Biota Europe Limited

Procomcure Biotech Gmbh

Bayer Cropscience Gmbh

Ares Trading S.a.

Teijin Pharma Limited

Bayer Cropscience S.a.

Dale Mitchell

John Atherall

Lloyd George Czaplewski

David John Haydon

Christopher Steele

Nicholas Palmer

Thomas Lawley Hough

Kamil Önder

Tamara Ladduwahetty

Roelf Datema

Donald James Simpson

Ivan Kondratov

Jean-Pierre A Vors

Anna Quattropani

Hiroaki Makino

Vincent Pomel

Darren James Mansfield

David Wyn Watson

Kenichiro Kataoka

Gen Unoki

Minoru Imai

Ben Whittaker

Gary Robert William Pitt

Tomomi Kosugi

David Hardick

Ian Collins

Vincent Gerusz

Laura Andrau

David Davies

Yuko Yamakoshi

James T Palmer

Mika Takakuwa

Lorraine Claire Axford

Edward Malcolm Tyndall

Derek Baldwin

Joelle Le

Christopher James Lunnis

Jos&eacute; Perez

David Tickle

David Eric Green

Wilfried Franke

Mark David Charles

Michael Blair

Chris Steele

Dirk Beher

Clifford John Harris

Daniel A Offermann

Kamil ÖNder

The present invention relates to therapeutic agents suitable for use in the treatment of microbial infection in mammals. The present invention further relates to the use of pharmaceutical compositions comprising said agents in the treatment of medical conditions in mammals, in particular in the treatment of microbial infection. The agents and pharmaceutical compositions of the invention are of particular relevance in the treatment of diseases associated with antibiotic-resistant microbes. In one particular embodiment, the pharmaceutical composition can have the structural moiety of formula (I) or a pharmaceutically-acceptable salt of said compound: wherein group A is selected from the formulae Group B is aryl, Ris an optionally substituted aryl ring, an optionally substituted benzyl ring, CH, or Calkyl, and Ris hydrogen, an alkyl group, a halogen, or &#x2014;(CH)N(CH)where n is an integer from 1 to 3.

Imidazole-based antimicrobial agents

The present invention relates to novel compounds of formula (I) suitable e.g. as therapeutic agents for use in the treatment of mammalian disease and in particular to novel therapeutic agents suitable for use in the treatment of microbial infection in mammals. The present invention further relates to the use of pharmaceutical compositions comprising said agents in the treatment of medical conditions in mammals, in particular in the treatment of microbial infection. The agents and pharmaceutical compositions of the invention are of particular relevance in the treatment of diseases associated with antibiotic-resistant microbes. The present invention also relates to processes for making said agents. 

Imidazole-based heterocyclic compounds

The present invention provides fused bicyclic triazole derivatives of Formula (I) useful as gamma secretase modulators (GSM), for the treatment of Alzheimer's disease and related diseases. 

Fused triazole derivatives as gamma secretase modulators

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 Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent MAPKAP-K2 inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for MAPKAP-K2 mediated disorder, such as inflammatory disease, autoimmune disease, destructive bone disorder, cancer and/or tumour growth. 

Pyrazolo[1,5-a]pyrimidine derivatives

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

Fungicidal phenyl(thio)urea and phenyl(thio)carbamate derivatives

Growing community of inventors

Essex, United Kingdom

Dale Mitchell