Fujisawa Pharmaceutical Company, Ltd.

Astellas Pharma Gmbh

Masaru Tsuboi

Satoshi Ueda

Seiji Hashimoto

Michio Yamashita

Masami Ezaki

Kazutoshi Sakamoto

Tomoji Higaki

Miho Tanaka

Nobutaka Oohata

Munekazu Kanda

Mitsunori Matsuda

Yoko Watamoto

Yasuhisa Tsurumi

Shiho Shimizu

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.

Method of producing FR901228

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.

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

Cyclic lipopeptide acylase

Process for the deacylation of cyclic lipopeptides

Process for preparing FR900482 and compounds analogous thereto

There is provided a cyclic lipopeptide acylase which is capable of deacylating the acyl side chain of a cyclic lipopeptide compound, e.g. Substance FR901379 or its analog, of the general formula &lsqb;I&rsqb; with effectiveness as well a method of producing a cyclic peptide compound which comprises using the acylase.

A process for producing a compound of the general formula (I):

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Chuo-ku, Japan

Masaru Tsuboi