Nrf2 regulators
AssigneesGlaxoSmithKline Intellectual Property Development Limited, Astex Therapeutics Limited
InventorsJeffrey K. Kerns, James Callahan, Thomas Daniel Heightman, Alison Jo-Anne Woolford, Ami Lakdawala Shah, Roderick S. Davis, David Norton, Jeffrey Charles Boehm, Nicole Cathleen Goodwin
Life of this patent
Estimating the term…
Abstract
Provided are aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.
Claims26
A compound of Formula (I)
- wherein,
- B is —(CH2)2-triazolyl which is unsubstituted or substituted by 1, 2, or 3 substituents independently selected from —C 1-3alkyl, —O—C1-3alkyl, CN, —(CH2)2—O—(CH2)2—OR4 and halo;
- D is —C(O)OH, —C(O)NHSO2CH3, —SO2NHC(O)CH3, 5-(trifluoromethyl)-4H-1,2,4-triazol-2-yl, or tetrazolyl;
- R1 is independently hydrogen, C1-3alkyl, F, or the two R1 groups together with the carbon to which they are attached form a cyclopropyl group;
- R2 is hydrogen, methyl, CF3, or halo;
- R4 is hydrogen or —C1-3alkyl;
- Linker is —CH2—, —CH2—N(cyclopropyl)—CH2—, —CH2—N(CH3)—CH2— or —N(CH3)—CH2—;
- A is tetrahydrobenzoxazepinyl or tetrahydro-pyrido-oxazepinyl, each of which is unsubstituted or substituted by 1, 2, or 3 substituents independently selected from —C1-3alkyl, C3-6spirocycloalkyl, halo, CN, —O—C1-3alkyl, —CH2—O—CH3, and OH;
- and
- X is CH;
- or a pharmaceutically acceptable salt thereof.
A compound which is 5-(1-Ethyl-1H-1,2,3-triazol-4-yl)-3-(3-(((R)-2-ethyl-2,3-dihydropyrido[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpentanoic acid:
- or a pharmaceutically acceptable salt thereof.
An enantiomer of a compound which is 5-(1-Ethyl-1H-1,2,3-triazol-4-yl)-3-(3-(((R)-2-ethyl-2,3-dihydropyrido[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpentanoic acid, or a pharmaceutically acceptable salt thereof.
A compound which is 5-(1-Ethyl-1H-1,2,3-triazol-4-yl)-3-(3-(((R)-2-ethyl-2,3-dihydropyrido[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpentanoic acid:
An enantiomer of a compound which is 5-(1-Ethyl-1H-1,2,3-triazol-4-yl)-3-(3-(((R)-2-ethyl-2,3-dihydropyrido[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)-2,2-dimethylpentanoic acid.
Dependencies are inferred from the claim text.