Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit transglutaminase 2 (TG2). Also described herein are methods for using such TG2 inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from TG2 inhibition.

The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TRβ mutation.

The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TRβ mutation.

Provided are a compound capable of improving the light-emitting efficiency, stability, and lifespan of an element; an organic electronic element using same; and an electronic device thereof.

The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TRβ mutation.

Novel crystalline forms of Resmetirom (Referred to as “Compound I”), and preparation methods thereof, pharmaceutical compositions containing the crystalline forms, and uses of the crystalline forms for preparing THR-β selective agonist drugs and drugs for treating NASH and HeFH. Compared with prior arts, the provided crystalline forms of Compound I have one or more improved properties, which is of great value to the optimization and development of the drugs containing Compound I.

##STR00001##

A compound of formula (II) or formula (III) ##STR00001##
As defined herein.

The present invention provides a compound substituted with an excellent control effect against a harmful arthropod, which is represented by formula (I)
Het-Q  (I)
wherein Q represents a group represented by Q1, etc., Het represents a group represented by Het1, etc., R.sup.2 represents a C1-C6 alkyl group, etc., G.sup.1 represents a nitrogen atom or CR.sup.3a, G.sup.2 represents a nitrogen atom or CR.sup.3b, G.sup.3 represents a nitrogen atom or CR.sup.3c, G.sup.4 represents a nitrogen atom or CR.sup.3d, R.sup.3a, R.sup.3b, R.sup.3c, and R.sup.3d are identical to or different from each other and represent a C1-C6 chain hydrocarbon group, etc., n represents 0, 1, or 2, T represents a C1-C10 chain hydrocarbon group substituted with one or more halogen atoms, etc., A.sup.2 represents a nitrogen atom or CR.sup.4a, A.sup.3 represents a nitrogen atom or CR.sup.4b, R.sup.4a and R.sup.4b are identical to or different from each other and represent a C1-C6 chain hydrocarbon group, W.sup.1 represents an oxygen atom, etc., and R.sup.6 represents a C1-C6 chain hydrocarbon group, etc. ##STR00001##

The invention provides a composition of matter which:

(i) consists of at least 90% by weight of an atropisomer (2A) and 0-10% by weight of an atropisomer of formula (2B); or
(ii) consists of at least 90% by weight of an atropisomer (2B) and 0-10% by weight of an atropisomer of formula (2A);
wherein the atropisomer of formula (2A) and the atropisomer of formula (2B) are represented by:

##STR00001##

or are pharmaceutically acceptable salts or tautomers thereof, wherein ring X is a benzene or pyridine ring; ring Y is selected from a benzene ring, a pyridine ring and a thiophene ring; R.sup.1 is trifluoromethyl; R.sup.2 is hydrogen; R.sup.3 is hydrogen; m is 0 or 1; n is 0, 1 or 2; Ar.sup.1 is a monocyclic aromatic ring selected from benzene and pyridine; each monocyclic aromatic ring being unsubstituted or substituted with 1 or 2 substituents R.sup.5 as defined herein; and R.sup.4; R.sup.5 when present, R.sup.6 and R.sup.7 independently selected from various substituents as defined herein.

Also provided are individual atropisomers, pharmaceutical compositions and the uses of the atropisomers and compositions are inhibitors of PLK1- and PLK4 kinases, for example in the treatment of cancers.

The invention provides a composition of matter which:

(i) consists of at least 90% by weight of an atropisomer (2A) and 0-10% by weight of an atropisomer of formula (2B); or
(ii) consists of at least 90% by weight of an atropisomer (2B) and 0-10% by weight of an atropisomer of formula (2A);
wherein the atropisomer of formula (2A) and the atropisomer of formula (2B) are represented by:

##STR00001##

or are pharmaceutically acceptable salts or tautomers thereof, wherein ring X is a benzene or pyridine ring; ring Y is selected from a benzene ring, a pyridine ring and a thiophene ring; R.sup.1 is trifluoromethyl; R.sup.2 is hydrogen; R.sup.3 is hydrogen; m is 0 or 1; n is 0, 1 or 2; Ar.sup.1 is a monocyclic aromatic ring selected from benzene and pyridine; each monocyclic aromatic ring being unsubstituted or substituted with 1 or 2 substituents R.sup.5 as defined herein; and R.sup.4; R.sup.5 when present, R.sup.6 and R.sup.7 independently selected from various substituents as defined herein.

Also provided are individual atropisomers, pharmaceutical compositions and the uses of the atropisomers and compositions are inhibitors of PLK1- and PLK4 kinases, for example in the treatment of cancers.