Astrazeneca Ab

Other

Thomas Geoffrey Colerick Bird

Jean-Claude Arnould

Grigorios Nikitidis

Joakim Larsson

Peter Storm

Mickael Louis Pierre Maudet

John Peter Bailey

Matthias Ferdinand Herdemann

Marie-Jeanne Pasquet

Jacques Pelleter

Malena Bengtsson

Edward Jolyon Griffen

The invention provides thiazole derivatives of formula (I), or pharmaceutically acceptable salts thereof in which Ring A, R, Rand Rare as defined in the specification; a processes for their preparation; pharmaceutical compositions containing them; and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.

5-heteroaryl thiazoles and their use as PI3K inhibitors

The invention relates to a group of novel pyrazole compounds of Formula (I): wherein: R, R, R, M and Rare as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.

Derivatives of 3-hydroxy-4-(cyclyl-alkylaminoalkyl)-5-phenyl-1h-pyrazole as antagonists of the gonadotropin releasing hormone (GnRH) for use in the treatment of sex hormone related conditions, such as prostatic of uterine cancer

This invention relates to novel compounds of Formula (I) for use as vascular damaging agents:wherein: X is selected from: &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;S(O)&#x2014;, &#x2014;S(O)&#x2014;, &#x2014;N(R)&#x2014; or &#x2014;N(R)CHC(O)&#x2014;; Ris independently selected from: amino, halo, hydroxy, &#x2014;OPOH, Calkyl, Calkoxy, N-Calkylamino, N,N-di-Calkanoylamino or Calkylthio wherein the amino group is optionally substituted by an amino acid residue and the hydroxy group is optionally esterified; Ris selected from: hydrogen or Calkyl; Ris selected from: hydrogen or Calkyl; Ris selected from: hydrogen or Calkyl; n is 0, 1 or 2; and p is 0, 1, 2 or 3; or a salt, pro-drug or solvate thereof. The invention also relates to methods for preparing compounds of Formula (I), to their use as medicaments (including methods for the treatment of angiogenesis or disease states associated with angiogenesis) and to pharmaceutical compositions containing compounds of Formula (I).

Benzoxazinone derivatives for use in the treatment of angiogenesis

Hydroxamic acids substituted by heterocycles useful for inhibition of tumor necrosis factor

Processes for preparing compounds of the formula (I) are described: P,OOC&mdash;CH(OH)&mdash;CHR,&mdash;CONH&mdash;Z wherein P,is hydrogen or a protecting group, Z is a group &mdash;CHR,COOP,or &mdash;CHR,CONR,R,wherein P,is hydrogen or a protecting group and R,-R,are values known in the TNF-inhibitor art. The compounds of the formula (I) are useful in inhibiting TNF and one or more matrix metalloproteinase enzymes. One intermediate in a process of the invention is formula (II).

Process for the preparation of N-(3-hydroxy-succinyl)-amino acid derivatives

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Reims, France

Thomas Geoffrey Colerick Bird