PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF BACTERIAL DISEASES

摘要

The present invention relates to novel compounds of formula I:;;or a pharmaceutically acceptable salt thereof, wherein the integers are as defined in the description.;The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.

主权项

1. A compound of formula I, wherein formula I represents: wherein: Y represents: (ii) —CF3; (iii) —N(C1-6 alkyl)2 (e.g. —N(CH3)2); or (iv) C3-6 cycloalkyl (e.g. cyclopropyl); Nv, Nw, Nx, Ny and Nz independently represent —N═ or —C(H)═ but wherein only a maximum of three of Nv, Nw, Nx, Ny and Nz may represent —N═; n represents 0, 1 or 2 (but preferably represents 0); X1 and X2 independently represent —N— or —C(H)—; when X1 represents —N—, Q1 represents a direct bond, —C(O)— or —S(O)2—; when X1 represents —C(H)—, Q1 represents a direct bond or —N(Rz)—; Rz represents hydrogen or C1-6 alkyl; Rx represents C1-6 alkyl (optionally substituted by one or more substituents selected from ═O and A1), aryl or heteroaryl (which latter two groups are each optionally substituted by one or more substituents selected from A2 and A3, respectively); Ry, Ry1 and Ry2 independently represent hydrogen, halo, —CN, —OR10, —N(R11)(R12) or C1-6 alkyl (optionally substituted by one or more halo (e.g. fluoro) atoms); A1, A2, A3 and A4 independently represent halo, —CN, —OR10, —S(O)0-2C1-3alkyl, C1-6 alkyl (optionally substituted by one or more halo substituents), heterocycloalkyl (optionally substituted by one or more substituents selected from C1-3 alkyl and halo), aryl or heteroaryl (which latter two groups are optionally substituted by one or more substituents selected from B1 and B2, respectively); each R1 and R10 independently represent hydrogen, C1-6 alkyl (optionally substituted by one or more halo substituents), aryl or heteroaryl (which latter two groups are optionally substituted by one or more substituents selected from halo, C1-3 alkyl and —O—C1-3 alkyl); R11 and R12 independently represent hydrogen or C1-6 alkyl; B1 and B2 independently represent halo (e.g. chloro or fluoro), —CN, C1-6 alkyl (optionally substituted by one or more halo (e.g. fluoro) atoms), —OH or —O—C1-6 alkyl (optionally substituted by one or more halo (e.g. fluoro) atoms), or a pharmaceutically acceptable salt thereof, with the proviso that the compound is not: