Identification of novel HSP90α/β isoform selective inhibitors using structure-based drug design. demonstration of potential utility in treating CNS disorders such as huntington's disease
A structure-based drug design strategy was used to optimize a novel benzolactam series of HSP90α/β inhibitors to achieve >1000-fold selectivity versus the HSP90 endoplasmic reticulum and mitochondrial isoforms (GRP94 and TRAP1, respectively). Selective HS
HSP-90 BINDING COMPOUNDS, COMPOSITIONS THEREOF, AND THEIR USE IΝ THE TREATMENT AND PREVENTION OF FUNGAL INFECTIONS
The invention relates to therapeutic compounds that bind to HSP90. The compounds disclosed herein bind HSP90 and alter the chaperoning capability of HSP90 proteins. The invention also relates to pharmaceutical compositions comprising these compounds, and methods of treating or preventing fungal infections.
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Page/Page column 82
(2012/10/08)
HSP90 MODULATING COMPOUNDS, COMPOSITIONS, METHODS AND USES
The invention relates to therapeutic compounds which bind to HSP90, said compounds containing a benzamide group bound to a tricyclic condensed ring system via the nitrogen atom of a pyrrole located in the center of the condensed system. The compounds disclosed herein bind HSP90 and alter the chaperoning capability of HSP90 proteins. Intermediate benzonitrile compounds which are precursors to the benzamide compounds are also disclosed. The invention also relates to pharmaceutical compositions comprising these compounds, and methods of treating diseases and disorders such as cancer, autoimmune diseases and other diseases.
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Page/Page column 65; 66
(2011/04/24)
Tetrahydroindole and Tetrahydroindazole Derivatives
The invention provides indole and indazole compounds of Formula (I) or pharmaceutically acceptable salts thereof which are useful for treating and/or preventing diseases and/or disorders ameliorated by the inhibition of Heat-Shock Protein 90. The invention further provides pharmaceutical compositions comprising compounds of Formula (I) and methods of preparing compounds of Formula (I).
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Page/Page column 39
(2008/12/04)
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