# US 5,705,388 A · CETP Ribozymes

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- Number: US 5,705,388 A
- Document ID: US5705388A
- Status: Granted
- Kind: A
- Application number: 08/363,240
- Filed: 1994-12-23
- Granted: 1998-01-06
- Earliest claimed: 1994-12-23
- Assignees: Ribozyme Pharmaceuticals, Inc.; Warner-Lambert Company
- Inventors: Larry Couture; Dan Stinchcomb; James McSwiggen; Charles Bisgaier; Michael Pape
- Web page: https://patentgrep.com/patent/US5705388A

## CPC

- C12N 15/113: Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; {Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing (when used in plants C12N15/8218)}
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/06: Antihyperlipidemics
- A61P 3/08: for glucose homeostasis (pancreatic hormones A61P5/48)
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- C12N 2310/111: spanning the whole gene, or a large part of it
- C12N 2310/121: Hammerhead
- C12N 2310/321: 2'-O-R Modification
- C12N 2310/322: 2'-R Modification
- C12N 2310/3523: Allyl
- C12N 2310/3527: Other alkyl chain
- C12N 2310/3531: Hydrogen
- C12N 2310/3533: Halogen
- C12N 2310/3535: Nitrogen
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

A nucleic acid molecule which blocks synthesis and/or expression of mRNAs associated with initial development, progression or regression of vascular disease.

## Claims

### Claim 1

An enzymatic RNA molecule which specifically cleaves RNA produced from the gene encoding cholesterol ester transfer protein (CETP).

### Claim 2 (depends on 1)

The enzymatic RNA molecule of claim 1, wherein said RNA molecule is in a hammerhead motif.

### Claim 3 (depends on 5)

The enzymatic RNA molecule of claim 5, wherein the binding arms of said enzymatic RNA molecule comprises sequences complementary to any of sequences defined as Seq ID Nos 2-258.

### Claim 4 (depends on 1)

The enzymatic RNA molecule of claim 1, wherein said RNA molecule is in a hairpin, hepatitis Delta virus, group I intron, VS nucleic acid or RNaseP RNA motif.

### Claim 5 (depends on 4)

The hairpin enzymatic RNA molecule of claim 4, wherein said hairpin RNA molecule comprises sequences complementary any of sequences defined as Seq ID Nos 1078-1125.

### Claim 6 (depends on 1)

The enzymatic RNA molecule of claim 1, wherein said enzymatic RNA molecule comprises at least one sugar modification.

### Claim 7 (depends on 1)

The enzymatic RNA molecule of claim 1, wherein said RNA comprises between 12 and 100 bases complementary to the RNA of said region.

### Claim 8 (depends on 1)

The enzymatic RNA molecule of claim 1, wherein said RNA molecule comprises between 14 and 24 bases complementary to the RNA of said region.

### Claim 9 (depends on 1)

The Enzymatic RNA molecule of claim 1, wherein said enzymatic RNA molecule comprises any of sequences shown as Seq ID Nos 259-515 and 1030-1077.

### Claim 10 (depends on 1)

A mammalian cell including an enzymatic RNA molecule of claim 1 in vitro.

### Claim 11 (depends on 10)

The mammalian cell of claim 10, wherein said cell is a human cell.

### Claim 12 (depends on 1)

An expression vector comprising nucleic acid encoding the enzymatic RNA molecule of claim 1, in a manner which allows expression and/or delivery of that enzymatic RNA molecule within a mammalian cell in vitro.

### Claim 13 (depends on 12)

A mammalian cell including the expression vector of claim 12 in vitro.

### Claim 14 (depends on 13)

The mammalian cell of claim 13, wherein said cell is a human cell.