Back to results
US 9,850,255 B2Granted
Heterocyclic derivatives as modulators of kinase activity
AssigneeMerck Patent GmbH
InventorsRuoxi Lan, Bayard R. Huck, Xiaoling Chen, Yufang Xiao
Life of this patent
Estimating the term…
Abstract
The invention provides novel imidazol-piperidinyl derivatives of the formula (I) in which R1, R2, W, X1, X2, X3, X4 and n have the meanings indicated in formula I, and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Claims12
A compound of formula (I),
- or a pharmaceutically acceptable salt, solvate, solvate of salts, tautomer or stereoisomer, including a mixture thereof in all ratios thereof,
- wherein:
- X1 is N,
- X2 is CH2 or NH,
- X3 is CO,
- X4 is NH,
- W is N or CH,
- R1 is Ar or Het,
- R2 is [C(R3)2]pHet1 or [C(R3)2]pN(R3)2,
- each R3 is independently H or alkyl with 1, 2, 3, or 4 C-atoms, which is optionally substituted;
- Ar is phenyl which is unsubstituted or mono-, di- or trisubstituted by Hal, A, phenyl, CON(R3)2, COOR3, NHCOA, NHSO2A, CHO, COA, SO2N(R3)2, SO2A, [C(R3)2]pOR3, [C(R3)2]pN(R3)2 and/or [C(R3)2]pCN,
- Het is furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, triazolyl, tetrazolyl, pyridyl, pyrimidyl, pyridazinyl, pyrazinyl, indolyl, isoindolyl, benzimidazolyl, indazolyl or quinolyl, which is unsubstituted or mono-, di- or trisubstituted by Hal, A, [C(R3)2]pOR3, [C(R3)2]pN(R3)2, NO2, CN, [C(R3)2]pCOOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)mA and/or O[C(R3)2]qN(R3)2,
- Het1 is dihydropyrrolyl, pyrrolidinyl, azetidinyl, oxetanyl, tetrahydroimidazolyl, dihydropyrazolyl, tetrahydropyrazolyl, tetrahydrofuranyl, dihydropyridyl, tetrahydropyridyl, piperidinyl, azepanyl, morpholinyl, hexahydropyridazinyl, hexahydropyrimidinyl, [1,3]dioxolanyl, tetrahydropyranyl, pyridyl or piperazinyl, which is unsubstituted or mono- or disubstituted by A,
- each A is independently unbranched or branched alkyl with 1-10 C-atoms, wherein one or two non-adjacent CH- and/or CH2-groups may be replaced by N-, O- and/or S-atoms and wherein 1-7 H-atoms may be replaced by F or Cl,
- each Hal is independently F, Cl, Br or I,
- each m is independently 0, 1 or 2,
- each n is independently 0, 1 or 2,
- each p is independently 0, 1, 2, 3 or 4,
- each q is independently 2, 3 or 4.
16 more elements
Dependencies are inferred from the claim text.