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US 6,555,530 B1Granted
Use of estrogens and delta-gonadien-21-Ol-3,20-diones for treating insulin dependent and non-insulin dependent diabetes
AssigneeNovo Nordisk A/S
InventorKarsten Wassermann
Life of this patent
Estimating the term…
Abstract
Analysis of full-blood glucose, serum insulin, serum triglycerides and total serum cholesterol were performed. Glucose levels in blood samples from the oral glucose tolerance test were used for calculation of the incremental Area Under the Curve (AUC0-120 min−baseline). All data are expressed as percentage change of vehicle treated animals (cf. FIGS. 1 and 2).
Claims14
A method of treating type I or type II diabetes, said method comprising administering to a subject in need of such treatment:
- (i) an effective amount of (a) an estrogen selected from the group consisting of 17-beta-estradiol and esters thereof, ethinylestradiol, estriol (trihydroxyestrin), estrone, conjugated estrogens, sodium estrone sulfate, 17alfa-dihydroequilin, equilenin, 17alfa-dihydroequilenin, esterified estrogens, and equilin, or (b) an estrogen receptor modulator selected from the group consisting of droloxifene, raloxifene, tamoxifen, 4-hydroxy-tamoxifen, idoxifene, centchroman, Cis-6-(4-fluoro-phenyl)-5-[4-2-piperidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol;
- (−)-Cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol;
- Cis-6-phenyl-5-[4(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol;
- Cis-1-[6′-pyrrolidinoethoxy-3′-pyridyl]-2-phenyl-6-hydroxy-1,2,3,4-tetrahydronaphthalene;
- 1-(4′-Pyrrolidinoethoxyphenyl)-2-(4′-fluorophenyl)-6-hydroxy-1,2,3,4-tetrahydroisoquinoline;
- Cis-6-(4-hydroxyphenyl)-5-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol;
- and 1-(4′-Pyrrolidinoethoxyphenyl)-2-phenyl-6-hydroxy-1,2,3,4-tetrahydroisoquinoline, in combination with:
- (ii) an effective amount of a compound of formula I
- wherein R1, R2 and R3 independently of each other are C1-12 alkyl, in the form of 21R or 21S epimers or mixtures thereof, or a pharmaceutically acceptable salt thereof, wherein said first and second amounts in combination are effective to treat said type I or type II diabetes.
6 more elements
A method of reducing blood glucose concentrations, said method comprising administering to a subject in need of such treatment:
- (i) an effective amount of (a) an estrogen selected from the group consisting of 17-beta-estradiol and esters thereof, ethinylestradiol, estriol (trihydroxyestrin), estrone, conjugated estrogens, sodium estrone sulfate, 17alfa-dihydroequilin, equilenin, 17alfa-dihydroequilenin, esterified estrogens, and equilin or (b) an estrogen receptor modulator selected from the group consisting of droloxifene, raloxifene, tamoxifen, 4-hydroxy-tamoxifen, idoxifene, centchroman, Cis-6-(4-fluoro-phenyl)-5-[4-2-piperidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol;
- (−)-Cis-6-phenyl-5-[4-(2-pyrrolidin-1 -yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol;
- (−)-Cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol;
- Cis-1-[6′-pyrrolidinoethoxy-3′-pyridyl]-2-phenyl-6-hydroxy-1,2,3,4-tetrahydronaphthalene;
- 1-(4′-Pyrrolidinoethoxyphenyl)-2-(4′-fluorophenyl)-6-hydroxy-1,2,3,4-tetrahydroisoquinoline;
- Cis-6-(4-hydroxyphenyl)-5-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol;
- and 1-(4′-Pyrrolidinoethoxyphenyl)-2-phenyl-6-hydroxy-1,2,3,4-tetrahydroisoquinoline, in combination with:
- (ii) an effective amount of a compound of formula I
- wherein R1, R2 and R3 independently of each other are C1-12 alkyl, in the form of 21R or 21S epimers or mixtures thereof, or a pharmaceutically acceptable salt thereof, wherein said effective amount of an estrogen or estrogen receptor modulator in combination with said effective amount of the compound of formula I are effective to reduce blood glucose concentrations.
6 more elements
Dependencies are inferred from the claim text.