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filingDate 2016-08-31-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2017-11-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-105875-A1
titleOfInvention DERIVATIVES OF 2-OXO-1,2-DIHYDROPIRIDINE AS BROMODOMINIUM INHIBITORS
abstract This refers to compounds of formula (1) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy. Claim 1: A compound of formula (1) or a salt thereof wherein: R¹ is -C₁₋₃ alkyl or cyclopropyl; R² is H or -C₀₋₃ alkyl-C ciclo cycloalkyl, where the cycloalkyl group is not substituted or is substituted by one, two or three R⁵ groups which may be the same or different; R³ is -H, -C₁₋₄ alkyl, cyclopropyl or - (CH₂) ₚOR¹⁰; R⁴ is a) phenyl (which may be unsubstituted or substituted with one, two or three R⁷ groups that may be the same or different); b) a 5- or 6-membered heteroaryl group (which may be unsubstituted or substituted with -C₁₋₃ alkyl, -O-C₁₋₃ alkyl, or halo); c) a 9 to 11-membered heteroaryl group (which may be unsubstituted or substituted with one, two or three groups, which may be the same or different, selected from -C₁₋₃-R⁸ alkyl, -OCH₃, -O-alkyl C₂₋₃-R⁸, halo, oxo, -O-CF₃ and -CN); or d) - (CH₂) ₙ-phenyl; p is 1 or 2; n is 1 or 2; R⁵ is halo, phenyl, -C₁₋₆-R⁸ alkyl, -CO₂H, -OCH₃, -O-C₂₋₆-R⁸ alkyl, -CN, -OH or -NHR⁶; R⁶ is -H, -C (O) OC (CH₃) ₃, -C₁₋₆ alkyl, -C₃₋₇ cycloalkyl, a 4- to 7-membered heterocyclyl group, or -C₂₋₃-O-C₁₋₃ alkyl wherein the groups -C₁₋₆ alkyl and -C₃₋₇ cycloalkyl may be optionally substituted with one, two or three fluoro; R⁷ is -NR¹¹R¹², -C₁₋₃ alkyl, halo, -CO₂R¹⁰, -CH₂OH, -CH (R¹¹) OR¹⁰, -C (O) C₁₋₃ alkyl, -CH (R¹⁰) NR¹¹R¹², -CN, -CHF₂, - CF₃, -OH, -OCHF₂, -OCF₃, -OCH₃, -O-C₂₋₆-R⁹ alkyl, -C₁₋₆-R⁹ alkyl or -O-piperidinyl; R⁸ is -H, -OR¹⁰, -CO₂C (CH₃) ₃ or -NR¹¹R¹²; R⁹ is -H, -OR¹⁰ or -NR¹¹R¹²; R¹⁰ is -H or -C₁₋₃ alkyl; R¹¹ and R¹² are each independently selected from -H, -C₁₋₃ alkyl and -C₁₋₃NR¹³R¹⁴ alkyl; or R¹¹ and R¹² can be linked together with the nitrogen to which they are attached to form a 4- to 7-membered heterocyclyl group, optionally substituted with one or two substituents independently selected from -C₁₋₃ alkyl, -OH and F; and R¹³ and R¹⁴ are each independently selected from -H, -C₁₋₃ alkyl and -C (O) CH₃.
priorityDate 2015-09-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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Total number of triples: 48.