초록

The present invention relates to indolopyrolocarbazole derivatives, to their use in methods of treatment or prophylaxis of at least one viral infection or cardiovascular diseases; and pharmaceutical formulations containing such derivatives.

대표청구항 ▼

A method of treatment of the symptoms or effects of a viral infection in an infected host which comprises administering to said host a therapeutically effective non-toxic amount of a compound of formula (I) [Figure] (I) wherein R1 represents: －H; －COR10, －COOR10 where R10 is C1-6alkyl, C3-7cycloalky

A method of treatment of the symptoms or effects of a viral infection in an infected host which comprises administering to said host a therapeutically effective non-toxic amount of a compound of formula (I) [Figure] (I) wherein R1 represents: －H; －COR10, －COOR10 where R10 is C1-6alkyl, C3-7cycloalkyl, aryl, arylalkyl, C1-6alkenyl, or H; －OR10 where R10 is as hereinbefore defined; －C1-8 alkyl, C1-8 alkenyl or C3-8 cycloalkyl where the alky, alkenyl or cycloalkyl moiety may be optionally substituted by one or more substituents selected from halogen, cyano, nitro, azido, C3-8cycloalkyl, －OR10, －SR10, －SOR10, －SO2R10, －NR11 R12 where R11 and R12, which may be the same or different, each represent H, －COR10 where R10 is as hereinbefore defined, C1-6 alkyl, C3-7 cycloalkyl, aryl, arylalkyl, tetrahydronaphthyl or indanyl or －R11R12 together with the N atom to which they are attached form a 3-,4-,5- or 6-membered heterocyclic ring in which from 1 to 3 of the carbon atoms may be replaced by heteroatoms independently selected from O, N and S, the ring being where possible, partially or completely unsaturated, [Figure] where T is NH or S, Z is NH, S or O and W is NR11R12 where R11 and R12 are each as defined above, non-aromatic heterocycle, －NH-non-aromatic-heterocycle and aryl, such heterocycle and aryl groups being optionally substituted by one or more substituents selected from －OR10, －NR11R12, －SR10, －SOR10, －SO2R10, －CO2R10, nitro, cyano, SCN, C C1-6 alkyl wherein one or more hydrogen atoms are optionally replaced by a halogen atom, C3-6 cycloalkyl, hydroxyC1-6alkyl, CONH2, halogen and methylenedioxy, where R10, R11 and R12 are each as defined above; －NR11R12 where R11 and R12 are each as defined above; -aryl optionally substituted by one or more substituents selected from OR10, －NR11R12, －SR10, －SOR10, －SO2R10, －CO2R10, nitro, cyano, SCN, C1-6 alkyl wherein one or more hydrogen atoms are optionally replaced by a halogen atom, C3-6cycloalkyl, hydroxy C1-6 alkyl, CONH2, halogen and methylenedioxy where R10, R11 and R12 are each as defined above; a cyclic group containing from 3 to 6 carbon atoms in which from 1 to 3 of said atoms may be replaced by heteroatoms independently selected from O, S and N; －NH-cyclic group containing from 3 to 6 carbon atoms in which from 1 to 3 of said atoms may be replaced by heteroatoms independently selected from O, S and N; R2 and R3, which may be the same or different, are each independently selected from: H; －COR10, －COOR10 where R10 is C1-6alkyl, C3-7 cycloalkyl, aryl, arylalkyl, C1-6 alkenyl, or H; －OR10 wherein R10 is as hereinbefore defined; －C1-8 alkyl, C1-8 alkenyl or C3-8 cycloalkyl where the alkyl, alkneyl or cycloalkyl moiety may be optionally substituted by one or more substituents selected from halogen, cyano, nitro, azido, C3-8 cycloalkyl, －OR10, －COR10, －CO2R10, －OCOR10, －SR10, －SOR10, －SO2R10, －CO2NR11R12, －NR11 R12 where R11 and R12, which may be the same or different, each represent H, －COR10 where R10 is as hereinbefore defined, C1-6alkyl, C3-7cycloalkyl, aryl, arylakyl, tetrahydronaphthyl or indanyl or －R11R12 together with the N atom to which they are attached from a 3-,4-,5- or 6-membered heterocyclic ring in which from 1 to 3 of the carbon atoms may be replaced by heteroatoms independently selected from O, N and S, the ring being where possible, partially or completely unsaturated; [Figure] where T is NH or S, Z is NH, S or O and W is NR11R12 where R11 and R12 are each as defined above, non-aromatic heterocycle, －NH-non-aromatic-heterocycle and aryl, such heterocycle and aryl groups being optionally substituted by one or more substituents selected from －OR10, －NR11R12, －SR10, －SOR10, －SO2R10, －CO2R10, nitro, cyano, SCN, C1-6 alkyl, wherein one or more hydrogen atoms are optionally replaced by a halogen atom, C3-6 cycloalkyl, hydroxy C1-6alkyl, CONH2, halogen and methylenedioxy, where R10,R11 and R12 are each as defined above; －NR11R12 where R11 and R12 are each as defined above; -aryl optionally substituted by one or more substituents selected from －OR10, －NR11 R12, SR10, －SOR10, －SO2R10, CO2R10, nitro, cyano, SCN, C1-6 alkyl, wherein one or more hydrogen atoms are optionally replaced by a halogen atom, C3-6cycloalkyl, hydroxy C1-6 alkyl, CONH2, halogen and methylenedioxy, where R10, R11, R12 are each as defined above; R6 and R7, which may be the same or different, each represent one or more ring substituents selected from: H; C1-6alkyl optionally substituted by one or more substituents independently selected from halogen －NR11R12, cyano, －OR10, azido, －SR10, －SOR10, SO2R10, wherein R10, R11, and R12 are as hereinbefore defined; cyano, nitro, halogen, methylenedioxy, －OR10, －SR10, －SOR10, －SO2R10, －NHSO2R10, －SO2NR11 R12, －CO2R10, CONR11R12, OCOR and －NR11 R12 where R10, R11 and R12 are as define above; or a salt, ester or physiologically functional derivative thereof or a solvate of any thereof.