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Papaverine thienyl-carboxylates and medicaments containing them

Assignee: Choay SA
•
Filing: 1975-01-15
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Granted: 1977-10-25
•
Expires: 1995-01-15
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Abstract

Abstract Novel salts of papaverine are constituted by the thienyl-carboxylates of papaverine notably papaverine thienyl-2-carboxylate. A papaverine thienyl-carboxylate is prepared by reacting papaverine base with the corresponding thiophene carboxylic acid. The medicaments comprise, as active principle, a papaverine thienyl-carboxylate associated with a solid excipient making it suitable for administration by the oral route, or with an excipient making it suitable for administration by the rectal route. The medicament, is useful for the treatment of hyperspasmodicity of the smooth muscles, and for the treatment of vascular disorders, notably due to senescence, more particularly those bringing into action cortical reactivity.

Inventors

  • 👤 Edgar Sache

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-25 07:54
CPC Classifications
C; C07; C07D; C07D333/00; C07D333/02; C07D333/04; C07D333/26; C07D333/38; C07D217/00; C07D217/12; C07D217/18; C07D217/20

Claims Analysis

Total Claims: 21
Claim 1
Independent Claim 14 words
The papaverine compounds selected from the group consisting of: papaverine thienyl-2-carboxylate and papaverine thienyl-3-carboxylate.
Claim 2
Dependent Claim 14 words
The papaverine compounds selected from the group consisting of: papaverine thienyl-2-carboxylate and papaverine thienyl-3-carboxylate.
Claim 3
Dependent Claim 2 words
Papaverine thienyl-2-carboxylate.
Claim 4
Dependent Claim 2 words
Papaverine thienyl-2-carboxylate.
Claim 5
Dependent Claim 2 words
Papaverine thienyl-3-carboxylate.
Claim 6
Dependent Claim 2 words
Papaverine thienyl-3-carboxylate.
Claim 7
Dependent Claim 33 words
Medicament comprising, a pharmaceutically acceptable carrier and as active principle in a therapeutically effective amount, for the treatment of hyperspasmodicity of smooth muscles and vascular disorders, a papaverine thienyl-carboxylate according to claim 1.
Claim 8
Dependent Claim 21 words
Medicament according to claim 4, wherein the papaverine thienyl-carboxylate is associated with a solid excipient making it suitable for oral administration.
Claim 9
Dependent Claim 20 words
Medicament according to claim 4, wherein the papaverine thienyl-carboxylate is associated with an excipient making it suitable for rectal administration.
Claim 10
Dependent Claim 25 words
Method for the treatment of hyperspasmodicity of the smooth muscles, in a non-human animal, comprising administering to the animal a medicament, according to claim 4.
Claim 11
Dependent Claim 26 words
Method for the treatment of vascular disorders and promoting cortical reactivity, in a non-human animal, comprising administering to the animal, a medicament, according to claim 4.
Claim 12
Dependent Claim 36 words
Method for treating hyperspasmodicity of the smooth muscles or disorders of platelet adhesivity or disturbance of cerebral electrogenesis resulting from vascular disorders comprising administering an effective amount of a thienyl-carboxylate of papaverine according to claim 1.
Claim 13
Dependent Claim 26 words
Method of treatment according to claim 9, wherein said thienyl-carboxylate of papaverine is administered at the rate of about 125 to 750 mg per daily dose.
Claim 14
Dependent Claim 30 words
A pharmaceutical composition comprising the papaverine of claim 2 in a therapeutically effective amount, for the treatment of hyperspasmodicity of smooth muscles and vascular disorders, and a pharmaceutically acceptable carrier.
Claim 15
Dependent Claim 37 words
The method of treatment of vascular disorders which comprises administering the composition of claim 11 to the subject in a daily dosage of about 90 to 500mg of the papaverine (calculated on the basis of the base).
Claim 16
Dependent Claim 7 words
The solid pharmaceutical composition of claim 11.
Claim 17
Dependent Claim 30 words
The solution of the product of claim 2 which is an isotonic chloride solution containing 1% methanol having the proportion of 13mg of papaverine thienyl-2-carboxylate per 100 ml of solution.
Claim 18
Dependent Claim 17 words
The method of claim 9 wherein the administration is for control of hyperspasmodicity of the smooth muscles.
Claim 19
Dependent Claim 16 words
The method of claim 9 wherein the administration is for control of disorders of platelet adhesivity.
Claim 20
Dependent Claim 18 words
The method of claim 9 wherein the administration is for control of cerebral electrogenesis caused by vascular disorders.
Claim 21
Dependent Claim 16 words
The method of claim 17 wherein the administration is for control of cerebral electrogenesis by senescence.

References Cited (Backward Citations)

US2027722A Cited
US2507086A Cited
US3823234A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-10-24 1981-04-25 1981-10-25 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-10-24 1985-04-25 1985-10-25 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-10-24 1989-04-25 1989-10-25 $7700.00 Window Closed / Lapsed

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