| 主权项 |
1. A compound including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, said compound comprising Formula I:
A-L-CR (I) where:
CR is heteroaryl, wherein said heteroaryl is optionally substituted with one or more groups selected from halogen, hydroxyl, cyano, nitro, azido, —NR21SO2R24, —SO2NR21R22, —NR21S(O)R4, —S(O)NR21R22, —C(O)R21, —C(O)OR21, —OC(O)R21, —OC(O)OR21, —NR21C(O)OR24, —NR21C(═NR21)NR22R23, —NR21C(O)R22, —C(O)NR21R22, —SR21, —S(O)R24, —SO2R24, —NR21R22, —NR21C(O)NR22R23, —NR21C(NCN)NR22R23, —OR21, C1-C4 alkyl, C1-C6 heteroalkyl, C2-C6 alkenyl, C2-C6 heteroalkenyl, C2-C6 alkynyl, C2-C6 heteroalkynyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, aryl, heteroaryl, arylalkyl and heteroarylalkyl, wherein any of said alkyl, heteroalkyl, alkenyl, heteroalkenyl, alkynyl, heteroalkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, arylalkyl and heteroarylalkyl are further optionally substituted with one or more groups selected from halogen, hydroxyl, cyano, nitro, azido, fluoromethyl, difluoromethyl, trifluoromethyl, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 heteroalkyl, C2-C6 heteroalkenyl, C2-C6 heteroalkynyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, —SR21, —S(O)R24, —SO2R24, —C(O)R21, C(O)OR21, —C(O)NR21R22, —NR21R22 and —OR21;L is selected from: where R12 is hydrogen, halogen, hydroxy, cyano, nitro, amino, azido, C1-C5 alkyl, C2-C5 alkenyl, C2-C5 alkynyl, C1-C5 heteroalkyl, C2-C5 heteroalkenyl or C2-C5 heteroalkynyl, wherein any of said alkyl, alkenyl, alkynyl, heteroalkyl, heteroalkenyl, and heteroalkynyl are optionally substituted with one or more groups independently selected from halogen, cyano, nitro, amino, azido, C1-C4 alkyl, fluoromethyl, difluoromethyl, trifluoromethyl, methoxy, fluoromethoxy, difluoromethoxy and trifluoromethoxy; A isW is N or CR15, provided that when L is a substituted or unsubstituted piperazinylene, W must be CR15;G is hydrogen, alkyl, heteroalkyl, alkenyl, heteroalkenyl, alkynyl, heteroalkynyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, wherein any of said alkyl, heteroalkyl, alkenyl, heteroalkenyl, alkynyl, heteroalkynyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl is optionally substituted with one or more groups selected from halogen, hydroxyl, cyano, amino, nitro, azido, —NR21SO2R24, —SO2NR21R22, —NR21S(O)R4, —S(O)NR21R22, —C(O)R21, —C(O)OR21, —OC(O)R21, —OC(O)OR21, —NR21C(O)OR24, —NR21C(═NR21)NR22R23, —NR21C(O)R22, —C(O)NR21R22, —SR21, —S(O)R24, —SO2R24, —NR21R22, —NR21C(O)NR22R23, —NR21C(NCN)NR22R23, —OR21, C1-C4 alkyl, C1-C4 heteroalkyl, C2-C4 alkenyl, C2-C4 heteroalkenyl, C2-C4 alkynyl, C2-C4 heteroalkynyl, cycloalkyl, heterocycloalkyl aryl and heteroaryl;B1 and B2 are independently absent or C1-C4 alkylene, C1-C4 heteroalkylene, C2-C4 alkenylene, C2-C4 heteroalkenylene, C2-C4 alkynylene, C2-C4 heteroalkynylene, C3-C6 cycloalkylene, and C3-C6 heterocycloalkylene, wherein any of said alkylene, heteroalkylene, alkenylene, heteroalkenylene, alkynylene, heteroalkynylene, cycloalkylene or heterocycloalkylene is optionally substituted with one or more groups independently selected from halogen, hydroxyl, cyano, nitro, azido, C1-C4 alkyl, C1-C4 heteroalkyl, C2-C4 alkenyl, C2-C4 heteroalkenyl, C2-C4 alkynyl, C2-C4 heteroalkynyl, NR21R22 and OR21;R21, R22 and R23 independently are hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 heteroalkyl, C2-C6 heteroalkenyl, C2-C6 heteroalkynyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl;R24 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 heteroalkyl, C2-C6 heteroalkenyl, C2-C6 heteroalkynyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl;or any two of R21, R22, R23 or R24 together with the atom(s) to which they are attached form a 4 to 10 membered carbocyclic, aryl, heteroaryl or heterocyclic ring, wherein any of said carbocyclic, aryl, heteroaryl or heterocyclic rings are optionally substituted with one or more groups independently selected from halogen, cyano, nitro, trifluoromethyl, difluoromethoxy, trifluoromethoxy, azido, aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl, and heterocyclylalkyl;R13 and R14 are independently hydrogen, hydroxyl, cyano, C1-C6 alkyl, C1-C6 heteroalkyl, C2-C6 alkenyl, C2-C6 heteroalkenyl, C2-C6 alkynyl, C2-C6 heteroalkynyl, C1-C6 cycloalkyl, C1-C6 heterocycloalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, —C(O)R21, C(O)OR21, C(═NR21)NR22R23 or —SO2R24, wherein any of said alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, heteroalkyl, heteroalkenyl, heteroalkynyl, arylalkyl or heteroarylalkyl is optionally substituted with one or more groups independently selected from halogen, hydroxyl, cyano, amino, nitro, azido, —NR21SO2R24, —SO2NR21R22, —NR21S(O)R4, —S(O)NR21R22, —C(O)R21, —C(O)OR21, —OC(O)R21, —OC(O)OR21, —NR21C(O)OR24, —NR21C(═NR21)NR22R23, —NR21C(O)R22, —C(O)NR21R22, —SR21, —S(O)R24, —SO2R24, —NR21R22, —NR21C(O)NR22R23, —NR21C(NCN)NR22R23, —OR21, C1-C4 alkyl, C1-C4 heteroalkyl, C2-C4 alkenyl, C2-C4 heteroalkenyl, C2-C4 alkynyl, C2-C4 heteroalkynyl, cycloalkyl, heterocycloalkyl aryl and heteroaryl;or R13 and R14 together with the atoms to which they are attached form a 4 to 10 membered carbocyclic, aryl, heteroaryl or heterocyclic ring, wherein any of said carbocyclic, aryl, heteroaryl and heterocyclic rings are optionally substituted with one or more groups independently selected from halogen, cyano, nitro, azido, C1-C4 alkyl, C1-C4 heteroalkyl, C2-C4 alkenyl, C2-C4 heteroalkenyl, C2-C4 alkynyl, C2-C4 heteroalkynyl, NR21R22 and OR21;or R13 and an atom of B2 together with N form a 4 to 10 membered carbocyclic, aryl, heteroaryl or heterocyclic ring, wherein any of said carbocyclic, aryl, heteroaryl and heterocyclic rings are optionally substituted with one or more groups independently selected from halogen, cyano, nitro, azido, C1-C4 alkyl, C1-C4 heteroalkyl, C2-C4 alkenyl, C2-C4 heteroalkenyl, C2-C4 alkynyl, C2-C4 heteroalkynyl, NR21R22 and OR21;R15 is hydrogen, C1-C4 alkyl, C1-C4 heteroalkyl, C2-C4 alkenyl, C2-C4 heteroalkenyl, C2-C4 alkynyl or C2-C4 heteroalkynyl, wherein any of said alkyl, heteroalkyl, alkenyl, heteroalkenyl, alkynyl or heteroalkynyl is optionally substituted with one or more groups independently selected from halogen, hydroxyl, cyano, nitro, azido, NR21R22 and OR21;or R13 and R15 together with atoms to which they are attached form a 3 to 10 membered carbocyclic, aryl, heteroaryl or heterocyclic ring, wherein any of said carbocyclic, aryl, heteroaryl and heterocyclic rings are optionally substituted with one or more groups independently selected from halogen, cyano, nitro, azido, C1-C4 alkyl, C1-C4 heteroalkyl, C2-C4 alkenyl, C2-C4 heteroalkenyl, C2-C4 alkynyl, C2-C4 heteroalkynyl, NR21R22 and OR21;or, when W is CR15, R15 and an atom of B1 or B2 together with C, form a 3 to 10 membered carbocyclic, aryl, heteroaryl or heterocyclic ring, wherein any of said carbocyclic, aryl, heteroaryl and heterocyclic rings are optionally substituted with one or more groups independently selected from halogen, cyano, nitro, azido, C1-C4 alkyl, C1-C4 heteroalkyl, C2-C4 alkenyl, C2-C4 heteroalkenyl, C2-C4 alkynyl, C2-C4 heteroalkynyl, NR21R22 and OR21. |
