Patent classifications
C07D235/24
BENZOIMIDAZOLES AS PROLYL HYDROXYLASE INHIBITORS
The present invention is directed to benzoimidazole compounds of the formula:
##STR00001##
and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
BENZOIMIDAZOLES AS PROLYL HYDROXYLASE INHIBITORS
The present invention is directed to benzoimidazole compounds of the formula:
##STR00001##
and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
Benzimidazole derivatives as PI3 kinase inhibitors
This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3 OH kinase family (hereinafter PI3 kinases), suitably, PI3K, PI3K, PI3K, and/or PI3K. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K selective benzimidazoles compounds for treating cancer.
SMALL MOLECULE ANTAGONIST TO PACAP RECEPTOR AND USES THEREOF
The disclosure relates to compounds that demonstrate efficacy in blocking PACAP receptors (e.g. PAC1) and associated methods of treating neurological diseases or disorders using the disclosed compounds. The neurological diseases or disorders include, but are not limited to, stress-related diseases (e.g. chronic stress, post-traumatic stress disorder (PTSD), panic disorder, anxiety, or general anxiety disorder), pain-related diseases (e.g. chronic pain, primary headache disorders, or migraines), or addiction (e.g. addiction to a substance (e.g. addiction to cocaine, amphetamines, methamphetamine, methylphenidate, nicotine, alcohol, prescription medication, marijuana, tobacco, or an opioid selected from heroin, fentanyl, codeine, hydrocodone, morphine, oxycodone, hydromorphone, and methadone)).
SMALL MOLECULE ANTAGONIST TO PACAP RECEPTOR AND USES THEREOF
The disclosure relates to compounds that demonstrate efficacy in blocking PACAP receptors (e.g. PAC1) and associated methods of treating neurological diseases or disorders using the disclosed compounds. The neurological diseases or disorders include, but are not limited to, stress-related diseases (e.g. chronic stress, post-traumatic stress disorder (PTSD), panic disorder, anxiety, or general anxiety disorder), pain-related diseases (e.g. chronic pain, primary headache disorders, or migraines), or addiction (e.g. addiction to a substance (e.g. addiction to cocaine, amphetamines, methamphetamine, methylphenidate, nicotine, alcohol, prescription medication, marijuana, tobacco, or an opioid selected from heroin, fentanyl, codeine, hydrocodone, morphine, oxycodone, hydromorphone, and methadone)).
Modulators of cystic fibrosis transmembrane conductance regulator
- Mark Thomas Miller ,
- Corey Anderson ,
- Vijayalaksmi Arumugam ,
- Brian Richard Bear ,
- Hayley Marie Binch ,
- Jeremy J. Clemens ,
- Thomas Cleveland ,
- Erica Conroy ,
- Timothy Richard Coon ,
- Bryan A. Frieman ,
- Peter Diederik Jan Grootenhuis ,
- Raymond Stanley Gross ,
- Sara Sabina Hadida-Ruah ,
- Haripada Khatuya ,
- Pramod Virupax Joshi ,
- Paul John Krenitsky ,
- Chun-Chieh Lin ,
- Gulin Erdogan Marelius ,
- Vito Melillo ,
- Jason McCartney ,
- Georgia McGaughey Nicholls ,
- Fabrice Jean Denis Pierre ,
- Alina Silina ,
- Andreas P. Termin ,
- Johnny Uy ,
- Jinglan Zhou
The present invention features a compound of formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, where R.sub.1, R.sub.2, R.sub.3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.
Modulators of cystic fibrosis transmembrane conductance regulator
- Mark Thomas Miller ,
- Corey Anderson ,
- Vijayalaksmi Arumugam ,
- Brian Richard Bear ,
- Hayley Marie Binch ,
- Jeremy J. Clemens ,
- Thomas Cleveland ,
- Erica Conroy ,
- Timothy Richard Coon ,
- Bryan A. Frieman ,
- Peter Diederik Jan Grootenhuis ,
- Raymond Stanley Gross ,
- Sara Sabina Hadida-Ruah ,
- Haripada Khatuya ,
- Pramod Virupax Joshi ,
- Paul John Krenitsky ,
- Chun-Chieh Lin ,
- Gulin Erdogan Marelius ,
- Vito Melillo ,
- Jason McCartney ,
- Georgia McGaughey Nicholls ,
- Fabrice Jean Denis Pierre ,
- Alina Silina ,
- Andreas P. Termin ,
- Johnny Uy ,
- Jinglan Zhou
The present invention features a compound of formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, where R.sub.1, R.sub.2, R.sub.3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.
COMPOUNDS FOR AFFINITY CHROMATOGRAPHY AND FOR EXTENDING THE HALF-LIFE OF A THERAPEUTIC AGENT
Compounds useful for affinity chromatography as presented, more particularly for use in affinity chromatography to purify serum albumin, especially human serum albumin (HSA) and fusion proteins thereof. Methods for extending the half-life of therapeutic agents are also presented, particularly therapeutic peptide agents and small molecules, such as by conjugation of compounds described herein to the therapeutic peptide or small molecule, which, upon administration, binds to HSA, thereby providing a prolonged release of the therapeutic agent.
COMPOUNDS FOR AFFINITY CHROMATOGRAPHY AND FOR EXTENDING THE HALF-LIFE OF A THERAPEUTIC AGENT
Compounds useful for affinity chromatography as presented, more particularly for use in affinity chromatography to purify serum albumin, especially human serum albumin (HSA) and fusion proteins thereof. Methods for extending the half-life of therapeutic agents are also presented, particularly therapeutic peptide agents and small molecules, such as by conjugation of compounds described herein to the therapeutic peptide or small molecule, which, upon administration, binds to HSA, thereby providing a prolonged release of the therapeutic agent.
Modulators of cystic fibrosis transmembrane conductance regulator
- Mark Thomas Miller ,
- Corey Anderson ,
- Vijayalaksmi Arumugam ,
- Brian Richard Bear ,
- Hayley Marie Binch ,
- Jeremy J. Clemens ,
- Thomas Cleveland ,
- Erica Conroy ,
- Timothy Richard Coon ,
- Bryan A. Frieman ,
- Peter Diederik Jan Grootenhuis ,
- Raymond Stanley Gross ,
- Sara Sabina Hadida Ruah ,
- Haripada Khatuya ,
- Pramod Virupax Joshi ,
- Paul John Krenitsky ,
- Chun-Chieh Lin ,
- Gulin Erdogan Marelius ,
- Vito Melillo ,
- Jason McCartney ,
- Georgia McGaughey Nicholls ,
- Fabrice Jean Denis Pierre ,
- Alina Silina ,
- Andreas P. Termin ,
- Johnny Uy ,
- Jinglan Zhou
The present invention features a compound of formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, where R.sub.1, R.sub.2, R.sub.3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.