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US 7,351,691 B2Granted
Glycopeptide phosphonate derivatives
AssigneeTheravance, Inc.
InventorsMichael R. Leadbetter, Martin S. Linsell
Life of this patent
Estimating the term…
Abstract
Disclosed are glycopeptides that are substituted with one or more substituents each comprising one or more phosphono groups; and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
Claims15
A compound of formula II:
- or a pharmaceutically-acceptable salt thereof;
- wherein R3, R5 and R20 are selected from:
- R3
- R5
- R20
- (a)
- phosphono-
- H
- CH3(CH2)9NHCH2CH2—
- methylamino
- (b)
- phosphono-
- H
- CH3(CH2)9OCH2CH2—
- methylamino
- (c)
- phosphono-
- H
- CH3(CH2)9SCH2CH2—
- methylamino
- (d)
- phosphono-
- H
- CH3(CH2)12—
- methylamino
- (e)
- phosphono-
- H
- 4-(4-chlorophenyl)benzyl
- methylamino
- (f)
- phosphono-
- H
- 2-(4-(4-chlorophenyl)-
- methylamino
- benzylamino)ethyl
- (g)
- phosphono-
- H
- 4-(4′-chlorobiphenyl)butyl
- methylamino
- (h)
- phosphono-
- H
- 5-(4′-chlorobiphenyl)pentyl
- methylamino
- (i)
- 3-phosphono-
- H
- CH3(CH2)9SCH2CH2—
- propylamino
- (j)
- 2-hydroxy-2-
- H
- 4-(4-chlorophenyl)benzyl
- phosphono-
- ethylamino
- (k)
- OH
- (phosphonomethyl)-
- CH3(CH2)9NHCH2CH2—
- aminomethyl
- (l)
- OH
- (phosphonomethyl)-
- CH3(CH2)9SCH2CH2—
- aminomethyl
- (m)
- OH
- (phosphonomethyl)-
- CH3(CH2)9OCH2CH2—
- aminomethyl
- (n)
- OH
- (phosphonomethyl)-
- CH3(CH2)12—
- aminomethyl
- (o)
- OH
- (phosphonomethyl)-
- 4-(4-chlorophenyl)benzyl
- aminomethyl
- (p)
- OH
- (phosphonomethyl)-
- 2-(4-(4-chlorophenyl)-
- aminomethyl
- benzylamino)ethyl
- (q)
- OH
- (phosphonomethyl)-
- 4-(4′-chlorobiphenyl)butyl
- aminomethyl
- (r)
- OH
- (phosphonomethyl)-
- 5-(4′-chlorobiphenyl)pentyl
- aminomethyl
- (s)
- OH
- (phosphonomethyl)-
- 3-[4-(4-chlorobenzyloxy)-
- aminomethyl
- benzylthio]propyl
- (t)
- OH
- N-(2-hydroxy-2-
- CH3(CH2)9SCH2CH2—
- phosphonoethyl)-
- aminomethyl
- (u)
- OH
- N-(carboxymethyl)-
- CH3(CH2)9SCH2CH2—
- N-2-phosphono-
- methyl)aminomethyl
- (v)
- OH
- N,N-bis(phosphono-
- CH3(CH2)9NHCH2CH2—
- methyl)aminomethyl
- (w)
- OH
- 3-phosphonopropyl-
- CH3(CH2)9SCH2CH2—
- aminomethyl
- (x)
- OH
- 3-phosphonopropyl-
- 4-(4-chlorophenyl)benzyl
- aminomethyl
- (y)
- phosphono-
- —CH2—N—(N—
- CH3(CH2)9NHCH2CH2—;
- methylamino
- CH3—D-glucamine
- and
- (z)
- OH
- (phosphonomethyl)-
- —(CH2)3NH—SO2—4-(4-
- aminomethyl
- chlorophenyl)phenyl.
141 more elements
Dependencies are inferred from the claim text.