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US 2010/0075929 A1Published application
9-aminoacyl tetracycline compounds and methods of use thereof
AssigneeParatek Pharmaceuticals, Inc.
InventorsCarmen García-Luzón, Juan Carlos Cuevas, Jose M. Fiandor, Araceli Mallo, Mark L. Nelson, Roger Frechette
Life of this patent
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Abstract
A compound of formula (I):
Claims18
A compound of formula (I):
- wherein:
- R represents hydrogen or NRaRb;
- R1 represents hydrogen or C1-6alkyl;
- R2 represents hydrogen or hydroxy;
- R3 represents hydrogen;
- R4 represents hydrogen;
- R5 represents hydrogen, C1-6alkyl or C1-6alkoxycarbonyl;
- X represents NRxRy or —OC1-6alkyl optionally substituted by one or more groups selected from hydroxyl, methoxy, halogen, amino and trifluoromethyl;
- Ra and Rb independently represent hydrogen or C1-6alkyl;
- and
- Rx and Ry independently represent hydrogen, benzyl, C3-6cycloalkyl, C3-6alkenyl, C3-6alkynyl, C1-6alkyl optionally substituted by one or more groups selected from hydroxy, methoxy, halogen, NRaRb and trifluoromethyl, —C1-6alkylcycloalkyl, —C1-6alkylheterocycle, C1-6alkylamino and C1-6alkylthio or together Rx and Ry form a heterocycle;
- or a pharmaceutically acceptable salt thereof.
9 more elements
A method for the treatment of a bacterial infection in a subject, which comprises administering to the subject an effective amount of a compound of formula (I):
- wherein:
- R represents hydrogen or NRaRb;
- R1 represents hydrogen or C1-6alkyl;
- R2 represents hydrogen or hydroxy;
- R3 represents hydrogen;
- R4 represents hydrogen;
- R5 represents hydrogen, C1-6alkyl or C1-6alkoxycarbonyl;
- X represents NRxRy or —OC1-6alkyl optionally substituted by one or more groups selected from hydroxyl, methoxy, halogen, amino and trifluoromethyl;
- Ra and Rb independently represent hydrogen or C1-6alkyl;
- and
- Rx and Ry independently represent hydrogen, benzyl, C3-6cycloalkyl, C3-6alkenyl, C3-6alkynyl, C1-6alkyl optionally substituted by one or more groups selected from hydroxy, methoxy, halogen, NRaRb and trifluoromethyl, —C1-6alkylcycloalkyl, —C1-6alkylheterocycle, C1-6alkylamino and C1-6alkylthio or together Rx and Ry form a heterocycle;
- or a pharmaceutically acceptable salt thereof.
9 more elements
A compound selected from the group consisting of:
- [4S-(4a,5,5a,6,12a)]-4-(Dimethylamino)-9-[1-(ethoxycarbonyl)ethyl]amino-1,4,4a,5,5a,6,11,12a-octahydro-3,5,10,12,12a-pentahydroxy-6-methyl-1,1′-dioxo-2-naphthacenecarboxamide, 4S-(4aα, 5α,5aα,6α,12aα)-4,7-(bis-dimethylamino)-9-[1-(ethoxycarbonyl)ethyl]amino-1,4,4a,5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,1′-dioxo-2-naphthacenecarboxamide and pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.