Eisai R&d Management Co., Ltd.

Eisai Company, Limited

Yuki Komatsu

Hiroyuki Chiba

Yongbo Hu

Kohshi Ueno

Huiming Zhang

Bryan Matthew Lewis

Susumu Inoue

Makoto Komatsu

Yoshimasa Machida

Norio Minami

Naoyuki Shimomura

Noritaka Kitazawa

Akiharu Kajiwara

Yoshiharu Yamanishi

Satoshi Nagato

Hitoshi Harada

Kozo Akasaka

Toshikazu Shimizu

Masahiro Yonaga

Masataka Ueno

Kunizo Higurashi

Naoki Ozeki

Atsushi Nagaoka

Yoshiaki Sato

Hiroshi Ishihara

Mamoru Miyazawa

Kimihiro Matsuo

Manabu Shasho

In general, the present invention features improved methods useful for the synthesis of analogs of halichondrin B, such as eribulin and pharmaceutically acceptable salts thereof (e.g., eribulin mesylate).

Methods useful in the synthesis of halichondrin B analogs

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

Crystalline and amorphous pyrimidine compounds and processes for preparing pyrimidine compounds

Process for production of indole derivatives and intermediates therefor

A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof:

Biphenyl derivatives

A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.

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Ibaraki, Japan

Yuki Komatsu