Hexahydropyrazolo[4,3-c]pyridine metabolites

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 471/04 (2006.01) A61K 31/437 (2006.01) A61K 31/706 (2006.01) A61K 38/05 (2006.01) A61P 3/04 (2006.01) A61P 9/04 (2006.01) A61P 17/02 (2006.01) A61P 19/10 (2006.01) C07H 15/26 (2006.01) C07K 5/072 (2006.01)

Patent

CA 2339528

The invention provides metabolites of the compound 2-amino-N-[2-(3a(R)- benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo-(4,3-c]pyridin-5-yl)-1- (R)- benzyl-oxymethyl-2-oxo-ethyl]-isobutyramide, the racemic-diastereomeric mixtures and optical isomers thereof, the prodrugs thereof, and the pharmaceutically acceptable salts of the metabolites, racemic-diastereomeric mixtures, optical isomers, and prodrugs; to pharmaceutical compositions thereof; and to methods of using the metabolites and the compositions in the treatment of diseases associated with reduced levels of growth hormone. The invention further provides a kit comprising a metabolite of the compound 2-amino-N-[2-(3a(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo-[4,3- c]pyridin-5-yl)-1-(R)-benzyl-oxymethyl-2-oxo-ethyl]-isobutyramide a racemic- diastereomeric mixture or optical isomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt of the metabolite, racemic-diastereomeric mixture, optical isomers, or prodrug, and a pharmaceutically acceptable carrier, vehicle or diluent in a first unit dosage form; estrogen, progesterone, Premarin®, or a bisphosphonate compound, preferably alendronate, and a pharmaceutically acceptable carrier, vehicle or diluent in a second unit dosage form; and a container.

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