A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 38/05 (2006.01) A61P 19/00 (2006.01) A61P 35/02 (2006.01)
Patent
CA 2717954
A cyclopenta[g]quinazoline derivative, containing an L-Glu-y-D-Glu dipeptide group, of formula (I): wherein: R1 is amino, C1-4 alkyl, C1-4 hydroxyalkyl, C1-4 fluoroalkyl or methoxy-C1-4 - alkyl; R2 is hydrogen, C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl C2-4 halogenoalkyl or C1-4 cyanoalkyl; 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, C1-4 alkyl and C1-4 alkoxy 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.
L'invention porte sur un dérivé de cyclopenta[g]quinazoline, contenant un groupe dipeptidique L-Glu-?-D-Glu, de formule (I) : dans laquelle : R1 représente amino, alkyle en C1-4, hydroxyalkyle en C1-4, fluoroalkyle en C1-4 ou méthoxy-alkyle en C1-4 ; R2 représente hydrogène, alkyle en C1-4, alcényle en C3-4, alcynyle en C3-4, hydroxyalkyle en C2-4, halogénoalkyle en C2-4 ou cyanoalkyle en C1-4 ; et Ar représente phénylène, thiophènediyle, thiazolédiyle, pyridinediyle ou pyrimidinediyle, qui peut facultativement supporter un ou plusieurs substituants choisis parmi halogéno, hydroxy, amino, nitro, cyano, trifluorométhyle, alkyle en C1-4 et alcoxy en C1-4, le composé (I) se présentant facultativement sous la forme d'un sel ou dun ester pharmaceutiquement acceptable. Le dérivé proposé par l'invention peut être utilisé pour le traitement de la polyarthrite rhumatoïde ou de la leucémie myéloïde aiguë.
Jackman Ann
Jansen Gerrit
Btg International Limited
Fetherstonhaugh & Co.
LandOfFree
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