C07D257/04

TEAD INHIBITORS AND USES THEREOF

The present disclosure provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

TEAD INHIBITORS AND USES THEREOF

The present disclosure provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

INHIBITORS OF PHOSPHOLIPID SYNTHESIS AND METHODS OF USE

Inhibitors of Glycerol 3-Phosphate Acyltransferase (GPAT) are provided; and methods of use in the treatment of cancer; and treatment of conditions relating to metabolic syndrome, hyperlipidemia, infection and inflammation.

TYPE 2 RYANODINE RECEPTOR ACTIVITY INHIBITOR

Providing a RyR2 activity inhibitor having an excellent RyR2 activity inhibitory effect.

A type 2 ryanodine receptor activity inhibitor comprising a compound represented by the following formula (α1) or a salt thereof, or a solvate of the compound or a salt thereof,

##STR00001##

wherein ring Q.sup.1 and ring Q.sup.2 each independently represent a condensed ring of a monocyclic heterocycle or monocyclic carbocyclic ring and a benzene ring, or a benzene ring, R.sup.1 and R.sup.2 each independently represent a substituted or unsubstituted hydrocarbon group having 1 to 9 carbon atoms, a substituted or unsubstituted alkoxy group having 1 to 8 carbon atoms, a substituted or unsubstituted alkoxycarbonyl group having 2 to 8 carbon atoms, a substituted or unsubstituted alkanoyl group having 2 to 8 carbon atoms, a substituted or unsubstituted alkanoyloxy group having 2 to 8 carbon atoms, a hydroxy group, a cyano group or a halogen atom, R.sup.3 represents a hydrogen atom or a substituted or unsubstituted hydrocarbon group having 1 to 8 carbon atoms, R.sup.4 represents a divalent hydrocarbon group having 1 to 8 carbon atoms, X represents an oxygen atom or a sulfur atom, Y represents a methine group or a nitrogen atom, and n and m each independently represent an integer of 0 to 5; with the proviso that, if n is an integer of 2 to 5, n number of R.sup.1 may be the same or different and two R.sup.1 may join together to form a ring; and if m is an integer of 2 to 5, m number of R.sup.2 may be the same or different and two R.sup.2 may join together to form a ring.

TYPE 2 RYANODINE RECEPTOR ACTIVITY INHIBITOR

Providing a RyR2 activity inhibitor having an excellent RyR2 activity inhibitory effect.

A type 2 ryanodine receptor activity inhibitor comprising a compound represented by the following formula (α1) or a salt thereof, or a solvate of the compound or a salt thereof,

##STR00001##

wherein ring Q.sup.1 and ring Q.sup.2 each independently represent a condensed ring of a monocyclic heterocycle or monocyclic carbocyclic ring and a benzene ring, or a benzene ring, R.sup.1 and R.sup.2 each independently represent a substituted or unsubstituted hydrocarbon group having 1 to 9 carbon atoms, a substituted or unsubstituted alkoxy group having 1 to 8 carbon atoms, a substituted or unsubstituted alkoxycarbonyl group having 2 to 8 carbon atoms, a substituted or unsubstituted alkanoyl group having 2 to 8 carbon atoms, a substituted or unsubstituted alkanoyloxy group having 2 to 8 carbon atoms, a hydroxy group, a cyano group or a halogen atom, R.sup.3 represents a hydrogen atom or a substituted or unsubstituted hydrocarbon group having 1 to 8 carbon atoms, R.sup.4 represents a divalent hydrocarbon group having 1 to 8 carbon atoms, X represents an oxygen atom or a sulfur atom, Y represents a methine group or a nitrogen atom, and n and m each independently represent an integer of 0 to 5; with the proviso that, if n is an integer of 2 to 5, n number of R.sup.1 may be the same or different and two R.sup.1 may join together to form a ring; and if m is an integer of 2 to 5, m number of R.sup.2 may be the same or different and two R.sup.2 may join together to form a ring.

FABP4/5 INHIBITORS, METHODS OF USE AND METHODS OF MAKING

Disclosed herein are FABP4 and FABP5 inhibitor compounds and their use in pharmaceutical compositions for treating diseases relating to fatty acid metabolism, including cancer. Also disclosed herein are methods for preparing the disclosed compounds.

MASP-2 INHIBITORS AND METHODS OF USE

The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.

MASP-2 INHIBITORS AND METHODS OF USE

The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.

Modulators of mas-related G-protein receptor X4 and related products and methods

Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): ##STR00001##
or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q.sub.1, Q.sub.2, Z, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

Methionine metabolic pathway inhibitors

The present invention provides novel 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.