- Proline Sulfonamide-Catalyzed, Domino Process for Asymmetric Synthesis of Amino- and Hydroxy-Substituted Bicyclo[2.2.2]octanes
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A generalized method for accessing highly functionalized amino-substituted bicyclo[2.2.2]octanes via p-dodecylphenylsulfonamide catalyst in a good enantio- and diastereoselective fashion has been developed. A discussion of the mechanistic underpinnings of this transformation is presented. Finally, an unexpected discovery enabling the extension of this protocol to the synthesis of OH-substituted bicyclo[2.2.2]octanes with encouraging levels of stereoselectivity is discussed.
- El-Mansy, Mohamed F.,Kang, Jun Yong,Lingampally, Rajinikanth,Carter, Rich G.
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- Design and Synthesis of Fungal-Selective Resorcylate Aminopyrazole Hsp90 Inhibitors
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The molecular chaperone Hsp90, essential in all eukaryotes, plays a multifaceted role in promoting survival, virulence, and drug resistance across diverse pathogenic fungal species. The chaperone is also critically important, however, to the pathogen's hu
- Huang, David S.,Leblanc, Emmanuelle V.,Shekhar-Guturja, Tanvi,Robbins, Nicole,Krysan, Damian J.,Pizarro, Juan,Whitesell, Luke,Cowen, Leah E.,Brown, Lauren E.
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p. 2139 - 2180
(2019/10/11)
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- HSP90 INHIBITORS AND USES THEREOF
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Herein is described the design and synthesis of resorcylate aminopyrazole compounds. These compounds show broad, potent and fungal-selective Hsp90 inhibitory activity. These compounds also find use in treating Hsp90 related deseases.
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Paragraph 00178; 00198
(2020/11/23)
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- INDOLE AHR INHIBITORS AND USES THEREOF
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The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.
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Paragraph 00548-00549
(2018/11/22)
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- CRF1 RECEPTOR LIGANDS COMPRISING FUSED BICYCLIC HETEROARYL MOIETIES
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Substituted heteroaryl fused pyridine, pyrazine, and related heterobicyclic compounds that act as selective modulators of CRF1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, gastrointestinal disorders, and eating disorders. Methods of treatment of such disorders as well as packaged pharmaceutical compositions are also provided. Compounds provided herein are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
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Page/Page column 65
(2008/12/07)
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- A Facile Synthesis of 8-(β-D-Ribofuranosyl)-4-thioxo-3H-pyrazolo-1,3,5-triazine and Its α-Anomer
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A versatile intermediate 2 for C-nucleoside synthesis was treated with thiosemicarbazide to obtain thiosemicarbazone 6, which was then converted to 3-aminopyrazol-2N-thiocarboxamide derivatives 7 and 8 by the reaction of 6 and sodium ethoxide. 4-Thioxo-4H-pyrazolo-1,3,5-triazine C-nucleosides 11 and 12 were obtained by the ring closure reaction of 7 and 8 with triethyl orthoformate.Brief treatment of 11 and 12 with 10percent methanolic hydrogen chloride afforded C-nucleosides 4 and 13, respectively, without anomerization.Identification of compounds 4 and 13 was madeon the basis of 1H nmr and uv spectra, as well as chemical conversion to known compounds with established configurations.Model compounds were also synthesized in order to confirm the heterocyclic moieties.
- Chu, Chung K.
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p. 389 - 392
(2007/10/02)
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