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US 8,796,456 B2Granted
Naphthalene diimide compounds
AssigneeUniversity College London
InventorsMekala Gunaratnam, Francisco Cuenca, Stephen Neidle
Life of this patent
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Abstract
The invention relates to novel compounds which are naphthalene diimides of general formula (I). The compounds are used in therapy, particularly in cancer treatment.
Claims30
A pharmaceutical composition comprising a compound that is of general formula (I) or is a salt, solvate, or prodrug thereof,
- wherein R1 and R2 are each independently divalent radicals selected from C1-20 alkyl, C2-20 alkenyl, C7-20 alkaryl, C2-10 alkynyl, C7-20 aralkyl, C2-20 heteroaralkyl, C3-30 heterocyclylalkyl, C3-30 alkylheterocyclyl, C3-20 cycloalkyl, C3-20 heterocyclyl, C2-20 heteroaryl, C5-20 aryl and C1-10 alkoxy;
- R is H or A2X4;
- wherein X1-X4 are each independently selected from halo, OH, OR3, COH, NH2, NHR3, NR3R4, COOH, CONH2, COOR3, CONHR3, CONR3R4, SH, SR3, COR3 and cyano, provided that at least one of groups X1-X4 is a tertiary amine;
- wherein R3 and R4 are independently selected from C1-6 alkyl, C6-20 aryl, and C7-20 aralkyl or R3 and R4 together with the nitrogen atom to which they are attached form a 3-8 membered ring, which is optionally substituted and optionally comprises other hetero atoms;
- A1 and A2 are each independently selected from NHR5;
- wherein R5 is a divalent radical selected from C1-20 alkyl, C6-20 aryl, C7-20 alkaryl and C7-20 aralkyl;
- wherein any of the groups R1-R5, A1 and A2 may be substituted with C1-20 alkyl, C2-20 alkenyl, C7-20 alkaryl, C2-10 alkynyl, C7-20 aralkyl, C2-20 heteroaralkyl, C3-30 heterocyclylalkyl, C3-30 alkylheterocyclyl, C3-20 cycloalkyl, C3-20 heterocyclyl, C2-20 heteroaryl, C5-20 aryl or C1-10 alkoxy, halo, OH, OR3, COH, NH2, NHR3, NR3R4, COOH, CONH2, COOR3, CONHR3, CONR3R4, SH, SR3, COR3 or cyano;
- and
- wherein the pharmaceutical composition also comprises a pharmaceutically acceptable carrier.
6 more elements
A compound that is of general formula (I) or is a salt, solvate, or prodrug thereof
- wherein R1 and R2 are each independently divalent radicals selected from C1-20 alkyl, C2-20 alkenyl, C7-20 alkaryl, C2-10 alkynyl, C7-20 aralkyl, C2-20 heteroaralkyl, C3-30 heterocyclylalkyl, C3-30 alkylheterocyclyl, C3-20 cycloalkyl, C3-20 heterocyclyl, C2-20 heteroaryl, C5-20 aryl and C1-10 alkoxy;
- R is H or A2X4;
- wherein X1-X4 are each independently selected from halo, OH, OR3, COH, NH2, NHR3, NR3R4, COOH, CONH2, COOR3, CONHR3, CONR3R4, SH, SR3, COR3 and cyano, provided that at least one of groups X1-X4 is a tertiary amine;
- wherein R3 and R4 are independently selected from C1-6 alkyl, C6-20 aryl, and C7-20 aralkyl or R3 and R4 together with the nitrogen atom to which they are attached form a 3-8 membered ring, which is optionally substituted and optionally comprises other hetero atoms;
- A1 and A2 are each independently selected from NHR5;
- wherein R5 is a divalent radical seleced from C1-20 alkyl, C6-20 aryl, C7-20 alkaryl and C7-20 aralkyl;
- wherein any of the groups R1-R5, Al and A2 may be substituted with C1-20 alkyl, C2-20 alkenyl, C7-20 alkaryl, C2-10 alkynyl, C7-20 aralkyl, C2-20 heteroaralkyl, C3-30 heterocyclylalkyl, C3-30 alkylheterocyclyl, C3-20 cycloalkyl, C3-20 heterocyclyl, C2-20 heteroaryl, C5-20 aryl or C1-10 alkoxy, halo, OH, OR3, COH, NH2, NHR3, NR3R4, COOH, CONH2, COOR3, CONHR3, CONR3R4, SH, SR3, COR3 or cyano.
4 more elements
Dependencies are inferred from the claim text.