C07D495/10

LOW MOLECULAR WEIGHT MODULATORS OF THE COLD MENTHOL RECEPTOR TRPM8 AND USE THEREOF

The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.

SPIRO COMPOUND AND MEDICAL USES THEREOF

The present invention relates to a spiro compound and medical uses thereof. Specifically, the present invention relates to a spiro compound represented by the general formula (I), a preparation method thereof, a pharmaceutical composition containing the same, and is used as an acetyl-Coenzyme A carboxylase (ACC) inhibitor and is used for treating diseases associated with ACC activity. Each substituent in the general formula (I) is as defined in description.

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SUBSTITUTED INDOLE AND INDAZOLE COMPOUNDS
20210403468 · 2021-12-30 ·

Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein X is CR.sub.1 or N; and G, A, R.sub.1; and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

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KRAS G12C INHIBITORS AND USES THEREOF

The invention relates to compounds of Formula I, and pharmaceutically acceptable salts thereof, and methods of making and using the same. The compounds of the invention are effective in inhibiting KRAS protein with a G12C mutation and are suitable for use in methods of treating cancers mediated, in whole or in part, by KRAS G12C mutation.

KRAS G12C INHIBITORS AND USES THEREOF

The invention relates to compounds of Formula I, and pharmaceutically acceptable salts thereof, and methods of making and using the same. The compounds of the invention are effective in inhibiting KRAS protein with a G12C mutation and are suitable for use in methods of treating cancers mediated, in whole or in part, by KRAS G12C mutation.

Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors
20210393623 · 2021-12-23 ·

The present invention provides a compound of formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, the present invention provides a pharmaceutical composition comprising the said compound.

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Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors
20210393623 · 2021-12-23 ·

The present invention provides a compound of formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, the present invention provides a pharmaceutical composition comprising the said compound.

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Quinoxaline derivatives as adenosine receptor antagonists

The invention relates to quinoxaline derivatives of the general formula I, ##STR00001##
and the use of the compounds of the present invention for the treatment and/or prevention of hyperproliferative or infectious diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.

Quinoxaline derivatives as adenosine receptor antagonists

The invention relates to quinoxaline derivatives of the general formula I, ##STR00001##
and the use of the compounds of the present invention for the treatment and/or prevention of hyperproliferative or infectious diseases and disorders in mammals, especially humans, and pharmaceutical compositions containing such compound.

N-AZASPIROCYCLOALKANE SUBSTITUTED N-HETEROARYL COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF SHP2

The present invention relates to compounds of formula I:

##STR00001## in which p, q, Y.sub.1, Y.sub.2, R.sub.1, R.sub.2a, R.sub.2b, R.sub.3a, R.sub.3b, R.sub.4a, R.sub.4b, R.sub.5a, R.sub.5b, R.sub.7 and R.sub.8 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.