Astrazeneca Ab

Michael James Waring

Kurt G Pike

Robert Hugh Bradbury

James Francis McCabe

Elaine Sophie Elizabeth Stokes

Darren Mckerrecher

Alfred Arthur Rabow

Darren McKerrecher

Steven Christopher Glossop

Arshed Mahmood

Zoe Ann Cotter

David Michael Andrews

Leonie Campbell

Roger John Butlin

Andrew Turner

Stuart Norman Lile Bennett

Rolf Peter Walker

Nathaniel George Martin

Craig Johnstone

Zbigniew Stanley Matusiak

Keith Hopkinson Gibson

Paul Michael Murray

Alan Martin Birch

Andrew Leach

Ulrik Jurva

Clive Green

Per Olof Ryberg

Graeme Richard Robb

Mark Andrew Graham

Christer Ralf Westerlund

Peter Gustaf Bonn

Craig Anthony Roberts

Anette Marie Svensson Henriksson

Volker Schnecke

Jonas Rickard Fägerhag

Abid Suleman

Mikael Dan Brink

Helen Claire Pointon

Robert Darren Morse Davies

James Francis Mccabe

Kurt Gordon Pike

The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R, Rand n have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use as anti-proliferative and/or cell-killing agents.

[1,2,4]triazolo[4,3-b]pyridazines for use in the treatment of proliferative diseases

[1,2,4]triazolo[4,3-B]pyridazines for use in the treatment of proliferative diseases

The invention concerns compounds of Formula (I) (Formula (I)) or pharmaceutically-acceptable salts thereof, wherein R, Rand n have any of the meanings defined herein before in the description; processes for their preparation, pharmaceutical compositions containing them and their use as anti-proliferative and/or cell-killing agents. 

The invention concerns benzamide compounds of formula (I): compound of formula (I): wherein Ris a C-linked pyrazole ring, which is optionally substituted by one or more groups selected from Calkyl, Ccycloalkyl, Calkoxy and Ccycloalkoxy;or a pharmaceutically acceptable salt or pro-drug form thereof. The invention also concerns processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumors or other proliferative conditions, which are sensitive to the inhibition of histone deacetylase (HDAC).

Benzamide compounds useful as histone deacetylase inhibitors

The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each Ris a group such as hydroxy, halo, trifluoromethyl and cyano; Ris halo and n is 0-2; and each Ris a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and Ris amino or hydroxy;or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof;processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by histone deacetylase.

Benzamide derivatives useful as histone deacetylase inhibitors

The invention concerns benzamide compounds of formula (I), wherein Ris a C-linked pyrazole ring, which is optionally substituted by one or more groups selected from Calkyl, Ccycloalkyl, Calkoxy and Ccycloalkoxy; or a pharmaceutically acceptable salt or pro-drug form thereof. The invention also concerns processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumors or other proliferative conditions, which are sensitive to the inhibition of histone deacetylase (HDAC). 

DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity 

Substituted pyrazines as DGAT-1 inhibitors

A compound of Formula (I): is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion.

Therapeutic agents

A compound (2S)-2-[1-(2,6-dichlorophenyl)pyrazolo[4,5-e]pyrimidin-4-yl]oxy-3-(3-hydroxyazetidin-1-yl)-N-(5-methylpyrazin-2-yl)propanamide is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion.

(2S)-2-[1-(2-Chloro-6-cyano-phenyl)pyrazolo[4,5-e]pyrimidin-4-yl]oxy-3-[(1R)-2-hydroxy-1-methyl-ethoxy]-N-(5-methylpyrazin-2-yl)propanamide or a pharmaceutically acceptable salt thereof is useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK or GK), leading to a decreased glucose threshold for insulin secretion.

Compounds of formula (I) wherein R, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.

Heteroaryl benzamide derivatives for use as GLK activators in the treatment of diabetes

The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R, R, R, n, A and HET-1 are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK) such as type 2 diabetes. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by GLK using said compounds and methods for preparing compounds of Formula (I).

Heteroarylbenzamide derivatives for use in the treatment of diabetes

Compounds of formula (I), wherein R, R, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described. 

The invention relates to a novel group of compounds of Formula (I) or a salt thereof: wherein R, A and HET-1 are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through glucokinase (GLK) such as type 2 diabetes. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by GLK using said compounds and methods for preparing compounds of Formula (I).

Growing community of inventors

Macclesfield, United Kingdom

Michael James Waring