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ANTITUMOUR 1,5-DIAZAANTHRAQUINONESCM Patents

Compounds having formula (I) wherein R<3>, R<4>, R<7>, and R<8> are independently selected from the group consisting of hydrogen, lower alkyl, halogen, amine, mono(lower)alkylamine, di(lower)alkylamine, phenyl, or substituted phenyl possess antitumour activity and are new with the exception of the compound in which R<3>, R<4>, R<7>, R<8> are all hydrogen and the compound in which R<3> and R<7> are hydrogen, R<4> is chlorine, and R<8> is a 2-nitrophenyl group.

Datos clave

CategoríaInvención

Índice de la ficha

Updated at
05/11/2026
Numero publicacion
EP.1080090.A1
Fecha publicacion
07/03/2001
Anio publicacion
2001

En detalle

Reivindicaciones

1. A compound having the formula (I): <img class="EMIRef" id="452401486-ib0012" /> and the dihydro derivative of formula (12): <img class="EMIRef" id="452401486-ib0013" /> wherein R<3> , R<4> , R<7> and R<8> are independently selected from the group consisting of hydrogen, C<1-6> alkyl, halogen, amine, mono(C<1-6> )alkylamine, di(C<1-6> )alkylamine, or phenyl (which may be substituted with 1 to 4 substituents selected from C<1-6> alkyl, halogen, amine, mono (C<1-6> )alkylamine, di(C<1-6> )alkylamine, nitro, hydroxy, C<1-6> alkoxy, or trifluoromethyl); with the exception of the compounds in which: R<3> , R<4> , R<7> and R<8> are all hydrogen; R<3> and R<7> are hydrogen, R<4> is chlorine, and R<8> is a 2-nitrophenyl group; R<3> and R<7> are hydrogen, R<4> is amino, and R<8> is a 2-nitrophenyl group; R<3> , R<7> and R<8> are hydrogen and R<4> is chlorine; and R<4> , R<7> and R<8> are hydrogen and R<3> is methyl. 2. A compound according to claim 1, which is selected from a compound of formula (4): <img class="EMIRef" id="452401486-ib0014" /> formula (8), <img class="EMIRef" id="452401486-ib0015" /> formula (11), <img class="EMIRef" id="452401486-ib0016" /> formula (13), and <img class="EMIRef" id="452401486-ib0017" /> formula (14), <img class="EMIRef" id="452401486-ib0018" /> wherein R<3> , R<4> , R<7> and R<8> are as defined in claim 1. 3. A compound according to claim 1 or 2, wherein the substituent groups R<3> , R<4> , R<7> and R<8> are chosen from hydrogen, methyl, ethyl, chlorine, dimethylamine, and nitrophenyl. 4. A compound according to claim 1 which is selected from: 3,7-diethyl-1,5-diazaanthraquinone; 3,7-dimethyl-1,5-diazaanthraquinone; 4,8-dimethyl-1,5-diazaanthraquinone; 4,8-dimethyl-3,7-dimethyl-1,5-diazaanthraquinone; 8-chloro-3-methyl-1,5-diazaanthraquinone; 8-chloro-1-dimethylamino-4-methyl-1,4-dihydro-1,5-diazaanthraquinone; 4-chloro-8-methyl-1,5-diazaanthraquinone; and 4-dimethylamino-8-methyl-1,5-diazaanthraquinone. 5. A pharmaceutical composition which includes as active ingredient a compound of any one of claims 1 to 4, together with a pharmaceutical carrier. 6. A compound according to any one of claims 1 to 4 for use as a medicament. 7. The use of a compound according to any of claims 1 to 4 or a pharmaceutical composition according to claim 5 in the manufacture of a medicament for the treatment of tumours.

Etiquetas

Inventores
Jose Maria PerezPerez Jose MariaBlanco M del MarM. del Mar BlancoMenendez Jose CarlosJose Carlos MenendezGarcia-Gravalos DoloresDolores Garcia-GravalosJesus Angel de la FuenteFuente Jesus Angel de laMartin Jesus MJesus Mð MartinCarmen AvendanoAvendano CarmenBlanco Maria del MarMaria del Mar BlancoMartin Maria JesusMaria Jesus MartinMenendez, Jose CarlosDe la Fuente, Jesus AngelDe la Fuente Jesus AngelAvendano, CarmenGarcia Gravalos, DoloresGarcia Gravalos DoloresPerez, Jose MariaBlanco, Maria del MarMartin, Maria JesusDel Mar Blanco, M.Del Mar Blanco MMenendez Jose CMenendez, Jose C.Blanco, M. del MarDe la Fuente Jesus Angel InstiDel Mar Blanco MariaDel Mar Blanco,MariaGravalos Dolores GarciaGravalos, Dolores GarciaDela Fuente Jesus AngelDela Fuente, Jesus AngelMartin, Jesus MaMartin Jesus Ma
Solicitantes
Universidad Complutense de MadridRuffles, Graham Keith
Clasificacion ipc
A61K 31/ 4375 A IA61P 35/ 00 A IC07D 471/ 04 A I
Clasificacion cpc
4C065/AA044C065/BB094C065/CC094C065/DD024C065/EE024C065/HH024C065/JJ024C065/KK014C065/LL044C065/PP014C086/AA014C086/AA024C086/CB094C086/MA014C086/MA044C086/NA144C086/ZB26A61K31/4375A61P35/00C07D471/04C07D471/04&112Z514/290514/291514/292546/79546/81
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