Back to results
US 6,645,981 B2Granted
Antimicrobial quinolones, their compositions and uses
AssigneeThe Procter & Gamble Company
InventorsBenoit Ledoussal, Xiufeng Eric Hu, Ji-In Kim Almstead, Jeffrey Lyle Gray
Life of this patent
Estimating the term…
Abstract
Compounds of the following formula: are effective antimicrobial agents.
Claims20
A compound having a structure according to Formula (I)
- wherein:
- (A)
- (1) A1 —is C(R8)—, where R8 is selected from hydrogen, halo, C1 to about C6 alkoxy, C1 to about C6 alkylthio, C1 to about C6 alkyl, C2 to about C6 alkene and alkyne;
- (2)
- (a) X is —C—, a is a double bond and b is a single bond;
- and
- (b) Y is —N(R1)—;
- (3) R1 is selected from C3 to about C6 cycloalkyl, C4 to about C6 heterocycloalkyl, C1 to about C6 alkyl, C2 to about C6 alkene, a 6-membered aryl and a 6-membered heteroaryl;
- (4) R2 is hydrogen;
- (5) R3 is selected from hydrogen and hydroxy;
- (6) R5 is selected from hydrogen, hydroxy, amino, halo, C1 to about C6 alkyl, C2 to about C6 alkene-and C1 to about C6 alkoxy;
- (7) R6 is selected from fluoro and chloro;
- (8) R7 is —Q—C(R11)(R11′)(R11″), where Q is selected from —S—, —O— and —C(R12)(R12′)—, where R12 and R12′ are each independently selected from hydrogen and fluoro;
- where R11, R11′ and R11″ are each independently selected from hydrogen, hydroxy and halo;
- and where R11 and R12 may also both be nil, such that a double bond is formed between the respective carbon atoms;
- (9) R9 and R9′ are each independently selected from hydrogen and C1 to about C15 alkyl, or R9 and R9′ join to form a heterocyclic ring containing the nitrogen atom to which they are bonded;
- and
- (10) R10 represents the moieties on the piperidine ring other than R7 and —NR9R9′, where each R10 is independently selected from hydrogen, C1 to about C6 alkyl and fluoro;
- or an optical isomer, diastereomer or enantiomer thereof;
- a pharmaceutically-acceptable salt, hydrate, or biohydrolyzable ester, amide or imide thereof.
17 more elements
A compound having a structure according to Formula (II)
- wherein:
- (A)
- (1) A1 is —C(R8)— where R8 is selected from hydrogen, halo, C1 to about C6 alkoxy, C1 to about C6 alkylthio, C1 to about C6 alkyl, C2 to about C6 alkene and C2 to about C6 alkyne;
- (2) R1 is selected from C3 to about C6 cycloalkyl, C4 to about C6 heterocycloalkyl, C1 to about C6 alkyl, C1 to about C6 alkene, a 6-membered aryl and a 6-membered heteroaryl;
- (5) R5 is selected from hydrogen, hydroxy, amino, halo, C1 to about C6 alkyl, C1 to about C6 alkene-and C1 to about C6 alkoxy;
- (6) R6 is selected from fluoro and chloro;
- and
- (7) R7 is —QC(R11)(R11′)(R1″), where Q is selected from —S—, —O—and —C(R12)(R12′)—, where R12 and R12′ are each independently selected from hydrogen and fluoro;
- where R11, R11′ and R11″ are each independently selected from hydrogen, hydroxy and halo;
- and where R11 and R12 may also both be nil, such that a double bond is formed between the respective carbon atoms;
- or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, hydrate, or biohydrolyzable ester, amide or imide thereof.
8 more elements
Dependencies are inferred from the claim text.