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US 9,428,478 B2Granted
Piperazine derivatives, compositions, and uses related thereto
AssigneeEmory University
InventorsThota Ganesh, Aiming Sun, Susane M. Smith, John David Lambeth
Life of this patent
Estimating the term…
Abstract
The disclosure relates to piperazine derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidase.
Claims4
A pharmaceutical composition comprising a compound of Formula IE,
- or pharmaceutically acceptable salt thereof, wherein;
- A is CR9;
- R9 is hydrogen, or alkyl;
- Y3 is methoxy, ethoxy, trifluoromethoxy, isopropoxy, or alkoxy;
- Y1, Y2, Y4 and Y5 are each, the same or different, hydrogen, alkyl, halogen, nitro, cyano, hydroxy, amino, mercapto, formyl, carboxy, carbamoyl, alkoxy, alkylthio, alkylamino, (alkyl)2amino, alkylsulfinyl, alkylsulfonyl, arylsulfonyl, carbocyclyl, or aryl;
- R3, R4, and R6 are each, the same or different, hydrogen, alkyl, halogen, nitro, cyano, hydroxy, amino, mercapto, formyl, carboxy, carbamoyl, alkoxy, alkylthio, alkylamino, (alkyl)2amino, alkylsulfinyl, alkylsulfonyl, arylsulfonyl, carbocyclyl, or aryl;
- R5 is alkylsulfonyl, alkoxycarbonyl, alkylcarbamoyl, alkanoyl, carboxy, or carbamoyl;
- X1 is hydrogen;
- X3, X4, X5, and X6 are each, the same or different, hydrogen, alkyl, halogen, nitro, cyano, hydroxy, amino, mercapto, formyl, carboxy, carbamoyl, alkoxy, alkylthio, alkylamino, (alkyl)2amino, alkylsulfinyl, alkylsulfonyl, arylsulfonyl, carbocyclyl, or aryl.
6 more elements
A pharmaceutical composition comprising a compound comprising Formula IIB,
- or pharmaceutically acceptable salt thereof, wherein;
- n is 1 or 2;
- R3, R4, R5, and R6 are each, the same or different, hydrogen, alkyl, halogen, nitro, cyano, hydroxy, amino, mercapto, formyl, carboxy, carbamoyl, alkoxy, alkylthio, alkylamino, (alkyl)2amino, alkylsulfinyl, alkylsulfonyl, arylsulfonyl, carbocyclyl, or aryl;
- R9 is amino, alkylamino, dialkylamino, piperidinyl, piperazinyl, or morpholinyl wherein R9 is optionally substituted with alkyl or dialkylamino;
- X1, X4, X5, and X6 are each, the same or different, hydrogen, alkyl, halogen, nitro, cyano, hydroxy, amino, mercapto, formyl, carboxy, carbamoyl, alkoxy, alkylthio, alkylamino, (alkyl)2amino, alkylsulfinyl, alkylsulfonyl, arylsulfonyl, carbocyclyl, or aryl;
- Y1, Y2, Y3, Y4, and Y5 are each, the same or different, hydrogen, alkyl, halogen, nitro, cyano, hydroxy, amino, mercapto, formyl, carboxy, carbamoyl, alkoxy, alkylthio, alkylamino, (alkyl)2amino, alkylsulfinyl, alkylsulfonyl, arylsulfonyl, carbocyclyl, or aryl.
3 more elements
A pharmaceutical composition comprising a compound selected from the group consisting of:
- (3-(((2-(diethylamino)ethyl)amino)methyl)-5-fluoro-1H-indol-2-yl)(4-(4-methoxyphenyl)piperazin-1-yl)methanone;
- (5-fluoro-3-(morpholinomethyl)-1H-indol-2-yl)(4-(4-methoxyphenyl)piperazin-1-yl)methanone;
- (5-fluoro-3-(((1-methylpiperidin-4-yl)amino)methyl)-1H-indol-2-yl)(4-(4-methoxyphenyl)piperazin-1-yl)methanone;
- (3-((4-ethylpiperazin-1-yl)methyl)-5-fluoro-1H-indol-2-yl)(4-(4-methoxyphenyl)piperazin-1-yl)methanone;
- and
- (3-((diethylamino)methyl)-5-fluoro-1H-indol-2-yl)(4-(4-methoxyphenyl)piperazin-1-yl)methanone
- or salts thereof.
4 more elements
Dependencies are inferred from the claim text.