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Derivatives of 2 - oxo - 1.2 - dihydropyridine as inhibitors of bromodomain
专利权人:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY (Nº 2) LIMITED
发明人:
申请号:
ARP160102662
公开号:
AR105875A1
申请日:
2016.08.31
申请国别(地区):
AR
年份:
2017
代理人:
摘要:
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-C₃₋₇ cycloalkyl,1. Cyclopropyl compounds have not been replaced or replaced with one, two or three r83099 substances, which may be the same or different;ciclopropilo o - (CH) ORR8308es (a) phenyl (may not be replaced or replaced by one, two or three r831181 groups, which 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-lessor c8321c83183323,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,-8.8323,-O-C₂₋₃-R⁸ alkyl,a. Halo, oxo-o-cf-8323 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;R es -H -C (O) OC (CH)-Apartment 83318326, No. c832183,-C₃₋₇ cycloalkyl,a 4- to 7-membered heterocyclyl group, or -C₂₋₃-O-C₁₋₃ alkyl where the groups -C₁₋₆ alkyl and -C₃₋₇ cycloalkyl can be optionally substituted with one, two or three fluoro; R⁷ is -NR¹¹R¹²,-Apartment c832183-31832323,halo -CO R-CH OH -CH (R) OR-C (O) C₁₋₃ alkyl,-CH (R) NR R-CN, -CHF₂,-CF8323,-Oh, ochf832222,-OCF8323,-8.8323,-O-C₂₋₆-R⁹ alkyl,-C₁₋₆-R⁹ alkyl or -O-piperidinyl; R⁸ is -H, -OR¹⁰,-CO C (CH) o -NR RR⁹ is -H, -OR¹⁰ or -NR¹¹R¹²;Rs8304es-h o-lessor c8321;R¹¹ and R¹² are each independently selected from -H, -C₁₋₃ alkyl and -C₁₋₃NR¹³R¹⁴ alkyl;O R1 and R1 2 can form an isomerization group of 4 to 7 members together with the attached nitrogen, and can optionally be replaced by one or two alternatives independent of - c83218331 tar selection;-Oh and f; R3 and r83088 were selected from - h-u-c83218331y-c (o) ch832323, respectively;La presente se refiere a co
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