Pharmaceutical compounds

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United States of America Patent

PATENT NO 7132419
APP PUB NO 20050143383A1
SERIAL NO

11024759

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) ##STR00001## wherein each of R.sup.1 to R.sup.4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C.sub.1 C.sub.6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C.sub.1 C.sub.6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO.sub.2R.sup.10, CON(R.sup.12).sub.2, OCON(R.sup.12), SR.sup.10, SOR.sup.11, SO.sub.2R.sup.11, SO.sub.2N(R.sup.12).sub.2, N(R.sup.12).sub.2, NR.sup.10SO.sub.2R.sup.11, N(SO.sub.2R.sub.11).sub.2 NR.sup.10(CH.sub.2).sub.nCN, NR.sup.10COR.sup.11, OCOR.sup.11 or COR.sup.10; each of R.sup.5 to R.sup.7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C.sub.1 C.sub.6 alkoxy, C.sub.1 C.sub.6 alkyl, SR.sup.10 and N(R.sup.12).sub.2; Q is C.sub.1 C.sub.6 alkylene which is unsubstituted or substituted by (i) C.sub.1 C.sub.6 alkyl which is unsubstituted or substituted, (ii) hydroxy, provided that the hydroxy group is not .alpha. to either of the N atoms adjacent to Q in formula (I), (iii) CO.sub.2R.sup.10, or (iv) CON(R.sup.12); R.sup.8 and R.sup.9, which are the same or different, are each hydrogen or C.sub.1 C.sub.6 alkyl, or R.sup.8 and R.sup.9 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered N-containing heterocyclic ring which may include one additional heteroatom selected from O, N and S, or one of R.sup.8 and R.sup.9 is an alkylene chain optionally interrupted by O, N or S, which is attached to a carbon atom on the alkylene chain represented by Q to complete a saturated 5- or 6-membered N-containing heterocyclic ring as defined above; R.sup.10 is hydrogen, C.sub.1 C.sub.6 alkyl, C.sub.3 C.sub.6 cycloalkyl, benzyl or phenyl; R.sup.11 is C.sub.1 C.sub.6 alkyl, C.sub.3 C.sub.6 cycloalkyl, benzyl or phenyl; each R.sup.12, which are the same or different, is hydrogen, C.sub.1 C.sub.6 alkyl cycloalkyl, benzyl or phenyl, or the two R.sup.12 groups form, together with the nitrogen atom to which they are attached a 5- or 6-membered saturated N-containing heterocyclic ring which may include 1 or 2 additional heteroatoms selected from O, N and S; and n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof; with the proviso that at least one of R.sup.1 to R.sup.4 is other than hydrogen.These compounds are inhibitors of topoisomerase I and/or topoisomerase II and can be used to treat tumours, including tumours which express MDR.

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Patent Owner(s)

  • XENOVA LIMITED

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Denny, William Alexander Auckland, NZ 66 1257
Folkes, Adrian Slough, GB 34 911
Milton, John Slough, GB 71 3846
Vicker, Nigel Slough, GB 22 104
Wang, Shouming Slough, GB 11 21

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