Patent classifications
A61K31/422
METHODS OF INCREASING CELL PHAGOCYTOSIS
Disclosed are methods for treatments of conditions involving CD47 upregulation using a compound of formula (I):
##STR00001##
Variables R.sub.1-R.sub.9, X, and Het are defined therein. Also disclosed are methods for increasing phagocytosis of a cell using such a compound and pharmaceutical compositions each containing the compound and an anti-cancer agent.
Long-acting injectable formulations comprising an isoxazoline active agent, methods and uses thereof
This invention relates to long-acting injectable formulations for combating parasites in animals, comprising at least one isoxazoline active agent, a poloxamer, and a co-solvent. This invention also provides for improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the long-acting injectable formulations of the invention to the animal in need thereof.
Long-acting injectable formulations comprising an isoxazoline active agent, methods and uses thereof
This invention relates to long-acting injectable formulations for combating parasites in animals, comprising at least one isoxazoline active agent, a poloxamer, and a co-solvent. This invention also provides for improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the long-acting injectable formulations of the invention to the animal in need thereof.
Heterocyclic amides as kinase inhibitors
Disclosed are compounds having the formula: ##STR00001## wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein, and methods of making and using the same.
Heterocyclic amides as kinase inhibitors
Disclosed are compounds having the formula: ##STR00001## wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein, and methods of making and using the same.
BENZIMIDAZOLE INHIBITORS OF PAD ENZYMES
The present invention provides compounds of Formula (I): or a pharmaceutically acceptable salt thereof, useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders. Variables rings A, B, R.sub.1, R.sub.3, R.sub.8, and other variables are as defined herein.
##STR00001##
BENZIMIDAZOLE INHIBITORS OF PAD ENZYMES
The present invention provides compounds of Formula (I): or a pharmaceutically acceptable salt thereof, useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders. Variables rings A, B, R.sub.1, R.sub.3, R.sub.8, and other variables are as defined herein.
##STR00001##
METHODS OF TREATING LIVER FIBROSIS USING CALPAIN INHIBITORS
Disclosed herein are methods of treating liver fibrosis by administering calpain inhibitors to subjects in need thereof.
PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X—Y is —NHSO.sub.2— or —SO.sub.2NH—; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.1 is H or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, C land alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, SO.sub.2NR.sub.12R.sub.13, heteroaryl, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; and R.sub.9 is H, alkyl or halo; R.sub.10 and R.sub.11 are each independently H or alkyl; and R.sub.12 and R.sub.13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (la) and (lb).
##STR00001##
PHENYL-SULFAMOYL.BENZOYC ACIDS AS ERAP1 MODULATORS
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X—Y is —NHSO.sub.2— or —SO.sub.2NH—; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.1 is H or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, C land alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, SO.sub.2NR.sub.12R.sub.13, heteroaryl, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; and R.sub.9 is H, alkyl or halo; R.sub.10 and R.sub.11 are each independently H or alkyl; and R.sub.12 and R.sub.13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (la) and (lb).
##STR00001##