US5235033A
Expired / Lapsed
US
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Alpha-morpholino ribonucleoside derivatives and polymers thereof
Assignee: Sarepta Therapeutics Inc
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Filing: 1989-12-20
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Granted: 1993-08-10
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Expires: 2009-12-20
Abstract
Abstract Alpha-morpholino subunits and polymer compositions composed of alpha-morpholino subunits are disclosed. These subunits can be linked together by uncharged linkages, one to three atoms in length, joining 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. The polymers of the present invention can be used in place of standard RNA or DNA oligomers for a number of standard laboratory procedures, for example, as probes in solid-phase systems and nucleic acid hybridization analyses. Further, the polymers of the present invention have potential use as therapeutic agents in anti-sense-type technologies.
Inventors
- 👤 James E. Summerton
- 👤 Dwight D. Weller
- 👤 Eugene P. Stirchak
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 20:35
CPC Classifications
C; C07; C07H; C07H21/00; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/54; A61K47/545; A61K47/56; A61K47/59; C07K; C07K14/00; C07K14/001; C07K14/003; 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: 17
Claim 1
Independent Claim
67 words
A polymer composition comprised of α-morpholino subunit structures of the form: ##STR2## where (i) the structures are linked together by uncharged 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
67 words
A polymer composition comprised of α-morpholino subunit structures of the form: ##STR2## where (i) the structures are linked together by uncharged 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
36 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.
Claim 6
Dependent Claim
46 words
The composition of claim 1, wherein the linkage is of the form: ##STR6## where R is H, CH 3 , or other alkyl; and, P j is a purine or pyrimidine base-pairing moiety effective to bind by base-specific hydrogen bonding to a base in a polynucleotide.
Claim 7
Dependent Claim
49 words
The composition of claim 1, wherein the linkage is of the form: ##STR7## where X is alkyl, alkoxy, thioalkoxy, or an unsubstituted, monosubstituted, or disubstituted nitrogen; and, P j is a purine or pyrimidine base-pairing moiety effective to bind by base-specific hydrogen bonding to a base in a polynucleotide.
Claim 8
Dependent Claim
56 words
The composition of claim 1, wherein the linkage is of the form: ##STR8## where X is alkyl, alkoxy, thioalkoxy, or an unsubstituted, monosubstituted, or disubstituted nitrogen; R is H or CH 3 ; and P j is a purine or pyrimidine base-pairing moiety effective to bind by base-specific hydrogen bonding to a base in a polynucleotide.
Claim 9
Dependent Claim
49 words
The composition of claim 1, wherein the linkage is of the form: ##STR9## where X is alkyl, alkoxy, thioalkoxy, or an unsubstituted, monosubstituted, or disubstituted nitrogen; and, P j is a purine or pyrimidine base-pairing moiety effective to bind by base-specific hydrogen bonding to a base in a polynucleotide.
Claim 10
Dependent Claim
56 words
The composition of claim 1, wherein the linkage is of the form: ##STR10## where X is alkyl, alkoxy, thioalkoxy, or an unsubstituted, monosubstituted, or disubstituted nitrogen; R is H or CH 3 ; and P j is a purine or pyrimidine base-pairing moiety effective to bind by base-specific hydrogen bonding to a base in a polynucleotide.
Claim 11
Dependent Claim
47 words
The composition of claim 1, wherein the linkage is of the form ##STR11## where R is H or CH 3 , or other alkyl; and P j is a purine or pyrimidine base-pairing moiety effective to bind by base-specific hydrogen bonding to a base in a polynucleotide.
Claim 12
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 polymer in aqueous medium.
Claim 13
Dependent Claim
12 words
The composition of claim 11, wherein the terminal moiety is polyethylene glycol.
Claim 14
Dependent Claim
12 words
The composition of claim 1, composed of at least 3 morpholino subunits.
Claim 15
Dependent Claim
16 words
The composition of claim 1, wherein at least one of the P i is a 2,6-diaminopurine.
Claim 16
Dependent Claim
16 words
The composition of claim 1, wherein at least one of the P i is a 5-halouracil.
Claim 17
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)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1996-08-09 | 1997-02-08 | 1997-08-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2000-08-09 | 2001-02-08 | 2001-08-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2004-08-09 | 2005-02-08 | 2005-08-10 | $7700.00 | Window Closed / Lapsed |