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WO2008030524A3 - Formulations pharmaceutiques liquides pour l'administration orale d'un antagoniste du cgrp - Google Patents

Formulations pharmaceutiques liquides pour l'administration orale d'un antagoniste du cgrp Download PDF

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Publication number
WO2008030524A3
WO2008030524A3 PCT/US2007/019461 US2007019461W WO2008030524A3 WO 2008030524 A3 WO2008030524 A3 WO 2008030524A3 US 2007019461 W US2007019461 W US 2007019461W WO 2008030524 A3 WO2008030524 A3 WO 2008030524A3
Authority
WO
WIPO (PCT)
Prior art keywords
oral administration
pharmaceutical formulations
liquid pharmaceutical
cgrp antagonist
oxo
Prior art date
Application number
PCT/US2007/019461
Other languages
English (en)
Other versions
WO2008030524A2 (fr
Inventor
David Breslin
Joyce Stellabott
Hossain Jahansouz
Laman L Alani
Karen Thompson
Original Assignee
Merck & Co Inc
David Breslin
Joyce Stellabott
Hossain Jahansouz
Laman L Alani
Karen Thompson
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 Merck & Co Inc, David Breslin, Joyce Stellabott, Hossain Jahansouz, Laman L Alani, Karen Thompson filed Critical Merck & Co Inc
Priority to AU2007293032A priority Critical patent/AU2007293032A1/en
Priority to CA002662748A priority patent/CA2662748A1/fr
Priority to EP07837821A priority patent/EP2063708A2/fr
Priority to JP2009527409A priority patent/JP2010502710A/ja
Publication of WO2008030524A2 publication Critical patent/WO2008030524A2/fr
Publication of WO2008030524A3 publication Critical patent/WO2008030524A3/fr

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Addiction (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention porte sur des formulations liquides qui renferment le composé 1-[1-({[(3R,6S)-6-(2,3-difluorophényl)-2-oxo-1-(2,2,2-trifluoroéthyl)azepan-3-yl]amino}carbonyl)pipéridin-4-yl]-2-oxo-1,2-dihydroimidazo[4,5-b]pyridin-3-ide. Les formulations de l'invention possèdent une biodisponibilité et une stabilité étonnament améliorées, en ce qu'elles comprennent du polyéthylène glycol, du Tween (polysorbate 80), du Cremophor® EL (polyoxyle 35-huile de ricin), du propylène glycol et, facultativement, de l'eau, et peuvent être placées dans des capsules de gélatine souple ou dure afin de traiter des troubles, parmi lesquels les maux de tête et les céphalées vasculaires de Horton.
PCT/US2007/019461 2006-09-08 2007-09-06 Formulations pharmaceutiques liquides pour l'administration orale d'un antagoniste du cgrp WO2008030524A2 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
AU2007293032A AU2007293032A1 (en) 2006-09-08 2007-09-06 Liquid pharmaceutical formulations for oral administration of a CGRP antagonist
CA002662748A CA2662748A1 (fr) 2006-09-08 2007-09-06 Formulations pharmaceutiques liquides pour l'administration orale d'un antagoniste du cgrp
EP07837821A EP2063708A2 (fr) 2006-09-08 2007-09-06 Formulations pharmaceutiques liquides pour l'administration orale d'un antagoniste du cgrp
JP2009527409A JP2010502710A (ja) 2006-09-08 2007-09-06 Cgrp拮抗薬の経口投与のための液体医薬製剤

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US84305206P 2006-09-08 2006-09-08
US60/843,052 2006-09-08

Publications (2)

Publication Number Publication Date
WO2008030524A2 WO2008030524A2 (fr) 2008-03-13
WO2008030524A3 true WO2008030524A3 (fr) 2008-10-02

Family

ID=39157840

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2007/019461 WO2008030524A2 (fr) 2006-09-08 2007-09-06 Formulations pharmaceutiques liquides pour l'administration orale d'un antagoniste du cgrp

Country Status (6)

Country Link
EP (1) EP2063708A2 (fr)
JP (1) JP2010502710A (fr)
CN (1) CN101511184A (fr)
AU (1) AU2007293032A1 (fr)
CA (1) CA2662748A1 (fr)
WO (1) WO2008030524A2 (fr)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2011103170A (ru) * 2008-06-30 2012-08-10 Мерк Шарп Энд Домэ Корп. (Us) Твердые дозированные составы телкагепанта калия
CN101756900B (zh) * 2010-02-25 2012-05-30 谢恬 一种榄香烯微乳
KR20210153745A (ko) * 2013-09-16 2021-12-17 머크 샤프 앤드 돔 코포레이션 Cgrp 수용체 길항제를 위한 제제
WO2015164657A1 (fr) * 2014-04-23 2015-10-29 Bcs Business Consulting Services Pte Ltd Incorporation de composant(s) soluble(s) dans l'eau dans des formulations anhydres
SG11202111251SA (en) * 2019-04-11 2021-11-29 R P Scherer Technologies Llc Formulation for oral delivery of proteins, peptides and small molecules with poor permeability
WO2023220109A1 (fr) * 2022-05-11 2023-11-16 Eli Lilly And Company Compositions pharmaceutiques à base de glp1

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6191105B1 (en) * 1993-05-10 2001-02-20 Protein Delivery, Inc. Hydrophilic and lipophilic balanced microemulsion formulations of free-form and/or conjugation-stabilized therapeutic agents such as insulin
WO2004092166A2 (fr) * 2003-04-15 2004-10-28 Merck & Co., Inc. Antagonistes des recepteurs cgrp

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6191105B1 (en) * 1993-05-10 2001-02-20 Protein Delivery, Inc. Hydrophilic and lipophilic balanced microemulsion formulations of free-form and/or conjugation-stabilized therapeutic agents such as insulin
WO2004092166A2 (fr) * 2003-04-15 2004-10-28 Merck & Co., Inc. Antagonistes des recepteurs cgrp

Also Published As

Publication number Publication date
EP2063708A2 (fr) 2009-06-03
CN101511184A (zh) 2009-08-19
AU2007293032A1 (en) 2008-03-13
JP2010502710A (ja) 2010-01-28
CA2662748A1 (fr) 2008-03-13
WO2008030524A2 (fr) 2008-03-13

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