主权项 |
1. A compound of formula Ior a pharmaceutically acceptable salt thereof, wherein:
each of X1 and X2, independently, is N, CH, or CR4; L1 is a bond, —C(O)—, —C(O)—O—, —S(O)2—, —C(O)N(Ra)—, or —S(O)2N(Ra)—; wherein each Ra, independently, is hydrogen or C1-4 alkyl; wherein when L1 is a bond and R3 is phenyl, naphthyl, or heteroaryl, R2 optionally joins with R7 to form an optionally substituted 5-7-membered heterocyclyl or an optionally substituted 5-6-membered heteroaryl; R1 is hydrogen or -L2-R6 wherein:
L2 is C1-4 alkylene, —C(O)—, —C(O)—O—, —S(O)—, —S(O)2—, —C(O)N(Rb)—, or —S(O)2N(Rb)—; wherein each Rb, independently, is hydrogen or C1-4 alkyl; andR6 is hydrogen, C1-6 aliphatic, 3-10-membered cycloaliphatic, phenyl, naphthyl, 3-10-membered heterocyclyl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or 5-10-membered heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of which being optionally substituted with 1-5 R7; or Rb and R6 combine to form a 3-10-membered heterocyclyl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur wherein said heterocyclyl is optionally substituted with 1-5 R7; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen, C1-6 aliphatic, 3-10-membered cycloaliphatic, phenyl, naphthyl, 3-10-membered heterocyclyl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or 5-10-membered heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; provided that if R3 is hydrogen, L1 is a bond; each of R3 being optionally substituted with 1-5 R7 wherein:
each R7 independently is —CN, halo, or -L3-R8 wherein:
L3 is a bond, C1-4 aliphatic, —O—, —N(Rc)—, —S—, —S(O)—, —S(O)2—, —C(O)—, —C(O)O—, —C(O)N(Rc)—, —N(Rc)C(O)—, —N(Rc)C(O)O—, —S(O)2NRc, —N(Rc)S(O)2—, —OC(O)N(Rc)—, —N(Rc)C(O)N(Rd)—, —N(Rc)S(O)2N(Rd)—, or —OC(O)—;each occurrence of Rc and Rd, independently, is hydrogen or C1-4 alkyl, andR8 is hydrogen, C1-6 aliphatic, 3-10-membered cycloaliphatic, phenyl, naphthyl, 3-10-membered heterocyclyl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or 5-10-membered heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each occurrence of R4 and R5, independently, is —CN, halo, or -L4-R9 wherein:
L4 is C1-4 alkylene, —O—, —N(Re)—, —S—, —S(O)—, —S(O)2—, —C(O)—, —CO2—, —C(O)N(Re)—, —N(Re)C(O)—, —N(Re)C(O)O—, —S(O)2N(Re)—, —N(Re)S(O)2—, —OC(O)N(Re)—, —N(Re)C(O)N(Rf)—, —N(Re)S(O)2N(Rf)—, or —OC(O)—;each occurrence of Re and Rf, independently, is hydrogen or C1-4 alkyl; andR9 is hydrogen, —NH2, or C1-6 aliphatic; m is 0-2; and n is 0-3. |