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US 7,247,617 B2Granted
Sixteen-member macrolide antiinfective agents
AssigneeKosan Biosciences, Inc.
InventorsHong Fu, Leonard Katz, David C. Myles
Life of this patent
Estimating the term…
Abstract
Sixteen membered macrolide anti-infective agents having a structure according to formula I where R1, R2, R3, R4, R5, and R6 are as defined herein, and related compounds are disclosed.
Claims27
A compound having a structure according to formula I
- and the pharmaceutically acceptable salts thereof,
- wherein
- R2 is CHO or
- R3 is H, CH2OH,
- R4 is MeO or Me;
- R5 is H or Me;
- R6 is Me or Et;
- R7 is H or C1-C4 alkyl;
- R8 and R9 are independently H, (C1-C4)alkyl, CH2OH, or CH2O(C1-C4)alkyl, or R8 and R9 combine to form (CHR10)m;
- each R10 is independently H, OH, O(C1-C4)alkyl, or (C1-C4)alkyl;
- Ar is an unsubstituted or substituted aromatic moiety selected from the group consisting of phenyl,
- wherein a substituted aromatic moiety Ar has one to three substituents independently selected from the group consisting of halo, hydroxy, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, trifluoromethyl, cyano, nitro, C1-C3 alkylamino or dialkylamino, and C1-C3 alkoxy;
- and
- Ar1 is phenyl or phenyl substituted with one to three substituents independently selected from the group consisting of halo, hydroxy, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, trifluoromethyl, cyano, nitro, C1-C3 alkylamino or dialkylamino, and C1-C3 alkoxy;
- m is 1, 2, 3, or 4;
- and
- n is 0, 1, or 2;
- subject to
- a first proviso (I) that when (a) R1 is other than
- (b) R2 is CHO, and (c) R3is other than
- then Ar is other than unsubstituted or substituted phenyl;
- and
- a second proviso (II) that when (a) R1 is H and (b) R2 is CHO, then R3 is
20 more elements
A compound having a structure according to formula IIa, IIb, IIc, or IId:
- and the pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.