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US 7,531,566 B2Granted
Anti-inflammatory medicaments
AssigneeDeciphera Pharmaceuticals, LLC
InventorsDaniel L. Flynn, Peter A. Petillo
Life of this patent
Estimating the term…
Abstract
Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.
Claims8
A method of modulating the activation state of p38 α-kinase comprising the step of contacting said kinase with a molecule having the formula
- wherein:
- R1 is selected from the group consisting of
- each R2 is individually selected from the group consisting of —H, alkyls, aminos, alkylaminos, arylaminos, cycloalkylaminos, heterocyclylaminos, halogens, alkoxys, and hydroxys;
- each R3 is individually selected from the group consisting of —H, alkyls, alkylaminos, arylaminos, cycloalkylaminos, heterocyclylaminos, alkoxys, hydroxys, cyanos, halogens, perfluoroalkyls, alkylsulfinyls, alkylsulfonyls, R4NHSO2—, and —NHSO2R4;
- each R5 is individually selected from the group consisting of —H, alkyls, aryls, heterocyclyls, alkylaminos, arylaminos, cycloalkylaminos, heterocyclylaminos, hydroxys, alkoxys, aryloxys, alkylthios, arylthios, cyanos, halogens, perfluoroalkyls, alkylcarbonyls, and nitros;
- and each W is individually selected from the group consisting of CH and N;
- each X is individually selected from the group consisting of —O—, —S—, —NR6—, —NR6SO2—, —NR6CO—, alkynyls, alkenyls, alkylenes, —O(CH2)h—, and —NR6(CH2)h—, where each h is individually selected from the group consisting of 1, 2, 3, or 4, and where for each of alkylenes, —O(CH2)h—, and —NR6(CH2)h—, one of the methylene groups present therein may be optionally double-bonded to a side-chain oxo group except that where —O(CH2)h—the introduction of the side-chain oxo group does not form an ester moiety;
- A is selected from the group consisting of phenyl, naphthyl, pyridyl, pyrimidyl, thienyl, furyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, indolyl, indazolyl, benzimidazolyl, benzotriazolyl, isoquinolyl, quinolyl, benzothiazolyl, benzofuranyl, benzothienyl, pyrazolylpyrimidinyl, imidazopyrimidinyl, purinyl, and
- where each W1 is individually selected from the group consisting of —CH— and —N—;
- D is phenyl or a five-membered heterocyclic ring selected from the group consisting of pyrazolyl, pyrrolyl, imidazolyl, oxazolyl, and thiazolyl;
- G is —CH2—;
- L is —C(O)—;
- j is 0 or 1;
- m is 0 or 1;
- n is 0 or 1;
- Q is
- each R4 group is individually selected from the group consisting of —H, alkyls, aminoalkyls, alkoxyalkyls, aryls, aralkyls, heterocyclyls, and heterocyclylalkyls except when the R4 substituent places a heteroatom on an alpha-carbon directly attached to a ring nitrogen on Q;
- when two R4 groups are bonded with the same atom, the two R4 groups optionally form an alicyclic or heterocyclic 4-7 membered ring;
- each R6 is individually selected from the group consisting of —H, alkyls, allyls, and β-trimethylsilylethyl;
- each Z is individually selected from the group consisting of —O— and —N(R4)—;
- each ring of formula (I) optionally includes one or more of R7, where R7 is a noninterfering substituent individually selected from the group consisting of —H, alkyls, aryls, heterocyclyls, alkylaminos, arylaminos, cycloalkylaminos, heterocyclylaminos, hydroxys, alkoxys, aryloxys, alkylthios, arthylthios, cyanos, halogens, nitrilos, nitros, alkylsulfinyls, alkylsulfonyls, aminosulfonyls, and perfluoroalkyls.
18 more elements
Dependencies are inferred from the claim text.