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US 2004/0176609 A1Published application
Oxazolidinones having a benzannulated 6- or 7-membered heterocycle
OwnerPaul D. Johnson, Paul Adrian Aristoff +2inventors
InventorsPaul D. Johnson, Paul Adrian Aristoff, Toni-Jo Poel, Lisa Marie Thomasco
Life of this patent
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Abstract
The present invention provides oxazolidinones having a benzannelated 6- or 7-membered heterocycle as antibacterial agents.
Claims40
A compound of formula I
- 69
- or a pharmaceutically acceptable salt thereof wherein
- Y is
- a) —NHC(═W)R1,
- b) —O-het, —S-het, or —NH-het;
- X is
- a) —O—,
- b) —S(═O)i—, or
- C) —S(═O)(═NR4)—;
- W is
- a) O, or
- b) S;
- R1 is
- a) H,
- b) C1-8alkyl,
- c) C3-6cycloalkyl,
- d) OC1-4 alkyl,
- e) SC1-4 alkyl,
- f) NH2,
- g) NHC1-6 alkyl, or
- h) N(C1-6 alkyl)2;
- R2 is
- a) H,
- b) halo, or
- c) C1-4 alkyl;
- R3 is
- a) H,
- b) C1-8alkyl,
- c) aryl,
- d) het,
- e) C(═W)R5,
- f) C(═O)OR6, or
- g) S(═O)iR7;
- R4 is
- a) H, or
- b) C1-8alkyl;
- R5 is
- a) H,
- b) aryl,
- c) het,
- d) NR8R9 ,or
- e) C1-8alkyl;
- R6 is
- a) C1-8alkyl,
- b) aryl, or
- c) het;
- R7 is
- a) aryl,
- b) het,
- c) NR8R9, or
- d) C1-8alkyl;
- R8 and R9 are independently
- a) H,
- b) C1-8alkyl, or
- c) aryl;
- wherein >G-E- is >N—C— and Q is a carbon atom, or >G-E is >C=C— and Q is a nitrogen atom;
- aryl is a phenyl radical or an ortho-fused bicyclic carbocyclic radical wherein at least one ring is aromatic;
- het is a C-linked five- (5) or six- (6) membered saturated or unsaturated heterocyclic ring having 1, 2, or 3 heteroatoms selected from the group consisting of oxygen, sulfur, and nitrogen, which is optionally fused to a benzene ring;
- at each occurrence, alkyl or cycloalkyl is optionally substituted with one or more OR8, halo, aryl, S(═O)iR7, C(═W)R8, OC(═O)C1-6alkyl, or NR8R9;
- at each occurrence, aryl is optionally substituted with one or more halo, OH, CF3, OC1-6alkyl, CN, C1-6 alkyl, S(═O)iR7, C(═W)R8, OC(═O)R8, NHC(═O)R8, or NR8R9;
- at each occurrence, het is optionally substituted with one or more halo, OH, CF3, OC1-6alkyl, CN, C1-6 alkyl, S(═O)iR7, C(═W)R8, OC(═O)R8, NHC(═O)R8, or NR8R9, oxo, or oxime;
- m is 0, 1, 2, 3, or 4;
- n is 0, 1, 2, 3, or 4;
- with the proviso that m and n taken together are 3 or 4;
- and
- i is 0, 1, or 2.
63 more elements
Dependencies are inferred from the claim text.