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PE20030641A1 - Composicion nanoparticulada de 2-(r)-(1-(r)-(3,5-bis(trifluorometil)fenil)etoxi)-3-(s)-(4-fluoro)fenil-4-(3-(5-oxo-1h,4h-1,2,4-triazolo)metil morfolina) - Google Patents

Composicion nanoparticulada de 2-(r)-(1-(r)-(3,5-bis(trifluorometil)fenil)etoxi)-3-(s)-(4-fluoro)fenil-4-(3-(5-oxo-1h,4h-1,2,4-triazolo)metil morfolina)

Info

Publication number
PE20030641A1
PE20030641A1 PE2002001173A PE2002001173A PE20030641A1 PE 20030641 A1 PE20030641 A1 PE 20030641A1 PE 2002001173 A PE2002001173 A PE 2002001173A PE 2002001173 A PE2002001173 A PE 2002001173A PE 20030641 A1 PE20030641 A1 PE 20030641A1
Authority
PE
Peru
Prior art keywords
phenyl
spheres
trifluorometil
etoxy
oxo
Prior art date
Application number
PE2002001173A
Other languages
English (en)
Inventor
Karen C Thompson
H William Bosch
Suhas D Shelukar
Elaine Liversidge
Original Assignee
Merck & Co 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=23331619&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20030641(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of PE20030641A1 publication Critical patent/PE20030641A1/es

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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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/145Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/167Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
    • A61K9/1676Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
    • 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
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/51Nanocapsules; Nanoparticles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

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  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Otolaryngology (AREA)
  • Rheumatology (AREA)
  • Physics & Mathematics (AREA)
  • Nanotechnology (AREA)
  • Optics & Photonics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A UNA COMPOSICION NANOPARTICULADA QUE COMPRENDE DE 5% A 60% DE UN ANTAGONISTA DEL RECEPTOR DE TAQUICININA TAL COMO 2-(R)-(1-(R)-(3,5-BIS(TRIFLUOROMETIL)FENIL)ETOXI)-3-(S)-(4-FLUORO)FENIL-4-(3-(5-OXO-1H,4H-1,2,4-TRIAZOL)METILMORFOLINA; DE 1% A 20% DE UN ESTABILIZANTE ABSORBIDO EN LA SUPERFICIE DEL COMPUESTO O EN UNA CANTIDAD PARA MANTENER UN PROMEDIO EFECTIVO DE TAMANO DE PARTICULAS MENOR DE 1000nm, TAL COMO CELULOSA HIDROXIPROPILICA, CELULOSA HIDROXIPROPILMETILICA, CELULOSA HIDROXIPROPILICA DE VISCOSIDAD SUPERBAJA, POLIVINILPIRROLIDONA, COPOLIMEROS DE OXIDO DE ETILENO, OXIDO DE PROPILENO, SULFOSUCCINATO DE DIOCTIL SODIO Y SULFATO DE LAURIL SODIO; DE 0% A 50% DE UN AGENTE REDISPENSANTE, DE 0% A 90% DE UN SOPORTE SOLIDO; DE 0% A 5% DE UN LUBRICANTE. LA COMPOSICION SE HA DESECADO POR ASPERSION O REVESTIDO POR ASPERSION SOBRE UN SOPORTE SOLIDO SELECCIONADO A PARTIR DE ESFERAS DE CELULOSA MICROCRISTALINA, ESFERAS DE AZUCAR ALMIDON Y ESFERAS DE LACTOSA. LA COMPOSICION PRESENTA UNA MAYOR BIODISPONIBILIDAD ORAL Y PUEDE SER UTIL PARA EL TRATAMIENTO DE TRASTORNOS DEL SISTEMA NERVIOSO CENTRAL, TRASTORNOS PSIQUIATRICOS, DEPRESION ANSIEDAD, ENFERMEDADES INFLAMATORIAS, EMESIS
PE2002001173A 2001-12-10 2002-12-05 Composicion nanoparticulada de 2-(r)-(1-(r)-(3,5-bis(trifluorometil)fenil)etoxi)-3-(s)-(4-fluoro)fenil-4-(3-(5-oxo-1h,4h-1,2,4-triazolo)metil morfolina) PE20030641A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US34004001P 2001-12-10 2001-12-10

Publications (1)

Publication Number Publication Date
PE20030641A1 true PE20030641A1 (es) 2003-07-23

Family

ID=23331619

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2002001173A PE20030641A1 (es) 2001-12-10 2002-12-05 Composicion nanoparticulada de 2-(r)-(1-(r)-(3,5-bis(trifluorometil)fenil)etoxi)-3-(s)-(4-fluoro)fenil-4-(3-(5-oxo-1h,4h-1,2,4-triazolo)metil morfolina)

Country Status (38)

Country Link
US (1) US8258132B2 (es)
EP (1) EP1455756B2 (es)
JP (1) JP4532114B2 (es)
KR (1) KR20040063991A (es)
CN (1) CN100352443C (es)
AR (1) AR037713A1 (es)
AT (1) ATE400254T1 (es)
AU (1) AU2002360824B8 (es)
BR (1) BRPI0214786B8 (es)
CA (1) CA2469315C (es)
CO (1) CO5590887A2 (es)
CY (1) CY1108354T1 (es)
DE (1) DE60227556D1 (es)
DK (1) DK1455756T4 (es)
DO (1) DOP2002000542A (es)
EA (1) EA007332B1 (es)
EC (1) ECSP045144A (es)
ES (1) ES2307820T5 (es)
GE (1) GEP20063875B (es)
HR (1) HRP20040532B1 (es)
HU (1) HU230736B1 (es)
IL (3) IL162296A0 (es)
IS (1) IS2991B (es)
JO (1) JO3060B1 (es)
ME (1) ME00450B (es)
MX (1) MXPA04005563A (es)
MY (1) MY155911A (es)
NO (1) NO336943B1 (es)
NZ (1) NZ534009A (es)
PE (1) PE20030641A1 (es)
PL (1) PL211243B6 (es)
PT (1) PT1455756E (es)
RS (1) RS52280B (es)
SI (1) SI1455756T2 (es)
TW (1) TWI249403B (es)
UA (1) UA76810C2 (es)
WO (1) WO2003049718A1 (es)
ZA (1) ZA200404012B (es)

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