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US 6,610,877 B1Granted
Aromatic carboxylic acid derivatives
AssigneeHoffman-La Roche Inc.
InventorsMichael Klaus, Peter Mohr
Life of this patent
Estimating the term…
Abstract
Compounds of the formula wherein R1 is a residue of the formula and R2-R10 have the significance given in the specification can be used as pharmaceuticals, particularly for the repair of photodamaged skin, other dermatological conditions, and oncological indications.
Claims87
A compound having the formula:
- wherein
- R2 is C2-8-alkanoyl, C2-8-alkyl, C2-8-alkenyl, C2-8-alkynyl or —OCH2R3;
- R3 is hydrogen, C1-6-alkyl, C2-6-alkenyl or C2-6-alkynyl;
- R5 and R7 each independently are hydrogen or C1-5-alkyl;
- R4 and R6 each independently are hydrogen or C1-5-alkyl, or taken together are methylene or ethylene which are unsubstituted or substituted by hydroxy;
- Ra and Rb each are independently hydrogen or C1-5-alkyl;
- R10 is carboxyl, C1-6-alkoxycarbonyl or mono- or di-(C1-6-alkyl)carbamoyl;
- and pharmaceutically acceptable salts of carboxylic acids of formula Ia.
5 more elements
A compound of the formula:
- wherein
- R2 is C2-8-alkanoyl, C2-8-alkyl, C2-8-alkenyl, C2-8-alkynyl or —OCH2R3;
- R3 is hydrogen, C1-6-alkyl, C2-6-alkenyl or C2-6-alkynyl;
- R5 and R7 each independently are hydrogen or C1-5-alkyl;
- R4 and R6 each independently are hydrogen or C1-5-alkyl, or taken together are methylene or ethylene which are unsubstituted or substituted by hydroxy;
- Ra, Ra′, Rb and Rb′ each are independently hydrogen or C1-5-alkyl;
- R10 is carboxyl, C1-6-alkoxycarbonyl or mono- or di-(C1-6-alkyl)carbamoyl;
- and pharmaceutically acceptable salts of carboxylic acids of formula Ib(1).
5 more elements
A compound having the formula:
- wherein
- R2 is C2-8-alkanoyl, C2-8-alkyl, C2-8-alkenyl, C2-8-alkynyl or —OCH2R3;
- R3 is hydrogen, C1-6-alkyl, C2-6-alkenyl or C2-6-alkynyl;
- R5 and R7 each independently are hydrogen or C1-5-alkyl;
- R4 and R6 each independently are hydrogen or C1-5-alkyl, or taken together are methylene or ethylene which are unsubstituted or substituted by hydroxy;
- Ra, Ra′, Rb and Rb′ each are independently hydrogen or C1-5-alkyl;
- R10 is carboxyl, C1-6-alkoxycarbonyl or mono- or di-(C1-6-alkyl)carbamoyl;
- and pharmaceutically acceptable salts of carboxylic acids of formula Ib(2).
5 more elements
A compound of the formula:
- wherein
- R2 is C2-8-alkanoyl, C2-8-alkyl, C2-8-alkenyl, C2-8-alkynyl or —OCH2R3;
- R3 is hydrogen, C1-6-alkyl, C2-6-alkenyl or C2-6-alkynyl;
- R5 and R7 each independently are hydrogen or C1-5-alkyl;
- R4 and R6 each independently are hydrogen or C1-5-alkyl, or taken together are methylene or ethylene which are unsubstituted or substituted by hydroxy;
- Ra, Ra′, Ra″, Rb Rb′ and Rb″ each are independently hydrogen or C1-5-alkyl;
- R10 is carboxyl, C1-6-alkoxycarbonyl or mono- or di-(C1-6-alkyl)carbamoyl;
- and pharmaceutically acceptable salts of carboxylic acids of formula Ic.
5 more elements
A compound having the formula:
- wherein
- R2 is C2-8-alkanoyl, C2-8-alkyl, C2-8-alkenyl, C2-8-alkynyl or —OCH2R3;
- R3 is hydrogen, C1-6-alkyl, C2-6-alkenyl or C2-6-alkynyl;
- R5 and R7 each independently are hydrogen or C1-5-alkyl;
- R4 and R6 each independently are hydrogen or C1-5-alkyl, or taken together are methylene or ethylene, which are unsubstituted or substituted by hydroxy;
- Ra and Rb each are independently hydrogen or C1-5-alkyl;
- R10 is carboxyl, C1-6-alkoxycarbonyl or mono- or di-(C1-6-alkyl)carbamoyl;
- and pharmaceutically acceptable salts of carboxylic acids of formula Id.
5 more elements
A compound having the formula:
- wherein:
- R2 is C2-8-alkanoyl, C2-8-alkenyl, C2-8-alkynyl or —OCH2R3;
- R3 is hydrogen, C1-6-alkyl, C2-6-alkenyl or C2-6-alkynyl;
- R5 and R7 each independently are hydrogen or C1-5-alkyl;
- R4 and R6 each independently are hydrogen or C1-5-alkyl, or taken together are methylene or ethylene which are unsubstituted or substituted by hydroxy;
- Ra, Ra′, Rb and Rb′ each are independently hydrogen or C1-5-alkyl;
- R10 is carboxyl, C1-6-alkoxycarbonyl or mono- or di-(C1-6-alkyl)carbamoyl;
- and pharmaceutically acceptable salts of carboxylic acids of formula Ie.
5 more elements
A compound having the formula:
- wherein
- R2 is C2-8-alkanoyl, C2-8-alkyl, C2-8-alkenyl, C2-8-alkynyl or —OCH2R3;
- R3 is hydrogen, C1-6-alkyl, C2-6-alkenyl or C2-6-alkynyl;
- R5 and R7 each independently are hydrogen or C1-5-alkyl;
- R4 and R6 each independently are hydrogen or C1-5-alkyl, or taken together are methylene or ethylene which are unsubstituted or substituted by hydroxy;
- Ra, Ra′, Ra″, Rb Rb′ and Rb″ each are independently hydrogen or C1-5-alkyl;
- R10 is carboxyl, C1-6-alkoxycarbonyl or mono- or di-(C1-6-alkyl)carbamoyl;
- and pharmaceutically acceptable salts of carboxylic acids of formula If.
5 more elements
Dependencies are inferred from the claim text.