Back to results
US 9,315,517 B2Granted
Imidazol-piperidinyl 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 formula (I) in which R1, R2, X1, X2, X3, X4 and n have the meanings indicated in above, and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Claims16
A compound of formula (I),
- or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof,
- wherein:
- X1 is N or CH,
- X2 is CH2 or NH,
- X3 is CH2 or CO,
- X4 is O, CH2 or NH,
- R1 is Ar, Het, or unbranched or branched alkyl with 1-10 C-atoms, each of which is substituted by 1-6 of 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;
- R2 is [C(R3)2]pHet1 or A,
- each R3 is independently H or alkyl with 1, 2, 3, or 4 C-atoms,
- 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,
- with the proviso, that compounds are excluded wherein
- X2=NH, X3=CO and n=0.
17 more elements
Dependencies are inferred from the claim text.