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compound or a pharmaceutically acceptable salt thereof, pharmaceutical composition, and use of a compound or a pharmaceutically acceptable salt thereof
专利权人:
N. V. ORGANON
发明人:
RALF PLATE,CHRISTIAAN GERARDUS JOHANNES MARIA JANS
申请号:
BRPI0615412
公开号:
BRPI0615412A2
申请日:
2006.08.25
申请国别(地区):
BR
年份:
2012
代理人:
摘要:
COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PHARMACEUTICAL COMPOSITION, AND USE OF COMPOUND OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF. This invention relates to novel amino acid derivatives of the general formula I: wherein the R groups have the following meanings: R 1 is -H or - (1-4C) alkyl; R2 is -C (O) R15 or -SO2 R15; R3 is -H, - (1-4C) alkyl or -OR16; R4 is -H, - (1-4C) alkyl or -OR16; R6 is -H or -C (R16) NOR16; R7 is -H, -halogen, -cyano; - (1-6C) alkyl, - (2-6C) alkenyl or - (2-6C) alkynyl, all optionally substituted with amino, - hydroxyl or - halogen; R 8 is -H, -cyano, -halogen, -nitro; - (1-6C) alkyl, - (2-6C) alkyleline, - (2-6C) alkynyl or - O (1-6C) alkyl, all optionally substituted with - starch, - hydroxyl or - halogen; - (hetero) aryl, optionally substituted with -cyano, -halogen, - (1-4C) alkyl, - (1-4C) alkoxy, - (1-4C) (1-4C) alkyloxy or - (hetero) aryl ; -C (R16) NOR16, -C (O) N (R17) 2, -C (O) R18, C (O) OR19, -NHC (O) R20, or -NHS (O) 2R21; -R 9 is -H, -halogen, -cyano, or - (1-4C) alkyl, optionally substituted with -halogen; -R 10 is -H or - (1-4C) alkyl; -R 11 is -H; -R 12 is -H, -cyano or - (1-4C) alkyl; R 13 is -H, (1-4C) alkyl, -halogen or -formyl; - R14 is - H, -halogen, - cyano, - (1-4C) alkyl or - (hetero) aryl; or a pharmaceutically acceptable salt thereof. The compounds of this invention are highly specific for the glucocorticoid receptor and may be used to treat inflammatory diseases.COMPOSTO OU UM SAL FARMACEUTICAMENTE ACEITáVEL DO MESMO, COMPOSIçãO FARMACêUTICA, E, USO DE UM COMPOSTO OU UM SAL FARMACEUTICAMENTE ACEITáVEL DO MESMO. Esta invenção se refere a novos derivados de aminoácido da fórmula geral I: Fórmula I em que os grupos R têm os significados seguintes: R1 é - H ou - (1-4C)alquila; R2 é - C(O) R15 ou - SO2R15; R3 é - H, - (1-4C) alquila ou -OR16; R4 é - H, -(1-4C)alquila ou -OR16; R6 é -H ou - C(R16)NOR16; R7 é - H, - halogênio, - ciano; -(1-6C) alquila, -(2-6C)alquenila ou - (2-6C)alquinila, todos opciona
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