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High molecular weight polymer-based prodrugs

Assignee: Viskase Holdings Inc
•
Filing: 1995-01-30
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Granted: 1997-03-25
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Expires: 2015-01-30
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Abstract

Abstract Water-soluble prodrugs of the formula: <IMAGE> (I) wherein: D is a biologically active nucleophile; M is X or Q; x is an electron withdrawing group; Q is a moiety containing a free electron pair positioned five or six atoms from Y'; Y and Y' are oxygen or sulfur; R is a polyalkylene oxide; and Z is OH, C1-4 alkyl moieties or <IMAGE> are disclosed.

Inventors

  • 👤 Richard B. Greenwald
  • 👤 Annapurna Pendri

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-03 21:24
CPC Classifications
C; C07; C07D; C07D305/00; C07D305/14; A; A61; A61K; A61K31/00; A61K31/33; A61K31/335; A61K31/74; A61K31/765; A61K31/77; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/59; A61K47/60; C07C; C07C217/00; C07C217/02; C07C217/04; C07C217/06; C07C217/08; C07C265/00; C07C265/02; C07C265/04; C07C265/14; C07C271/00; C07C271/06; C07C271/32; C07C271/34; C07C275/00; C07C275/04; C07C275/06; C07C275/10; C07C331/00; C07C331/16; C07C331/18; C07C331/20

Claims Analysis

Total Claims: 12
Claim 1
Independent Claim 36 words
A composition of the formula: ##STR26## wherein: R 1 is C 6 H 5 or (CH 3 ) 3 CO; R 2 is H or CH 3 CO; and R 3 is aryl, aralkyl or heteroaryl.
Claim 2
Dependent Claim 36 words
A composition of the formula: ##STR26## wherein: R 1 is C 6 H 5 or (CH 3 ) 3 CO; R 2 is H or CH 3 CO; and R 3 is aryl, aralkyl or heteroaryl.
Claim 3
Dependent Claim 10 words
The composition of claim 1, wherein R 3 is phenyl.
Claim 4
Dependent Claim 95 words
A taxane-based composition, comprising the formula: ##STR27## wherein: R 1 is C 6 H 5 (CH 3 ) 3 CO; R 2 is H or CH 3 CO; R 3 is aryl, aralkyl or heteroaryl; M is X or Q; X is an electron withdrawing group; Q is a moiety containing a free electron pair positioned five or six atoms from Y', Y and Y' are independently O or S; R is a polyalkylene oxide; and Z is one of OH, a C 1-4 alkyl moiety or ##STR28## wherein D is a biologically active nucleophile.
Claim 5
Dependent Claim 95 words
A taxane-based composition, comprising the formula: ##STR27## wherein: R 1 is C 6 H 5 (CH 3 ) 3 CO; R 2 is H or CH 3 CO; R 3 is aryl, aralkyl or heteroaryl; M is X or Q; X is an electron withdrawing group; Q is a moiety containing a free electron pair positioned five or six atoms from Y', Y and Y' are independently O or S; R is a polyalkylene oxide; and Z is one of OH, a C 1-4 alkyl moiety or ##STR28## wherein D is a biologically active nucleophile.
Claim 6
Dependent Claim 11 words
The composition of claim 3, wherein R is a polyethylene glycol.
Claim 7
Dependent Claim 13 words
The composition of claim 3, wherein X, Y and Y' are each O.
Claim 8
Dependent Claim 9 words
The composition of claim 3, wherein Z is methyl.
Claim 9
Dependent Claim 39 words
The composition of claim 3 comprising the structure: ##STR29## wherein: R 1 is C 6 H 5 or (CH 3 ) 3 CO; R 2 is H or CH 3 CO; and R 3 is aryl, aralkyl or heteroaryl.
Claim 10
Dependent Claim 20 words
The composition of claim 3, wherein said polyalkylene oxide has a molecular weight of from about 20,000 to about 80,000.
Claim 11
Dependent Claim 20 words
The composition of claim 8, wherein said polyalkylene oxide has a molecular weight of from about 25,000 to about 45,000.
Claim 12
Dependent Claim 20 words
The composition of claim 9, wherein said polyalkylene oxide has a molecular weight of from about 30,000 to about 42,000.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 2000-03-24 2000-09-23 2001-03-25 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 2004-03-24 2004-09-23 2005-03-25 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2008-03-24 2008-09-23 2009-03-25 $7700.00 Window Closed / Lapsed

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