The present disclosure relates to bifunctional compounds, which find utility as modulators of enhancer of zeste homolog 2 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

The present disclosure relates to bifunctional compounds, which find utility as modulators of enhancer of zeste homolog 2 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

This disclosure provides multifunctional conjugate molecules in which at least one therapeutic agent is covalently attached to a cannabinoid. The disclosed conjugate molecules are designed to deliver therapeutic benefits of both components, with release of the cannabinoid upon binding of the therapeutic agent component to its target conveying further therapeutic benefits, and can be used to treat cancer, glaucoma, confusion or dementia, and other disorders.

This disclosure provides multifunctional conjugate molecules in which at least one therapeutic agent is covalently attached to a cannabinoid. The disclosed conjugate molecules are designed to deliver therapeutic benefits of both components, with release of the cannabinoid upon binding of the therapeutic agent component to its target conveying further therapeutic benefits, and can be used to treat cancer, glaucoma, confusion or dementia, and other disorders.

Disclosed are bispecific compounds (degraders) that target ERK5 for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat cancer and inflammatory diseases.

Disclosed are bispecific compounds (degraders) that target ERK5 for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds to treat cancer and inflammatory diseases.

The present invention provides a BET (protein) degrader, specifically a BET degrader containing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof:

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wherein L1 and L2 are the same or different and each represents a small molecular ligand for BET protein, and S represents a group represented by a formula selected from the group consisting of formulas (S1) to (S18).

The present invention provides a BET (protein) degrader, specifically a BET degrader containing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof:

##STR00001##

wherein L1 and L2 are the same or different and each represents a small molecular ligand for BET protein, and S represents a group represented by a formula selected from the group consisting of formulas (S1) to (S18).

Neurotrophin receptor binding conjugate compositions for delivering an active agent to nerve cells are provided. Conjugate compositions of the present disclosure according to certain embodiments include a one or more active agent compounds (e.g., a dye or small molecule therapeutic) covalently bonded to a protein, peptide or peptidomimetic that binds selectively to a neurotrophin receptor. In embodiments of the compositions, the average ratio of active agent compound to protein, peptide or peptidomimetic in the conjugates is 5 or less. Dual color imaging compositions are also described. Methods for delivering an active agent conjugate selectively into nerve cells (e.g., intraocular delivery) are provided. Also included are methods of making compositions having neurotrophin receptor binding conjugates

Neurotrophin receptor binding conjugate compositions for delivering an active agent to nerve cells are provided. Conjugate compositions of the present disclosure according to certain embodiments include a one or more active agent compounds (e.g., a dye or small molecule therapeutic) covalently bonded to a protein, peptide or peptidomimetic that binds selectively to a neurotrophin receptor. In embodiments of the compositions, the average ratio of active agent compound to protein, peptide or peptidomimetic in the conjugates is 5 or less. Dual color imaging compositions are also described. Methods for delivering an active agent conjugate selectively into nerve cells (e.g., intraocular delivery) are provided. Also included are methods of making compositions having neurotrophin receptor binding conjugates