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US 12,595,255 B2Granted
Heteroaryl-substituted imidazole derivatives
AssigneeHoffmann-La Roche Inc.
InventorsChristian Lerner, Mingming Li, Yongqiang Liu, Jianhua Wang, Min Wang, Yongguang Wang, Song Yang, Chengang Zhou
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Abstract
The invention provides novel heteroaryl-substituted imidazole derivatives having the general formula (I), and pharmaceutically acceptable salts thereof, wherein A and R1 to R6 are as described herein: Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.
Claims25
A compound of formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is selected from:
- (i) a group
- (ii) a group
- and
- (iii) a group
- R2 is selected from hydrogen, halogen, cyano, C1-C6-alkyl, C1-C6-alkoxy, halo-C1-C6-alkyl, and halo-C1-C6-alkoxy;
- R3 is selected from C1-C6-alkyl and halo-C1-C6-alkyl;
- R4, R5, and R6 are each independently selected from hydrogen, halogen, cyano, hydroxy, C1-C6-alkyl, C1-C6-alkoxy, halo-C1-C6-alkyl, halo-C1-C6-alkoxy, amino, C1-C6-alkyl-NH—, and (C1-C6-alkyl)2N—;
- R7 is selected from hydroxy-C1-C6-alkyl, amino-C1-C6-alkyl, C1-C6-alkyl-NH—C1-C6-alkyl-, (C1-C6-alkyl)2N—C1-C6-alkyl-, (C1-C6-alkyl)3N+—C1-C6-alkyl-, amino-C1-C6-alkoxy-C1-C6-alkyl, C1-C6-alkyl-NH—C1-C6-alkoxy-C1-C6-alkyl-, (C1-C6-alkyl)2N—C1-C6-alkoxy-C1-C6-alkyl-, (C1-C6-alkyl)3N+—C1-C6-alkoxy-C1-C6-alkyl, and a group
- R8 is selected from hydroxy-C1-C6-alkyl, amino-C1-C6-alkyl, C1-C6-alkyl-NH—C1-C6-alkyl-, (C1-C6-alkyl)2N—C1-C6-alkyl-, (C1-C6-alkyl)3N+—C1-C6-alkyl-, amino-C1-C6-alkoxy-C1-C6-alkyl, C1-C6-alkyl-NH—C1-C6-alkoxy-C1-C6-alkyl-, (C1-C6-alkyl)2N—C1-C6-alkoxy-C1-C6-alkyl-, (C1-C6-alkyl)3N+—C1-C6-alkoxy-C1-C6-alkyl, and a group
- R9 and R11 are each independently selected from hydrogen and C1-C6-alkyl;
- R10 is selected from hydrogen, C1-C6-alkyl, hydroxy-C1-C6-alkyl, amino-C1-C6-alkyl-, C1-C6-alkyl-NH—C1-C6-alkyl-, (C1-C6-alkyl)2N—C1-C6-alkyl-, and (C1-C6-alkyl)3N+—C1-C6-alkyl-;
- R12, R13, R14, R15, R16, and R17 are each independently selected from hydrogen, halogen, cyano, hydroxy, amino, C1-C6-alkyl, C1-C6-alkoxy, halo-C1-C6-alkyl, halo-C1-C6-alkoxy, hydroxy-C1-C6-alkyl, amino-C1-C6-alkyl, C1-C6-alkyl-NH—C1-C6-alkyl-, (C1-C6-alkyl)2N—C1-C6-alkyl-, and (C1-C6-alkyl)3N+—C1-C6-alkyl-;
- A is a 5- to 14-membered heteroaryl;
- B and C are are each independently selected from 3- to 14-membered heterocycloalkyl, and C3-C10-cycloalkyl;
- X1, X2, and Y are each independently selected from N and CH;
- m, n, p, and q are each independently 0 or 1;
- and
- L1 and L2 are each independently selected from carbonyl, —C(O)—C1-C6-alkyl-, —C1-C6-alkyl-C(O)—, —NH—C(O)—, and—C(O)—NH—;
- provided that A is not pyrazole.
18 more elements
Dependencies are inferred from the claim text.