DK2550966T3 - Dabigatran-amidoxinsyreestere som prodrugs og deres anvendelse som medikament - Google Patents
Dabigatran-amidoxinsyreestere som prodrugs og deres anvendelse som medikament Download PDFInfo
- Publication number
- DK2550966T3 DK2550966T3 DK11175230.9T DK11175230T DK2550966T3 DK 2550966 T3 DK2550966 T3 DK 2550966T3 DK 11175230 T DK11175230 T DK 11175230T DK 2550966 T3 DK2550966 T3 DK 2550966T3
- Authority
- DK
- Denmark
- Prior art keywords
- dabigatran
- amidoxime
- composition according
- succinic acid
- formula
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- 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
- A61K9/10—Dispersions; Emulsions
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Dispersion Chemistry (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Enzymes And Modification Thereof (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (14)
1. Sammensætning, med formlen
i hvilken R1 repræsenterer en forgrenet eller ikke-forgrenet, mættet eller ikke-mættet, ikke-substitueret hydrocarbon-kæde, hvis længde er 1 til 12, og n er lig med 2.
2. Sammensætning ifølge krav 1, hvorved R1 repræsenterer ethyl.
3. Salte, solvater og solvater af salte af sammensætningerne ifølge krav 1 til 2.
4. Sammensætning ifølge et hvilket som helst af kravene 1 til 3 med henblik på anvendelse ved behandlingen og/eller profylakse af sygdomme.
5. Sammensætning ifølge et hvilket som helst af kravene 1 til 3 med henblik på anvendelse ved behandlingen og/eller profylakse af thrombotiske sygdomme.
6. Sammensætning ifølge et hvilket som helst af kravene 1 til 3 med henblik på anvendelse ved behandlingen og/eller profylakse af thrombotiske hændelser, navnlig venøs thromboembolisme (VTE).
7. Sammensætning ifølge et hvilket som helst af kravene 1 til 3 med henblik på anvendelse ved behandlingen og/eller profylakse af slagtilfælde, hjerte-infarkt og/elle atrie-flimren og arrhytmier.
8. Sammensætning ifølge et hvilket som helst af kravene 1 til 3 med henblik på anvendelse og/eller profylakse af onkologiske sygdomme med en hvilken som helst patogenese.
9. Medikament, omfattende i det mindste en sammensætning ifølge et hvilket som helst af kravene 1 til 3, og som har en forlængende virkning på thrombin-tid, en thrombin-hæmmende virkning og/eller en hæmmende virkning på relaterede serinproteaser.
10. Medikament, omfattende i det mindste en sammensætning ifølge et hvilket som helst af kravene 1 til 3, i givet fald i kombination med eet eller flere inerte, ikke-toksiske, farmaceutisk egnede hjælpestoffer.
11. Medikament, omfattende i det mindste én sammensætning ifølge et hvilket som helst af kravene 1 til 3 i kombination med eet eller flere yderligere, aktive midler.
12. Medikament, omfattende i det mindste én sammensætning ifølge et hvilket som helst af kravene 1 til 3 med henblik på oral eller parenteral indgivelse.
13. Medikament ifølge et hvilket som helst af kravene 9 til 11, kendetegnet ved, at medikamentet er formuleret som resisten over for mavesyre.
14. Fremgangsmåde til fremstilling af en sammensætning ifølge et hvilket som helst af kravene 1 til 3, kendetegnet ved, at et nitril med formlen (A)
hvori R1 repræsenterer en -H, en forgrenet eller ikke-forgrenet, mættet eller ikke-mættet, ikke substitueret hydrocarbon-kæde med en længde på 1 til 12, er konverteret til et amidoxin ifølge formel (B)
og at det således opnåede amidoxim konverteres ved reaktion med en di-carbonsyre-anhydrid ifølge formel (C).
hvori n repræsenterer 2, overføres til en sammensætning med formlen
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP11175230.9A EP2550966B1 (de) | 2011-07-25 | 2011-07-25 | Dabigatran-Amidoximsäureesters als Prodrugs und ihre Verwendung als Arzneimittel |
Publications (1)
Publication Number | Publication Date |
---|---|
DK2550966T3 true DK2550966T3 (da) | 2017-02-06 |
Family
ID=46466528
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK11175230.9T DK2550966T3 (da) | 2011-07-25 | 2011-07-25 | Dabigatran-amidoxinsyreestere som prodrugs og deres anvendelse som medikament |
Country Status (20)
Country | Link |
---|---|
US (1) | US8853245B2 (da) |
EP (2) | EP2550966B1 (da) |
JP (1) | JP2014521619A (da) |
KR (1) | KR20140049021A (da) |
CN (1) | CN103945845A (da) |
AU (1) | AU2012289112B2 (da) |
BR (1) | BR112014001970A2 (da) |
CA (1) | CA2842304A1 (da) |
CY (1) | CY1118294T1 (da) |
DK (1) | DK2550966T3 (da) |
ES (1) | ES2611610T3 (da) |
HK (1) | HK1201738A1 (da) |
HR (1) | HRP20161675T1 (da) |
HU (1) | HUE032862T2 (da) |
LT (1) | LT2550966T (da) |
PL (1) | PL2550966T3 (da) |
PT (1) | PT2550966T (da) |
RU (1) | RU2014106866A (da) |
SI (1) | SI2550966T1 (da) |
WO (1) | WO2013013946A1 (da) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20040045742A1 (en) * | 2001-04-10 | 2004-03-11 | Halliburton Energy Services, Inc. | Force-balanced roller-cone bits, systems, drilling methods, and design methods |
CN106470987A (zh) * | 2014-08-06 | 2017-03-01 | 四川海思科制药有限公司 | 一种达比加群酯衍生物及其制备方法和在药学上的用途 |
CN107027308A (zh) * | 2014-08-06 | 2017-08-08 | 四川海思科制药有限公司 | 一种达比加群硫酯衍生物及其制备方法和在药学上的用途 |
DE102016102887A1 (de) * | 2016-02-18 | 2017-08-24 | Develco Pharma Schweiz Ag | Orale Darreichungsform eines Dabigatran-Prodrugs zur Behandlung von Krankheiten |
CN110448557A (zh) * | 2019-09-05 | 2019-11-15 | 黄筱茜 | 抗凝血药达比加群酯的新药用途 |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PE121699A1 (es) * | 1997-02-18 | 1999-12-08 | Boehringer Ingelheim Pharma | Heterociclos biciclicos disustituidos como inhibidores de la trombina |
DE10235639A1 (de) | 2002-08-02 | 2004-02-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Prodrugs von 1-Methyl-2-(4-amidinophenylaminomethyl)-benzimidazol-5-yl-carbonsäure-(N-2-pyridyl-N-2-hydroxycarbonylethyl)-amid, ihre Herstellung und ihre Verwendung als Arzneimittel |
DE10341043A1 (de) | 2003-09-03 | 2005-03-31 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue oral zu applizierende Darreichungsform für 3-[(2-{[4-Hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionsäure-ethylester und dessen Salze |
JP2009543843A (ja) * | 2006-07-17 | 2009-12-10 | 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 | 直接トロンビン阻害剤に関する新規適応 |
DE102008007440A1 (de) * | 2008-02-01 | 2009-08-13 | Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co.Kg | Aminosäurederivate als Arzneistoffe |
DE102008007381A1 (de) * | 2008-02-01 | 2009-08-13 | Dritte Patentportfolio Beteiligungsgesellschaft Mbh & Co.Kg | Amidine und Guanidine und deren Derivate zur Behandlung von Krankheiten |
KR20110082563A (ko) * | 2008-11-11 | 2011-07-19 | 베링거 인겔하임 인터내셔날 게엠베하 | 통상의 와파린 요법에 비해 효능이 향상된 다비가트란 에텍실레이트 또는 이의 염을 사용하여 혈전증을 치료하거나 예방하는 방법 |
BRPI0921354A2 (pt) * | 2008-11-11 | 2019-09-24 | Boehringer Ingelheim Int | método para tratamento ou prevenção de trombose usando etexilato de dabigatran ou um sal do mesmo com aprimorada eficácia em relação à terapia convencional com varfarina. |
DE102009004204A1 (de) * | 2009-01-09 | 2010-07-15 | Christian-Albrechts-Universität Zu Kiel | Verfahren zur verbesserten Bioaktivierung von Arzneistoffen |
-
2011
- 2011-07-25 SI SI201130999A patent/SI2550966T1/sl unknown
- 2011-07-25 ES ES11175230.9T patent/ES2611610T3/es active Active
- 2011-07-25 DK DK11175230.9T patent/DK2550966T3/da active
- 2011-07-25 HU HUE11175230A patent/HUE032862T2/en unknown
- 2011-07-25 LT LTEP11175230.9T patent/LT2550966T/lt unknown
- 2011-07-25 EP EP11175230.9A patent/EP2550966B1/de active Active
- 2011-07-25 PL PL11175230T patent/PL2550966T3/pl unknown
- 2011-07-25 PT PT111752309T patent/PT2550966T/pt unknown
-
2012
- 2012-07-05 RU RU2014106866/04A patent/RU2014106866A/ru not_active Application Discontinuation
- 2012-07-05 AU AU2012289112A patent/AU2012289112B2/en not_active Ceased
- 2012-07-05 CA CA2842304A patent/CA2842304A1/en not_active Abandoned
- 2012-07-05 JP JP2014522017A patent/JP2014521619A/ja active Pending
- 2012-07-05 CN CN201280037040.2A patent/CN103945845A/zh active Pending
- 2012-07-05 KR KR1020147004769A patent/KR20140049021A/ko not_active Application Discontinuation
- 2012-07-05 EP EP12733105.6A patent/EP2773347B1/de not_active Not-in-force
- 2012-07-05 BR BR112014001970A patent/BR112014001970A2/pt not_active IP Right Cessation
- 2012-07-05 WO PCT/EP2012/063071 patent/WO2013013946A1/de active Application Filing
- 2012-07-24 US US13/556,612 patent/US8853245B2/en active Active
-
2015
- 2015-03-06 HK HK15102313.9A patent/HK1201738A1/xx unknown
-
2016
- 2016-12-06 CY CY20161101252T patent/CY1118294T1/el unknown
- 2016-12-08 HR HRP20161675TT patent/HRP20161675T1/hr unknown
Also Published As
Publication number | Publication date |
---|---|
HK1201738A1 (en) | 2015-09-11 |
CY1118294T1 (el) | 2017-06-28 |
LT2550966T (lt) | 2017-01-25 |
CN103945845A (zh) | 2014-07-23 |
ES2611610T3 (es) | 2017-05-09 |
RU2014106866A (ru) | 2015-08-27 |
HUE032862T2 (en) | 2017-11-28 |
EP2773347B1 (de) | 2017-09-13 |
SI2550966T1 (sl) | 2017-01-31 |
WO2013013946A1 (de) | 2013-01-31 |
PT2550966T (pt) | 2017-01-31 |
US8853245B2 (en) | 2014-10-07 |
EP2550966A1 (de) | 2013-01-30 |
HRP20161675T1 (hr) | 2017-02-24 |
JP2014521619A (ja) | 2014-08-28 |
PL2550966T3 (pl) | 2017-03-31 |
KR20140049021A (ko) | 2014-04-24 |
AU2012289112B2 (en) | 2017-01-05 |
BR112014001970A2 (pt) | 2017-02-21 |
US20130030023A1 (en) | 2013-01-31 |
CA2842304A1 (en) | 2013-01-31 |
EP2773347A1 (de) | 2014-09-10 |
AU2012289112A1 (en) | 2014-02-13 |
EP2550966B1 (de) | 2016-10-19 |
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