Pfizer Corporation

Other

Paul S Changelian

Matthew Frank Brown

Mark Edward Flanagan

Todd A Blumenkopf

David R Anderson

Eric Jon Jacobsen

James Robert Blinn

Paramita Mukherjee

Canxin Xu

The present invention relates to new pyrrolopyridine compounds having the structures of Formula (I)-(IV), wherein the R groups, A, B, C, D and n are as defined in the detailed description, and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of JAK kinase activity in a human or animal subject are also provided for the treatment diseases such as pruritus, alopecia, androgenetic alopecia, alopecia areata, vitiligo and psoriasis.

Substituted pyrrolopyridines as JAK inhibitors

A compound of the formula wherein R, Rand Rare as defined above, which are inhibitors of the enzyme protein tyrosine kinases such as Janus Kinase 3 and as such are useful therapy as immunosuppressive agents for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type 1 diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases.

Pyrrolo[2,3-d]pyrimidine compounds

A method of treating or preventing chronic organ transplant rejection comprising administering a compound of the formula wherein R, Rand Rare as defined above.

Method of treatment of transplant rejection

A compound of the formulawherein R, Rand Rare as defined above, which are inhibitors of the enzyme protein tyrosine kinases such as Janus Kinase 3 and as such are useful therapy as immunosuppressive agents for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases.

Pyrrolo [2,3-D] pyrimidine compounds

Novel pyrrolo&lsqb;2,3-d&rsqb;pyrimidine compounds useful as inhibitors of the enzyme protein tyrosine kinases such as Janus Kinase 3 as well as immunosuppressive agents for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases are described.

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E. Greenwich, CT, United States of America

Paul S Changelian