Fujisawa Pharmaceutical Company, Ltd.

Matsushita Electric Industrial Co., Ltd.

Astellas Pharma Gmbh

Tsubakimoto Chain Company

Matsushita Electronics Corporation

Satoshi Ueda

Masaru Tsuboi

Fumio Shimojo

Rinta Ibuki

Michio Yamashita

Seiji Hashimoto

Masami Ezaki

Kazutoshi Sakamoto

Tomoji Higaki

Miho Tanaka

Nobutaka Oohata

Mitsunori Matsuda

Takeo Hirose

Yoko Watamoto

Munekazu Kanda

Tetsuya Ueda

Kousaku Yano

Yukihiro Nomura

Eiji Hashimoto

Noboru Nomura

Tatsuo Sugiyama

Masayuki Endo

Takashi Saitoh

Shigeki Tamura

Toshio Ideno

Kazunari Yamashita

Takehisa Hata

Sumihisa Kimura

Masayuki Yamanaka

Toshihiko Toyoda

Takashi Uehara

Hiroshi Yuasa

Norio Ohnishi

Kiyoshi Fukuyama

Akifumi Katayama

Erika Yoshida

Keijirou Mori

Shunji Sakura

Kenshi Suzuki

Tomoyasu Murakami

Tomoyuki Saji

Yuka Terai

Akira Kagayama

Yoshio Ueda

Atsuhiro Yamano

Saburo Murata

Yuji Tokunaga

Tomoo Suko

Masahiro Sudare

Katsuhiko Suwa

Naoto Shibata

Yoshifumi Takeuchi

Yasuyuki Suyama

Hisami Yamaguchi

Kohei Nakanishi

Masateru Kodani

Shuichi Mayumi

Kazuhiko Kishimoto

Shiroh Inoue

Kousaka Yano

Kazusa Mori

Satoshi Umehara, Deceased

Yoshiyuki Nishimura

Masami Tsuji

Takeo Chayamachi 525 Hirose

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

A sustained-release formulation is provided comprising a solid dispersion composition comprising a tricyclic compound or a pharmaceutically acceptable salt thereof in a mixture comprising a water-soluble polymer and a water-insoluble polymer, and an excipient.

Sustained-release formulation

The invention relates to an engagement chain type driving device including a pair of driving sprockets, which rotate positively and reversely in opposite directions about a pair of rotating shafts, a pair of engagement chains, which engage with each other by the pair of driving sprockets so to be integrated together, and a driving source, which drives the pair of driving sprockets, wherein the engagement chain includes inner tooth plates and outer tooth plates, which each include buckling limiting flat surfaces, the inner tooth plates and outer tooth plates being brought opposite to each other and into contact with each other when the engagement chains are integrated by the pair of driving sprockets, such that the flat surfaces hold the chain engagement position.

Engagement chain type driving device

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

Sustained release formulation containing tacrolimus or its hydrate is provided. The time (T63.2%) required for 63.2% of the maximum amount of tacrolimus or its hydrate to be dissolved is 0.7 to 15 hours. The time is measured in accordance to the Japanes Pharmacopocia, the 13-th edition, Dissolution Test, No. 2 (Puddles method, 50 rpm) using an aqueous 0.005% hydroxypropyl cellulose solution. This aqueous test solution is adjusted to pH 4.5, accordingly. The formulation further comprises a solid base which is a water-soluble or water-insoluble polymer. The formulation is in the form of a powder, fine powder, granule, tablet or capsule. The formulation is administered to a patient once a day for preventing organ or tissue rejection by transplantation or autoimmune disease. In addition, a solid dispersion composition is provided. The solid dispersion comprises tacrolimus or its hydrate in a mixture containing water-soluble or water-insoluble polymer and an excipient.

Sustained release formulation containing tacrolimus

Cyclic lipopeptide acylase

To provide a pharmaceutical composition comprising a macrolide compound, such as tricyclic compound (I) or its pharmaceutically acceptable salt, a dissolution/absorption promoter, a pharmaceutical base, and optionally a compatibilizing agent and/or a thickener. It is satisfactory in stability and absorption kinetics and/or a low irritation potential.

Medicinal compositions

Sustained release formulation containing tacrolimus or its hydrate is provided. The time (T63.2%) required for 63.2% of the maximum amount of tacrolimus or its hydrate to be dissolved is 0.7 to 15 hours. The time is measured in accordance to the Japanese Pharmacopoeia, the 13-th edition, Dissolution Test, No. 2 (Puddle method, 50 rpm) using an aqueous 0.005% hydroxypropyl cellulose solution. This aqueous test solution is adjusted to pH 4.5, accordingly. The formulation further comprise a solid base which is a water-soluble polymer and/or wax. The formulation is in the form of a powder, fine powder, granule, tablet or capsule. Furthermore, the formulation is administered to a patient once a day for preventing organ or tissue rejection by transplantation or autoimmune diseases.

Sustained release formulations containing tacrolimus

Process for the deacylation of cyclic lipopeptides

Growing community of inventors

Kawanishi, Japan

Satoshi Ueda