BRPI0508048A - derivados de pirrol como inibidores do fator xa - Google Patents
derivados de pirrol como inibidores do fator xaInfo
- Publication number
- BRPI0508048A BRPI0508048A BRPI0508048-7A BRPI0508048A BRPI0508048A BR PI0508048 A BRPI0508048 A BR PI0508048A BR PI0508048 A BRPI0508048 A BR PI0508048A BR PI0508048 A BRPI0508048 A BR PI0508048A
- Authority
- BR
- Brazil
- Prior art keywords
- factor
- compounds
- formulas
- factor viia
- inhibitors
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 3
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical class C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 title abstract 2
- 108010054265 Factor VIIa Proteins 0.000 abstract 4
- 108010074860 Factor Xa Proteins 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 229940012414 factor viia Drugs 0.000 abstract 4
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 230000002785 anti-thrombosis Effects 0.000 abstract 1
- 230000023555 blood coagulation Effects 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229940088598 enzyme Drugs 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 208000037803 restenosis Diseases 0.000 abstract 1
- 230000002441 reversible effect Effects 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
- 230000009424 thromboembolic effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- 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
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
DERIVADOS DE PIRROL COMO INIBIDORES DO FATOR Xa. A presente invenção refere-se à compostos das fórmulas (I) e (Ia), em que R¬0¬; R¬1¬; R¬2¬; R¬3¬; R¬4¬; R¬22¬, Q; V, G e M têm os significados indicados nas reivindicações. Os compostos das fórmulas I e Ia são compostos farmacologicamente ativos valiosos. Eles exibem um forte efeito anti-trombótico e são adequados para a terapia e profilaxia de distúrbios cardiovasculares tais como doenças trombo-embólicas ou restenoses. Eles são inibidores reversíveis das enzimas de coagulação sangüinea fator Xa (FXa) e/ou fator VIIa (FVIIa), e podem em geral ser aplicados em condições nas quais uma atividade indesejada de fator Xa e/ou fator VIIa está presente ou para a cura ou prevenção das quais uma inibição de fator Xa e/ou fator VIIa é pretendida. A invenção além disso refere-se à processos para a preparação de compostos das fórmulas (I) e (Ia), o emprego deles, em particular como ingredientes ativos em produtos farmacêuticos, e preparações farmacêuticas compreendendo-os.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04004503A EP1568698A1 (en) | 2004-02-27 | 2004-02-27 | Pyrrole-derivatives as factor Xa inhibitors |
| PCT/EP2005/001423 WO2005085239A2 (en) | 2004-02-27 | 2005-02-12 | PYRROLE-DERIVATIVES AS FACTOR Xa INHIBITORS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0508048A true BRPI0508048A (pt) | 2007-07-17 |
Family
ID=34745922
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0508048-7A BRPI0508048A (pt) | 2004-02-27 | 2005-02-12 | derivados de pirrol como inibidores do fator xa |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US7465806B2 (pt) |
| EP (2) | EP1568698A1 (pt) |
| JP (1) | JP4861306B2 (pt) |
| CN (1) | CN1926137A (pt) |
| AU (1) | AU2005219507A1 (pt) |
| BR (1) | BRPI0508048A (pt) |
| CA (1) | CA2557270A1 (pt) |
| IL (1) | IL177253A0 (pt) |
| PE (1) | PE20051170A1 (pt) |
| TW (1) | TW200538110A (pt) |
| UY (1) | UY28778A1 (pt) |
| WO (1) | WO2005085239A2 (pt) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7358268B2 (en) * | 2002-12-04 | 2008-04-15 | Sanofi-Aventis Deutschland Gmbh | Imidazole derivatives as factor Xa inhibitors |
| US7429581B2 (en) | 2002-12-23 | 2008-09-30 | Sanofi-Aventis Deutschland Gmbh | Pyrazole-derivatives as factor Xa inhibitors |
| EP1479675A1 (en) * | 2003-05-19 | 2004-11-24 | Aventis Pharma Deutschland GmbH | Indazole-derivatives as factor Xa inhibitors |
| EP1571154A1 (en) * | 2004-03-03 | 2005-09-07 | Aventis Pharma Deutschland GmbH | Beta-aminoacid-derivatives as factor Xa inhibitors |
| TW200840815A (en) * | 2007-04-13 | 2008-10-16 | Chang Chun Plastics Co Ltd | Method for preparing melamine salt of bis(pentaerythritol phosphate)phosphoric acid |
| EP2155720B1 (en) * | 2007-06-08 | 2013-07-17 | Advinus Therapeutics Private Limited | Pyrrole-2-carboxamide derivatives as glucokinase activators, their process and pharmaceutical application |
| EP3613743B1 (en) | 2008-01-04 | 2022-03-16 | Intellikine, LLC | Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| EP2435072A2 (en) | 2009-05-27 | 2012-04-04 | Yeda Research and Development Co. Ltd. | Proteasome inhibitors and uses thereof |
| TWI674262B (zh) | 2011-01-10 | 2019-10-11 | 美商英菲尼提製藥股份有限公司 | 製備異喹啉酮之方法及異喹啉酮之固體形式 |
| US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
| EP2914296B2 (en) | 2012-11-01 | 2021-09-29 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| GB201300304D0 (en) | 2013-01-08 | 2013-02-20 | Kalvista Pharmaceuticals Ltd | Benzylamine derivatives |
| IL239682B (en) | 2013-01-08 | 2018-10-31 | Kalvista Pharmaceuticals Ltd | History of benzylamine and 2-(aminomethyl)pyridine |
| TWI636047B (zh) | 2013-08-14 | 2018-09-21 | 英商卡爾維斯塔製藥有限公司 | 雜環衍生物 |
| WO2015160975A2 (en) | 2014-04-16 | 2015-10-22 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
| GB201421085D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| IL263235B (en) | 2016-05-31 | 2022-07-01 | Kalvista Pharmaceuticals Ltd | History of pyrazoles as plasma kallikrein inhibitors |
| GB201609603D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide |
| GB201609607D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts |
| RU2754507C2 (ru) | 2016-06-24 | 2021-09-02 | Инфинити Фармасьютикалз, Инк. | Комбинированная терапия |
| HUE057912T2 (hu) | 2017-11-29 | 2022-06-28 | Kalvista Pharmaceuticals Ltd | Plazma kallikrein inhibitort tartalmazó dózisformák |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| WO2021028645A1 (en) | 2019-08-09 | 2021-02-18 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| CN113192004B (zh) * | 2021-04-01 | 2022-01-18 | 温州医科大学附属第二医院(温州医科大学附属育英儿童医院) | 一种基于冠脉多模影像裂纹形成和扩展的简化计算方法与斑块破裂风险量化的评估系统 |
| WO2025024685A2 (en) * | 2023-07-27 | 2025-01-30 | Thomas Jefferson University | Inhibitors of cib1 interactions and methods of use |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA873607B (en) * | 1986-06-13 | 1988-12-28 | Warner Lambert Co | N-1h-tetrazol-5-yl-2-thiophene carboxamides,n-1h-tetrazol-5-yl-2-pyrrole carboxamides n-1h-tetrazol-5-yl-2-furan carboxamides |
| US5506134A (en) | 1990-10-22 | 1996-04-09 | Corvas International, Inc. | Hypridoma and monoclonal antibody which inhibits blood coagulation tissue factor/factor VIIa complex |
| US5788965A (en) | 1991-02-28 | 1998-08-04 | Novo Nordisk A/S | Modified factor VII |
| US5833982A (en) | 1991-02-28 | 1998-11-10 | Zymogenetics, Inc. | Modified factor VII |
| SI9520044B (sl) | 1994-04-26 | 2004-08-31 | Aventis Pharmaceuticals Inc. | Inhibitorji Xa faktorja |
| IT1282797B1 (it) * | 1995-04-21 | 1998-03-31 | Colla Paolo | Pirril-(indolil)-aril-sulfoni e relativo processo di produzione ed impiego nella terapia delle infezioni da virus dell'aids |
| US6020357A (en) * | 1996-12-23 | 2000-02-01 | Dupont Pharmaceuticals Company | Nitrogen containing heteroaromatics as factor Xa inhibitors |
| CN1246847A (zh) * | 1996-12-23 | 2000-03-08 | 杜邦药品公司 | 作为Xa因子抑制剂的含氮杂芳族化合物 |
| US6432947B1 (en) * | 1997-02-19 | 2002-08-13 | Berlex Laboratories, Inc. | N-heterocyclic derivatives as NOS inhibitors |
| IL136637A0 (en) * | 1997-12-22 | 2001-06-14 | Du Pont Pharm Co | Nitrogen containing heteroaromatics with ortho-substituted pi's as factor xa inhibitors |
| HU227568B1 (en) * | 1997-12-24 | 2011-08-29 | Sanofi Aventis Deutschland | Indole derivatives, as inhibitors os factor xa |
| EP1072263A4 (en) * | 1998-03-26 | 2004-03-31 | Japan Tobacco Inc | AMID DERIVATIVES AND NOCICEPTINANT AGONISTS |
| EP0987274A1 (en) | 1998-09-15 | 2000-03-22 | Hoechst Marion Roussel Deutschland GmbH | Factor VIIa Inhibitors |
| CN1230421C (zh) * | 1999-02-10 | 2005-12-07 | 三菱制药株式会社 | 酰胺化合物及其药物用途 |
| WO2001032628A1 (en) * | 1999-11-03 | 2001-05-10 | Bristol-Myers Squibb Pharma Company | Cyano compounds as factor xa inhibitors |
| MY138097A (en) * | 2000-03-22 | 2009-04-30 | Du Pont | Insecticidal anthranilamides |
| WO2002000651A2 (en) * | 2000-06-27 | 2002-01-03 | Bristol-Myers Squibb Pharma Company | Factor xa inhibitors |
| AU2001295098A1 (en) | 2000-09-05 | 2002-03-22 | Medical Research Council | Monoclonal antibody against ovarian carcinoma |
| EP1217000A1 (en) | 2000-12-23 | 2002-06-26 | Aventis Pharma Deutschland GmbH | Inhibitors of factor Xa and factor VIIa |
| WO2002053155A1 (en) * | 2000-12-30 | 2002-07-11 | Geron Corporation | Telomerase inhibitor |
| WO2002053157A1 (en) * | 2000-12-30 | 2002-07-11 | Geron Corporation | Thiazolidine derivative |
| TWI243164B (en) * | 2001-02-13 | 2005-11-11 | Aventis Pharma Gmbh | Acylated indanyl amines and their use as pharmaceuticals |
| PE20020870A1 (es) * | 2001-02-13 | 2002-11-18 | Aventis Pharma Gmbh | 6,7,8,9-tetrahidro-5h-benzocicloheptenil aminas aciladas |
| EP1314733A1 (en) | 2001-11-22 | 2003-05-28 | Aventis Pharma Deutschland GmbH | Indole-2-carboxamides as factor Xa inhibitors |
| EP1388341A1 (en) * | 2002-08-07 | 2004-02-11 | Aventis Pharma Deutschland GmbH | Acylamino-substituted heteroaromatic compounds and their use as pharmaceuticals |
| AU2003268184A1 (en) * | 2002-08-23 | 2004-03-11 | Chiron Corporation | Pyrrole based inhibitors of glycogen synthase kinase 3 |
| EP1562931A2 (en) * | 2002-10-25 | 2005-08-17 | Genesoft Pharmaceuticals, Inc. | Anti-infective biaryl compounds |
| US7358268B2 (en) | 2002-12-04 | 2008-04-15 | Sanofi-Aventis Deutschland Gmbh | Imidazole derivatives as factor Xa inhibitors |
| US7429581B2 (en) | 2002-12-23 | 2008-09-30 | Sanofi-Aventis Deutschland Gmbh | Pyrazole-derivatives as factor Xa inhibitors |
| CN100395234C (zh) * | 2003-01-02 | 2008-06-18 | 霍夫曼-拉罗奇有限公司 | 新cb1受体反激动剂 |
| EP1479675A1 (en) | 2003-05-19 | 2004-11-24 | Aventis Pharma Deutschland GmbH | Indazole-derivatives as factor Xa inhibitors |
| US7317027B2 (en) | 2003-05-19 | 2008-01-08 | Sanofi-Aventis Deutschland Gmbh | Azaindole-derivatives as factor Xa inhibitors |
| US7741341B2 (en) | 2003-05-19 | 2010-06-22 | Sanofi-Aventis Deutschland Gmbh | Benzimidazole-derivatives as factor Xa inhibitors |
| EP1571154A1 (en) | 2004-03-03 | 2005-09-07 | Aventis Pharma Deutschland GmbH | Beta-aminoacid-derivatives as factor Xa inhibitors |
-
2004
- 2004-02-27 EP EP04004503A patent/EP1568698A1/en not_active Withdrawn
-
2005
- 2005-02-12 WO PCT/EP2005/001423 patent/WO2005085239A2/en not_active Ceased
- 2005-02-12 JP JP2007500094A patent/JP4861306B2/ja not_active Expired - Fee Related
- 2005-02-12 CN CNA2005800062350A patent/CN1926137A/zh active Pending
- 2005-02-12 BR BRPI0508048-7A patent/BRPI0508048A/pt not_active IP Right Cessation
- 2005-02-12 EP EP05707352A patent/EP1725550A2/en not_active Withdrawn
- 2005-02-12 CA CA002557270A patent/CA2557270A1/en not_active Abandoned
- 2005-02-12 AU AU2005219507A patent/AU2005219507A1/en not_active Abandoned
- 2005-02-15 PE PE2005000176A patent/PE20051170A1/es not_active Application Discontinuation
- 2005-02-24 TW TW094105507A patent/TW200538110A/zh unknown
- 2005-02-25 UY UY28778A patent/UY28778A1/es unknown
-
2006
- 2006-08-02 IL IL177253A patent/IL177253A0/en unknown
- 2006-08-25 US US11/467,277 patent/US7465806B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| EP1568698A1 (en) | 2005-08-31 |
| WO2005085239A3 (en) | 2005-10-13 |
| US7465806B2 (en) | 2008-12-16 |
| AU2005219507A1 (en) | 2005-09-15 |
| US20070049573A1 (en) | 2007-03-01 |
| CA2557270A1 (en) | 2005-09-15 |
| UY28778A1 (es) | 2005-09-30 |
| JP2007523927A (ja) | 2007-08-23 |
| JP4861306B2 (ja) | 2012-01-25 |
| KR20070000487A (ko) | 2007-01-02 |
| WO2005085239A2 (en) | 2005-09-15 |
| PE20051170A1 (es) | 2006-02-07 |
| CN1926137A (zh) | 2007-03-07 |
| TW200538110A (en) | 2005-12-01 |
| EP1725550A2 (en) | 2006-11-29 |
| IL177253A0 (en) | 2006-12-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 7A ANUIDADE. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2158 DE 15/05/2012. |