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US 5,846,562 AGranted
Oral composition of fumagillol derivative
AssigneeTakeda Chemical Industries, Ltd.
InventorsShigeo Yanai, Katsuichi Sudo, Yohko Akiyama, Naoki Nagahara
Life of this patent
Estimating the term…
Abstract
The present invention relates to a pharmaceutical composition for oral administration in which a fumagillol derivative is stabilized and exhibits remarkable antiangiogenesis activity in oral administration.
Claims28
A method for treating or preventing angiogenesis associated diseases which comprises orally administering a pharmaceutical composition comprising a fumagillol derivative of the formula:
- ##STR3## wherein R.sup.1 represents hydrogen, R.sup.2 represents halogen, N(O).sub.m R.sup.5 R.sup.6, N.sup.+ R.sup.5 R.sup.6 R.sup.7.X.sup.-, S(O).sub.n R.sup.5, or S.sup.+ R.sup.5 R.sup.6.X.sup.- (wherein R.sup.5, R.sup.6, and R.sup.7 respectively represent an optionally substituted hydrocarbon group or heterocyclic group, X.sup.- represents a counter anion, m represents an integer of 0 or 1;
- n represents an integer of 0-2;
- R.sup.5 and R.sup.6 may taken together with the adjacent nitrogen or sulfur atom to form an optionally condensed nitrogen- or sulfur-containing heterocyclic group which may be substituted), or R.sup.1 and R.sup.2 together represent a chemical bond;
- R.sup.3 represents an optionally substituted 2-methyl-1-propenyl or isobutyl group;
- A represents O or NR.sup.8 (R.sup.8 represents hydrogen, an optionally substituted 2-methyl-1-propenyl or isobutyl group, or an optionally substituted aryl group);
- R.sup.4 represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted acyl group;
- or a salt thereof and a fatty acid alcohol ester, to a patient in need thereof.
4 more elements
A method for treating or preventing angiogenesis-associated diseases which comprises orally administering a pharmaceutical composition comprising a fumagillol derivative of the formula:
- ##STR4## wherein R.sup.1 represents hydrogen, R.sup.2 represents halogen, N(O).sub.m R.sup.5 R.sup.6, N.sup.+ R.sup.5 R.sup.6 R.sup.7.X.sup.-, S(O).sub.n R.sup.5, or S.sup.+ R.sup.5 R.sup.6.X.sup.- (wherein R.sup.5, R.sup.6, and R.sup.7 respectively represent an optionally substituted hydrocarbon group or heterocyclic group, X.sup.- represents a counter anion, m represents an integer of 0 or 1;
- n represents an integer of 0-2;
- R.sup.5 and R.sup.6 may taken together with the adjacent nitrogen or sulfur atom to form an optionally condensed nitrogen- or sulfur-containing heterocyclic group which may be substituted), or R.sup.1 and R.sup.2 together represent a chemical bond;
- R.sup.3 represents an optionally substituted 2-methyl-1-propenyl or isobutyl group;
- A represents O or NR.sup.8 (R.sup.8 represents hydrogen, an optionally substituted 2-methyl-1-propenyl or isobutyl group, or an optionally substituted aryl group);
- R.sup.4 represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted acyl group;
- or a salt thereof and a fatty acid alcohol ester, and a gastric acid secretion-inhibitor to a patient in need thereof.
4 more elements
A method for treating or preventing angiogenesis-associated diseases which comprises orally administering a pharmaceutical composition comprising a fumagillol derivative of the formula:
- ##STR5## wherein R.sup.1 represents hydrogen, R.sup.2 represents halogen, N(O).sub.m R.sup.5 R.sup.6, N.sup.+ R.sup.5 R.sup.6 R.sup.7.X.sup.-, S(O).sub.n R.sup.5, or S.sup.+ R.sup.5 R.sup.6.X.sup.- (wherein R.sup.5, R.sup.6, and R.sup.7 respectively represent an optionally substituted hydrocarbon group or heterocyclic group, X.sup.- represents a counter anion, m represents an integer of 0 or 1;
- n represents an integer of 0-2;
- R.sup.5 and R.sup.6 may taken together with the adjacent nitrogen or sulfur atom to form an optionally condensed nitrogen- or sulfur-containing heterocyclic group which may be substituted), or R.sup.1 and R.sup.2 together represent a chemical bond;
- R.sup.3 represents an optionally substituted 2-methyl- 1-propenyl or isobutyl group;
- A represents O or NR.sup.8 (R.sup.8 represents hydrogen, an optionally substituted 2-methyl-1 -propenyl or isobutyl group, or an optionally substituted aryl group);
- R.sup.4 represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted acyl group;
- or a salt thereof and a fatty acid alcohol ester, and an antacid to a patient in need thereof.
4 more elements
A method for treating or preventing angiogenesis-associated diseases which comprises orally administering, a pharmaceutical composition comprising a fumagillol derivative of the formula:
- ##STR6## wherein R.sup.1 represents hydrogen, R.sup.2 represents halogen, N(O).sub.m R.sup.5 R.sup.6, N.sup.+ R.sup.5 R.sup.6 R.sup.7.X.sup.-, S(O).sub.n R.sup.5, or S.sup.+ R.sup.5 R.sup.6.X.sup.- (wherein R.sup.5, R.sup.6, and R.sup.7 respectively represent an optionally substituted hydrocarbon group or heterocyclic group, X.sup.- represents a counter anion, m represents an integer of 0 or 1;
- n represents an integer of 0-2;
- R.sup.5 and R.sup.6 may taken together with the adjacent nitrogen or sulfur atom to form an optionally condensed nitrogen- or sulfur-containing heterocyclic group which may be substituted), or R.sup.1 and R.sup.2 together represent a chemical bond;
- R.sup.3 represents an optionally substituted 2-methyl-1-propenyl or isobutyl group;
- A represents O or NR.sup.8 (R.sup.8 represents hydrogen, an optionally substituted 2-methyl- 1-propenyl or isobutyl group, or an optionally substituted aryl group);
- R.sup.4 represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted acyl group;
- or a salt thereof and a fatty acid alcohol ester, a gastric acid secretion-inhibitor and an antacid to a patient in need thereof.
4 more elements
Dependencies are inferred from the claim text.