Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R3 and R4 is H, and the other is selected from C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, and C6-12-aralkyl; or R3 and R4 are each independently selected from C1-6-alkyl and halo; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high efficacies for human cathepsin S, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, Sjogrens syndrome, Grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.
Type:
Grant
Filed:
October 4, 2013
Date of Patent:
January 13, 2015
Assignee:
Amura Limited
Inventors:
Martin Quibell, John Paul Watts, Nicholas Sean Flinn
Abstract: An oxapenem compound which is, or is capable of forming, a zwitterion of formula wherein R is a C1-C8 branched or straight chain alkyl group which is substituted by a protonated nitrogen base. The compounds find particular use as high bioavailability ?-lactamase inhibitors.
Type:
Grant
Filed:
October 11, 2001
Date of Patent:
July 24, 2007
Assignee:
Amura Limited
Inventors:
Hans Rudolf Pfaendler, Iain Nelson Simpson