# US 2014/0194453 A1 · Multicomponent crystalline system of rosuvastatin calcium salt and vanillin

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- Number: US 2014/0194453 A1
- Document ID: US20140194453A1
- Status: Published application
- Kind: A1
- Application number: 14/169,844
- Filed: 2014-01-31
- Published: 2014-07-10
- Earliest claimed: 2011-04-18
- Assignees: BASF SE
- Applicants: BASF SE
- Inventors: Andreas HAFNER; Fritz BLATTER; Martin SZELAGIEWICZ; Bernd SIEBENHAAR
- Web page: https://patentgrep.com/patent/US20140194453A1

## CPC

- A61K 31/505: Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K 31/11: Aldehydes
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61P 9/00: Drugs for disorders of the cardiovascular system
- C07D 239/42: One nitrogen atom (nitro radicals C07D239/30)
- 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

A novel solid form of Rosuvastatin comprises as the active ingredient a salt of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)-amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] and vanillin or vanillin derivatives. The crystal comprising the two components, and minor amounts of water, shows improved properties such as crystallization behavior stability and decreased hydroscopic behavior.

## Claims

### Claim 1

A single phase solid form of a bis[(E)-7[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)-amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxylhept-6-enoic acid] salt comprising vanillin or vanillic acid or isovanillin or ortho-vanillin or ethylvanillin or acetovanillon.

### Claim at position 2

2-15. (canceled)