| 摘要 |
592608 Disclosed are 4-amino-pyrazolo[3,4-d]pyrimidine derivatives as represented by the general formula II-A-1, or a pharmaceutically acceptable salt thereof, wherein: X1 and X2 are N; R1 is hydrogen, -L-alkyl, -L-cycloalkyl, -L-alkylheterocyclyl, -L-heteroalkyl, or -L-heterocyclyl, each of which is unsubstituted or substituted by one or more independent R3 substituents; L is a bond, C=O, -C(=O)O-, -C(=O)N(R31)-, -S-, -S(O)-, -S(O)2-, -S(O)2N(R31)-, or -N(R31)-; E2 is H; each of R31 and R32 are independently H or unsubstituted alkyl; wherein heterocyclyl is a substituted or unsubstituted 3-, 4-, 5-, or 6- membered saturated or partially unsaturated ring containing one, two, or three heteroatoms independently selected from oxygen, nitrogen and sulfur; or to a bicyclic ring system containing up to 10 atoms including at least one heteroatom independently selected from oxygen, nitrogen, and sulfur wherein the ring containing the heteroatom is saturated; and wherein the remaining substituents are as defined herein. Representative compounds include 4-amino-1-(1-hydroxy-2-methyl-propan-2-yl)-3-(2-amino-1,3-benzoxazol-5-yl)-pyrazolo[3,4-d]pyrimidine. Also disclosed is a pharmaceutical composition which comprises a compound or pharmaceutically acceptable salt as defined above, and further comprising a pharmaceutical excipient, for inhibiting activity of a protein kinase and/or a lipid kinase present in a cell, such as mTor, and for the treatment of cancer, bone disorder, inflammatory disease, immune disease, nervous system disease, metabolic disease, respiratory disease, and cardiac disease. |
