Icahn School of Medicine at Mount Sinai

Nilesh Zaware

Michael H Ohlmeyer

Ming-Ming Zhou

Adam Vincek

Claudia Kim

David Kastrinsky

Chunyan Ren

Matthew Galsky

Sudeh Izadmehr

A genus of bicyclic inhibitors of CBX chromodomains is disclosed. The compounds are of the following genus: in which A, E, and G represent carbon or nitrogen such that the compounds are indoles or benzimidazoles. A particular subgenus of 1,3-disubstituted-1,3-dihydro-2H-benzo[d]imidazol-2-imines is of the general formula: The compounds inhibit CBX proteins.

Bicyclic inhibitors of CBX chromodomains

A genus of arylsulfonamide derivatives of heterocyclic constrained tricyclic compounds is disclosed. The compounds are of the following genus:  The compounds induce FOXO1 transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a therapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.

Heterocyclic constrained tricyclic sulfonamides as anti-cancer agents

A process for the stereoselective synthesis of chiral 3-heterocyclyl-1,2-dihydroxy cyclohexanes is disclosed. The process involves reacting a tricyclic nitrogenous heterocycle with an allyl carbonate in the presence of a chiral palladium catalyst followed by oxidation of the olefinic bond to provide 3-heterocyclyl-1,2-dihydroxy cyclohexanes, cyclopentanes and corresponding alicyclic heterocycles. Also disclosed are methods for converting the heterocyclyl-1,2-dihydroxy cyclohexanes to 2-amino-6-(heteroaryl)cyclohexanols (and related cyclic compounds).

Stereospecific process for 3-heterocyclylcycloaliphatic-1,2-diols

Cyclic vinylogous amides of Formula I are disclosed The compounds are useful for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are inhibitors of bromodomain.

Cyclic vinylogous amides as bromodomain inhibitors

Cyclic vinylogous amides of Formula I are disclosed  The compounds are useful for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are inhibitors of bromodomain.

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Briarwood, NY, United States of America

Nilesh Zaware