Novel combined administration
OwnerGuenter Gross, Joseph Tardioinventors
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Abstract
The present invention is directed to the combined administration of a thioester therapeutic agent (preferably of formula I) and at least one esterase inhibitor. Also provided are a pharmaceutical composition, package, and a kit comprising the aforementioned active ingredients, as well as a method for increasing the bioavailability of said thioester for the treatment and prophylaxis of a cardiovascular disorder.
Claims13
A method for increasing the bioavailability of a thioester, wherein a dosage form containing an esterase inhibitor is administered in combination with a dosage form containing the thioester.
A composition, package, or kit comprising (a) a thioester that forms S-[2-([[1-(2-ethylbutyl)cyclohexyl]carbonyl]amino)phenyl]thiol in vivo and (b) at least an esterase inhibitor.
A pharmaceutical composition, package, or kit comprising:
- (a) a thioester of formula I:
- wherein:
- R is selected from the group consisting of:
- (1) a C1-C10alkyl, (2) a C2-C10alkenyl, (3) a haloC1-C4alkyl, (4) a C3-C10cycloalkyl, (5) a C5-C8cycloalkenyl, (6) a C3-C10cycloalkylC1-C10alkyl, (7) aryl, (8) aralkyl, and (9) a 5- or 6-membered heterocyclic group having 1 to 3 nitrogen, oxygen or sulfur atoms,
- X1, X2, X3 and X4 are independently selected from the group consisting of:
- (1) hydrogen, (2) halogen, (3) a C1-C4alkyl, (4) a haloC1-C4alkyl, (5) a C1-C4alkoxy, (6) cyano, (7) nitro, (8) acyl, and (9) aryl,
- Y is —CO— or —SO2;
- Z is a C1-C10alkyl, a C3-C10cycloalkyl or a C3-C10cycloalkylC1-C10alkyl;
- and
- (b) an esterase inhibitor which is 1-(3-hexyl-4-oxo-oxetan-2-yl)tridecan-2-yl 2-formyl-amino-4-methyl-pentanoate.
A method for the treatment or prophylaxis of a cardiovascular disorder in a patient, which comprises treating the patient with a therapeutically effective amount of a combination of:
- (a) a thioester that forms S-[2-([[1-(2-ethylbutyl)cyclohexyl]carbonyl]amino)phenyl]thiol in vivo, and (b) at least one esterase inhibitor.
Dependencies are inferred from the claim text.