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US 8,772,481 B2Granted
Aza- and diaza-phthalazine compounds as P38 map kinase modulators and methods of use thereof
AssigneeAmgen Inc.
InventorsAndrew Tasker, Liping H. Pettus, Ryan Wurz
Life of this patent
Estimating the term…
Abstract
The present invention comprises a new class of compounds useful for the prophylaxis and treatments of protein kinase mediated diseases, including inflammation and related conditions.
Claims13
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein
- each of A1, A2, and A3, independently, is CR3 or N, provided that at least one of A1, A2, and A3, independently, is N;
- A4 is CR5 or N;
- L is O, S or NR4,
- R1 is C1-10-alkyl, —OC1-10-alkyl, —NHC1-10-alkyl, —N(C1-10-alkyl)2, C2-10-alkenyl, C2-10-alkynyl or C3-10-cycloalkyl, each of the C1-10-alkyl, —OC1-10-alkyl, —NHC1-10-alkyl, —N(C1-10-alkyl)2, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl and C4-10-cycloalkenyl, each of which is optionally comprising 1-4 heteroatoms selected from N, O and S and optionally substituted with 1-5 substituents of R6;
- or R1 is a 3-8 membered monocyclic or 6-12 membered bicyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic or 1-6 heteroatoms if bicyclic, said heteroatoms selected from O, N, or S, wherein said ring system is optionally substituted independently with 1-5 substituents of R6;
- R2 is H, F, Cl, Br, CF3, NO2, CN, C1-3-alkyl, C1-3-alkoxyl, C1-3-thioalkyl, C1-3-aminoalkyl;
- each R3, independently, is H, F, Cl, Br, CF3, NO2, CN, OH, C1-3-alkyl, C1-3-alkoxyl, C1-3-thioalkyl, C1-3-aminoalkyl or acetyl;
- R4 is H or C1-3-alkyl;
- each R5, independently, is H, F, Br, Cl, I, haloalkyl, NO2, CN, C1-6-alkyl, C1-6-alkoxyl, C1-6-thioalkyl, C1-6-aminoalkyl or di-C1-6-aminoalkyl;
- each R6, independently, is halo, haloalkyl, CN, OH, NO2, NH2, acetyl, oxo, C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl, —S(O)2C1-10-alkyl, —C(O)NHC1-10-alkyl, —C(O)NH2, a saturated or partially or fully unsaturated 5-8 membered monocyclic, 6-12 membered bicyclic, or 7-14 membered tricyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic, 1-6 heteroatoms if bicyclic, or 1-9 heteroatoms if tricyclic, said heteroatoms selected from O, N, or S or —C(O)— saturated or partially or fully unsaturated 3-8 membered monocyclic or 6-12 membered bicyclic ring system, said ring system formed of carbon atoms optionally including 1-3 heteroatoms if monocyclic or 1-6 heteroatoms if bicyclic, said heteroatoms selected from O, N, or S, wherein each of the C1-10-alkyl, C2-10-alkenyl, C2-10-alkynyl, C3-10-cycloalkyl, C4-10-cycloalkenyl, C1-10-alkylamino-, C1-10-dialkylamino-, C1-10-alkoxyl, C1-10-thioalkoxyl and each ring of said ring system and —C(O)-ring system is optionally substituted independently with 1-3 substituents of halo, haloalkyl, CN, NO2, NH2, OH, oxo, methyl, methoxyl, ethyl, ethoxyl, propyl, propoxyl, isopropyl, cyclopropyl, butyl, isobutyl, tert-butyl, methylamine, dimethylamine, ethylamine, diethylamine, propylamine, isopropylamine, dipropylamine, diisopropylamine, benzyl or phenyl;
- and
- m is 0, 1, 2, 3 or 4.
10 more elements
Dependencies are inferred from the claim text.