Back to results
US 8,273,890 B2Granted
Thiophene-imidazopyridines
Assignee4Sc AG
InventorsThomas Stengel, Mathias Schmidt, Steffen Weinbrenner, Alexander Weber, Petra Gimmnich, Volker Gekeler, Thomas Beckers, Astrid Zimmermann, Thomas Maier, Beate Schmidt, Florian Dehmel
Life of this patent
Estimating the term…
Abstract
The invention relates to thiophene-imidazopyridine compounds according to formula (I), wherein the substituents and symbols are as defined in the description. The compounds are inhibitors of PIk1.
Claims19
A compound of formula (I)
- wherein
- R1 is —CH2N(R3)R4;
- R2 is phenyl optionally having 1 to 3 substituents independently selected from the group consisting of —F, —Cl, —Br, —I, —CN, —OH, —NO2, —SO2CH3, C1-C4 alkyl optionally being substituted with 1 to 3 F atoms, C1-C4 alkoxy optionally being substituted with 1 to 3 F atoms, C1-C4 alkylamino, and C1-C4 dialkylamino;
- Y is —OH or —NH2;
- R3 and R4 together with the nitrogen atom they are bound to, form a saturated four- to seven-membered heterocycle,
- the heterocycle optionally containing one more heteroatoms selected from the group consisting of N, O and S, wherein S is optionally oxidized to a —SO— group or a —SO2— group,
- and the heterocycle optionally being substituted by one or two substituents which independently are —OH, —F, amino, C1-C4 alkylamino, C1-C4 dialkylamino, C1-C4 alkyl optionally being substituted with 1 to 3 F atoms, C1-C4 acyl, benzoyl, phenoxy, 1-carboxamidyl optionally being substituted with C1-C4 alkyl or phenyl, 1-carboximidamidyl, sulfonyl optionally being substituted with C1-C4 alkyl or phenyl, 2-aminoethyl, 2-N—(C1-C4 alkyl)aminoethyl, 2-N,N-di(C1-C4 alkyl)aminoethyl, phenyl, pyridyl, pyrimidyl, benzyl, allyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyanomethyl, 2-cyanoethyl, 2-methansulfonylethyl, hydroxymethyl, 2-hydroxyethyl, 3-hydroxypropyl, (C1-C4 alkoxy)methyl, 2-(C1-C4 alkoxy)ethyl, 3-(C1-C4 alkoxy)propyl, N-methylpiperidyl, 1-phenylethyl, pyridylmethyl, N-methylpiperidylmethyl, 2-morpholinylethyl, morpholinocarbonylethyl, N,N-dimethylcarbonylmethyl, anilinocarbonylmethyl, N-methylanilinocarbonylmethyl, N-pyrrolidinocarbonylmethyl, N,N-dimethylsulfonyl, N-methylpiperazinyl, N-methylpiperazinylcarbonyl, or oxo, and
- R7 is —H, methyl, ethyl, —CH2OH or —CF3;
- or a salt thereof.
6 more elements
A compound, which is
- 5-{6-[(Cyclopropylamino)methyl]-1H-imidazo[4,5-c]pyridin-1-yl}-3-{[2-(trifluoromethyl)benzyl]oxy}thiophene-2-carboxamide, or
- 5-{6-[(4-Methylpiperazin-1-yl)methyl]-1H-imidazo[4,5-c]pyridin-1-yl}-3-{[2-(trifluoromethyl)benzyl]oxy}thiophene-2-carboxamide,
- or a salt thereof.
Dependencies are inferred from the claim text.