| 主权项 |
1. A compound of general formula Iwherein
m is 0-3; n is 2, 4, 6, or 8; A is N; R2 is hydrogen; R1 and R9 independently are selected from the group consisting of hydrogen, halogen, cyano, —NH2, —SO2NH2, —SONH2, and —CONH2; or R1 and R9 independently are selected from the group consisting of alkyl-, alkenyl-, alkynyl-, alkenylalkyl-, alkynylalkyl-, cycloalkyl-, cycloalkenyl-, cycloalkylalkyl-, cycloalkylalkenyl-, cycloalkylalkynyl-, cycloalkenylalkyl-, cycloalkenylalkenyl-, cycloalkenylalkynyl-, heterocyclyl-, heterocyclylalkyl-, heterocyclylalkenyl-, heterocyclylalkynyl-, R1aO-L-, R1aS-L, (R1a)2N-L-, R1b—C(═O)-L-, R1bO—C(═O)-L, (R1b)2N—C(═O)-L-, R1b—C(═O)N(R1c)-L-, R1bO—C(═O)N(R1c)-L-, (R1b)2N—C(═O)N(R1c)-L-, R1b—C(═O)O-L-, R1bO—C(═O)O-L-, (R1b)2N—C(═O)O-L-, R1b—S(═O)-L-, R1b—S(═O)2-L-, R1bO—S(═O)-L-, R1bO—S(═O)2-L-, (R1b)2N—S(═O)-L-, (R1b)2N—S(═O)2-L-, R1b—S(═O)N(R1c)-L-, R1b—S(═O)2N(R1c)-L-, R1bO—S(═O)N(R1c)-L-, R1bO—S(═O)2N(R1c)-L-, (R1b)2N—S(═O)2N(R10)-L-, R1b—S(═O)O-L-, R1b—S(═O)2O-L-, R1bO—S(═O)O-L-, R1bO—S(═O)2O-L-, (R1b)2N—S(═O)O-L-, (R1b)2N—S(═O)2O-L-, aryl-, arylalkyl-, arylalkenyl-, arylalkynyl-, arylcycloalkyl-, aryloxy-, aryloxyalkyl-, aryloxycycloalkyl-, heteroaryl-, heteroarylalkyl-, heteroarylalkenyl-, heteroarylalkynyl, heteroarylcycloalkyl-, heteroaryloxy-, heteroaryloxyalkyl-, and heteroaryloxycycloalkyl-, either of which may be optionally substituted with one or more R1d; L is a covalent bond or L is independently at each occurrence selected from the group consisting of alkyl-, cycloalkyl-, alkylcycloalkyl- and cycloalkylalkyl-; R1a is hydrogen; or R1a independently at each occurrence is selected from the group consisting of alkyl-, alkenyl-, alkynyl-, cycloalkyl, -heterocyclyl-, aryl- and heteroaryl-, either of which may be optionally substituted with one or more R1e; or in the case where two R1as are attached to the same N, they may together with the N atom to which they are attached form a heterocycle which may be optionally substituted with one or more R1e; R1b and R1c independently at each occurrence are selected from the group consisting of alkyl-, alkenyl-, alkynyl-, cycloalkyl-, cycloalkenyl-, cycloalkylalkyl-, cycloalkylalkenyl-, cycloalkylalkynyl-, cycloalkenylalkyl-, cycloalkenylalkenyl-, cycloalkenylalkynyl-, heterocyclyl-, heterocyclylalkyl-, heterocyclylalkenyl-, heterocyclylalkynyl-, aryl-, arylalkyl-, arylalkenyl-, arylalkynyl-, arylcycloalkyl-, aryloxyalkyl-, aryloxycycloalkyl-, heteroaryl-, heteroarylalkyl-, heteroarylalkenyl-, heteroarylalkynyl-, heteroarylcycloalkyl, heteroaryloxyalkyl-, and heteroaryloxycycloalkyl-, either of which may be optionally substituted with one or more R1e; or in the case where two R1bs or two R1cs are attached to the same N, they may together with the N atom to which they are attached form a heterocycle which may be optionally substituted with one or more R1e; R1d and R1e independently at each occurrence are selected from the group consisting of halogen, cyano, hydroxy, oxo, —NH2, —SO2NH2, —SONH2, —CONH2, alkyl-, alkenyl-, alkynyl-, cycloalkyl-, cycloalkenyl-, heterocyclyl-, R1fO-L-, R1fS-L-, (R1f)2N-L-, R1fO—R1fO-L-, R1f—C(═O)-L-, R1fO—C(═O)-L-, (R1f)2N—C(═O)-L-, R1f—C(═O)N(R1f)-L-, R1fO—C(═O)N(R1f)-L-, (R1f)2N—C(═O)N(R1f)-L-, R1f—C(═O)O-L-, R1fO—C(═O)O-L-, (R1f)2N—C(═O)O-L-, R1fO—S(═O)2-L-, (R1f)2N—S(═O)2-L-, R1f—S(═O)2N(R1f)-L-, R1fO—S(═O)2N(R1f)-L-, (R1f)2N—S(═O)2N(R1f)-L-, R1f—S(═O)2O-L-, R1fO—S(═O)2O-L-, (R1f)2N—S(═O)2O-L-, aryl-, aryloxy-, heteroaryl-, and heteroaryloxy-; R1f independently at each occurrence is selected from the group consisting of alkyl-, alkenyl-, alkynyl-, cycloalkyl-, heterocyclyl-, aryl- and heteroaryl-; R3 is independently at each occurrence a covalent bond or alkyl- or heteroalkyl-, which may be optionally substituted with one or more R3a, wherein any two R3s form, together with the ring atom(s) to which they are attached, a cycloalkyl or heterocycle, with the proviso that said two R3s are either attached to the same C atom or to two non-adjacent C atoms; R3a independently at each occurrence is selected from the group consisting of halogen, cyano, hydroxy, oxo, —NH2, —SO2NH2, —SONH2, —CONH2, alkyl-, alkenyl-, alkynyl-, alkenylalkyl-, alkynylalkyl-, cycloalkyl-, cycloalkenyl-, cycloalkylalkyl-, cycloalkylalkenyl-, cycloalkylalkynyl-, cycloalkenylalkyl-, cycloalkenylalkenyl-, cycloalkenylalkynyl-, heterocyclyl-, heterocyclylalkyl-, heterocyclylalkenyl-, heterocyclylalkynyl-, R3bO-L-, R3bS-L-, (R3b)2N-L-, R3b—C(═O)-L-, R3bO—C(═O)-L-, (R3b)2N—C(═O)-L-, R3b—C(═O)N(R3c)-L-, R3bO—C(═O)N(R3c)-L-, (R3b)2N—C(═O)N(R3c)-L-, R3b—C(═O)O-L-, R3bO—C(═O)O-L-, (R3b)2N—C(═O)O-L-, R3b—S(═O)-L-, R3b—S(═O)2-L-, R3bO—S(═O)-L-, R3bO—S(═O)2-L-, (R3b)2N—S(═O)-L-, (R3b)2N—S(═O)2-L-, R3b—S(═O)N(R3c)-L-, R3b—S(═O)2N(R3c)-L-, R3bO—S(═O)N(R3c)-L-, R3bO—S(═O)2N(R3c)-L-, (R3b)2N—S(═O)2N(R3c)-L-, R3b—S(═O)O-L-, R3b—S(═O)2O-L-, R3bO—S(═O)O-L-, R3bO—S(═O)2O-L-, (R3b)2N—S(═O)O-L-, (R3b)2N—S(═O)2O-L-, aryl-, arylalkyl-, arylalkenyl-, arylalkynyl-, arylcycloalkyl-, aryloxy-, aryloxyalkyl-, aryloxycycloalkyl-, heteroaryl-, heteroarylalkyl-, heteroarylalkenyl-, heteroarylalkynyl-, heteroarylcycloalkyl, heteroaryloxy-, heteroaryloxyalkyl-, and heteroaryloxycycloalkyl-; R3b and R3c independently at each occurrence are selected from the group consisting of hydrogen, alkyl-, alkenyl-, alkynyl-, cycloalkyl-, heterocyclyl-, aryl- and heteroaryl-; R5 independently at each occurrence is selected from the group consisting of halogen, cyano, hydroxy, oxo, —NH2, —SO2NH2, —SONH2, —CONH2, alkyl-, alkenyl-, alkynyl-, alkenylalkyl-, alkynylalkyl-, cycloalkyl-, cycloalkenyl-, cycloalkylalkyl-, cycloalkylalkenyl-, cycloalkylalkynyl-, cycloalkenylalkyl-, cycloalkenylalkenyl-, cycloalkenylalkynyl-, heterocyclyl-, heterocyclylalkyl-, heterocyclylalkenyl-, heterocyclylalkynyl-, R5aO-L-, R5aS-L-, (R5a)2N-L-, R5a—C(═O)-L-, R5aO—C(═O)-L-, (R5a)2N—C(═O)-L-, R5a—C(═O)N(R5b)-L-, R5aO—C(═O)N(R5b)-L-, (R5a)2N—C(═O)N(R5b)-L-, R5a—C(═O)O-L-, R5aO—C(═O)O-L-, (R5a)2N—C(═O)O-L-, R5a—S(═O)-L-, R5a—S(═O)2-L-, R5aO—S(═O)-L-, R5aO—S(═O)2-L-, (R5a)2N—S(═O)-L-, (R5a)2N—S(═O)2-L-, R5a—S(═O)N(R5b)-L-, R5a—S(═O)2N(R5b)-L-, R5aO—S(═O)N(R5b)-L-, R5aO—S(═O)2N(R5b)-L-, (R5a)2N—S(═O)2N(R5b)-L-, R5a—S(═O)O-L-, R5a—S(═O)2O-L-, R5aO—S(═O)O-L-, R5aO—S(═O)2O-L-, (R5a)2N—S(═O)O-L-, (R5a)2N—S(═O)2O-L-, aryl-, arylalkyl-, arylalkenyl-, arylalkynyl-, arylcycloalkyl-, aryloxy-, aryloxyalkyl-, aryloxycycloalkyl-, heteroaryl-, heteroarylalkyl-, heteroarylalkenyl-, heteroarylalkynyl-, heteroarylcycloalkyl, heteroaryloxy-, heteroaryloxyalkyl-, and heteroaryloxycycloalkyl-; R5a and R5b independently at each occurrence are selected from the group consisting of hydrogen, alkyl-, alkenyl-, alkynyl-, cycloalkyl-, heterocyclyl-, aryl- and heteroaryl-; R4 is selected from the group consisting ofwherein
X is O or S; Y is O or N—R7; Z is C1-6-alkylene, C2-6-alkenylene, or C2-6-alkynylene, either of which may be optionally substituted with one or more R8; G1 is selected from the group consisting of cycloalkyl-, cycloalkenyl-, heterocyclyl-, aryl- and heteroaryl-, either of which may be optionally substituted with one or more RG; G2 is selected from the group consisting of alkyl-, alkenyl-, alkynyl-, RG2aO-L-, RG2aS-L-, (RG2a)2N-L-, RG2a—C(═O)-L-, RG2aO—C(═O)-L-, (RG2a)2N—C(═O)-L-, RG2a—C(═O)N(RG2b)-L-, RG2aO—C(═O)N(RG2b)-L-, (RG2a)2N—C(═O)N(RG2b)-L-, RG2a—C(═O)O-L-, RG2aO—C(═O)O-L-, (RG2a)2N—C(═O)O-L-, RG2a—S(═O)-L-, RG2a—S(═O)2-L-, RG2aO—S(═O)-L-, RG2aO—S(═O)2-L-, (RG2a)2N—S(═O)-L-, (RG2a)2N—S(═O)2-L-, RG2a—S(═O)N(RG2b)-L-, RG2a—S(═O)2N(RG2b)-L-, RG2aO—S(═O)N(RG2b)-L-, RG2aO—S(═O)2N(RG2b)-L-, (RG2a)2N—S(═O)2N(RG2b)-L-, RG2a—S(═O)O-L-, RG2a—S(═O)2O-L-, RG2aO—S(═O)O-L-, RG2a—S(═O)2O-L-, (RG2a)2N—S(═O)O-L-, and (RG2a)2N—S(═O)2O-L-; either of which may be optionally substituted with one or more RG; RG2a and RG2b independently at each occurrence are selected from the group consisting of hydrogen, alkyl-, alkenyl-, alkynyl-, cycloalkyl-, heterocyclyl-, aryl- and heteroaryl-; RG is selected from the group consisting of halogen, cyano, hydroxy, oxo, —NH2, —SO2NH2, —SONH2, —CONH2, alkyl- and cycloalkyl-, wherein said alkyl- or cycloalkyl- is optionally substituted by one or more substituents selected from the group consisting of halogen, cyano, hydroxy, trifluoromethyl and —NH2; or RG is selected from the group consisting of alkenyl-, alkynyl-, alkenylalkyl-, alkynylalkyl-, cycloalkenyl-, cycloalkylalkyl-, cycloalkylalkenyl-, cycloalkylalkynyl-, cycloalkenylalkyl-, cycloalkenylalkenyl-, cycloalkenylalkynyl-, heterocyclyl-, heterocyclylalkyl-, heterocyclylalkenyl-, heterocyclylalkynyl-, RGaO-L-, RGaS-L-, (RGa)2N-L-, RGa—C(═O)-L-, RGaO—C(═O)-L-, (RGa)2N—C(═O)-L-, RGa—C(═O)N(RGb)-L-, RGaO—C(═O)N(RGO-L-, (RGa)2N—C(═O)N(RGb)-L-, RGa—C(═O)O-L-, RGaO—C(═O)O-L-, (RGa)2N—C(═O)O-L-, RGa—S(═O)-L-, RGa—S(═O)2-L-, RGaO—S(═O)-L-, RGaO—S(═O)2-L-, (RGa)2N—S(═O)-L-, (RGa)2N—S(═O)2-L-, RGb—C(═O)—(RGa)N—(RGa)2N—S(═O)2-L, RGbO—C(═O)—(RGa)N—(RGa)2N—S(═O)2-L, RGa—S(═O)N(RGb)-L-, RGa—S(═O)2N(RGb)-L-, RGaO—S(═O)N(RGb)-L-, RGaO—S(═O)2N(RGb)-L-, (RGa)2N—S(═O)2N(RGb)-L-, RGa—S(═O)O-L-, RGa—S(═O)2O-L-, RGaO—S(═O)O-L-, RGaO—S(═O)2O-L-, (RGa)2N—S(═O)O-L-, (RGa)2N—S(═O)2O-L-, aryl-, arylalkyl-, arylalkenyl-, arylalkynyl-, arylcycloalkyl-, aryloxy-, aryloxyalkyl-, aryloxycycloalkyl-, heteroaryl-, heteroarylalkyl-, heteroarylalkenyl-, heteroarylalkynyl-, heteroarylcycloalkyl, heteroaryloxy-, heteroaryloxyalkyl-, and heteroaryloxycycloalkyl-; RGa and RGb independently at each occurrence are selected from the group consisting of hydrogen, alkyl-, alkenyl-, alkynyl-, cycloalkyl-, heterocyclyl-, heterocyclylalkyl, aryl-, heteroaryl- and heteroarylalkyl; wherein said alkyl-, alkenyl-, alkynyl-, cycloalkyl-, heterocyclyl-, heterocyclylalkyl, aryl-, heteroaryl- or heteroarylalkyl group is optionally substituted one or more times by a substituent selected from the group consisting of halogen, cyano, hydroxy, methyl, trifluoromethyl, methoxy and —NH2; R7 is hydrogen or is independently at each occurrence selected from the group consisting of alkyl-, alkenyl-, alkynyl-, cycloalkyl-, heterocyclyl-, aryl- and heteroaryl-, either of which may be optionally substituted with one or more R7a; R7a independently at each occurrence is selected from the group consisting of halogen, cyano, hydroxy, oxo, —NH2, —SO2NH2, —SONH2, —CONH2, alkyl-, alkenyl-, alkynyl-, cycloalkyl-, heterocyclyl-, aryl- and heteroaryl-; R8 independently at each occurrence is selected from the group consisting of hydrogen, halogen, cyano, hydroxy, oxo, —NH2, —SO2NH2, —SONH2, —CONH2, alkyl- and cycloalkyl, wherein said alkyl- or cycloalkyl- is optionally substituted by one or more substituents selected from the group consisting of halogen, cyano, hydroxy, trifluoromethyl and —NH2; or two R8s may, together with the C atom(s) to which they are attached, form an optionally substituted cycloalkyl or heterocycle;and pharmaceutically acceptable salts, hydrates, or solvates thereof. |
