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US 7,605,169 B2Granted
Antibacterial agents
AssigneeGlaxo Group Limited
InventorsWilliam Henry Miller, Mark Andrew Seefeld
Life of this patent
Estimating the term…
Abstract
Napthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans, are disclosed.
Claims21
A compound of formula (I)
- or a pharmaceutically acceptable salt thereof, wherein:
- Z1, Z3, and Z4 are independently N or CR1a;
- Z2, Z5, and Z6 are each CR1a;
- R1 and R1a are independently at each occurrence hydrogen;
- cyano;
- halogen;
- hydroxy;
- (C1-6)alkoxy unsubstituted or substituted by (C1-6)alkoxy, hydroxy, amino, piperidyl, guanidino or amidino any of which is unsubstituted or N-substituted by one or two (C1-6)alkyl, acyl, (C1-6)alkylsulphonyl, CONH2, hydroxy, (C1-6)alkylthio, heterocyclylthio, heterocyclyloxy, arylthio, aryloxy, acylthio, acyloxy or (C1-6)alkylsulphonyloxy;
- (C1-6)alkyl;
- (C1-6)alkylthio;
- trifluoromethyl;
- trifluoromethoxy;
- nitro;
- azido;
- acyl;
- acyloxy;
- acylthio;
- (C1-6)alkylsulphonyl;
- (C1-6) alkylsulphoxide;
- arylsulphonyl;
- arylsulphoxide;
- or an amino, piperidyl, guanidino or amidino group unsubstituted or N-substituted by one or two (C1-6)alkyl, acyl or (C1-6)alkylsulphonyl groups;
- or R1 and R1a of Z2 together form ethylenedioxy;
- W1, W2, and W3 are each CR3R4;
- B is CR6R7 or C═O;
- R3, R4, R6, and R7 are independently at each occurrence hydrogen;
- thiol;
- (C1-6)alkylthio;
- halogen;
- trifluoromethyl;
- azido;
- (C1-6)alkyl;
- (C2-6)alkenyl;
- (C1-6)alkoxycarbonyl;
- (C1-6)alkylcarbonyl;
- (C2-6)alkenylcarbonyl;
- (C2-6)alkenyloxycarbonyl;
- aralkyl;
- aryl;
- heterocyclyl;
- heterocyclylalkyl;
- hydroxy;
- NR1bR1b;
- (C1-6)alkylsulphonyl;
- (C2-6)alkenylsulphonyl;
- or (C1-6)aminosulphonyl wherein the amino group is optionally and independently substituted by hydrogen, (C1-6)alkyl, (C2-6)alkenyl or aralkyl;
- R5 is hydrogen;
- halogen;
- hydroxyl;
- or (C1-6)alkyl;
- R2 and R8 are independently hydrogen;
- trifluoromethyl;
- (C1-6)alkyl;
- (C2-6)alkenyl;
- (C1-6)alkoxycarbonyl;
- (C1-6)alkylcarbonyl;
- (C2-6)alkenyloxycarbonyl;
- aryl;
- aralkyl;
- (C3-8)cycloalkyl;
- heterocyclyl;
- or heterocyclylalkyl;
- R1b and R1b are independently at each occurrence hydrogen;
- (C1-6)alkyl;
- aralkyl;
- aryl;
- heterocyclyl;
- heterocyclylalkyl;
- or together with the nitrogen to which they are attached form an aziridine, azetidine, pyrrolidine, piperidine or hexamethyleneimine ring (wherein said aziridine, azetidine, pyrrolidine, piperidine or hexamethyleneimine ring are optionally substituted with from 1 to 3 substituents selected from halogen;
- hydroxy;
- cyano;
- nitro;
- (C1-6)alkyl;
- and aryl);
- R9 is UR10,
- U is OH2;
- C(═O);
- or SO2;
- R10 is a group:
- R11, R13 and R14 are at each occurrence independently selected from:
- H;
- (C1-4)alkylthio;
- halo;
- (C1-4)alkyl;
- (C2-4)alkenyl;
- hydroxy;
- hydroxy(C1-4)alkyl;
- mercapto(C1-4)alkyl;
- (C1-4)alkoxy;
- trifluoromethoxy;
- nitro;
- cyano;
- carboxy;
- amino;
- and aminocarbonyl:
- wherein said amino and amino carbonyl may be unsubstituted or substituted by (C1-4)alkyl;
- and “acyl” is a C(═O)(C1-13)alkyl or a C(═O)aryl radical, in which aryl is optionally substituted phenyl or naphthyl.
94 more elements
Dependencies are inferred from the claim text.