PI3K and/or mTOR inhibitor

摘要

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, a stereoisomer or a solvate thereof, wherein R1, R2, R3, R4, X, Y, A and B are as defined in the specification. The present invention further relates to a method for preparing these compounds, a pharmaceutical composition containing these compounds, and a use of these compounds in manufacture of a medicament for treating and/or preventing proliferative diseases.;

主权项

1. A compound of formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof:wherein
X and Y are each O; A and B are each CH; R1 is 6- to 10-membered aryl, 5- to 6-membered monocyclic heteroaryl, 9- to 10-membered fused heteroaryl, 5- to 6-membered monocyclic heterocyclic group, or 9- to 10-membered fused heterocyclic group, all of which may be optionally substituted with 1-3 R7a(s); R2 is 6- to 10-membered aryl, 5- to 6-membered monocyclic heteroaryl, 9- to 10-membered fused heteroaryl, 5- to 6-membered monocyclic heterocyclic group, or 9- to 10-membered fused heterocyclic group, all of which may be optionally substituted with 1-3 R7b(s); R3 is hydrogen; R4 is hydrogen or C1-6alkyl, wherein C1-6alkyl may be optionally substituted with 1-3 substituents selected from halogen, hydroxy and carboxyl; R7a and R7b are each independently (1) halogen, cyano, hydroxy, —(CH2)nNR8aR8b, —(CH2)nC(O)R9, —(CH2)nS(O)mR9, —(CH2)nS(O)mNR8aR8b, —(CH2)nN(R8a)S(O)mR9, —(CH2)nC(O)NR8aR8b, —(CH2)nOC(O)R9, —(CH2)nC(O)(CH2)nOR9, or —(CH2)nN(R8a)C(O)R9, (2) C1-6alkyl or C1-6alkoxy, both of which may be optionally substituted with 1-3 substituents selected from halogen, hydroxy and cyano, or; (3) 5- to 10-membered heteroaryl or 5- to 10-membered heterocyclic group, both of which may be optionally substituted with 1-3 substituents selected from halogen, hydroxy, cyano, trifluoromethyl, C1-6alkyl, C1-6alkoxy, —(CH2)nNR8aR8b, —(CH2)nC(O)R9, —(CH2)nC(O)NR8aR8b, —(CH2)nS(O)mR9, —(CH2)nS(O)mNR8aR8b, —(CH2)nN(R8a)S(O)mR9, —(CH2)nOC(O)R9, and —(CH2)nN(R8a)C(O)R9; R8a and R8b are each independently hydrogen or C1-6alkyl; R9 is hydrogen or C1-6alkyl, wherein C1-6alkyl may be optionally substituted with 1-3 substituents selected from halogen, cyano, hydroxy, and —NR8aR8b; m is 0, 1 or 2; and n is 0-3.