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US 12,735,409 B2Granted
Benzoxazinone derivatives as selective cytotoxic agents
AssigneeMerck Sharp & Dohme Corp.
InventorsAbdellatif El Marrouni, Antonella Converso, Ashley Forster
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Abstract
The present disclosure is directed to benzoxazinone derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV naïve cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).
Claims10
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is halo or —C1-8alkyl unsubstituted or substituted with 1 to 7 of —F;
- R2 is —H, halo, —CN, —C1-8alkyl, —C2-8alkenyl, —C(O)OC1-8alkyl, —C(O)C1-8alkyl or —NR6R7;
- R3 is —H or halo;
- R4 is —H or halo;
- R5 is a 5 or 6-membered ring selected from phenyl, pyrimidinyl, pyrimidinone, pyrazinone, pyrazolyl and pyridinyl, wherein each ring is unsubstituted or substituted with one or more substituents up to the maximum number allowed by valence, independently selected at each occurrence from:
- (i) halo,
- (ii) —CN,
- (iii) —NR6R7,
- (iv) —SO2—NR6R7,
- (v) —C1-8alkyl unsubstituted or substituted with 1 to 8 substituents independently selected at each occurrence from —OH and halo,
- (vi) —C1-4alkyl-O—C1-4alkyl unsubstituted or substituted with 1 to 8 substituents independently selected at each occurrence from —OH or halo, and
- (vii) —OC1-8alkyl unsubstituted or substituted with 1 to 8 substituents independently selected at each occurrence from —OH and halo;
- R6 is —H or —C1-8alkyl unsubstituted or substituted with 1 to 8 substituents independently selected at each occurrence from —OH and halo;
- and
- R7 is —H or —C1-8alkyl unsubstituted or substituted with 1 to 8 substituents independently selected at each occurrence from —OH and halo.
13 more elements
Dependencies are inferred from the claim text.