# US 5,707,651 A · Soft capsules containing dinreburnamenine compounds

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- Number: US 5,707,651 A
- Document ID: US5707651A
- Status: Granted
- Kind: A
- Application number: 08/608,284
- Filed: 1996-02-28
- Granted: 1998-01-13
- Earliest claimed: 1995-03-03
- Assignees: Roussel Uclaf
- Inventors: Philippe Becourt; Jean-Luc Dubois; Pierre Metziger
- Web page: https://patentgrep.com/patent/US5707651A

## CPC

- A61K 31/4375: the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
- A61K 9/4858: {Organic compounds}
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/24: Antidepressants
- A61P 25/26: Psychostimulants, e.g. nicotine, cocaine
- 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 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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

## Abstract

A soft capsule containing a) a capsule casing containing gelatin and optionally a plasticizer and other additives, b) a compound of the formula ##STR1## wherein R1, R2 and R3 are individually selected from the group consisting of hydrogen, halogen, alkyl and alkoxy of 1 to 5 carbon atoms, --OH, --CF3, --NO2, --NH2, alkylamino and dialkylamino of 1 to 5 alkyl carbon atoms and acylamino of acyl of an aliphatic carboxylic acid of 1 to 6 carbon atoms or a non-toxic, pharmaceutically acceptable acid addition salt thereof and c) at least one mineral oil and optionally a pharmaceutical carrier.

## Claims

### Claim 1

A soft capsule comprising a) a capsule casing containing gelatin and optionally a plasticizer and additives, b) a compound of the formula ##STR5## wherein R1, R2 and R3 are individually selected from the group consisting of hydrogen, halogen, alkyl and alkoxy of 1 to 5 carbon atoms, --OH, CF3, --NO2, --NH2, alkylamino and dialkylamino of 1 to 5 alkyl carbon atoms and acylamino of acyl of an aliphatic carboxylic acid of 1 to 6 carbon atoms or a non-toxic, pharmaceutically acceptable acid addition salt thereof and c) at least one mineral oil and optionally a pharmaceutical carrier.

### Claim 2 (depends on 1)

A soft capsule of claim 1, wherein R1 and R2 are hydrogen and R3 is alkyl of 1 to 5 carbon atoms.

### Claim 3 (depends on 1)

A soft capsule of claim 1 wherein R1 and R2 are hydrogen and R3 is 11-methyl.

### Claim 4 (depends on 1)

A soft capsule of claim 1 wherein components b) and c) are at least one member of the group consisting of vaseline, vaseline oil and silicone fluid.

### Claim 5 (depends on 1)

A soft capsule of claim 1 containing a mixture of vaseline and vaseline oil.

### Claim 6 (depends on 1)

A soft capsule of claim 1 containing 1 g to 20% by weight of (3.alpha.)11-methyl-20,21-dinoreburnamenine maleate or fumarate.

### Claim 7 (depends on 1)

A process for the preparation process of soft capsules of claim 1 comprising forming a mixture of gelatin and optionally a plasticizer and additives, forming a capsule casing from said mixture and filling the soft capsule with a mixture of a compound of formula I of claim 1 and at least one mineral oil.