ES2164663T3 - Derivados de paclitaxel unidos a polimeros. - Google Patents

Derivados de paclitaxel unidos a polimeros.

Info

Publication number
ES2164663T3
ES2164663T3 ES93912905T ES93912905T ES2164663T3 ES 2164663 T3 ES2164663 T3 ES 2164663T3 ES 93912905 T ES93912905 T ES 93912905T ES 93912905 T ES93912905 T ES 93912905T ES 2164663 T3 ES2164663 T3 ES 2164663T3
Authority
ES
Spain
Prior art keywords
phe
gly
leu
ala
beta
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES93912905T
Other languages
English (en)
Inventor
Nicola Mongelli
Francesco Angelucci
Enrico Pesenti
Antonio Suarato
Giovanni Biasoli
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pfizer Italia SRL
Original Assignee
Pharmacia and Upjohn SpA
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 Pharmacia and Upjohn SpA filed Critical Pharmacia and Upjohn SpA
Application granted granted Critical
Publication of ES2164663T3 publication Critical patent/ES2164663T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D305/00—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
    • C07D305/14—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—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 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
    • A61K47/58—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 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 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Abstract

UN POLIMERO CONJUGADO QUE SE COMPONE ESENCIALMENTE DE : DESDE 90 A 99,9 MOLES % DE UNIDADES REPRESENTADAS POR LA FORMULA (A); DESDE 0,1 A 5 MOLES % DE UNIDADES REPRESENTADAS POR FORMULA (B), EN DONDE UNO DE R1 Y R2 ES UN RESIDUO COPOLIMERO DE FORMULA (C), Y EL OTRO ES ATOMO DE HIDROGENO; DE 0 A 9,9 MOLES % DE UNIDADES REPRESENTADAS POR FORMULA (D), EN DONDE R ES UN GRUPO FENILO O GRUPO T-BUTOXILO, R3 ES H O UN GRUPO ACETILO, A Y A1 LOS CUALES PUEDEN SER EL MISMO O DIFERENTE, REPRESENTAN UN SIMPLE ENLACE QUIMICO, UN RESIDUO AMINO ACIDO O PEPTIDA SEPARADORA SELECCIONADA DE (BETA) ALA, GLY, PHE-GLY, PHE-PHE, LEU-GLY, VAL-ALA, PHE-ALA, LEU-PHE, LEU-ALA, PHE-LEU-GLY, PHE-PHE-LEU, LEU-LEU-GLY, PHE-GLY-PHE, PHE-PHE-GLY, PHE-LEU-GLY-PHE, GLY-PHE-LEU-GLY-PHE, GLY-(BETA) ALA, PHE-GLY-(BETA)ALA, PHE-PHE-(BETA)ALA, LEU-GLY-(BETA)ALA, VAL-ALA-(BETA)ALA, PHE-ALA-(BETA)ALA, LEU-PHE-(BETA)ALA, LEU-GLY-(BETA)ALA, PHE-LEU-GLY-(BETA)ALA, PHE-PHE-LEU-(BETA)ALA, LEU-LEU-GLY-(BETA)ALA, PHE-TYR-ALA-(BETA)ALA, PHE-GLY-PHE-(BETA), PHE-PHE-GLY(BETA)ALA, PHE-LEU-GLY-PHE-(BETA)ALA O GLY-PHE-LEU-GLY-PHE-(BETA)ALA. LOS COMPUESTOS ESTAN TERMINADOS CON ACTIVIDAD ANTI-TUMOR Y MUESTRAN SOLUBILIDAD EN AGUA MEJORADA Y REDUCIDA TOXICIDAD EN COMPARACION CON PACLITAXEL O SUS ANALOGOS CONOCIDOS. UN METODO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN TAMBIEN SE DESCRIBEN.
ES93912905T 1992-06-19 1993-06-07 Derivados de paclitaxel unidos a polimeros. Expired - Lifetime ES2164663T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB929213077A GB9213077D0 (en) 1992-06-19 1992-06-19 Polymerbound taxol derivatives

Publications (1)

Publication Number Publication Date
ES2164663T3 true ES2164663T3 (es) 2002-03-01

Family

ID=10717411

Family Applications (1)

Application Number Title Priority Date Filing Date
ES93912905T Expired - Lifetime ES2164663T3 (es) 1992-06-19 1993-06-07 Derivados de paclitaxel unidos a polimeros.

Country Status (25)

Country Link
US (4) US5362831A (es)
EP (1) EP0600062B1 (es)
JP (1) JP3693340B2 (es)
KR (1) KR100281606B1 (es)
CN (1) CN1041281C (es)
AT (1) ATE205725T1 (es)
AU (2) AU659750B2 (es)
CA (1) CA2112482A1 (es)
CZ (1) CZ62094A3 (es)
DE (1) DE69330776T2 (es)
ES (1) ES2164663T3 (es)
FI (1) FI940733A (es)
GB (1) GB9213077D0 (es)
HU (2) HUT67914A (es)
IL (1) IL106023A (es)
MX (1) MX9303598A (es)
MY (1) MY109213A (es)
NZ (1) NZ253116A (es)
PL (1) PL173898B1 (es)
RU (1) RU2130462C1 (es)
SG (1) SG49248A1 (es)
TW (1) TW266201B (es)
UA (1) UA39926C2 (es)
WO (1) WO1994000156A1 (es)
ZA (1) ZA934388B (es)

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