Patent classifications
C07D271/07
Compounds which are inhibitors of Notum
A compound for use in the treatment of a disease ameliorated by the inhibition of Notum of formula (I): (I) ##STR00001##
Compounds which are inhibitors of Notum
A compound for use in the treatment of a disease ameliorated by the inhibition of Notum of formula (I): (I) ##STR00001##
Heterocyclic P2X7 antagonists
Disclosed are compounds of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions containing them, and to a process for the preparation of the compounds: ##STR00001##
R.sup.1 is independently selected from hydrogen atom, amine group, monocyclic or bicyclic aliphatic, aromatic, heteroaliphatic or heteroaromatic ring. R.sup.2 is independently selected from monocyclic or bicylic aliphatic, heteroaliphatic, aromatic or heteroaromatic ring, C.sub.1-C.sub.6 alkyl, alkenyl or alkynyl chain. n is 1 or 2; preferably n is 1. m is 0, 1 or 2; preferably m is 0. R.sup.3 and R.sup.4 can be, independently, —H, —F, C.sub.1-C.sub.4 alkyl, —OH, —OC.sub.1-C.sub.4 alkyl; preferably they are both —H. X is O or S. R.sup.5 is —H or —CH.sub.3 optionally substituted by one or more fluorine atoms; preferably R.sup.5 is hydrogen. The compounds can be used in the treatment of conditions or diseases mediated by P2X7 receptor.
Heterocyclic P2X7 antagonists
Disclosed are compounds of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions containing them, and to a process for the preparation of the compounds: ##STR00001##
R.sup.1 is independently selected from hydrogen atom, amine group, monocyclic or bicyclic aliphatic, aromatic, heteroaliphatic or heteroaromatic ring. R.sup.2 is independently selected from monocyclic or bicylic aliphatic, heteroaliphatic, aromatic or heteroaromatic ring, C.sub.1-C.sub.6 alkyl, alkenyl or alkynyl chain. n is 1 or 2; preferably n is 1. m is 0, 1 or 2; preferably m is 0. R.sup.3 and R.sup.4 can be, independently, —H, —F, C.sub.1-C.sub.4 alkyl, —OH, —OC.sub.1-C.sub.4 alkyl; preferably they are both —H. X is O or S. R.sup.5 is —H or —CH.sub.3 optionally substituted by one or more fluorine atoms; preferably R.sup.5 is hydrogen. The compounds can be used in the treatment of conditions or diseases mediated by P2X7 receptor.
INHIBITORS OF PHOSPHOLIPID SYNTHESIS AND METHODS OF USE
Inhibitors of Glycerol 3-Phosphate Acyltransferase (GPAT) are provided; and methods of use in the treatment of cancer; and treatment of conditions relating to metabolic syndrome, hyperlipidemia, infection and inflammation.
FABP4/5 INHIBITORS, METHODS OF USE AND METHODS OF MAKING
Disclosed herein are FABP4 and FABP5 inhibitor compounds and their use in pharmaceutical compositions for treating diseases relating to fatty acid metabolism, including cancer. Also disclosed herein are methods for preparing the disclosed compounds.
FABP4/5 INHIBITORS, METHODS OF USE AND METHODS OF MAKING
Disclosed herein are FABP4 and FABP5 inhibitor compounds and their use in pharmaceutical compositions for treating diseases relating to fatty acid metabolism, including cancer. Also disclosed herein are methods for preparing the disclosed compounds.
Modulators of mas-related G-protein receptor X4 and related products and methods
Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): ##STR00001##
or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q.sub.1, Q.sub.2, Z, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.
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.