GB979680A - Pharmaceutical compositions containing esters of quaternary atropinium salts - Google Patents

Pharmaceutical compositions containing esters of quaternary atropinium salts

Info

Publication number
GB979680A
GB979680A GB43882/62A GB4388262A GB979680A GB 979680 A GB979680 A GB 979680A GB 43882/62 A GB43882/62 A GB 43882/62A GB 4388262 A GB4388262 A GB 4388262A GB 979680 A GB979680 A GB 979680A
Authority
GB
United Kingdom
Prior art keywords
anion
aralkyl
physiologically acceptable
acid
halide
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.)
Expired
Application number
GB43882/62A
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.)
Schwarz Arzneimittelfabrik G M
Original Assignee
Schwarz Arzneimittelfabrik G M
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 Schwarz Arzneimittelfabrik G M filed Critical Schwarz Arzneimittelfabrik G M
Publication of GB979680A publication Critical patent/GB979680A/en
Expired legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms
    • C07D451/10—Oxygen atoms acylated by aliphatic or araliphatic carboxylic acids, e.g. atropine, scopolamine

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Compounds of formula <FORM:0979680/C1/1> wherein R1 is an aliphatic acyl radical having 2 to 5 carbon atoms, R2 is an aralkyl radical, and X- is the anion of a physiologically acceptable acid, are prepared by either (1) esterifying the hydroxyl group of an atropine salt, preferably the hydrobromide, with an acid anhydride, converting the product to the free base, and quaternising the nitrogen atom with an aralkyl halide, or (ii) quaternising atropine with an aralkyl halide and then esterifying with an acid anhydride; in either case the halide anion may be replaced by that of another physiologically compatible acid. In specific examples R1 is an acetyl or propionyl group and R2 is a p-bromobenzyl or 4-biphenylylmethyl group. Specification 808,926 is referred to.ALSO:The invention comprises pharmacological preparations containing compounds of formula <FORM:0979680/A5-A6/1> (see Division C2) wherein R1 is an aliphatic acyl radical having 2 to 5 carbon atoms, R2 is an aralkyl radical, and X- is the anion of a physiologically acceptable acid, in combination with a physiologically acceptable carrier. Specified groups R2 are 4-biphenylylmethyl and 4-bromobenzyl groups. The active compounds have ganglion-blocking action, and the compositions may be used in forms suitable for oral or parenteral administration, e.g. tablets or ampoules. An exemplified composition also contains ethyl urethane. Specification 808,926 is referred to.
GB43882/62A 1961-11-21 1962-11-20 Pharmaceutical compositions containing esters of quaternary atropinium salts Expired GB979680A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE1961SC030593 DE1165037B (en) 1961-11-21 1961-11-21 Process for the preparation of esters of quaternary atropinium salts.

Publications (1)

Publication Number Publication Date
GB979680A true GB979680A (en) 1965-01-06

Family

ID=7431805

Family Applications (1)

Application Number Title Priority Date Filing Date
GB43882/62A Expired GB979680A (en) 1961-11-21 1962-11-20 Pharmaceutical compositions containing esters of quaternary atropinium salts

Country Status (3)

Country Link
DE (1) DE1165037B (en)
FR (1) FR1950M (en)
GB (1) GB979680A (en)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019087146A1 (en) * 2017-11-03 2019-05-09 Novartis Ag Azabicyclo and diazepine derivatives for treating ocular disorders
RU2795521C2 (en) * 2017-11-03 2023-05-04 Алькон Инк. Azabicyclic and diazepine derivatives for the treatment of ophthalmic disorders
EP3989935A4 (en) * 2019-07-30 2023-07-26 Cellix Bio Private Limited Composition and methods for the treatment of anal and rectal disorders

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL128810C (en) * 1964-10-27
DE1950378C2 (en) * 1969-02-18 1985-10-03 Eisai K.K., Tokio/Tokyo Quaternary atropinium and hyoscyaminium salts

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE937895C (en) * 1952-08-21 1956-01-19 Drug Houses Of Australia Ltd Process for the preparation of therapeutically valuable acyl derivatives of hyoscine (ú ¢ scopolamine) or atroscine (ú ¢ dl-hyoscine) or their salts
DE1062704B (en) * 1956-08-07 1959-08-06 Licencia Talalmanyokat Process for the production of quaternary atropines

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019087146A1 (en) * 2017-11-03 2019-05-09 Novartis Ag Azabicyclo and diazepine derivatives for treating ocular disorders
AU2018362010B2 (en) * 2017-11-03 2021-05-13 Alcon Inc. Azabicyclo and diazepine derivatives for treating ocular disorders
US11306090B2 (en) 2017-11-03 2022-04-19 Alcon Inc. Azabicyclo and diazepine derivatives
RU2795521C2 (en) * 2017-11-03 2023-05-04 Алькон Инк. Azabicyclic and diazepine derivatives for the treatment of ophthalmic disorders
EP3989935A4 (en) * 2019-07-30 2023-07-26 Cellix Bio Private Limited Composition and methods for the treatment of anal and rectal disorders

Also Published As

Publication number Publication date
DE1165037B (en) 1964-03-12
FR1950M (en) 1963-08-05

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