C07C257/18

Class A GPCR-binding compound modifier
12275687 · 2025-04-15 · ·

To provide a novel class-A GPCR antagonist, a production method therefor, or a novel compound that interacts with a Na.sup.+-water cluster binding site of a class-A GPCR. Used is a compound or a salt thereof comprising a structure comprising a class-A GPCR-binding compound linked to a functional group that can bind to a Na.sup.+-water cluster binding site of the class-A GPCR. Also used is a method for producing a class-A GPCR antagonist, comprising the step of linking one compound with another compound that can bind to a Na.sup.+-water cluster binding site of the class-A GPCR.

Pharmaceutical compositions with attenuated release of phenolic opioids

Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

Pharmaceutical compositions with attenuated release of phenolic opioids

Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

Benzamide compounds and related methods of use

Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.

Benzamide compounds and related methods of use

Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.

Selenium-containing nano HOF, antioxidant nanozyme, preparation method and application thereof

A multi-enzyme cascade antioxidant nano HOF and preparation method and application thereof are provided. The present invention discloses a nano HOF based on selenium-containing ligand for the first time, the nano HOF does not contain metal and has good biocompatibility, which is a universal loading platform, and has high porosity, acid and alkali resistance and thermal stability, and is size-tunable, it can coat various types of enzymes at the same time, stabilize the conformation of the enzyme through the confinement effect, the high porosity can not only provide enough space for the enzyme, but also facilitate the transport of substances and the play of catalytic properties of the enzyme, 85-90% of the activity of the coated enzyme can be maintained, ROS can be effectively scavenged through the cascade catalysis between various enzymes, which provides a new idea for the construction of bio-friendly antioxidants.

Selenium-containing nano HOF, antioxidant nanozyme, preparation method and application thereof

A multi-enzyme cascade antioxidant nano HOF and preparation method and application thereof are provided. The present invention discloses a nano HOF based on selenium-containing ligand for the first time, the nano HOF does not contain metal and has good biocompatibility, which is a universal loading platform, and has high porosity, acid and alkali resistance and thermal stability, and is size-tunable, it can coat various types of enzymes at the same time, stabilize the conformation of the enzyme through the confinement effect, the high porosity can not only provide enough space for the enzyme, but also facilitate the transport of substances and the play of catalytic properties of the enzyme, 85-90% of the activity of the coated enzyme can be maintained, ROS can be effectively scavenged through the cascade catalysis between various enzymes, which provides a new idea for the construction of bio-friendly antioxidants.

COMPOSITIONS FOR AND METHODS OF MODULATING RNA STABILITY
20250270165 · 2025-08-28 ·

Disclosed herein are compositions for and methods of modulating the expression and/or function of disease associated and/or diseasing causing secondary RNA structures and tertiary RNA structures.

COMPOSITIONS FOR AND METHODS OF MODULATING RNA STABILITY
20250270165 · 2025-08-28 ·

Disclosed herein are compositions for and methods of modulating the expression and/or function of disease associated and/or diseasing causing secondary RNA structures and tertiary RNA structures.

Analogues of pentamidine and uses therefor

The present disclosure provides a group of aromatic (e.g., pyridinyl, pyrimidinyl, pyrazinyl, or phenyl) diamidine analogs and pharmaceutically acceptable salts that are useful for treating a proliferative disease. The proliferative disease may include solid cancer or blood cancer. Compositions, methods of synthesizing the same and methods for treating various cancer using the analogs are disclosed herein. The present disclosure also provides pharmaceutical formulations comprising at least one of the compounds with a pharmaceutically acceptable carrier, diluent or excipient therefor.