Patent classifications
C07D519/00
TRICYCLIC HETEROCYCLIC COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS
Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C.sub.1-C.sub.10 alkyl) or S; each X is independently CH or N; R.sup.1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R.sup.2 is (LQ).sub.mY; and each R.sup.3 is independently H, C.sub.1-C.sub.10 alkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110δ, and therefore have utility in therapy.
##STR00001##
THERAPEUTIC COMPOUNDS AND USES THEREOF
The present invention relates to compounds of formula (I):
##STR00001##
and to salts thereof, wherein R.sup.1-R.sup.6 have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of TAF1. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various TAF1-mediated disorders.
THERAPEUTIC COMPOUNDS AND USES THEREOF
The present invention relates to compounds of formula (I):
##STR00001##
and to salts thereof, wherein R.sup.1-R.sup.6 have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of TAF1. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various TAF1-mediated disorders.
DEUTERATED ORGANIC COMPOUND, MIXTURE AND COMPOSITION CONTAINING SAID COMPOUND, AND ORGANIC ELECTRONIC DEVICE
The present disclosure discloses a deuterated organic compound and a formulation and an organic electronic device containing the same, wherein the deuterated organic compound has the following structural formula:
##STR00001##
wherein Ar is an aromatic or heteroaromatic structural unit, D is an electron donor group, A is an electron acceptor group, n and m are an integer between 1 and 6; and wherein for the organic compound, (S1-T1)≦0.25 eV, and at least one H atom of the organic compound is substituted by deuterium. The present disclosure achieves the improvement of the electroluminescence quantum efficiency and the lifetime of the organic compound by replacing the H atom in the organic compound with deuterium and having (S1-T1)≦0.35 eV, and the material of the present disclosure has a great application potential and application range due to its low cost and relatively simple synthesis process.
IMIDAZOPYRAZINE ANALOGS WITH 3-TERTIARY CARBON SUBSTITUTIONS AS BTK INHIBITORS
The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, Formula (I) or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
##STR00001##
IMIDAZOPYRAZINE ANALOGS WITH 3-TERTIARY CARBON SUBSTITUTIONS AS BTK INHIBITORS
The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, Formula (I) or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
##STR00001##
Tricyclic heterocyclic compounds as phosphoinositide 3-kinase inhibitors
A compound of formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C.sub.1-C.sub.10 alkyl) or S; each X is independently CH or N; R.sup.1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R.sup.2 is LY; each L is a direct bond, C.sub.1-C.sub.10 alkylene, C.sub.2-C.sub.10 alkenylene or C.sub.2-C.sub.10 alkynylene; Y is an optionally substituted fused, bridged or spirocyclic non-aromatic 5-12 membered heterocycle containing up to 4 heteroatoms selected from N or O; and each R.sup.3 is independently H, C.sub.1-C.sub.10 alkyl, halogen, fluoro C.sub.1-C.sub.10 alkyl, O—C.sub.1-C.sub.10 alkyl, NH—C.sub.1-C.sub.10 alkyl, S—C.sub.1-C.sub.10 alkyl, O-fluoro C.sub.1-C.sub.10 alkyl, NH-acyl, NH—C(O)—NH—C.sub.1-C.sub.10 alkyl, C(O)—NH—C.sub.1-C.sub.10 alkyl, aryl or heteroaryl, are useful as inhibitors of the class IA phosphoinositide 3-kinase enzyme, PI3K-p110δ, and therefore have potential utility in the therapy of cancer, immune and inflammatory diseases.
Tricyclic heterocyclic compounds as phosphoinositide 3-kinase inhibitors
A compound of formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C.sub.1-C.sub.10 alkyl) or S; each X is independently CH or N; R.sup.1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R.sup.2 is LY; each L is a direct bond, C.sub.1-C.sub.10 alkylene, C.sub.2-C.sub.10 alkenylene or C.sub.2-C.sub.10 alkynylene; Y is an optionally substituted fused, bridged or spirocyclic non-aromatic 5-12 membered heterocycle containing up to 4 heteroatoms selected from N or O; and each R.sup.3 is independently H, C.sub.1-C.sub.10 alkyl, halogen, fluoro C.sub.1-C.sub.10 alkyl, O—C.sub.1-C.sub.10 alkyl, NH—C.sub.1-C.sub.10 alkyl, S—C.sub.1-C.sub.10 alkyl, O-fluoro C.sub.1-C.sub.10 alkyl, NH-acyl, NH—C(O)—NH—C.sub.1-C.sub.10 alkyl, C(O)—NH—C.sub.1-C.sub.10 alkyl, aryl or heteroaryl, are useful as inhibitors of the class IA phosphoinositide 3-kinase enzyme, PI3K-p110δ, and therefore have potential utility in the therapy of cancer, immune and inflammatory diseases.
Azaindole derivatives and their use as ERK kinase inhibitors
The present invention concerns a compound of formula (I), or one of its pharmaceutically acceptable salts, especially for use as inhibitors of the ERK kinase activity in particular ERK2 activity, it also concerns prodrugs of these compounds. ##STR00001##
Azaindole derivatives and their use as ERK kinase inhibitors
The present invention concerns a compound of formula (I), or one of its pharmaceutically acceptable salts, especially for use as inhibitors of the ERK kinase activity in particular ERK2 activity, it also concerns prodrugs of these compounds. ##STR00001##