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US 2013/0252935 A1Published application
Monobactams
AssigneePfizer Inc.
InventorsMatthew F. Brown, Mark J. Mitton-Fry, Seungil Han, Manjinder Lall, Mark Plummer, Hud Lawrence Risley, Veerabahu Shanmugasundaram, Jeremy Starr
Life of this patent
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Abstract
The present invention is directed to a new class of monobactam derivatives and their use for treating bacterial infections.
Claims17
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein
- R1 and R2 are each independently hydrogen, optionally substituted (C1-C6)alkyl, or phenyl(C1-C6)alkyl wherein the phenyl and the (C1-C6)alkyl moieties of the phenyl(C1-C6)alkyl are optionally substituted;
- or
- R1 and R2 together, with the carbon atom to which they are attached, form an optionally substituted (C3-C6)cycloalkyl or an optionally substituted 4-6-membered heterocycle;
- E is C(H), C(F), C(Cl), or N;
- X is —O—C(═O)—, —NH—C(═O)—, —NH—SO2—, —NH—C(═N—CN)—, —NH-T-, or triazole;
- L is absent, —(CH2)p—, —(CH2)p—NH—(CH2)q, —(CH2)p—O—(CH2)q—, —(CH2)p—C(═O)—NH—(CH2)q—, —(CH2)p—NH—C(═O)—(CH2)q—, —CH(CH3)—NH—C(═O)—(CH2)q—, —(CH2)p—NH—C(═O)—NH—(CH2)q—, —CH(CH3)—NH—C(═O)—NH—(CH2)q—, —(CH2)p-T-SO2—NH—(CH2)q—, —(CH2)p-T-(CH2)q, —(CH2)p-T-C(═O)—NH—(CH2)q—, —(CH2)p-T-(CH2)q—NH—C(═O)—, —NH—(CH2)p-T-, —O—(CH2)p-T-, —(CH2)p—Y—C(═O)—(CH2)q—, or —(CH2)p—Y—(CH2)q—;
- T is an optionally substituted phenyl or an optionally substituted 5- or 6-membered heteroaryl;
- Y is an optionally substituted 4-6 membered heterocycle;
- p and q are each independently 0, 1, 2, or 3;
- A is
- and
- R3 is hydrogen, (C1-C3)alkyl, or OH;
- provided that Formula (I) does not include 2-(((1-(2-aminothiazol-4-yl)-2-(((2S,3R)-2-((3-((1,5-dihydroxy-4-oxo-1,4-dihydropyridin-2-yl)methyl)ureido)methyl)-4-oxo-1-sulfoazetidin-3-yl)amino)-2-oxoethylidene)amino)oxy)-2-methylpropanoic acid.
12 more elements
A compound of Formula (IA):
- or a pharmaceutically acceptable salt thereof,
- wherein
- R1 and R2 are each independently hydrogen, optionally substituted (C1-C6)alkyl, or phenyl(C1-C6)alkyl wherein the phenyl and the (C1-C6)alkyl moieties of the phenyl(C1-C6)alkyl are optionally substituted;
- or
- R1 and R2 together, with the carbon atom to which they are attached, form an optionally substituted (C3-C6)cycloalkyl or an optionally substituted 4-6-membered heterocycle;
- E is C(H), C(F), C(Cl), or N;
- X is —O—C(═O)—, —NH—C(═O)—, —NH—SO2—, —NH—C(═N—CN)—, —NH-T-, or triazole;
- L is absent, —(CH2)p—, —(CH2)p—NH—(CH2)q—, —(CH2)p—O—(CH2)q, —(CH2)p—C(═O)—NH—(CH2)q—, —(CH2)p—NH—C(═O)—(CH2)q—, —CH(CH3)—NH—C(═O)—(CH2)q—, —(CH2)p—NH—C(═O)—NH—(CH2)q—, —CH(CH3)—NH—C(═O)—NH—(CH2)q—, —(CH2)p-T-SO2—NH—(CH2)q—, —(CH2)p-T-(CH2)q, —(CH2)p-T-C(═O)—NH—(CH2)q—, —(CH2)p-T-(CH2)q—NH—C(═O)—, —NH—(CH2)p-T-, —O—(CH2)p-T-, —(CH2)p—Y—C(═O)—(CH2)q—, or —(CH2)p—Y—(CH2)q—;
- T is an optionally substituted phenyl or an optionally substituted 5- or 6-membered heteroaryl;
- Y is an optionally substituted 4-6 membered heterocycle;
- p and q are each independently 0, 1, 2, or 3;
- A is
- and
- R3 is hydrogen, (C1-C3)alkyl, or OH.
11 more elements
A compound of formula
- or a pharmaceutically acceptable salt thereof.
A compound of formula
- or a pharmaceutically acceptable salt thereof.
A compound of formula
- or a pharmaceutically acceptable salt thereof.
(canceled)
Dependencies are inferred from the claim text.