7 153 959

7,153,959 Title:

Substituted pyrazoles as p38 kinase inhibitors

Abstract:

A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as described in the specification.

Claims:

We claim:

1. A process for preparing a pyrazole corresponding in structure to: ##STR05890## comprising the steps: a. condensing a ketone corresponding in structure to: ##STR05891## with ahydrazine corresponding in structure to: NH.sub.2 to form a hydrazide corresponding in structure to: ##STR05892## b. contacting a hydrazide with an acyl halide corresponding in structure to: ##STR05893## to form an acyl hydrazone corresponding instructure to: ##STR05894## to form the pyrazole.

2. A process for preparing a pyrazole corresponding in structure to: ##STR05895## comprising the steps: a. contacting a ketone corresponding in structure to: ##STR05896## with an acyl hydrazide corresponding in structure to: ##STR05897## toform an acyl hydrazone corresponding in structure to: ##STR05898## to form the pyrazole.

3. A process for preparing a pyrazole corresponding in structure to: ##STR05899## comprising contacting a ketone corresponding in structure to: ##STR05900## with an acyl hydrazide corresponding in structure to: ##STR05901## to form thepyrazole.

4. A process according to claim 2 wherein the acyl hydrazone is heated to a temperature of from about 180.degree. C. to about 200.degree. C.

5. The process of claim 3 wherein the treatment of the ketone with the acyl hydrazide is carried out in an acidic solvent.

6. The process of claim 5 wherein the acidic solvent is acetic acid.

7. The process of claim 5 wherein the acidic solvent is an organic solvent containing an acid.

8. A process according to claim 1 wherein the acyl hydrazone is heated to a temperature of from about 180.degree. C. to about 200.degree. C.

9. A process according to claim 2 wherein the contacting of the ketone with the acyl hydrazide is performed at a temperature from about 25.degree. C. to about 200.degree. C.