Patent classifications
C07D413/02
ARYL HETEROBICYCLIC COMPOUNDS AS Kv1.3 POTASSIUM SHAKER CHANNEL BLOCKERS
A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is described, where the substituents are as defined herein. Pharmaceutical compositions including the same and method of using the same are also described.
##STR00001##
ARYL HETEROBICYCLIC COMPOUNDS AS Kv1.3 POTASSIUM SHAKER CHANNEL BLOCKERS
A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is described, where the substituents are as defined herein. Pharmaceutical compositions including the same and method of using the same are also described.
##STR00001##
Pesticidally active pyrazole derivatives
A compound of formula (II) or formula (III) ##STR00001##
As defined herein.
Pesticidally active pyrazole derivatives
A compound of formula (II) or formula (III) ##STR00001##
As defined herein.
PHARMACEUTICAL COMPOUNDS
The invention provides a composition of matter which:
(i) consists of at least 90% by weight of an atropisomer (2A) and 0-10% by weight of an atropisomer of formula (2B); or
(ii) consists of at least 90% by weight of an atropisomer (2B) and 0-10% by weight of an atropisomer of formula (2A);
wherein the atropisomer of formula (2A) and the atropisomer of formula (2B) are represented by:
##STR00001##
or are pharmaceutically acceptable salts or tautomers thereof, wherein ring X is a benzene or pyridine ring; ring Y is selected from a benzene ring, a pyridine ring and a thiophene ring; R.sup.1 is trifluoromethyl; R.sup.2 is hydrogen; R.sup.3 is hydrogen; m is 0 or 1; n is 0, 1 or 2; Ar.sup.1 is a monocyclic aromatic ring selected from benzene and pyridine; each monocyclic aromatic ring being unsubstituted or substituted with 1 or 2 substituents R.sup.5 as defined herein; and R.sup.4; R.sup.5 when present, R.sup.6 and R.sup.7 independently selected from various substituents as defined herein.
Also provided are individual atropisomers, pharmaceutical compositions and the uses of the atropisomers and compositions are inhibitors of PLK1- and PLK4 kinases, for example in the treatment of cancers.
PHARMACEUTICAL COMPOUNDS
The invention provides a composition of matter which:
(i) consists of at least 90% by weight of an atropisomer (2A) and 0-10% by weight of an atropisomer of formula (2B); or
(ii) consists of at least 90% by weight of an atropisomer (2B) and 0-10% by weight of an atropisomer of formula (2A);
wherein the atropisomer of formula (2A) and the atropisomer of formula (2B) are represented by:
##STR00001##
or are pharmaceutically acceptable salts or tautomers thereof, wherein ring X is a benzene or pyridine ring; ring Y is selected from a benzene ring, a pyridine ring and a thiophene ring; R.sup.1 is trifluoromethyl; R.sup.2 is hydrogen; R.sup.3 is hydrogen; m is 0 or 1; n is 0, 1 or 2; Ar.sup.1 is a monocyclic aromatic ring selected from benzene and pyridine; each monocyclic aromatic ring being unsubstituted or substituted with 1 or 2 substituents R.sup.5 as defined herein; and R.sup.4; R.sup.5 when present, R.sup.6 and R.sup.7 independently selected from various substituents as defined herein.
Also provided are individual atropisomers, pharmaceutical compositions and the uses of the atropisomers and compositions are inhibitors of PLK1- and PLK4 kinases, for example in the treatment of cancers.
COMPOUNDS ACTIVE TOWARDS BROMODOMAINS
Disclosed are compounds towards bromodomains, pharmaceutical compositions containing the compounds and use of the compounds in therapy.
##STR00001##
COMPOUNDS ACTIVE TOWARDS BROMODOMAINS
Disclosed are compounds towards bromodomains, pharmaceutical compositions containing the compounds and use of the compounds in therapy.
##STR00001##
ANIMAL AND HUMAN ANTI-TRYPANOSOMONAL AND ANTI-LEISHMANIA AGENTS
Provided herein are Aminopurine compounds of Formula I:
##STR00001## or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing animal and human protozoal infections.
ANIMAL AND HUMAN ANTI-TRYPANOSOMONAL AND ANTI-LEISHMANIA AGENTS
Provided herein are Aminopurine compounds of Formula I:
##STR00001## or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing animal and human protozoal infections.