NO940567L - Polymer-bound paclitaxel derivatives - Google Patents
Polymer-bound paclitaxel derivativesInfo
- 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
Links
Landscapes
- 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.
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) |
-
1994
- 1994-02-18 NO NO940567A patent/NO940567L/en not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
NO940567D0 (en) | 1994-02-18 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FC2A | Withdrawal, rejection or dismissal of laid open patent application |