Princeton University

Crescenta Biosciences

Hahn Kim

Joshua D Rabinowitz

Gregory S Ducker

Jonathan M Ghergurovich

Emre Koyuncu

Gokhan Hotamisligil

Hsin-Jung Li

Zemer Gitai

Max Wilson

James Martin

A method for treating a viral disease in a subject comprising administering to said subject a therapeutically effective dose of one or more compounds that bind to fatty acid binding protein FABP4, with compounds described in the specification some having the general formula, Formula I-Formula XII, where W-W, Z-Z, Z-Z, X, Y, n, and R-Rare as defined in the claims and description of embodiments. In examples, the ring Z contains Z-Z. In other examples, the ring Z contains Z-Z.

Antiviral use of FABP4 modulating compounds

A novel class of compounds according to Formula I, II, or III, wherein W-W, Z-Z, Z-Z, X, Y, n, and R-Rare as defined in the claims and description of embodiments that bind to fatty acid binding protein FABP4 and modulate adipocyte metabolism to drive enhanced glucose utilization, as well as pharmaceutical compositions comprising the class of compounds, in combination with a pharmaceutically acceptable diluent or carrier, and optionally, further in combination with a therapeutically active agent, and the use of these compounds in medicine and for the preparation of a medicament in the treatment of disorders acting on the FABP4. In examples, the ring Z contains Z-Z. In other examples, the ring Z contains Z-Z.

Cell metabolism modulating compounds and uses thereof

The disclosure provides compounds. In certain embodiments, compounds of the disclosure are capable of inhibiting a mammalian SHMT, such as human SMHT1 and/or SHMT2. Compounds of the disclosure have numerous uses.

SHMT inhibitors

In one aspect, methods of treating bacterial infections are described herein employing compounds having more than one target for antibacterial activity. Additionally pharmaceutical compositions comprising such compounds are also described.

Compounds having antibacterial activity and methods of use

The disclosure provides compounds of Formulae (I)-(IX). The disclosed compounds are capable of inhibiting a mammalian SHMT. Compounds of the disclosure have numerous uses, such as for treatment of cancer or autoimmune disorders.

The present invention relates to a method for the treatment of cancer or an autoimmune disorder, comprising the administration of a serine hydroxymethyltransferase (SHMT) inhibitor, and in particular the administration of pyrazolopyran compounds of Formula (VI) as presently described, wherein the compounds are capable of inhibiting a mammalian SHMT, such as human SHMT1 and/or SHMT2. The treatment method further comprises the optional administration of an additional agent as a rescue therapy to reduce toxicity, wherein said agent may be chosen from formate, a formate salt, folinic acid, formate ester, or leucovorin.

The disclosure provides compounds of Formulae (I)-(IX). The disclosed compounds are capable of inhibiting a mammalian SHMT. Compounds of the disclosure have numerous uses, such as for treatment of cancer or autoimmue disorders.

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Princeton, NJ, United States of America

Hahn Kim