Northwestern University

Dow Global Technolgoies LLC

University of Chicago

Karl A Scheidt

Bi-Shun Zeng

Raymond C Bergan

Gary E Schiltz

Rick C Betori

Herbert Y Meltzer

Ansoo Lee

Li Xu

Omar K Farha

Joseph T Hupp

Brice E Uno

Benjamin R McDonald

Richard C Betori

Christopher Check

John M Roberts

Ashkaan Younai

Kipo P Jang

Stephen Joseph Kron

John M Torkelson

William Hoy Heath

Nathan Wilmot

Steven T Rosen

Matthew R Clutter

Yue Liu

Nancy L Krett

Javier Izquierdo Ferrer

Michael Todd Hovey, Jr

Vincent Lombardo

Emily Leitsch

Elizabeth Dhulst

Elizabeth O McCusker

Ada J Kwong

Margaret Marie Biddle

Mark A Maskeri

Adam J Csakai

Disclosed herein are agents that target telomerase reverse transcriptase (TERT) for treating cancer and sensitizing cancer cells to genotoxic therapy. The methods include inhibiting induction of an immunosuppressive factor in a subject in need thereof, the method comprising administering an inhibitor of TERT to the subject.

Agents that target telomerase reverse transcriptase (TERT) for treating cancer and sensitizing cancer cells to genotoxic therapy

Disclosed are 3-methylideneoxan-4-one compounds, derivatives thereof, and methods of their synthesis and methods of their use in treating a disease or disorder in a subject in need thereof, such as diseases and disorders that are associated with telomerase activity such as cancer. The disclosed compounds may be formulated in a pharmaceutical composition for treating diseases and disorders that are associated with telomerase activity such as cancer.

3-methylideneoxan-4-one compounds and substituted derivates thereof as inhibitors of telomerase

Disclosed are chromane compounds, analogs thereof, and methods of their synthesis and use. The compounds may be synthesized by methods involving reductive annulations of arylidene malonates with unsaturated electrophiles using photoredox/Lewis acid cooperative catalysis. The compounds may be formulated in a pharmaceutical composition for treating one of the aforementioned diseases or disorders.

Substituted chromanes, analogs thereof, and methods of use and synthesis

Disclosed are compounds, pharmaceutical compositions, and methods of treatment. The disclosed compounds are based on fused 1,4-diazepine and pyrrolidinedione scaffolds. The compounds may be utilized in pharmaceutical compositions and methods for treating diseases and disorders associated with cell proliferation such as cancer and may have a formula illustrated as follows:

Substituted fused pyrrolo-diazepinones and uses thereof

Disclosed are complexes and methods of using the complexes as catalysts for addition of amines to unsaturated electrophiles, as well as novel compounds produced by the disclosed complexes and methods. The disclosed methods may utilize the disclosed complexes as catalysts for adding unprotected primary amines and secondary amines to unsaturated electrophiles in an enantioselective manner to produce novel compounds which may include amino substituted succinimide compounds.

Catalysts and methods for enantioselective conjugate addition of amines to unsaturated electrophiles

Disclosed are enantioselective cross dehydrogenative coupling reactions for synthesizing tetrahydropyran compounds. Novel tetrahydropyran compounds may be synthesized by the disclosed methods as well as tetrahydropyran precursor compounds for synthesizing various naturally occurring compounds. The enantioselective cross dehydrogenative coupling reactions utilize in situ Lewis Acid activation in combination with oxidative formation of an oxocarbenium ion to provide a highly efficient and selective coupling reaction for synthesizing tetrahydropyran compounds.

Enantioselective cross dehydrogenative coupling reactions and compounds synthesized by the reactions

3-methylideneoxan-4-one compounds and substituted derivatives thereof as inhibitors of telomerase

Disclosed are novel small molecules, methods of synthesis of the small molecules, and uses of the small molecules for modulating activity of the human serotonin receptor 2C (5-HT), preferably selectively. The small molecules have a substituted beta-carboline core structure, which optionally may be saturated at one or more bonds to provide a dihydro-beta-carboline core or a tetrahydro-beta-carboline core. The small molecules may be administered to treat and/or prevent diseases, disorders, and/or conditions associated with human serotonin receptor 2C (5-HT) including psychiatric, mental, and/or neurological diseases, disorders, and conditions such as cognitive impairment, addiction, and obsessive compulsive disorder. The disclosed small molecules also may be administered to treat and/or prevent obesity, for example, via appetite suppression.

Beta-carbolines as positive allosteric modulators of the human serotonin receptor 2C (5-HT)

Disclosed herein are tetrahydropyranoindole compounds and derivatives thereof, as well as their methods of synthesis and use. The disclosed compounds may be synthesized by methods that utilize a cooperative hydrogen bond donor/Br&#xf8;nsted acid system. The disclosed compounds may be useful for treating a disease, disorder, or a symptom thereof in a subject in need thereof, such as pain, swelling, and joint stiffness. The disclosed compounds also may be useful for treating cell proliferative diseases and disorders such as cancer.

Substituted tetrahydropyranoindoles, derivatives thereof, and their methods of synthesis and use

Disclosed are dihydrobenzoxazinone compounds, dihydroquinolone compounds, and methods of their synthesis. The disclosed compounds may be prepared by reacting a benzoxazinedione compound and a ketone compound in the presence of an N-heterocyclic carbine (NHC) catalyst to perform a NHC-catalyzed decarboxylative cycloaddition. The disclosed compounds may be utilized to treat diseases and disorders associated with the biological activity of dihydrobenzoxazinone compounds and dihydroquinolone compounds.

Substituted dihydrobenzoxazinones, dihydroquinolones, and methods of  their use and synthesis

Disclosed are indazole compounds and derivatives thereof for use as modulators of the activity of mitogen-activated protein kinase 4 (MEK4). The disclosed compounds include 3-Arylindazoles which may be formulated in pharmaceutical composition for treating cell proliferative diseases and disorders associated with MEK4 activity, including cancer.

3-arylindazoles as selective MEK4 inhibitors

Disclosed are compounds, pharmaceutical compositions, and methods of treatment. The disclosed compounds are based on fused 1,4-diazepine and pyrrolidinedione scaffolds. The compounds may be utilized in pharmaceutical compositions and methods for treating diseases and disorders associated with cell proliferation such as cancer and may have a formula illustrated as follows: 

Catalysts and methods for enantioselective conjugate additions of amines to unsaturated electrophiles

Growing community of inventors

Evanston, IL, United States of America

Karl A Scheidt