Lactol derivatives, their production and use
AssigneeTakeda Chemical Industries, Ltd.
InventorsTakashi Sohda, Yukio Fujisawa, Satoru Oi, Junji Mizoguchi
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AssigneeTakeda Chemical Industries, Ltd.
InventorsTakashi Sohda, Yukio Fujisawa, Satoru Oi, Junji Mizoguchi
Estimating the term…
The present invention provides novel compound of the formulas (Ia) or (I): ##STR1## wherein Q is one or two amino acid residues which may be substituted; R.sup.3 is a carboxyl group which may be esterified or an acyl group; A is an alkylene group; B is hydrogen or an alkyl group which may be substituted or an acyl group; or a salt thereof; ##STR2## wherein R.sup.1 and R.sup.2 may be the same or different and each is hydrogen or a hydrocarbon residue which may be substituted; R.sup.3, A and B have the same definitions as those shown above; m and n each is 0 or 1; provided that where both m and n are both equal to 0, R.sup.3 is a carboxyl group which may be esterified or an acyl group having not less than 7 carbon atoms; or a salt thereof. The compound (Ia) or (I) shows cathepsin L inhibitory and bone resorption inhibitory activities and are useful as a prophylactic/therapeutic agent for osteoporosis.
A compound of the general formula
A compound of the general formula ##STR80## wherein R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen or a hydrocarbon group which may or may not be substituted;
A compound selected from (3S)-3-[[N-dibenzylacetyl]amino]-2-hydroxytetrahydrofuran and (3S)-3-[[N-7,7-diphenyl-6-heptenyoyl]amino]-2-hydroxytetrahydrofuran, or a salt of the compound.
A cathepsin L inhibitory composition comprising a compound of the general formula. ##STR81## wherein Q represents one or two amino acid residues which may or may not be substituted;
A cathepsin L inhibitory composition comprising a compound of the general formula ##STR82## wherein R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen or a hydrocarbon residue which may or may not be substituted;
A bone resorption inhibitory composition comprising a compound of the general formula ##STR83## wherein Q represents one or two amino acid residues which may or may not be substituted;
A bone resorption inhibitory composition comprising a compound of the general formula ##STR84## wherein R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen or a hydrocarbon residue which may or may not be substituted;
A cathepsin L inhibitory composition according to claim 14 or 20 for the prophylaxis or therapy of osteoporosis.
A method for prophylaxis or treatment of a mammal suffering from osteoporosis which comprises administering to said mammal an effective amount of a compound of the formula ##STR85## wherein Q represents one or two amino acid residues which may or may not be substituted;
A method for prophylaxis or treatment of a mammal suffering from osteoporosis which comprises administering to said mammal an effective amount of a compound of the formula ##STR86## wherein R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen or a hydrocarbon residue which may or may not be substituted;
Dependencies are inferred from the claim text.