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US 7,598,273 B2Granted
Inhibitors of the gastric H+, K+-ATPase with enhanced therapeutic properties
AssigneeAuspex Pharmaceuticals, Inc.
InventorsThomas G. Gant, Sepehr Sarshar
Life of this patent
Estimating the term…
Abstract
Chemical syntheses and medical uses of novel inhibitors of the gastric H+, K+-ATPase for the treatment and/or management of duodenal ulcers, heartburn, acid reflux, other conditions mediated by gastric acid secretion and/or psoriasis are described.
Claims12
A compound of Formula 1
- or a single enantiomer, a mixture of the (+)-enantiomer and the (−)-enantiomer, an individual diastereomer, a mixture of diastereomers, or a pharmaceutically acceptable salt thereof, wherein:
- R1, R4, R9 and R10 are each independently hydrogen or deuterium;
- R2, R3, R6 and R8 are each independently selected from the group consisting of hydrogen, deuterium, C1-C6 alkyl, and C1-C6 alkyloxy;
- R5 is selected from the group consisting of —CH2—, —CHD— and —CD2—;
- and
- R7 is selected from the group consisting of hydrogen, deuterium, —NO2, C1-C6 alkyl, and C1-C6 alkyloxy;
- if R1, R3, and R4 are deuterium, R2 is —OCH3, R6 is CH3, R7 is OCH3, and R8 is —CH3, then at least one of R5, R9, and R10 has deuterium enrichment of at least about 1%;
- if R1, R2, R3, and R4 are deuterium, is R6 is —CH3, and R7 is —OCH2CF3, then at least one of R8, R9, and R10 has deuterium enrichment of at least about 1%;
- if R2 is —OCHF2, R6 is —OCH3, and R7 is —OCD3, then at least one of R1, R3, R4, R5, R8, R9, and R10 has deuterium enrichment of at least about 1%;
- provided that said compound of Formula 1 contains at least one deuterium atom;
- and
- provided that deuterium enrichment in said compound of Formula 1 is at least about 1%.
9 more elements
A compound selected from the group consisting of:
- or a single enantiomer, a mixture of the (+)-enantiomer and the (−)-enantiomer, a mixture of about 90% or more by weight of the (−)-enantiomer and about 10% or less by weight of the (+)-enantiomer, a mixture of about 90% or more by weight of the (+)-enantiomer and about 10% or less by weight of the (−)-enantiomer, an individual diastereomer, a mixture of diastereomers, or a pharmaceutically acceptable salt thereof.
A compound selected from the group consisting of:
- or a single enantiomer, a mixture of the (+)-enantiomer and the (−)-enantiomer, a mixture of about 90% or more by weight of the (−)-enantiomer and about 10% or less by weight of the (+)-enantiomer, a mixture of about 90% or more by weight of the (+)-enantiomer and about 10% or less by weight of the (−)-enantiomer, an individual diastereomer, a mixture of diastereomers, or a pharmaceutically acceptable salt thereof.
A compound selected from the group consisting of:
- or a single enantiomer, a mixture of the (+)-enantiomer and the (−)-enantiomer, a mixture of about 90% or more by weight of the (−)-enantiomer and about boo or less by weight of the (+)-enantiomer, a mixture of about 90% or more by weight of the (+)-enantiomer and about 10% or less by weight of the (−)-enantiomer, an individual diastereomer, a mixture of diastereomers, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.