US3400203A - Treatment of parkinsonism in humans with nu, nu-diphenyl carbamates of alkylaminoalkanols - Google Patents

Treatment of parkinsonism in humans with nu, nu-diphenyl carbamates of alkylaminoalkanols Download PDF

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Publication number
US3400203A
US3400203A US456808A US45680865A US3400203A US 3400203 A US3400203 A US 3400203A US 456808 A US456808 A US 456808A US 45680865 A US45680865 A US 45680865A US 3400203 A US3400203 A US 3400203A
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US
United States
Prior art keywords
parkinsonism
treatment
humans
carbamates
alkylaminoalkanols
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Expired - Lifetime
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US456808A
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English (en)
Inventor
Stille Gunther
Theodor J Wagner-Jauregg
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Siegfried AG
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Siegfried AG
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Publication date
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Publication of US3400203A publication Critical patent/US3400203A/en
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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids

Definitions

  • Thls ⁇ m/entlon relates to a methPd of treatlng Parkm each of the following carbamates of the above listed sonism in humans and more particularly relates to the alkylammoalkanols;
  • a high figure indicates low mydriasis (undesired side effect).
  • a high figure is R2 an expression for high antitremor activity combined with wherein R and R are the same or difierent groups sea low undesired side effect.
  • R with orphenadrin further demonstrates that in this field and R are phenyl, R and R are methyl or ethyl and structural resemblance does not enable prediction of a 3 specific kind of biological activity.
  • R phenyl
  • R and R are methyl or ethyl and structural resemblance does not enable prediction of a 3 specific kind of biological activity.
  • its lower homologue containing two methyl groups instead of the two ethyls of SD-25, is a particularly effective antitremorine agent.
  • the compound SD-25 is known in the literature approximately since 50 years and its local anesthetic effect and other pharamadocynamic properties have been described. Sekera and Vrba (Arc. Int., Pharmacodyn, 125, 316, 1960) state that their S-25 (identical with our SD-25) possesses 0.5-1 times the anticholinergic action of the well known spasmolytic agent Trasentine.
  • Trasentine is a mainly musculotropically acting, ie a papaverinelike antispasmodic; it is evaluated in general against BaCI -induced spasms.
  • the acid when isolating any of the compounds of Formula I in the form of an acid addition salt, the acid is preferably selected so as to contain an anion which is non-toxic and pharmacologically acceptable at least in usual therapeutic doses.
  • Representative acid addition salts are hydrochlorides, hydrobromides, sulphates, phosphates, nitrates, acetates, lactates, maleates, citrates, tartrates and bitart-rates, succinates, oxalates, methanesulphonates and ethanesulphonates.
  • Other acid addition salts are likewise suitable and may be employed if desired.
  • SD- [gamm a- (N-methyl piperazino) -propyl] -phenothiazin- 2-sulfonic acid dimethylamide (thioperazin) are administered to patients (medicamental parkinsonism).
  • SD- can be administered either together with the neuroleptic agent, afterwards or even before.
  • SD-25 is well tolerated and no deleterious effects have been observed, even when the drug was given for more than one year.
  • the patients do not complain of dryness of the mouth or other side effects, which frequently are observed when other antiparkinson remedies are administered.
  • SD-25 can be given perorally and parenterally (intravenously or intramuscularly) in average doses of 15 to 50 mg., 2-4 times p.d. It is possible to inject it i.v. re-
  • a 1-3%, preferably 2.5% aqueous solution, containing 25 mg. of SD-25 per ml. is generally used.
  • the optimal dose is individually different and can be ascertained by the physician for singular cases.
  • compositions used in the present invention can be brought into a unit dosage form by any suitable technique known to the man skilled in the art.
  • a typical example of a method to prepare tablets containing the preferred 2-diethylaminoethyl-N-diphenylcarbamate will be given below: p I
  • any other suitable carriers such as talc, mannose, corn starch, magnesium stearate, etc.
  • a method of treating parkinsonism in human comprising administering to said humans afflicted with parkinsonism an effective amount of a compound selected from the group consisting of compounds having the following formula and pharmaceutically acceptable acid addition salts thereof wherein R and R are phenyl, R is lower alkylene and R and R independently are lower'alkyl.
  • R and R are independently selected from the group consisting of methyl and ethyl.
  • a method according to claim'4 wherein the compound is administered 2-4 times per day in a dosage unit between about 15 and 50 mg. of the compound.

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Emergency Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
US456808A 1961-03-29 1965-05-18 Treatment of parkinsonism in humans with nu, nu-diphenyl carbamates of alkylaminoalkanols Expired - Lifetime US3400203A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH370961A CH405266A (de) 1961-03-29 1961-03-29 Verfahren zur Herstellung von als Antiparkinsonmittel verwendbaren Verbindungen
US18335662A 1962-03-29 1962-03-29

Publications (1)

Publication Number Publication Date
US3400203A true US3400203A (en) 1968-09-03

Family

ID=55539354

Family Applications (1)

Application Number Title Priority Date Filing Date
US456808A Expired - Lifetime US3400203A (en) 1961-03-29 1965-05-18 Treatment of parkinsonism in humans with nu, nu-diphenyl carbamates of alkylaminoalkanols

Country Status (4)

Country Link
US (1) US3400203A (enExample)
BE (1) BE630069A (enExample)
CH (1) CH405266A (enExample)
FR (1) FR2704M (enExample)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996008468A1 (en) * 1994-09-14 1996-03-21 H. Lundbeck A/S Carbamoyloxy amine compounds

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
None *

Also Published As

Publication number Publication date
FR2704M (enExample) 1964-09-04
BE630069A (fr) 1963-07-15
CH405266A (de) 1966-01-15

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