DAVID LANCIA JR.,ANNA ERICSSON,R. BRUCE DIEBOLD,JUSTIN A. CARAVELLA,DAVID JOSEPH GUERIN,DARBY RYE SCHMIDT,ANN CAMPBELL,MINGHUA MARIE - WANG,ALEXANDRE JOSEPH BUCKMELTER,BRUCE FOLLOWS,ADAM TALBOT,STEPHA
申请号：
ARP150104312
公开号：
AR103297A1
申请日:
2015.12.28
申请国别(地区):
AR
年份:
2017
代理人:
摘要：
USP7 inhibitors for the treatment of cancer, neurodegenerative diseases, immune disorders, inflammation, cardiovascular diseases, ischemic diseases, viral diseases and infections, as well as bacterial diseases and infections. 1. Claim 1: a formula compound (1),or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, steroisomer and tautomer thereof, wherein: X¹ is C, S, or S (O)；X2 is cr8311o o n； R1 is h, D, oh, h, h, nh832222；-NHC alquil -N (C alquil)or F； R² is C₁₋₈ alkyl, aryl, heteroaryl, C₃₋₈ cycloalkyl, heterocyclyl, -NR¹⁰R¹¹,or -OR¹⁰,1. Among them, tar, aril, cyclopentyl and acylopentyl can be replaced by one or more r831222；each R³ is independent at each selected occurrence of D, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ alkoxy, C₁₋₆ haloalkyl, C₁₋₆ haloalkoxy, aryl, heteroaryl, C₃₋₈ cycloalkyl, heterocyclyl, -CN, -OH, -C (O) R¹⁷,-C (O) OR-OC (O) OR-OC (O) NR R-8311； 8312；-8311； (C (o) r831222；-8311； (C (o) or 831222；C (O) NR R-8311； (C (o) 8311； (R1 8312)；-S (O) qNR R-S (O) qR R-No. 8311； s (o) qr18311； R1 8312；O halogen, wherein tar can be replaced by one or more substitutes independently selected in Oh o-nh83222；or two R³ together when on adjacent carbons they form a C₃₋₈ cycloalkyl optionally substituted by one or more R¹⁹；or two R³ together form a C₃₋₈ spirocycloalkyl which is optionally substituted by one or more R¹⁹；O 2 cubes are added together to form a helix optionally substituted by one or more r8313；If aril rings are formed in the adjacent carbides, one or more r8313 can be substituted；O 2r3 added together, if a heteromorphic ring is formed in the adjacent carbide, it is replaced by one or more r8313；R⁴ is C₁₋₆ alkyl, -C₀₋₃ alkylene, aryl, heteroaryl, C₃₋₈ cycloalkyl, CD₃,Or heterosexual, where aril, heterosexual, heterosexual and cyclopentanediol are replaced by one or more arcs；R⁵ and R⁵ are independently H, D, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ alkoxy, C₁₋₆ haloalkyl, C₁₋₆ haloalkoxy, or halogen； or R⁵ and R⁵ together for
