主权项 |
1. A dry powder formulation comprising a compound of formula (I) wherein R1 is selected from the group consisting of hydrogen, and a saturated or unsaturated, branched or unbranched C1-15 alkyl chain, wherein optionally one or more carbons is/are replaced by a heteroatom selected from the group consisting of, OH, N, NH, NH2, and S(O)p, wherein said chain is optionally substituted by one or more groups independently selected from the group consisting of oxo, halogen, aryl, heteroaryl, carbocyclyl and heterocyclyl,
each aryl, heteroaryl, carbocyclyl or heterocyclyl group bearing:
0 to 3 substituents selected from the group consisting of halogen, -hydroxyl, —C1-6 alkyl, —C1-6 alkoxy, —C2-3 alkoxyOC1-3alkyl, —C2-3 alkylOC1-3 alkyl, —C1-3 hydroxyalkyl, —C1-6 haloalkyl, amino, —C1-4 mono or —C2-8 di-alkyl amino, —C1-4 mono or —C2-8 di-acyl amino, —C0-6 alkylS(O)p, C1-6 alkyl, —C0-6 alkylS(O)pNR6R7, —C0-6 alkylNR8C0-6 alkylS(O)pC1-6 alkyl, —C0-6 alkylC(O)OC0-6 alkyl, —NR8C0-6 alkylC(O)NR6R7—NR8C0-6 alkylC(O)C0-6 alkyl, —C0-6 alkylC(O)NR6R7, and —C0-6 alkylC(O)C1-6 alkyl;and/or one aryl, heterocyclyl or carbocyclyl; X is C6-10 aryl or a C5-9 heteroaryl each independently substituted by R2a and by R2b wherein R2a is selected from the group consisting of hydrogen, —C1-3 alkyl, halo, hydroxyl, cyano, —C1-3 haloalkyl, —C1-3 alkoxy, —C2-3 alkoxyOC1-3 alkyl, —C2-3 alkylOC1-3 alkyl, —C1-3 hydroxyalkyl, —C0-6 alkylS(O)qC1-3 alkyl, —C0-6 alkylS(O)pNR6R7, —C0-6 alkylNR8C0-6 alkylS(O)pC1-6 alkyl, —C0-6 alkylC(O)OH, —C0-6 alkylC(O)OC1-6 alkyl, —NR8C0-6 alkylC(O)NR6R7, —NR8C0-6 alkylC(O)C1-6 alkyl, —C0-6 alkylC(O)NR6R7 and —C0-6 alkylC(O)C1-6 alkyl; R2b is selected from the group consisting of hydrogen, C1-3 alkyl, halo, hydroxyl, cyano, —C1-3 haloalkyl, —C1-3 alkoxy, and —C0-6 alkylS(O)qC1-3 alkyl; R3a is hydroxyl; R3b is selected from the group consisting of hydrogen, hydroxyl, halo, cyano, —C1-3 haloalkyl, —C1-3 hydroxyalkyl, —C1-3 alkoxy, and —S(O)qC1-3 alkyl; R4 is hydrogen or —C1-3 alkyl; R5 is hydrogen or —C1-3 alkyl; R6 is hydrogen or —C1-6 alkyl; R7 is hydrogen or —C1-6 alkyl; R8 is hydrogen or —C1-6 alkyl; p is 0, 1 or 2; and q is 0, 1 or 2; or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof, wherein the compound of formula (I) is in finely divided form. |