Publication number: 20110112089
Abstract: A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(?O)2; where Ra is H, C1-C4 alkyl or CH3C(?O); R5 is independently selected from H or methyl; E is —C(?O)—, —S(?O)m—, —NR5S(?O)m—, —NR5C(?O)—, —OC(?O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or hetorocycle; m is independently 0, 1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
Type:
Application
Filed:
January 19, 2011
Publication date:
May 12, 2011
Applicant:
Medivir AB
Inventors:
Magnus NILSSON, Xiao-Xiong ZHOU, Lourdes ODEN, Bjorn CLASSON, Rolf NOREN, Urszula GRABOWSKA, Philip JACKSON, Philip FALLON, Andrew CARR, Mark LILEY, Matt TOZER, Tony JOHNSON, Victor DIAZ, Laia CRESPO, Jussi KANGASMETSA, Thierry BONNAUD
Patent number: 7915300
Abstract: A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(?O)2; where Ra is H, C1-C4 alkyl or CH3C(?O); R5 is independently selected from H or methyl; E is —C(?O)—, —S(?O)m—, —NR5S(?O)m—, —NR5C(?O)—, —OC(?O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or heterocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
Type:
Grant
Filed:
January 6, 2005
Date of Patent:
March 29, 2011
Assignee:
Medivir AB
Inventors:
Magnus Nilsson, Xiao-Xiong Zhou, Lourdes Oden, Bjorn Classon, Rolf Noren, Urszula Grabowska, Philip Jackson, Philip Fallon, Andrew Carr, Mark Liley, Matt Tozer, Tony Johnson, Victor Diaz, Laia Crespo, Jussi Kangasmetsa, Thierry Bonnaud
Publication number: 20080234260
Abstract: A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(?O)2; where Ra is H, C1-C4 alkyl or CH3C(?O); R5 is independently selected from H or methyl; E is —C(?O)—, —S(?O)m—, —NR5S(?O)m—, —NR5C(?O)—, —OC(?O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or heterocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
Type:
Application
Filed:
January 6, 2005
Publication date:
September 25, 2008
Inventors:
Magnus Nilsson, Xiao-Xiong Zhou, Lourdes Oden, Bjorn Classon, Rolf Noren, Urszula Grabowska, Philip Jackson, Philip Fallon, Andrew Carr, Mark Liley, Matt Tozer, Tony Johnson, Victor Diaz, Laia Crespo, Jussi Kangasmetsa, Thierry Bonnaud