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, a stereoisomer or a solvate thereof: X and Y are each independently O or S; A and B are each independently CR6, R6 is hydrogen, halogen, cyano, hydroxy, carboxyl, —(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, —(CH2)nN(R8a)C(O)R9, C1-6alkyl or C1-6alkoxy, wherein C1-6alkyl and C1-6alkoxy may be optionally substituted with 1-3 substituents selected from halogen, hydroxy and carboxyl; R1 is hydrogen, C1-6alkyl, C2-8alkenyl, C2-8alkynyl, C3-8cycloalkyl, 6- to 14-membered aryl, 5- to 14-membered heteroaryl, 3- to 14-membered heterocyclic group, 7- to 12-membered spirocyclic group, or 7- to 12-membered bridge group, all of which except hydrogen may be optionally substituted with 1-5 R7a(s); R2 is hydrogen, C1-6alkyl, C2-8alkenyl, C2-8alkynyl, C3-8cycloalkyl, 6- to 14-membered aryl, 5- to 14-membered heteroaryl, 3- to 14-membered heterocyclic group, 7- to 12-membered spirocyclic group, or 7- to 12-membered bridge group, all of which except hydrogen may be optionally substituted with 1-5 R7b(s); R3 is hydrogen, carboxyl, or C1-6alkyl, wherein C1-6alkyl may be optionally substituted with 1-3 substituents selected from halogen, hydroxy and carboxyl; R4 is hydrogen, C3-8cycloalkyl, 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, C2-8alkenyl, C2-8alkynyl, or C1-6alkoxy, all of which may be optionally substituted with 1-3 substituents selected from halogen, hydroxy, and cyano, or (3) C3-8cycloalkyl, 6- to 14-membered aryl, 5- to 14-membered heteroaryl, or 3- to 14-membered heterocyclic group, all of which may be optionally substituted with 1-3 substituents selected from halogen, hydroxy, cyano, trifluoromethyl, C1-6alkyl, C2-8alkenyl, C2-8alkynyl, 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, C1-6alkyl, C3-8cycloalkyl, 6- to 14-membered aryl, 5- to 14-membered heteroaryl, or 3- to 14-membered heterocyclic group, all of which except hydrogen may be optionally substituted with 1-3 substituents selected from hydroxy, halogen, cyano, carboxyl, —(CH2)nNR8aR8b, sulfamoyl, carbamoyl, and sulfamino; R9 is hydrogen, C1-6alkyl, or C1-6alkoxy, all of which except hydrogen may be optionally substituted with 1-3 substituents selected from halogen, cyano, hydroxy, carboxyl, —(CH2)nNR8aR8b, sulfamoyl, and carbamoyl; m is 0, 1 or 2; and n is 0-4.