# US 7,612,072 B2 · Amorphous form of a phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor

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- Number: US 7,612,072 B2
- Document ID: US7612072B2
- Status: Granted
- Kind: B2
- Application number: 11/660,722
- Filed: 2005-09-09
- Published: 2007-12-06
- Granted: 2009-11-03
- Earliest claimed: 2004-09-15
- Assignees: Merck & Co., Inc.
- Inventors: Russell R. Ferlita; Robert M. Wenslow
- Web page: https://patentgrep.com/patent/US7612072B2

## CPC

- C07D 487/04: Ortho-condensed systems
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 7/12: Antidiuretics, e.g. drugs for diabetes insipidus (ADH A61P5/10)
- A61P 9/12: Antihypertensives
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to a novel amorphous form of the dihydrogenphosphate salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-α]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine of structural formula I as well as a process for its preparation, pharmaceutical compositions containing this novel form, and methods of use of the novel form and pharmaceutical compositions for the treatment of diabetes, obesity, and high blood pressure.

## Claims

### Claim 1

An amorphous form of the dihydrogenphosphate salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-α]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine of structural formula I:
characterized by the X-ray powder diffraction pattern of FIG.1.

### Claim 2 (depends on 1)

The amorphous form of claim 1 characterized by a solid-state fluorine-19 magic-angle spinning (MAS) nuclear magnetic resonance spectrum showing signals at −63.7, −118.5, −136.6, and −143.3 p.p.m.

### Claim 3 (depends on 1)

The amorphous form of claim 1 further characterized by the solid-state fluorine-19 magic-angle spinning (MAS) nuclear magnetic resonance spectrum of FIG. 3.

### Claim 4 (depends on 1)

The amorphous form of claim 1 characterized by a solid-state carbon-13 cross-polarization magic-angle spinning (CPMAS) nuclear magnetic resonance spectrum showing signals at 169.6, 150.6, 120.1, and 41.9 p.p.m.

### Claim 5 (depends on 4)

The amorphous form of claim 4 further characterized by the solid-state carbon-13 cross-polarization magic-angle spinning (CPMAS) nuclear magnetic resonance spectrum of FIG. 2.

### Claim 6 (depends on 1)

The amorphous form of claim 1 characterized by the thermogravimetric analysis curve of FIG. 5.

### Claim 7 (depends on 1)

The amorphous form of claim 1 characterized by the differential scanning calorimetric (DSC) curve of FIG. 4.

### Claim 8 (depends on 1)

A pharmaceutical composition in solid form comprising a therapeutically effective amount of the amorphous form of claim 1 in association with one or more pharmaceutically acceptable carriers or excipients.