主权项 |
1. A compound of formula (I): or a pharmaceutically acceptable salt or isotopically labelled form thereof, wherein: R1 is selected from the group consisting of C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, C3-C6cycloalkylC1-C6alkyl, 4-7-membered heterocycle and 4-7-membered heterocycleC1-C6alkyl, wherein each of the 4-7-membered heterocycles in the two last mentioned radicals are saturated or have one endocyclic double bond;
a) the C1-C6alkyl, the C2-C6alkenyl, the C2-C6alkynyl, the C1-C6alkyl of C3-C6cycloalkylC1-C6alkyl, and the C1-C6alkyl of 4-7-membered heterocycleC1-C6alkyl are unsubstituted or substituted with one or more substituents R1a independently selected from the group consisting of C1-C6alkoxy, C1-C6alkylcarbonylamino, C1-C6alkylsulfonylamino, amido, carboxy, cyano, halogen, hydroxy, and oxo;b) the C3-C6cycloalkyl, the C3-C6cycloalkyl of C3-C6cycloalkylC1-C6alkyl, 4-7-membered heterocycle, and the 4-7-membered heterocycle of 4-7-membered heterocycleC1-C6alkyl are unsubstituted or substituted with one or more substituents R1b independently selected from the group consisting of C1-C6alkoxy, C1-C6alkyl, amido, C1-C6alkylcarbonylamino, C1-C6alkylsulfonylamino, carboxy, cyano, halogen, haloC1-C6alkyl, hydroxy, hydroxyC1-C6alkyl, and oxo; R2 is selected from the group consisting of hydrogen, C1-C6alkyl, and haloC1-C6alkyl; or R1, R2 and the nitrogen to which they are attached form a saturated 4-7-membered N-bound heterocycle, which in addition to the nitrogen atom may have one further heteroatom selected from O, S and N as a ring member, wherein:
each such 4-7-membered heterocycle is unsubstituted or substituted with one or more identical or different substituents R1c, where R1c is selected from the group consisting of C1-C6alkoxy, C1-C6alkyl, C1-C6alkylcarbonylamino, C1-C6alkylsulfonylamino, amido, carboxy, cyano, halogen, haloC1-C6alkyl, amino, hydroxy, hydroxyC1-C6alkyl, oxo, spirocyclic bound C3-C6cycloalkyl; and spirocyclic bound saturated 4-6-membered heterocycle; wherein
each spirocyclic bound C3-C6cycloalkyl and spirocyclic bound 4-6-membered heterocycle is unsubstituted or substituted with one or more substituents independently selected from the group consisting of C1-C6alkyl, cyano, halogen, haloC1-C6alkyl, hydroxy, and hydroxyC1-C6alkyl; R3 is hydrogen, C1-C6alkyl, or haloC1-C6alkyl; R4 is hydrogen, C1-C6alkyl, or haloC1-C6alkyl; or R3 and R4 are joined to form a C3-C7alkylene; L1 is selected from the group consisting of —(CR5R6)m—, —(CH2)nCR5a═CR6a(CH2)p—, and wherein
c) R5, R5a, R5b, R6, R6a and R6b are, at each occurrence, independently selected from the group consisting of hydrogen, C1-C6alkyl, fluorine, haloC1-C6alkyl and phenyl, wherein;
phenyl is unsubstituted or substituted with one or more substituents selected from the group consisting of C1-C6alkyl, halogen, or haloC1-C6alkyl; ord) R5 or R6 is a C2-C4alkylene attached to G1;e) m is 1, 2, 3 or 4;f) n is, at each occurrence, independently 0, 1, or 2;g) p is, at each occurrence, independently 0, 1, or 2; and G1 is selected from the group consisting of C5-C10cycloalkyl, 5-6-membered heteroaryl, 5-6-membered heterocycle, which is saturated or has one endocyclic double bond, and phenyl; wherein
each C5-C10cycloalkyl, 5-6-membered heteroaryl, 5-6-membered heterocycle, and phenyl is unsubstituted or substituted with one or more identical or different substituents RG, where RG is selected from the group consisting of C1-C6alkyl, cyano, haloC1-C6alkyl, halogen, C1-C6alkoxy and haloC1-C6alkoxy. |