Patent classifications
C07D417/12
N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamides useful as CCR6 inhibitors
The present invention relates to N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamide compounds of Formulae (IA and 1B) ##STR00001##
or a pharmaceutically acceptable salt or hydrate thereof, that inhibit CC chemokine receptor 6 (CCR6), pharmaceutical compositions containing these compounds, and the use of these compounds for treating or preventing diseases, conditions, or disorders ameliorated by inhibition of CCR6.
Human plasma kallikrein inhibitors
Disclosed are compounds of formula I: ##STR00001## as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one such compound, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
Human plasma kallikrein inhibitors
Disclosed are compounds of formula I: ##STR00001## as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one such compound, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
Protease inhibitors for treatment of coronavirus infections
- Arnab K. Chatterjee ,
- Jian Jeffrey Chen ,
- Elshan Nakath ,
- Alireza Rahimi ,
- Anil Kumar Gupta ,
- Gennadii Grabovyi ,
- Katy Wilson ,
- Sourav Ghorai ,
- Armen Nazarian ,
- James Pedroarena ,
- Wrickban Mazumdar ,
- Frank Weiss ,
- Lirui Song ,
- Malina A. Bakowski ,
- Laura Riva ,
- Karen Wolff ,
- Case W. McNamara ,
- Thomas F. Rogers ,
- Jacqueline Malvin ,
- Shuangwei Li ,
- Sean Joseph ,
- Ashley Woods ,
- Yuyin Liu ,
- Neechi Okwor
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.
IMMUNOMODULATOR COMPOUNDS
Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (II):
##STR00001##
including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Fungicidal oxadiazoles
Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, wherein R.sup.1, L and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. ##STR00001##
Inhibitors of NLRP3 inflammasome
The present disclosure relates to compounds that act as inhibitors of NLRP3 inflammasomes; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with inflammation and inflammaging, including hearing loss and other diseases associated with aging; wherein the inhibitors of NLRP3 inflammasomes are compounds of Formula VII: ##STR00001##
or a pharmaceutically acceptable salt thereof.
Inhibitors of NLRP3 inflammasome
The present disclosure relates to compounds that act as inhibitors of NLRP3 inflammasomes; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with inflammation and inflammaging, including hearing loss and other diseases associated with aging; wherein the inhibitors of NLRP3 inflammasomes are compounds of Formula VII: ##STR00001##
or a pharmaceutically acceptable salt 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.
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.