Patent classifications
C07C229/34
METHODS FOR PRACTICAL SYNTHESIS OF DEUTERATED AMINO ACIDS
Disclosed are a deuterated compound of fomula (I), or a salt thereof, and methods for preparation thereof. The present disclosure may provide a mild, versatile organophotoredox method for the preparation of diverse, enantioenriched α-deuterated α-amino acids. In particular, the present disclosure may address the long-standing challenge of installing sterically demanding side chains into α-amino acids, including late-stage modifications on medicinal agents and natural products.
METHODS FOR PRACTICAL SYNTHESIS OF DEUTERATED AMINO ACIDS
Disclosed are a deuterated compound of fomula (I), or a salt thereof, and methods for preparation thereof. The present disclosure may provide a mild, versatile organophotoredox method for the preparation of diverse, enantioenriched α-deuterated α-amino acids. In particular, the present disclosure may address the long-standing challenge of installing sterically demanding side chains into α-amino acids, including late-stage modifications on medicinal agents and natural products.
Pyrrolidinones and a process to prepare them
This application is directed to a compound of Formula II Also disclosed is a process for preparing a compound of Formula II comprising using the compounds of Formulae IV and V Also disclosed is a method for preparing a compound of Formula I comprising contacting a compound of Formula II with a compound of a compound of Formula VI wherein A.sup.1, A.sup.2 A.sup.3, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4, B.sup.1, B.sup.2 and B.sup.3, are as defined in the disclosure. ##STR00001##
DITERPENOID COMPOUNDS THAT ACT ON PROTEIN KINASE C (PKC)
This present disclosure relates to protein kinase C (PKC) modulating compounds, methods of treating a subject with cancer using the compounds, and combination treatments with a second therapeutic agent.
DITERPENOID COMPOUNDS THAT ACT ON PROTEIN KINASE C (PKC)
This present disclosure relates to protein kinase C (PKC) modulating compounds, methods of treating a subject with cancer using the compounds, and combination treatments with a second therapeutic agent.
Artificial single guide RNA and use thereof
The invention provides an artificial sgRNA and a CRISPR/Cas9 system by combining the artificial sgRNA and Cas9. Activity of the sgRNA can be retained even when a nucleotide linker region for forming a single strand by linking the 3′-terminal of crRNA and the 5′-terminal of tracrRNA in sgRNA is substituted with an amino acid derivative linker, when the linker region existing between stem-loop 1 and stem-loop 2 of tracrRNA and/or the loop portion of stem-loop 2 are/is substituted with an amino acid derivative linker, or when an amino acid derivative linker is added/inserted into the vicinity of the 5′-terminal and/or the 3′-terminal of sgRNA. Stability in vivo can be improved by introducing one or more amino acid derivative linkers into the sgRNA.
Artificial single guide RNA and use thereof
The invention provides an artificial sgRNA and a CRISPR/Cas9 system by combining the artificial sgRNA and Cas9. Activity of the sgRNA can be retained even when a nucleotide linker region for forming a single strand by linking the 3′-terminal of crRNA and the 5′-terminal of tracrRNA in sgRNA is substituted with an amino acid derivative linker, when the linker region existing between stem-loop 1 and stem-loop 2 of tracrRNA and/or the loop portion of stem-loop 2 are/is substituted with an amino acid derivative linker, or when an amino acid derivative linker is added/inserted into the vicinity of the 5′-terminal and/or the 3′-terminal of sgRNA. Stability in vivo can be improved by introducing one or more amino acid derivative linkers into the sgRNA.
Enamine compounds for absorbance of electromagnetic energy
The present invention describes compounds and uses thereof in applications relating to absorption of electromagnetic energy. Preferred compounds are double bond-containing compounds capable of absorbing electromagnetic radiation energy and having improved properties.
Enamine compounds for absorbance of electromagnetic energy
The present invention describes compounds and uses thereof in applications relating to absorption of electromagnetic energy. Preferred compounds are double bond-containing compounds capable of absorbing electromagnetic radiation energy and having improved properties.
TRNA SYNTHETASE INHIBITORS
Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.