Other

Cancer Research Technology Limited

The Institute of Cancer Research

Vernalis &r&d) Ltd.

Vernalis (cambridge) Limited

Christofe Fromont

Allan Michael Jordan

Brian William Dymock

Martin James Drysdale

Xavier Barril-Alonso

Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, cancer: wherein Ris a group of formula &#x2014;(Ar)-(Alk)-(Z)-(Alk2)-Q wherein Aris an optionally substituted aryl or heteroaryl radical, Alk' and Alk 2 are optionally substituted divalent C-Calkylene or C-Calkenylene radicals, m, p, r and s are independently 0 or 1, Z is &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;(C&#x2550;O)&#x2014;, &#x2014;(C&#x2550;S)&#x2014;, &#x2014;SO&#x2014;, &#x2014;C(&#x2550;O)O&#x2014;, &#x2014;C(&#x2550;O)NR&#x2014;, &#x2014;C(&#x2550;S)NR&#x2014;, &#x2014;SONR&#x2014;, &#x2014;NRC(&#x2550;O)&#x2014;, &#x2014;NRSO&#x2014; or &#x2014;NR&#x2014; wherein Ris hydrogen or C-Calkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; Ris hydrogen, an optional substituent, or an optionally substituted (C-C)alkyl, aryl or heteroaryl radical; and Ris a carboxylic ester, carboxamide or sulfonamide group. 

Substituted thieno[2,3-d]pyrimidines as HSP90 inhibitors

Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, Cancer: wherein Ris a group of formula &#x2014;(Ar)-(Alk)-(Z)-(Alk 2)-Q wherein Aris an optionally substituted aryl or heteroaryl radical, Alk' and Alk 2 are optionally substituted divalent C-Calkylene or C-Calkenylene radicals, m, p, r and s are independently 0 or 1, Z is &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;(C&#x2550;O)&#x2014;, &#x2014;(C&#x2550;S)&#x2014;, &#x2014;SO&#x2014;, &#x2014;C(&#x2550;O)O&#x2014;, &#x2014;C(&#x2550;O)NR&#x2014;, &#x2014;C(&#x2550;S)NR&#x2014;, &#x2014;SONR&#x2014;, &#x2014;NRC(&#x2550;O)_, &#x2014;NRSO- or &#x2014;NR&#x2014;wherein Ris hydrogen or C-Calkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; Ris hydrogen, an optional substituent, or an optionally substituted (C-C)alkyl, aryl or heteroaryl radical; and Ris a carboxylic ester, carboxamide or sulfonamide group. 

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Abington, United Kingdom

Christofe Fromont