# US 9,040,520 B2 · Noribogaine salt ansolvates

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- Number: US 9,040,520 B2
- Document ID: US9040520B2
- Status: Granted
- Kind: B2
- Application number: 13/619,520
- Filed: 2012-09-14
- Published: 2013-03-21
- Granted: 2015-05-26
- Earliest claimed: 2011-09-15
- Assignees: Demerx, Inc.
- Applicants: Richard D. Gless, Jr.; William C. Schinzer
- Inventors: Richard D. Gless, Jr.; William C. Schinzer
- Web page: https://patentgrep.com/patent/US9040520B2

## CPC

- C07D 471/22: in which the condensed systems contains four or more hetero rings
- A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/30: for treating abuse or dependence
- A61P 25/36: Opioid-abuse
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- C07D 453/06: containing isoquinuclidine ring systems
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

Stable noribogaine salt ansolvates are useful for preparing pharmaceutical compositions and for alleviating nociceptive pain in a patient. Such ansolvates can be prepared by slurrying solvated forms, preferably MeOH solvated noribogaine hydrochloride in EtOH/water.

## Claims

### Claim 1

A stable pharmaceutically acceptable salt of noribogaine ansolvate, which is amorphous or
is a crystalline hydrochloride salt having an X-ray powder diffraction pattern comprising peaks at 11.6±0.2° 2θ, 12.1±0.2° 2θ, 13.5±0.2° 2θ, 13.9±0.2° 2θ, 14.9±0.2° 2θ, 15.7±0.2° 2θ, 17.1±0.2° 2θ, 17.9±0.2° 2θ, 18.3±0.2° 2θ, 19.8±0.2° 2θ, 20.8±0.2° , 21.0±0.2° 2θ, 21.9±0.2° 2θ, 22.8±0.2° 2θ, 23.3±0.2° 2θ, 24.9±0.2° 2θ, 25.9±0.2° , 26.4±0.2° 2θ, 29.3±0.2° 2θ and 29.8±0.2° 2θ as shown in FIG. 3; or
is a crystalline sulfate salt having an X-ray powder diffraction pattern comprising peaks at 8.5±0.2° 2θ, 11.4±0.2° 2θ, 12.0±0.2° 2θ, 13.3±0.2° 2θ, 15.4±0.2° 2θ, 16.6±0.2° , 17.2±0.2° 2θ, 18.3±0.2° 2θ, 20.6±0.2° 2θ, 21.0±0.2° 2θ and 21.5±0.2° 2θ as shown in FIG. 8;
when analyzed using CuKα X-ray radiation.

### Claim 2 (depends on 1)

The crystalline salt of claim 1, having an X-ray powder diffraction pattern comprising peaks at 11.6±0.2° 2θ, 12.1±0.2° 2θ, 13.5±0.2° 2θ, 13.9±0.2° 2θ, 14.9±0.2° , 15.7±0.2° 2θ, 17.1±0.2° 2θ, 17.9±0.2° 2θ, 18.3±0.2° 2θ, 19.8±0.2° 2θ, 20.8±0.2° , 2θ, 21.0±0.2° 2θ, 21.9±0.2° 2θ, 22.8±0.2° 2θ, 23.3±0.2° 2θ, 24.9±0.2° 2θ, 25.9±0.2° , 26.4±0.2° 2θ, 29.3±0.2° 2θ and 29.8±0.2° 2θ as shown in FIG. 3, when analyzed using CuKα X-ray radiation.

### Claim 3

A crystalline noribogaine hydrochloride solvate polymorph having an X-ray powder diffraction pattern comprising peaks at 9.7±0.2° 2θ, 10.2±0.2° 2θ, 12.0±0.2° 2θ, 13.3±0.2° 2θ, 13.7±0.2° 2θ, 16.0±0.2° 2θ, 16.3±0.2° 2θ, 17.7±0.2° 2θ, 18.0±0.2° 2θ, 19.4±0.2° 2θ, 21.4±0.2° 2θ, 22.1±0.2° 2θ, 22.8±0.2° 2θ, 24.4±0.2° 2θand 25.1±0.2° 2θ as shown in FIG. 4, when analyzed using CuKα X-ray radiation.

### Claim 4 (depends on 1)

The crystalline salt of claim 1, having an X-ray powder diffraction pattern comprising peaks at 8.5±0.2° 2θ, 11.4±0.2° 2θ, 12.0±0.2° 2θ, 13.3±0.2° 2θ, 15.4±0.2° 2θ, 16.6±0.2° 2θ, 17.2±0.2° 2θ, 18.3±0.2° 2θ, 20.6±0.2° 2θ, 21.0±0.2° 2θand 21.5±0.2° 2θ as shown in FIG. 8, when analyzed using CuKα X-ray radiation.

### Claim 5 (depends on 1)

A composition comprising the stable noribogaine ansolvate salt of claim 1.

### Claim 6 (depends on 5)

The composition of claim 5, further comprising a pharmaceutically acceptable excipient.

### Claim 7

A crystalline polymorph of a phosphate salt of noribogaine, having an X-ray powder diffraction pattern comprising peaks as shown in FIG. 5, when analyzed using CuKα X-ray radiation.