Patent classifications
C07D413/06
Prolyl Hydroxylase Inhibitors
The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I)
##STR00001##
which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
Bicyclic [4,6,0] hydroxamic acids as HDAC inhibitors
The present invention relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with HDAC6, having a Formulae I or Formula II: ##STR00001##
where R, L, X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, Y.sup.1, Y.sup.2, Y.sup.3, and Y.sup.4 are described herein.
Bicyclic [4,6,0] hydroxamic acids as HDAC inhibitors
The present invention relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with HDAC6, having a Formulae I or Formula II: ##STR00001##
where R, L, X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, Y.sup.1, Y.sup.2, Y.sup.3, and Y.sup.4 are described herein.
MACROCYCLES COMPRISING A 4-AMIDO-2,4-PENTADIENOATE MOIETY FOR THE TREATMENT OF HYPOXIC CANCERS
The present disclosure provides macrocyclic compounds comprising a 4-amido-2,4-pentadienoate (APD) moiety. The compounds exhibit toxicity that is selective to the hypoxic micro-environments often found in cancerous tissues. The disclosed compounds are therefore suitable for treatment of hypoxic cancer cells.
MACROCYCLES COMPRISING A 4-AMIDO-2,4-PENTADIENOATE MOIETY FOR THE TREATMENT OF HYPOXIC CANCERS
The present disclosure provides macrocyclic compounds comprising a 4-amido-2,4-pentadienoate (APD) moiety. The compounds exhibit toxicity that is selective to the hypoxic micro-environments often found in cancerous tissues. The disclosed compounds are therefore suitable for treatment of hypoxic cancer cells.
HETEROCYCLIC COMPOUNDS FOR MEDICAL TREATMENT
The present invention provides heterocyclic compounds that bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and their use for the treatment of abnormal cellular proliferation in a human or other host. The present invention also provides compounds that can be used as synthetic intermediates in the synthesis of bifunctional compounds used for targeted protein degradation.
COMPOUNDS AND THEIR METHODS OF USE
The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.
COMPOUNDS AND THEIR METHODS OF USE
The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.
ISOXAZOLIDINES AS RIPK1 INHIBITORS AND USE THEREOF
The present invention relates to isoxazolidines of formula I and their use as receptor-interacting protein kinase 1 inhibitors, for example in the treatment of diseases and disorders mediated by RIP kinase (1) such as rheumatoid arthritis (RA), psoriasis, inflammatory bowel disease (IBD), Crohn’s disease or ulcerative colitis.
##STR00001##
ISOXAZOLIDINES AS RIPK1 INHIBITORS AND USE THEREOF
The present invention relates to isoxazolidines of formula I and their use as receptor-interacting protein kinase 1 inhibitors, for example in the treatment of diseases and disorders mediated by RIP kinase (1) such as rheumatoid arthritis (RA), psoriasis, inflammatory bowel disease (IBD), Crohn’s disease or ulcerative colitis.
##STR00001##