PE20060773A1 - Derivados de oligosacarido que comprenden un residuo de biotina como inhibidores duales antitromboticos - Google Patents

Derivados de oligosacarido que comprenden un residuo de biotina como inhibidores duales antitromboticos

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Publication number
PE20060773A1
PE20060773A1 PE2005001503A PE2005001503A PE20060773A1 PE 20060773 A1 PE20060773 A1 PE 20060773A1 PE 2005001503 A PE2005001503 A PE 2005001503A PE 2005001503 A PE2005001503 A PE 2005001503A PE 20060773 A1 PE20060773 A1 PE 20060773A1
Authority
PE
Peru
Prior art keywords
residue
oligosacaride
biotin
activity
dual inhibitors
Prior art date
Application number
PE2005001503A
Other languages
English (en)
Inventor
Kort Martin De
Boeckel Constant Adriaan Anton Van
Original Assignee
Organon Nv
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.)
Filing date
Publication date
Application filed by Organon Nv filed Critical Organon Nv
Publication of PE20060773A1 publication Critical patent/PE20060773A1/es

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    • BPERFORMING OPERATIONS; TRANSPORTING
    • B82NANOTECHNOLOGY
    • B82YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/61Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/66Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid the modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/66Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid the modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells
    • A61K47/665Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid the modifying agent being a pre-targeting system involving a peptide or protein for targeting specific cells the pre-targeting system, clearing therapy or rescue therapy involving biotin-(strept) avidin systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory 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
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • 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
    • 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
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26Acyclic or carbocyclic radicals, substituted by hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Biotechnology (AREA)
  • Cell Biology (AREA)
  • Nanotechnology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biophysics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Cardiology (AREA)
  • Medical Informatics (AREA)
  • General Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Surgery (AREA)
  • Oncology (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

REFERIDA A UN COMPUESTO DE FORMULA (I) TAL COMO OLIGOSACARIDO-ESPACIADOR-A, DONDE EL OLIGOSACARIDO ES UN RESIDUO DE OLIGOSACARIDO CARGADO NEGATIVAMENTE QUE COMPRENDE DE 2 A 25 UNIDADES DE MONOSACARIDOS, QUE TIENE ACTIVIDAD ANTI-Xa Y DONDE LA CARGA ESTA COMPENSADA POR CONTRAIONES CARGADOS POSITIVAMENTE; EL ESPACIADOR ES UN RESIDUO ENLAZADOR FLEXIBLE QUE ES FARMACOLOGICAMENTE INACTIVO Y TIENE UNA LONGITUD DE CADENA DE 10 A 70 ATOMOS; A ES EL RESIDUO -CH[NH-SO2-R1][CO-NR2-CH(4-BENZAMIDINA)-CO-NR3R4], DONDE R1 ES FENILO, NAFTILO, 1,2,3,4-TETRAHIDRONAFTILO, ENTRE OTROS, R2 Y R3 SON H O ALQUILO C1-C8, R4 ES ALQUILO C1-C8, CICLOALQUILO C3-C8, ENTRE OTROS. EL COMPUESTO DE FORMULA (I) COMPRENDE UN ENLACE COVALENTE CON UN RESIDUO DE BIOTINA O UN ANALOGO DE LA MISMA. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DUALES TANTO DE LA ACTIVIDAD ANTITROMBINA (FACTOR IIA) COMO DE LA ACTIVIDAD ANTI-Xa MEDIADA POR ANTITROMBINA III Y SON UTILES EN EL TRATAMIENTO O PREVENCION DE TROMBOSIS O EMBOLIA VENOSA POSTOPERATORIA, ATEROESCLEROSIS, ENTRE OTRAS
PE2005001503A 2004-12-23 2005-12-16 Derivados de oligosacarido que comprenden un residuo de biotina como inhibidores duales antitromboticos PE20060773A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP04106964 2004-12-23

Publications (1)

Publication Number Publication Date
PE20060773A1 true PE20060773A1 (es) 2006-09-01

Family

ID=35160114

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2005001503A PE20060773A1 (es) 2004-12-23 2005-12-16 Derivados de oligosacarido que comprenden un residuo de biotina como inhibidores duales antitromboticos

Country Status (29)

Country Link
US (3) US8168595B2 (es)
EP (1) EP1830887B1 (es)
JP (2) JP5130051B2 (es)
KR (1) KR101284922B1 (es)
CN (1) CN101087622A (es)
AR (1) AR053657A1 (es)
AT (1) ATE500846T1 (es)
AU (1) AU2005318134B2 (es)
BR (1) BRPI0518560A2 (es)
CA (1) CA2592436C (es)
DE (1) DE602005026859D1 (es)
DK (1) DK1830887T3 (es)
ES (1) ES2361921T3 (es)
HK (1) HK1106712A1 (es)
HR (1) HRP20110330T1 (es)
IL (2) IL183713A (es)
MX (1) MX2007007837A (es)
MY (1) MY146121A (es)
NO (1) NO20072878L (es)
NZ (1) NZ555739A (es)
PE (1) PE20060773A1 (es)
PL (1) PL1830887T3 (es)
PT (1) PT1830887E (es)
RU (1) RU2403259C2 (es)
SI (1) SI1830887T1 (es)
TW (1) TWI403334B (es)
UA (1) UA88793C2 (es)
WO (1) WO2006067173A2 (es)
ZA (1) ZA200705088B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI403334B (zh) * 2004-12-23 2013-08-01 Merck Sharp & Dohme 包含生物素殘基之抗血栓雙重抑制劑
JP6109574B2 (ja) 2009-12-18 2017-04-05 カタラン、フランス、バインハイム、ソシエテ、アノニムCatalent France Beinheim Sa 合成オリゴサッカリドを含有する医薬経口剤形
FR2974478A1 (fr) 2011-04-28 2012-11-02 Endotis Pharma Conjugues d'oligosaccharides en prevention des lesions d'ischemie-reperfusion
EP2721044B1 (en) 2011-06-17 2015-11-18 Carbomimetics Synthetic pentasaccharides having short half-life and high activity
WO2013007762A1 (en) 2011-07-11 2013-01-17 Endotis Pharma Combination of an anticoagulant and avidin useful in surgical intervention and clinical procedure
US10660973B2 (en) 2015-04-28 2020-05-26 Duke University Thrombus imaging aptamers and methods of using same
CN109982707A (zh) 2016-09-16 2019-07-05 杜克大学 血管性血友病因子(vwf)靶向剂及其使用方法

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4252951A (en) * 1979-10-09 1981-02-24 Eli Lilly And Company Isolation of syn-7-(2-amino-4-thiazolyl)-(methoxyimino)acetamido-3-acetoxymethyl-3-cephem-4-carboxylic acid
DK0454220T3 (da) 1990-04-23 1993-11-22 Sanofi Elf Carbohydratderivater omfattende en trisaccharidenhed
IL102758A (en) 1991-08-23 1997-03-18 Akzo Nv Glycosaminoglycanoid derivatives, their preparation and pharmaceutical compositions comprising them
ATE190619T1 (de) 1993-09-01 2000-04-15 Akzo Nobel Nv Biskonjugate, die zwei saccharide und einen spacer enthalten
FR2749849B1 (fr) * 1996-06-14 1998-09-04 Sanofi Sa Polysaccharides synthetiques, procede pour leur preparation et compositions pharmaceutiques les contenant
FR2751334B1 (fr) 1996-07-19 1998-10-16 Sanofi Sa Polysaccharides synthetiques, procede pour leur preparation et compositions pharmaceutiques les contenant
FR2773804B1 (fr) 1998-01-19 2000-02-18 Sanofi Sa Polysaccharides de synthese, procede pour leur preparation et compositions pharmaceutiques le contenant
FR2773801B1 (fr) * 1998-01-19 2000-05-12 Sanofi Sa Nouveaux pentasaccharides, procedes pour leurs preparations et compositions pharmaceutiques les contenant
CN1261450C (zh) * 1998-06-17 2006-06-28 阿克佐诺贝尔公司 抗血栓形成化合物
TWI289566B (en) * 1999-12-07 2007-11-11 N.V.Organon Antithrombotic compound
FR2814463B1 (fr) 2000-09-22 2002-11-15 Sanofi Synthelabo Nouveaux polysaccharides a activite antithrombotique comprenant au moins une liaison covalente avec la biotine ou un derive de la biotine
TWI403334B (zh) * 2004-12-23 2013-08-01 Merck Sharp & Dohme 包含生物素殘基之抗血栓雙重抑制劑
CN101312747B (zh) * 2005-10-10 2013-03-20 Msd欧斯股份有限公司 包括生物素标记的抗血栓形成双重抑制剂

Also Published As

Publication number Publication date
WO2006067173A2 (en) 2006-06-29
PT1830887E (pt) 2011-05-31
ES2361921T3 (es) 2011-06-24
MY146121A (en) 2012-06-29
EP1830887B1 (en) 2011-03-09
ATE500846T1 (de) 2011-03-15
IL217047A0 (en) 2012-01-31
WO2006067173A3 (en) 2007-04-26
RU2007127859A (ru) 2009-01-27
BRPI0518560A2 (pt) 2008-11-25
MX2007007837A (es) 2007-07-25
TW200633724A (en) 2006-10-01
TWI403334B (zh) 2013-08-01
US8168595B2 (en) 2012-05-01
JP5632886B2 (ja) 2014-11-26
JP5130051B2 (ja) 2013-01-30
EP1830887A2 (en) 2007-09-12
CA2592436A1 (en) 2006-06-29
KR20070092304A (ko) 2007-09-12
NZ555739A (en) 2009-11-27
AU2005318134B2 (en) 2010-05-20
US20120238512A1 (en) 2012-09-20
US20120245109A1 (en) 2012-09-27
AR053657A1 (es) 2007-05-16
IL183713A (en) 2013-07-31
DE602005026859D1 (de) 2011-04-21
KR101284922B1 (ko) 2013-07-10
CN101087622A (zh) 2007-12-12
DK1830887T3 (da) 2011-06-06
RU2403259C2 (ru) 2010-11-10
IL183713A0 (en) 2007-09-20
US8445450B2 (en) 2013-05-21
CA2592436C (en) 2012-04-17
US20100004186A1 (en) 2010-01-07
JP2008525373A (ja) 2008-07-17
AU2005318134A1 (en) 2006-06-29
HK1106712A1 (en) 2008-03-20
PL1830887T3 (pl) 2011-07-29
SI1830887T1 (sl) 2011-06-30
HRP20110330T1 (hr) 2011-06-30
JP2013035851A (ja) 2013-02-21
UA88793C2 (ru) 2009-11-25
ZA200705088B (en) 2008-08-27
NO20072878L (no) 2007-09-17

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