Bicyclic compounds as ring-constrained inhibitors of protein-tyrosine kinase p56lck

A study was undertaken to prepare inhibitors of the lymphocyte protein-tyrosine kinase p56lck. Using the known p56lck inhibitor 3,4-dihydroxy-alpha-cyanoci...

TR Burke，B Lim，VE Marquez，... - 《Journal of Medicinal Chemistry》

Discovery of Novel Selective Acetyl-CoA Carboxylase (ACC) 1 Inhibitors

We initiated our structure鈥揳ctivity relationship (SAR) studies for selective ACC1 inhibitors from 1a as a lead compound. SAR studies of bicyclic scaffolds revealed many potent and selective ACC1 inhibitors represented by 1f; however mo...

R Mizojiri，M Asano，D Tomita，... - 《Journal of Medicinal Chemistry》

BICYCLIC ACETYL-COA CARBOXYLASE INHIBITORS AND USES THEREOF

Clairmont, Cambridge, MA (US); Scott (58) Field of Classification Search Louis Cohen, Cambridge, MA (US); USPC .......... 548/407, 408,409, 465, 503: 514/4...

LC Kirman

Synthesis and evaluation of novel 8,6-fused bicyclic peptidomimetic compounds as interleukin-1β converting enzyme inhibitors

Two novel 8,6-fused bicyclic peptidomimetic ring systems were synthesized utilizing olefin metathesis as the key reaction for the formation of the eight-me...

Steven V. O’Neil and Yili Wang and Michael C. Laufersweiler and Kofi A. Oppong and David L. Soper and John A. Wos and Christopher D. Ellis and Mark W. Baize and Gregory K. Bosch and Amy N. Fancher and Wei Lu and Maureen K. Suchanek and Richard L. Wang and Biswanath De and Thomas P. Demuth Jr. - 《Bioorganic & Medicinal Chemistry Letters》

New Bicyclic compounds as PI3-K and mTor inhibitors

There is provided compounds of formula (I), wherein A1, A4, A4a,A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compou...

JP Fernandez，SM Gonzalez，A Rodriguez，...

BICYCLIC HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE

Bicyclic heteroaromatic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnorma...

RAMTOHUL YEEMAN K.，LI CHUN SING，LECLERC JEAN-PHILIPPE

Bridged bicyclic amino thiazine dioxide compounds as inhibitors of beta-secretase and methods of use thereof

The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Fo...

RT Lewis，JR Allen，J Brown，...

Benzodiazepine Compounds as Inhibitors of the Src Protein Tyrosine Kinase: Screening of a Combinatorial Library of 1,4-Benzodiazepines

We screened 1680 spatially separated compounds of a diverse combinatorial library of 1,4-benzodiazepines for their ability to inhibit the kinase activity o...

Latha，Ramdas，and，... - 《Archives of Biochemistry & Biophysics》