Patent classifications
C07F9/65324
Synthesis of Phosphoramidates
A process for the preparation of a compound of formula (I) including all isomers, stereoisomers, enantiomers and diastereomers thereof (I), and salts thereof; the process comprising providing a mixture comprising a compound of formula (II) and a compound of formula (III) subjecting the mixture provided in a) to reaction conditions in the presence of one or more Lewis acids to the mixture provided in a), obtaining a mixture comprising the compound of formula (I).
##STR00001##
Compounds and method for treating autoimmune diseases
Compounds and embodiments of a method for treating and/or preventing autoimmune diseases are disclosed. The method includes administering to a subject having an autoimmune disease, such as an inflammatory bowel disease, a therapeutically effective amount of a compound according to formula I ##STR00001##
wherein X and Y independently are O or NR.sup.1; each R.sup.1 is independently H or C.sub.1-C.sub.6 alkyl; ring A is aryl; each R.sup.2 independently is H, alkyl, alkoxy, amide, cyano, halo, haloalkyl, hydroxyalkyl, heteroalkyl, heterocyclyl, sulfonyl, sulfonamide, or two R.sup.2 groups, taken together with the atom or atoms to which they are attached, combine to form a 4-10 membered ring system; p is 0, 1, 2, 3, or 4; R.sup.3 and R.sup.4 independently are H or C.sub.1-C.sub.6 alkyl; and R.sup.5 is halo, cyano, or C.sub.1-C.sub.6 alkyl.
COMPOUNDS, COMPOSITIONS AND METHODS FOR STABILIZING TRANSTHYRETIN AND INHIBITING TRANSTHYRETIN MISFOLDING
Provided herein are compounds having activity against TTR related conditions, and pharmaceutically accepted salts and solvates thereof. Also provided are methods of using the compounds for inhibiting and preventing TTR aggregation and/or amyloid formation in the peripheral nerves, kidney, cardiac tissue, eye and CNS, and of treating a subject with peripheral TTR amyloidosis.
COMPOUNDS AND METHOD FOR TREATING AUTOIMMUNE DISEASES
Compounds and embodiments of a method for treating and/or preventing autoimmune diseases are disclosed. The method includes administering to a subject having an autoimmune disease, such as an inflammatory bowel disease, a therapeutically effective amount of a compound according to formula I
##STR00001##
wherein X and Y independently are O or NR.sup.1; each R.sup.1 is independently H or C.sub.1-C.sub.6 alkyl; ring A is aryl; each R.sup.2 independently is H, alkyl, alkoxy, amide, cyano, halo, haloalkyl, hydroxyalkyl, heteroalkyl, heterocyclyl, sulfonyl, sulfonamide, or two R.sup.2 groups, taken together with the atom or atoms to which they are attached, combine to form a 4-10 membered ring system; p is 0, 1, 2, 3, or 4; R.sup.3 and R.sup.4 independently are H or C.sub.1-C.sub.6 alkyl; and R.sup.5 is halo, cyano, or C.sub.1-C.sub.6 alkyl.
Heterocyclic bridged biphenyls
The present invention relates electroluminescent devices, comprising a compound of the formula ##STR00001##
especially as host for phosphorescent compounds. The hosts may function with phosphorescent materials to provide improved efficiency, stability, manufacturability, or spectral characteristics of electroluminescent devices.
Substituted tricyclic heterocyclic compounds
Disclosed are compounds of Formula (I), Formula (II), Formula (III), and Formula (IV) or salts thereof, wherein R.sub.2 is OH or OP(O)(OH).sub.2; and R.sub.1 is defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease. ##STR00001##
COMPOUNDS AND METHOD FOR TREATING AUTOIMMUNE DISEASES
Compounds and embodiments of a method for treating and/or preventing autoimmune diseases are disclosed. The method includes administering to a subject having an autoimmune disease, such as an inflammatory bowel disease, a therapeutically effective amount of a compound according to formula I
##STR00001##
wherein X and Y independently are O or NR.sup.1; each R.sup.1 is independently H or C.sub.1-C.sub.6 alkyl; ring A is aryl; each R.sup.2 independently is H, alkyl, alkoxy, amide, cyano, halo, haloalkyl, hydroxyalkyl, heteroalkyl, heterocyclyl, sulfonyl, sulfonamide, or two R.sup.2 groups, taken together with the atom or atoms to which they are attached, combine to form a 4-10 membered ring system; p is 0, 1, 2, 3, or 4; R.sup.3 and R.sup.4 independently are H or C.sub.1-C.sub.6 alkyl; and R.sup.5 is halo, cyano, or C.sub.1-C.sub.6 alkyl.
Compounds and method for treating autoimmune diseases
Compounds and embodiments of a method for treating and/or preventing autoimmune diseases are disclosed. The method includes administering to a subject having an autoimmune disease, such as an inflammatory bowel disease, a therapeutically effective amount of a compound according to formula I ##STR00001##
wherein X and Y independently are O or NR.sup.1; each R.sup.1 is independently H or C.sub.1-C.sub.6 alkyl; ring A is aryl; each R.sup.2 independently is H, alkyl, alkoxy, amide, cyano, halo, haloalkyl, hydroxyalkyl, heteroalkyl, heterocyclyl, sulfonyl, sulfonamide, or two R.sup.2 groups, taken together with the atom or atoms to which they are attached, combine to form a 4-10 membered ring system; p is 0, 1, 2, 3, or 4; R.sup.3 and R.sup.4 independently are H or C.sub.1-C.sub.6 alkyl; and R.sup.5 is halo, cyano, or C.sub.1-C.sub.6 alkyl.
SUBSTITUTED TRICYCLIC HETEROCYCLIC COMPOUNDS
Disclosed are compounds of Formula (I), Formula (II), Formula (III), and Formula (IV) or salts thereof, wherein R.sub.2 is OH or OP(O)(OH).sub.2; and R.sub.1 is defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
##STR00001##
Heterocyclic bridged biphenyls
The present invention relates electroluminescent devices, comprising a compound of the formula
##STR00001##
especially as host for phosphorescent compounds. The hosts may function with phosphorescent materials to provide improved efficiency, stability, manufacturability, or spectral characteristics of electroluminescent devices.