Astrazeneca Ab

Bayer Schering Pharma Ag

Astra Zeneca U.k. Limited

Bayer Pharma Aktiengesellschaft

Darren Mckerrecher

Patrick Ple

Kurt G Pike

Michael James Waring

Laurent F A Hennequin

Hartmut Rehwinkel

Markus Berger

Graham C Crawley

Craig Johnstone

Matti Juhani Lepistö

Magnus Munck Af Rosenschöld

Anders Eriksson

Martin Hemmerling

Karl Henrik Edman

Stinabritt Nilsson

Balint Gabos

Jeffrey Philip Poyser

Svetlana Ivanova

Krister Henriksson

Thomas Hansson

Jan Dahmén

Camilla Taflin

Nathaniel George Martin

Elaine S E Stokes

Laurent Francois Andre Hennequin

Clifford David Jones

Roger James

Michael Howard Block

John Wall Rayner

Rodney Brian Hargreaves

Christine Marie Paul Lambert

Suzanne Saxon Bowker

Scott Boyd

Peter William Rodney Caulkett

Christine M P Lambert

Matti Lepistö

Lena Bergström

Karl Edman

Elaine Sophie Stokes

Laurent François André Hennequin

The invention relates to the use of compounds of formula (I) and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula I. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis. 

Quinazoline derivatives as angiogenesis inhibitors

Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments.

Chemical compounds 572

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

The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R, R, R, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).

Compounds effecting glucokinase

Compounds of Formula (I) wherein: Ris hydroxymethyl; Ris selected from &#x2014;C(O)NRR, SONRR, S(O)Rand HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; Ris selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; Ris selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; Ris hydrogen or (1-4C)alkyl; or Rand Rtogether with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described. 

Heteroaryl benzamide derivatives as GLK activators

Compound of formula (I) wherein A is selected from pyridin-2-yl or thiazol-2-yl and R, Rand Rare as described in the specification and their use in the treatment or prevention of a disease or medical conditions mediated through glucokinase. 

Benzofuran derivatives, process for their preparation and intermediates thereof

Heteroaryl benzamide derivatives

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 concerns the use of a quinazoline derivative of Formula (I) wherein Qincludes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q&#x2014;X&#x2014; wherein Xincludes a direct bond and O and Qincludes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of Rand Ris hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Qincludes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human. 

Method of producing an antiangiogenic or vascular permeability reducing effect

The invention relates to the use of compounds of formula (I), wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1&#x2013;3 heteroatoms selected independently from O, N and S; Z is &#x2014;O&#x2014;, &#x2014;NH&#x2014;, &#x2014;S&#x2014;, &#x2014;CH&#x2014; or a direct bond; n is 0&#x2013;5; m is 0&#x2013;3; Rrepresents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, Calkyl, Calkoxy, Calkylsulphanyl, &#x2014;NRR(wherein Rand R, which may be the same or different, each represents hydrogen or Calkyl), or RX&#x2014; (wherein Xand Rare as defined herein; Rrepresents hydrogen, oxo, halogeno, hydroxy, Calkoxy, Calkyl, Calkoxymethyl, Calkanoyl, Chaloalkyl, cyano, amino, Calkenyl, Calkynyl, Calkanoyloxy, nitro, Calkanoylamino, Calkoxycarbonyl, Calkylsulphanyl, Calkylsulphinyl, Calkylsulphonyl, carbamoyl, N&#x2014;Calkylcarbamoyl, N,N-di(Calkylcarbamoyl, aminosulphonyl, N&#x2014;Calkylaminosulphonyl, N,N-di(Calkyl)aminosulphonyl, N&#x2014;(Calkylsulphonyl)amino, N&#x2014;(Calkylsulphonyl)-N&#x2014;(Calkyl)amino, N,N-di(Calkylsulphonyl)amino, a Calkylene chain joined to two ring C carbon atoms, CalkanoylaminoCalkyl, carboxy or a group RX(wherein Xand Rare as defined herein); and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula (I). The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis. 

The invention concerns quinazoline derivatives of Formula (I) wherein Q includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q &mdash;X &mdash; wherein X includes a direct bond and O and Q includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R and R is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal.

Quinazoline derivatives

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Macclesfield, United Kingdom

Darren Mckerrecher