Arrow Therapeutics Limited

Elisa Henderson

Malcolm Clive Carter

Debra Taylor

Lara Wilson

Richard Kelsey

Stan Tyms

Verity Dowdell

Phil Chambers

Dagmar Alber

Kenneth Powell

Philip Chambers

Stanley Tyms

A pharmaceutical composition which comprises a pharmaceutically acceptable carrier or diluent and: (a) an inhibitor of the RSV fusion protein; and (b) a benzodiazepine derivative capable of inhibiting RSV replication is found to be highly active against RSV.

Pharmaceutical composition comprising a benzodiazepine derivative and an inhibitor of the RSV fusion protein

Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV Formula (I) Wherein: &#x2014;Rrepresents Calkyl, aryl or heteroaryl; &#x2014;Rrepresents hydrogen or Calkyl; -each Ris the same or different and represents halogen, hydroxy, Calkyl, Calkoxy, Calkylthio Chaloalkyl, Chaloalkoxy, amino, mono(Calkyl)amino, di(Calkyl)amino, nitro, cyano, &#x2014;COR', CONR&#x2032;R&#x2033;, &#x2014;NH&#x2014;CO&#x2014;R&#x2032;, &#x2014;S(O)R&#x2032;, &#x2014;S(O)R&#x2032;, &#x2014;NH&#x2014;S(O)R&#x2032;, &#x2014;S(O)NR&#x2032;R&#x2033; or &#x2014;S(O)NR&#x2032;R&#x2033; wherein each R&#x2032; and R&#x2033; is the same or different and represents hydrogen or Calkyl; -n is from 0 to 3; Rrepresents hydrogen or Calkyl; &#x2014;Rrepresents Calkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(Calkyl)-, heteroaryl-(Calkyl)-, carbocyclyl-(Calkyl)-, heterocyclyl-(Calkyl)-, aryl-C(O)&#x2014;C(O)&#x2014;, heteroaryl-C(O)&#x2014;C(O)&#x2014;, carbocyclyl-C(O)&#x2014;C(O)&#x2014;, heterocyclyl-C(O)&#x2014;C(O)&#x2014; or, &#x2014;XR; &#x2014;X represents &#x2014;CO&#x2014;, &#x2014;S(O)&#x2014; or &#x2014;S(0)&#x2014;; and &#x2014;Rrepresents Calkyl, hydroxy, Calkoxy, Calkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(Calkyl)-, heteroaryl-(Calkyl)-, carbocyclyl-(Calkyl)-, heterocyclyl-(Calkyl)-, aryl-(Chydroxyalkyl)-, heteroaryl-(Chydroxyalkyl)-, carbocyclyl-(Chydroxyalkyl)-, heterocyclyl-(Chydroxyalkyl)-, aryl-(Calkyl)-O&#x2014;, heteroaryl-(Calkyl)-O&#x2014;, carbocyclyl-(Calkyl)-O&#x2014;, heterocyclyl-(Calkyl)-O&#x2014; or &#x2014;NR&#x2032;R&#x2033; wherein each R&#x2032; and R&#x2033; is the same or different and represents hydrogen, Calkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(Calkyl)-, heteroaryl-(Calkyl)-, carbocyclyl-(Calkyl)- or heterocyclyl-(Calkyl)-. 

Benzodiazepine derivatives and pharmaceutical compositions containing them

Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV. Formula (I) Wherein: &#x2014;Rrepresents Calkyl, aryl or heteroaryl; &#x2014;Rrepresents hydrogen or Calkyl; &#x2014;each Ris the same or different and represents halogen, hydroxy, Calkyl, Calkoxy, Calkylthio, Chaloalkyl, Chaloalkoxy, amino, mono(Calkyl)amino, di(Calkyl)amino, nitro, cyano, &#x2014;COR', &#x2014;CONR&#x2032;R&#x2033;, &#x2014;NH&#x2014;CO&#x2014;R&#x2032;, &#x2014;S(O)R&#x2032;, &#x2014;S(O)R&#x2032;, &#x2014;NH&#x2014;S(O)R&#x2032;, &#x2014;S(O)NR&#x2032;R&#x2033; or &#x2014;S(O)NR&#x2032;R&#x2033; wherein each R&#x2032; and R&#x2033; is the same or different and represents hydrogen or Calkyl; &#x2014;n is from 0 to 3; Rrepresents hydrogen or Calkyl; &#x2014;Rrepresents Calkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(Calkyl)-, heteroaryl-(Calkyl)-, carbocyclyl-(Calkyl)-, heterocyclyl-(Calkyl)-, aryl-C(O)&#x2014;C(O)&#x2014;, heteroaryl-C(O)&#x2014;C(O)&#x2014;, carbocyclyl-C(O)&#x2014;C(O)&#x2014;, heterocyclyl-C(O)&#x2014;C(O)&#x2014; or, &#x2014;XR; &#x2014;X represents &#x2014;CO&#x2014;, &#x2014;S(O)&#x2014; or &#x2014;S(O)&#x2014;; and &#x2014;Rrepresents Calkyl, hydroxy, Calkoxy, Calkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(Calkyl)-, heteroaryl-(Calkyl)-, carbocyclyl-(Calkyl)-, heterocyclyl-(Calkyl)-, aryl-(Chydroxyalkyl)-, heteroaryl-(Chydroxyalkyl)-, carbocyclyl-(Chydroxyalkyl)-, heterocyclyl-(Chydroxyalkyl)-, aryl-(Calkyl)-O&#x2014;, heteroaryl-(Calkyl)-O&#x2014;, carbocyclyl-(Calkyl)-O&#x2014;, heterocyclyl-(Calkyl)-O&#x2014; or &#x2014;NR&#x2032;R&#x2033; wherein each R&#x2032; and R&#x2033; is the same or different and represents hydrogen, Calkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(Calkyl)-, heteroaryl-(Calkyl)-, carbocyclyl-(Calkyl)- or heterocyclyl-(Calkyl)-. 

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London, United Kingdom

Elisa Henderson