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Novel compounds useful for the treatment of degenerative and inflammatory diseases
专利权人:
GALAPAGOS N.V.
发明人:
MENET, CHRISTEL JEANNE MARIE,VAN ROMPAEY, LUC JULIAAN CORINA,FLETCHER, STEPHEN ROBERT,BLANC, JAVIER,JOUANNIGOT, NOLWENN,HODGES, ALASTAIR JAMES,SMITS, KOEN KURT
申请号:
ES09781072
公开号:
ES2485913T3
申请日:
2009.07.24
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
Compound according to formula III: in which L1 is selected from a single bond, -O-, -N (R4a) -, -C (O) -, C [>; = N (R4a)] -, -CON (R4a ) -, -SO2N (R4a) -, -S (O) 2-, - N (R4a) SO2- and -N (R4a) CO-; n1 is 0, 1, 2, 3 or 4; and R3b is substituted or unsubstituted C6-10 aryl, substituted or unsubstituted 5-10 membered heteroaryl comprising 1 to 3 heteroatoms selected from N, O or S, substituted or unsubstituted C3-C7 cycloalkyl, 4- 4- heterocycloalkyl 7 substituted or unsubstituted members comprising 1 to 3 heteroatoms selected from N, O or S; R4a is H, substituted or unsubstituted C1-C4 alkyl, substituted or unsubstituted C1-C4 alkoxy; wherein the substituents for the term "substituted" in the definition of R3b and R4a are selected from the group consisting of: halo, cyano, nitro, trifluoromethyl, trifluoromethoxy, azido, -NR "'SO2R', -SO2NR" R ' '', -C (O) R ", -C (O) OR", -OC (O) R ", - NR '" C (O) R ", -C (O) NR" R "', - NR'R "', - (CR"' R "') mOR"', in which each R "is independently selected from H, C1-C8 alkyl, - (CH2) t (C6-C10 aryl), - ( CH2) t (5-10 membered heteroaryl comprising 1 to 3 heteroatoms selected from N, O or S), - (CH2) t (C3-C10 cycloalkyl) and - (CH2) t (4-10 membered heterocycloalkyl) comprising 1 to 3 heteroatoms selected from N, O or S), in which t is an integer from 0 to 4; and * any alkyl group present may in turn be substituted with halo or hydroxyl; and * any aryl, heteroaryl, cycloalkyl or heterocycloalkyl group present may in turn be substituted with unsubstituted C1-C4 alkyl, halo, unsubstituted C1-C4 alkoxy, unsubstituted C1-C4 haloalkyl, unsubstituted C1-C4 hydroxyalkyl or haloalkoxyl C1-C4 unsubstituted or hydroxyl; each R "'independently represents H or C1-C6 alkyl; and provided that i) when L1 is -O-, -N (R4a) -, -CON (R4a) - or -SO2N (R4a) - and R3b is different from 5-10 membered cycloalkyl, aryl or heteroaryl, then n1 be 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereof, for use in the treatment and / or prevention
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