US4217347A
Expired / Lapsed
US
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Method of treating hypertension and medicaments therefor
Assignee: ER Squibb and Sons LLC
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Filing: 1978-11-09
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Granted: 1980-08-12
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Expires: 1998-11-09
Abstract
Abstract A method for reducing blood pressure comprises administering a combination of a diuretic compound and a compound having the general formula <IMAGE>
Inventors
- 👤 Zola P. Horovitz
- 👤 Bernard Rubin
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 06:21
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/495; A61K31/505; A61K31/40; A61K31/54; A61K31/56; A61K31/58; A61K31/585; A61K31/63; A61K31/635
Claims Analysis
Total Claims: 29
Claim 1
Independent Claim
131 words
A method for reducing blood pressure which comprises orally administering to a mammalian species having elevated blood pressure a daily dosage of a combination comprising about 30 to 600 mg. of a compound having the formula ##STR3## wherein: R is hydroxy, lower alkoxy or NH 2 ; R 1 and R 4 each is hydrogen, lower alkyl or phenyl-lower alkyl; R 2 is hydrogen or R 5 -CO; R 3 is hydrogen, hydroxy or lower alkyl; R 5 is lower alkyl, phenyl or phenyl-lower alkyl; and n is 0, 1 or 2 and about 15 to 300 mg. of a diuretic selected from the group consisting of chlorothiazide, hydrochlorothiazide, flumethiazide, amiloride, hydroflumethiazide, bendroflumethiazide, methyclothiazide, trichlormethiazide, polythiazide, benzthiazide, ethacrynic acid, ticrynafen, chlorthalidone, furosemide, bumetanide, triamterene and spironolactone or salts of said compounds.
Claim 2
Independent Claim
131 words
A method for reducing blood pressure which comprises orally administering to a mammalian species having elevated blood pressure a daily dosage of a combination comprising about 30 to 600 mg. of a compound having the formula ##STR3## wherein: R is hydroxy, lower alkoxy or NH 2 ; R 1 and R 4 each is hydrogen, lower alkyl or phenyl-lower alkyl; R 2 is hydrogen or R 5 -CO; R 3 is hydrogen, hydroxy or lower alkyl; R 5 is lower alkyl, phenyl or phenyl-lower alkyl; and n is 0, 1 or 2 and about 15 to 300 mg. of a diuretic selected from the group consisting of chlorothiazide, hydrochlorothiazide, flumethiazide, amiloride, hydroflumethiazide, bendroflumethiazide, methyclothiazide, trichlormethiazide, polythiazide, benzthiazide, ethacrynic acid, ticrynafen, chlorthalidone, furosemide, bumetanide, triamterene and spironolactone or salts of said compounds.
Claim 3
Dependent Claim
30 words
A method as in claim 1 wherein the combination comprises about 30 to 300 mg. of the compound of the formula and about 15 to 200 mg. of the diuretic.
Claim 4
Dependent Claim
52 words
A method as in claim 1 wherein the compound of the formula has R as hydroxy or lower alkoxy; R 1 as hydrogen or lower alkyl; R 2 as hydrogen or lower alkanoyl; R 3 as hydrogen or hydroxy; R 4 as hydrogen or lower alkyl; and n as 0 or 1.
Claim 5
Dependent Claim
44 words
A method as in claim 1 wherein the compound of the formula has R as hydroxy; R 1 as hydrogen or methyl; R 2 as hydrogen or acetyl; R 3 as hydrogen; R 4 as hydrogen or methyl; and n as 0 or 1.
Claim 6
Dependent Claim
16 words
A method as in claim 1 wherein the diuretic is chlorothiazide, hydrochlorothiazide, furosemide, ticrynafen or triameterene.
Claim 7
Dependent Claim
13 words
A method as in claim 1 wherein the diuretic is hydrochlorothiazide or furosemide.
Claim 8
Dependent Claim
62 words
A method as in claim 1 wherein the compound of the formula has R as hydrogen or lower alkoxy; R 1 as hydrogen or lower alkyl; R 2 as hydrogen or lower alkanoyl; R 3 as hydrogen or hydroxy; R 4 as hydrogen or lower alkyl; and n as 0 or 1; and the diuretic is chlorothiazide, hydrochlorothiazide, furosemide, ticrynafen or triamterene.
Claim 9
Dependent Claim
68 words
A method as in claim 1 comprising about 30 to 300 mg. of a compound of the formula wherein R is hydroxy or lower alkoxy; R 1 and R 4 each is hydrogen or lower alkyl; R 2 is hydrogen or lower alkanoyl, R 3 is hydrogen or hydroxy; and n is 0 or 1, and about 15 to 200 mg. of chlorothiazide, hydrochlorothiazide, furosemide, ticrynafen or triamterene.
Claim 10
Dependent Claim
21 words
A method as in claim 1 wherein the compound of the formula is (D-3-mercapto-2-methylpropanoyl)-L-proline and the diuretic is hydrochlorothiazide or furosemide.
Claim 11
Dependent Claim
37 words
A method as in claim 1 wherein the compound of the formula is (D-3-mercapto-2-methylpropanoyl)-L-proline in an amount of about 30 to 300 mg. and the diuretic is hydrochlorothiazide in an amount of about 15 to 200 mg.
Claim 12
Dependent Claim
37 words
A method as in claim 1 wherein the compound of the formula is (D-3-mercapto-2-methylpropanoyl)-L-proline in an amount of about 30 to 300 mg. and the diuretic is furosemide in an amount of about 15 to 200 mg.
Claim 13
Dependent Claim
112 words
An oral antihypertensive composition comprising about 30 to 600 mg. of a compound of the formula ##STR4## wherein: R is hydroxy, lower alkoxy or NH 2 ; R 1 and R 4 each is hydrogen, lower alkyl or phenyl-lower alkyl; R 2 is hydrogen or R 5 -CO; R 3 is hydrogen, hydroxy or lower alkyl; R 5 is lower alkyl, phenyl or phenyl-lower alkyl; n is 0, 1 or 2, about 15 to 300 mg. of a diuretic selected from the group consisting of chlorothiazide, hydrochlorothiazide, amiloride, flumethiazide, hydroflumethiazide, bendroflumethiazide, methylclothiazide, trichlormethiazide, polythiazide, benzthiazide, ethacrynic acid, ticrynafen, chlorthalidone, furosemide, bumetanide, triamterene, spironolactone and salts thereof, and a physiologically acceptable carrier therefor.
Claim 14
Dependent Claim
112 words
An oral antihypertensive composition comprising about 30 to 600 mg. of a compound of the formula ##STR4## wherein: R is hydroxy, lower alkoxy or NH 2 ; R 1 and R 4 each is hydrogen, lower alkyl or phenyl-lower alkyl; R 2 is hydrogen or R 5 -CO; R 3 is hydrogen, hydroxy or lower alkyl; R 5 is lower alkyl, phenyl or phenyl-lower alkyl; n is 0, 1 or 2, about 15 to 300 mg. of a diuretic selected from the group consisting of chlorothiazide, hydrochlorothiazide, amiloride, flumethiazide, hydroflumethiazide, bendroflumethiazide, methylclothiazide, trichlormethiazide, polythiazide, benzthiazide, ethacrynic acid, ticrynafen, chlorthalidone, furosemide, bumetanide, triamterene, spironolactone and salts thereof, and a physiologically acceptable carrier therefor.
Claim 15
Dependent Claim
27 words
A composition as in claim 12 comprising about 30 to 300 mg. of the compound of the formula and about 15 to 200 mg. of the diuretic.
Claim 16
Dependent Claim
52 words
A composition as in claim 12 wherein the compound of the formula has R as hydroxy or lower alkoxy; R 1 as hydrogen or lower alkyl; R 2 as hydrogen or lower alkanoyl; R 3 as hydrogen or hydroxy; R 4 as hydrogen or lower alkyl; and n as 0 or 1.
Claim 17
Dependent Claim
44 words
A composition as in claim 12 wherein the compound of the formula has R as hydroxy; R 1 as hydrogen or methyl; R 2 as hydrogen or acetyl; R 3 as hydrogen; R 4 as hydrogen or methyl; and n as 0 or 1.
Claim 18
Dependent Claim
16 words
A composition as in claim 12 wherein the diuretic is chlorothiazide, hydrochlorothiazide, furosemide, ticrynafen or triamterene.
Claim 19
Dependent Claim
13 words
A composition as in claim 12 wherein the diuretic is hydrochlorothiazide or furosemide.
Claim 20
Dependent Claim
62 words
A composition as in claim 12 wherein the compound of the formula has R as hydrogen or lower alkoxy; R 1 as hydrogen or lower alkyl; R 2 as hydrogen or lower alkanoyl; R 3 as hydrogen or hydroxy; R 4 as hydrogen or lower alkyl; and n as 0 or 1; and the diuretic is chlorothiazide, hydrochlorothiazide, furosemide, ticrynafen or triamterene.
Claim 21
Dependent Claim
21 words
A composition as in claim 12 wherein the compound of the formula is (D-3-mercapto-2-methyl-propanoyl)-L-proline and the diuretic is hydrochlorothiazide or furosemide.
Claim 22
Dependent Claim
22 words
A composition as in claim 12 comprising about 30 to 300 mg. of (D-3-mercapto-2-methylpropanoyl)-L-proline and about 15 to 200 mg. of hydrochlorothiazide.
Claim 23
Dependent Claim
22 words
A composition as in claim 13 comprising about 30 to 300 mg. of (D-3-mercapto-2-methylpropanoyl)-L-proline and about 15 to 200 mg. of furosemide.
Claim 24
Dependent Claim
22 words
A composition as in claim 25 comprising about 5 to 125 mg. of (D-3-mercapto-2-methylpropanoyl)-L-proline and about 2.5 to 50 mg. of hydrochlorothiazide.
Claim 25
Dependent Claim
22 words
A composition as in claim 25 comprising about 5 to 125 mg. of (D-3-mercapto-2-methylpropanoyl)-L-proline and about 2.5 to 50 mg. of furosemide.
Claim 26
Dependent Claim
20 words
An oral hypertensive composition comprising about 5 to 125 mg. of (D-3-mercapto-2-methylpropanoyl)-L-proline and about 5 to 75 mg. of triamterene.
Claim 27
Dependent Claim
20 words
An oral hypertensive composition comprising about 5 to 125 mg. of (D-3-mercapto-2-methylpropanoyl)-L-proline and about 5 to 75 mg. of triamterene.
Claim 28
Dependent Claim
113 words
An oral antihypertensive composition comprising about 5 to 125 mg. of a compound of the formula ##STR5## wherein: R is hydroxy, lower alkoxy or NH 2 ; R 1 and R 4 each is hydrogen, lower alkyl or phenyl-lower alkyl; R 2 is hydrogen or R 5 -CO; R 3 is hydrogen, hydroxy or lower alkyl; R 5 is lower alkyl, phenyl or phenyl-lower alkyl; and n is 0, 1 or 2, about 2.5 to 50 mg. of a diuretic selected from the group consisting of chlorothiazide, hydrochlorothiazide, amiloride, flumethiazide, hydroflumethiazide, bendroflumethiazide, methylclothiazide, trichlormethiazide, polythiazide, benzthiazide, ethacrynic acid, ticrynafen, chlorthalidone, furosemide, bumetanide, triamterene, spironolactone and salts thereof, and a physiologically acceptable carrier therefor.
Claim 29
Dependent Claim
113 words
An oral antihypertensive composition comprising about 5 to 125 mg. of a compound of the formula ##STR5## wherein: R is hydroxy, lower alkoxy or NH 2 ; R 1 and R 4 each is hydrogen, lower alkyl or phenyl-lower alkyl; R 2 is hydrogen or R 5 -CO; R 3 is hydrogen, hydroxy or lower alkyl; R 5 is lower alkyl, phenyl or phenyl-lower alkyl; and n is 0, 1 or 2, about 2.5 to 50 mg. of a diuretic selected from the group consisting of chlorothiazide, hydrochlorothiazide, amiloride, flumethiazide, hydroflumethiazide, bendroflumethiazide, methylclothiazide, trichlormethiazide, polythiazide, benzthiazide, ethacrynic acid, ticrynafen, chlorthalidone, furosemide, bumetanide, triamterene, spironolactone and salts thereof, and a physiologically acceptable carrier therefor.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-08-12 | 1984-02-11 | 1984-08-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-08-12 | 1988-02-11 | 1988-08-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-08-12 | 1992-02-11 | 1992-08-12 | $7700.00 | Window Closed / Lapsed |