- Practical synthesis of a cathepsin S Inhibitor: Route identification, purification strategies, and serendipitous discovery of a crystalline salt form
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Chemical Equation Presented A redox economical strategy resulted in a concise, modular synthesis of compound 1, a potent Cathepsin S inhibitor. Starting from three building blocks, crude drug substance was prepared, in a two-step sequence in high yield. Efficient purification of the crude drug substance was accomplished via the formation of an unusual monoethyl oxalate salt.
- Deng, Xiaoliu,Liang, Jimmy T.,Peterson, Matthew,Rynberg, Raymond,Cheung, Eugene,Mani, Neelakandha S.
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experimental part
p. 1940 - 1947
(2010/05/18)
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- PROCESSES FOR THE PREPARATION OF CARBON-LINKED TETRAHYDRO-PYRAZOLO-PYRIDINE MODULATORS OF CATHEPSIN S
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Method of making carbon-linked tetrahydro-pyrazolo-pyridine compounds of the following Formula (I) and pharmaceutically acceptable salts thereof: comprising reacting a compound of formula (IX): with a compound of formula (X): to form a compound of Formula
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- Pyrazole-based cathepsin S inhibitors with arylalkynes as P1 binding elements
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A crystal structure of 1 bound to a Cys25Ser mutant of cathepsin S helped to elucidate the binding mode of a previously disclosed series of pyrazole-based CatS inhibitors and facilitated the design of a new class of arylalkyne analogs. Optimization of the
- Ameriks, Michael K.,Axe, Frank U.,Bembenek, Scott D.,Edwards, James P.,Gu, Yin,Karlsson, Lars,Randal, Mike,Sun, Siquan,Thurmond, Robin L.,Zhu, Jian
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scheme or table
p. 6131 - 6134
(2010/06/13)
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- CARBON-LINKED TETRAHYDRO-PYRAZOLO-PYRIDINE MODULATORS OF CATHEPSIN S
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Carbon-linked tetrahydro-pyrazolo-pyridine compounds are described, which are useful as cathepsin S modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by cathepsin S activity, such as psoriasis, pain, multiple sclerosis, atherosclerosis, and rheumatoid arthritis.
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