JP2009543843A - 直接トロンビン阻害剤に関する新規適応 - Google Patents

直接トロンビン阻害剤に関する新規適応 Download PDF

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JP2009543843A
JP2009543843A JP2009519955A JP2009519955A JP2009543843A JP 2009543843 A JP2009543843 A JP 2009543843A JP 2009519955 A JP2009519955 A JP 2009519955A JP 2009519955 A JP2009519955 A JP 2009519955A JP 2009543843 A JP2009543843 A JP 2009543843A
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disease
compound
dabigatran
group
methyl
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JP2009543843A5 (enExample
Inventor
アンドレアス クレメンス
ポール エイ ライリー
Original Assignee
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
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Publication of JP2009543843A publication Critical patent/JP2009543843A/ja
Publication of JP2009543843A5 publication Critical patent/JP2009543843A5/ja
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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
    • A61K31/397Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/55Protease inhibitors
    • A61K38/57Protease inhibitors from animals; from humans
    • A61K38/58Protease inhibitors from animals; from humans from leeches, e.g. hirudin, eglin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/02Suppositories; Bougies; Bases therefor; Ovules
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2009519955A 2006-07-17 2007-07-13 直接トロンビン阻害剤に関する新規適応 Pending JP2009543843A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP06117345 2006-07-17
EP07102513 2007-02-15
PCT/EP2007/057256 WO2008009639A2 (en) 2006-07-17 2007-07-13 New indications for direct thrombin inhibitors

Publications (2)

Publication Number Publication Date
JP2009543843A true JP2009543843A (ja) 2009-12-10
JP2009543843A5 JP2009543843A5 (enExample) 2010-09-24

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Application Number Title Priority Date Filing Date
JP2009519955A Pending JP2009543843A (ja) 2006-07-17 2007-07-13 直接トロンビン阻害剤に関する新規適応

Country Status (7)

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US (2) US20080200514A1 (enExample)
EP (1) EP2043632A2 (enExample)
JP (1) JP2009543843A (enExample)
AR (1) AR062057A1 (enExample)
CA (1) CA2657269A1 (enExample)
TW (1) TW200813012A (enExample)
WO (1) WO2008009639A2 (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2716642C (en) * 2008-03-28 2017-02-28 Boehringer Ingelheim International Gmbh Method for manufacturing acid pellets
RU2010143901A (ru) * 2008-03-28 2012-05-10 Бёрингер Ингельхайм Интернациональ Гмбх (De) Способ получения композиций дабигатрана для перорального введения
RU2529798C2 (ru) 2008-07-14 2014-09-27 Бёрингер Ингельхайм Интернациональ Гмбх Способ получения лекарственных соединений, содержащих дабигатран
US20110306640A1 (en) * 2008-08-19 2011-12-15 Boehringer Ingelheim International Gmbh Dabigatran in tumour therapy
EP2358368A1 (en) 2008-11-11 2011-08-24 Boehringer Ingelheim International GmbH Method for treating or preventing thrombosis using dabigatran etexilate or a salt thereof with improved safety profile over conventional warfarin therapy
NZ593787A (en) * 2009-02-02 2013-09-27 Boehringer Ingelheim Int Lyophilised dabigatran
WO2010130758A1 (en) * 2009-05-14 2010-11-18 Boehringer Ingelheim International Gmbh New combination therapy in treatment of cancer and fibrotic diseases
EP2429520A1 (en) * 2009-05-14 2012-03-21 Boehringer Ingelheim International GmbH New combination therapy in treatment of oncological and fibrotic diseases
EP2322163A1 (en) * 2009-11-03 2011-05-18 Pharnext New therapeutics approaches for treating alzheimer disease
EA201201202A1 (ru) * 2010-03-01 2013-04-30 Рациофарм Гмбх Пероральная фармацевтическая композиция, содержащая этексилат дабигатрана
EP2550966B1 (de) * 2011-07-25 2016-10-19 Dritte Patentportfolio Beteiligungsgesellschaft mbH & Co. KG Dabigatran-Amidoximsäureesters als Prodrugs und ihre Verwendung als Arzneimittel
US20130345262A1 (en) 2012-06-25 2013-12-26 Boehringer Ingelheim International Gmbh Method for prevention of stroke
CN105440017B (zh) * 2014-08-19 2018-03-02 天津药物研究院 达比加群酯香草酸盐及其制备方法和应用
CN104628733A (zh) * 2015-03-02 2015-05-20 中国药科大学 四氢苯并[4,5]咪唑并[1,2-a]吡嗪类凝血酶抑制剂
WO2025136810A1 (en) * 2023-12-19 2025-06-26 The Research Institute At Nationwide Children's Hospital Anticoagulants for treating nephrotic syndrome

Citations (3)

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JP2001509815A (ja) * 1997-02-18 2001-07-24 ベーリンガー インゲルハイム ファルマ コマンディトゲゼルシャフト 二置換二環式複素環化合物、これらの調製及び医薬組成物としてのこれらの使用
JP2004503508A (ja) * 2000-06-10 2004-02-05 アストラゼネカ アクチボラグ メラガトラン及びXa因子阻害剤を含んでなる組合せ製品
WO2004026252A2 (en) * 2002-09-23 2004-04-01 The Regents Of The University Of Michigan Glioma treatments

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JP2000514788A (ja) * 1996-06-25 2000-11-07 イーライ・リリー・アンド・カンパニー 抗凝固剤
US5863292A (en) * 1996-09-26 1999-01-26 Tosic; Aleksandar Articulated external orthopedic fixation system and method of use
US20030181488A1 (en) * 2002-03-07 2003-09-25 Boehringer Ingelheim Pharma Gmbh & Co. Kg Administration form for the oral application of 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionic acid ethyl ester and the salts thereof
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
KR20040076203A (ko) * 2003-02-24 2004-08-31 주식회사 엘지생명과학 음식물-약물 상호작용을 방지하기 위한 경구 투여용약제학적 조성물 및 방법
CA2523157A1 (en) * 2003-04-24 2004-11-04 Boehringer Ingelheim International Gmbh Use of dipyridamole or mopidamole for treatment and prevention of thrombo-embolic diseases and disorders caused by excessive formation of thrombin and/or by elevated expression ofthrombin receptors
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JP2001509815A (ja) * 1997-02-18 2001-07-24 ベーリンガー インゲルハイム ファルマ コマンディトゲゼルシャフト 二置換二環式複素環化合物、これらの調製及び医薬組成物としてのこれらの使用
JP2004503508A (ja) * 2000-06-10 2004-02-05 アストラゼネカ アクチボラグ メラガトラン及びXa因子阻害剤を含んでなる組合せ製品
WO2004026252A2 (en) * 2002-09-23 2004-04-01 The Regents Of The University Of Michigan Glioma treatments

Non-Patent Citations (1)

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Title
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Publication number Publication date
CA2657269A1 (en) 2008-01-24
AR062057A1 (es) 2008-10-15
WO2008009639A2 (en) 2008-01-24
TW200813012A (en) 2008-03-16
EP2043632A2 (en) 2009-04-08
WO2008009639A3 (en) 2008-06-26
US20080200514A1 (en) 2008-08-21
US20100173947A1 (en) 2010-07-08

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