C07D519/00

1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS

Compounds according to formula I are useful as agonists of Toll-like receptor 7 (TLR7). (I) Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.

##STR00001##

1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS

Compounds according to formula I are useful as agonists of Toll-like receptor 7 (TLR7). (I) Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.

##STR00001##

METHODS AND MATERIALS FOR INHIBITING NF-kB ACTIVITY
20230041576 · 2023-02-09 ·

This document provides compounds that are inhibitors of NF-κB activity, as well as the methods of using such compounds for treating diseases and conditions such as cancer, inflammatory conditions, or autoimmune diseases.

POTENT AND SELECTIVE AZAINDOLE INHIBITORS OF CDK8 AND CDK19
20230040191 · 2023-02-09 ·

Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with CDK8 and/or CDK19.

POTENT AND SELECTIVE AZAINDOLE INHIBITORS OF CDK8 AND CDK19
20230040191 · 2023-02-09 ·

Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with CDK8 and/or CDK19.

Cystine Diamide Analogs For Cystinuria

This document discloses novel cystine analogs, methods of making cystine analogs, compositions containing cystine analogs and methods of using such analogs for inhibiting cystine stone formation and treatment of cystinuria.

CD73 COMPOUNDS

The present disclosure provides pyrimidine dione compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors. The compounds can be used alone or in combination with other anti-cancer agents.

CD73 COMPOUNDS

The present disclosure provides pyrimidine dione compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors. The compounds can be used alone or in combination with other anti-cancer agents.

SSTR5 ANTAGONISTS
20230041621 · 2023-02-09 ·

This disclosure is directed, at least in part, to SSTR5 antagonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the SSTR5 antagonists are gut-restricted compounds. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome.

COMPOSITIONS AND METHODS RELATED TO MOLECULAR CONJUGATION

The invention relates to activated Michael acceptor (AMA) compounds that can undergo conjugation with biomolecules containing Michael donor moieties, thereby providing plasma-stable antibody-drug conjugates (ADCs). Pharmaceutical compositions of the ADCs are disclosed as well. Also provided herein are a number of applications (e.g., therapeutic applications) in which the compositions are useful.