C07D209/42

SULPHONAMIDES AS METHIONINE METABOLIC PATHWAY INHIBITORS
20230232828 · 2023-07-27 ·

The present invention provides novel sulphonamide inhibitors of cystathionin gamma synthase (CGS), their use as selective and non-selective herbicides, agricultural and non-agricultural herbicides, herbicides in integrated pest management, herbicides for gardening, clearing waste ground, clearing industrial or constructions sites, clearing railways and railway embankments, pesticide, fungicide, agricultural plant stimulant or antimicrobial agent. Also provided is a method for the control of undesired vegetation or clearing areas from the undesired vegetation comprising applying to the locus of said undesired vegetation, to the undesired plants or to a habitat thereof, a herbicidally effective amount of the compound of the present invention.

INDOLE CARBOXAMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME

Indole carboxamide compounds of Formula (II) or pharmaceutically acceptable salt thereof have activity of inhibiting production of prostaglandin E.sub.2 (PGE.sub.2) through inhibition of microsomal prostaglandin E.sub.2 synthase-1 (mPGES-1). The indole carboxamide compounds and salts can be effectively used in treating or preventing inflammation, arthritis, high fever, pain, cancer, stroke or brain diseases such as Alzheimer's disease. A pharmaceutical composition contains the indole carboxamide compound as an active ingredient.

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BENZOTHIOPHENE DERIVATIVE REGULATOR, PREPARATION METHOD THEREFOR AND USE THEREOF
20230002364 · 2023-01-05 ·

A nitrogen-containing ring derivative regulator, a preparation method therefor and use thereof. In particular, the present invention relates to a compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and use thereof as a G protein-coupled receptor regulator in the treatment or prevention of central nervous system diseases and/or mental diseases.

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Treatment of infectious disease

The present disclosure relates to 2-(3-indoyl)indolin-3-one derivatives of the natural product isatisine A, synthesized from dual catalytic synthesis on metallocarbene-azide cascade chemistry, useful for treating a subject having or suspected of having an infectious disease, wherein the infection disease is caused by a virus, wherein the virus is from the family flaviviridae or paramyxoviridae.

PROCESSES FOR THE PREPARATION OF 4,6,7-TRIFLUORO-1H-INDOLE-2-CARBOXYLIC ACID

The present invention relates to processes for preparing a Compound (1):

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or a pharmaceutically acceptable salt or solvate thereof. Compound (1) is useful as in many pharmaceutical agents, especially is useful as key intermediate in the synthesis of certain SARS-CoV-2 3CLpro inhibitors.

PROCESSES FOR THE PREPARATION OF 4,6,7-TRIFLUORO-1H-INDOLE-2-CARBOXYLIC ACID

The present invention relates to processes for preparing a Compound (1):

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or a pharmaceutically acceptable salt or solvate thereof. Compound (1) is useful as in many pharmaceutical agents, especially is useful as key intermediate in the synthesis of certain SARS-CoV-2 3CLpro inhibitors.

PROTEASE INHIBITORS AS ANTIVIRALS
20230026438 · 2023-01-26 ·

Provided herein, inter alia, are compounds, pharmaceutical compositions and methods related to the treatment of viral infections caused by coronavirus or enterovirus. Provided herein are compounds of Formula (I), (II) and (III)

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and methods of using the compounds for therapy. These compounds are peptidomimetics that inhibit protease 3CL of a coronavirus, and are useful for treating conditions caused by viral infections, including COVID-19.

MODULATORS OF E3 LIGASES

Provided herein are methods, oligonucleotides, and compositions for modulating levels of at least one target protein in a cell, e.g., by reducing levels of the mRNA of the target protein or inhibiting translation of the mRNA. In some embodiments, the target protein can be the ubiquitin ligase polypeptide, including, but not limited to WWP1, WWP2, and NEDD4. Also provided herein are methods, oligonucleotides, and compositions for treating, ameliorating, delaying or reducing a symptom of a cancer. The present disclosure also relates to compounds, methods and compositions for modulating at least one target protein selected from ubiquitin protein ligase. Also provided herein are compounds, methods, and compositions for treating, ameliorating, delaying or reducing a symptom of a cancer or a viral infection. In particular, the present disclosure is directed to specific small-molecule modulators of HECT domain E3 ligases that are useful in the therapy and diagnosis of cancer and viral infection.

Indole compounds and analogues thereof

Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising a compound of formula I, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by aberrant complement system activity. ##STR00001##

Indole compounds and analogues thereof

Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising a compound of formula I, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by aberrant complement system activity. ##STR00001##