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WO1993020819A1 - Traitement de la vidange gastrique retardee - Google Patents

Traitement de la vidange gastrique retardee Download PDF

Info

Publication number
WO1993020819A1
WO1993020819A1 PCT/EP1993/000781 EP9300781W WO9320819A1 WO 1993020819 A1 WO1993020819 A1 WO 1993020819A1 EP 9300781 W EP9300781 W EP 9300781W WO 9320819 A1 WO9320819 A1 WO 9320819A1
Authority
WO
WIPO (PCT)
Prior art keywords
gastric emptying
treatment
diphenylmethoxy
piperidine
prevention
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.)
Ceased
Application number
PCT/EP1993/000781
Other languages
English (en)
Inventor
Robert Michael Wallis
Stephen Alaric Williams
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.)
Pfizer Corp Belgium
Pfizer Ltd Great Britain
Pfizer Research and Development Co NV SA
Pfizer Inc
Original Assignee
Pfizer Corp Belgium
Pfizer Ltd Great Britain
Pfizer Research and Development Co NV SA
Pfizer Inc
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 Pfizer Corp Belgium, Pfizer Ltd Great Britain, Pfizer Research and Development Co NV SA, Pfizer Inc filed Critical Pfizer Corp Belgium
Publication of WO1993020819A1 publication Critical patent/WO1993020819A1/fr
Anticipated expiration legal-status Critical
Ceased 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine

Definitions

  • This invention relates to treatment of medical conditions associated with delayed gastric emptying using 3R- or 3R,S-diphenylmethoxy-l-(3,4- - methylenedioxyphenethyl)piperidine, a compound disclosed in European Patent Application EP-A-0350309.
  • Diphenylmethoxy-1-(3 ,4-methylenedioxyphenethyl)- piperidine is of formula (I) :
  • the dose required for treating the above-mentioned diseases is typically 3.5 to 350 mg daily for an average human adult weighing 70 kg. It is known that muscarinic receptor antagonists, besides inhibiting small and large bowel motility, also tend to inhibit gastric emptying. Antagonists for which this effect has been discussed in the literature include propantheline (Hurwitz, Robinson and Herrin, 1977, Clin. Pharmacol. Therap. 2.206-210) , pirenzepine (Soffer, Kumar r Mridha, Das-Gupta r Britto and Wingate, 1988, Gastroenterol. 23.146-150) , atropine (Rashid and Bateman, 1990, Br. J. Clin. Pharmacol.
  • 3R and 3R,S-diphenylmethoxy-1-(3,4-methylenedioxyphenethyl)- piperidine are capable of increasing gastric emptying rates when administered to patients at doses within the range which are likely to be used for treatment as muscarinic receptor antagonists.
  • This effect which is quite contrary to what might have been expected from existing knowledge , renders this compound suitable for the treatment of a number of conditions in patients for whom inhibition of gastric emptying is undesirable. These conditions include non-ulcer dyspepsia, neurogenic and non-neurogenic gastroparesis, idiopathic delayed gastric emptying, gastro-oesophageal reflux, nausea and vomiting.
  • UK-76,654 has a significant effect in increasing gastric emptying rate of doses within or less than the range of 3.5-350 mg, particularly at doses around the 10 mg level.
  • the dose administered for treatment of non-ulcer dyspepsia, gastroparesis, ideopathic delayed gastric emptying, gastro-oesophageal reflux, nausea and vomiting will be determined by a physician bearing in mind the age, weight, response and medical history of the patient but for average adults (70 kg) it is likely to be in the range of 1 to 100 mg.
  • 3R- or 3R,S-diphenylmethoxy-l-(3,4- methylenedioxyphenethyl)piperidine or its acid addition salts may be administered alone but will generally be administered in admixture with a pharmaceutical carrier selected with regard to the intended route of administration and standard pharmaceutical practice.
  • a pharmaceutical carrier selected with regard to the intended route of administration and standard pharmaceutical practice.
  • they may be administered orally in the form of tablets containing excipients such as starch or lactose or in capsules or ovules either alone or in combination with excipients or in the form of elixirs or suspensions containing flavouring or colouring agents.
  • They may be injected parenterally, for example, intravenously, intramuscularly or subcutaneously.
  • one aspect of the invention comprises 3R- or 3R r S-diphenylmethoxy-1-(3,4-methylenedioxyphenethyl)- piperidine, or a pharmaceutically acceptable acid addition salt thereof, for use in the treatment of conditions requiring antagonism of muscarinic receptors and increase, or prevention of reduction, in gastric emptying.
  • the invention also provides a method of treating conditions requiring antagonism of muscarinic receptors and increase, or prevention of reduction, in gastric emptying, which comprises adminstering to the patient an effective amount of 3R- or 3R,S-diphenylmethoxy-l-(3,4- methylenedioxyphenethyl)piperidine or a pharmaceutically acceptable salt thereof.
  • the above-mentioned conditions include non-ulcer dyspepsia, gastroparesis, idiopathic delayed gastric emptying, gastro-oesophageal reflux r nausea and vomiting.

Landscapes

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

Abstract

Utilisation de 3R et de 3R,S-diphénylméthoxy-1-(3,4-méthylènedioxyphénéthyle)-pipéridine pour traiter des états nécessitant l'antagonisme des récepteurs muscariniques et l'intensification, ou la prévention de la réduction de la vidange gastrique.
PCT/EP1993/000781 1992-04-14 1993-03-29 Traitement de la vidange gastrique retardee Ceased WO1993020819A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB929208230A GB9208230D0 (en) 1992-04-14 1992-04-14 Treatment of delayed gastric emptying
GB9208230.4 1992-04-14

Publications (1)

Publication Number Publication Date
WO1993020819A1 true WO1993020819A1 (fr) 1993-10-28

Family

ID=10714037

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1993/000781 Ceased WO1993020819A1 (fr) 1992-04-14 1993-03-29 Traitement de la vidange gastrique retardee

Country Status (7)

Country Link
AU (1) AU3891093A (fr)
GB (1) GB9208230D0 (fr)
IL (1) IL105313A0 (fr)
MX (1) MX9302142A (fr)
TW (1) TW219331B (fr)
WO (1) WO1993020819A1 (fr)
ZA (1) ZA932583B (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5561127A (en) * 1994-12-19 1996-10-01 Allelix Biopharmaceuticals, Inc. Muscarinic receptor ligands
WO2008144602A1 (fr) * 2007-05-18 2008-11-27 Auspex Pharmaceuticals, Inc. Dérivés de zamifénacine deutérés
US8152821B2 (en) 2000-03-03 2012-04-10 C.R. Bard, Inc. Endoscopic tissue apposition device with multiple suction ports
US9149270B2 (en) 2004-08-27 2015-10-06 Davol, Inc. (a C.R. Bard Company) Endoscopic tissue apposition device and method of use

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0350309A1 (fr) * 1988-07-08 1990-01-10 Pfizer Limited Dérivés de pipéridine

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0350309A1 (fr) * 1988-07-08 1990-01-10 Pfizer Limited Dérivés de pipéridine

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
BR. J. PHARMACOL. vol. 30, 1990, pages 839 - 845 STACHER ET AL. 'Fat preload delays gastric emptying: reversal by cisapride' cited in the application *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5561127A (en) * 1994-12-19 1996-10-01 Allelix Biopharmaceuticals, Inc. Muscarinic receptor ligands
US5674877A (en) * 1994-12-19 1997-10-07 Allelix Biopharmaceuticals Inc. Muscarinic receptor ligands
US8152821B2 (en) 2000-03-03 2012-04-10 C.R. Bard, Inc. Endoscopic tissue apposition device with multiple suction ports
US9149270B2 (en) 2004-08-27 2015-10-06 Davol, Inc. (a C.R. Bard Company) Endoscopic tissue apposition device and method of use
WO2008144602A1 (fr) * 2007-05-18 2008-11-27 Auspex Pharmaceuticals, Inc. Dérivés de zamifénacine deutérés

Also Published As

Publication number Publication date
IL105313A0 (en) 1993-08-18
ZA932583B (en) 1994-10-13
TW219331B (fr) 1994-01-21
AU3891093A (en) 1993-11-18
MX9302142A (es) 1994-05-31
GB9208230D0 (en) 1992-05-27

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