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Claims for Patent: 6,956,041

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Claims for Patent: 6,956,041

Title: Pyrrolo[2,3-d]pyrimidine compounds
Abstract:A compound of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, which are inhibitors of the enzyme protein kinases such as Janus Kinase 3 and as such are useful therapy as immunosuppressive agents for organ transplants, xeno transplation, 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.
Inventor(s): Blumenkopf; Todd A. (Old Lyme, CT), Flanagan; Mark E. (Gales Ferry, CT), Munchhof; Michael J. (Salem, CT)
Assignee: Pfizer Inc. (New York, NY)
Application Number:10/640,227
Patent Claims: 1. A pharmaceutical composition comprising a compound selected from the group consisting of: Methyl-[4-methyl-1-(propane-1-sulfonyl)-piperidin-3-yl]-(7H-pyrrolo[2,3-d]p yrimidin-4-yl)-amine; 4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidine-1-ca rboxylic acid methyl ester; 3,3,3-Trifluoro-1-{4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-am ino]-piperidin-1-yl}-propan-1-one; 4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidine-1-ca rboxylic acid dimethylamide; 3-{4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1- yl}-3-oxo-propionitrile; 3,3,3-Trifluoro-1-{4-methyl-3-[methyl-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin- 4-yl-amino]-piperidin-1-yl}-propan-1-one; 1-{4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1- yl}-but-3-yn-1-one; 1-{3-[(5-Chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-methyl-amino]4-methyl-pipe ridin-1-yl}-propan-1-one; and 1-{3-[(5-Fluoro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-methyl-amino]4-methyl-pipe ridin-1-yl}-propan-1-one; or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.

2. The pharmaceutical composition of claim 1, wherein said compound is 3-{4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4yl)amino]-piperidin-1-y l}-3-oxo-propionitrile, or pharmaceutically acceptable salt thereof.

3. The pharmaceutical composition of any one of claim 1 or 2, further comprising one or more additional agents is selected from the group consisting of cyclosporin A, rapamycin, tacrolimus, leflunomide, deoxyspergualin, mycophenolate, azathioprine, daclizumab, muromonab-CD3, antithymocyte globulin, aspirin, acetaminophen, ibuprofen, naproxen, piroxicam, and anti-inflammatory steroid.

4. A method for the inhibition of Janus Kinase 3 (JAK3) in a mammal, including a human, comprising administering to said mammal an effective amount of a compound selected from the group consisting of: Methyl-[4-methyl-1-(propane-1-sulfonyl)-piperidin-3-yl]-(7H-pyrrolo[2,3-d]p yrimidin-4-yl)-amine; 4-Methyl-3-[methy1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidine-1-ca rboxylic acid methyl ester; 3,3,3-Trifluoro-1-{4-methyl-3-[methyl-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin- 4-yl)-amino]-piperidin-1-yl}-propan-1-one; 4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidine-1-ca rboxylic acid dimethylamide; 3-{4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4 -yl)-amino]-piperidine-1-yl}-3-oxo-propionitrile; 3,3,3-Trifluoro-1-{4-methyl-3-[methyl-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin- 4-yl-amino]-piperidin-1-yl}-propan-1-one; 1-{4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidine-1 -yl}-but-3-yn-1-one; 1-{3-[(5-Chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-methyl-amino]4-methyl-pipe ridin-1-yl}-propan-1-one; and 1-{3-[(5-Fluoro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-methyl-amino]4-methyl-pipe ridin-1-yl}-propan-1-one; or a pharmaceutically acceptable salt thereof.

5. The method of claim 4 wherein, said compound is 3-{4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1 -yl}-3-oxo-propionitrile, or pharmaceutically acceptable salt thereof.
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