Combination effective for the treatment of impotence
First Claim
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1. A method of treating impotence comprising co-administering to a patient in need of such treatment an effective amount of:
- (1) a potassium channel opener selected from the group consisting of nicorandil, cromokalim, levcromakalim, lemakalim, pinacidil, diazoxide and minoxidil or a pharmaceutically acceptable salt thereof, and (2) a compound which elevates cGMP levels;
wherein (1) and (2) are each administered orally.
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Abstract
This invention relates to the treatment of erectile dysfunction with a combination of (1) a compound selected from potassium channel openers, and (2) a compound selected from compounds which elevate cGMP levels. Sildenafil or a pharmaceutically acceptable salt thereof is preferred as the cGMP PDE elevator. Also included are compositions and kits comprising such impotence treating compounds.
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Citations
25 Claims
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1. A method of treating impotence comprising co-administering to a patient in need of such treatment an effective amount of:
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(1) a potassium channel opener selected from the group consisting of nicorandil, cromokalim, levcromakalim, lemakalim, pinacidil, diazoxide and minoxidil or a pharmaceutically acceptable salt thereof, and (2) a compound which elevates cGMP levels;
wherein (1) and (2) are each administered orally. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13)
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14. A method for achieving a synergistic therapeutically effective level of impotence treatment, comprising co-administering orally to a mammal in need of such treatment
(1) an amount of a potassium channel opener selected from the group consisting of nicorandil, cromokalim, levcromakalim, lemakalim, pinacidil, diazoxide and minoxidil or a pharmaceutically acceptable salt thereof; - and
(2) an amount of a second compound selected from compounds which elevate cGMP levels;
wherein the amount of the potassium channel opener alone and the amount of the second compound alone is insufficient to achieve the synergistic therapeutically effective level of impotence treatment, but wherein the combined effect of the amounts of the potassium channel opener and the second compound is greater than the sum of the levels of therapeutic effects of impotence treatment achievable with the individual amounts of the potassium channel opener and the second compound. - View Dependent Claims (15, 16, 17, 18, 19, 20, 21, 22, 23, 24)
or is a pharmaceutically acceptable salt thereof. -
21. A method as defined in claim 15 wherein said wherein said cGMP PDE inhibitor is 3-ethyl-5-[2-(2-methoxyethoxy)-5-(4-methylpiperazin-1-ylsulphonyl)pyridin-3-yl]-2-(pyridin-2-yl)methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one;
- 3-ethyl-5-[5-(4-ethylpiperazin-1-ylsulphonyl)-2)2-methoxyethoxy)pyridin-3-yl]-2-(pyridin-2-yl)methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one;
3-ethyl-5-[5-(4-ethyl-4-oxidopiperazin-1-ylsulphonyl)-2-(2-methoxyethoxy)pyridin-3-yl]-2-(pyridin-2-yl)methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one;
5-[2-(2-methoxyethyoxy)-5-(4-methylpiperazin-1-ylsulphonyl)pyridin-3-yl]-3-n-propyl-2-(pyridin-2-yl)methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one;
5-[5-(4-ethylpiperazin-1-ylsulphonyl)-2-(2-methoxyethoxy)pyridin-3-yl]-3-n-propyl-2-(pyridin-2-yl)methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one;
(+)-3-ethyl-5-[5-(4-ethylpiperazin-1-ylsulphonyl)-2-(2-methoxy-1(R)-methylethoxy)pyridin-3-yl]-2-methyl-2,6-dihydro-7-Hpyrazolo[4,3-d]pyrimidin-7-one;
3-ethyl-5-[5-(4-ethylpiperazin-1-ylsulphonyl)-2-(2-methoxy-1(R)-methylethoxy)pyridin-3-yl]-2-(6-methylpyridin-2-yl)methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one;
5-[2-ethoxy-5-(4-ethylpiperazin-1-ylsulphonyl)pyridin-3-yl]-3-ethyl-2-(6-methoxypyridin-2-yl)methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one;
5-[2-i-butoxy-5-(4-ethylpiperazin-1-ylsulphonyl)pyridin-3-yl]-2,3-diethyl-2,6-dihydro-7H-pyrazolo[[4,3-d]pyrimidin-7-one;
or 5-[2-ethoxy-5-(4-ethylpiperazin-1-ylsulphonyl)pyridin-3-yl]-3-ethyl-2-[1-pyridin-2-yl)ethyl]2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one or the pharmaceutically acceptable salts of said compounds.
- 3-ethyl-5-[5-(4-ethylpiperazin-1-ylsulphonyl)-2)2-methoxyethoxy)pyridin-3-yl]-2-(pyridin-2-yl)methyl-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one;
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22. A method as defined in claim 14 wherein said potassium channel opener is nicorandil or a pharmaceutically acceptable salt thereof.
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23. A method as defined in claim 14 which comprises (1) nicorandil;
- and (2) sildenafil or a pharmaceutically acceptable salt thereof.
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24. A method as defined in claim 14 wherein said potassium channel opener (1) is nicorandil or a pharmaceutically acceptable salt thereof and (2) is sidenafil citrate.
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25. A method for achieving a synergistic therapeutically effective level of treatment of female sexual dysfunction, comprising co-administering orally to a mammal in need of such treatment
(1) an amount of a first compound selected from potassium channel openers; - and
(2) an amount of a second compound selected from compounds which elevate cGMP levels;
wherein the amount of the first compound alone and the amount of the second compound alone is insufficient to achieve the synergistic therapeutically effective level of treatment of female sexual dysfunction, but wherein the combined effect of the amounts of the first and second compounds is greater than the sum of the levels of therapeutic effects of female sexual dysfunction treatment achievable with the individual amounts of the first and second compound said first potassium channel opener compound is selected from the group consisting of nicorandil, cromokalim, leucromakalim, lemakalim, pinacidil, diazoxide, and minoxidil, or pharmaceutically acceptable salts thereof.
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Specification