Patent classifications
C07D207/46
Nitrone herbicides
Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, J.sup.2, Q.sup.1, Q.sup.2, T and Y are as defined in the disclosure. Also disclosed are compositions containing the compounds, N-oxides and salts, and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound, N-oxide, salt or composition. ##STR00001##
Nitrone herbicides
Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, J.sup.2, Q.sup.1, Q.sup.2, T and Y are as defined in the disclosure. Also disclosed are compositions containing the compounds, N-oxides and salts, and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound, N-oxide, salt or composition. ##STR00001##
QUATERNARY HETEROATOM CONTAINING COMPOUNDS
The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II):
##STR00001##
comprising treating a compound of Formula (I):
##STR00002##
with a transition metal catalyst and under alkylation conditions as valence and stability permit.
QUATERNARY HETEROATOM CONTAINING COMPOUNDS
The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II):
##STR00001##
comprising treating a compound of Formula (I):
##STR00002##
with a transition metal catalyst and under alkylation conditions as valence and stability permit.
Branched type hetero monodispersed polyethylene glycol, production method thereof, and conjugate thereof
A branched type hetero monodispersed polyethylene glycol represented by formula (1) ##STR00001##
where X.sup.1, Y.sup.1, n, E, L.sup.1, L.sup.2 and L.sup.3 are as defined herein.
Prodrug Comprising a Drug-Linker Conjugate
The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein -D is an amine containing biologically active moiety; and -L is a non-biologically active linker moiety -L.sup.1 represented by formula (I):
##STR00001##
wherein the dashed line indicates the attachment to the amine of the biologically active moiety and wherein R.sup.1, R.sup.1a, R.sup.2, R.sup.2a, R.sup.3, R.sup.3a, X, X.sup.1, X.sup.2, X.sup.3 have the meaning as indicated in the description and the claims and wherein L.sup.1 is substituted with one to four groups L.sup.2-Z and optionally further substituted, provided that the hydrogen marked with the asterisk in formula (I) is not replaced by a substituent; wherein L.sup.2 is a single chemical bond or a spacer; and Z is a carrier group. The invention also relates to A-L, wherein A is a leaving group, pharmaceutical composition comprising said prodrugs and their use as medicaments.
REAGENTS FOR QUANTITATIVE MASS SPECTROMETRY
In some embodiments, a mass spectrometry tag may comprise a linker region, a mass balance region, and a reporter region. The mass spectrometry tag may be configured to fragment in a mass spectrometer via an energy dependent process to produce multiple reporter molecules. For example, the reporter region of the tag may be configured to produce at least two reporter molecules via fragmentation. In some embodiments, one or more regions of the tag may comprise at least one heavy isotope. In some such embodiments, the ability to fragment into multiple reporter molecules as well as the placement and/or number of heavy isotope(s) allows the mass spectrometry tag to be distinguished from other similar mass spectrometry tags. In some such embodiments, the ability to distinguish between tags having the same or substantially similar total mass to charge ratio and reporter region mass may allow the system to have a greater multiplexing capacity than conventional systems.
REAGENTS FOR QUANTITATIVE MASS SPECTROMETRY
In some embodiments, a mass spectrometry tag may comprise a linker region, a mass balance region, and a reporter region. The mass spectrometry tag may be configured to fragment in a mass spectrometer via an energy dependent process to produce multiple reporter molecules. For example, the reporter region of the tag may be configured to produce at least two reporter molecules via fragmentation. In some embodiments, one or more regions of the tag may comprise at least one heavy isotope. In some such embodiments, the ability to fragment into multiple reporter molecules as well as the placement and/or number of heavy isotope(s) allows the mass spectrometry tag to be distinguished from other similar mass spectrometry tags. In some such embodiments, the ability to distinguish between tags having the same or substantially similar total mass to charge ratio and reporter region mass may allow the system to have a greater multiplexing capacity than conventional systems.
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.