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US 6,476,053 B1Granted
Mycobacterial inhibitors
AssigneeAstraZeneca AB
InventorsMeenakshi Balganesh, Kantharaj Ethirajulu, Babita Singh Ganguly, Ramachandran Janakiraman, Parvinder Kaur, Rangarao Kajipalya, Santosh Nandan, Ramanujulu Pondi Murugappan, Narayanan Ramamurthy, Balasubramanian Venkataraman
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Abstract
The invention provides the use of certain succinimide compounds in the treatment of mycobacterial diseases.
Claims7
A method of treating a patient suffering from, or at risk of, a mycobacterial disease, which comprises administering to the patient a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof,
- wherein x is 0 or 1;
- R1 represents a hydrogen atom, or a C1-C20 alkyl or myrtanyl group, or a phenyl or benzyl group optionally substituted in the aromatic ring by one or more substituents selected from amino, nitro, hydroxyl, carboxyl, halogen, trifluoromethyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxycarbonyl, piperidyl, piperazinyl and morpholinyl, or a group (CH2)yCONH—R5 where y is an integer from 1 to 6 and R5 represents a phenyl group optionally substituted by one or more substituents selected from amino, nitro, hydroxyl, carboxyl, halogen, trifluoromethyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxycarbonyl, piperidyl, piperazinyl and morpholinyl;
- and either
- R2 represents a hydrogen atom or a C1-C6 alkyl group, or R2 together with R3 represents a carbon-carbon single bond provided that x is 0, or R2 together with R4 represents a group ═CH2,
- R3 represents a hydrogen atom or is linked to R2 as defined above, and
- R4 represents a hydrogen atom or a C1-C6 alkyl group;
- or a C1-C10 alkylamino group optionally substituted by a di(C1-C6 alkyl)amino substituent group;
- or an anilino group substituted in the aromatic ring by one or more substituents selected from amino, nitro, hydroxyl, carboxyl, trifluoromethyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxycarbonyl, piperidyl, piperazinyl and morpholinyl;
- or a group —SCH2CH2OH, —SCH2CH2NH2, —SCH2CH2(NH2) CO2H or —SCH2CH2NHCO—R6 where R6 represents a C1-C10 alkyl or C3-C6 cycloalkyl group, or a phenyl group optionally substituted by one or more substituents selected from amino, nitro, hydroxyl, carboxyl, halogen, trifluoromethyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkoxycarbonyl, piperidyl, piperazinyl and morpholinyl;
- or R4 is linked to R2 as defined above;
- or
- R2, R3 and R4 together represent a phenyl group;
- with the provisos that;
- (i) R1, R2, R3 and R4 do not each simultaneously represent a hydrogen atom, and
- (ii) when x is 0, R1 represents a 4-fluorophenyl group and R4 represents a hydrogen atom, then R2 and R3 do not together represent a carbon-carbon single bond.
12 more elements
Dependencies are inferred from the claim text.