Salt forms of (2E)-5-amino-5-methylhex-2-enoic acid N-methyl-N-((1R)-1-(N-methyl-N-((1R)-1-(methylcarbamoyl)-2-phenylethyl)carbamoyl)-2-(2-naphthyl)ethyl)amide
AssigneeNovo Nordisk A/S
InventorClaus Ulrich Jessen
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Abstract
The compounds disclosed are salts of (2E)-5-amino-5-methylhex-2-enoic acid N-methyl-N-((1R)-1-(N-methyl-N-((1R)-1-(methylcarbamoyl)-2-phenylethyl)carbamoyl)-2-(2-naphthyl)ethyl)amide of Formula I which have an aqueous solubility of at least 5 mg/ml, and a hygroscopicity of less than about 8 at 98% RH. These compounds are useful in the treatment of growth hormone deficiency.
Claims10
(2E)-5-amino-5-methylhex-2-enoic acid N-methyl-N-((1R)-1-(N-methyl-N-((1R)-1-(methylcarbamoyl)-2-phenylethyl)carbamoyl)-2-(2-naphthyl)ethyl)amide,hemi fumarate.
(2E)-5-amino-5-methylhex-2-enoic acid N-methyl-N-((1R)-1-(N-methyl-N-((1R)-1-(methylcarbamoyl)-2-phenylethyl)carbamoyl)-2-(2-naphthyl)ethyl)amide,hemi fumarate monohydrate.
- 3.(2E)-5-amino-5-methylhex-2-enoic acid N-methyl-N-((1R)-1-(N-methyl-N-((1R)-1--(methylcarbamoyl)-2-phenylethyl)carbamoyl)-2-(2-naphthyl)ethyl)amide,L(+)-mandelate.
A pharmaceutical composition comprising the hemifumarate salt, the hemifumarate monohydrate salt or the L(+)-mandelate salt of (2E)-5-amino-5-methylhex-2-enoic acid N-methyl-N-((1R)-1-(N-methyl-N-((1R)-1-(methylcarbamoyl)-2-phenylethyl)carbamoyl)-2-(2-naphthyl)ethyl)amide, together with a pharmaceutically acceptable carrier or diluent.
A method for stimulating the release of growth hormone in a patient comprising administering to the patient a therapeutically effective amount of the hemifumarate salt, the hemifumarate monohydrate salt or the L(+)-mandelate salt of (2E)-5-amino-5-methylhex-2-enoic acid N-methyl-N-((1R)-1-(N-methyl-N-((1R)-1-(methylcarbamoyl)-2-phenylethyl) carbamoyl)-2-(2-naphthyl)ethyl)amide.
The compound of claim 3 having an aqueous solubility of at least about 5 mg/ml and a hygroscopicity of less than about 8 at 98% RH.
Dependencies are inferred from the claim text.