US5514786A
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Compositions for inhibiting RNA activity
Assignee: Ionis Pharmaceuticals Inc
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Filing: 1992-09-10
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Granted: 1996-05-07
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Expires: 2012-09-10
Abstract
Abstract Compositions and methods for modulating the activity of RNA are disclosed. In accordance with preferred embodiments, antisense compositions are prepared comprising targeting and reactive portions. The reactive portions preferably comprise one or two imidazole functionalities conjugated to the targeting oligonucleotide via linkers with or without intervening intercalating moieties. Therapeutics, diagnostics and research methods also are disclosed, as are synthetic nucleosides and nucleoside fragments that can be elaborated into oligonucleotides.
Inventors
- 👤 Phillip D. Cook
- 👤 Thomas Bruice
- 👤 Charles J. Guinosso
- 👤 Andrew M. Kawasaki
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 17:29
CPC Classifications
C; C12; C12N; C12N15/00; C12N15/09; C12N15/11; C12N15/113; A; A61; A61K; A61K48/00; A61P; A61P31/00; A61P31/12; A61P43/00; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/06; C07H19/10; C07H19/16; C07H19/20; C07H21/00; C07H23/00; C07J; C07J43/00; C07J43/003; C07K; C07K14/00; C07K14/005; C12N15/1137; C12N9/00; C12N9/0004; C12N9/0069; C12Q; C12Q1/00; C12Q1/68; C12Q1/6813; C12Y; C12Y113/00; C12Y113/11; C12Y113/11012; A61K38/00; C12N2310/00; C12N2310/30; C12N2310/31; C12N2310/312; C12N2310/3125; C12N2310/315; C12N2310/32; C12N2310/321; C12N2310/322; C12N2310/33; C12N2310/333; C12N2310/336; C12N2310/35; C12N2310/351; C12N2310/3511; C12N2310/352; C12N2310/3521; C12N2310/3523; C12N2310/3527; C12N2310/353; C12N2310/3531; C12N2310/3533; C12N2740/00; C12N2740/00011; C12N2740/10011; C12N2740/16011; C12N2740/16311; C12N2740/16322
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
42 words
A compound of the structure: G.sub.0 --G.sub.1 --G.sub.2 --G.sub.3 wherein: G 0 is a nucleoside, a nucleotide or an oligonucleotide; G 1 is O--alkyl, O--alkenyl, or O--alkynyl; G 2 is an aryl moiety; and G 3 includes at least one imidazole moiety.
Claim 2
Dependent Claim
42 words
A compound of the structure: G.sub.0 --G.sub.1 --G.sub.2 --G.sub.3 wherein: G 0 is a nucleoside, a nucleotide or an oligonucleotide; G 1 is O--alkyl, O--alkenyl, or O--alkynyl; G 2 is an aryl moiety; and G 3 includes at least one imidazole moiety.
Claim 3
Dependent Claim
32 words
The compound of claim 1 wherein G 2 is a polycyclic moiety having from two to six rings, at least two of said rings being joined to form a conjugated ring system.
Claim 4
Dependent Claim
11 words
The compound of claim 2 wherein G 2 is an intercalator.
Claim 5
Dependent Claim
16 words
The compound of claim 1 wherein G 2 is naphthalene, anthracene, phenanthrene, benzonaphthalene, fluorene, or pyrene.
Claim 6
Dependent Claim
79 words
The compound of claim 1 wherein G 3 is an imidazole; a C2-substituted imidazole; an imidazole substituted at a C4 or C5 position with an electrophilic catalyst; a bis-imidazole; a C2-substituted bis-imidazole; a bis-imidazole wherein at least one C4 or C5 position is substituted with an electrophilic catalyst; a bis-imidazole wherein both C4 positions or both C5 positions are substituted with electrophilic catalyst; or a bis-imidazole wherein the linkage between the imidazole rings is substituted with an electrophilic catalyst.
Claim 7
Dependent Claim
17 words
The compound of claim 5 wherein said electrophilic catalyst comprises a nitrogen functionality that can be protonated.
Claim 8
Dependent Claim
18 words
The compound of claim 6 wherein said nitrogen functionality is an amine, a nitrogen heterocycle, guanidine or amidine.
Claim 9
Dependent Claim
18 words
The compound of claim 1 wherein G 2 and G 3 are connected through a single covalent bond.
Claim 10
Dependent Claim
22 words
The compound of claim 8 wherein G 3 includes at least one imidazole moiety covalently bound through a C4 or C5 position.
Claim 11
Dependent Claim
22 words
The compound of claim 1 wherein G 1 connects to G 0 at a 2' sugar position of said G 0 .
Claim 12
Dependent Claim
77 words
A compound of the structure: ##STR10## T 5 is H, a hydroxyl protecting group, a phosphate group, a nucleotide or an oligonucleotide; T 3 is H, a hydroxyl protecting group, a nucleotide, an oligonucleotide, a phosphate group, an activated phosphate group or solid phase support; G 1' is O; G 1" is alkyl, alkenyl, or alkynyl; G 2 is an aryl moiety; G 3 includes at least one imidazole moiety; and Bx is a heterocyclic base moiety.
Claim 13
Dependent Claim
77 words
A compound of the structure: ##STR10## T 5 is H, a hydroxyl protecting group, a phosphate group, a nucleotide or an oligonucleotide; T 3 is H, a hydroxyl protecting group, a nucleotide, an oligonucleotide, a phosphate group, an activated phosphate group or solid phase support; G 1' is O; G 1" is alkyl, alkenyl, or alkynyl; G 2 is an aryl moiety; G 3 includes at least one imidazole moiety; and Bx is a heterocyclic base moiety.
Claim 14
Dependent Claim
11 words
The compound of claim 11 wherein G 2 is an intercalator.
Claim 15
Dependent Claim
10 words
The compound of claim 11 wherein G 1" is alkynyl.
Claim 16
Dependent Claim
12 words
The compound of claim 11 wherein G 2 includes a polycyclic system.
Claim 17
Dependent Claim
23 words
The compound of claim 14 wherein said polycyclic system has two to six rings and at least two of said rings are conjugated.
Claim 18
Dependent Claim
16 words
The compound of claim 11 wherein G 2 is naphthalene, anthracene, phenanthrene, benzonaphthalene, fluorene, or pyrene.
Claim 19
Dependent Claim
12 words
The compound of claim 11 wherein G 3 is an imidazole moiety.
Claim 20
Dependent Claim
12 words
The compound of claim 11 wherein G 3 is a bis-imidazole moiety.
Claim 21
Dependent Claim
12 words
The compound of claim 11 wherein Bx is a purine heterocyclic base.
Claim 22
Dependent Claim
78 words
A compound of the structure: ##STR11## T 5 is H, a hydroxyl protecting group, a phosphate group, a nucleotide or an oligonucleotide; T 3 is H, a hydroxyl protecting group, a nucleotide, an oligonucleotide, a phosphate group, an activated phosphate group or a solid phase support; G 1' is O; G 1" is alkynyl; and Bx is a heterocyclic base moiety, provided that when Bx is uracil then T 3 and T 5 are not H or acetyl.
Claim 23
Dependent Claim
78 words
A compound of the structure: ##STR11## T 5 is H, a hydroxyl protecting group, a phosphate group, a nucleotide or an oligonucleotide; T 3 is H, a hydroxyl protecting group, a nucleotide, an oligonucleotide, a phosphate group, an activated phosphate group or a solid phase support; G 1' is O; G 1" is alkynyl; and Bx is a heterocyclic base moiety, provided that when Bx is uracil then T 3 and T 5 are not H or acetyl.
Claim 24
Dependent Claim
10 words
The compound of claim 20 wherein G 1" is propargyl.
References Cited (Backward Citations)
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