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US4131678A Expired / Lapsed US ⏱️ 0.0 years remaining

Urapidil/furosemide compounds, compositions and use

Assignee: Takeda GmbH
•
Filing: 1977-02-09
•
Granted: 1978-12-26
•
Expires: 1997-02-09
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Abstract

Abstract A combination of urapidil and furosemide, e.g., in the form of an acid-addition salt, in the form of a physical admixture or in the form of two distinct components collectively constitutes an effective active ingredient in the treatment of hypertension. The combination is advantageously incorporated in a standard dosage form and administered by various routes to mammals afflicted with high blood pressure. By combining furosemide with urapidil on one of the noted forms, the maximum hypotensive activity of urapidil is increased, while the side effects and toxicity of urapidil are reduced.

Inventors

  • 👤 Hermann Amschler
  • 👤 Kurt Klemm
  • 👤 Gerhard Ludwig

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-07 23:42
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/52; C07D239/54; C07D239/545; A; A61; A61P; A61P9/00; A61P9/12; C07D307/00; C07D307/02; C07D307/34; C07D307/38; C07D307/52

Claims Analysis

Total Claims: 17
Claim 1
Independent Claim 52 words
A first component which, in free-base form, is urapidil in combination with a second component which, in free form, is furosemide; the proportion of the second component being sufficient to increase the effectiveness of the first as a hypotensive agent and the combination of the two components being physiologically active and pharmacologically-acceptable.
Claim 2
Dependent Claim 52 words
A first component which, in free-base form, is urapidil in combination with a second component which, in free form, is furosemide; the proportion of the second component being sufficient to increase the effectiveness of the first as a hypotensive agent and the combination of the two components being physiologically active and pharmacologically-acceptable.
Claim 3
Dependent Claim 23 words
A combination according to claim 1 wherein the molar ratio of the first component to the second component is from 5:1 to 1:5.
Claim 4
Dependent Claim 17 words
A combination according to claim 1 wherein the second component is chemically combined with the first component.
Claim 5
Dependent Claim 17 words
A combination according to claim 3 in the form of the 1:1 furosemide acid-addition salt of urapidil.
Claim 6
Dependent Claim 23 words
A combination according to claim 1 wherein the molar ratio of the first component to the second component is from 3:1 to 1:3.
Claim 7
Dependent Claim 21 words
A physical combination according to claim 1 wherein the molar ratio of the first component to the second component is 1:1.
Claim 8
Dependent Claim 14 words
A combination according to claim 2 comprising a physical admixture of furosemide with urapidil.
Claim 9
Dependent Claim 27 words
A blood-pressure reducing medicament for subjects afflicted with hypertension and which comprises an effective concentration of a combination according to claim 1 and suitable diluent or excipient.
Claim 10
Dependent Claim 9 words
Medicament according to claim 8 in unit dosage form.
Claim 11
Dependent Claim 31 words
A pharmacologically-acceptable composition having a physiologically-active component and at least one component which is essentially therapeutically inactive, the active component comprising an effective concentration of a combination according to claim 1.
Claim 12
Dependent Claim 21 words
A process which comprises administering to a mammal afflicted with hypertension a blood-pressure-reducing amount of a combination according to claim 1.
Claim 13
Dependent Claim 12 words
A process according to claim 11 wherein the mammal is a human.
Claim 14
Dependent Claim 17 words
A process for reducing the toxicity of urapidil which comprises combining therewith a toxicity-reducing amount of furosemide.
Claim 15
Dependent Claim 17 words
A process for reducing the toxicity of urapidil which comprises combining therewith a toxicity-reducing amount of furosemide.
Claim 16
Dependent Claim 24 words
A process according to claim 13 which comprises physically combining furosemide with urapidil in a form in which the two are not chemically combined.
Claim 17
Dependent Claim 13 words
A process according to claim 13 which comprises chemically combining furosemide with urapidil.

References Cited (Backward Citations)

US3058882A Cited
US3957786A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1981-12-25 1982-06-26 1982-12-26 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1985-12-25 1986-06-26 1986-12-26 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1989-12-25 1990-06-26 1990-12-26 $7700.00 Window Closed / Lapsed

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