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US 6,617,315 B1Granted
Therapeutic compounds
OwnerStanley Dawes Chamberlain, George Walter Koszalka +2inventors
InventorsStanley Dawes Chamberlain, George Walter Koszalka, Jeffrey H. Tidwell, Nanine Agneta Vandraanen
Life of this patent
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Abstract
The present invention relates to benzimidazole derivatives and their use in medical therapy particularly for the treatment or prophylaxis of restenosis.
Claims5
A method for the treatment of restenosis in a mammal said method comprising administering a therapeutically effective amount of a compound of formula (I):
- wherein
- R1 represents hydrogen, a halo atom, azido,
- —NR8R9 where R8 and R9 are the same or different and are each independently selected from the group consisting of hydrogen, hydroxyl, C1-12 alkyl where the alkyl moiety is optionally substituted by one or more substituents selected from the group consisting of halo, amino, azido, hydroxy, cyano, NO2, NHR10, SO2R10, SR10, OR10, COR10 and haloC1-8 alkyl where R10 is C1-6 alkyl, C3-6 alkenyl, C2-6 alkynyl, or aryl, C2-8 alkenyl, C1-6 alkoxy, C3-7 cycloalkyl, C2-8 alkynyl, C3-7 cycloalkenyl, C3-7 cycloalkylC1-5 alkyl, aryl, arylC1-6 alkyl, heteroaryl, heteroarylC1-6 alkyl, heterocyclyl and heterocyclylC1-6 alkyl or R8R9 together with the N atom to which they are attached form a 3,4,5 or 6 membered heterocyclic ring;
- —NHNR11R12 where R11 and R12 are the same or different and each represent hydrogen or C1-6 alkyl;
- —N═NC1-6 alkyl or —NHOC1-6 alkyl;
- R2 represents hydrogen, halo atom, C1-6 alkyl or C2-6 alkenyl;
- R3 and R4 are the same or different and each represent hydrogen, halogen or NO2;
- wherein the sugar moiety of Formula I is selected from the group consisting of:
- with the proviso that when R2 represents hydrogen, R3 and R4 each represent chloro, and the sugar moiety is
- then R1 represents:
- azido,
- —NR8R9 where R8 and R9 are the same or different and are each independently selected from the group consisting of hydroxyl, C1-6 alkyl, where the alkyl moiety is substituted by one or more substituents selected from the group consisting of amino, azido, NO2, NHR10, SO2R10, SO2R10, OR10, haloC1-6 alkyl where R10 is as hereinbefore defined, C7-12 alkyl, where the alkyl moiety is optionally substituted by one or more substituents selected from the group consisting of halo, amino, azido, hydroxy, cyano, NO2, NHR10, SO2R10, SR10, OR10, COR10 and haloC1-6 alkyl where R10 is as herein before defined, C1-6 alkoxy, C3-7 cycloalkenyl, heteroaryl, heteroaryl C1-6 alkyl and heterocyclyl;
- —NHNR11R12 where R11 and R12 are as hereinbefore defined;
- —N═NC1-6 alkyl or
- —NHOC1-6 alkyl;
- or a pharmaceutically acceptable derivative thereof.
13 more elements
A method for the treatment of restenosis following angloplasty in a mammal, said method comprising administering a therapeutically effective amount of a compound of formula (I):
- wherein
- R1 represents hydrogen, a halo atom, azido,
- —NR8R9 where R8 and R9 are the same or different and are each independently selected from the group consisting of hydrogen, hydroxyl, C1-2 alkyl where the alkyl moiety is optionally substituted by one or more substituents selected from the group consisting of halo, amino, azido, hydroxy, cyano, NO2, NHR10, SO2R10, SR2O10, OR10, COR10 and haloC1-6 alkyl where R10 is C1-6 alkyl, C3-5 alkenyl, C2-6 alkynyl, or aryl, C2-8 alkenyl, C1-6 alkoxy, C3-7 cycloalkyl, C2-8 alkynyl, C3-7 cycloalkenyl, C3-7 cycloalkylC1-6 alkyl, aryl, arylC1-6 alkyl, heteroaryl, heterocarylC1-6 alkyl, heterocyclyl and heterocyclylC1-6 alkyl or R8R9 together with the N atom to which they are attached form a 3,4,5 or 6 membered heterocyclic ring;
- —NHNR11R12 where R11 and R12 are the same or different and each represent hydrogen or C1-6 alkyl;
- —N═NC1-6 alkyl or —NHOC1-6 alkyl;
- R2 represents hydrogen, halo atom, C1-6 alkyl or C2-6 alkenyl;
- R3 and R4 are the same or different and each represent hydrogen, halogen or NO2;
- wherein the sugar moiety of Formula I is selected from the group consisting of:
- with the proviso that when R2 represents hydrogen, R3 and R4 each represent chloro, and the sugar moiety is
- then R1 represents:
- azido,
- —NR8R9 where R8 and R9 are the same or different and are each independently selected from the group consisting of hydroxyl, C1-6 alkyl, where the alkyl moiety is substituted by one or more substituents selected from the group consisting of amino, azido, NO2, NHR10, SO2R10, SR10, OR10, haloC1-6 alkyl where R10 is as hereinbefore defined, C7-12 alkyl, where the alkyl moiety is optionally substituted by one or more substituents selected from the group consisting of halo, amino, azido, hydroxy, cyano, NO2, NHR10, SO2R10, SR10, OR10, COR10 and haloC1-6 alkyl where R10 is as hereinbefore defined, C1-6 alkoxy, C3-7 cycloalkenyl, heteroaryl, heteroaryl C1-6 alkyl and heterocyclyl;
- —NHNR11R12 where R11 and R12 are as hereinbefore defined;
- —N═NC1-6 alkyl or
- —NHOC1-6 alkyl;
- or a pharmaceutically acceptable derivative thereof.
13 more elements
Dependencies are inferred from the claim text.