C07D451/02

Heterocyclic compounds useful as aurora a selective inhibitors

Provided are compounds of formula (I), or pharmaceutically acceptable salts thereof, which can be used for inhibiting the activity of Aurora A and treating cancer mediated by Aurora A. ##STR00001##

Histone acetylase p300 inhibitor and use thereof

A compound represented by formula (I), or a stereochemical isomer thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof, can inhibit the activity of histone acetylase p300 and inhibit the proliferation activity of a variety of tumor cells.

##STR00001##

Histone acetylase p300 inhibitor and use thereof

A compound represented by formula (I), or a stereochemical isomer thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof, can inhibit the activity of histone acetylase p300 and inhibit the proliferation activity of a variety of tumor cells.

##STR00001##

QUINOLINYL-PYRAZINE-CARBOXAMIDE COMPOUNDS AND USES THEREOF
20220081412 · 2022-03-17 ·

This invention is in the field of medicinal chemistry. In particular, the invention relates to anew class of small-molecules having a quinolinyl-pyrazine-carboxamide (or similar) structure which function as activators of the cholesterol biosynthesis pathway within cancer cells and/or immune cells, which function as activators of the cell cycle regulation pathway within cancer cells and/or immune cells, and which function as up-regulators of HMGCS1 protein expression within cancer cells and/or immune cells, and which function as effective therapeutic agents for treating, ameliorating, and preventing various forms of cancer and other inflammatory disease.

QUINOLINYL-PYRAZINE-CARBOXAMIDE COMPOUNDS AND USES THEREOF
20220081412 · 2022-03-17 ·

This invention is in the field of medicinal chemistry. In particular, the invention relates to anew class of small-molecules having a quinolinyl-pyrazine-carboxamide (or similar) structure which function as activators of the cholesterol biosynthesis pathway within cancer cells and/or immune cells, which function as activators of the cell cycle regulation pathway within cancer cells and/or immune cells, and which function as up-regulators of HMGCS1 protein expression within cancer cells and/or immune cells, and which function as effective therapeutic agents for treating, ameliorating, and preventing various forms of cancer and other inflammatory disease.

THERAPEUTIC COMBINATIONS AS ANTIDOTES FOR ORGANOPHOSPHATE EXPOSURE

In alternative embodiments, the provided are therapeutic combinations comprising: nucleophilic hydroxyimino-acetamido alkylamine antidotes that cross the blood-brain barrier (BBB) to catalyze the hydrolysis of organophosphate (OP)-inhibited human acetylcholinesterase (hAChE) in the central nervous system (CNS); and, a brain efflux transporter inhibitor, or an inhibitor of renal tubular secretion, wherein optionally the brain efflux transporter inhibitor or the inhibitor of renal tubular secretion comprises a P-glycoprotein inhibitor, an organic anion transporter (OAT) inhibitor and/or an organic cation (OCT) transporter inhibitor.

Substituted benzenecarboxamides as IL-17A modulators

The disclosure herein provides compounds and pharmaceutical compositions for the modulation of IL-17A useful for the treatment of inflammatory conditions, such as psoriasis.

IMMUNOMODULATORS, COMPOSITIONS AND METHODS THEREOF
20220098183 · 2022-03-31 ·

Provided herein are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

##STR00001##

IMMUNOMODULATORS, COMPOSITIONS AND METHODS THEREOF
20220098183 · 2022-03-31 ·

Provided herein are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

##STR00001##

Diamine derivatives as inhibitors of leukotriene A4 hydrolase

This invention is directed to compounds of formula (I): ##STR00001##
where r, q, R, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c, R.sup.6a, R.sup.6b, R.sup.6c, R.sup.7, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.