Astrazeneca Ab

Hutchison Medipharma Limited

Andrew Turner

Michael James Waring

Elaine Sophie Elizabeth Stokes

Karl Henrik Edman

David Michael Andrews

Philip Cornwall

Johan Kajanus

Michael Kossenjans

Gavin O'Mahony

Robert Hugh Bradbury

Laurent Francois Andre Hennequin

Jason Grant Kettle

James Francis McCabe

Bo Liu

Zhenping Tian

Keith Raymond Mulholland

Richard Chubb

Carl Anders Hogner

Wei Yu

Karl Anders Hogner

Gareth Paul Howell

Malcolm Allan Young Gall

Neil Keith Adlington

Qisun Gong

Karl Edman

Jerome Dubiez

This specification generally relates to an improved method for the manufacture of 3-[(1S)-1-imidazo[1,2-a]pyridin-6-ylethyl]-5-(1-methylpyrazol-4-yl)triazolo[4,5-b]pyrazine (I), or pharmaceutically acceptable salts thereof; polymorphic forms thereof, and intermediates useful in the manufacture of such compounds and salts thereof.

Method for the manufacture of 3-[(1S)-1-imidazo[1,2-a]pyridin-6-ylethyl]-5-(1-methylpyrazol-4-yl)triazolo[4,5-b]pyrazine and polymorphic forms thereof

Disclosed are certain derivatives of benzoxazinone amides of formula (I), or pharmaceutically acceptable salts thereof, (Formula (I)) that act as mineralocorticoid (MR) receptor modulators that may reduce oxidative stress in endothelium and hence improve vascular function, to methods for their potential therapeutic use, to pharmaceutical compositions containing them and to processes for preparing such compounds. 

Benzoxazinone amides as mineralocorticoid receptor modulators

Disclosed are certain derivatives of benzoxazinone amides of formula (I), or pharmaceutically acceptable salts thereof, that act as mineralocorticoid (MR) receptor modulators that may reduce oxidative stress in endothelium and hence improve vascular function, to methods for their potential therapeutic use, to pharmaceutical compositions containing them and to processes for preparing such compounds.

The invention concerns benzamide compounds of formula (I): compound of formula (I): wherein Ris a C-linked pyrazole ring, which is optionally substituted by one or more groups selected from Calkyl, Ccycloalkyl, Calkoxy and Ccycloalkoxy;or a pharmaceutically acceptable salt or pro-drug form thereof. The invention also concerns processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumors or other proliferative conditions, which are sensitive to the inhibition of histone deacetylase (HDAC).

Benzamide compounds useful as histone deacetylase inhibitors

The invention concerns benzamide compounds of formula (I), wherein Ris a C-linked pyrazole ring, which is optionally substituted by one or more groups selected from Calkyl, Ccycloalkyl, Calkoxy and Ccycloalkoxy; or a pharmaceutically acceptable salt or pro-drug form thereof. The invention also concerns processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumors or other proliferative conditions, which are sensitive to the inhibition of histone deacetylase (HDAC). 

The invention concerns quinazoline derivatives of Formula I wherein Rand Rhave any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB, particularly EGF, receptor tyrosine kinases.

Quinazoline derivatives

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Macclesfield, United Kingdom

Andrew Turner