Eisai R&d Management Co., Ltd.

Mercian Corporation

Hiroshi Ishihara

Kenji Hyodo

Hiroshi Kikuchi

Yoshiaki Sato

Hitoshi Harada

Hiroyuki Chiba

Koichi Ito

Masato Ueda

Tetsuya Kawahara

Nobuhisa Watanabe

Satoshi Nagato

Kohshi Ueno

Atsushi Kamada

Katsura Hata

Manabu Sasho

Masashi Yoshida

Yuki Komatsu

Susumu Takeda

Naoki Ozeki

Yukiko Sugaya

Susumu Inoue

Tomonari Yamada

Teiji Takigawa

Keizo Sato

Hiroki Terauchi

Hiroki Muto

Takashi Kamahara

Geoff Hird

Yoshiaki Asahi

Koichiro Koyama

Sachiko Kikuchi

The present invention provides a novel liposome composition containing eribulin or its pharmacologically permissible salt, and its method of manufacture.

Liposome composition

A formulation comprising liposomes, wherein the liposomes comprise, based on the liposome, 0.7 to 3.0 mol % of eritoran or a pharmaceutically acceptable salt thereof and 0.5 to 3.0 mol % of a PEGylated phospholipid.

Formulation comprising liposomes

The present invention provides a method of manufacture of a liposome composition including a step in which: a liposome dispersion liquid containing a liposome, and further containing cyclodextrin in the liposome internal phase is provided and a step in which an active compound is introduced into said liposome internal phase, and the liposome composition.

Method of manufacture of liposome composition

The present invention provides the compound of formula (I) in a solid form which, as a bulk medicament for pharmaceutical manufacture, is uniform, has a high purity, and is easy to work with. The invention further provides a process for preparing this compound, and pharmaceutical compositions containing the same. A solid form of (8E,12E,14E)-7-{(4-cycloheptylpiperazin-1-yl)carbonyl}oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide which has uniform specifications and is easy to work with was developed.

Macrolide compound in solid form, process for preparation thereof, and pharmaceutical composition containing the same

Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one having a diffraction peak at a diffraction angle (2&#x3b8;&#xb1;0.2&#xb0;) of 9.7&#xb0; and/or 21.9&#xb0; in a powder X-ray diffraction are suitable for an active ingredient of a preventing and therapeutic agent for diseases such as constipation. Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one hydrate and amorphous 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one hydrate are also suitable for an active ingredient of a preventing and therapeutic agent for diseases such as constipation.

Crystals of pyrimidine compound and process for producing the same

An acid addition salt of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one or a hydrate thereof, wherein the acid is selected from the group consisting of benzenesulfonic acid, p-toluenesulfonic acid, hydrochloric acid, hydrobromic acid, sulfuric acid, methanesulfonic acid, fumaric acid, tartaric acid, succinic acid and benzoic acid. 

Salt of 1,2-dihydropyridine compound

The present invention provides a method for stabilizing a macrolide compound, and an efficient method for producing the compound. Specifically, it provides a method for stabilizing a macrolide compound, in which a 12-membered ring macrolide compound, such as a compound expressed by the formula (1) and a cyclodextrin are both present, and a method for producing a macrolide compound, in which a cyclodextrin is made to be present in a culture broth of actinomycetes having an ability of producing the macrolide compound.

Method for stabilizing macrolide compounds

Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one having a diffraction peak at a diffraction angle (2&#x3b8;&#xb1;0.2&#xb0;) of 12.8&#xb0;, 18.1&#xb0; and/or 23.5&#xb0; in a powder X-ray diffraction are excellent in stability against light, therefore are suitable for an active ingredient of a preventing and therapeutic agent for diseases such as constipation.

Crystals of 5-[2-amino-4-(2-furyl) pyrimidin-5-yl]-1-methylpyridin-2(1H)-one and processes for preparing the same

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Tsukuba, Japan

Hiroshi Ishihara