Xention Limited

Biota Europe Limited

Agrevo UK Limited

Bayer Cropscience Gmbh

Merck Serono S. A.

Prolysis Ltd.

John Atherall

David John Madge

John Ford

Lloyd George Czaplewski

David John Haydon

Dale Mitchell

Nicholas John Palmer

Thomas Lawley Hough

Nicholas Palmer

Christopher Steele

Tamara Ladduwahetty

John H Parsons

Stephen David Lindell

Derek Edward John

Mary Josephine O'Mahony

Elizabeth Anne Saville-Stones

Matthias Schwarz

Patrick Naxos Page

Stefano Crosignani

Dennis Church

David Wyn Watson

Dale Robert Mitchell

Gary Robert William Pitt

Ian Collins

Christophe Cleva

Jacqueline Anne Macritchie

Laura Andrau

James T Palmer

David Davies

Eric Sebille

Lorraine Claire Axford

Mark Bushfield

Donald James Simpson

Edward Malcolm Tyndall

Cedric Merlot

Doris Pupowicz

Brad Sherborne

Edward Benedict Stevens

Christopher Richard Steele

Christopher James Lunnis

Mark David Charles

Daniel A Offermann

Wilfried Franke

Michael Blair

David Eric Green

Derek John

The present invention provides a compound of the following formula and salts thereof: Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.

Antibacterial compounds

Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C-Calkylene, alkenylene or alkynylene radical which may contain an ether (&#x2014;O&#x2014;), thioether (&#x2014;S&#x2014;) or amino (&#x2014;NR)&#x2014; link, wherein R is hydrogen, &#x2014;CN or C-Calkyl; X is &#x2014;C(&#x2550;O)NR&#x2014;, &#x2014;S(O)NR&#x2014;, &#x2014;C(&#x2550;O)O&#x2014; or &#x2014;S(&#x2550;O)O&#x2014; wherein Ris hydrogen, optionally substituted C-Calkyl, C-Calkenyl, C-Calkynyl, -Cyc, or &#x2014;(C-Calkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N; Rand Rare as defined in the description.

Antibacterial compositions

Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C-Calkylene, alkenylene or alkynylene radical which may contain an ether (&#x2014;O&#x2014;), thioether (&#x2014;S&#x2014;) or amino (&#x2014;NR)&#x2014; link, wherein R is hydrogen, &#x2014;CN or C-Calkyl; X is &#x2014;C(&#x2550;O)NR&#x2014;, &#x2014;S(O)NR&#x2014;, &#x2014;C(&#x2550;O)O&#x2014; or &#x2014;S(&#x2550;O)O&#x2014; wherein Ris hydrogen, optionally substituted C-Calkyl, C-Calkenyl, C-Calkynyl, -Cyc, or &#x2014;(C-Calkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; Rand Rare as defined in the description.

The present invention is related to the use of spiro derivatives of Formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of spiro derivatives for the modulation of CRTH2 activity. 

Tricyclic spiro derivatives as CRTH2 modulators

The invention provides compounds of the formula:  These compounds find use as inhibitors of potassium ion channels and thus are useful in the treatment of various conditions including arrhythmia and type-2 diabetes mellitus.

Thieno[2 3-b]pyridines as potassium channel inhibitors

This invention relates to novel compound of formula (I) or pharmaceutically acceptable salts thereof. The invention is also directed to the uses of compounds having formula (I) in the treatment or prevention of diseases or disorders which requires potassium channel inhibition to an animal, mammal or human in need thereof. The invention is also directed to the use of compounds having formula (I) in the treatment or prevention of arrhythmia to an animal, mammal or human in need thereof.

Substituted thieno[2,3-d]pyrimidines as potassium channel inhibitors

Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C-Calkylene, alkenylene or alkynylene radical which may contain an ether (&#x2014;O&#x2014;), thioether (&#x2014;S&#x2014;) or amino (&#x2014;NR)&#x2014; link, wherein R is hydrogen, &#x2014;CN or C-Calkyl; X is &#x2014;C(&#x2550;O)NR&#x2014;, &#x2014;S(O)NR&#x2014;, &#x2014;C(&#x2550;O)O&#x2014; or &#x2014;S(&#x2550;O)O&#x2014; wherein Ris hydrogen, optionally substituted C-Calkyl, C-Calkenyl, C-Calkynyl, -Cyc, or &#x2014;(C-Calkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; Rand Rare as defined in the description. 

The invention provides compounds of the formula: wherein These compounds find use as inhibitors of potassium ion channels and thus are useful in the treatment of various conditions including arrhythmia and type-2 diabetes mellitus.

Thieno[2,3-B] pyridines as potassium channel inhibitors

Furanopyrimidine compounds as potassium ion channel inhibitors

The invention provides fungicidal compounds of formula (I) and salts thereof wherein: Ris alkyl, alkenyl, alkynyl, carbocyclyl or heterocyclyl, each of which may be substituted, or hydrogen; Rand R, which may be the same or different, are any group defined for R; cyano; acyl; &#x2014;ORor &#x2014;SR, where Ris alkyl, alkenyl, alkynyl, carbocyclyl or heterocyclyl, each of which may be substituted; or Rand R, or Rand R, together with their interconnecting atoms may form a ring, which may be substituted; Ris alkyl, alkenyl, alkynyl, carbocyclyl or heterocyclyl, each of which may be substituted; hydroxy; mercapto; azido; nitro; halogen; cyano; acyl; optionally substituted amino; cyanato; thiocyanato; &#x2014;SF; &#x2014;OR; &#x2014;SRor &#x2014;Si(R); m is 0 to 3; when present R, which may be the same or different to any other R, is any group defined for R; Ris optionally substituted carbo- or heterocylclyl; and A is a defined linking group, or &#x2014;A&#x2014;Rand Rtogether with benzene ring M form an optionally substituted fused ring system.

N2-phenylamidine derivatives

The invention provides the use in combating fungi of compounds of general formula I wherein R is hydrogen, hydroxy, acyl, acyloxy, optionally substituted amino, R , R Si, R S or R O, where R is optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted cycloalkenyl, optionally substituted aryl or optionally substituted heterocyclyl; Z is oxygen or sulfur; M is a thiophene ring; and R and R , which may be the same or different, have the same meaning as R or can be optionally substituted amino, hydrogen, halogen, cyano, nitro or a group OR or S(O) R , where R has the same meaning as R or is hydrogen or acyl and m is 0, 1 or 2; or R and R together with the atoms to which they are attached form an optionally substituted carbocyclic or heterocyclic ring; together with tautomers of compounds where R is hydrogen.

Fungicides

The invention provides the use in combating fungi of compounds of general formula (I) wherein R is hydrogen, hydroxy, acyl, acyloxy, optionally substituted amino, R , R Si, R S or R O, where R is optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted cycloalkenyl, optionally substituted aryl or optionally substituted heterocyclyl; R has the same meaning as R or can be hydrogen; Z is oxygen or sulfur, M is a thiophene ring, and R and R , which may be the same or different, have the same meaning as R or can be optionally substituted amino, hydrogen, halogen, cyano, nitro or a group OR or S(O) R , where R has the same meaning as R or is hydrogen or acyl and m is 0, 1 or 2; or R and R together with the atoms to which they are attached form an optionally substituted carbocyclic or heterocyclic ring; together with tautomers of compounds where R is hydrogen.

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Essex, United Kingdom

John Atherall