Btg International Limited

Cancer Research Technology Limited

Ann Lesley Jackman

Vasilios Bavetsias

Vassilios Bavetsias

Lorraine Skelton

Gerrit Jansen

Vassilis Bavetsias

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, 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. 

Anti-cancer cyclopenta(g)quinazoline compounds

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&#x2014;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. 

Anti-cancer cyclopenta [g] quinazoline compounds

A cyclopenta[g]quinazoline derivative, containing an L-Glu-&#x3b3;-D-Glu dipeptide group, of formula (I): wherein Ris amino, Chydroxyalkyl, Cfluoroalkyl or methoxy-C-alkyl; Ris hydrogen, Calkyl, Calkenyl, Calkynyl, Chydroxyalkyl Chalogenoalkyl or Ccyanoalkyl; and Ar is 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, the compound (I) optionally being in the form of a pharmaceutically acceptable salt or ester; may be used for the treatment of rheumatoid arthritis or acute myeloid leukaemia.

Cyclopenta{G}quinazoline derivatives for the treatment of rheumatoid arthritis or acute myeloid leukaemia

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

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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 Ccyanalkyl, 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. 

Anti-cancer cyclopenta[G]quinazoline compounds

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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Horsham, United Kingdom

Ann Lesley Jackman