DE10338403A1 - Pulverformulierung, enthaltend den CGRP-Antagonisten 1-[N2-[3,5-Dibrom-N-[[4-(3,4-dihydro-2(1H)-oxochinazolin-3-yl]-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyrindinyl)-piperazin, Verfahren zu dessen Herstellung sowie dessen Verwendung als Inhalativum - Google Patents

Pulverformulierung, enthaltend den CGRP-Antagonisten 1-[N2-[3,5-Dibrom-N-[[4-(3,4-dihydro-2(1H)-oxochinazolin-3-yl]-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyrindinyl)-piperazin, Verfahren zu dessen Herstellung sowie dessen Verwendung als Inhalativum Download PDF

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Publication number
DE10338403A1
DE10338403A1 DE10338403A DE10338403A DE10338403A1 DE 10338403 A1 DE10338403 A1 DE 10338403A1 DE 10338403 A DE10338403 A DE 10338403A DE 10338403 A DE10338403 A DE 10338403A DE 10338403 A1 DE10338403 A1 DE 10338403A1
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DE
Germany
Prior art keywords
powder
active substance
drying gas
spray
organic
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.)
Withdrawn
Application number
DE10338403A
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German (de)
English (en)
Inventor
Michael Dr. Trunk
Claudius Weiler
Christel Schmelzer
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.)
Boehringer Ingelheim Pharma GmbH and Co KG
Boehringer Ingelheim Pharmaceuticals Inc
Original Assignee
Boehringer Ingelheim Pharma GmbH and Co KG
Boehringer Ingelheim Pharmaceuticals 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 Boehringer Ingelheim Pharma GmbH and Co KG, Boehringer Ingelheim Pharmaceuticals Inc filed Critical Boehringer Ingelheim Pharma GmbH and Co KG
Priority to DE10338403A priority Critical patent/DE10338403A1/de
Priority to US10/909,624 priority patent/US20050042180A1/en
Priority to EP04764097A priority patent/EP1660046A1/de
Priority to CA002536053A priority patent/CA2536053A1/en
Priority to JP2006523585A priority patent/JP2007502792A/ja
Priority to PCT/EP2004/009103 priority patent/WO2005018614A1/de
Priority to TW093124725A priority patent/TW200516077A/zh
Priority to ARP040102955A priority patent/AR045461A1/es
Publication of DE10338403A1 publication Critical patent/DE10338403A1/de
Withdrawn legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682—Processes
    • A61K9/1688—Processes resulting in pure drug agglomerate optionally containing up to 5% of excipient

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  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Medicinal Preparation (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pain & Pain Management (AREA)
  • Organic Chemistry (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
DE10338403A 2003-08-18 2003-08-18 Pulverformulierung, enthaltend den CGRP-Antagonisten 1-[N2-[3,5-Dibrom-N-[[4-(3,4-dihydro-2(1H)-oxochinazolin-3-yl]-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyrindinyl)-piperazin, Verfahren zu dessen Herstellung sowie dessen Verwendung als Inhalativum Withdrawn DE10338403A1 (de)

Priority Applications (8)

Application Number Priority Date Filing Date Title
DE10338403A DE10338403A1 (de) 2003-08-18 2003-08-18 Pulverformulierung, enthaltend den CGRP-Antagonisten 1-[N2-[3,5-Dibrom-N-[[4-(3,4-dihydro-2(1H)-oxochinazolin-3-yl]-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyrindinyl)-piperazin, Verfahren zu dessen Herstellung sowie dessen Verwendung als Inhalativum
US10/909,624 US20050042180A1 (en) 2003-08-18 2004-08-02 Powder formulation containing the CGRP antagonist 1 [N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2 (1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazin, process for preparing and the use thereof as inhalation powder
EP04764097A EP1660046A1 (de) 2003-08-18 2004-08-13 Pulverinhalativum enthaltend den cgrp-antagonisten 1-(n2-(3,5-dibrom-n-((4-(3,4-dihydro-2(1h)-oxochinazolin-3-yl)-1-piperidinyl)carbonyl)-d-tyrosyl)-l-lysyl)-4-(4-pyridinyl)-piperazin
CA002536053A CA2536053A1 (en) 2003-08-18 2004-08-13 Powder formulation comprising the cgrp antagonist 1-(n2-(3,5-dibromo-n-(4-(3,4-dihydro-2(1h)-oxoquinazolin-3-yl)- 1-piperidinyl)carbonyl)-d-tyrosyl)-l-lysyl)-4-(4-pyridinyl)-piperazine
JP2006523585A JP2007502792A (ja) 2003-08-18 2004-08-13 Ｃｇｒｐアンタゴニスト１−［ｎ２−［３，５−ジブロモ−ｎ−［［４−（３，４−ジヒドロ−２（１ｈ）−オキソキナゾリン−３−イル）−１−ピペリジニル］カルボニル］−ｄ−チロシル］−ｌ−リシル］−４−（４−ピリジニル）−ピペラジンを含有する粉末製剤、その吸入粉末としての製造方法及び使用
PCT/EP2004/009103 WO2005018614A1 (de) 2003-08-18 2004-08-13 Pulverformulierung, enthaltend den cgrp-antagonisten 1- (n2-(3,5-dibrom-n-(4-(3,4-dihydro-2(1h)-oxochinazolin-3-yl)- 1-piperidinyl)carbonyl)-d-tyrosyl)-l-lysyl)-4-(4-pyridinyl)-piperazin
TW093124725A TW200516077A (en) 2003-08-18 2004-08-17 Powder formulation containing the CGRP antagonist 1-[n2-[3,5-dibromo-n-[[4-(3,4-dihydro-2(1h)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-d-tyrosyl]-l-lysyl]-4-(4-pyridinyl)-piperazin, process for preparing and the use thereof as inhalation powder
ARP040102955A AR045461A1 (es) 2003-08-18 2004-08-18 Formulacion en polvo que contiene el antagonista de cgrp 1-[n2-[3,5-dibromo-n-[[4-(3,4-dihidro-2(1h)-oxoquinazolin-3-il)-1- piperidinil]-carbonil]-d-tirosil]-l-lisil]-4-(4-piridinil)-piperazina, procedimiento para su preparacion y su uso como inhalador

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10338403A DE10338403A1 (de) 2003-08-18 2003-08-18 Pulverformulierung, enthaltend den CGRP-Antagonisten 1-[N2-[3,5-Dibrom-N-[[4-(3,4-dihydro-2(1H)-oxochinazolin-3-yl]-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyrindinyl)-piperazin, Verfahren zu dessen Herstellung sowie dessen Verwendung als Inhalativum

Publications (1)

Publication Number Publication Date
DE10338403A1 true DE10338403A1 (de) 2005-03-17

Family

ID=34201782

Family Applications (1)

Application Number Title Priority Date Filing Date
DE10338403A Withdrawn DE10338403A1 (de) 2003-08-18 2003-08-18 Pulverformulierung, enthaltend den CGRP-Antagonisten 1-[N2-[3,5-Dibrom-N-[[4-(3,4-dihydro-2(1H)-oxochinazolin-3-yl]-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyrindinyl)-piperazin, Verfahren zu dessen Herstellung sowie dessen Verwendung als Inhalativum

Country Status (7)

Country Link
EP (1) EP1660046A1 (enExample)
JP (1) JP2007502792A (enExample)
AR (1) AR045461A1 (enExample)
CA (1) CA2536053A1 (enExample)
DE (1) DE10338403A1 (enExample)
TW (1) TW200516077A (enExample)
WO (1) WO2005018614A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10338407A1 (de) * 2003-08-18 2005-03-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Inhalationspulver enthaltend den CGRP-Antagonisten 1-[N2-[3,5-Dibrom-N-[[4-(3,4-dihydro-2(1H)-oxochinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)-piperazin
DE10338399A1 (de) * 2003-08-18 2005-03-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Mikropartikel, enthaltend den CGRP-Antagonisten 1-[N2-[3,5-Dibrom-N-[[4-(3,4-dihydro-2(1H)-oxochinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-Iysyl]-4-(4-pyridinyl)-piperazin, Verfahren zu deren Herstellung sowie deren Verwendung als Inhalaltionspulver
DE10338402A1 (de) * 2003-08-18 2005-03-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Sprühgetrocknetes, amorphes BIBN 4096, Verfahren zu dessen Herstellung sowie dessen Verwendung als Inhalativum
GB0613925D0 (en) * 2006-07-13 2006-08-23 Unilever Plc Improvements relating to nanodispersions

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1242211A (en) * 1967-08-08 1971-08-11 Fisons Pharmaceuticals Ltd Pharmaceutical composition
MA25590A1 (fr) * 1998-09-14 2002-12-31 Inhale Therapeutic Syst Agent actif de delivraison de poudre seche
DE10139410A1 (de) * 2001-08-17 2003-02-27 Boehringer Ingelheim Pharma Verwendung von BIBN4096 in Kombination mit anderen Arzneistoffen gegen Migräne für die Behandlung von Migräne
DE10206770A1 (de) * 2002-02-19 2003-08-28 Boehringer Ingelheim Pharma Verfahren zur Herstellung eines Pulverinhalativums enthaltend ein Salz des CGRP-Antagonisten BIBN4096
DE10207026A1 (de) * 2002-02-20 2003-08-28 Boehringer Ingelheim Kg Pulverinhalativum, enthaltend den CGRP-Antagonisten BIBN4096 und Verfahren zu dessen Herstellung

Also Published As

Publication number Publication date
TW200516077A (en) 2005-05-16
WO2005018614A1 (de) 2005-03-03
AR045461A1 (es) 2005-10-26
EP1660046A1 (de) 2006-05-31
JP2007502792A (ja) 2007-02-15
CA2536053A1 (en) 2005-03-03

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