AR040077A1 - Composiciones farmaceuticas y metodos de uso de derivados de epotilona modificados por c-21 - Google Patents

Composiciones farmaceuticas y metodos de uso de derivados de epotilona modificados por c-21

Info

Publication number
AR040077A1
AR040077A1 ARP030101689A ARP030101689A AR040077A1 AR 040077 A1 AR040077 A1 AR 040077A1 AR P030101689 A ARP030101689 A AR P030101689A AR P030101689 A ARP030101689 A AR P030101689A AR 040077 A1 AR040077 A1 AR 040077A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
substituted
aryl
substituted alkyl
Prior art date
Application number
ARP030101689A
Other languages
English (en)
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR040077A1 publication Critical patent/AR040077A1/es

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Dermatology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Molecular Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Composiciones farmacéuticas que contienen derivados de epotilona modificados por C-21, métodos para su preparación y régimen de dosis para la administración de estos compuestos de epotilona. Las composiciones son estables y fácilmente preparables para la administración al disolver en vehículos acuosos apropiados para administración intravenosa. Se describe el progreso para formar derivados de epotilona modificados por C-21 para administración oral y parenteral. Reivindicación 1: Una composición farmacéutica que comprende el compuesto de epotilona modificado por C-21 de la fórmula (1) en donde: P-Q es un enlace doble C, C o un epóxido, G es un resto del grupo de fórmulas (2); R es seleccionado del grupo de H, alquilo, y alquilo sustituido; R1 es seleccionado del grupo que consiste de fórmula (3); R2 es de fórmula (4); G1 es seleccionado del grupo de H, halógeno, CN, alquilo y alquilo sustituido; G2 es seleccionado del grupo de H, alquilo, y alquilo sustituido; G3 es seleccionado del grupo de O, S, y NZ1; G4 es seleccionado del grupo de H, alquilo, alquilo sustituido, OZ2, NZ2Z3, Z2C=O, Z4SO2, y glicosilo opcionalmente sustituido; G5 es seleccionado del grupo de halógeno, N3, NCS, SH, CN, NC, N(Z1)3+ y heteroarilo; G6 es seleccionado del grupo de H, alquilo, alquilo sustituido, CF3, OZ5, SZ5, y NZ5Z6; G7 es CZ7 o N; G8 es seleccionado del grupo de H, halógeno, alquilo, alquilo sustituido, OZ10, SZ10, NZ10 Z11; G9 es seleccionado del grupo de O, S, -NH-NH y -N=N-; G10 es N o CZ12; G11 es seleccionado del grupo de H2N, H2N sustituido, alquilo, alquilo sustituido, arilo, y arilo sustituido; Z1, Z6, Z9, y Z11 se seleccionan independientemente del grupo H, alquilo, alquilo sustituido, acilo, y acilo sustituido; Z2 es seleccionado del grupo de H, alquilo, alquilo sustituido, arilo, arilo sustituido, y heterociclo; Z3, Z5, Z8, y Z10 se seleccionan independientemente del grupo H, alquilo, alquilo sustituido, acilo, acilo sustituido, arilo, y arilo sustituido; Z4 es seleccionado del grupo de alquilo, alquilo sustituido, arilo, arilo sustituido, y heterociclo; Z7 es seleccionado del grupo de H, halógeno, alquilo, alquilo sustituido, arilo, arilo sustituido, OZ8, SZ8, y NZ8Z9; y Z12 es seleccionado del grupo H, halógeno, alquilo, alquilo sustituido, arilo, y arilo sustituido; con la condición de que cuando R1 es de fórmula (5) G1, G2, G3 y G4 no pueden tener simultáneamente los siguientes significados: G1 y G2 = H, G3 = O y G4 = H o Z2C=O donde Z2 = grupo alquilo, y con la condición de que cuando R1 es de fórmula (6) G1, G2 o G5 no tienen simultáneamente los siguientes significados: G1 y G2 = H, y G5 = F; o una sal, solvato, clatrato, hidrato o profármaco farmacéuticamente aceptable del mismo. Reivindicación 5: La composición de conformidad con la reivindicación 1, que comprende además un ácido carboxílico dibásico y un polímero farmacéuticamente aceptable.
ARP030101689A 2002-05-15 2003-05-15 Composiciones farmaceuticas y metodos de uso de derivados de epotilona modificados por c-21 AR040077A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US38063402P 2002-05-15 2002-05-15

Publications (1)

Publication Number Publication Date
AR040077A1 true AR040077A1 (es) 2005-03-16

Family

ID=29549990

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030101689A AR040077A1 (es) 2002-05-15 2003-05-15 Composiciones farmaceuticas y metodos de uso de derivados de epotilona modificados por c-21

Country Status (6)

Country Link
US (1) US7053069B2 (es)
EP (1) EP1505969A2 (es)
AR (1) AR040077A1 (es)
AU (1) AU2003234545A1 (es)
TW (1) TW200400191A (es)
WO (1) WO2003096975A2 (es)

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US20050171167A1 (en) * 2003-11-04 2005-08-04 Haby Thomas A. Process and formulation containing epothilones and analogs thereof
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Also Published As

Publication number Publication date
AU2003234545A1 (en) 2003-12-02
US20040053978A1 (en) 2004-03-18
TW200400191A (en) 2004-01-01
WO2003096975A2 (en) 2003-11-27
WO2003096975A3 (en) 2003-12-24
US7053069B2 (en) 2006-05-30
AU2003234545A8 (en) 2003-12-02
EP1505969A2 (en) 2005-02-16

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