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非類固醇型醣皮質素受體調節劑
专利权人:
MSD OSS B. V.
发明人:
PLATE, RALF,瑞夫 帕莱特,瑞夫 帕萊特,JANS, CHRISTIAAN GERARDUS JOHANNES MARIA,克里斯坦 詹斯,瑞夫 帕莱特,瑞夫 帕萊特,克里斯坦 詹斯
申请号:
TW095129231
公开号:
TWI375676B
申请日:
2006.08.09
申请国别(地区):
TW
年份:
2012
代理人:
摘要:
This invention relates to novel amino acid derivatives of formula (I) wherein the R groups have the following meanings: -R1 is -H or -(1-4C)alkyl; -R2 is -C(O)R15 or -S(O)2R15; -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; -R8 is -H, -cyano, -halogen, -nitro; -(1-6C)alkyl, -(2-6C)alkenyl, -(2-6C)alkynyl or -O(1-6C)alkyl, all optionally substituted with -amino, -hydroxyl or -halogen; -(hetero)aryl, optionally substituted with -cyano, -halogen, -(1-4C)alkyl, -(1-4C)alkoxy, -(1-4C)alkoxy(1-4C)alkyl or -(hetero)aryl; -C(R16)NOR16; -C(O)N(R17)2; -C(O)R18, -C(O)OR19, -NHC(O)R20, or -NHS(O)2R21; -R9 is -H, -halogen, -cyano, or -(1-4C)alkyl, optionally substituted with -halogen; -R10 is -H or -(1-4C)alkyl; -R11 is -H; -R12 is -H, -cyano or -(1-4C)alkyl; -R13 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 for treating inflammatory diseases.本發明係關於式I所示之新穎胺基酸衍生物或彼等之藥學上可接受的鹽類,;式I;其中R基團具有下列定義:-R1示-H或-(C1-4)烷基;-R2示-C(O)R15或-S(O)2R15;-R3示-H、-(C1-4)烷基或-OR16;-R4示-H、-(C1-4)烷基或-OR16;-R6示-H或-C(R16)NOR16;-R7示-H、-鹵素、-氰基、-(C1-6)烷基、-(C2-6)烯基或-(C2-6)炔基,彼等皆任意經-胺基、-羥基或-鹵素所取代;-R8示-H、-氰基、-鹵素、-硝基、-(C1-6)烷基、-(C2-6)烯基、-(C2-6)炔基或-O(C1-6)烷基,彼等皆任意經-胺基、-羥基或-鹵素所取代;-(雜)芳基,其任意經-氰基、-鹵素、-(C1-4)烷基、-(C1-4)烷氧基、-(C1-4)烷氧基(C1-4)烷基或-(雜)芳基所取代;-C(R16)NOR16;-C(O)N(R17)2;-C(O)R18、-C(O)OR19;-NHC(O)R20或-NHS(O)2R21;-R9示-H、-鹵素、-氰基、或任意經-鹵素所取代的-(C1-4)烷基;-R10示-H或-(C1-4)烷基;-R11示-H;-R12示-H、-氰基或-(C1-4)烷基;-R13示-H、-(C1-4)烷基、-鹵素或-甲醯基;-R14示-H、-鹵素、-氰基、-(C1-4)烷基或-(雜)芳基;-R15示-H;-(C1-6)烷基、-(C2-C6)烯基、-(C2-C6)炔基、-O(C2-6)烷基、-O(C2-6)烯基或-O(C2-6)炔基,彼等皆任意經一或多個-OH、-鹵素、-氰基或-(雜)芳基所取代;-(雜)芳基,其任意經-(C1-4)烷基、-鹵素或-NH2所取代;-NH2;-(二)(C1-4)烷基胺基;-(C1-4)烷硫基(C1-4)烷基或-(C1-
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