C07D309/04

IMMUNOREGULATORY AGENTS

Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.

Aminoalkyl compound
11440896 · 2022-09-13 · ·

The present invention directs to provide a novel compound for treating and/or preventing pain, having excellent skin permeation and reduced skin irritation. The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof (R.sup.1: a methyl group or other like group, R.sup.2: a fluorine atom or other like group, R.sup.3: a methyl group or other like group, R.sup.4: a methyl group or other like group, R.sup.5: a methyl group or other like group) ##STR00001##

WDR5-MYC INHIBITORS

Substituted N-phenyl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.

WDR5-MYC INHIBITORS

Substituted N-phenyl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.

Quaternary heteroatom containing compounds

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): ##STR00001##
comprising treating a compound of Formula (I): ##STR00002##
with a transition metal catalyst and under alkylation conditions as valence and stability permit.

Quaternary heteroatom containing compounds

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): ##STR00001##
comprising treating a compound of Formula (I): ##STR00002##
with a transition metal catalyst and under alkylation conditions as valence and stability permit.

PHENOXY(HETERO)ARYL ETHERS OF ANTIPROLIFERACTIVE ACTIVITY

The present invention comprises novel aromatic molecules, which can be used in the treatment of pathological conditions, such as cancer, skin diseases, muscle disorders, and immune system-related disorders such as disorders of the haematopoietic system including the haematologic system in human and veterinary medicine.

PHENOXY(HETERO)ARYL ETHERS OF ANTIPROLIFERACTIVE ACTIVITY

The present invention comprises novel aromatic molecules, which can be used in the treatment of pathological conditions, such as cancer, skin diseases, muscle disorders, and immune system-related disorders such as disorders of the haematopoietic system including the haematologic system in human and veterinary medicine.

SUBSTITUTED AMIDE COMPOUNDS USEFUL AS FARNESOID X RECEPTOR MODULATORS

Disclosed are compounds of Formula (I) or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, wherein Q is a 5-membered heterocyclyl or 5-membered heteroaryl having 1 to 4 heteroatoms independently selected from N, O, and S, substituted with zero to 4 R.sup.1; and A, X.sup.1, X.sup.2, X.sup.3, X.sup.4, Z.sup.1, Z.sup.2, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

##STR00001##

SUBSTITUTED AMIDE COMPOUNDS USEFUL AS FARNESOID X RECEPTOR MODULATORS

Disclosed are compounds of Formula (I) or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, wherein Q is a 5-membered heterocyclyl or 5-membered heteroaryl having 1 to 4 heteroatoms independently selected from N, O, and S, substituted with zero to 4 R.sup.1; and A, X.sup.1, X.sup.2, X.sup.3, X.sup.4, Z.sup.1, Z.sup.2, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

##STR00001##