244768-98-7Relevant academic research and scientific papers
Inhibitors of Bruton's Tyrosine Kinase
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Page/Page column 110, (2012/03/08)
This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y4, are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
Azabicyclic sulfonamides as potent 11β-HSD1 inhibitors
Shah, Unmesh,Boyle, Craig D.,Chackalamannil, Samuel,Baker, Hana,Kowalski, Timothy,Lee, Julie,Terracina, Giuseppe,Zhang, Lili
scheme or table, p. 1551 - 1554 (2010/06/16)
Inhibition of 11β-HSD1 has demonstrated potential in the treatment of various components of metabolic syndrome. We wish to report herein the discovery of novel azabicyclic sulfonamide based 11β-HSD1 inhibitors. Highly potent compounds exhibiting inhibitor
SUBSTITUTED BICYCLIC PIPERIDINYL-AND PIPERAZINYL- SULFONAMIDES USEFUL TO INHIBIT 11β-HYDROXYSTEROID DEHYDROGENASE TYPE-1
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Page/Page column 53, (2009/04/25)
In its many embodiments, the present invention relates to a novel class of substituted bicyclic piperidinyl- and piperazinylsulfonamide compounds useful to inhibit 11β-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11β-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
Synthesis of substituted 2,5-diazabicyclo[2.2.1]heptanes
Yakovlev,Lobanov,Potekhin
, p. 429 - 431 (2007/10/03)
A new method is proposed for the synthesis of substituted 2,5-diazabicyclo[2.2.1]heptanes from 1-(tertbutoxycarbonyl)-4-tosyloxy-2-(tosyloxymethyl)pyrrolidine. 1H NMR spectroscopy indicated multiple conformations of 2-(tert-butoxycarbonyl)-2,5-
