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US 2002/0055472 A1Published application
Macrolide antiinfective agents
AssigneeKosan Biosciences, Inc.
InventorDaniel T.W. Chu
Life of this patent
Estimating the term…
Abstract
The invention is directed towards antibacterial compounds. The invention concerns macrolide antibiotics useful as antiinfective agents.
Claims22
A compound of the formula
- 45
- wherein
- Ra is substituted or unsubstituted alkyl (1-10C);
- substituted or unsubstituted alkenyl (2-10C);
- substituted or unsubstituted alkynyl (2-10C);
- substituted or unsubstituted aryl (3-20C);
- substituted or unsubstituted arylalkyl (4-20C);
- or ORa is replaced by H;
- Rb is H or halogen;
- Rc is H or a protecting group;
- Rd is methyl, unsubstituted alkyl (3-10C);
- substituted alkyl (1-10C);
- substituted or unsubstituted alkenyl (2-10C);
- substituted or unsubstituted alkynyl (2-10C);
- substituted or unsubstituted aryl (3-20C);
- or substituted or unsubstituted arylalkyl (4-20C);
- substituted or unsubstituted arylalkenyl (5-20C);
- substituted or unsubstituted arylalkynyl (5-20C);
- substituted or unsubstituted amidoarylalkyl (5-20C);
- substituted or unsubstituted amidoarylalkenyl (5-20C);
- or substituted or unsubstituted amidoarylalkynyl (5-20C)
- Re is H or a protecting group;
- each of A, B, D and E is independently H, substituted or unsubstituted alkyl (1-10C) wherein any pair of said A, B, D and E forms a 3-7-membered ring optionally containing one or more heteroatoms, with the proviso that at least two of said A, B, D and E must be hydrogen;
- including any pharmaceutically acceptable salts thereof and any stereoisomeric forms and mixtures of stereoisomeric forms thereof.
21 more elements
A compound of the formula
- 46
- wherein
- Ra is substituted or unsubstituted alkyl (1-10C);
- substituted or unsubstituted alkenyl (2-10C);
- substituted or unsubstituted alkynyl (2-10C);
- substituted or unsubstituted aryl;
- substituted or unsubstituted arylalkyl;
- or ORa is replaced by H;
- Rb is H or halogen;
- Rc is H or a protecting group;
- Rd′ is H, substituted or unsubstituted alkyl (1-10C);
- substituted or unsubstituted alkenyl (2-10C);
- substituted or unsubstituted alkynyl (2-10C);
- substituted or unsubstituted aryl (3-10C);
- substituted or unsubstituted arylalkyl (4-10C);
- substituted or unsubstituted arylalkynyl (5-20C);
- substituted or unsubstituted amidoarylalkyl (5-20C);
- substituted or unsubstituted amidoarylalkenyl (5-20C);
- or substituted or unsubstituted amidoarylalkynyl (5-20C);
- Re is H or a protecting group;
- L is methylene or carbonyl;
- T is —O—, —N(R)—, or —N(OR)—, —N(NHCOR)—, —N(N═CHR)—, or —N(NHR)— wherein R is H or Ra as defined above, with the proviso that when L is methylene, T is —O—;
- one of Z and Y is H and the other is OH, protected OH, or amino, mono- or dialkylamino, protected amino, or an amino heterocycle or
- Z and Y together are ═O, ═NOH or a derivatized oxime;
- including any pharmaceutically acceptable salts thereof and any stereoisomeric forms and mixtures of stereoisomeric forms thereof.
22 more elements
The compound of claim 18 wherein Ra is methyl.
Dependencies are inferred from the claim text.