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US5776907A
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Mitomycin oligonucleotide conjugates
Assignee: Encysive Pharmaceuticals Inc
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Filing: 1996-05-20
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Granted: 1998-07-07
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Expires: 2016-05-20
Abstract
Abstract The present invention provides conjugates of mitomycin C or derivatives thereof and oligonucleotides. A conjugate of the present invention corresponds to formula I, below: <IMAGE> I where R is H, CH3, or C(O)SCH3, R' is O or NH, m is an integer from 1 to 10 and Ogn is an oligonucleotide. Pharmaceutical compositions and methods of using such conjugates to inhibit gene product expression are also provided.
Inventors
- 👤 Harold L. Kohn
- 👤 Nam Huh
- 👤 Timothy P. Kogan
- 👤 Ajay A. Rege
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 16:23
CPC Classifications
C; C07; C07D; C07D487/00; C07D487/12; C07D487/14; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/54; A61K47/549; C07H; C07H21/00; C12; C12N; C12N15/00; C12N15/09; C12N15/11; C12N15/113; C12N15/1135; C12N15/1138; A61K38/00; C12N2310/00; C12N2310/30; C12N2310/35; C12N2310/351
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
21 words
A conjugate comprising an antisense oligonucleotide conjugated to the carbon atom at position 10 of mitomycin C or a derivative thereof.
Claim 2
Dependent Claim
21 words
A conjugate comprising an antisense oligonucleotide conjugated to the carbon atom at position 10 of mitomycin C or a derivative thereof.
Claim 3
Dependent Claim
27 words
The conjugate of claim 1 wherein the antisense oligonucleotide is conjugated to mitomycin C via an alkylamino spacer group attached to the 5' end of the oligonucleotide.
Claim 4
Dependent Claim
15 words
The conjugate of claim 2 wherein the spacer group contains one to 10 carbon atoms.
Claim 5
Dependent Claim
15 words
The conjugate of claim 3 wherein the alkylamino group contains five or six carbon atoms.
Claim 6
Dependent Claim
16 words
The conjugate of claim 1 wherein the oligonucleotide contains from about 10 to about 50 nucleotides.
Claim 7
Dependent Claim
16 words
The conjugate of claim 5 wherein the oligonucleotide contains from about 20 to about 40 nucleotides.
Claim 8
Dependent Claim
22 words
The conjugate of claim 1 wherein nucleotides of the oligonucleotide are linked by pseudophosphate bonds resistant to cleavage by exo- or endonucleases.
Claim 9
Dependent Claim
40 words
The conjugate of claim 3 having the structure I, below: ##STR11## where R is H, CH 3 or C(O)SCH 3 , R' is O or NH, m is an integer from 1 to 10 and Ogn is an antisense oligonucleotide.
Claim 10
Dependent Claim
20 words
The conjugate of claim 8 wherein R is CH 3 , R' is NH and m is 5 or 6.
Claim 11
Dependent Claim
19 words
The conjugate of claim 8 wherein the Ogn has the nucleotide sequence of any of SEQ ID NOs: 1-6.
Claim 12
Dependent Claim
14 words
A pharmaceutical composition comprising a conjugate of claim 1 in a physiologically acceptable carrier.
Claim 13
Dependent Claim
42 words
A process of inhibiting expression of a gene in a vascular smooth muscle cell comprising exposing the cell to a conjugate of claim 1 containing an antisense oligonucleotide that hybridizes to a portion of the gene and inhibits expression of the gene.
Claim 14
Dependent Claim
25 words
The process of claim 12 wherein the gene is the human A-raf-1 gene and the oligonucleotide has the nucleotide sequence of SEQ ID NO: 1.
Claim 15
Dependent Claim
31 words
The process of claim 12 wherein the gene is the human fibroblast growth factor receptor 1 gene and the oligonucleotide has the nucleotide sequence of any of SEQ ID NOs: 2-6.
Claim 16
Dependent Claim
42 words
A process of inhibiting vascular smooth muscle cell proliferation comprising exposing the vascular smooth muscle cell to a conjugate of claim 1 wherein the Ogn is an antisense oligonucleotide directed against the human A-raf-1 or human fibroblast growth factor receptor 1 gene.
Claim 17
Dependent Claim
19 words
The process of claim 15 wherein the oligonucleotide has the nucleotide sequence of any of SEQ ID NOs: 1-6.
References Cited (Backward Citations)
US5593974A
Cited
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