CASTANEDO, Georgette,DOTSON, Jennafer,GOLDSMITH, Richard,GUNZNER, Janet,HEFFRON, Tim,MATHIEU, Simon,OLIVERO, Alan,STABEN, Steven,SUTHERLIN, Daniel P.,TSUI, Vickie,WANG, Shumei,ZHU, Bing-Yan,BAYLISS, T
申请号:
ES07865255
公开号:
ES2571028T3
申请日:
2007.12.05
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound selected from Formula Ia and Formula Ib: ** Formula ** and its stereoisomers, tautomers and pharmaceutically acceptable salts, wherein: X is O or S; R1 is selected from F, Cl, Br, I, -C (C1-C6 alkyl) 2NR10R11, - (CR14R15) tNR10R11, -C (R14R15) nNR12C (>; = Y) R10, - (CR14R15) nNR12S (O) 2R10 , -CH (OR10) R10, - (CR14R15) nOR10, - (CR14R15) nS (O) 2R10, - (CR14R15) nS (O) 2NR10R11, - C (>; = Y) R10, -C (>; = Y) OR10, -C (>; = Y) NR10R11, -C (>; = Y) NR12OR10, -C (>; = O) NR12S (O) 2R10, -C (>; = O) NR12 (CR14R15) mNR10R11, NO2, -NHR12 , -NR12C (>; = Y) R11, -NR12C (>; = Y) OR11, -NR12C (>; = Y) NR10R11, -NR12 (O) 2R10, -NR12SO2NR10R11, -S (O) 2R10, - S (O) 2NR10R11, -SC (>; = Y) R10, -SC (>; = Y) OR10, C1-C12 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C3-C12 carbocyclyl, C2-C20 heterocyclyl, C6-C20 aryl or C1-C20 heteroaryl; R2 is selected from H, F, Cl, Br, I, C6-C20 aryl, C1-C20 heteroaryl and C1-C6 alkyl; R3 is a monocyclic heteroaryl group selected from ** Formula ** R10, R11 and R12 are independently H, C1-C12 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C3-C12 carbocyclyl, C2-C20 heterocyclyl, C6 aryl- C20 or C1-C20 heteroaryl, or R10 and R11 together with the nitrogen to which they are optionally attached form a C3-C20 heterocyclic ring that optionally contains one or more additional ring atoms selected from N, O or S, wherein said heterocyclic ring is optionally substituted with one or more groups independently selected from oxo, (CH2) mOR10, CH2) mNR10R11, CF3, F, Cl, Br, I, SO2R10, C (>; = O) R10, NR12C (>; = Y) R11, C (>; = Y) NR10R11, C1-C12 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C3-5 C12 carbocyclyl, C2-C20 heterocyclyl, C6-C20 aryl and C1-C20 heteroaryl; R14 and R15 are independently selected from H, C1-C12 alkyl or - (CH2) n-aryl, or R14 and R15 together with the atoms to which they are attached form a saturated or partially unsaturated C3-C12 carbocyclic ring, wherein said alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, ar