# US 7,608,280 B2 · Method of producing FR901228

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- Number: US 7,608,280 B2
- Document ID: US7608280B2
- Status: Granted
- Kind: B2
- Application number: 12/049,746
- Filed: 2008-03-17
- Published: 2008-09-18
- Granted: 2009-10-27
- Earliest claimed: 2000-09-01
- Assignees: Astellas Pharma Inc.
- Inventors: Satoshi Ueda; Yoko Watamoto; Masaru Tsuboi; Munekazu Kanda; Tomoji Higaki; Mitsunori Matsuda
- Web page: https://patentgrep.com/patent/US7608280B2

## CPC

- C12P 21/02: having a known sequence of two or more amino acids, e.g. glutathione
- A61P 31/04: Antibacterial agents
- A61P 35/00: Antineoplastic agents
- C07K 5/101: {the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu}
- C12P: FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE {(brewing of beer C12C; producing vinegar C12J; producing specific peptides or proteins C07K; producing enzymes C12N9/00; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; measuring or testing processes involving enzymes or microorganisms C12Q; measuring or testing processes involving nucleic acid amplification reactions C12Q1/6844; fermentation processes to form a food composition, A21 or A23; compounds in general, see the relevant compound class, e.g. C01, C07)}
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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)

## Abstract

Depsipeptides and congeners thereof are disclosed having structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion. Also provided are crystalline forms of FR901228, e.g., type A and type B crystalline forms of FR901228.

## Claims

### Claim 1

A type B crystalline form of compound FR901228:

### Claim 2 (depends on 1)

The type B crystalline form of claim 1 obtained from hexanes.

### Claim 3

A type B crystalline form of compound FR901228:
which crystalline form is characterized by a powder X-ray diffraction pattern substantially similar to FIG. 5.

### Claim 4

A composition comprising a type B crystalline form of compound FR901228:
wherein the composition is characterized by having one or more peaks in its X-ray diffraction pattern selected from those at about 7.1, about 11.7, about 11.9, and about 15.1 degrees 2-theta.

### Claim 5 (depends on 4)

The composition of claim 4, wherein the composition is characterized by having two or more peaks in its powder X-ray diffraction pattern selected from those at about 7.1, about 11.7, about 11.9, and about 15.1 degrees 2-theta.

### Claim 6 (depends on 4)

The composition of claim 4, wherein the composition is characterized by having three or more peaks in its powder X-ray diffraction pattern selected from those at about 7.1, about 11.7, about 11.9, and about 15.1 degrees 2-theta.

### Claim 7 (depends on 4)

The composition of claim 4, wherein the composition is characterized by having four peaks in its powder X-ray diffraction pattern at about 7.1, about 11.7, about 11.9, and about 15.1 degrees 2-theta.