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US5185444A Expired / Lapsed US ⏱️ 0.0 years remaining

Uncharged morpolino-based polymers having phosphorous containing chiral intersubunit linkages

Assignee: Sarepta Therapeutics Inc
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Filing: 1991-11-21
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Granted: 1993-02-09
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Expires: 2011-11-21
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Abstract

Abstract A polymer composition is disclosed composed of morpholino subunit structures linked together by uncharged, chiral linkages, one-three atoms in length. These chiral linkages join the morpholino nitrogen of one subunit to the 5' exocyclic carbon of an adjacent subunit. Each subunit contains a purine or pyrimidine base-pairing moiety effective to bind by hydrogen bonding to a specific base or base-pair in a target polynucleotide.

Inventors

  • 👤 James E. Summerton
  • 👤 Dwight D. Weller

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-05 07:08
CPC Classifications
C; C07; C07H; C07H21/00; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/54; A61K47/545; A61K47/548; A61K47/56; A61K47/59; A61K47/60; A61K47/605; C07K; C07K14/00; C07K14/001; C07K14/003; C08; C08G; C08G79/00; C08G79/02; C12; C12Q; C12Q1/00; C12Q1/68; C12Q1/6813; C12Q1/6816; C12Q1/682; B; B01; B01J; B01J2219/00; B01J2219/00274; B01J2219/00718; B01J2219/0072

Claims Analysis

Total Claims: 16
Claim 1
Independent Claim 69 words
A polymer composition comprised of morpholino subunit structures of the form: ##STR2## where (i) the structures are linked together by uncharged phosphorous-containing, chiral linkages, one to three atoms long, joining the morpholino nitrogen of one subunit to the 5', exocyclic carbon of an adjacent subunit, and (ii) P i is a purine or pyrimidine base-pairing moiety effective to bind by base-specific hydrogen bonding to a base in a polynucleotide.
Claim 2
Dependent Claim 69 words
A polymer composition comprised of morpholino subunit structures of the form: ##STR2## where (i) the structures are linked together by uncharged phosphorous-containing, chiral linkages, one to three atoms long, joining the morpholino nitrogen of one subunit to the 5', exocyclic carbon of an adjacent subunit, and (ii) P i is a purine or pyrimidine base-pairing moiety effective to bind by base-specific hydrogen bonding to a base in a polynucleotide.
Claim 3
Dependent Claim 28 words
The composition of claim 1, wherein P i is selected from the group consisting of: ##STR3## where X is H, CH 3 , F, Cl, Br, or I.
Claim 4
Dependent Claim 19 words
The composition of claim 1, wherein the linked structures have a form selected from the group consisting of: ##STR4##
Claim 5
Dependent Claim 82 words
The composition of claim 1, wherein the linkage is of the form: ##STR5## where P j is a purine or pyrimidine base-pairing moiety effective to bind by base-specific hydrogen bonding to a base in a polynucleotide; and, X is F, CH 2 R, O--CH 2 R, S--CH 2 R, or NR 1 R 2 ; and each of R, R 1 and R 2 is H, CH 3 , or other moiety that does not interfere with said base specific hydrogen bonding.
Claim 6
Dependent Claim 83 words
The composition of claim 1, wherein the linkage is of the form: ##STR6## where P j is a purine or pyrimidine base-pairing moiety effective to bind by base-specific hydrogen bonding to a base in a polynucleotide; and, X is F, CH 2 R, O--CH 2 R, S--CH 2 R, or NR 1 R 2 ; and each of R, R 1 and R 2 , is H, CH 3 , or other moiety that does not interfere with said base specific hydrogen bonding.
Claim 7
Dependent Claim 42 words
The composition of claim 1, wherein the linkage is of the form: ##STR7## where P j is a purine or pyrimidine base-pairing moiety effective to bind by base-specific hydrogen bonding to a base in a polynucleotide; and, Z is O or S.
Claim 8
Dependent Claim 42 words
The composition of claim 1, wherein the linkage is of the form: ##STR8## where P j is a purine or pyrimidine base-pairing moiety effective to bind by base-specific hydrogen bonding to a base in a polynucleotide; and, Z is O or S.
Claim 9
Dependent Claim 83 words
The composition of claim 1, wherein the linkage is of the form: ##STR9## where P j is a purine or pyrimidine base-pairing moiety effective to bind by base-specific hydrogen bonding to a base in a polynucleotide; and, X is F, CH 2 R, O--CH 2 R, S--CH 2 R, or NR 1 R 2 ; and each of R, R 1 and R 2 , is H, CH 3 , or other moeity which does not interfere with said base specific hydrogen bonding.
Claim 10
Dependent Claim 83 words
The composition of claim 1, wherein the linkage is of the form: ##STR10## where P j is a purine or pyrimidine base-pairing moiety effective to bind by base-specific hydrogen bonding to a base in a polynucleotide; and, X is F, CH 2 R, O--CH 2 R, S--CH 2 R, or NR 1 R 2 ; and each of R, R 1 and R 2 , is H, CH 3 , or other moeity which does not interfere with said base specific hydrogen bonding.
Claim 11
Dependent Claim 28 words
The composition of claim 1, which further includes a moiety at one or both termini which is effective to enhance the solubility of the molecules in aqueous medium.
Claim 12
Dependent Claim 16 words
The composition of claim 10, wherein the moiety at one or both termini is polyethylene glycol.
Claim 13
Dependent Claim 12 words
The composition of claim 1, composed of at least 3 morpholino subunits.
Claim 14
Dependent Claim 16 words
The composition of claim 1, wherein at least one of the P i is a 2,6-diaminopurine.
Claim 15
Dependent Claim 16 words
The composition of claim 1, wherein at least one of the P i is a 5-halouracil.
Claim 16
Dependent Claim 17 words
The composition of claim 1, wherein at least 70% of the P i are 2-amine containing purines.

References Cited (Backward Citations)

US4558047A Cited
WO1986005519A1 Cited
WO1986005518A1 Cited
US5034506A Cited
WO1991018898A1 Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1996-02-09 1996-08-10 1997-02-09 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 2000-02-09 2000-08-10 2001-02-09 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2004-02-09 2004-08-10 2005-02-09 $7700.00 Window Closed / Lapsed

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