Patent classifications
C07K5/06147
METHOD FOR PHOTOCLEAVAGE OF AMIDE BONDS
The present disclosure provides a method for photocleavage of an amide bond, the method has mild reaction conditions and can realize the cleavage of amide bonds by using light. The method comprises the following steps: subjecting 2,4-dinitrofluorobenzene to a reaction with an amino group of a substance represented by structural formula I with an α-amino acid at the end to produce a compound 1 represented by structural formula II; then under light irradiation, subjecting the compound 1 to a cleavage reaction of amide bond;
##STR00001##
Wherein, R1 is the side chain group of α-amino acid; R2 is: aryl, aliphatic hydrocarbon, —CH(R)—COOH or polypeptide.
PSMA-TARGETED NIR DYES AND THEIR USES
The present disclosure relates to prostate specific membrane antigen (PSMA) targeted compounds conjugated to near-infra red (NIR) dyes and methods for their therapeutic and diagnostic use. More specifically, this disclosure provides compounds and methods for diagnosing and treating diseases associated with cells and/or vasculature expressing prostate specific membrane antigen (PSMA), such as prostate cancer and related diseases. The disclosure further describes methods and compositions for making and using the compounds, methods incorporating the compounds, and kits incorporating the compounds.
RATIONALE, DESIGN, SYNTHESIS AND VALIDATION OF A SMALL MOLECULE ANTICANCER AGENT
LIN28 is an RNA binding protein that binds and inhibits the expression and maturation of Iet7 microRNA that carries key tumor suppressor functions. Thus, LIN28 is a feasible and effective molecular target for directed inhibition with the potential to provide therapeutic benefit to a diverse group of aggressive malignancies. The present disclosure relates generally to the Rationale, Design, Synthesis and Validation of a Novel Small Molecule Inhibitor of LIN28, coined Compound of formula (I), for the Treatment of Adult and Pediatric Malignancies. In addition, indications of this agent to block cancer metastasis, inhibit cancer stem cells to prevent relapse, and to synergize with immunotherapy, chemotherapy and radiotherapy are also been described.
METAL COMPOUND HAVING PHASE TRANSFORMATION AND METHOD OF PREPARING THE SAME
The present invention relates to a metal phase transformation compound and a method for preparing the same.
Tripeptide epoxy ketone protease inhibitors
Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): ##STR00001##
and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.
Enhancers of Neurolysin Activity
The present invention includes a composition and method of allosterically potentiating the activity of neurolysin comprising contacting the neurolysin with an amount of a histidine-containing dipeptide that is an allosteric that increases the activity of neurolysin.
Amide derivatives of N-urea substituted amino acids as formyl peptide receptor like-1 (FPRL-1) receptor modulators
The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
METHOD FOR PRODUCING AMIDE
A method for producing an amide includes: dehydrating and condensing carboxylic acids and then reacting them with a base, and reacting them with an amine.
NMDA ANTAGONIST PRODRUGS
Prodrugs of an NMDA antagonist, (S)-1-phenyl-2-(pyridin-2-yl)ethanamine, useful for the treatment of depression (particularly major depressive disorder) or pain; compositions comprising them, and methods of making them.
ANTIMICROBIAL COMPOUNDS AND/OR MODULATORS OF MICROBIAL INFECTIONS AND METHODS OF USING THE SAME
Some embodiments include compounds that can inhibit the growth of bacterial and/or inhibit or reduce microbial infections caused by one or more microorganisms (e.g., Pseudomonas aeruginosa and Cryptococcus neoformans) and methods of using these compounds to treat microbial infection and outbreaks and/or to reduce the formation of biofilms. Other embodiments include synthesis of the compounds that can inhibit the growth of one or more microorganisms and/or inhibit or reduce microbial infections.