C07D403/12

Heterocyclic compounds for inhibiting TYK2 activities

The present invention is directed to Compounds 1-8, and their pharmaceutically acceptable salts or prodrugs thereof. Compounds 1-8 are selective binders to TYK2's JH2 and they exhibit significant inhibitory effects on the physiological function of TYK2 and they have excellent in vivo pharmacokinetic properties. Compounds 1-5 and 7 have several deuterium substitutions on methyl to improve pharmacokinetic (PK) properties.

BMS-986165 CRYSTAL FORM, PREPARATION METHOD THEREFOR AND USE THEREOF
20230039086 · 2023-02-09 ·

A crystal form of a compound I and a preparation method therefor, a pharmaceutical composition containing the crystal form, and a use of the crystal form in the preparation of a TYK2 inhibitor drug and a drug for treating psoriasis, systemic lupus erythematosus, and Crohn's disease. The crystallization of the compound I has one or more improved properties compared to the existing technology, and has an important value to the future optimization and development of the drug.

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BMS-986165 CRYSTAL FORM, PREPARATION METHOD THEREFOR AND USE THEREOF
20230039086 · 2023-02-09 ·

A crystal form of a compound I and a preparation method therefor, a pharmaceutical composition containing the crystal form, and a use of the crystal form in the preparation of a TYK2 inhibitor drug and a drug for treating psoriasis, systemic lupus erythematosus, and Crohn's disease. The crystallization of the compound I has one or more improved properties compared to the existing technology, and has an important value to the future optimization and development of the drug.

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AROMATIC SULPHONAMIDES DERIVATIVES THAT INHIBITS PDI A3, THEIR SYNTHESIS AND USE

The invention relates to a new group of aromatic sulphonamides derivatives of formula (I) and their synthesis and use for modulation of the activity of protein disulfide isomerase (PDI). More particularly, the invention provides small molecule inhibitors of PDI A1 that display antiplatelet, antithrombotic and anticancer activities.

AROMATIC SULPHONAMIDES DERIVATIVES THAT INHIBITS PDI A3, THEIR SYNTHESIS AND USE

The invention relates to a new group of aromatic sulphonamides derivatives of formula (I) and their synthesis and use for modulation of the activity of protein disulfide isomerase (PDI). More particularly, the invention provides small molecule inhibitors of PDI A1 that display antiplatelet, antithrombotic and anticancer activities.

MATRIPTASE 2 INHIBITORS AND USES THEREOF

The present invention provides compounds for inhibiting matriptase 2, or a mutant thereof, and compositions and methods of use thereof.

MATRIPTASE 2 INHIBITORS AND USES THEREOF

The present invention provides compounds for inhibiting matriptase 2, or a mutant thereof, and compositions and methods of use thereof.

SMALL MOLECULE MODULATORS OF SIGMA-1 AND SIGMA-2 RECEPTORS AND USES THEREOF

This invention is in the field of medicinal chemistry. In particular, the invention relates to anew class of small-molecules having a tetrahydroindazole structure which function as modulators (e.g., activators or inhibitors) of sigma-1 and/or sigma-2 receptors, and their use as therapeutics for the treatment of cancer and other diseases (e.g., neurological conditions) characterized with sigma-1 and/or sigma-2 receptor activity.

SMALL MOLECULE MODULATORS OF SIGMA-1 AND SIGMA-2 RECEPTORS AND USES THEREOF

This invention is in the field of medicinal chemistry. In particular, the invention relates to anew class of small-molecules having a tetrahydroindazole structure which function as modulators (e.g., activators or inhibitors) of sigma-1 and/or sigma-2 receptors, and their use as therapeutics for the treatment of cancer and other diseases (e.g., neurological conditions) characterized with sigma-1 and/or sigma-2 receptor activity.

ALKENE-CONTAINING AMIDE COMPOUND AND APPLICATION THEREOF

An alkene-containing amide compound of formula (I) and agriculturally acceptable salts thereof can be used as herbicides.

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