C07D311/12

Chemical enhancement by nanomaterials under X-ray irradiation

A method for dynamic enhancement of chemical reactions by nanomaterials under hard X-ray irradiation. The nanomaterials were gold and platinum nanoparticles, and the chemical reaction employed was the hydroxylation of coumarin carboxylic acid. The reaction yield was enhanced 2000 times over that predicted on the basis of the absorption of X-rays only by the nanoparticles, and the enhancement was found for the first time to depend on the X-ray dose rate. The maximum turnover frequency was measured at 1 1610-4 s-1 Gy-1. We call this process chemical enhancement, which is defined as the increased yield of a chemical reaction due to the chemical properties of the added materials. The chemical enhancement described here is believed to be ubiquitous and may significantly alter the outcome of chemical reactions under X-ray irradiation with the assistance of nanomaterials.

USE OF COUMARIN DERIVATIVES FOR THE PREPARATION OF DRUGS FOR TREATING SKIN DISEASES

A compound of formula (I-1)

##STR00001##

wherein n equals 0 or 1, Z represents O or S, R1 represents one group chosen among the group consisting of hydrogen, C1-C7 alkyl, substituted, or not, by a halogen, a hydroxyl or a OR12 group, wherein R12 is a C1-C7 alkyl, a group CH.sub.2OCOR5 wherein R5 is chosen among a hydrogen atom and a C1-C7 alkyl, substituted or not by at least one halogen, a group OR13, wherein R13 is chosen among hydrogen and a C1-C7 alkyl, an amine or a CH.sub.2-amine, R1 represents a group chosen among hydrogen and OR14, wherein R14 is chosen among hydrogen and a C1-C7 alkyl, and R2 is chosen among the group consisting of a C1-C7 alkyl, a C3-C6 cycloalkyl, an aryl group, and an heteroaryl group for the treatment of pathologies involving excess activity of at least one member of the kallikrein family.

Therapeutic compounds

The invention provides compounds of formula I: ##STR00001##
or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating cancer or treating autoimmune diseases or preventing transplant rejection using compounds of formula I.

Therapeutic compounds

The invention provides compounds of formula I: ##STR00001##
or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating cancer or treating autoimmune diseases or preventing transplant rejection using compounds of formula I.

Coumarin-based compounds and related methods
20170015652 · 2017-01-19 ·

The present invention generally relates to coumarin-based compounds that can be used for the labeling of biological molecules, as well as related synthetic and testing methods. The coumarin-based compounds typically survive conditions necessary for automated synthesis of nucleic acids without undergoing any substantial degree of degradation or alteration.

Use of coumarin derivatives for the preparation of drugs for treating skin diseases

A compound of formula (I-1) ##STR00001##
wherein n equals 0 or 1, Z represents O or S, R1 represents one group chosen among the group consisting of hydrogen, C1-C7 alkyl, substituted, or not, by a halogen, a hydroxyl or a OR12 group, wherein R12 is a C1-C7 alkyl, a group CH.sub.2OCOR5 wherein R5 is chosen among a hydrogen atom and a C1-C7 alkyl, substituted or not by at least one halogen, a group OR13, wherein R13 is chosen among hydrogen and a C1-C7 alkyl, an amine or a CH.sub.2-amine, R1 represents a group chosen among hydrogen and OR14, wherein R14 is chosen among hydrogen and a C1-C7 alkyl, and R2 is chosen among the group consisting of a C1-C7 alkyl, a C3-C6 cycloalkyl, an aryl group, and an heteroaryl group for the treatment of pathologies involving excess activity of at least one member of the kallikrein family.

Use of coumarin derivatives for the preparation of drugs for treating skin diseases

A compound of formula (I-1) ##STR00001##
wherein n equals 0 or 1, Z represents O or S, R1 represents one group chosen among the group consisting of hydrogen, C1-C7 alkyl, substituted, or not, by a halogen, a hydroxyl or a OR12 group, wherein R12 is a C1-C7 alkyl, a group CH.sub.2OCOR5 wherein R5 is chosen among a hydrogen atom and a C1-C7 alkyl, substituted or not by at least one halogen, a group OR13, wherein R13 is chosen among hydrogen and a C1-C7 alkyl, an amine or a CH.sub.2-amine, R1 represents a group chosen among hydrogen and OR14, wherein R14 is chosen among hydrogen and a C1-C7 alkyl, and R2 is chosen among the group consisting of a C1-C7 alkyl, a C3-C6 cycloalkyl, an aryl group, and an heteroaryl group for the treatment of pathologies involving excess activity of at least one member of the kallikrein family.

COUMARIN COMPOUNDS AND USES THEREOF

Disclosed in the present invention are a series of coumarin compounds and the uses thereof, and particularly disclosed are compounds as shown in formula (I) and pharmaceutically acceptable salts thereof.

##STR00001##

COUMARIN COMPOUNDS AND USES THEREOF

Disclosed in the present invention are a series of coumarin compounds and the uses thereof, and particularly disclosed are compounds as shown in formula (I) and pharmaceutically acceptable salts thereof.

##STR00001##

Methods and materials for inhibiting NF-kB activity

This document provides compounds that are inhibitors of NF-B activity, as well as the methods of using such compounds for treating diseases and conditions such as cancer, inflammatory conditions, or autoimmune diseases.