DE10351663A1 - Pulverförmige Arzneimittel enthaltend ein Tiotropiumsalz und Salmeterolxinafoat - Google Patents

Pulverförmige Arzneimittel enthaltend ein Tiotropiumsalz und Salmeterolxinafoat Download PDF

Info

Publication number: DE10351663A1
Authority: DE; Germany
Prior art keywords: inhalation; powder; tiotropium; salmeterol; salmeterol xinafoate
Prior art date: 2002-12-20
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 Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Withdrawn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

DE10351663A

Other languages

German (de)

English (en)

Inventor

Hagen Graebner

Mareke Hartig

Peter Sieger

Rainer Soyka

Michael Trunk

Michael Walz

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.)

2002-12-20

Filing date

2003-11-05

Publication date

2004-07-01

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=32404034&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DE10351663(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2003-11-05 Application filed by Boehringer Ingelheim Pharma GmbH and Co KG, Boehringer Ingelheim Pharmaceuticals Inc filed Critical Boehringer Ingelheim Pharma GmbH and Co KG

2003-11-05 Priority to DE10351663A priority Critical patent/DE10351663A1/de

2004-07-01 Publication of DE10351663A1 publication Critical patent/DE10351663A1/de

Status Withdrawn legal-status Critical Current

Links

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Classifications

- A—HUMAN NECESSITIES
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- A61K9/00—Medicinal preparations characterised by special physical form
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- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
- A—HUMAN NECESSITIES
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- 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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics

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Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Epidemiology (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Pulmonology (AREA)
Emergency Medicine (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Organic Chemistry (AREA)
Otolaryngology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicinal Preparation (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

DE10351663A 2002-12-20 2003-11-05 Pulverförmige Arzneimittel enthaltend ein Tiotropiumsalz und Salmeterolxinafoat Withdrawn DE10351663A1 (de)

Priority Applications (1)

Application Number	Priority Date	Filing Date	Title
DE10351663A DE10351663A1 (de)	2002-12-20	2003-11-05	Pulverförmige Arzneimittel enthaltend ein Tiotropiumsalz und Salmeterolxinafoat

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
DE10259912.2		2002-12-20
DE10259912		2002-12-20
DE10351663A DE10351663A1 (de)	2002-12-20	2003-11-05	Pulverförmige Arzneimittel enthaltend ein Tiotropiumsalz und Salmeterolxinafoat

Publications (1)

Publication Number	Publication Date
DE10351663A1 true DE10351663A1 (de)	2004-07-01

Family

ID=32404034

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
DE10351663A Withdrawn DE10351663A1 (de)	2002-12-20	2003-11-05	Pulverförmige Arzneimittel enthaltend ein Tiotropiumsalz und Salmeterolxinafoat

Country Status (21)

Country	Link
EP (1)	EP1581198A1 (es)
JP (1)	JP2006516135A (es)
KR (1)	KR20050086930A (es)
CN (1)	CN1728988B (es)
AU (1)	AU2003288226B2 (es)
BR (1)	BR0317443A (es)
CA (1)	CA2510779A1 (es)
DE (1)	DE10351663A1 (es)
EA (1)	EA010588B1 (es)
EC (1)	ECSP055855A (es)
FR (1)	FR2848849B1 (es)
HR (1)	HRP20050570A2 (es)
IT (1)	ITMI20032473A1 (es)
MX (1)	MXPA05006519A (es)
NO (1)	NO20053548L (es)
NZ (1)	NZ541303A (es)
PL (1)	PL376231A1 (es)
RS (1)	RS20050484A (es)
UA (1)	UA83813C2 (es)
WO (1)	WO2004058233A1 (es)
ZA (1)	ZA200503692B (es)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US7407955B2 (en)	2002-08-21	2008-08-05	Boehringer Ingelheim Pharma Gmbh & Co., Kg	8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
DE102004054054A1 (de)	2004-11-05	2006-05-11	Boehringer Ingelheim Pharma Gmbh & Co. Kg	Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine
JP4342426B2 (ja) *	2004-11-24	2009-10-14	科研製薬株式会社	イトラコナゾール経口投与用製剤
JP2009504603A (ja) *	2005-08-06	2009-02-05	ベーリンガーインゲルハイムインターナショナルゲゼルシャフトミットベシュレンクテルハフツング	チオトロピウム塩とサルメテロールの塩とを組合せて投与する呼吸困難の治療方法
PT1869035E (pt) *	2005-12-19	2013-01-10	Sicor Inc	Novas formas de brometo de tiotrópio e processos para sua preparação
PE20080251A1 (es)	2006-05-04	2008-04-25	Boehringer Ingelheim Int	Usos de inhibidores de dpp iv
EP1852108A1 (en)	2006-05-04	2007-11-07	Boehringer Ingelheim Pharma GmbH & Co.KG	DPP IV inhibitor formulations
BRPI0711558A2 (pt)	2006-05-04	2011-11-08	Boeringer Ingelheim Internat Gmbh	polimorfos
DE102007036411A1 (de) *	2007-07-20	2009-02-12	Boehringer Ingelheim Pharma Gmbh & Co. Kg	Pulverinhalator
PE20090907A1 (es) *	2007-07-21	2009-08-05	Boehringer Ingelheim Int	Nuevos medicamentos pulverulentos que contienen tiotropio y salmeterol, asi como lactosa como excipiente
PE20140960A1 (es)	2008-04-03	2014-08-15	Boehringer Ingelheim Int	Formulaciones que comprenden un inhibidor de dpp4
BRPI0916997A2 (pt)	2008-08-06	2020-12-15	Boehringer Ingelheim International Gmbh	Inibidor de dpp-4 e seu uso
UY32030A (es)	2008-08-06	2010-03-26	Boehringer Ingelheim Int	"tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
US20200155558A1 (en)	2018-11-20	2020-05-21	Boehringer Ingelheim International Gmbh	Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
EP2382216A1 (en)	2008-12-23	2011-11-02	Boehringer Ingelheim International GmbH	Salt forms of organic compound
AR074990A1 (es)	2009-01-07	2011-03-02	Boehringer Ingelheim Int	Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina
EA034869B1 (ru)	2009-11-27	2020-03-31	Бёрингер Ингельхайм Интернациональ Гмбх	Лечение генотипированных пациентов с диабетом ингибиторами дпп-4, такими как линаглиптин
MX341025B (es)	2010-05-05	2016-08-04	Boehringer Ingelheim Int Gmbh *	Terapia de combinacion.
PH12012502524A1 (en)	2010-06-24	2014-02-10	Boehringer Ingelheim Int	Diabetes therapy
US9034883B2 (en)	2010-11-15	2015-05-19	Boehringer Ingelheim International Gmbh	Vasoprotective and cardioprotective antidiabetic therapy
EP3517539B1 (en)	2011-07-15	2022-12-14	Boehringer Ingelheim International GmbH	Substituted dimeric quinazoline derivative, its preparation and its use in pharmaceutical compositions for the treatment of type i and ii diabetes
US9555001B2 (en)	2012-03-07	2017-01-31	Boehringer Ingelheim International Gmbh	Pharmaceutical composition and uses thereof
US20130303554A1 (en)	2012-05-14	2013-11-14	Boehringer Ingelheim International Gmbh	Use of a dpp-4 inhibitor in sirs and/or sepsis
JP6224084B2 (ja)	2012-05-14	2017-11-01	ベーリンガーインゲルハイムインターナショナルゲゼルシャフトミットベシュレンクテルハフツング	糸球体上皮細胞関連障害及び／又はネフローゼ症候群の治療に用いるｄｐｐ−４阻害薬としてのキサンチン誘導体
WO2013174767A1 (en)	2012-05-24	2013-11-28	Boehringer Ingelheim International Gmbh	A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
US9526728B2 (en)	2014-02-28	2016-12-27	Boehringer Ingelheim International Gmbh	Medical use of a DPP-4 inhibitor
KR101748796B1 (ko) *	2015-09-30	2017-06-19	한미약품 주식회사	활성성분의 전달량이 향상된 흡입용 캡슐제
CN109310697A (zh)	2016-06-10	2019-02-05	勃林格殷格翰国际有限公司	利格列汀和二甲双胍的组合
AU2019380421B2 (en)	2018-11-13	2025-07-24	Cocrystal Pharma, Inc.	Formulations of influenza therapeutics

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CN1056974C (zh) *	1992-02-11	2000-10-04	格拉克索公司	适宜于微粒化的药物材料的制备方法
WO1993016031A1 (en) *	1992-02-11	1993-08-19	Glaxo Group Limited	Benzenedimethanol derivative suitable for micronisation
GB9313650D0 (en) *	1993-07-01	1993-08-18	Glaxo Group Ltd	Method and apparatus for the formation of particles
DE19921693A1 (de) *	1999-05-12	2000-11-16	Boehringer Ingelheim Pharma	Neuartige Arzneimittelkompositionen auf der Basis von anticholinergisch wirksamen Verbindungen und ß-Mimetika
UA75375C2 (en) *	2000-10-12	2006-04-17	Boehringer Ingelheim Pharma	Method for producing powdery preparations for inhaling
DE10056104A1 (de) *	2000-11-13	2002-05-23	Boehringer Ingelheim Pharma	Neue Arzneimittelkompositionen auf der Basis von Tiotropiumsalzen und Salzen des Salmeterols
DE10104367A1 (de) *	2001-02-01	2002-08-08	Boehringer Ingelheim Pharma	Betamimetika enthaltende Arzneimittelkompositionen mit geringeren Nebenwirkungen
DE10130371A1 (de) *	2001-06-23	2003-01-02	Boehringer Ingelheim Pharma	Neue Arzneimittelkompositionen auf der Basis von Anticholinergika, Corticosteroiden und Betamimetika
JP2004537377A (ja) *	2001-08-09	2004-12-16	グラクソ　グループ　リミテッド	製薬組成物を有する吸入装置
EP1429768B1 (de) *	2001-09-14	2016-11-16	Boehringer Ingelheim Pharma GmbH & Co.KG	Neue arzneimittel zur inhalation

2003
- 2003-04-12 UA UAA200507088A patent/UA83813C2/ru unknown
- 2003-11-05 DE DE10351663A patent/DE10351663A1/de not_active Withdrawn
- 2003-12-04 CN CN2003801069216A patent/CN1728988B/zh not_active Expired - Fee Related
- 2003-12-04 HR HR20050570A patent/HRP20050570A2/xx not_active Application Discontinuation
- 2003-12-04 EA EA200500902A patent/EA010588B1/ru not_active IP Right Cessation
- 2003-12-04 AU AU2003288226A patent/AU2003288226B2/en not_active Ceased
- 2003-12-04 MX MXPA05006519A patent/MXPA05006519A/es unknown
- 2003-12-04 BR BR0317443-3A patent/BR0317443A/pt not_active IP Right Cessation
- 2003-12-04 NZ NZ541303A patent/NZ541303A/en unknown
- 2003-12-04 RS YUP-2005/0484A patent/RS20050484A/sr unknown
- 2003-12-04 CA CA002510779A patent/CA2510779A1/en not_active Abandoned
- 2003-12-04 KR KR1020057011668A patent/KR20050086930A/ko not_active Ceased
- 2003-12-04 WO PCT/EP2003/013691 patent/WO2004058233A1/de not_active Ceased
- 2003-12-04 JP JP2004562686A patent/JP2006516135A/ja active Pending
- 2003-12-04 PL PL03376231A patent/PL376231A1/xx not_active Application Discontinuation
- 2003-12-04 EP EP03780120A patent/EP1581198A1/de not_active Withdrawn
- 2003-12-16 IT IT002473A patent/ITMI20032473A1/it unknown
- 2003-12-19 FR FR0315082A patent/FR2848849B1/fr not_active Expired - Fee Related
2005
- 2005-05-09 ZA ZA200503692A patent/ZA200503692B/en unknown
- 2005-06-15 EC EC2005005855A patent/ECSP055855A/es unknown
- 2005-07-19 NO NO20053548A patent/NO20053548L/no not_active Application Discontinuation

Also Published As

Publication number	Publication date
FR2848849B1 (fr)	2007-01-05
NO20053548L (no)	2005-09-02
AU2003288226A1 (en)	2004-07-22
MXPA05006519A (es)	2005-08-26
UA83813C2 (ru)	2008-08-26
EA200500902A1 (ru)	2006-02-24
NZ541303A (en)	2008-11-28
CN1728988A (zh)	2006-02-01
HRP20050570A2 (en)	2006-07-31
CA2510779A1 (en)	2004-07-15
KR20050086930A (ko)	2005-08-30
AU2003288226B2 (en)	2010-01-07
EA010588B1 (ru)	2008-10-30
BR0317443A (pt)	2005-11-16
ITMI20032473A1 (it)	2004-06-21
RS20050484A (sr)	2007-11-15
FR2848849A1 (fr)	2004-06-25
WO2004058233A1 (de)	2004-07-15
EP1581198A1 (de)	2005-10-05
CN1728988B (zh)	2010-04-28
PL376231A1 (en)	2005-12-27
JP2006516135A (ja)	2006-06-22
ECSP055855A (es)	2005-11-22
ZA200503692B (en)	2006-10-25

Legal Events

Date	Code	Title	Description
2011-02-03	8141	Disposal/no request for examination

Publication	Publication Date	Title
EP1292281B1 (de)	2004-09-08	Neue tiotropium-haltige inhalationspulver
EP1581198A1 (de)	2005-10-05	Pulverformige arzneimittel zur inhalation enthaltend ein tiotropiumsalz und salmeterolxinafoat
EP1379220B1 (de)	2004-12-29	Inhalationskapseln
EP2182933B1 (de)	2016-09-07	Neue pulverförmige arzneimittel enthaltend tiotropium und salmeterol sowie laktose als hilfsstoff
EP1785422B1 (de)	2016-11-16	Kristallines Mikronisat des Tiotropiumbromids
EP1326585B1 (de)	2006-03-08	Verfahren zur herstellung von pulverformulierungen
EP1283036B1 (de)	2008-01-02	Multidosis-Trockenpulverinhalator mit Pulverreservoir
DE10141377A1 (de)	2003-03-13	Aufstreuverfahren zur Herstellung von Pulverformulierungen
EP1424996B1 (de)	2005-04-27	Verfahren zur herstellung von inhalationspulvern
EP1567135B1 (de)	2008-07-23	Tiotropiumhaltige pulverformulierung für die inhalation
DE60308497T2 (de)	2007-02-22	Pulverzubereitungen zur inhalation
EP2298415B1 (de)	2013-06-12	Tiotropiumbromid-Mikronisat
EP1646365B1 (de)	2009-01-14	Pulverformulierungen für die inhalation enthaltend ein neues anticholinergikum
DE10338407A1 (de)	2005-03-17	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
DE10138022A1 (de)	2003-02-20	Verfahren zur Herstellung von Pulverformulierungen