Patent classifications
C07D237/28
ARYL ETHER COMPOUNDS AS TEAD MODULATORS
The present invention is directed to a compound of Formula I: or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising them and methods of using such compounds or pharmaceutical salts thereof.
##STR00001##
ARYL ETHER COMPOUNDS AS TEAD MODULATORS
The present invention is directed to a compound of Formula I: or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising them and methods of using such compounds or pharmaceutical salts thereof.
##STR00001##
Compounds and their use
The specification generally relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where R.sup.1, R.sup.2A, R.sup.2B, R.sup.2C, R.sup.2D, W, X, Y, and Z have the meanings defined herein. Such compounds are useful in inhibiting NLRP3 inflammasome activity and may be useful as therapeutic agents. The specification also relates to the use of such compounds to treat or prevent diseases and conditions in which the NLRP3 inflammasome is implicated. The specification further relates to compositions comprising such compounds. ##STR00001##
Compounds and their use
The specification generally relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where R.sup.1, R.sup.2A, R.sup.2B, R.sup.2C, R.sup.2D, W, X, Y, and Z have the meanings defined herein. Such compounds are useful in inhibiting NLRP3 inflammasome activity and may be useful as therapeutic agents. The specification also relates to the use of such compounds to treat or prevent diseases and conditions in which the NLRP3 inflammasome is implicated. The specification further relates to compositions comprising such compounds. ##STR00001##
KIT KINASE INHIBITORS AND METHODS OF USE THEREOF
Described herein are compounds that are inhibitors of wild type and oncogenic mutant c-KIT kinase and their use in the treatment of disorders such as cancers.
KIT KINASE INHIBITORS AND METHODS OF USE THEREOF
Described herein are compounds that are inhibitors of wild type and oncogenic mutant c-KIT kinase and their use in the treatment of disorders such as cancers.
SUBSTITUTED BICYCLIC HETEROARYL ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
The present disclosure relates to compounds of formula (I) that are useful as modulators of 7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation.
##STR00001##
Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
Inhibitors of tryptophan-2,3-dioxygenase or indoleamine-2,3-dioxygenase
Provided is a compound for use in medicine for inhibiting tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO), which compound comprises formula (I) wherein X.sup.1, X.sup.2, and X.sup.7, may be the same or different and each is independently selected from C and N; X.sup.3, X.sup.4, X.sup.5, and X.sup.6 may be the same or different and each is independently selected from C, N, O and S wherein when X.sup.3 is N it has a double bond and wherein when X.sup.6 is N it has a double bond; the dotted line is a bond which may be present or absent; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that at least one of R.sup.2, R.sup.3, R.sup.4 and R.sup.6 comprises a group Y; and provided that the number of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 groups present is such that the respective valencies of X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, X.sup.6, and X.sup.7 are maintained; and wherein Y is a group having a formula selected from (II), (III), (IV), (V) wherein L may be present or absent, and may be a substituted or unsubstituted organic linking group, and R.sup.31 and R.sup.32 may be the same or different and are selected from H and a substituted or unsubstituted organic group, X.sup.8 is selected from C and N, and each R.sup.313 may be the same or different and is selected from H and a substituted or unsubstituted organic group. ##STR00001##