Patent classifications
C07D233/70
THIOL COMPOUND, METHOD FOR SYNTHESIZING SAME, AND USES FOR SAID THIOL COMPOUND
An objective of the present invention is to provide: a novel thiol compound; a method for synthesizing the thiol compound; a curing agent containing the thiol compound; a resin composition containing the thiol compound and an epoxy compound; and a resin composition containing the thiol compound and an enic compound having an intramolecular carbon-carbon double bond. The thiol compound of the present invention, as exemplified by the compounds listed below, is a reaction product of a certain type of dialkene compound and a thiol compound, and has two or more intramolecular thioether bonds but no ester bonds.
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MILD AND SITE-SELECTIVE 18F-LABELING OF SMALL MOLECULES AND/OR BIOMOLECULES VIA A THIOL-REACTIVE SYNTHON
Site-selective conjugation to biomolecules via thiol-based chemistry is superior to the unselective modification of lysine residues, which produce a mixed product and can potentially interfere with binding affinity of the biomolecule. However, in physiological environments, the maleimide-thiol conjugation product which is the current gold-standard for site-selective thiol-conjugation can be susceptible to hydrolysis or a retro-Michael reaction via exchange with reactive thiols such as those in albumin or glutathione residues yet the degradation is relatively slow. Therefore, for in vivo studies, the maleimide-thiol conjugation proposes instability issues. The compositions and methods disclosed herein provide an alternative thiol-based linkage, one that overcomes the instability issues with conventional reagents and methods. The compositions and methods disclosed herein are useful in various contexts, for example, for .sup.18F-labeling of peptides/proteins in the preparation of positron emission tomography (PET) probes.
MILD AND SITE-SELECTIVE 18F-LABELING OF SMALL MOLECULES AND/OR BIOMOLECULES VIA A THIOL-REACTIVE SYNTHON
Site-selective conjugation to biomolecules via thiol-based chemistry is superior to the unselective modification of lysine residues, which produce a mixed product and can potentially interfere with binding affinity of the biomolecule. However, in physiological environments, the maleimide-thiol conjugation product which is the current gold-standard for site-selective thiol-conjugation can be susceptible to hydrolysis or a retro-Michael reaction via exchange with reactive thiols such as those in albumin or glutathione residues yet the degradation is relatively slow. Therefore, for in vivo studies, the maleimide-thiol conjugation proposes instability issues. The compositions and methods disclosed herein provide an alternative thiol-based linkage, one that overcomes the instability issues with conventional reagents and methods. The compositions and methods disclosed herein are useful in various contexts, for example, for .sup.18F-labeling of peptides/proteins in the preparation of positron emission tomography (PET) probes.
METHOD OF TREATING A CONDITION ASSOCIATED WITH NEURODEGENERATION USING INHIBITORS OF OAT3
The present disclosure relates to therapeutic agents that may be useful intreatment and prophylaxis of neurodegenerative disorders and/or neural inflammation.
DIARYLHYDANTOIN COMPOUNDS
The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
DIARYLHYDANTOIN COMPOUNDS
The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE
The present disclosure discloses compounds capable of modulating the activity of α-amino-β-carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD.sup.+ biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE
The present disclosure discloses compounds capable of modulating the activity of α-amino-β-carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD.sup.+ biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.
Proteasome inhibitors and uses thereof
The compounds of the present invention are represented by the following compounds having Formula (I) where the substituents R, R.sup.1-R.sup.5, k, m, n, and q are as defined herein. These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders, infectious disease, or for providing immunosuppression for transplanted organs or tissues. ##STR00001##
Proteasome inhibitors and uses thereof
The compounds of the present invention are represented by the following compounds having Formula (I) where the substituents R, R.sup.1-R.sup.5, k, m, n, and q are as defined herein. These compounds are used in the treatment of cancer, immunologic disorders, autoimmune disorders, neurodegenerative disorders, or inflammatory disorders, infectious disease, or for providing immunosuppression for transplanted organs or tissues. ##STR00001##