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US 2009/0264644 A1Published application
Novel Macrolide Compounds With Antibiotic and Antineoplastic Properties
AssigneeWeihe Pharma{grave over (c)}euticals Co. Ltd.
InventorsGenhui Chen, Bin Li, John M. Webster, Kaiji Hu, Jianxiong Li
Life of this patent
Estimating the term…
Abstract
The invention is drawn to novel macrolide compounds of formula I having antibiotic and antineoplastic activities, useful as medicaments and/or agrochemicals for microorganism infections, in particularly for infectious diseases involving drug-resistant Staphylococcus, and for treatment of human and animal cancers.
Claims18
A compound of formula I, or a salt thereof:
- wherein R1, R2, R3, and R4, are independently selected from the groups consisting of H, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl or aralkyl group, halo, nitro, CN, hydroxyl, amino, COR8, NR9R10, S(O)2NR9R10, S(O)nR9, n=0-2, OR11 and heterocyclic group.
- R5 and R6 are independently selected from the groups consisting of H, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl or aralkyl group, halo, nitro, CN, hydroxyl, amino, COR8, NR9R10,
- R7 is selected from the groups consisting of H, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl or aralkyl and heterocyclic group.
- R8 is selected from H, unsubstituted or substituted alkyl, cycloalkyl, aryl, or aralkyl;
- R9 and R10 are selected from H, unsubstituted or substituted alkyl, cycloalkyl, aryl or aralkyl;
- R11 is selected from H, unsubstituted or substituted alkyl, cycloalkyl, aryl, aralkyl or acyl.
- —(X-Z)- is a structure as following:
- R12, R13, R14 and R15 are independently selected from the groups consisting of H, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl or aralkyl halo, nitro, CN, hydroxyl, amino, COR8, NR9R10, S(O)2NR9R10, S(O)nR9, n=0-2, OR11, and heterocyclic group.
5 more elements
A pharmaceutical composition comprising:
- a compound of formula I, or a salt thereof
- wherein R1, R2, R3, and R4, are independently selected from the groups consisting of H, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl or aralkyl group, halo, nitro, CN, hydroxyl, amino, COR8, NR9R10, S(O)2NR9R10, S(O)nR9, n=0-2, OR11, and heterocyclic group.
- R5 and R6 are independently selected from the groups consisting of H, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl or aralkyl group, halo, nitro, CN, hydroxyl, amino, COR8, NR9R10,
- R7 is selected from the groups consisting of H, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl or aralkyl and heterocyclic group.
- R8 is selected from H, unsubstituted or substituted alkyl, cycloalkyl, aryl, or aralkyl;
- R9 and R10 are selected from H, unsubstituted or substituted alkyl, cycloalkyl, aryl or aralkyl;
- R11 is selected from H, unsubstituted or substituted alkyl, cycloalkyl, aryl, aralkyl or acyl.
- —(X-Z)- is a structure as following:
- R12, R13, R14 and R15 are independently selected from the groups consisting of H, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl or aralkyl halo, nitro, CN, hydroxyl, amino, COR8, NR9R10, S(O)2NR9R10, S(O)nR9, n=0-2, OR11, and heterocyclic group.
6 more elements
The use of a compound of formula I, or a salt thereof, in the preparation of a medication for treating a disorder comprising micro-organism infection and neoplastic diseases:
- wherein R1, R2, R3, and R4, are independently selected from the groups consisting of H, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl or aralkyl group, halo, nitro, CN, hydroxyl, amino, COR8, NR9, R10, S(O)2NR9R10, S(O)nR9, n=0-2, OR11, and heterocyclic group.
- R5 and R6 are independently selected from the groups consisting of H, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl or aralkyl group, halo, nitro, CN, hydroxyl, amino, COR8, NR9R10,
- R7 is selected from the groups consisting of H, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl or aralkyl and heterocyclic group.
- R8 is selected from H, unsubstituted or substituted alkyl, cycloalkyl, aryl, or aralkyl;
- R9 and R10 are selected from H, unsubstituted or substituted alkyl, cycloalkyl, aryl or aralkyl;
- R11 is selected from H, unsubstituted or substituted alkyl, cycloalkyl, aryl, aralkyl or acyl.
- —(X-Z)- is a structure as following:
- R12, R13, R14 and R15 are independently selected from the groups consisting of H, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl or aralkyl halo, nitro, CN, hydroxyl, amino, COR8, NR9R10, S(O)2NR9R10, S(O)nR9, n=0-2, OR11, and heterocyclic group.
5 more elements
Dependencies are inferred from the claim text.