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    • 4. 发明授权
    • Protease inhibitors
    • 蛋白酶抑制剂
    • US06369077B1
    • 2002-04-09
    • US09423325
    • 1999-11-04
    • Robert W. MarquisYu RuDaniel F. VeberStephen M. LoCastro
    • Robert W. MarquisYu RuDaniel F. VeberStephen M. LoCastro
    • A61K31445
    • C07D401/12A61K38/00C07D207/14C07D403/12C07D405/12C07D409/12C07D417/12C07K5/06139
    • This invention relates to compounds of formula (I): wherein: Y is Ar or NR1R2; R1 is R″, R″C(O), R″C(S), R″SO2, R″OC(O), R″R′NC(O), or R″R′NC(S); R2 is H, C1-6alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R3 is H, C2-6alkenyl, C2-6alkynyl, Het, Ar or C1-6alkyl optionally substituted by OR′, SR′, NR′2, N(R′)C(O)OR″, CO2R′, CO2NR′2, N(C═NH)NH2, Het or Ar; R4 is H, C1-6alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R5 is  Ar-C0-6alkyl, Het-C0-6alkyl, adamantyl-C(O)—, Ar-C(O)—, Het-C(O)— or; R6 is R″, R″C(O), R″C(S), R″SO2, R″OC(O), R″R′NC(O), R″R′NC(S), or R″OC(O)NR′CH(R*)C(O); R7 is C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, Ar-C0-6alkoxy, Het-C0-6alkoxy, or C1-6alkyl optionally substituted by OR′, SR′, NR′2, N(R′)C(O)OR″, CO2R′, CO2NR′2, N(C═NH)NH2, Het or Ar; R* is H, C1-6alkyl, C2-6alkenyl, C3-6cycloalkyl-C0-6-alkyl, Ar-C0-6alkyl, Het-C0-6alkyl; each R′ independently is H, C1-6alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; each R″ independently is C1-6alkyl, C3-6cycloalkyl-C0-6-alkyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R′″ is H, C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, or Het-C0-6alkyl; Z is C(O) or CH2; and n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof, which are inhibitors of cysteine proteases, particularly cathepsin K, and are useful in the treatment of diseases in which inhibition of bone loss is a factor.
    • 本发明涉及式(I)化合物:其中:Y是Ar或NR1R2; R1是R“,R''C(O),R''C(S),R''SO2,R''OC (O),R''R'NC(O)或R''R'NC(S); R2是H,C1-6烷基,C2-6烯基,Ar-C0-6烷基或Het-C0-6烷基; R 3是H,C 2-6烯基,C 2-6炔基,Het,Ar或任选被OR',SR',NR'2,N(R')C(O)OR“,CO 2 R',CO 2 NR' 2,N(C = NH)NH 2,Het或Ar; R 4是H,C 1-6烷基,C 2-6烯基,Ar-C 1-6烷基或Het-C 0-6烷基; R 5是Ar-C 1-6烷基,Het-C 0 烷基,金刚烷基-C(O) - ,Ar-C(O) - ,Het-C(O) - 或R6为R“,R''C(O),R''C(S) R''SO2,R''OC(O),R''R'NC(O),R''R'NC(S)或R''OC(O)NR'CH(R *)C( O); R 7为任选被OR',SR'取代的C 3-6环烷基-C 0-6烷基,Ar-C 1-6烷基,Het-C 0-6烷基,Ar-C 0-6烷氧基,Het-C 0-6烷氧基或C 1-6烷基, NR'2,N(R')C(O)OR“,CO 2 R',CO 2 NR'2,N(C = NH)NH 2,Het或Ar; R *是H,C 1-6烷基,C 2-6烯基,C 3 C 1-6烷基,C 0-6烷基,Het-C 1-6烷基;各R'独立地为H,C 1-6烷基,C 2-6烯基,Ar-C 1-6烷基或Het-C 0-6烷基; R“独立地为C1-6 烷基,C 3-6环烷基-C 0-6烷基,Ar-C 1-6烷基或Het-C 0-6烷基; R“'是H,C 1-6烷基,C 3-6环烷基-C 0-6烷基,Ar-C 1-6烷基, 或Het-C0-6烷基; Z是C(O)或CH2; 和n是1,2或3;或其药学上可接受的盐,其是半胱氨酸蛋白酶的抑制剂,特别是组织蛋白酶K,并且可用于治疗其中抑制骨丢失的因素。