C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 403/12 (2006.01) A61K 31/505 (2006.01) A61K 31/513 (2006.01) A61K 38/05 (2006.01) C07D 239/70 (2006.01) C07D 401/12 (2006.01) C07D 403/14 (2006.01) C07D 409/12 (2006.01) C07D 417/12 (2006.01) C07F 7/10 (2006.01) C07K 5/02 (2006.01) C07K 5/06 (2006.01)
Patent
CA 2187449
Cyclopentaquinazoline of formula (I), wherein R1 is hydrogen, amino, C1-4 alkyl, C1-4 alkoxy, C1-4 hydroxyalkyl or C1-4 fluoroalkyl; wherein R2 is hydrogen, C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl; Ar1 is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C1-4 alkyl and C1-4 alkoxy; and wherein R3 is a group of the formula: -A1-Ar2-A2-Y1, in which A1 is a bond between the .alpha.-carbon atom of the group -CONHCH(CO2H)- and Ar2 or is a C1-2 alkylene group; Ar2 is phenylene, tetrazoldiyl, tiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which in the case of phenylene may optionally bear one or two substituents on the ring selected from halogeno, nitro, C1-4 alkyl and C1-4 alkoxy; A2 is a C1-3 alkylene or C2-3 alkenylene group; and a pharmaceutically acceptable salt or ester thereof are of therapeutic value particularly in the treatment of cancer.
Cyclopentaquinazoline représenté par la formule (I), dans laquelle R?1¿ représente hydrogène, amino, alkyle C¿1-4?, alcoxy C¿1-4? , hydroxyalkyle C¿1-4? ou fluoroalkyle C¿1-4?; dans laquelle R?2¿ représente hydrogène, alkyle C¿1-4?, alcényle C¿3-4?, alcynyle C¿3-4?, hydroxyalkyle C¿2-4?, alogénoalkyle C¿2-4? ou cyanoalkyle C¿1-4?; Ar?1¿ représente phenylène, thiophénediyle, thiazolediyle, pyridinediyle ou pyrimidinediyle pouvant éventuellement porter un ou deux substituants sélectionés à partir de halogéno, hydroxy, amino, nitro, cyano, trifluorométhyle, alkyle C¿1-4? et alcoxy C¿1-4?; et dans laquelle R?3¿ représente un groupe de formule: -A?1¿-Ar?2¿-A?2¿-Y?1¿, dans laquelle A?1¿ représente une liaison entre l'atome de .alpha.-carbone du groupe -CONHCH(CO¿2?H) et un groupe alkylène C¿1-2?; Ar?2¿ représente phénylène, tétrazoldiyle, tiophénediyle, thiazolediyle, pyridinediyle ou pyrimidinediyle qui, dans le cas de phénylène, peut éventuellement porter un ou deux substituants sur le noyau sélectionnés à partir de halogéno, nitro, alkyle C¿1-4? et alcoxy C¿1-4?; A?2¿ représente un groupe alkylène C¿1-3? ou alkénylène C¿2-3?; ainsi qu'un de ses sels ou de ses esters présentant une valeur thérapeutique, en particulier, dans le traitement du cancer.
Bavetsias Vassilios
Boyle Francis Thomas
Hennequin Laurent Francois Andre
Marriott Jonathan Hugh
British Technology Group Limited
Btg International Limited
Fetherstonhaugh & Co.
Zeneca Limited
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