Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
1. A method of treating graft versus host disease in a patient in need thereof, comprising administering to the patient a pharmaceutical composition comprising a compound, which is 3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier; wherein the composition is suitable for oral administration and for providing sustained release of the compound or the salt.
2. The method of claim 1 , wherein the compound is (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof.
3. The method of claim 2 , wherein the composition is a unit dosage form.
4. The method of claim 3 , wherein the unit dosage form is a tablet.
5. The method of claim 3 , wherein the unit dosage form is a capsule.
6. The method of claim 3 , wherein the unit dosage form further comprises an enteric coating.
7. The method of claim 3 , wherein the unit dosage form comprises from about 5 to about 1000 mg of the compound or the salt.
8. The method of claim 2 , wherein the composition further comprises one or more excipients selected from lactose, dextrose, sucrose, sorbitol, mannitol, starches, gum acacia, calcium phosphate, alginates, tragacanth, gelatin, calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose, water, syrup, and methyl cellulose.
9. The method of claim 2 , wherein the composition further comprises microcrystalline cellulose.
10. The method of claim 2 , wherein the composition further comprises lactose.
11. The method of claim 2 , wherein the composition further comprises microcrystalline cellulose and lactose.