Ici Pharma

Astrazeneca Ab

Imperial Chemical Industries Limited

Zeneca Limited

Frederic H Jung

Andrew Mortlock

Gareth Morse Davies

Nicola Murdoch Heron

Georges Rene Pasquet

Annie A Olivier

Jean J Lohmann

Alain M Bertrandie

Robert Hugh Bradbury

Patrick Ple

Thomas G Bird

Peter R Marsham

Georges Pasquet

Michael John Betts

Nicholas John Keen

Frank Loftus

Jean-Claude Arnould

Andrew George Brewster

Ronald H Galt

Jean-Jacques M Lohmann

Quinazoline derivatives of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.

Methods of treatment using N-(3-fluorophenyl)-2-{3-[(7-{3-[ethyl(2-hydroxyethyl)amino]propoxy}-quinazolin-4-yl)amino]-1H-pyrazol-5-yl}acetamide

Phosphonoxy quinazoline derivatives and their pharmaceutical use

The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of X, p, R, q, R, R, R, R, Ring A, r and Rhas any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability. 

Quinazoline derivatives

The invention concerns quinoline derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of X, p, R, q, R, R, R, R, Ring A, r and Rhas any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.

Quinoline derivatives

The use of a compound of formula (I) or a salt, ester, amide or prodrug thereof; where X is O, or S, S(O) or S(O), NH or NRwhere Ris hydrogen or Calkyl; Ris selected from a group NHC(O)OR, NHC(O)R, NHS(O)R, C(O)R, C(O)OR, S(O)R, S(O)OR, S(O)OR, C(O)NRR, S(O)NRRS(O)ONRR, where R, Ror Rare various specified organic groups; Ris hydrogen, optionally substituted hydrocarbyl or optionally substituted heterocyclyl; Rand Rare various specified organic groups, and R, R, R, Rare independently selected from halogeno, cyano, nitro, Calkylsulphanyl, &#x2014;N(OH)R&#x2014; (wherein Ris hydrogen, or Calkyl), or RX&#x2014; (wherein Xrepresents a direct bond, &#x2014;O&#x2014;, &#x2014;CH&#x2014;, &#x2014;OCO&#x2014;, carbonyl, &#x2014;S&#x2014;, &#x2014;SO&#x2014;, &#x2014;SO&#x2014;, &#x2014;NRCO&#x2014;, &#x2014;CONR&#x2014;, &#x2014;SONR&#x2014;, &#x2014;NRSO&#x2014; or &#x2014;NR&#x2014; (wherein R, Rand Reach independently represents hydrogen, Calkyl or Calkoxy Calkyl), and Ris hydrogen, optionally substituted hydrocarbyl, optionally substituted heterocyclyl or optionally substituted alkoxy; in the preparation of a medicament for use in the inhibition of aurora 2 kinase. 

Quinazoline derivatives and their use as pharmaceuticals

Quinazoline derivatives of formula (I); for use in the treatment of proliferative diseases such as cancer and in the preparation of medicaments for use in the treatment of proliferative diseases, and to process for their preparation, as well as pharmaceutical compositions containing them as active ingredient. 

Chemical compounds

The invention provides quinazoline derivatives of formula (I): in the preparation of a medicament for use in the inhibition of Aurora kinase and also novel quinazoline derivatives, processes for their preparation, pharamceutical compositions containing them and their use in therapy 

Substituted quinazoline derivatives as inhibitors of aurora kinases

A compound of formula (I)or a salt, ester, amide or prodrug thereof; Ris an optionally substituted 6-membered aromatic ring containing at least one nitrogen atom, and R, R, R, Rare independently selected from halogeno, cyano, nitro, Calkylsulphonyl, &#x2014;N(OH)R&#x2014; (wherein Ris hydrogen, or Calkyl), or RX&#x2014; (wherein Xrepresents a direct bond, &#x2014;O&#x2014;, &#x2014;CH&#x2014;, &#x2014;OC(O)&#x2014;, &#x2014;C(O)&#x2014;, &#x2014;S&#x2014;, &#x2014;SO&#x2014;, &#x2014;SO&#x2014;, &#x2014;NRC(O)&#x2014;, &#x2014;C(O)NR&#x2014;, &#x2014;SONR&#x2014;, &#x2014;NRSO&#x2014; or &#x2014;NR&#x2014; (wherein R, R, R, Rand Reach independently represents hydrogen, Calkyl or CalkoxyCalkyl), and Ris hydrogen, optionally substituted hydrocarbyl, optionally substituted heterocyclyl or optionally substituted alkoxy); provided that at least one of Ror Ris other than hydrogen. These compounds are inhibitors of aurora 2 kinase. Thus they, and pharmaceutical compositions containing them, are useful in methods of treatment of proliferative disease such as cancer and in particular cancers such as colorectal or breast cancer where aurora 2 is upregulated.

Quinoline derivatives and their use as aurora 2 kinase inhibitors

The use of a compound of formula (I)or a salt, ester or amide thereof;where X is O, or S, S(O) or S(O), or NRwhere Ris hydrogen or Calkyl; Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed.

Substituted quinazoline derivatives and their use as inhibitors of aurora-2 kinase

The present invention relates to carbapenems and provides a compound of the formula (I) ##STR1## wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxyethyl;

Antibiotic compounds

The present invention relates to carbapenems and provides a compound of the formula (I) ##STR1## wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;

Antibiotic carbapenem compounds

The present invention provides a compound of the formula: ##STR1## or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein:

Growing community of inventors

Rilly la Montagne, France

Frederic H Jung