EP 0923535 A1 19990623 - INHIBITORS OF CYSTEINE PROTEASE
Title (en)
INHIBITORS OF CYSTEINE PROTEASE
Title (de)
INHIBITOREN DER CYSTEIN-PROTEASE
Title (fr)
INHIBITEURS DE CYSTEINE PROTEASE
Publication
Application
Priority
- US 9715029 W 19970826
- US 2484896 P 19960828
Abstract (en)
[origin: WO9808802A1] This invention relates to compounds of formula (I), wherein R<1> is (i), (ii), (iii), or (iv); R<2> is 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)-, adamantyl-C(O)- or (v); 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; each R<3> independently is H, C2-6alkenyl, C2-6alkynyl, Het, Ar or C1-6alkyl optionally substituted by OR', SR', NR'2, R'NC(O)OR<5>, CO2R', CO2NR'2, N(C=NH)NH2, Het or Ar; R<4> is 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)-, or R<5>OC(O)NR'CH(R')C(O)-; each R<5> independently 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, R'NC(O)OR<5>, CO2R', CO2NR'2, N(C=NH)NH2, Het or Ar; R<6> is H, C1-6alkyl, Ar-C0-6alkyl or Het-C0-6alkyl and R<7> is 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)- or R<5>OC(O)NR'CH(R')C(O)-; or R<6> and R<7> 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 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.
IPC 1-7
IPC 8 full level
C07D 307/91 (2006.01); A61K 31/165 (2006.01); A61K 31/166 (2006.01); A61K 31/215 (2006.01); A61K 31/343 (2006.01); A61P 19/02 (2006.01); A61P 19/10 (2006.01); C07C 237/04 (2006.01); C07C 271/22 (2006.01)
CPC (source: EP)
A61P 19/02 (2017.12); A61P 19/10 (2017.12); C07C 237/04 (2013.01); C07C 271/22 (2013.01); C07C 2601/08 (2017.04); C07C 2601/14 (2017.04)
Designated contracting state (EPC)
BE CH DE DK FR GB IT LI NL
DOCDB simple family (publication)
WO 9808802 A1 19980305; EP 0923535 A1 19990623; EP 0923535 A4 20010110; JP 2000517319 A 20001226
DOCDB simple family (application)
US 9715029 W 19970826; EP 97938632 A 19970826; JP 51185898 A 19970826