- Proteasome inhibitor delanzomib for use in the treatment of lupus
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The present invention provides a method for treating lupus in a subject, comprising the step of administering to the subject Compound A.
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Page/Page column 19
(2016/06/06)
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- Development and scale-up of an optimized route to the peptide boronic acid, CEP-18770
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CEP-18770 is an unstable peptide boronic acid and an amorphous solid, making it a challenging synthetic target. Process R&D led to a new process that avoided chromatography through crystalline intermediates, increased atom and volume efficiency, provided
- Roemmele, Renee C.,Christie, Michael A
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p. 422 - 426
(2013/06/05)
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- PROTEASOME INHIBITORS AND PROCESSES FOR THEIR PREPARATION, PURIFICATION AND USE
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The invention provides boronic esters of Formula (I) wherein R1, R2, R3, and R4 are as described herein, and methods for the preparation and purification thereof.
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Page/Page column 118-119
(2011/08/04)
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- Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer
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The ubiquitin-proteasome pathway plays a central role in regulation of the production and destruction of cellular proteins. These pathways mediate proliferation and cell survival, particularly in malignant cells. The successful development of the 20S human proteasome inhibitor bortezomib for the treatment of relapsed and refractory multiple myeloma has established this targeted intervention as an effective therapeutic strategy. Herein, the potent, selective, and orally bioavailable threonine-derived 20S human proteasome inhibitor that has been advanced to preclinical development, [(1R)-1-[[2S,3R)-3-hydroxy-2-[(6-phenylpyridine-2-carbonyl)amino]-1-oxobutyl] amino]-3-methylbutyl]boronic acid 20 (CEP-18770), is disclosed.
- Dorsey, Bruce D.,Iqbal, Mohamed,Chatterjee, Sankar,Menta, Ernesto,Bernardini, Raffaella,Bernareggi, Alberto,Cassarà, Paolo G.,D'Arasmo, Germano,Ferretti, Edmondo,De Munari, Sergio,Oliva, Ambrogio,Pezzoni, Gabriella,Allievi, Cecilia,Strepponi, Ivan,Ruggeri, Bruce,Ator, Mark A.,Williams, Michael,Mallamo, John P.
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p. 1068 - 1072
(2008/12/22)
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- PROTEASOME INHIBITORS AND METHODS OF USING THE SAME
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The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.
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Page/Page column 200
(2008/06/13)
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