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US 2009/0275572 A1Published application
Fab i inhibitors
AssigneeAffinium Pharmaceuticals, Inc.
InventorsWilliam H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas, Walter E. Dewolf, JR., Dalia R. Jakas
Life of this patent
Estimating the term…
Abstract
Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.
Claims6
A composition comprising:
- a compound according to formula (I):
- wherein:
- R1 is H or C1-4alkyl;
- R2 is H, C1-4alkyl or C3-6cycloalkyl;
- R3 is
- R4 is H or C1-4alkyl;
- indicates that one of the two designated bonds is a double bond and the other is a single bond;
- R5 is CH2 when the bond to which it is attached is a double bond;
- or R5 is H or C1-4 alkyl when the bond to which it is attached is a single bond;
- R6 is H or C1-4alkyl;
- R7 is H, C1-6alkyl or —C0-6alkyl-Ar;
- Y is H, C1-4alkyl, N(R′)2, NHC(O)R′, NHCH2C(O)R′ or NHC(O)CH═CHR′;
- each X independently is H, C1-4alkyl, CH2OH, OR′, SR′, CN, N(R′)2, CH2N(R′)2, NO2, CF3, CO2R′, CON(R′)2, COR′, NR′C(O)R′, F, Cl, Br, I or —S(O)rCF3;
- W is S or O;
- Q is H or C1-4alkyl;
- M is CH2 or O;
- L is CH2 or C(O);
- E is O or NR′;
- each R′ independently is H, C1-6alkyl or —C0-6alkyl-Ar;
- and
- r is 0, 1 or 2;
- or a pharmaceutically acceptable salt thereof;
- and
- a pharmaceutically acceptable excipient.
21 more elements
3-7. (canceled)
9-19. (canceled)
A method of screening for an inhibitor of FabI or FabK which comprises:
- (i) providing a reaction mixture comprising FabI or FabK, crotonyl-ACP and NADPH or NADH;
- ii) contacting a candidate compound to said reaction mixture;
- and
- (iii) detecting inhibition of FabI or FabK.
1 more element
Dependencies are inferred from the claim text.