Patent classifications
C07D207/26
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.
METHODS AND COMPOSITIONS FOR TARGETING PD-L1
The present disclosure related to compounds that can be useful as inhibitors of PD-1, PD-L1 or the PD-1/PD-L1 interaction. Also disclosed herein are pharmaceutical compositions of that can include a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and uses of or methods of using a compound of Formula (I), or a pharmaceutically acceptable salt thereof, for the treatment of PD-L1 related diseases including but not limited to liver diseases, cancer, hepatocellular carcinoma, viral diseases, or hepatitis B.
PROTEASE INHIBITORS AS ANTIVIRALS
Provided herein, inter alia, are compounds, pharmaceutical compositions and methods related to the treatment of viral infections caused by coronavirus or enterovirus. Provided herein are compounds of Formula (I), (II) and (III)
##STR00001##
and methods of using the compounds for therapy. These compounds are peptidomimetics that inhibit protease 3CL of a coronavirus, and are useful for treating conditions caused by viral infections, including COVID-19.
PROTEASE INHIBITORS AS ANTIVIRALS
Provided herein, inter alia, are compounds, pharmaceutical compositions and methods related to the treatment of viral infections caused by coronavirus or enterovirus. Provided herein are compounds of Formula (I), (II) and (III)
##STR00001##
and methods of using the compounds for therapy. These compounds are peptidomimetics that inhibit protease 3CL of a coronavirus, and are useful for treating conditions caused by viral infections, including COVID-19.
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.
Bicyclic-fused heteroaryl or aryl compounds
- John David Trzupek ,
- Katherine Lin Lee ,
- Mark Edward Bunnage ,
- Seungil Han ,
- David Hepworth ,
- Frank Eldridge Lovering ,
- John Paul Mathias ,
- Nikolaos Papaioannou ,
- Betsy Susan Pierce ,
- Joseph Walter Strohbach ,
- Stephen Wayne Wright ,
- Christoph Wolfgang Zapf ,
- Lori Krim Gavrin ,
- Arthur Lee ,
- David Randolph Anderson ,
- Kevin Joseph Curran ,
- Christoph Martin Dehnhardt ,
- Eddine Saiah ,
- Joel Adam Goldberg ,
- Xiaolun Wang ,
- Horng-Chih Huang ,
- Richard Vargas ,
- Michael Dennis Lowe ,
- Akshay Patny
Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, ##STR00001##
as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Bicyclic-fused heteroaryl or aryl compounds
- John David Trzupek ,
- Katherine Lin Lee ,
- Mark Edward Bunnage ,
- Seungil Han ,
- David Hepworth ,
- Frank Eldridge Lovering ,
- John Paul Mathias ,
- Nikolaos Papaioannou ,
- Betsy Susan Pierce ,
- Joseph Walter Strohbach ,
- Stephen Wayne Wright ,
- Christoph Wolfgang Zapf ,
- Lori Krim Gavrin ,
- Arthur Lee ,
- David Randolph Anderson ,
- Kevin Joseph Curran ,
- Christoph Martin Dehnhardt ,
- Eddine Saiah ,
- Joel Adam Goldberg ,
- Xiaolun Wang ,
- Horng-Chih Huang ,
- Richard Vargas ,
- Michael Dennis Lowe ,
- Akshay Patny
Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, ##STR00001##
as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
SARS-COV-2 MAIN PROTEASE INHIBITORS
The present disclosure relates to certain molecules, pharmaceutical compositions containing them, and methods of using them to treat viral infections.
IL-6 inhibitors and methods of treatment
The instant invention describes compounds having IL-6 modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by IL-6.
COMPOUNDS FOR THE TREATMENT OF SARS
Inhibitors of SARS-CoV-2 (COVID), pharmaceutical compositions comprising same; and methods of treating a severe acute respiratory syndrome.