Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as AXL inhibitors
View Patent ↗Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
1. A compound which is N 3 -(3-(bicyclo[2.2.1]heptan-2-yl)-1,2,3,4,5,6-hexahydrobenzo[d]azocin-8-yl)-1-(2-chloro-7-methylthieno[3,2-d]pyrimidin-4-yl)-1H-1,2,4-triazole-3,5-diamine, as an isolated stereoisomer or a mixture of stereoisomers, or a pharmaceutically acceptable salt thereof.
2. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and the compound of claim 1 , as an isolated stereoisomer or a mixture of stereoisomers, or a pharmaceutically acceptable salt thereof.
3. A method of inhibiting Axl activity in a mammal, comprising administering to the mammal an effective amount of the compound of claim 1 , as an isolated stereoisomer or a mixture of stereoisomers, or a pharmaceutically acceptable salt thereof.
4. The method of claim 3 wherein the inhibition of Axl activity in the mammal alleviates a disease or condition in the mammal.
5. The method of claim 4 wherein the disease or condition is selected from the group consisting of rheumatoid arthritis, vascular disease, vascular injury, psoriasis, visual impairment due to macular degeneration, diabetic retinopathy, retinopathy of prematurity, kidney disease, osteoporosis, osteoarthritis and cataracts.
6. The method of claim 4 , wherein a manifestation of the disease or condition is solid tumor formation in the mammal.
7. The method of claim 6 , wherein the disease or condition is selected from the group consisting of breast carcinoma, renal carcinoma, endometrial carcinoma, ovarian carcinoma, thyroid carcinoma, non-small cell lung carcinoma, melanoma, prostate carcinoma, sarcoma, gastric cancer and uveal melanoma.
8. The method of claim 6 , wherein a manifestation of the disease or condition is liquid tumor formation in the mammal.
9. The method of claim 8 , wherein the disease or condition is myeloid leukemia or lymphoma.
10. The method of claim 4 wherein the disease or condition is endometriosis.