197080-73-2Relevant articles and documents
A New Lead Identification Strategy: Screening an sp3-rich and Lead-like Compound Library Composed of 7-Azanorbornane Derivatives
Karaki, Fumika,Umemoto, Sho,Ashizawa, Karin,Oki, Tomoya,Sato, Noriko,Ogino, Takumi,Ishibashi, Naoto,Someya, Ryoto,Miyano, Kanako,Hirayama, Shigeto,Uezono, Yasuhito,Fujii, Hideaki
, p. 1840 - 1848 (2019)
Although the advantages of sp3-rich, sterically complicated molecules in drug development have been pointed out, modern screening libraries are filled with planar, sp2-rich components. Compounds that are sp3-rich are difficult to synthesize, and thus we aimed to invent an efficient method to construct sp3-rich libraries. By modifying sp3-rich 7-azanorbornane scaffolds through click chemistry, we efficiently prepared a small set of compounds. These compounds were not only sp3-rich, but also had sufficient “lead-like” properties in view of molecular weights and hydrophobicity. Screening assays of this library provided weak κ opioid receptor agonists and growth hormone secretagogue receptor agonists with high hit rates. These results indicate that the 7-azanorbornane scaffold may be a “privileged structure” for lead identification in drug discovery.
PYRROLOPYRIDINE RETINOIC ACID RECEPTOR-RELATED ORPHAN RECEPTOR MODULATORS AND USES THEREOF
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Paragraph 0140; 0141, (2017/11/06)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.
COMPOUNDS AND USES THEREOF FOR THE MODULATION OF HEMOGLOBIN
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Paragraph 0344, (2015/05/26)
Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.