Patent classifications
C07D209/02
COMPOSITIONS AND METHODS FOR INHIBITING Mpro and PLpro PROTEASE ACTIVITY AND FOR PREVENTING AND TREATING SARS-CoV-2 INFECTION
This invention is in the field of medicinal chemistry and relates to a new class of small-molecules having a pyrrolidinone-acetamide (or similar) structure (e.g.,
##STR00001##
Formula I) which function as inhibitors of the SARS-CoV-2 papain-like protease (PL.sup.pro), which function as inhibitors of the SARS-CoV-2 related viral 3CL protease (MP.sup.pro), which function as therapeutics for the treatment of viral infection characterized with PLP.sup.pro and/or M.sup.pro protease activity and/or expression (e.g., COVID-19), and which function as therapeutics for the treatment of other conditions characterized with PLP.sup.pro and/or M.sup.pro protease activity and/or expression.
COMPOSITIONS AND METHODS FOR INHIBITING Mpro and PLpro PROTEASE ACTIVITY AND FOR PREVENTING AND TREATING SARS-CoV-2 INFECTION
This invention is in the field of medicinal chemistry and relates to a new class of small-molecules having a pyrrolidinone-acetamide (or similar) structure (e.g.,
##STR00001##
Formula I) which function as inhibitors of the SARS-CoV-2 papain-like protease (PL.sup.pro), which function as inhibitors of the SARS-CoV-2 related viral 3CL protease (MP.sup.pro), which function as therapeutics for the treatment of viral infection characterized with PLP.sup.pro and/or M.sup.pro protease activity and/or expression (e.g., COVID-19), and which function as therapeutics for the treatment of other conditions characterized with PLP.sup.pro and/or M.sup.pro protease activity and/or expression.
COMPOUNDS COMPRISING A FIBROBLAST ACTIVATION PROTEIN LIGAND AND USE THEREOF
The present invention is related to a compound comprising a cyclic peptide
of formula (I)
##STR00001##
and an N-terminal modification group A attached to Xaa1,
wherein
each and any one of Xaa1, Xaa2, Xaa3, Xaa4, Xaa5, Xaa6 and Xaa7 is a residue of an amino acid, and
Yc is a structure of formula (X)
##STR00002##
COMPOUNDS COMPRISING A FIBROBLAST ACTIVATION PROTEIN LIGAND AND USE THEREOF
The present invention is related to a compound comprising a cyclic peptide
of formula (I)
##STR00001##
and an N-terminal modification group A attached to Xaa1,
wherein
each and any one of Xaa1, Xaa2, Xaa3, Xaa4, Xaa5, Xaa6 and Xaa7 is a residue of an amino acid, and
Yc is a structure of formula (X)
##STR00002##
TEAD INHIBITORS AND USES THEREOF
The present invention provides compounds, compositions thereof, and methods of using the same.
Nitration
A process for preparing a nitrated compound, including the step of reacting a compound (A) including at least one substituted or unsubstituted aromatic or heteroaromatic ring, wherein the heteroaromatic ring includes at least one heteroatom selected from the group consisting of oxygen, sulfur, phosphor, selenium and nitrogen, with a compound of formula (I) ##STR00001##
wherein Y is selected from the group consisting of hydrogen and nitro.
2,3-DIHYDRO-1H-INDOLE COMPOUNDS
The present invention relates to certain novel 2,3-dihydro-1H-indole compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, more particularly for the treatment of cancer selected from the group consisting of melanoma, acute myeloid leukemia, chronic lymphocytic leukemia, colorectal cancer, breast cancer, lung cancer, ovarian cancer, fallopian tube carcinoma, primary peritoneal carcinoma, cervical cancer, gastric cancer, liver cancer, pancreatic cancer, thyroid cancer, glioma, non-Hodgkin's lymphoma, and Hodgkin's lymphoma.
2,3-DIHYDRO-1H-INDOLE COMPOUNDS
The present invention relates to certain novel 2,3-dihydro-1H-indole compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, more particularly for the treatment of cancer selected from the group consisting of melanoma, acute myeloid leukemia, chronic lymphocytic leukemia, colorectal cancer, breast cancer, lung cancer, ovarian cancer, fallopian tube carcinoma, primary peritoneal carcinoma, cervical cancer, gastric cancer, liver cancer, pancreatic cancer, thyroid cancer, glioma, non-Hodgkin's lymphoma, and Hodgkin's lymphoma.
Bisamide sarcomere activating compounds and uses thereof
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof. ##STR00001##
Bisamide sarcomere activating compounds and uses thereof
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof. ##STR00001##