Inhibitors of cathepsin k

Details Inhibitors of cathepsin k Inhibitors of cathepsin k

C - Chemistry, Metallurgy

07

D

C07D 413/14 (2006.01) A61K 31/40 (2006.01) A61K 31/415 (2006.01) A61K 31/445 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/505 (2006.01) A61K 31/535 (2006.01) C07D 207/14 (2006.01) C07D 207/24 (2006.01) C07D 207/273 (2006.01) C07D 211/58 (2006.01) C07D 211/72 (2006.01) C07D 211/74 (2006.01) C07D 211/96 (2006.01) C07D 401/06 (2006.01) C07D 401/10 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C12N 9/64 (2006.01) C12Q 1/37 (2006.01) G01N 33/573

Patent

CA 2262668

This invention relates to compounds of formula (I), wherein A is C(O) or CH(OH); R1 is (1), (2), (3) or (4); R2 is H, C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-b6alkyl, R5C(O)-, R5C(S)-, R5SO2- ,~R5OC(O)-, R5R'NC(O)-, R5R'NC(S)-, adamantyl- C(O)-, or (5); R'' is H, C1-6alkyl, Ar-C0-6alkyl, or Het- C0-6alkyl; R''' is H, C2-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, or Het-C0-6alkyl; each R3 independently is H, C2-6alkenyl, C2-6alkynyl, Het, Ar or C1-6alkyl op- tionally substituted by OR', SR', NR'2, R'NC(O)OR5, CO2R', CO2NR'2, N(C=NH)NH2, Het or Ar; R4 is H, C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, R5C(O)-, R5C(S)-, R5SO2-, R5OC(O)- ,~R5R'NC(O)-, R5R'NC(S)-, R'HNCH(R')C(O)-, or R5OC(O)NR'CH(R')C(O)-; each R5 independently is C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, Ar-C0-6alkoxy, Het-C0-6alkoxy, or C1-6alkyl option- ally substituted by OR', SR', NR'2, R'NC(O)OR5, CO2R', CO2NR'2, N(C=NH)NH2, Het or Ar; R6 is H, C1-6alkyl, Ar-C0-6alkyl, or Het-C0-6alkyl and R7 is H, C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, R5C(O)-, R5C(S)-, R5SO2-, R5OC(O)-, R5R'NC(O)-, R5R'NC(S)-, R'HNCH(R')C(O)-, or R5OC(O)NR'CH(R')C(O)-; or R6 and R7 are connected to form a pyrrolidine, a piperidine, or a morpholine ring; each R' independently is H, C1-6alkyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R* is H, C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, or Het-C0-6alkyl; Y is a single bond or O; each Z independently is CO or CH2; and n is 0, 1, or 2; 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.

L'invention porte sur des composés de formule (I) dans laquelle: A est C(O) ou CH(OH); R<1> est (1), (2), (3) ou (4), R<2> est H, C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, R<5>C(O)-, R<5>SO2-, R<5>OC(O)-, R<5>R'NC(O)-, R<5>R'NC(S)-, adamantyl-C(O)-, ou (5); R" est H, C1-6alkyl, Ar-C0-6alkyl, ou Het-C0-6alkyl; R"' est H, C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, ou Het-C0-6alkyl; chaque R<3> est indépendamment H, C2-6alcényl, C2-6alcynyl, Het, Ar ou C1-6alkyl facultativement substitué par OR', SR', NR'2, R'NC(O)OR<5>, CO2R', CO2NR'2, N(C=NH)NH2, Het ou Ar; R<4> est H, C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, R<5>C(O)-, R<5>C(S)-, R<5>SO2-, R<5>OC(O)-, R<5>R'NC(O)-, R<5>R'NC(S)-, R'HNCH(R')C(O)-, ou R<5>OC(O)NR'CH(R')C(O)-; chaque R<5> est indépendamment C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, Ar-C0-6alkoxy, Het-C0-6alkoxy, ou C1-6alkyl facultativement substitué par OR', SR', NR'2, R'NC(O)OR<5>, CO2R', CO2NR'2, NC(C=NH)NH2, Het ou Ar; R<6> est H, C1-6alkyl, Ar-C0-6alkyl, ou Het-C0-6alkyl et R<7> est H, C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, R<5>C(O)-, R<5>C(S)-, R<5>SO2-, R<5>-OC(O)-, R<5>R'NC(O)-, R<5>R'NC(S)-, R'HNCH(R')C(O)-, ou R<5>OC(O)NR'CH(R')C(O)-; ou R<6> et R<7> sont liés pour constituer un cycle pyrrolidine, pipéridine ou morpholine; chaque R' est indépendamment H, C1-6alkyl, Ar-C0-6alkyl, ou Het-C0-6alkyl; R* est H, C1-6alkyl, C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, ou Het-C0-6alkyl; Y est une liaison simple ou O; chaque Z est indépendamment CO ou CH2; et n est 0, 1 or 2; ou leurs sels pharmacocompatibles qui sont des inhibiteurs de la protéase à cystéine et en particulier de la cathépsine K et servent au traitement de maladies dans lesquelles l'inhibition de la déperdition osseuse joue un rôle.

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