Patent classifications
C07D295/16
Tricyclic sulfones as ROR gamma modulators
There are described ROR modulators of the formula (I), ##STR00001##
or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR activity, for example, autoimmune and/or inflammatory disorders.
Tricyclic sulfones as ROR gamma modulators
There are described ROR modulators of the formula (I), ##STR00001##
or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR activity, for example, autoimmune and/or inflammatory disorders.
ARYLSULFONAMIDES AS OREXIN RECEPTOR AGONISTS
The present disclosure provides novel arylsulfonamide compounds as embodiments of the present disclosure. The compounds are believed to be orexin receptor agonists, useful for the treatment of diseases and conditions caused by reduced activity of orexin.
ARYLSULFONAMIDES AS OREXIN RECEPTOR AGONISTS
The present disclosure provides novel arylsulfonamide compounds as embodiments of the present disclosure. The compounds are believed to be orexin receptor agonists, useful for the treatment of diseases and conditions caused by reduced activity of orexin.
Cyclic vinylogous amides as bromodomain inhibitors
Cyclic vinylogous amides of Formula I are disclosed ##STR00001##
The compounds are useful for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are inhibitors of bromodomain.
Cyclic vinylogous amides as bromodomain inhibitors
Cyclic vinylogous amides of Formula I are disclosed ##STR00001##
The compounds are useful for treating diseases that arise from inappropriate activity of proteins containing an acetyl-lysine. The compositions comprise a genus of cyclic vinylogous amides that are inhibitors of bromodomain.
Bromotriazole intermediates
Bromotriazole intermediates are useful in the synthesis of agonists of the APH receptor. Such compounds include those selected from ##STR00001##
Bromotriazole intermediates
Bromotriazole intermediates are useful in the synthesis of agonists of the APH receptor. Such compounds include those selected from ##STR00001##
Fluorination method
The present invention relates to a process for producing an organic compound comprising an .sup.18F atom. The compounds comprising an .sup.18F can be useful as PET ligands for use in diagnostics and/or scanning. The process of the invention comprises treating an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp.sup.2 hybridized carbon atom, with (i) .sup.18F and (ii) a copper compound. The invention also provides the use of an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp.sup.2 hybridized carbon atom, in a process for producing an organic compound comprising an .sup.18F atom, which process comprises treating the organoboron compound with (i).sup.18F and (ii) a copper compound. The invention also provides a compound of formula (XXXVII): wherein: each PG.sup.A is independently H or an alcohol protecting group; PG.sup.B is H or a carboxylic acid protecting group; each PG.sup.C is independently an amine protecting group; Z is a group selected from a boronic ester group, a boronic acid group, a borate group, and a trifluoroborate group; and a is an integer from 0 to 4. ##STR00001##
Fluorination method
The present invention relates to a process for producing an organic compound comprising an .sup.18F atom. The compounds comprising an .sup.18F can be useful as PET ligands for use in diagnostics and/or scanning. The process of the invention comprises treating an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp.sup.2 hybridized carbon atom, with (i) .sup.18F and (ii) a copper compound. The invention also provides the use of an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp.sup.2 hybridized carbon atom, in a process for producing an organic compound comprising an .sup.18F atom, which process comprises treating the organoboron compound with (i).sup.18F and (ii) a copper compound. The invention also provides a compound of formula (XXXVII): wherein: each PG.sup.A is independently H or an alcohol protecting group; PG.sup.B is H or a carboxylic acid protecting group; each PG.sup.C is independently an amine protecting group; Z is a group selected from a boronic ester group, a boronic acid group, a borate group, and a trifluoroborate group; and a is an integer from 0 to 4. ##STR00001##