Patent classifications
C07D295/16
Covalent inhibitors of kras G12C
Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
Covalent inhibitors of kras G12C
Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
BROMOTRIAZOLE INTERMEDIATES
Bromotriazole intermediates are useful in the synthesis of agonists of the APH receptor. Such compounds include those selected from
##STR00001##
BROMOTRIAZOLE INTERMEDIATES
Bromotriazole intermediates are useful in the synthesis of agonists of the APH receptor. Such compounds include those selected from
##STR00001##
Cyanopyridine derivatives as liver X receptor beta agonists, compositions, and their use
In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X- receptor (LXR) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease. ##STR00001##
Cyanopyridine derivatives as liver X receptor beta agonists, compositions, and their use
In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X- receptor (LXR) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease. ##STR00001##
Triazole agonists of the APJ receptor
- Ning Chen ,
- Xiaoqi Chen ,
- Yinhong Chen ,
- Alan C. Cheng ,
- Richard V. Connors ,
- Jeffrey Deignan ,
- Paul John Dransfield ,
- Xiaohui Du ,
- Zice Fu ,
- Julie Anne Heath ,
- Daniel B. Horne ,
- Jonathan Houze ,
- Matthew R. Kaller ,
- Aarif Yusuf Khakoo ,
- David John KOPECKY ,
- Su-Jen LAI ,
- Zhihua Ma ,
- Lawrence R. McGee ,
- Julio C. Medina ,
- Jeffrey T. Mihalic ,
- Nobuko Nishimura ,
- Steven H. Olson ,
- Vatee Pattaropong ,
- Gayathri Swaminath ,
- Xiaodong Wang ,
- Kevin Yang ,
- Wen-Chen Yeh ,
- Mikkel V. DEBENEDETTO ,
- Robert P. FARRELL ,
- Simon J. HEDLEY ,
- Ted C. JUDD ,
- Frank Kayser
Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: ##STR00001##
where the definitions of the variables are provided herein.
Triazole agonists of the APJ receptor
- Ning Chen ,
- Xiaoqi Chen ,
- Yinhong Chen ,
- Alan C. Cheng ,
- Richard V. Connors ,
- Jeffrey Deignan ,
- Paul John Dransfield ,
- Xiaohui Du ,
- Zice Fu ,
- Julie Anne Heath ,
- Daniel B. Horne ,
- Jonathan Houze ,
- Matthew R. Kaller ,
- Aarif Yusuf Khakoo ,
- David John KOPECKY ,
- Su-Jen LAI ,
- Zhihua Ma ,
- Lawrence R. McGee ,
- Julio C. Medina ,
- Jeffrey T. Mihalic ,
- Nobuko Nishimura ,
- Steven H. Olson ,
- Vatee Pattaropong ,
- Gayathri Swaminath ,
- Xiaodong Wang ,
- Kevin Yang ,
- Wen-Chen Yeh ,
- Mikkel V. DEBENEDETTO ,
- Robert P. FARRELL ,
- Simon J. HEDLEY ,
- Ted C. JUDD ,
- Frank Kayser
Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: ##STR00001##
where the definitions of the variables are provided herein.
Small Molecule Agonists and Antagonists of NR2F6 Activity in Animals
The present technology is directed to modulators of nuclear receptor activity, specifically to the modulation of NR2F6 activity and NR2F6 utilizing compounds, and the immune modulation and modulation of cancer stem cell activity through administration of compounds described herein to animals.
Small Molecule Agonists and Antagonists of NR2F6 Activity in Animals
The present technology is directed to modulators of nuclear receptor activity, specifically to the modulation of NR2F6 activity and NR2F6 utilizing compounds, and the immune modulation and modulation of cancer stem cell activity through administration of compounds described herein to animals.