NO940567L - Polymer-bound paclitaxel derivatives - Google Patents

Polymer-bound paclitaxel derivatives

Info

Publication number
NO940567L
NO940567L NO940567A NO940567A NO940567L NO 940567 L NO940567 L NO 940567L NO 940567 A NO940567 A NO 940567A NO 940567 A NO940567 A NO 940567A NO 940567 L NO940567 L NO 940567L
Authority
NO
Norway
Prior art keywords
phe
gly
leu
pala
ala
Prior art date
Application number
NO940567A
Other languages
Norwegian (no)
Other versions
NO940567D0 (en
Inventor
Nicola Mongelli
Francesco Angelucci
Enrico Pesenti
Antonio Suarato
Giovanni Biasoli
Original Assignee
Erba Farmitalia
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
Priority claimed from GB929213077A external-priority patent/GB9213077D0/en
Application filed by Erba Farmitalia filed Critical Erba Farmitalia
Publication of NO940567D0 publication Critical patent/NO940567D0/en
Publication of NO940567L publication Critical patent/NO940567L/en

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  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Polymerkonjugat bestående hovedsakelig av: fra 90 til 99,9 mol% av enheter med formel: -CH2 CH3-C-CO-NH-CHj-CHOH-CH3 fra 0,1 til 5 mol% av enheter representert med formel hvor en av Ra eller R2 er en kopolymer rest med formel T1 CH3-C-CO-NH-CH2-CO-A- og den andre er et hydrogenatom; fra O til 9,9 mol% av enheter representert ved formel r- CH3-C-CO-NH-CH2-CO-A-NH-CH2-CHOH-CH3 hvor R er en fenyl- eller t-butoksygruppe, R3 er H eller en acetylgruppe, A og Aj, som kan være like eller forskjellige, representerer en kjemisk enkeltbinding, en aminosyrerest eller en peptid-avstandsholder valgt fra pAla, 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-Tyr-Ala, Phe-Gly-Phe, Pge-Phe-Gly, Phe- Leu-TGly-Phe, Gly-Phe-Leu-Gly-Phe, Gly-pAla, Phe-Gly- pAla, Phe-Phe-pAla, Leu-Gly-pAla, Val-Ala-pAla, Phe- Ala-pAla, Leu-Phe-pAla, Leu-Gly-pAla, Phe-Leu-Gly-PAla, Phe-Phe-Leu-pAla, Leu-Leu-Gly-pAla, Phe-Tyr-Ala-pAla, Phe-Gly-Phe-p,. Phe-Phe-Gly-pAla, Phe-Leu-Gly-Phe-pAla eller Gly-Phe-Leu-Gly-Phe-pAla. Forbindelsene har antitumoraktivitet og forbedret vannoppløselighet og redusert toksisitet sammenlignet med paclitaxel eller dets kjente analoger. En fremgangsmåte for deres frem- stilling og farmasøytiske sammensetninger inneholdende dem er også beskrevet.Polymer conjugate consisting mainly of: from 90 to 99.9 mol% of units of formula: -CH 2 CH 3 -C-CO-NH-CH 2 -CHOH-CH 3 from 0.1 to 5 mol% of units represented by formula wherein one of Ra or R2 is a copolymer residue of formula T1 CH3-C-CO-NH-CH2-CO-A- and the other is a hydrogen atom; from 0 to 9.9 mol% of units represented by formula r-CH3-C-CO-NH-CH2-CO-A-NH-CH2-CHOH-CH3 where R is a phenyl or t-butoxy group, R3 is H or an acetyl group, A and Aj, which may be the same or different, represent a single chemical bond, an amino acid residue or a peptide spacer selected from pAla, 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-Tyr-Ala, Phe-Gly-Phe, Pge-Phe-Gly, Phe-Leu -TGly-Phe, Gly-Phe-Leu-Gly-Phe, Gly-pAla, Phe-Gly-pAla, Phe-Phe-pAla, Leu-Gly-pAla, Val-Ala-pAla, Phe-Ala-pAla, Leu -Phe-pAla, Leu-Gly-pAla, Phe-Leu-Gly-PAla, Phe-Phe-Leu-pAla, Leu-Leu-Gly-pAla, Phe-Tyr-Ala-pAla, Phe-Gly-Phe-p ,. Phe-Phe-Gly-pAla, Phe-Leu-Gly-Phe-pAla or Gly-Phe-Leu-Gly-Phe-pAla. The compounds have antitumor activity and improved water solubility and reduced toxicity compared to paclitaxel or its known analogues. A process for their preparation and pharmaceutical compositions containing them is also described.

NO940567A 1992-06-19 1994-02-18 Polymer-bound paclitaxel derivatives NO940567L (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB929213077A GB9213077D0 (en) 1992-06-19 1992-06-19 Polymerbound taxol derivatives
PCT/EP1993/001433 WO1994000156A1 (en) 1992-06-19 1993-06-07 Polymer-bound paclitaxel derivatives

Publications (2)

Publication Number Publication Date
NO940567D0 NO940567D0 (en) 1994-02-18
NO940567L true NO940567L (en) 1994-02-18

Family

ID=26070033

Family Applications (1)

Application Number Title Priority Date Filing Date
NO940567A NO940567L (en) 1992-06-19 1994-02-18 Polymer-bound paclitaxel derivatives

Country Status (1)

Country Link
NO (1) NO940567L (en)

Also Published As

Publication number Publication date
NO940567D0 (en) 1994-02-18

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