C07D263/52

HEPATITIS B ANTIVIRAL AGENTS

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:


X-A-Y-L-R(I)

which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

HEPATITIS B ANTIVIRAL AGENTS

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:


X-A-Y-L-R(I)

which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

CAMPTOTHECIN DERIVATIVE INTERMEDIATE, AND PREPARATION METHOD THEREFOR AND USE THEREOF
20250059143 · 2025-02-20 ·

Disclosed in the present invention are a camptothecin derivative intermediate, and a preparation method therefor and the use thereof. The structural formula of the camptothecin derivative intermediate of the present invention is as shown in formula (I), and the definition of each substituent is as described in the description and claims. The intermediate (I) of the present invention can be used for preparing an intermediate (III), and can be further used for preparing exatecan and a derivative thereof. The preparation method of the present invention has the advantages of cheap and easily available raw materials, a novel method and simple route, mild conditions, a high yield, few by-products, suitability for scale-up synthesis and industrial production, etc.

##STR00001##

CAMPTOTHECIN DERIVATIVE INTERMEDIATE, AND PREPARATION METHOD THEREFOR AND USE THEREOF
20250059143 · 2025-02-20 ·

Disclosed in the present invention are a camptothecin derivative intermediate, and a preparation method therefor and the use thereof. The structural formula of the camptothecin derivative intermediate of the present invention is as shown in formula (I), and the definition of each substituent is as described in the description and claims. The intermediate (I) of the present invention can be used for preparing an intermediate (III), and can be further used for preparing exatecan and a derivative thereof. The preparation method of the present invention has the advantages of cheap and easily available raw materials, a novel method and simple route, mild conditions, a high yield, few by-products, suitability for scale-up synthesis and industrial production, etc.

##STR00001##

NITROGEN-CONTAINING COMPOUND, ORGANIC ELECTROLUMINESCENT DEVICE, AND ELECTRONIC APPARATUS
20250051317 · 2025-02-13 ·

The present application relates to the technical field of organic electroluminescent materials, and provides a nitrogen-containing compound, an organic electroluminescent device comprising same, and an electronic apparatus. The nitrogen-containing compound of the present application comprises a parent nucleus structure of a benzophenoxazole/thiazole group. When the nitrogen-containing compound is used as a host material for an emission layer of the organic electroluminescent device, the luminous efficiency and service life of the device can be remarkably improved.

TETRACYCLINE DERIVATIVES WITH REDUCED ANTIBIOTIC ACTIVITY AND NEUROPROTECTIVE BENEFITS

The present disclosure is directed to compositions and methods which utilize the tetracycline scaffold, preferably the scaffold of tetracycline or minocycline, and which significantly lack antibiotic activity. The compounds have neuroprotective attributes without interfering with the drugs capacity to pass through the blood brain barrier. These compounds have neuroprotective activity because of their inhibition of neuronal cell cycle progression. The compounds are characterized in part by a fifth ring joining positions 9 and 10.

TETRACYCLINE DERIVATIVES WITH REDUCED ANTIBIOTIC ACTIVITY AND NEUROPROTECTIVE BENEFITS

The present disclosure is directed to compositions and methods which utilize the tetracycline scaffold, preferably the scaffold of tetracycline or minocycline, and which significantly lack antibiotic activity. The compounds have neuroprotective attributes without interfering with the drugs capacity to pass through the blood brain barrier. These compounds have neuroprotective activity because of their inhibition of neuronal cell cycle progression. The compounds are characterized in part by a fifth ring joining positions 9 and 10.

Tetracycline derivatives with reduced antibiotic activity and neuroprotective benefits

The present disclosure is directed to compositions and methods which utilize the tetracycline scaffold, preferably the scaffold of tetracycline or minocycline, and which significantly lack antibiotic activity. The compounds have neuroprotective attributes without interfering with the drugs capacity to pass through the blood brain barrier. These compounds have neuroprotective activity because of their inhibition of neuronal cell cycle progression. The compounds are characterized in part by a fifth ring joining positions 9 and 10.

Tetracycline derivatives with reduced antibiotic activity and neuroprotective benefits

The present disclosure is directed to compositions and methods which utilize the tetracycline scaffold, preferably the scaffold of tetracycline or minocycline, and which significantly lack antibiotic activity. The compounds have neuroprotective attributes without interfering with the drugs capacity to pass through the blood brain barrier. These compounds have neuroprotective activity because of their inhibition of neuronal cell cycle progression. The compounds are characterized in part by a fifth ring joining positions 9 and 10.

AZASPIRO DERIVATIVES AS TRPM8 ANTAGONISTS
20170002016 · 2017-01-05 · ·

The present invention relates to azaspiro derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.

##STR00001##