The present invention relates to methods and compounds for regulating or enhancing erthropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease.

The present invention relates to methods and compounds for regulating or enhancing erthropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease.

Described herein is the bromodomain inhibitor 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one, including crystalline forms, amorphous forms, solvates, and hydrates thereof, as well as pharmaceutical compositions that include this bromodomain inhibitor. In some embodiments, the pharmaceutical composition comprises 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one that has been processed by micronization or spray dried dispersion. In some embodiments, the pharmaceutical composition further comprises at least one polymer. In some embodiments, the pharmaceutical composition comprises a solid polymer matrix comprising 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one and at least one polymer. Pharmaceutical compositions comprising 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one are useful for the treatment of cancer or neoplastic disease.

Described herein is the bromodomain inhibitor 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one, including crystalline forms, amorphous forms, solvates, and hydrates thereof, as well as pharmaceutical compositions that include this bromodomain inhibitor. In some embodiments, the pharmaceutical composition comprises 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one that has been processed by micronization or spray dried dispersion. In some embodiments, the pharmaceutical composition further comprises at least one polymer. In some embodiments, the pharmaceutical composition comprises a solid polymer matrix comprising 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one and at least one polymer. Pharmaceutical compositions comprising 4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one are useful for the treatment of cancer or neoplastic disease.

The present invention provides a heterocyclic compound having an RORγt inhibitory action. The present invention relates to a compound represented by the formula (I): ##STR00001##
wherein
Ar is a the partial structure (1) to the partial structure (5),
Q is a bivalent group selected from the group consisting of (Ia)-(If), and
B is a ring optionally having substituent(s),
or a salt thereof.

The present invention provides a heterocyclic compound having an RORγt inhibitory action. The present invention relates to a compound represented by the formula (I): ##STR00001##
wherein
Ar is a the partial structure (1) to the partial structure (5),
Q is a bivalent group selected from the group consisting of (Ia)-(If), and
B is a ring optionally having substituent(s),
or a salt thereof.

The present invention relates to a compound of formula (Ia), or a pharmaceutically acceptable salt or solvate thereof, (I) wherein: ring A is a 5- or 6-membered monocyclic aromatic or heteroaromatic ring, or a 9- or 10-membered bicyclic aromatic or heteroaromatic ring, each of which is optionally substituted with one or more substituents selected from F, Cl, Br, I, CN, alkoxy, NR.sub.11R.sub.11′, OH, SO.sub.2-alkyl, CO.sub.2-alkyl, alkyl, haloalkyl, aralkyl, aryl, and heteroaryl, and wherein said aryl and heteroaryl substituents are in turn optionally substituted with one or more substituents each independently selected from F, Cl, Br, I, CN, alkoxy, NR.sub.11R.sub.11′, OH, alkyl, haloalkyl, and aralkyl; Y and Z are each independently CR10R.sub.10′, wherein R.sub.10 and R.sub.10′ are each independently selected from H, F, alkyl, and haloalkyl; R.sub.1, R.sub.4, and R.sub.5 are each independently selected from H, F, Cl, Br, I and haloalkyl; R.sub.2 and R.sub.3 are each independently selected from H, F, Cl, Br, I, CN, and haloalkyl; wherein at least two of R.sub.2, R.sub.3 and R.sub.4 are other than H; and R.sub.11 and R.sub.11′ are each independently selected from H, alkyl, haloalkyl, COR.sub.12, and SO.sub.2R.sub.13, wherein R.sub.12 and R.sub.13 are both alkyl; wherein the compound is other than: N-(3,4-Dichlorophenyl)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxamide; N-(3,4-Dichlorophenyl)-5,8-dihydropyrido[3,4-d]pyrimidine-7(6H)-carboxamide; N-(4-Chloro-3-(trifluoromethyl)phenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide; N-(3,4-dichlorophenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide; N-(3,4-Dichlorophenyl)-6,7-dihydroisoxazolo[4,5-c]pyridine-5(4H)-carboxamide; and N-(3,4-Dichlorophenyl)-4-methyl-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-carboxamide. Further aspects of the invention relate to such compounds for use in the field of immunooncology, immunology, and related applications.

##STR00001##

The present Specification provides a di-polycyclic compound, and a polymer chain consisting of alternating electron donor compounds and electron acceptor compounds, which include the di-polycyclic compound.

The present Specification provides a di-polycyclic compound, and a polymer chain consisting of alternating electron donor compounds and electron acceptor compounds, which include the di-polycyclic compound.

This invention relates to compounds of Formula (I) wherein Cy.sup.1, L.sup.1, Y, R.sup.1, L.sup.2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions. ##STR00001##