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US 7,342,037 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.
Claims13
A compound having the formula
- wherein:
- 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 selected from the group consisting of phenyl, pyrazolyl, pyrrolyl, imidazolyl, oxazolyl, thiazolyl, furyl, oxadiazolyl, thiadiazolyl, thienyl, pyridyl, and pyrimidyl;
- G is —CH2—, N(R6), O;
- 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 and alkyls;
- each Z is individually selected from the group consisting of —O— and —N(R4)—;
- R7″ is selected from the group consisting of alkyls, aryls, heterocyclyls, and perfluoroalkyls;
- wherein A or Q is optionally substituted with one or more R7′ substituents selected from the group consisting of —H, alkyls, aryls, heterocyclyls, alkylaminos, arylaminos, cycloalkylaminos, heterocyclylaminos, hydroxys, alkoxys, aryloxys, alkylthios, arthylthios, cyanos, halogens, nitros, alkylsulfinyls, alkylsulfonyls, aminosulfonyls, and perfluoroalkyls;
- and each R9′ is individually and independently selected from the group consisting of F and alkyls, wherein when two R9′ groups are alkyl groups, said alkyl groups may be cyclized to form a 3-6 membered ring.
10 more elements
A method of modulating the activation state of a p38-alpha kinase comprising the step of contacting said kinase with a molecule having the formula
- wherein:
- 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 selected from the group consisting of phenyl, pyrazolyl, pyrrolyl, imidazolyl, oxazolyl, thiazolyl, furyl, oxadiazolyl, thiadiazolyl, thienyl, pyridyl, and pyrimidyl;
- G is —CH2—, N(R6), O;
- 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)—;
- R7″ is selected from the group consisting of alkyls, aryls, heterocyclyls, and perfluoroalkyls;
- wherein A or Q is optionally substituted with one or more R7′ substituents selected from the group consisting of —H, alkyls, aryls, heterocyclyls, alkylaminos, arylaminos, cycloalkylaminos, heterocyclylaminos, hydroxys, alkoxys, aryloxys, alkylthios, arthylthios, cyanos, halogens, nitros, alkylsulfinyls, alkylsulfonyls, aminosulfonyls, and perfluoroalkyls;
- and each R9′ is individually and independently selected from the group consisting of F and alkyls, wherein when two R9′ groups are alkyl groups, said alkyl groups may be cyclized to form a 3-6 membered ring.
10 more elements
An adduct comprising a molecule bound with a kinase, said molecule having the formula
- wherein:
- 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 selected from the group consisting of phenyl, pyrazolyl, pyrrolyl, imidazolyl, oxazolyl, thiazolyl, furyl, oxadiazolyl, thiadiazolyl, thienyl, pyridyl, and pyrimidyl;
- G is —CH2—, N(R6), O;
- 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)—;
- R7″ is selected from the group consisting of alkyls, aryls, heterocyclyls, and perfluoroalkyls;
- wherein A or Q is optionally substituted with one or more R7′ substituents selected from the group consisting of —H, alkyls, aryls, heterocyclyls, alkylaminos, arylaminos, cycloalkylaminos, heterocyclylaminos, hydroxys, alkoxys, aryloxys, alkylthios, arthylthios, cyanos, halogens, nitros, alkylsulfinyls, alkylsulfonyls, aminosulfonyls, and perfluoroalkyls;
- and each R9′ is individually and independently selected from the group consisting of F and alkyls, wherein when two R9′ groups are alkyl groups, said alkyl groups may be cyclized to form a 3-6 membered ring.
10 more elements
Dependencies are inferred from the claim text.