# US 8,772,245 B2 · Crystalline form of cyclosporine A, methods of preparation, and methods for use thereof

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- Number: US 8,772,245 B2
- Document ID: US8772245B2
- Status: Granted
- Kind: B2
- Application number: 13/480,710
- Filed: 2012-05-25
- Published: 2013-01-24
- Granted: 2014-07-08
- Earliest claimed: 2011-05-27
- Assignees: Allergan, Inc.
- Applicants: Anuradha V. Gore; Kiomars Karami; Ke Wu; Richard S. Graham; Scott W. Smith
- Inventors: Anuradha V. Gore; Kiomars Karami; Ke Wu; Richard S. Graham; Scott W. Smith
- Web page: https://patentgrep.com/patent/US8772245B2

## CPC

- C07K 7/645: {Cyclosporins; Related peptides}
- A61K 38/13: Cyclosporins
- A61P 27/02: Ophthalmic agents
- A61P 27/04: Artificial tears; Irrigation solutions
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- C07K 1/306: {by crystallization}
- A61K 9/48: Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)}
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- 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
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

The present invention relates generally to crystalline forms of cyclosporine A and particularly to a newly identified form of cyclosporine A. The invention further relates to methods for its preparation and to methods for treating certain ocular disorders.

## Claims

### Claim 1

Cyclosporine A having the structure
in crystalline form 2.

### Claim 2

A crystalline form of cyclosporine A having an X-ray powder diffraction pattern with major peaks at (2θ): 7.5, 8.8, 10.2, 11.3, 12.7, 13.8, 14.5, 15.6 and 17.5.

### Claim 3

A crystalline form of cyclosporine A having the X-ray diffraction pattern as shown in FIG. 2.

### Claim 4 (depends on 1)

The crystalline form of claim 1 free of other crystalline forms.

### Claim 5

A crystalline form as set forth by the formula
wherein X is 0-3.

### Claim 6 (depends on 5)

The crystalline form of claim 5, wherein X is 2.