Inhibitors of myeloperoxidase
AssigneeAstraZeneca AB
InventorsTord Inghardt, Eva-Lotte Lindstedt, Ulrik Jurva, Nidhal Selmi
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Abstract
The specification generally relates to compounds of Formula (I), (Ia), and (Ib): and pharmaceutically acceptable salts thereof, where X, Y1, Y2, Y3, Y4, and Y5 and X1, X2, r, and q, have any of the meanings defined herein, together with compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO, and are thereby particularly useful in the treatment or prophylaxis of diseases or conditions in which modulation of the activity of the enzyme myeloperoxidase (MPO) is desirable, including diseases with inflammatory, cardiovascular, respiratory, renal, hepatic and/or neurological components, as well as neutrophilic driven diseases.
Claims17
A Compound of formula (I)
- wherein
- X=CH or N
- Y1=CZ1 or N, Y2=CZ2 or N, Y3=CZ3 or N, Y4=CZ4 or N, and Y5=CZ5 or N
- Z1, Z2, Z3, Z4, and Z5, are, if present, independently, H, halo, CF3, Q or T,
- provided that no more than one of Y1, Y2, Y3, Y4, or Y5 is N, at least two of Y1, Y2, Y3, Y4, or Y5 are CH, no more than one of Z1, Z2, Z3, Z4, and Z5 is halo or CF3, and one, and only one, of Z1, Z2, Z3, Z4, and Z5 is Q or T,
- Q is
- wherein m is 0, 1, 2, or 3,
- T is
- p is 0 or 1,
- s is 0, 1 or 2,
- n is 1 or 2,
- A is CH2, CF2, CHF, CHR2, CFR2, NR3, or O,
- wherein;
- R1 and R2, if present, are independently CH2F, CHF2, or CF3
- R3, if present, is independently H or CH3,
- or any stereoisomer thereof or pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.