# US 7,612,047 B2 · Degradation-resistant mononucleoside phosphate compounds

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- Number: US 7,612,047 B2
- Document ID: US7612047B2
- Status: Granted
- Kind: B2
- Application number: 12/208,265
- Filed: 2008-09-10
- Published: 2009-03-19
- Granted: 2009-11-03
- Earliest claimed: 2002-02-27
- Assignees: Inspire Pharmaceuticals, Inc.
- Inventors: James G. Douglass, III; Benjamin R. Yerxa; Sammy R. Shaver; Ward M. Peterson; Edward G. Brown; Christopher S. Crean; José L. Boyer
- Web page: https://patentgrep.com/patent/US7612047B2

## CPC

- C07H 19/10: with the saccharide radical esterified by phosphoric or polyphosphoric acids
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/02: Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61P 7/10: Antioedematous agents; Diuretics
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/02: Nasal agents, e.g. decongestants
- A61P 11/10: Expectorants
- A61P 11/16: Central respiratory analeptics
- A61P 15/02: for disorders of the vagina
- A61P 27/02: Ophthalmic agents
- A61P 27/04: Artificial tears; Irrigation solutions
- A61P 27/06: Antiglaucoma agents or miotics
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- C07H 19/20: with the saccharide radical esterified by phosphoric or polyphosphoric acids
- C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation-resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation-resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides. The mononucleoside phosphate compounds of the present invention are useful in preventing and treating epithelial tissue diseases or diseases or disorders associated with platelet aggregation.

## Claims

### Claim 1

A pyrimidine diphosphate selected from the group consisting of Compound 37-72, or a pharmaceutically acceptable salt, solvate, or hydrate thereof:

### Claim 2 (depends on 1)

The pyrimidine diphosphate according to claim 1, which is Compound 37.

### Claim 3 (depends on 1)

The pyrimidine diphosphate according to claim 1, which is Compound 45.

### Claim 4 (depends on 1)

The pyrimidine diphosphate according to claim 1, which is Compound 63.

### Claim 5

A pyrimidine triphosphate or a pyrimidine tetraphosphate selected from the group consisting of Compounds 131-168:

### Claim 6

A adenonsine triphosphate or an adenonsine tetraphosphate selected from the group consisting of Compound 193-216, or a pharmaceutically acceptable salt, solvate, or hydrate thereof:
