# US 8,569,371 B2 · Crystal forms of O-desmethylvenlafaxine fumarate

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- Number: US 8,569,371 B2
- Document ID: US8569371B2
- Status: Granted
- Kind: B2
- Application number: 13/074,364
- Filed: 2011-03-29
- Published: 2011-09-29
- Granted: 2013-10-29
- Earliest claimed: 2010-03-29
- Assignees: Pliva Hrvatska D.O.O.
- Applicants: Marina Ratkaj; Gustavo Frenkel
- Inventors: Marina Ratkaj; Gustavo Frenkel
- Web page: https://patentgrep.com/patent/US8569371B2

## CPC

- C07C 217/74: with rings other than six-membered aromatic rings being part of the carbon skeleton
- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61P 25/24: Antidepressants
- C07C 57/15: Fumaric acid
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- C07C 2601/14: The ring being saturated
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- 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

Provided are crystalline forms of O-desmethylvenlafaxine fumarate, methods for their preparation, and pharmaceutical composition thereof.

## Claims

### Claim 1

The crystalline Form N of O-desmethylvenlafaxine fumarate, characterized by data selected from: a powder XRD pattern with peaks at about 9.5, 13.2, 14.6, 21.8 and 24.8° 2θ±0.2° 2θ; a powder XRD pattern as depicted in FIG. 1, a 13C NMR spectrum having signals at about 167.87, 131.33 and 114.43±0.2 ppm; a solid state 13C NMR spectrum as depicted in FIG. 4, or combinations thereof.

### Claim 2 (depends on 1)

The crystalline Form N of O-desmethylvenlafaxine fumarate according to claim 1, characterized by a powder XRD pattern with peaks at about 9.5, 13.2, 14.6, 21.8 and 24.8° 2θ±0.2° 2θ.

### Claim 3 (depends on 2)

The crystalline form N of claim 2, further characterized by additional X-ray powder diffraction peaks at 5.2, 10.4, 16.7 and 26.1° 2θ±0.2° 2θ.

### Claim 4 (depends on 1)

The crystalline Form N of O-desmethylvenlafaxine fumarate according to claim 1, characterized by a powder XRD pattern as depicted in FIG. 1.

### Claim 5 (depends on 1)

The crystalline Form N of O-desmethylvenlafaxine fumarate according to claim 1, characterized by a 13C NMR spectrum having signals at about 167.87, 131.33 and 114.43±0.2 ppm.

### Claim 6 (depends on 1)

The crystalline Form N of O-desmethylvenlafaxine fumarate according to claim 1, characterized by a solid state 13C NMR spectrum as depicted in FIG. 4.

### Claim 7 (depends on 1)

The crystalline Form N of O-desmethylvenlafaxine fumarate according to claim 1, wherein the crystalline form is a monohydrate.

### Claim 8 (depends on 1)

A composition containing the crystalline form of O-desmethylvenlafaxine fumarate of claim 1 and not more than about 10% by weight of a crystalline form of O-desmethylvenlafaxine fumarate characterized by a PXRD pattern having peaks at about 10.6, 13.5, 14.8, 24.5 and 26.7° 2θ±0.2° 2θ.

### Claim 9 (depends on 2)

A pharmaceutical composition comprising the crystalline Form N of O-desmethylvenlafaxine fumarate according to claim 2, and at least on pharmaceutically acceptable excipient.

### Claim 10 (depends on 2)

A method for treating depression, comprising administering a pharmaceutically effective amount of the crystalline Form N of O-desmethylvenlafaxine fumarate according to claim 2, to a subject in need of such treatment.