mTOR selective kinase inhibitors

摘要

The 4-urea-phenyl substituted 6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidine derivatives are potent and selective inhibitors of mTOR kinase and are useful in treating disorders related to abnormal mTOR activities such as cancer, immune disorders, cardiovascular disease, ocular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.

主权项

1. A compound of Formula II:or a salt thereof; wherein X is CH;
R1is 1 ) heterocyclyl optionally substituted with C(O)OR15, C(O)R16, or S(O)2R17; or 2) cycloalkyl optionally substituted with OH, C(O)OR15, or R17; R2 is hydrogen or alkyl; R3 is hydrogen; each R4 is independently 1) alkyl; or 2) aryl optionally substituted with R16 or C(O)R16; R5 is hydrogen; or each R2 and R5 together with the atom(s) that each is respectively attached to can form a cyclo or heterocyclo structure; R15 is hydrogen or C1-C4 alkyl; R16 is heterocyclyl or C1-C4 alkyl, wherein each of said heterocyclyl or C1-C4 alkyl is independently optionally substituted with OH, halogen, C1-C4 alkyl, C1-C4 alkoxy, or NH2; and R17 is C1-C4 alkyl optionally substituted with OH.