ar1), CONH(Ar1), NHCO(Ar1), NHCONH(Ar1), NHSO2(Ar1), CO(Ar1) or SO2(Ar1),
- Ar1 is a monocyclic aromatic homo- or heterocycle having 0, 1, 2 or 3 N, O and/or S atoms and 5 or 6 skeleton atoms, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by Hal, LA, OH, SH, O(LA), NH2, NH(LA), N(LA), NO2, CN, OCN, SCN, COOH, COO(LA), CONH2, CONH(LA), CON(LA)2, NHCO(LA), CHO, CO(LA), SO2NH2, SO2(LA) and/or SO2Hal,
- LA is unbranched or branched, linear alkyl having 1, 2, 3 or 4 C atoms, wherein 1, 2 or 3 H atoms may be replaced by Hal,
- Hal is F, Cl or Br.
10 more elements
Dependencies are inferred from the claim text.