Patent classifications
A61K31/5355
INHIBITORS OF PEPTIDYLARGININE DEIMINASES
- Daniel H. Byun ,
- Zhenhong R. Cai ,
- Eda Y. Canales ,
- Laurent P. Debien ,
- Timothy R. Hansen ,
- Richard Huang ,
- Petr Jansa ,
- Rick A. Lee ,
- Jennifer A. Loyer-Drew ,
- Ryan McFadden ,
- Michael L. Mitchell ,
- Hyung-Jung Pyun ,
- Roland D. Saito ,
- Michael S. Sangi ,
- Adam J. Schrier ,
- Marina E. Shatskikh ,
- James G. Taylor ,
- Joshua J. Van Veldhuizen ,
- Lianhong Xu
The present disclosure relates to novel compounds for use in therapeutic treatment of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.
ANTI-VIRAL COMPOUNDS
Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
ANTI-VIRAL COMPOUNDS
Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
Inhibitors of heat shock factors and uses thereof
The present disclosure relates to a class of mammalian heat shock factor (HSF) inhibitors, to pharmaceutical compositions comprising these inhibitors as well as to methods for using the inhibitors. The inhibitors inhibit stress-induced expression from heat shock gene promoters. Furthermore, the inhibitors are cytotoxic to a variety of human cancer cells types.
Compounds and compositions for the treatment of parasitic diseases
The present invention provides a compound of formula (Ia) or a pharmaceutically acceptable salt thereof; ##STR00001## a method for manufacturing the compounds of the invention, solid forms, combinations of pharmacologically active agents, pharmaceutical compositions and methods of using such compounds and solid forms thereof to treat or prevent parasitic diseases, for example malaria.
Compounds and compositions for the treatment of parasitic diseases
The present invention provides a compound of formula (Ia) or a pharmaceutically acceptable salt thereof; ##STR00001## a method for manufacturing the compounds of the invention, solid forms, combinations of pharmacologically active agents, pharmaceutical compositions and methods of using such compounds and solid forms thereof to treat or prevent parasitic diseases, for example malaria.
MODULATORS OF BCL6 PROTEOLYSIS AND ASSOCIATED METHODS OF USE
Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand that 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 bifunctional compounds of the present disclosure exhibit 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.
MODULATORS OF BCL6 PROTEOLYSIS AND ASSOCIATED METHODS OF USE
Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand that 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 bifunctional compounds of the present disclosure exhibit 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.
3-(4-((4-(morpholinomethyl-benzyl)oxy)-1 -oxoisoindolin-2-yl)piperidine-2,6-dione for the treatment of systemic lupus erythematosus
Provided herein are methods of using compounds and compositions for treating, managing, and/or preventing systemic lupus erythematosus (SLE). Pharmaceutical compositions and dosing regimens for use in the methods are also provided herein.
3-(4-((4-(morpholinomethyl-benzyl)oxy)-1 -oxoisoindolin-2-yl)piperidine-2,6-dione for the treatment of systemic lupus erythematosus
Provided herein are methods of using compounds and compositions for treating, managing, and/or preventing systemic lupus erythematosus (SLE). Pharmaceutical compositions and dosing regimens for use in the methods are also provided herein.