Patent Number: 8,877,927

Title: Furo[3,2-B] pyrrol -3-one derivatives and their use as cysteinyl proteinase inhibitors

Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof (I), wherein: one of R.sup.1 and R.sup.2 is H, and the other is selected from F and Cl, or R.sup.1 and R.sup.2 are both F; R.sup.3 is selected from cyclopentyl and cyclohexyl; R.sup.4 is an optionally substituted 5- or 6-membered monocyclic or an 8- to 10-membered bicyclic aryl or heteroaryl ring which includes up to four heteroatoms. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain. ##STR00001##

Inventors: Quibell; Martin (Cambridge, GB), Watts; John Paul (Cambridge, GB)

Assignee: Grunenthal GmbH

International Classification: A61K 31/496 (20060101); A61P 29/00 (20060101); A61K 31/454 (20060101); A61P 19/00 (20060101); G01N 33/53 (20060101); C07D 491/044 (20060101)

Expiration Date: 2019-11-04 0:00:00