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US 8,133,871 B2Granted
Dihydropseudoerythromycin derivatives
AssigneesThe Kitasato Institute, Aphoenix, Inc.
InventorsSatoshi Omura, Toshiaki Sunazuka, Kenichiro Nagai, Hideaki Shima, Haruko Yamabe
Life of this patent
Estimating the term…
Abstract
A compound represented by the formula [I] wherein each symbol is as defined in the specification or a pharmacologically acceptable salt thereof, and a pharmaceutical composition containing the compound as an active ingredient.
Claims25
A compound represented by the following formula [I]
- wherein Me is a methyl group,
- R1 and R2 are the same or different and each is a hydrogen atom, an alkyl group, an acyl group, a sulfonyl group, a substituted or unsubstituted aryl-substituted alkyl group, an aryl-substituted alkyloxycarbonyl group, an alkenyl group or an alkynyl group, or R1 and R2 in combination form, together with the adjacent nitrogen atom, a substituted or unsubstituted alicyclic heterocyclic group,
- R3 is a hydrogen atom, a substituted or unsubstituted acyl group or an aryl-substituted alkyloxycarbonyl group,
- A is a hydrogen atom, B is a hydroxyl group or a group represented by the following formula [II]
- wherein Me is a methyl group and R4 is a hydrogen atom or an acyl group, or A and B in combination show ═O,
- R is a group represented by the following formula [III]
- wherein Me is a methyl group, R5 and R6 are the same or different and each is a hydrogen atom or an acyl group, or R5 and R6 in combination show a carbonyl group or a substituted or unsubstituted alkylene group, a substituent represented by the following formula [IV]
- wherein Me is a methyl group, D is O or N—OH, or D is a hydrogen atom and a hydroxyl group (—H, —OH), or a substituent represented by the following formula [V]
- wherein Me is a methyl group,
- or a pharmacologically acceptable salt thereof.
7 more elements
The following compound
- (1) 9-dihydro-pseudoerythromycin A 6,9-epoxide
- (2) de(3′-N-methyl)-9-dihydro-pseudoerythromycin A 6,9-epoxide
- (3) de(3′-N-methyl)-3′-N-benzyl-9-dihydro-pseudoerythromycin A 6,9-epoxide
- (4) bis-de(3′-N-methyl)-9-dihydro-pseudoerythromycin A 6,9-epoxide
- (5) bis-de(3′-N-methyl)-bis-(3′-N-benzyl)-9-dihydro-pseudoerythromycin A 6,9-epoxide
- (6) de(3′-N-methyl)-3′-N-(p-chlorobenzyl)-9-dihydro-pseudoerythromycin A 6,9-epoxide
- (7) de[12-(1-hydroxypropyl)]-9-dihydro-12-oxo-pseudoerythromycin A 6,9-epoxide
- (8) de[12-(1-hydroxypropyl)]-9-dihydro-12-hydroxyoxime-pseudoerythromycin A 6,9-epoxide
- (9) de[12-(1-hydroxypropyl)]-9-dihydro-pseudoerythromycin A 6,9-epoxide
- (10) 12,13-epoxy-9-dihydro-pseudoerythromycin A 6,9-epoxide
- (11) de(3-O-cladinosyl)-9-dihydro-pseudoerythromycin A 6,9-epoxide
- (12) 4″,13-O-diacetyl-9-dihydro-pseudoerythromycin A 6,9-epoxide
- (13) 2′-O-acetyl-9-dihydro-pseudoerythromycin A 6,9-epoxide
- (14) de(3′-dimethylamino)-3′-morpholino-9-dihydro-pseudoerythromycin A 6,9-epoxide
- (15) 2′-O-acetyl-de(3-O-cladinosyl)-9-dihydro-3-keto-pseudoerythromycin A 6,9-epoxide 12,13-carbonate
- (16) de(3-O-cladinosyl)-9-dihydro-3-keto-pseudoerythromycin A 6,9-epoxide 12,13-carbonate
- (17) de(3′-N-methyl)-3′-N-(p-chlorobenzyl)-de(3-O-cladinosyl)-9-dihydro-pseudoerythromycin A 6,9-epoxide
- (18) 2′-O-acetyl-de(3-O-cladinosyl)-9-dihydro-3-keto-de(3′-dimethylamino)-3′-morpholino-pseudoerythromycin A 6,9-epoxide 12,13-carbonate
- (19) de(3-O-cladinosyl)-9-dihydro-3-keto-de(3′-dimethylamino)-3′-morpholino-pseudoerythromycin A 6,9-epoxide 12,13-carbonate
- (20) de(3′-N-methyl)-2′-O-3′-N-bis(benzyloxycarbonyl)-de(3-O-cladinosyl)-9-dihydro-pseudoerythromycin A 6,9-epoxide 12,13-carbonate
- (21) de(3′-N-methyl)-3′-N-(p-chlorobenzyl)-de(3-O-cladinosyl)-9-dihydro-3-keto-pseudoerythromycin A 6,9-epoxide 12,13-carbonate
- (22) de(3-O-cladinosyl)-9-dihydro-de(3′-dimethylamino)-3′-morpholino-pseudoerythromycin A 6,9-epoxide 12,13-carbonate
- (23) de(3′-N-methyl)-3′-N-(p-chlorobenzyl)-de(3-O-cladinosyl)-9-dihydro-3-keto-pseudoerythromycin A 6,9-epoxide 12,13-isopropylidene acetal or
- (24) de(3′-N-methyl)-3′-N-(p-chlorobenzyl)-de(3-O-cladinosyl)-9-dihydro-3-keto-pseudoerythromycin A 6,9-epoxide,
- or a pharmacologically acceptable salt thereof.
22 more elements
The following compound
- (1) 9-dihydro-pseudoerythromycin A 6,9-epoxide
- (2) de(3′-N-methyl)-3′-N-(p-chlorobenzyl)-9-dihydro-pseudoerythromycin A 6,9-epoxide
- (3) de(3′-dimethylamino)-3′-morpholino-9-dihydro-pseudoerythromycin A 6,9-epoxide or
- (4) de(3′-N-methyl)-3′-N-(p-chlorobenzyl)-de (3-O-cladinosyl)-9-dihydro-3-keto-pseudoerythromycin A 6,9-epoxide 12,13-carbonate,
- or a pharmacologically acceptable salt thereof.
2 more elements
Dependencies are inferred from the claim text.