C07F5/025

Silicone Hydrogel Based Fluorescent Assay and Contact Lens
20230025694 · 2023-01-26 ·

A material, article, system and method include a probe composition that includes a hydrophobic portion, a hydrophilic portion, an analyte-binding portion and a fluorophore portion. The analyte-binding portion is configured to bind to an analyte in an aqueous solution. The fluorophore portion is configured to change an optical property of fluorescent light emitted in response to incident excitation light when the probe composition changes between a first state in which the analyte is not bound to the analyte-binding portion and a second state in which the analyte binds to the analyte-binding portion. A material includes the probe composition and a silicone hydrogel substrate having a hydrogel network that allows flow of aqueous solution through the solution and a silicone network that occupies interstices of the hydrogel network. A contact lens having the material enables remote detection of glucose concentration in tear fluid of a subject.

COMPOUNDS FOR SENSING REACTIVE OXYGEN SPECIES AND METHODS FOR USING THE SAME
20230227477 · 2023-07-20 ·

Provided herein according to some embodiments of the invention are aryl boronate and/or aryl diaminoboryl compounds. Also provided are methods of detecting the presence of hydrogen peroxide (H.sub.2O.sub.2) and/or other reactive oxygen species (ROS) in a cell and/or tissue by contacting the cell and/or tissue with aryl boronate and/or aryl diaminoboryl compounds. Also provided according to embodiments of the invention are methods of producing persulfides in the presence of hydrogen peroxide (H.sub.2O.sub.2) and/or other reactive oxygen species (ROS) in a cell and/or tissue by contacting the cell and/or tissue with aryl boronate and/or aryl diaminoboryl compounds.

AZAINDOLE DERIVATIVES AND THEIR USE AS ERK KINASE INHIBITORS

The present invention concerns a compound of formula (I):

##STR00001##

or one of its pharmaceutically acceptable salts, especially for use as inhibitors of the ERK kinase activity, in particular ERK2 activity.

Boron-containing compounds

Described herein are boron-containing compounds, compositions, and methods for their preparation.

MODIFIED GUANIDINE-CONTAINING POLYMERS FOR BIOLOGIC DELIVERY

The subject invention provides materials and methods for intracellular deliver of molecules and/or therapeutic agents. The subject invention also provides methods for synthesizing polymeric systems and nanomaterials that enhance or assist the passage of molecules and/or therapeutic agents across biological membranes. The compound, polymer or nanoparticle of the subject invention comprises a modified guanidine moiety in a plurality of repeating units of a polymer or on the surface of a nanoparticle where the guanidine moiety comprises, for example, a carbamoyl or thiourea modification. The polymer or nanoparticle can be used in a cancer treatment formulation.

Conjugates of active pharmaceutical ingredients

The present inventions provides drug-drug conjugates, drug-porphyrin conjugates, nanoparticles of the conjugates, as well as modified nanoparticles having PEGylated exteriors or encapsulated by red blood cell vesicles. The conjugates, nanoparticles and nanocarriers are useful for treating cancers and other diseases, as well as for imaging diseased tissue or organs.

Substituted 1,2-oxaborolan-2-ols as PDE4 inhibitors

The present invention relates to boron containing compounds of Formula (IA): ##STR00001##
that inhibit phosphodiesterase 4 (PDE4). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating diseases, conditions, or disorders ameliorated by inhibition of PDE4.

Oxo-substituted compound

Provided is a novel compound that has an excellent β-lactamase inhibitory effect. More specifically, provided is a compound represented by formula (1a), (1b) or (11) having an excellent β-lactamase inhibitory effect or a pharmaceutically acceptable salt thereof. By using this compound either in combination with a β-lactam drug or alone, a useful preventive or therapeutic agent for bacterial infections is provided. Also provided are useful preventive or therapeutic agents for treating various diseases with the combined use of the aforesaid compound and β-lactam drugs.

SUBSTITUTED THIAZOLE AROMATIC RING-BASED COMPOUND AND PREPARATION METHOD THEREFOR, HERBICIDAL COMPOSITION AND USE THEREOF
20230015308 · 2023-01-19 ·

A substituted thiazole aromatic ring compound and a preparation method therefor, a herbicidal composition and use thereof. The substituted thiazole aromatic ring compound is as shown in general formula I:

##STR00001##

Wherein, Y represents halogen, halogenated alkyl, cyano, nitro or amino; Q represents

##STR00002##

M represents CH or N; X represents

##STR00003##

X.sub.1 represents O or S; X.sub.2 represents OX.sub.3, SX.sub.3 or N(X.sub.3).sub.2. The compound has excellent herbicidal activity against gramineous weeds, broadleaf weeds, and so on even at low application rates, and has high selectivity for crops.

ENPP1 inhibitors and their use for the treatment of cancer

Compounds, compositions and methods are provided for the inhibition of ENPP1. Aspects of the subject methods include contacting a sample with a ENPP1 inhibitor to inhibit cGAMP hydrolysis activity of ENPP1. In some cases, the ENPP1 inhibitor is cell impermeable. Also provided are compositions and methods for treating cancer. Aspects of the methods include administering to a subject a therapeutically effective amount of a ENPP1 inhibitor to treat the subject for cancer. In certain cases, the cancer is a solid tumor cancer. Also provided are methods of administering radiation therapy to a subject either before or after administering an ENPP1 inhibitor. The radiation therapy can be administered at a dosage and/or frequency effective to reduce radiation damage to the subject. In certain cases, the method is performed in combination with a chemotherapeutic agent, or a checkpoint inhibitor, or both.