NOVEL HETEROARYL HETEROCYCLYL COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASE
The present invention relates to compounds of formula (I), ab (I), wherein R1 to R3 and L are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
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Page/Page column 86-87
(2020/01/08)
GLYCOSIDASE INHIBITORS
Compounds of formula (I) wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
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Page/Page column 113; 114
(2017/09/15)
GLYCOSIDASE INHIBITORS
Compounds of formula (I) wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
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Page/Page column 98-99
(2017/09/15)
Novel Autotaxin Inhibitors for the Treatment of Osteoarthritis Pain: Lead Optimization via Structure-Based Drug Design
In an effort to develop a novel therapeutic agent aimed at addressing the unmet need of patients with osteoarthritis pain, we set out to develop an inhibitor for autotaxin with excellent potency and physical properties to allow for the clinical investigation of autotaxin-induced nociceptive and neuropathic pain. An initial hit identification campaign led to an aminopyrimidine series with an autotaxin IC50 of 500 nM. X-ray crystallography enabled the optimization to a lead compound that demonstrated favorable potency (IC50 = 2 nM), PK properties, and a robust PK/PD relationship.
Jones, Spencer B.,Pfeifer, Lance A.,Bleisch, Thomas J.,Beauchamp, Thomas J.,Durbin, Jim D.,Klimkowski, V. Joseph,Hughes, Norman E.,Rito, Christopher J.,Dao, Yen,Gruber, Joseph M.,Bui, Hai,Chambers, Mark G.,Chandrasekhar, Srinivasan,Lin, Chaohua,McCann, Denis J.,Mudra, Daniel R.,Oskins, Jennifer L.,Swearingen, Craig A.,Thirunavukkarasu, Kannan,Norman, Bryan H.
supporting information
p. 857 - 861
(2016/10/12)
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