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US 5,668,111 AGranted
Sustained-release preparation
AssigneeTakeda Chemical Industries, Ltd.
InventorsShigeru Kamei, Yasutaka Igari, Yasuaki Ogawa
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AssigneeTakeda Chemical Industries, Ltd.
InventorsShigeru Kamei, Yasutaka Igari, Yasuaki Ogawa
Estimating the term…
A sustained-release preparation which comprises a physiologically active peptide of general formula ##STR1## wherein X represents an acyl group; R.sub.1, R.sub.2 and R.sub.4 each represents an aromatic cyclic group; R.sub.3 represents a D-amino acid residue or a group of the formula ##STR2## wherein R.sub.3 ' is a heterocyclic group; R.sub.5 represents a group of the formula --(CH.sub.2).sub.n --R.sub.5 ' wherein n is 2 or 3, and R.sub.5 ' is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group; R.sub.6 represents a group of the formula --(CH.sub.2).sub.n --R.sub.6 ' wherein n is 2 or 3, and R.sub.6 ' is an amino group which may optionally be substituted; R.sub.7 represents a D-amino acid residue or an azaglycyl residue; and Q represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group. The sustained-release preparation shows a constant release of the peptide over a long time and is substantially free from an initial burst.
A method for treating a luteinizing hormone-dependent disease or a follicle stimulating hormone-dependent disease in a mammal which comprises administering to a mammal in need thereof a therapeutically effective amount of a sustained-release preparation comprising a physiologically active peptide of the following formula:
A method for antagonizing LH-RH activity in a mammal which comprises administering to a mammal in need thereof a therapeutically effective amount of a sustained-release preparation comprising a physiologically active peptide of the following formula:
A method for antagonizing LH-RH activity in a mammal which comprises administering to a mammal in need thereof a therapeutically effective amount of a sustained-release preparation comprising a physiologically active peptide of the following formula:
A sustained-release preparation for treating a hormone-dependent diseases comprising an effective amount of a physiologically active peptide of the following formula:
A sustained-release preparation for antagonizing LH-RH activity comprising an effective amount of a physiologically active peptide of the following formula:
A method for treating a gonad-derived steroid hormone-dependent disease in a mammal which comprises administering to a mammal in need thereof a therapeutically effective amount of a sustained-release preparation comprising a physiologically active peptide of the following formula:
Dependencies are inferred from the claim text.