C07D235/02

COMPOUND, COMPOSITION, AND USE THEREOF IN PREPARATION OF DRUG
20210115014 · 2021-04-22 ·

The disclosure relates to a compound, having a structure of Formula I or a pharmaceutically acceptable salt thereof, herein, R1 is selected from hydrogen, fluorine, and chlorine; R2 and R3 are independently selected from hydrogen, alkyl, a substituted alkyl, alkenyl or a substituted alkenyl, alkynyl or a substituted alkynyl, and aryl, or R2 and R3 are connected to form a ring selected from a cycloalkyl, a substituted cycloalkyl, an aromatic heterocycle or a non-aromatic heterocycle; R4 is selected from hydrogen, cyano, alkyl, a substituted alkyl, alkenyl or a substituted alkenyl, alkynyl or a substituted alkynyl, and aryl; and R5 is selected from hydrogen, halogen, and haloalkyl. The disclosure further relates to a pharmaceutical composition containing the compound. The compound and the composition of the disclosure show significant activity in an aspect of treating AR-prostate cancer and triple-negative breast cancer.

COMPOUND, COMPOSITION, AND USE THEREOF IN PREPARATION OF DRUG
20210115014 · 2021-04-22 ·

The disclosure relates to a compound, having a structure of Formula I or a pharmaceutically acceptable salt thereof, herein, R1 is selected from hydrogen, fluorine, and chlorine; R2 and R3 are independently selected from hydrogen, alkyl, a substituted alkyl, alkenyl or a substituted alkenyl, alkynyl or a substituted alkynyl, and aryl, or R2 and R3 are connected to form a ring selected from a cycloalkyl, a substituted cycloalkyl, an aromatic heterocycle or a non-aromatic heterocycle; R4 is selected from hydrogen, cyano, alkyl, a substituted alkyl, alkenyl or a substituted alkenyl, alkynyl or a substituted alkynyl, and aryl; and R5 is selected from hydrogen, halogen, and haloalkyl. The disclosure further relates to a pharmaceutical composition containing the compound. The compound and the composition of the disclosure show significant activity in an aspect of treating AR-prostate cancer and triple-negative breast cancer.

PHOTOELECTRIC CONVERSION ELEMENT, IMAGING ELEMENT, OPTICAL SENSOR, AND COMPOUND

The present invention is to provide a photoelectric conversion element having excellent heat resistance. In addition, an imaging element and an optical sensor which include the photoelectric conversion element are provided. Furthermore, a compound applied to the photoelectric conversion element is provided. A photoelectric conversion element according to the present invention includes a conductive film, a photoelectric conversion film, and a transparent conductive film, in this order, in which the photoelectric conversion film contains a compound represented by Formula (1).

##STR00001##

In Formula (1), Y.sup.1 represents a group represented by Formula (1-1) or a group represented by Formula (1-2).

2-SUBSTITUTED AMINO-NAPHTH (1,2-D) IMIDAZOL-5-ONE COMPOUNDS OF PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
20210061768 · 2021-03-04 ·

Provided herein are therapeutic and/or prophylactic compounds for mitochondrial or oxidative stress diseases such as cancer, amyotrophic lateral sclerosis, Creutzfeldt-Jakob disease, Machado-Joseph disease, spinocerebellar ataxia, Huntington disease, Parkinson disease, Alzheimer disease, myocardial infarction, cerebral infarction, diseases related to aging, diabetes, alcoholic liver injury, chronic obstructive pulmonary disease, mitochondrial myopathy, encephalopathy, lactic acidosis, and stroke-like episodes (MELAS), and the like, wherein the compound is represented by formula (1), or reduced forms thereof, or pharmaceutically acceptable salts thereof.

##STR00001##

2-SUBSTITUTED AMINO-NAPHTH (1,2-D) IMIDAZOL-5-ONE COMPOUNDS OF PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
20210061768 · 2021-03-04 ·

Provided herein are therapeutic and/or prophylactic compounds for mitochondrial or oxidative stress diseases such as cancer, amyotrophic lateral sclerosis, Creutzfeldt-Jakob disease, Machado-Joseph disease, spinocerebellar ataxia, Huntington disease, Parkinson disease, Alzheimer disease, myocardial infarction, cerebral infarction, diseases related to aging, diabetes, alcoholic liver injury, chronic obstructive pulmonary disease, mitochondrial myopathy, encephalopathy, lactic acidosis, and stroke-like episodes (MELAS), and the like, wherein the compound is represented by formula (1), or reduced forms thereof, or pharmaceutically acceptable salts thereof.

##STR00001##

AROMATIC VINYL OR AROMATIC ETHYL DERIVATIVE, PREPARATION METHOD THEREFOR, INTERMEDIATE, PHARMACEUTICAL COMPOSITION, AND APPLICATION
20210061755 · 2021-03-04 ·

Disclosed in the present invention are an aromatic vinyl or aromatic ethyl derivative, a preparation method therefor, an intermediate, a pharmaceutical composition, and an application. The aromatic vinyl or aromatic ethyl derivative in the present invention is as represented by general formula (I). The aromatic vinyl or aromatic ethyl derivative in the present invention has an obvious inhibitory effect on PD-1/PD-L1, is a very effective small-molecule PD-1/PD-L1 inhibitor, and can effectively alleviate or treat relevant diseases such as cancer.

##STR00001##

AROMATIC VINYL OR AROMATIC ETHYL DERIVATIVE, PREPARATION METHOD THEREFOR, INTERMEDIATE, PHARMACEUTICAL COMPOSITION, AND APPLICATION
20210061755 · 2021-03-04 ·

Disclosed in the present invention are an aromatic vinyl or aromatic ethyl derivative, a preparation method therefor, an intermediate, a pharmaceutical composition, and an application. The aromatic vinyl or aromatic ethyl derivative in the present invention is as represented by general formula (I). The aromatic vinyl or aromatic ethyl derivative in the present invention has an obvious inhibitory effect on PD-1/PD-L1, is a very effective small-molecule PD-1/PD-L1 inhibitor, and can effectively alleviate or treat relevant diseases such as cancer.

##STR00001##

Method for preparing imidazolin-2 ketone compound

A method of preparing an imidazolin-2-tones compound includes: dissolving a cycloheptatrienone and an aromatic isocyanate in a solvent; and reacting the cycloheptatrienone and the aromatic isocyanate in the solvent without an oxidant and a catalyst to obtain the imidazolin-2-tone compound.

Method for preparing imidazolin-2 ketone compound

A method of preparing an imidazolin-2-tones compound includes: dissolving a cycloheptatrienone and an aromatic isocyanate in a solvent; and reacting the cycloheptatrienone and the aromatic isocyanate in the solvent without an oxidant and a catalyst to obtain the imidazolin-2-tone compound.

Antiviral compounds

The invention provides a compound of formula I, formula II, or formula III: ##STR00001##
or a salt thereof, wherein R.sup.1-R.sup.10 have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as HIV-1 CA-targeting molecules and as antiviral agents.