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US 2009/0156578 A1Published application
3-Heterocyclylacrylamide Compounds as Fab I Inhibitors and Antibacterial Agents
OwnerHenry Pauls, Judd M. Bermaninventors
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Abstract
In part, the present invention is directed towards compounds with FabI inhibiting properties. Such compounds may also inhibit other enzymes, including those similar to FabI either structurally or functionally, for example, Fab K. Kits and compositions that include the disclosed compounds are also provided. Methods of treating a subject with a bacterial illness is also disclosed.
Claims47
A compound of formula I:
- wherein, independently for each occurrence,
- A is a monocyclic ring of 4-7 atoms containing 0-2 heteroatoms, a bicyclic ring of 8-12 atoms containing 0-4 heteroatoms or a tricyclic ring of 8-12 atoms containing 0-6 heteroatoms wherein the rings are independently aliphatic, aromatic, heteroaryl or heterocyclic in nature, the heteroatoms are selected from N, S or O and the rings are optionally substituted with one or more groups selected from C1-4 alkyl, OR″, CN, OCF3, F, Cl, Br, I;
- wherein R″ is H, alkyl, aralkyl, or heteroaralkyl;
- R is
- wherein, independently for each occurrence,
- R1 is OH or —O(CH2)n—Ar;
- wherein,
- n is an integer from 1 to 6 inclusive, and
- Ar is aryl or heteroaryl;
- R2 is H or —C(O)R3;
- R3 is H, alkyl, or aryl;
- R4 is OH or N(R3)2;
- the two R5 taken together form a spirocyloalkane, a spiroaryl, or a spiroheterocycloalkane;
- R6 is H, OH, alkyl, or aryl;
- R7 is alkyl, aryl, cycloalkane, or heterocycloalkane;
- M is H or OH, or two M taken together form O or N(R3);
- provided that when R is
- R′ is (R)-Me;
- and
- pharmaceutically acceptable salts thereof.
17 more elements
Dependencies are inferred from the claim text.