Invention Grant
- Patent Title: Furo[3, 2-B] pyrrol-3-ones as cathespin S inhibitors
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Application No.: US13745413Application Date: 2013-01-18
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Publication No.: US08552202B2Publication Date: 2013-10-08
- Inventor: Martin Quibell , John Paul Watts , Nicholas Sean Flinn
- Applicant: Amura Therapeutics Limited
- Applicant Address: GB Cambridge
- Assignee: Amura Therapeutics Limited
- Current Assignee: Amura Therapeutics Limited
- Current Assignee Address: GB Cambridge
- Agency: Sunstein Kann Murphy & Timbers LLP
- Priority: GB0804701.1 20080313
- Main IPC: C07D417/14
- IPC: C07D417/14 ; A61K31/428
![Furo[3, 2-B] pyrrol-3-ones as cathespin S inhibitors](/abs-image/US/2013/10/08/US08552202B2/abs.jpg.150x150.jpg)
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.
Public/Granted literature
- US20130150345A1 FURO[3, 2-B] PYRR0L-3-ONES AS CATHESPIN S INHIBITORS Public/Granted day:2013-06-13
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