Btg International Limited

Vasilios Bavetsias

Ann Lesley Jackman

Cyclopenta[g]quinazolines of the formula (I):&#x2014; wherein:

[object Object]

Cyclopenta[g]quinazolines of the formula (I): wherein: A is a group OR or NRRwherein Rand Rare each independently hydrogen Calkyl, Calkenyl, Calkynyl, Chydroxyalkyl, Chalogenoalkyl or Ccyanoalkyl, or Rand Rtogether with the intermediate N form a five- or six-membered heterocyclic ring, p is an integer in the range 1 to 4, Ris hydrogen Calkyl, Calkenyl, Calkynyl, Chydroxyalkyl, Chalogenoalkyl or Ccyanoalkyl; Aris phenylene, thiophenediyl, amino, nitro, cyano, trifluoromethyl, Calkyl and Calkoxy, and Ris a group of one of the following formulae: -A-Ar-A-Y-A-CON(R)CH(Y)Y-A-X-Arand pharmaceutically acceptable salts or esters thereof are of therapeutic value particularly in the treatment of cancer. 

Anti-cancer cyclopenta[g]quinazoline compounds

Method for aiding regression and palliation of a solid tumor in a patient in need of such treatment, comprising administering to the patient an effective amount of a cyclopenta[g]quinazoline of the formula (I) as set forth in the specification, wherein A is hydrogen or a group OR or NRRwherein Rand Rare each independently hydrogen Calkyl, Calkenyl, Calkynyl, Chydroxyalkyl, Chalogenoalkyl or Ccyanoalkyl, or Rand Rtogether with the intermediate N form a five- or six-membered heterocyclic ring; p is an integer in the range 1 to 4; Ris hydrogen, Calkyl, Calkenyl, Calkynyl, Chydroxyalkyl, Chalogenoalkyl or Ccyanoalkyl; Aris phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, Calkyl and Calkoxy; and Ris a group the formula -A-CON(R)CH(Y)Y, and pharmaceutically acceptable salts or esters. 

Cyclopenta[g]quinazolines of the formula (I):&#x2014;wherein: A is a group OR or NRRwherein Rand Rare each independently hydrogen Calkyl, Calkenyl, Calkynyl, Chydroxyalkyl, Chalogenoalkyl or Ccyanoalkyl, or Rand Rtogether with the intermediate N form a five- or six-membered heterocyclic ring, p is an integer in the range 1 to 4, Ris hydrogen, Calkyl, Calkenyl, Calkynyl, Chydroxyalkyl, Chalogenoalkyl or Ccyanoalkyl; Aris phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, Calkyl and Calkoxy, and Ris a group of one of the following formulae: -A-Ar-A-Y-A-CON(R)CH(Y)Y-A-X&#x2014;Arand pharmaceutically acceptable salts or esters thereof are of therapeutic value particularly in the treatment of cancer 

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Sutton, United Kingdom

Vasilios Bavetsias