IP Library Granted Patent US 7,144,911
Granted Patent B2
US 7,144,911 · App. 10/746,460 · Granted Dec 5, 2006

Anti-inflammatory medicaments

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Quick Facts
Patent No.
US 7,144,911
App. No.
10/746,460
Granted
Dec 5, 2006
Kind
B2
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.

Claims (28)

1. A compound having the formula

wherein:

R 1 is selected from the group consisting of

each R 2 is individually selected from the group consisting of —H, alkyls, aminos, alkylaminos, arylaminos, cycloalkylaminos, heterocyclylaminos, halogens, alkoxys, and hydroxys;

each R 3 is individually selected from the group consisting of —H, alkyls, alkylaninos, arylaminos, cycloalkylaminos, heterocyclylaminos, alkoxys, hydroxys, cyanos, halogens, perfluoroalkyls, alkylsulfinyls, alkylsulfonyls, R 4 NHSO 2 —, and —NHSO 2 R 4 ;

each R 5 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—, —NR 6 —, —NR 6 SO 2 —, —NR 6 CO—, alkynyls, alkenyls, alkylenes, —O(CH 2 ) h —, and —NR 6 (CH 2 ) h —, where each h is individually selected from the group consisting of 1, 2, 3, or 4, and where for each of alkylenes, —O(CH 2 ) h —, and —NR 6 (CH 2 ) h —, one of the methylene groups present therein may be optionally double-bonded to a side-chain oxo group except that where —O(CH 2 ) 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 W 1 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, thiazolyl;

G is —CH 2 —;

L is selected from the group consisting of —C(O)— and —S(O) 2 —;

j is 0 or 1;

m is 0 or 1;

n is 0 or 1;

Q is

each R 4 group is individually selected from the group consisting of —H, alkyls, aminoalkyls, alkoxyalkyls, aryls, aralkyls, heterocyclyls, and heterocyclylalkyls except when the R 4 substituent places a heteroatom on an alpha-carbon directly attached to a ring nitrogen on Q;

when two R 4 groups are bonded with the same atom, the two R 4 groups optionally form an alicyclic or heterocyclic 4–7 membered ring;

each R 6 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(R 4 )—;

each ring of formula (I) optionally includes one or more of R 7 , where R 7 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.

2. The compound of claim 1 , wherein m is 0; wherein D is substituted by a first R 7 substituent.

3. The compound of claim 2 , wherein A is phenyl substituted by one or more second R 7 substituents, said second R 7 substituents being halogens.

4. The compound of claim 2 , wherein A is an R 7 — substituted naphthyl.

5. The compound of claim 1 , wherein in is 1; R 1 is taken from the group consisting of

6. The compound of claim 5 , wherein A is taken from phenyl or naphthyl.

7. The compound of claim 1 having the formula IB

8. A compound of claim 1 having the formula IC

Assignments (2)
RELEASE OF SECURITY INTEREST Recorded Dec 24, 2015
From: BRIGHTSTAR ASSOCIATES, LLC
To: DECIPHERA PHARMACEUTICALS, LLC
Reel/Frame 037359/0866 →
SECURITY AGREEMENT Recorded Jul 5, 2012
From: DECIPHERA PHARMACEUTICALS, LLC
To: BRIGHTSTAR ASSOCIATES LLC
Reel/Frame 028503/0011 →