Claims for Patent: 7,608,280

Summary for Patent: 7,608,280

Title:	Method of producing FR901228
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.
Inventor(s):	Ueda; Satoshi (Chuo-ku, JP), Watamoto; Yoko (Chuo-ku, JP), Tsuboi; Masaru (Chuo-ku, JP), Kanda; Munekazu (Chuo-ku, JP), Higaki; Tomoji (Chuo-ku, JP), Matsuda; Mitsunori (Chuo-ku, JP)
Assignee:	Astellas Pharma Inc. (Tokyo, JP)
Application Number:	12/049,746
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,608,280
Patent Claims:	1. A type B crystalline form of compound FR901228: ##STR00002## 2. The type B crystalline form of claim 1 obtained from hexanes. 3. A type B crystalline form of compound FR901228: ##STR00003## which crystalline form is characterized by a powder X-ray diffraction pattern substantially similar to FIG. 5. 4. A composition comprising a type B crystalline form of compound FR901228: ##STR00004## 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. 5. 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. 6. 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. 7. 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.