FR2338044A1 - Glycero-phosphates of papaverine and ethaverine - have same musculotropic spasmolytic activity as free bases and hydrochlorides, but higher solubility - Google Patents

Glycero-phosphates of papaverine and ethaverine - have same musculotropic spasmolytic activity as free bases and hydrochlorides, but higher solubility

Info

Publication number
FR2338044A1
FR2338044A1 FR7600793A FR7600793A FR2338044A1 FR 2338044 A1 FR2338044 A1 FR 2338044A1 FR 7600793 A FR7600793 A FR 7600793A FR 7600793 A FR7600793 A FR 7600793A FR 2338044 A1 FR2338044 A1 FR 2338044A1
Authority
FR
France
Prior art keywords
alpha
ethaverine
hydrochlorides
glycerophosphate
degrees
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
FR7600793A
Other languages
French (fr)
Other versions
FR2338044B1 (en
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SOBIO LAB
Original Assignee
SOBIO LAB
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by SOBIO LAB filed Critical SOBIO LAB
Priority to FR7600793A priority Critical patent/FR2338044A1/en
Publication of FR2338044A1 publication Critical patent/FR2338044A1/en
Application granted granted Critical
Publication of FR2338044B1 publication Critical patent/FR2338044B1/fr
Granted legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/18—Aralkyl radicals
    • C07D217/20—Aralkyl radicals with oxygen atoms directly attached to the aromatic ring of said aralkyl radical, e.g. papaverine

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The alpha- and beta-glycerophosphates of papaverine and ethaverine are new. They have greater solubility then the free bases or hydrochlorides (>50% for the papering derivs. and 7% and 2.5% for the alpha- and beta-ethaverine derivs. esp.) They have reduced toxicity and the same musculotropic spasmolytic activity as the hydrochlorides. LD50 for ethererine alpha-glycerophosphate (i.v.) is 70 mg/kg compared with 51 for the hydrochloride. typical tables contain 100 mg ethererine beta-glycerophosphate. Dose is 1-4 tablets/day. In an example, an aq. soln. of alpha-glycerophosphoric acid (obtd. by treating disodium alpha-glycerophosphate with a strongly acid cationic resin) contg. 1/10 mole of acid in 1 l H2O was heated to 50 degrees C. It was mixed with a soln. of 1/10 mole papering in 400 ml ethanol, also at 50 degrees C. Prod. was filtered and conc. in vacuo at 50 degrees C. Recrystallisation from 400 ml hot 95% ethanol have papering alpha-glycerophosphate, m.pt. 110-120 degrees C.
FR7600793A 1976-01-14 1976-01-14 Glycero-phosphates of papaverine and ethaverine - have same musculotropic spasmolytic activity as free bases and hydrochlorides, but higher solubility Granted FR2338044A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
FR7600793A FR2338044A1 (en) 1976-01-14 1976-01-14 Glycero-phosphates of papaverine and ethaverine - have same musculotropic spasmolytic activity as free bases and hydrochlorides, but higher solubility

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR7600793A FR2338044A1 (en) 1976-01-14 1976-01-14 Glycero-phosphates of papaverine and ethaverine - have same musculotropic spasmolytic activity as free bases and hydrochlorides, but higher solubility

Publications (2)

Publication Number Publication Date
FR2338044A1 true FR2338044A1 (en) 1977-08-12
FR2338044B1 FR2338044B1 (en) 1980-04-30

Family

ID=9167892

Family Applications (1)

Application Number Title Priority Date Filing Date
FR7600793A Granted FR2338044A1 (en) 1976-01-14 1976-01-14 Glycero-phosphates of papaverine and ethaverine - have same musculotropic spasmolytic activity as free bases and hydrochlorides, but higher solubility

Country Status (1)

Country Link
FR (1) FR2338044A1 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004017971A1 (en) * 2002-08-08 2004-03-04 Ursapharm Arzneimittel Gmbh & Co. Kg Use of a papaverine-like vasodilator and pharmaceutical composition

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004017971A1 (en) * 2002-08-08 2004-03-04 Ursapharm Arzneimittel Gmbh & Co. Kg Use of a papaverine-like vasodilator and pharmaceutical composition

Also Published As

Publication number Publication date
FR2338044B1 (en) 1980-04-30

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