# US 2010/0168201 A1 · Polymorphs of [R-(R*, R*) ]-2-(4-Fluorophenyl)-Beta, Delta-Dihydroxy-5-(1-Methylethyl)-3-Phenyl-4-[(Phenylamino)Carbonyl]-1H-Pyrrole-1-Heptanoic Acid Magnesium Salt (2:1)

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- Number: US 2010/0168201 A1
- Document ID: US20100168201A1
- Status: Published application
- Kind: A1
- Application number: 12/085,255
- Filed: 2005-11-29
- Published: 2010-07-01
- Earliest claimed: 2005-11-29
- Assignees: Biocan Limited
- Inventors: Joy Mathew; Chandrashekar Aswathanarayanappa; Tom Thomas Puthiaparampil
- Web page: https://patentgrep.com/patent/US20100168201A1

## CPC

- C07D 207/327: Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- A61P 3/06: Antihyperlipidemics
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Crystalline and amorphous polymorphic forms of Atorvastatin magnesium and processes for their preparation are claimed.

## Claims

### Claim at position 1

1-18. (canceled)

### Claim 19

Crystalline form of Atorvastatin magnesium.

### Claim 20

Amorphous form of Atorvastatin magnesium.

### Claim 21

Crystalline form B1 of Atorvastatin magnesium.

### Claim 22

Crystalline form B2 of Atorvastatin magnesium.

### Claim 23

Amorphous form B3 of Atorvastatin magnesium.

### Claim 24 (depends on 19)

The crystalline form of Atorvastatin magnesium of claim 19 having XRD pattern as shown in FIG. 1.

### Claim 25 (depends on 19)

The crystalline form of Atorvastatin magnesium of claim 19 having XRD pattern as shown in FIG. 2.

### Claim 26 (depends on 20)

The amorphous form of Atorvastatin magnesium of claim 20 having XRD pattern as shown in FIG. 3.

### Claim 27

A process for preparation of crystalline form of Atorvastatin magnesium comprising:
a. treating Atorvastatin magnesium with one or more solvents or solvent mixtures,
b. optionally subjecting the mixture to a suitable temperature range, stirring, filtering the mixture, and
c. isolating the crystalline form of Atorvastatin magnesium.

### Claim 28

A process for the preparation of amorphous form of Atorvastatin magnesium comprising:
a. treating Atorvastatin magnesium with one or more solvents or solvent mixtures, and
b. isolating the amorphous form of Atorvastatin magnesium.

### Claim 29 (depends on 27)

The process of claim 27, wherein the solvent is selected from protic, aprotic, water miscible, water immiscible, polar or non-polar solvent.

### Claim 30 (depends on 28)

The process of claim 28, wherein the solvent is selected from protic, aprotic, water miscible, water immiscible, polar or non-polar solvent.

### Claim 31 (depends on 29)

The process of claim 29, wherein one or more solvent is selected from water, acetonitrile, methanol, ethanol, acetone, ethyl acetate, chloroform, isopropyl alcohol, THF, dichloromethane, t-butanol, iso-butanol, carbon tetrachloride, 1,4-dioxan, n-butanol, di-isopropyl ether or di-ethyl ether.

### Claim 32 (depends on 30)

The process of claim 30, wherein one or more solvent is selected from water, acetonitrile, methanol, ethanol, acetone, ethyl acetate, chloroform, isopropyl alcohol, THF, dichloromethane, t-butanol, iso-butanol, carbon tetrachloride, 1,4-dioxan, n-butanol, di-isopropyl ether or di-ethyl ether.

### Claim 33 (depends on 27)

The process of claim 27 to afford crystalline form B1 of Atorvastatin magnesium.

### Claim 34 (depends on 28)

The process claim 28 to afford crystalline form B1 of Atorvastatin magnesium.

### Claim 35 (depends on 27)

The process of claim 27 to afford crystalline form B2 of Atorvastatin magnesium.

### Claim 36 (depends on 28)

The process of claim 28 to afford crystalline form B2 of Atorvastatin magnesium.

### Claim 37 (depends on 27)

The process of claim 27 to afford amorphous form B3 of Atorvastatin magnesium.

### Claim 38 (depends on 28)

The process of claim 28 to afford amorphous form B3 of Atorvastatin magnesium.

### Claim 39 (depends on 27)

The process of claim claim 27 wherein the temperature is raised or lowered to afford the crystalline or amorphous form of atorvastatin magnesium.

### Claim 40

A pharmaceutical composition comprising atorvastatin magnesium form B1, B2 or B3.

### Claim 41

A method of treatment or prevention of cholesterolemia in a subject comprising administering to the subject atorvastatin magnesium form B1, B2 or B3.