C07C229/14

MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same.

MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same.

P62-ZZ CHEMICAL INHIBITOR
20230406813 · 2023-12-21 ·

A method for treating a p62-mediated disease (e.g., multiple myeloma) in a subject, the method comprising administering to the subject a therapeutically effective amount of at least one p62-ZZ inhibitor compound.

P62-ZZ CHEMICAL INHIBITOR
20230406813 · 2023-12-21 ·

A method for treating a p62-mediated disease (e.g., multiple myeloma) in a subject, the method comprising administering to the subject a therapeutically effective amount of at least one p62-ZZ inhibitor compound.

BICYCLIC COMPOUNDS AS INHIBITORS OF PD1/PD-L1 INTERACTION/ACTIVATION

The compounds of Formula I is described herein along with their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof. The compounds described herein, their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof are bicyclic compounds that are inhibitors of PD-1/PD-L1 interaction/activation.

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Automated Synthesis of Small Molecules Using Chiral, Non-Racemic Boronates
20210009508 · 2021-01-14 ·

Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.

Automated Synthesis of Small Molecules Using Chiral, Non-Racemic Boronates
20210009508 · 2021-01-14 ·

Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.

INDANES AS PD-L1 INHIBITORS

Compounds represented by Formula (I) or (II):

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are provided herein, or a pharmaceutically acceptable salt, or a prodrug or bioisostere thereof; wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, Y, Y, and the subscripts m and n are as defined herein.

COMPOUNDS FOR TREATMENT OF PD-L1 DISEASES

Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I)

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including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.3, R.sup.3a, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and the subscript n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

UNIVERSAL BUILDING BLOCKS FOR RADIOLABELING

The present invention describes novel chelators (multidentate ligands) and precompounds for complexation of radiometals and non-radioactive counterparts, for use in radiopharmacy. The invention includes a process and a kit involving such chelators.

Active moieties directing to a pharmaceutical target (such as peptides or proteins) can be attached to the chelator very easily via the so called click-chemistry forming a triazole-ring moiety. The aromatic triazole-nitrogen itself acts as a new and soft nucleophilic site enabling for complexation of various radiometals or non-radioactive counterparts. The chelators are capable of fast complexation at low temperature.

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