Patent classifications
C07D239/47
Pyrimidine compounds as mTOR and PI3K inhibitors
The present invention relates to pyrimidine compounds of formula (I): ##STR00001##
which are useful in treating mTOR kinase- or PI3K kinase-related diseases.
Pyrimidine compounds as mTOR and PI3K inhibitors
The present invention relates to pyrimidine compounds of formula (I): ##STR00001##
which are useful in treating mTOR kinase- or PI3K kinase-related diseases.
Process for Producing Fluorocytosine and Fluorocytosine Derivatives
The present invention relates to a method of manufacturing a fluorocytosine-based compound of Formula I.
##STR00001##
The invention also relates to a compound obtained by such a method, a pharmaceutical drug substance and a method for its manufacture, a pharmaceutical composition, and also various uses in therapy of the compounds, pharmaceutical drug substances, and pharmaceutical compositions of the invention.
Process for Producing Fluorocytosine and Fluorocytosine Derivatives
The present invention relates to a method of manufacturing a fluorocytosine-based compound of Formula I.
##STR00001##
The invention also relates to a compound obtained by such a method, a pharmaceutical drug substance and a method for its manufacture, a pharmaceutical composition, and also various uses in therapy of the compounds, pharmaceutical drug substances, and pharmaceutical compositions of the invention.
TRIFLUOROMETHOXYLATION OF ARENES VIA INTRAMOLECULAR TRIFLUOROMETHOXY GROUP MIGRATION
The present invention provides a process of producing a trifluoromethoxylated aryl or trifluoromethoxylated heteroaryl having the structure:
##STR00001##
wherein A is an aryl or heteroaryl, each with or without subsutitution; and R.sub.1 is —H, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(alkylaryl), -(alkylheteroaryl), —NH-(alkyl), —N(alkyl).sub.7, —NH-(alkenyl), —NH-(alkynyl) —NH-(aryl), —NH-(heteroaryl), —O-(alkyl), —O-(alkenyl), —O-(alkynyl), —O-(aryl), —O-(heteroaryl), —S-(alkyl), —S-(alkenyl), —S-(alkynyl), —S-(aryl), or —S-(heteroaryl), comprising: (a) reacting a compound having the structure:
##STR00002##
with a trifluoromethylating agent in the presence of a base in a first suitable solvent under conditions to produce a compound having the structure:
##STR00003##
and (b) maintaining the compound produced in step (a) in a second suitable solvent under conditions sufficient to produce the trifluoromethoxylated aryl or trifluormethoxylated heteroaryl having the structure:
##STR00004##
Substituted acylaminopyrimidines as inducers of alpha interferon production
This invention relates to acylaminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy.
Substituted acylaminopyrimidines as inducers of alpha interferon production
This invention relates to acylaminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy.
Kinase inhibitors
There are provided compounds of formula I, ##STR00001##
wherein R.sup.1 to R.sup.5, X.sup.1, X.sup.2, Ar, L, E, A, A.sup.1, G and G.sup.1 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
Kinase inhibitors
There are provided compounds of formula I, ##STR00001##
wherein R.sup.1 to R.sup.5, X.sup.1, X.sup.2, Ar, L, E, A, A.sup.1, G and G.sup.1 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
Kinase inhibitors
There are provided compounds of formula IIb, ##STR00001##
wherein LG.sup.1 represents imidazolyl, chloro or aryloxy, which compounds are useful in the preparation of compounds that have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.