ECSP099501A - Formulaciones de dosis unitaria y métodos para el tratamiento de la trombosis con un inhibidor oral del factor xa - Google Patents

Formulaciones de dosis unitaria y métodos para el tratamiento de la trombosis con un inhibidor oral del factor xa

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Publication number
ECSP099501A
ECSP099501A EC2009009501A ECSP099501A ECSP099501A EC SP099501 A ECSP099501 A EC SP099501A EC 2009009501 A EC2009009501 A EC 2009009501A EC SP099501 A ECSP099501 A EC SP099501A EC SP099501 A ECSP099501 A EC SP099501A
Authority
EC
Ecuador
Prior art keywords
factor
coagulation
inhibitors
patient
inhibitor
Prior art date
Application number
EC2009009501A
Other languages
English (en)
Inventor
Uma Sinha
Stanley J Hollenbach
Keith Abe
Original Assignee
Millenium Pharmaceuticals Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39110529&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ECSP099501(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Millenium Pharmaceuticals Inc filed Critical Millenium Pharmaceuticals Inc
Publication of ECSP099501A publication Critical patent/ECSP099501A/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • 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
    • 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
    • A61K31/4409Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
    • 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
    • A61K31/4412Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

RESUMEN DEL INVENTOLa modelación comparativa de la medida de cambios en actividad de protominasa a niveles de eficacia antitrombótica ha llevado al descubrimiento de la actividad terapéutica en humanos de inhibidores de factor Xa. Este invento está dirigido a un método para inhibir coagulación en un paciente humano utilizando una cantidad inhibitoria cantidad inhibidora de la coagulación de un inhibidor de factor Xa. Específicamente, inhibidores directos oralmente disponibles de factor Xa son efectivos para inhibir coagulación en un paciente humano cuando se administran al paciente en una cantidad diaria agregada de entre 0.01 y 2.0 miligramos por kilogramo aproximadamente con base en el peso total del paciente ("mg/kg") . Se contempla que esta dosis será efectiva para cualquier compuesto el cual específicamente inhibe factor Xa y particularmente efectiva para inhibidores de factor Xa de las Fórmula I, II, III, IV o V descritas a continuación.El invento también está dirigido a un método de evaluar el estado de la coagulación del paciente. Se contempla que este método de evaluar el estado de la coagulación se puede utilizar para probar un número de clases diferentes de anticoagulantes además de inhibidores de factor Xa.Gráfico (Imagen en formato jpg)
EC2009009501A 2006-12-08 2009-07-08 Formulaciones de dosis unitaria y métodos para el tratamiento de la trombosis con un inhibidor oral del factor xa ECSP099501A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US87379206P 2006-12-08 2006-12-08
US94762907P 2007-07-02 2007-07-02

Publications (1)

Publication Number Publication Date
ECSP099501A true ECSP099501A (es) 2010-01-29

Family

ID=39110529

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2009009501A ECSP099501A (es) 2006-12-08 2009-07-08 Formulaciones de dosis unitaria y métodos para el tratamiento de la trombosis con un inhibidor oral del factor xa

Country Status (18)

Country Link
US (1) US8404724B2 (es)
EP (1) EP2101760B1 (es)
KR (1) KR101472765B1 (es)
CN (1) CN105193799A (es)
AU (1) AU2007333377B2 (es)
CA (2) CA2671502C (es)
CO (1) CO6220933A2 (es)
CR (1) CR10914A (es)
EC (1) ECSP099501A (es)
ES (1) ES2409090T3 (es)
IL (1) IL199219A (es)
MA (1) MA31086B1 (es)
NI (1) NI200900145A (es)
NZ (1) NZ578180A (es)
PT (1) PT2101760E (es)
RU (2) RU2452484C2 (es)
SG (1) SG10201504425SA (es)
WO (1) WO2008073670A2 (es)

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Publication number Publication date
PT2101760E (pt) 2013-05-07
AU2007333377A1 (en) 2008-06-19
RU2452484C2 (ru) 2012-06-10
US20080153876A1 (en) 2008-06-26
MA31086B1 (fr) 2010-01-04
CN105193799A (zh) 2015-12-30
HK1134031A1 (en) 2010-04-16
KR101472765B1 (ko) 2014-12-15
KR20090107499A (ko) 2009-10-13
EP2101760A2 (en) 2009-09-23
CA2913963A1 (en) 2008-06-19
CA2671502A1 (en) 2008-06-19
RU2012104816A (ru) 2013-08-20
AU2007333377B2 (en) 2014-01-16
EP2101760B1 (en) 2013-02-27
ES2409090T3 (es) 2013-06-24
RU2009126147A (ru) 2011-01-20
SG10201504425SA (en) 2015-07-30
IL199219A0 (en) 2010-03-28
CR10914A (es) 2009-08-12
WO2008073670A3 (en) 2008-11-27
US8404724B2 (en) 2013-03-26
WO2008073670A2 (en) 2008-06-19
IL199219A (en) 2013-10-31
CO6220933A2 (es) 2010-11-19
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