Patent classifications
C07D239/47
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.
Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the disclosure.
Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the disclosure.
KINASE INHIBITORS
There are provided compounds of formula I,
##STR00001##
wherein T, A, Q, Z, G, R.sup.4, R.sup.5a, R.sup.5b and n 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 T, A, Q, Z, G, R.sup.4, R.sup.5a, R.sup.5b and n 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.
2-AMINOPYRIMIDINE COMPOUND AND PHARMACEUTICAL COMPOSITION AND USE THEREOF
Disclosed are a 2-aminopyrimidine compound and pharmaceutical composition and use thereof. The structure of the 2-aminopyrimidine compound is as represented by formula I, in the formula, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, X, Y, Z, W, (i) being as defined in the specification and the claims. Such compounds effectively inhibit the growth of a variety of tumor cells and have inhibitory effects on EGFR and IGF1R protease, and can be used for preparing antineoplastic drugs and overcome the tolerance induced by the existing drugs such as gefitinib, erlotinib and the like. The compound has selectivity for tumors, in particular the wild-type non-small cell lung cancer and have good pharmacokinetic characteristics.
##STR00001##
CYCLOBUTYL NUCLEOSIDE ANALOGS AS ANTI-VIRALS
Described herein are cyclobutyl nucleoside analogs of Formula (I), pharmaceutical compositions that include one or more cyclobutyl nucleoside analogs and methods of using the same to treat HBV, HDV and/or HIV.
##STR00001##
CYCLOBUTYL NUCLEOSIDE ANALOGS AS ANTI-VIRALS
Described herein are cyclobutyl nucleoside analogs of Formula (I), pharmaceutical compositions that include one or more cyclobutyl nucleoside analogs and methods of using the same to treat HBV, HDV and/or HIV.
##STR00001##
Small molecule CD4 mimetics and uses thereof
The invention provides for compounds of formula I: wherein Z is absent or (CR.sub.AR.sub.B).sub.nW; each RA and RB is independently (i) H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, haloalkyl, each of which may be optionally substituted; (ii) OH, ORc, NH2, NHR.sub.c, NR.sub.cR.sub.c, SH, S(O).sub.mR.sub.c; or (iii) R.sub.A and R.sub.B together form C(O); W is absent, C(O), C(O)O, C(O)NR.sub.cR.sub.c, O, S(O).sub.m, or NR.sub.cR.sub.c; Y is an optionally substituted heterocyclic, optionally substituted heteroaryl, optionally substituted cycloalkyl, optionally substituted aryl, or NR.sub.XR.sub.Y; wherein R.sub.x and R.sub.y are each independently H, alkyl or aryl; X.sup.1 is selected from the group consisting of halogen, methyl, and hydroxyl; X2 is a halogen; each R.sub.c is independently alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, each of which may be optionally substituted; m is O, 1, or 2; and n is 1, 2, 3, 4, 5, or 6; and pharmaceutically acceptable salts thereof. ##STR00001##
Small molecule CD4 mimetics and uses thereof
The invention provides for compounds of formula I: wherein Z is absent or (CR.sub.AR.sub.B).sub.nW; each RA and RB is independently (i) H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, haloalkyl, each of which may be optionally substituted; (ii) OH, ORc, NH2, NHR.sub.c, NR.sub.cR.sub.c, SH, S(O).sub.mR.sub.c; or (iii) R.sub.A and R.sub.B together form C(O); W is absent, C(O), C(O)O, C(O)NR.sub.cR.sub.c, O, S(O).sub.m, or NR.sub.cR.sub.c; Y is an optionally substituted heterocyclic, optionally substituted heteroaryl, optionally substituted cycloalkyl, optionally substituted aryl, or NR.sub.XR.sub.Y; wherein R.sub.x and R.sub.y are each independently H, alkyl or aryl; X.sup.1 is selected from the group consisting of halogen, methyl, and hydroxyl; X2 is a halogen; each R.sub.c is independently alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, each of which may be optionally substituted; m is O, 1, or 2; and n is 1, 2, 3, 4, 5, or 6; and pharmaceutically acceptable salts thereof. ##STR00001##