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publicationDate 2018-11-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-10118920-B2
titleOfInvention Isoxazolyl substituted benzimidazoles
abstract A compound which is a benzimidazolyl isoxazole of formula (I): wherein: R 0 and R, which are the same or different, are each H or C 1-6 alkyl; R 9 , R 9 and R 9 , which are the same or different, are each H or F; X is -(alk n -, -alk-C(═O)—NR—, -alk-NR—C(═O)— or -alk-C(═O)—; R 1 is selected from —S(═O) 2 R′; a 4- to 6-membered, C-linked heterocyclic group which is unsubstituted or substituted; and an N-linked spiro group of the following formula: R 2 and R 2′ , which are the same or different, are each H or C 1-6 alkyl, or R 2 and R 2′ form, together with the C atom to which they are attached, a C 3-6 cycloalkyl group; R 3 and R 3 , which are the same or different, are each H, C 1-6 alkyl, OH or F; R 4 is phenyl or a 5- to 12-membered, N-containing heteroaryl group and is unsubstituted or substituted; alk is C 1-6 alkylene; R′ is C 1-6 alkyl; and n is 0 or 1; or a pharmaceutically acceptable salt thereof. The compound has activity in modulating the activity of p300 and/or CBP and is used to treat cancer, particularly prostate cancer.
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Total number of triples: 1095.