Patent classifications
C07D453/02
INHIBITORS OF CBL-B AND METHODS OF USE THEREOF
- Paul A. BARSANTI ,
- Neil F. BENCE ,
- Jennifa GOSLING ,
- Anjanabha SAHA ,
- Asad M TAHERBHOY ,
- Christoph W. ZAPF ,
- Kathleen BOYLE ,
- Mario CARDOZO ,
- Jeffrey MIHALIC ,
- Morgan LAWRENZ ,
- Mark GALLOP ,
- Jilliane BRUFFEY ,
- Thomas CUMMINS ,
- Daniel ROBBINS ,
- Hiroko TANAKA ,
- Chenbo WANG ,
- Frederick Cohen ,
- Wylie PALMER ,
- Arthur T. SANDS ,
- Hunter SHUNATONA
Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo.
INHIBITORS OF CBL-B AND METHODS OF USE THEREOF
- Paul A. BARSANTI ,
- Neil F. BENCE ,
- Jennifa GOSLING ,
- Anjanabha SAHA ,
- Asad M TAHERBHOY ,
- Christoph W. ZAPF ,
- Kathleen BOYLE ,
- Mario CARDOZO ,
- Jeffrey MIHALIC ,
- Morgan LAWRENZ ,
- Mark GALLOP ,
- Jilliane BRUFFEY ,
- Thomas CUMMINS ,
- Daniel ROBBINS ,
- Hiroko TANAKA ,
- Chenbo WANG ,
- Frederick Cohen ,
- Wylie PALMER ,
- Arthur T. SANDS ,
- Hunter SHUNATONA
Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo.
Tricyclic compounds as histone methyltransferase inhibitors
The present disclosure provides certain tricyclic compounds that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinopathies (e.g., beta-thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Tricyclic compounds as histone methyltransferase inhibitors
The present disclosure provides certain tricyclic compounds that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinopathies (e.g., beta-thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
FERROPTOSIS INHIBITORS - DIARYLAMINE PARA-ACETAMIDES
Provided are compounds that inhibit ferroptosis activity, or modulate or inhibit a disease associated with ferroptosis dysregulation, such as neuropathy, ischemia reperfusion injury, acute kidney failure and cancer, including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
Methods and Compositions for Targeting Tregs using CCR8 Inhibitors
The present invention provides compounds of Formula (I) which can be used as CCR8 inhibitors, which can be used as treatment or prevention of cancer using CCR8 inhibitors targeted tumor specific T regulatory cells.
##STR00001##
GPR84 ANTAGONISTS AND USES THEREOF
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of GPR84, and the treatment of GPR84-mediated disorders.
Sulfonamide carboxamide compounds
The present invention relates to compounds of formula (I): ##STR00001##
wherein Q is selected from O or S; R.sup.1 is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R.sup.1 is attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein R.sup.1 may optionally be substituted; and R.sup.2 is a cyclic group substituted at the α-position, wherein R.sup.2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.
Sulfonamide carboxamide compounds
The present invention relates to compounds of formula (I): ##STR00001##
wherein Q is selected from O or S; R.sup.1 is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R.sup.1 is attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein R.sup.1 may optionally be substituted; and R.sup.2 is a cyclic group substituted at the α-position, wherein R.sup.2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.
ARYLMETHYLENE HETEROCYCLIC COMPOUNDS AS KV1.3 POTASSIUM SHAKER CHANNEL BLOCKERS
A compound of Formula (I) or a pharmaceutically acceptable salt thereof is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.
##STR00001##