C07D403/06

Monoacylglycerol lipase modulators

3.1.0 and 4.1.0 Azabicycle compounds of Formula (I), pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, bipolar disorder), cancers and eye conditions. ##STR00001##
wherein X, Y, R.sup.1, R.sup.2a, and R.sup.2b are defined herein.

Monoacylglycerol lipase modulators

3.1.0 and 4.1.0 Azabicycle compounds of Formula (I), pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, bipolar disorder), cancers and eye conditions. ##STR00001##
wherein X, Y, R.sup.1, R.sup.2a, and R.sup.2b are defined herein.

Protease inhibitors for treatment of coronavirus infections

Provided herein are compounds of Formula (I), their pharmaceutically acceptable salts, and their pharmaceutical compositions: ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4, R.sup.5, and A are defined in the present disclosure. The compounds are potent inhibitors of the main protease (M.sup.pro) of severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2), and they are useful in treating or preventing COVID-19 in a subject.

YAP1 INHIBITORS THAT TARGET THE INTERACTION OF YAP1 WITH OCT4

Binding of the transcriptional co-activator, YAP1, to the transcription factor Oct4, induces Sox2, which is a transcription actor necessary for the self-renewal of stem-like cells from non-small cell lung cancer. The WW domain of YAP1 binds to the PPxY motif of Oct4 to induce Sox2. Delivering a peptide corresponding to the WW domain could prevent the induction of Sox2 and sternness. Similarly, peptides and mimetics of the PPxY motif would be able to inhibit sternness. Disclosed are compounds that affect the Yap1:Oct4 interaction.

YAP1 INHIBITORS THAT TARGET THE INTERACTION OF YAP1 WITH OCT4

Binding of the transcriptional co-activator, YAP1, to the transcription factor Oct4, induces Sox2, which is a transcription actor necessary for the self-renewal of stem-like cells from non-small cell lung cancer. The WW domain of YAP1 binds to the PPxY motif of Oct4 to induce Sox2. Delivering a peptide corresponding to the WW domain could prevent the induction of Sox2 and sternness. Similarly, peptides and mimetics of the PPxY motif would be able to inhibit sternness. Disclosed are compounds that affect the Yap1:Oct4 interaction.

CRBN LIGANDS AND USES THEREOF
20230234950 · 2023-07-27 ·

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.

CRBN LIGANDS AND USES THEREOF
20230234950 · 2023-07-27 ·

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.

Imidazotriazines and Imidazopyrimidines as Kinase Inhibitors

The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.

Imidazotriazines and Imidazopyrimidines as Kinase Inhibitors

The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.

Azirine Containing Compounds as Anti-Angiogenesis Agents and a Process for the Preparation Thereof

The present invention relates to azirine containing compounds useful as anti-angiogenesis agents and preparation thereof. Particularly the present invention relates to azirine containing compounds of formula I, Formula I wherein R.sub.1, R.sub.2 and R.sub.3 are same as defined in the description. The compounds of the present invention are with asymmetric centers this, they are mixture of enantiomers and mixture of diastereomers in some cases. The present invention includes the individual enantiomers and diastereomeric forms of the compound formula I besides the mixtures thereof.

##STR00001##