# US 8,541,601 B2 · Piperazine dithioctate and pharmaceutical composition comprising the same

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- Number: US 8,541,601 B2
- Document ID: US8541601B2
- Status: Granted
- Kind: B2
- Application number: 13/379,528
- Filed: 2010-06-18
- Published: 2012-04-26
- Granted: 2013-09-24
- Earliest claimed: 2009-06-24
- Assignees: Celltrion Chemical Research Institute; Celltrion Pharm, Inc.
- Applicants: Kyoung Soo Kim; Young Jun Park; Hyun-Nam Song; In Suk Lee; Joon Woo Kim
- Inventors: Kyoung Soo Kim; Young Jun Park; Hyun-Nam Song; In Suk Lee; Joon Woo Kim
- Web page: https://patentgrep.com/patent/US8541601B2

## CPC

- C07D 339/02: Five-membered rings
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/06: Antihyperlipidemics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- 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 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 39/06: Free radical scavengers or antioxidants
- C07D 295/027: containing only one hetero ring
- C07D 339/04: having the hetero atoms in positions 1 and 2, e.g. lipoic acid
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to piperazine dithioctate, a novel addition salt of thioctic acid with a base and a pharmaceutical composition comprising the same. The piperazine dithioctate according to the present invention has good thermal and moisture stability and high water-solubility as well as dosage increase lower than other addition salts, thereby being effectively used for preparing a pharmaceutical composition for antioxidation or for preventing or treating diabetic polyneuropathy, etc.

## Claims

### Claim 1

A crystalline piperazine dithioctate of formula (I):
which shows an X-ray powder diffraction pattern characterized by peaks having I/Io values of at least 10% (I is the intensity of each peak; Io is the intensity of the highest peak) at diffraction angles (2θ) of 13.9±0.2, 16.3±0.2, 17.1±0.2, 17.3±0.2, 18.2±0.2, 18.9±0.2, 20.5±0.2, 22.2±0.2, 22.8±0.2, 24.2±0.2, and 39.3±0.2.

### Claim 2

A crystalline piperazine dithioctate of formula (I):
wherein the thioctate is R-(+)-thioctate or S-(−)-thioctate-; and wherein the crystalline piperazine dithioctate shows an X-ray powder diffraction pattern characterized by peaks having I/Io values of at least 10% (I is the intensity of each peak; Io is the intensity of the highest peak) at diffraction angles (2θ) of 14.0±0.2, 19.1±0.2, 20.6±0.2, 22.2±0.2, and 22.7±0.2.

### Claim 3 (depends on 1)

A pharmaceutical composition comprising the piperazine dithioctate according to claim 1 together with a pharmaceutically acceptable carrier.

### Claim 4 (depends on 2)

A pharmaceutical composition comprising the piperazine dithioctate according to claim 2 together with a pharmaceutically acceptable carrier.