# US 7,745,431 B2 · Pharmaceutical composition of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine and uses thereof

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- Number: US 7,745,431 B2
- Document ID: US7745431B2
- Status: Granted
- Kind: B2
- Application number: 10/728,261
- Filed: 2003-12-03
- Published: 2004-08-12
- Granted: 2010-06-29
- Earliest claimed: 2002-12-03
- Assignees: Vela Acquisition Corporation
- Inventors: Herbert W. Harris; Robert F. Kucharik; Steven M. Leventer
- Web page: https://patentgrep.com/patent/US7745431B2

## CPC

- A61K 31/5513: 1,4-Benzodiazepines, e.g. diazepam {or clozapine}
- A61K 31/551: having two nitrogen atoms, e.g. dilazep
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- A61P 9/12: Antihypertensives
- A61P 11/06: Antiasthmatics
- A61P 13/12: of the kidneys
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 17/06: Antipsoriatics
- A61P 19/00: Drugs for skeletal disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/06: Antimigraine agents
- A61P 25/08: Antiepileptics; Anticonvulsants
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/24: Antidepressants
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- 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 35/00: Antineoplastic agents
- A61P 37/02: Immunomodulators
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

Pharmaceutical compositions comprising 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine; or a pharmaceutically acceptable salt thereof. The compositions are used for treating, preventing or delaying the onset of disorders mediated by LTB4, TXA2 or adenosine.

## Claims

### Claim 1

A pharmaceutical composition comprising a pharmaceutically acceptable carrier and 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The pharmaceutical composition according to claim 1, comprising (R)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine substantially free of the corresponding (S)-enantiomer; or a pharmaceutically acceptable salt thereof.

### Claim 3 (depends on 2)

The composition according to claim 2 wherein the amount of (R)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 85% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.

### Claim 4 (depends on 3)

The composition according to claim 3 wherein the amount of (R)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 90% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl -7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.

### Claim 5 (depends on 4)

The composition according to claim 4 wherein the amount of (R)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 95% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl -7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.

### Claim 6 (depends on 5)

The composition according to claim 5 wherein the amount of (R)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 99% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.

### Claim 7 (depends on 1)

The pharmaceutical composition according to claim 1, comprising (S)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine substantially free of the corresponding (R)-enantiomer; or a pharmaceutically acceptable salt thereof.

### Claim 8 (depends on 7)

The composition according to claim 7 wherein the amount of (S)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 85% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.

### Claim 9 (depends on 8)

The composition according to claim 8 wherein the amount of (S)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 90% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl -7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.

### Claim 10 (depends on 9)

The composition according to claim 9 wherein the amount of (S)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 95% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.

### Claim 11 (depends on 10)

The composition according to claim 10 wherein the amount of (S)-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or pharmaceutically acceptable salt thereof, in the composition is 99% by weight or more of the total weight of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl -7-methoxy-8-hydroxy-5H-2,3-benzodiazepine.

### Claim 12 (depends on 1)

The pharmaceutical composition according to claim 1, comprising a racemic mixture of the (R)- and (S)-enantiomers of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7-methoxy-8-hydroxy-5H-2,3-benzodiazepine, or a pharmaceutically acceptable salt thereof.

### Claim 13 (depends on 1)

A method of treating a disorder characterized by convulsive seizures in an individual in need of such treatment, comprising administering to said individual a therapeutically effective amount of the composition according to claim 1 sufficient to inhibit convulsive seizures in said individual.

### Claim 14 (depends on 2)

A method of treating a disorder characterized by convulsive seizures in an individual in need of such treatment, comprising administering to said individual a therapeutically effective amount of the composition according to claim 2 sufficient to inhibit convulsive seizures in said individual.

### Claim 15 (depends on 7)

A method of treating a disorder characterized by convulsive seizures in an individual in need of such treatment, comprising administering to said individual a therapeutically effective amount of the composition according to claim 7 sufficient to inhibit convulsive seizures in said individual.

### Claim 16 (depends on 12)

A method of treating a disorder characterized by convulsive seizures in an individual in need of such treatment, comprising administering to said individual a therapeutically effective amount of the composition according to claim 12 sufficient to inhibit convulsive seizures in said individual.