ORAL DOSAGE FORM COMPRISING A CYCLOPROPANECARBOXAMIDE DERIVATIVE FOR USE IN TREATING INSOMNIA

ORAL DOSAGE FORM COMPRISING A CYCLOPROPANECARBOXAMIDE DERIVATIVE FOR USE IN TREATING INSOMNIA

In the present invention relates to the dosage form for use in the treatment of insomnia comprising a therapeutically effective amount of compound A and at least one pharmaceutically acceptable excipient, wherein said therapeutically effective amount is a single daily dose ranging from 2.5 mg to 10...

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Hauptverfasser: ZAIMA, YASUHIRO, SUZUKI, NOBUYA, PASTINO, GINA, AKIMOTO, YURIE, MOLINE, MARGARET, YOSHIDA, NOBUO
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Sprache:eng ; fre
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HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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creator ZAIMA, YASUHIRO
SUZUKI, NOBUYA
PASTINO, GINA
AKIMOTO, YURIE
MOLINE, MARGARET
YOSHIDA, NOBUO
description In the present invention relates to the dosage form for use in the treatment of insomnia comprising a therapeutically effective amount of compound A and at least one pharmaceutically acceptable excipient, wherein said therapeutically effective amount is a single daily dose ranging from 2.5 mg to 10 mg, wherein said single daily dose achieves a mean Cmax of from about 3.0 ng/ml to about 7.2 ng/ml, a mean AUC(0-24) of from about 15.9 ng*hr/ml, or a mean AUC(0-inf) of from about 19.8 ng*hr/ml to about 53.1 ng*hr/ml to about 23.8 ng*hr/ml for each 1 mg of compound A after administration to human subjects, and said compound A is (1R,2S)-2-(((2,4-dimethylpyrimidin-5-yl)oxy)methyl)-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl) cyclopropanecarboxamide represented by the following formula. (see above formula) Selon la présente invention, des composés tels que le (1R,2S)-2-(((2,4-diméthylpyrimidin-5-yl)oxy)méthyl)-2-(3-fluorophényl)-N-(5-fluoropyridin-2-yl) cyclopropanecarboxamide se sont révélés être de puissants antagonistes des récepteurs de l'orexine, et peuvent être utiles pour le traitement de troubles du sommeil, tels que l'insomnie, ainsi que pour d'autres utilisations thérapeutiques.
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subjects HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title ORAL DOSAGE FORM COMPRISING A CYCLOPROPANECARBOXAMIDE DERIVATIVE FOR USE IN TREATING INSOMNIA
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