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US5362831A Expired / Lapsed US ⏱️ 0.0 years remaining

Polymer-bound paclitaxel derivatives

Assignee: Pfizer Italia SRL
•
Filing: 1993-06-16
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Granted: 1994-11-08
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Expires: 2013-06-16
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Abstract

Abstract A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula <IMAGE> from 0.1 to 5 mol % of units represented by the formula <IMAGE> wherein one of R1 and R2 is a copolymer residue of the formula <IMAGE> and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula <IMAGE> wherein R is a phenyl or t-butoxy group, R3 is H or an acetyl group, A and A1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from 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-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe,- 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 or Gly-Phe-Leu-Gly-Phe- beta Ala. The compounds are endowed with antitumor activity and show improved water solubility and decreased toxicity in comparison with paclitaxel or its known analogs. A method for their preparation and pharmaceutical compositions containing them are also described.

Inventors

  • 👤 Nicola Mongelli
  • 👤 Francesco Angelucci
  • 👤 Enrico Pesenti
  • 👤 Antonino Suarato
  • 👤 Giovanni Biasoli

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 14:39
CPC Classifications
C; C07; C07D; C07D305/00; C07D305/14; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/58; A61P; A61P35/00

Claims Analysis

Total Claims: 4
Claim 1
Independent Claim 144 words
A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR12## from 0.1 to 5 mol % of units represented by the formula ##STR13## wherein one of R 1 and R 2 is a copolymer residue of the formula ##STR14## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR15## wherein R is a phenyl or t-butoxy group, the same or an acetyl group, A and A 1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from β 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-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe, Gly-βAla, Phe-Gly-βAla, Phe-Phe-βAla, Leu-Gly-βAla, Val-Ala-βAla, Phe-Ala-βAla, Leu-Phe-βAla, Leu-Gly-βAla, Phe-Leu-Gly-βAla, Phe-Phe-Leu βAla, Leu-Leu-Gly-βAla, Phe-Tyr-Ala-βAla, Phe-Gly-Phe-β, Phe-Phe-Gly βAla, Phe-Leu-Gly-Phe-βAla or Gly-Phe-Leu-Gly-Phe-βAla.
Claim 2
Dependent Claim 144 words
A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by the formula ##STR12## from 0.1 to 5 mol % of units represented by the formula ##STR13## wherein one of R 1 and R 2 is a copolymer residue of the formula ##STR14## and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by the formula ##STR15## wherein R is a phenyl or t-butoxy group, the same or an acetyl group, A and A 1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from β 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-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe, Gly-βAla, Phe-Gly-βAla, Phe-Phe-βAla, Leu-Gly-βAla, Val-Ala-βAla, Phe-Ala-βAla, Leu-Phe-βAla, Leu-Gly-βAla, Phe-Leu-Gly-βAla, Phe-Phe-Leu βAla, Leu-Leu-Gly-βAla, Phe-Tyr-Ala-βAla, Phe-Gly-Phe-β, Phe-Phe-Gly βAla, Phe-Leu-Gly-Phe-βAla or Gly-Phe-Leu-Gly-Phe-βAla.
Claim 3
Dependent Claim 28 words
A polymer conjugate according to claim 1, in which R represents a phenyl group, R 3 is an acetyl group and A is a Phe-Leu-Gly or Phe-Leu-Gly-βAla residue.
Claim 4
Dependent Claim 18 words
A polymer conjugate according claim 1 or 2, which is a copolymer of 1-methacryloylamino-2-hydroxypropane, (methacryloylglycyl-phenylalanylleucylglycyl)3'-amino-2-hydroxypropane and 2'-(methacryloylglycylphenylalanyl-leucylglycyl-βalanyl) paclitaxel.

References Cited (Backward Citations)

US4097470A Cited
EP0187547A2 Cited
US4960790A Cited
EP0393575A1 Cited
EP0537905A1 Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1997-11-07 1998-05-09 1998-11-08 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 2001-11-07 2002-05-09 2002-11-08 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2005-11-07 2006-05-09 2006-11-08 $7700.00 Window Closed / Lapsed

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