JP5923110B2 - トリプシン様セリンプロテアーゼ阻害剤、その調製、ならびに凝固因子ＩＩａおよびＸａの選択的阻害剤としての使用 - Google Patents
トリプシン様セリンプロテアーゼ阻害剤、その調製、ならびに凝固因子ＩＩａおよびＸａの選択的阻害剤としての使用 Download PDFInfo
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- 239000010935 stainless steel Substances 0.000 description 1
- 229910001220 stainless steel Inorganic materials 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 229910052715 tantalum Inorganic materials 0.000 description 1
- GUVRBAGPIYLISA-UHFFFAOYSA-N tantalum atom Chemical compound [Ta] GUVRBAGPIYLISA-UHFFFAOYSA-N 0.000 description 1
- 125000004213 tert-butoxy group Chemical group [H]C([H])([H])C(O*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- XJJBXZIKXFOMLP-ZETCQYMHSA-N tert-butyl (2s)-pyrrolidine-2-carboxylate Chemical compound CC(C)(C)OC(=O)[C@@H]1CCCN1 XJJBXZIKXFOMLP-ZETCQYMHSA-N 0.000 description 1
- CWXPZXBSDSIRCS-UHFFFAOYSA-N tert-butyl piperazine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCNCC1 CWXPZXBSDSIRCS-UHFFFAOYSA-N 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 description 1
- 125000005505 thiomorpholino group Chemical group 0.000 description 1
- 230000002537 thrombolytic effect Effects 0.000 description 1
- 229910052719 titanium Inorganic materials 0.000 description 1
- 239000010936 titanium Substances 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 238000011144 upstream manufacturing Methods 0.000 description 1
- 229960005356 urokinase Drugs 0.000 description 1
- 239000003039 volatile agent Substances 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 229940055725 xarelto Drugs 0.000 description 1
- 229960001522 ximelagatran Drugs 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06104—Dipeptides with the first amino acid being acidic
- C07K5/06113—Asp- or Asn-amino acid
- C07K5/06121—Asp- or Asn-amino acid the second amino acid being aromatic or cycloaliphatic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- 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
- A61P9/10—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06104—Dipeptides with the first amino acid being acidic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06104—Dipeptides with the first amino acid being acidic
- C07K5/06113—Asp- or Asn-amino acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201061425597P | 2010-12-21 | 2010-12-21 | |
| US61/425,597 | 2010-12-21 | ||
| PCT/CA2011/001398 WO2012083436A1 (en) | 2010-12-21 | 2011-12-21 | Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors iia and xa |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014500280A JP2014500280A (ja) | 2014-01-09 |
| JP2014500280A5 JP2014500280A5 (enExample) | 2015-02-05 |
| JP5923110B2 true JP5923110B2 (ja) | 2016-05-24 |
Family
ID=46312955
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013544981A Expired - Fee Related JP5923110B2 (ja) | 2010-12-21 | 2011-12-21 | トリプシン様セリンプロテアーゼ阻害剤、その調製、ならびに凝固因子ＩＩａおよびＸａの選択的阻害剤としての使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US8497245B2 (enExample) |
| EP (1) | EP2655399B1 (enExample) |
| JP (1) | JP5923110B2 (enExample) |
| CN (1) | CN103403018B (enExample) |
| AU (1) | AU2011349022B2 (enExample) |
| CA (1) | CA2822350A1 (enExample) |
| ES (1) | ES2654440T3 (enExample) |
| NO (1) | NO2655399T3 (enExample) |
| WO (1) | WO2012083436A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10301300B4 (de) | 2003-01-15 | 2009-07-16 | Curacyte Chemistry Gmbh | Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein |
| WO2012004678A2 (en) | 2010-07-07 | 2012-01-12 | The Medicines Company (Leipzig) Gmbh | Serine protease inhibitors |
| GB201311888D0 (en) * | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| EP3449261B1 (en) * | 2016-04-25 | 2023-08-30 | Instrumentation Laboratory Company | Method and kit for identifying lupus anticoagulant (la) associated with antiphospholipid syndrome |
| WO2018093716A1 (en) * | 2016-11-18 | 2018-05-24 | Merck Sharp & Dohme Corp. | FACTOR XIIa INHIBITORS |
| GB201805174D0 (en) * | 2018-03-29 | 2018-05-16 | Univ Leeds Innovations Ltd | Compounds |
| GB201807014D0 (en) * | 2018-04-30 | 2018-06-13 | Univ Leeds Innovations Ltd | Factor xlla inhibitors |
| EP3939968A4 (en) * | 2019-03-29 | 2022-12-14 | Medicinal Bioconvergence Research Center | NOVEL COMPOUND HAVING ANTICANCER ACTIVITY, AND METHOD FOR PRODUCTION THEREOF |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3163469D1 (en) * | 1980-05-12 | 1984-06-14 | Choay Sa | Oligopeptides with specific inhibiting properties of collagen induced aggregation, process for preparing the same and pharmaceutical compositions containing them |
| CA1241120A (en) | 1985-10-01 | 1988-08-23 | Sami A. Aly | Alternate mark inversion (ami) receiver |
| US5955576A (en) * | 1992-02-14 | 1999-09-21 | Corvas International, Inc. | Inhibitors of thrombosis |
| EP0684830B1 (en) * | 1993-02-12 | 1999-06-16 | Corvas International, Inc. | Inhibitors of thrombosis |
| EP0648780A1 (en) * | 1993-08-26 | 1995-04-19 | Bristol-Myers Squibb Company | Heterocyclic thrombin inhibitors |
| JPH07138298A (ja) * | 1993-11-19 | 1995-05-30 | Japan Energy Corp | ヒルジン類縁体硫酸エステル化体またはその塩の製造方法 |
| AU1025795A (en) * | 1994-01-27 | 1995-08-03 | Mitsubishi Chemical Corporation | Prolineamide derivatives |
| IL112795A (en) * | 1994-03-04 | 2001-01-28 | Astrazeneca Ab | Peptide derivatives as antithrombic agents their preparation and pharmaceutical compositions containing them |
| US5914319A (en) * | 1995-02-27 | 1999-06-22 | Eli Lilly And Company | Antithrombotic agents |
| EP0960885A4 (en) * | 1996-06-25 | 2002-08-28 | Nisshin Seifun Group Inc | DEPSIPEPTIDES AND MEDICATIONS, WHICH CONTAIN THE SAME AS ACTIVE INGREDIENCIES |
| EP1036063B1 (en) | 1997-11-26 | 2006-11-02 | Ortho-McNeil Pharmaceuticals, Inc. | Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors |
| DE10029014A1 (de) | 2000-06-15 | 2001-12-20 | Univ Schiller Jena | Urokinase-Hemmstoffe |
| DE10029015A1 (de) | 2000-06-15 | 2001-12-20 | Curacyte Ag | Hemmstoffe für den Gerinnungsfaktor Xa |
| JP2004516286A (ja) | 2000-12-18 | 2004-06-03 | メルク エンド カムパニー インコーポレーテッド | ベンジルアミン誘導体およびそれのトロンビン阻害薬としての使用 |
| DE10102878A1 (de) | 2001-01-23 | 2002-08-01 | Haemosys Gmbh | Oligo- oder Polyalkylengekoppelte Thrombininhibitoren |
| JP4898091B2 (ja) | 2002-03-11 | 2012-03-14 | ザ メディシンズ カンパニー （ライプツィヒ） ゲーエムベーハー | ウロキナーゼの阻害剤、それらの製造および使用 |
| DE10227668A1 (de) | 2002-06-20 | 2004-01-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Arzneimittel zur Behandlung des systemic inflammatory response syndrome |
| DE10227666A1 (de) | 2002-06-20 | 2004-01-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | (R)-2-(4-Amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1-(pyrrolidinocarbonyl)- ethyl]-benzimidazol, dessen Monohydrochlorid, Verfahren zu deren Herstellung sowie Verwendung als Arzneimittel |
| DE10301300B4 (de) | 2003-01-15 | 2009-07-16 | Curacyte Chemistry Gmbh | Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein |
| DE10322191B4 (de) | 2003-05-16 | 2014-02-27 | The Medicines Company (Leipzig) Gmbh | N-sulfonylierte Aminosäurederivate, Verfahren zu ihrer Herstellung und ihre Verwendung |
| DE10342108A1 (de) | 2003-09-11 | 2005-04-14 | Curacyte Chemistry Gmbh | Basisch-substituierte Benzylaminanaloga als Inhibitoren des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung |
| DE102005044319A1 (de) * | 2005-09-16 | 2007-03-22 | Curacyte Chemistry Gmbh | 2-(Aminomethyl)-5-Chlor-Benzylamid-Derivate und ihre Verwendung als Hemmstoffe des Gerinnungsfaktors Xa |
| DE102006050672A1 (de) | 2006-10-24 | 2008-04-30 | Curacyte Discovery Gmbh | Hemmstoffe des Plasmins und des Plasmakallikreins |
| JP5424887B2 (ja) * | 2006-11-08 | 2014-02-26 | チョンシー ユー | ペプチド及び関連化合物の経皮送達システム |
| WO2012004678A2 (en) | 2010-07-07 | 2012-01-12 | The Medicines Company (Leipzig) Gmbh | Serine protease inhibitors |
-
2011
- 2011-12-21 NO NO11850640A patent/NO2655399T3/no unknown
- 2011-12-21 EP EP11850640.1A patent/EP2655399B1/en not_active Not-in-force
- 2011-12-21 CA CA2822350A patent/CA2822350A1/en not_active Abandoned
- 2011-12-21 JP JP2013544981A patent/JP5923110B2/ja not_active Expired - Fee Related
- 2011-12-21 AU AU2011349022A patent/AU2011349022B2/en not_active Ceased
- 2011-12-21 CN CN201180065191.4A patent/CN103403018B/zh not_active Expired - Fee Related
- 2011-12-21 WO PCT/CA2011/001398 patent/WO2012083436A1/en not_active Ceased
- 2011-12-21 US US13/332,900 patent/US8497245B2/en not_active Expired - Fee Related
- 2011-12-21 ES ES11850640.1T patent/ES2654440T3/es active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US8497245B2 (en) | 2013-07-30 |
| AU2011349022B2 (en) | 2017-04-13 |
| AU2011349022A1 (en) | 2013-07-11 |
| US20120252743A1 (en) | 2012-10-04 |
| CA2822350A1 (en) | 2012-06-28 |
| ES2654440T3 (es) | 2018-02-13 |
| CN103403018B (zh) | 2015-08-19 |
| NO2655399T3 (enExample) | 2018-02-24 |
| JP2014500280A (ja) | 2014-01-09 |
| EP2655399A4 (en) | 2014-07-30 |
| EP2655399B1 (en) | 2017-09-27 |
| WO2012083436A1 (en) | 2012-06-28 |
| CN103403018A (zh) | 2013-11-20 |
| EP2655399A1 (en) | 2013-10-30 |
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