Aminoglycoside antibiotics
View Patent ↗This invention relates to novel aminoglycoside antibiotics, which have potent antimicrobial activity against bacteria, which induce infectious diseases, particularly MRSA, and has no significant nephrotoxicity, and process for producing them. More particularly, the present invention relates to compounds represented by formula (Ia) or their pharmacologically acceptable salts or solvates, or their diastereomer mixtures, antimicrobial agents comprising them, and a process for producing them.
1. A compound represented by formula (Ia) or its pharmacologically acceptable salt or solvate, or their diastereomer mixture with respect to the carbon atom attached with *:
wherein
R 5ax and R 5eq , which are different from each other, represent a hydrogen atom or hydroxyl,
R 4″ax and R 4″eq , which are different from each other, represent a hydrogen atom or hydroxyl,
n is an integer of 1 to 4, and
the steric configuration of carbon atom attached with * represents R or S.
2. The compound according to claim 1 or its pharmacologically acceptable salt or solvate, or their diastereomer mixture with respect to the carbon atom attached with *, wherein
R 5ax represents a hydrogen atom and
R 5eq represents hydroxyl.
3. The compound according to claim 1 or its pharmacologically acceptable salt or solvate, or their diastereomer mixture with respect to the carbon atom attached with *, wherein
R 5ax represents hydroxyl and
R 5eq represents a hydrogen atom.
4. A compound represented by formula (I) or its pharmacologically acceptable salt:
5. A pharmaceutical composition comprising a compound according to claim 1 or its pharmacologically acceptable salt or solvate, or their diastereomer mixture with respect to the carbon atom attached with *.
6. A pharmaceutical composition comprising a compound according to claim 4 or its pharmacologically acceptable salt.
7. An antimicrobial agent comprising a compound according to claim 1 or its pharmacologically acceptable salt or solvate, or their diastereomer mixture with respect to the carbon atom attached with *.
8. An antimicrobial agent comprising a compound according to claim 4 or its pharmacologically acceptable salt.
9. An anti-methicillin-resisant Staphlococcus aureus agent comprising a compound according to claim 1 or its pharmacologically acceptable salt, or their diastereomer mixture with respect to the carbon atom attached with *.
10. An anti-methicillin-resisant Staphlococcus aureus agent comprising a compound according to claim 4 or its pharmacologically acceptable salt.