EP 1015438 A4 20001108 - PROTEASE INHIBITORS
Title (en)
PROTEASE INHIBITORS
Title (de)
PROTEASE INHIBITOREN
Title (fr)
INHIBITEURS DE PROTEASES
Publication
Application
Priority
- US 9818289 W 19980903
- US 5752797 P 19970904
Abstract (en)
[origin: WO9911637A1] The present invention provides compounds of Formula (I) wherein X, X1, X2, and X3 are independently selected from -H, -C1-6alkyl, -C1-6alkyl substituted by 1-3 fluorines, -C3-7cycloalkyl, -CN, -C(O)R1, -C(O)OR1, -C(O)NR1R2, -C(NR1)NR1R2, -C(NCN)NR1R2, -C(NCN)SR3, -NO2, -NR1SO2R3, -NR1C(O)R1, -NR1R2, -NR1(C=NR1)NR1R2, -NR1C(O)NR1R2, -NR1C(O)R1, -NR1C(O)OR3, -NR1C(NCN)SR3, -NR1C(NCN)NR1R2, -NR1C(O)C(O)NR1R2, -NR1C(O)C(O)R2, -Cl, -Br, -I, -F, -OR1, -O(CH2)qOR3, -O(CH2)2OH, -OC(O)R1, -O(CH2)qC(O)NR1R2, -O(CH2)qC(O)R1, -SR1, -SO2NR1R2 or -S(O)mR3; m is 0, 1 or 2; q is 1 or 2; n is 0 to 2; R1 is -H, -C1-6alkyl, -CF3 or -CH2CF3; or when R1 and R2 are taken together as NR1R2, they may together with the nitrogen form a 5 to 7 membered ring comprised of carbon or carbon and one or more additional heteroatoms selected from O, N, or S; R2 is H, -C1-6alkyl, -CF3 or -CH2CF3; R3 is -C1-6alkyl, -CF3 or -CH2CF3; and X4 is -H, -C1-6alkyl, -C3-7cycloalkyl, -COAr, -COOC1-6alkyl, or COOAr; which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease therewith.
IPC 1-7
IPC 8 full level
A61K 31/426 (2006.01); A61K 31/427 (2006.01); A61P 1/02 (2006.01); A61P 19/02 (2006.01); A61P 19/08 (2006.01); A61P 19/10 (2006.01); A61P 29/00 (2006.01); A61P 43/00 (2006.01); C07D 277/20 (2006.01); C07D 277/42 (2006.01); C07D 277/48 (2006.01)
CPC (source: EP)
A61P 1/02 (2017.12); A61P 19/00 (2017.12); A61P 19/02 (2017.12); A61P 19/08 (2017.12); A61P 19/10 (2017.12); A61P 29/00 (2017.12); A61P 43/00 (2017.12); C07D 277/48 (2013.01)
Citation (search report)
- [A] PATENT ABSTRACTS OF JAPAN vol. 009, no. 091 (C - 277) 19 April 1985 (1985-04-19)
- See references of WO 9911637A1
Designated contracting state (EPC)
BE CH DE ES FR GB IT LI NL
DOCDB simple family (publication)
WO 9911637 A1 19990311; AU 9300298 A 19990322; CA 2302361 A1 19990311; CO 4970736 A1 20001107; EP 1015438 A1 20000705; EP 1015438 A4 20001108; JP 2001514257 A 20010911; MA 26540 A1 20041220; PE 115699 A1 20000113; SA 98190653 A 20051203; ZA 988064 B 19990528
DOCDB simple family (application)
US 9818289 W 19980903; AU 9300298 A 19980903; CA 2302361 A 19980903; CO 98050517 A 19980903; EP 98945850 A 19980903; JP 2000508676 A 19980903; MA 25238 A 19980901; PE 00083098 A 19980904; SA 98190653 A 19981017; ZA 988064 A 19980903