# US 8,772,488 B2 · Crystals of prasugrel hydrobromate

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- Number: US 8,772,488 B2
- Document ID: US8772488B2
- Status: Granted
- Kind: B2
- Application number: 13/262,093
- Filed: 2010-03-31
- Published: 2012-04-19
- Granted: 2014-07-08
- Earliest claimed: 2009-03-31
- Assignees: Shanghai Institute of Pharmaceutical Industry; Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
- Applicants: Zhedong Yuan; Xingdong Cheng; Yulei Yang; Ling Tong; Xiong Yu; Laifang Zhang; Wenliang Zhou
- Inventors: Zhedong Yuan; Xingdong Cheng; Yulei Yang; Ling Tong; Xiong Yu; Laifang Zhang; Wenliang Zhou
- Web page: https://patentgrep.com/patent/US8772488B2

## CPC

- A61K 31/4365: the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 495/04: Ortho-condensed systems
- 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
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present application discloses crystals of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine hydrobromate, crystal compositions and pharmaceutical compositions comprising them and their use. The crystals of prasugrel hydrobromate of the present application possess excellent stability and solubility.

## Claims

### Claim 1

A crystal of a compound having formula II:
wherein:
Sol is acetic acid; and
m is 1.

### Claim 2 (depends on 1)

The crystal of claim 1, wherein in an X-ray powder diffraction pattern of the crystal measured with Cu-Kα radiation, diffraction peaks expressed as interplanar spacing d are found at about 10.43 Å, 8.63 Å, 7.20 Å, 6.33 Å, 5.15 Å, and 3.47 Å.

### Claim 3 (depends on 2)

The crystal of claim 2, wherein in the X-ray powder diffraction pattern of the crystal measured with Cu-Kα radiation, diffraction peaks expressed as interplanar spacing d are found at about 10.43 Å, 8.63 Å, 7.20 Å, 6.33 Å, 5.15 Å, 4.80 Å, 4.73 Å, 3.77 Å, 3.68 Å, and 3.47 Å.

### Claim 4 (depends on 3)

The crystal of claim 3, wherein in the X-ray powder diffraction pattern of the crystal measured with Cu-Kα radiation, diffraction peaks expressed as interplanar spacing d are found at about 12.38 Å, 10.43 Å, 8.63 Å, 7.20 Å, 6.33 Å, 5.15 Å, 4.96 Å, 4.80 Å, 4.73 Å, 4.02 Å, 3.77 Å, 3.68 Å, 3.47 Å, 3.36 Å, 2.99 Å, and 2.95 Å.

### Claim 5 (depends on 1)

The crystal of claim 1, wherein the crystal is of orthorhombic structure, and the space group thereof is Pnma; the lattice parameters thereof approximately are: a=15.33 Å; b=7.39 Å; c=20.82 Å; α=β=γ=90′; and the lattice volume thereof is 2356.89 Å3.

### Claim 6

A pharmaceutical composition comprising a therapeutically effect amount of a crystal of a compound having formula II:
wherein:
Sol is acetic acid; and
m is 1.

### Claim 7

A method for preventing diseases associated with thrombus in an animal, comprising administering to the animal in need thereof a therapeutically effective amount of a crystal of a compound having formula II:
wherein:
Sol is acetic acid, and
m is 1.

### Claim 8 (depends on 1)

A crystal composition comprising the crystal of claim 1 in an amount of 60% or more by weight.

### Claim 9 (depends on 1, 8)

The crystal composition of claim 8, comprising the crystal of claim 1 in an amount of 90% or more by weight.

### Claim 10 (depends on 1, 8)

The crystal composition of claim 8, comprising the crystal of claim 1 in an amount of 95% or more by weight.

### Claim 11 (depends on 1, 8)

The crystal composition of claim 8, comprising the crystal of claim 1 in an amount of 99% or more by weight.