Isoxazolyl substituted benzimidazoles
US10118920B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Apr 20, 2016 |
| Grant date | Nov 6, 2018 |
| Priority date | — |
| Expiry date | Apr 20, 2036 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D471/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A compound which is a benzimidazolyl isoxazole of formula (I): wherein: R0 and R, which are the same or different, are each H or C1-6 alkyl; R9, R9 and R9, which are the same or different, are each H or F; X is -(alkn-, -alk-C(═O)—NR—, -alk-NR—C(═O)— or -alk-C(═O)—; R1 is selected from —S(═O)2R′; a 4- to 6-membered, C-linked heterocyclic group which is unsubstituted or substituted; and an N-linked spiro group of the following formula: R2 and R2′, which are the same or different, are each H or C1-6 alkyl, or R2 and R2′ form, together with the C atom to which they are attached, a C3-6 cycloalkyl group; R3 and R3, which are the same or different, are each H, C1-6 alkyl, OH or F; R4 is phenyl or a 5- to 12-membered, N-containing heteroaryl group and is unsubstituted or substituted; alk is C1-6 alkylene; R′ is C1-6 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.