Hoffmann-la Roche Inc.

Basilea Pharmaceutica Ag

Ebara Corporation

Absize, Inc.

Osaka University

Chugai Seiyaku Kabushiki Kaisha

Basilea Pharmaceutica Ag, a Swiss Company

Isao Umeda

Nobuo Shimma

Jun Ohwada

Tadakatsu Hayase

Masao Tsukazaki

Hiroshi Fukuda

Nobuhiro Oikawa

Masahiro Sakaitani

Eisaku Mizuguchi

Hideo Ishitsuka

Chikako Murasaki

Shigeyasu Ichihara

Kazuya Hirata

Hiroyuki Kato

Takuo Tsukuda

Hiroshi Masuhara

Yasuji Suhara

Toru Okuda

Masanori Miwa

Tsuyoshi Asahi

Kazunao Masubuchi

Teruki Sugiyama

Isamu Oh

Sen-ichi Ryo

Yuhko Aoki

Hiromichi Kotaki

Michio Shirai

Daisuke Sawada

Noriko Ohga

Kazuo Watanabe

Motohiko Nohmi

Yoshiaki Isshiki

Sawako Ozawa

Kazuteru Yokose

Toshikazu Yamazaki

Morio Fujiu

Haruyoshi Shirai

Isami Kuruma

Motohiro Arasaki

Nobuo Shinma

Akio Ishiguro

Toshiya Sakai

Tetsu Go

Pingli Liu

Jun Chugai Seiyaku Kabushiki Kaisha Ohwada

Sawako Chugai Seiyaku Kabushiki Kaisha Ozawa

A method of producing water-insoluble anti-cancer drug in the form of particulates, the method including preparing a water-insoluble anti-cancer drug having at least one multiple bond in the structure, and irradiating said water-insoluble anti-cancer drug with a laser beam having a wavelength of a low absorption portion in the vicinity of the foot of an absorption curve on the long wavelength side within the absorption band until said water-insoluble anti-cancer drug is formed into particulates having an average particle diameter of 50 to 200 nm.

Water-insoluble medicine

An objective of the present invention is to provide water-soluble prodrugs that can be administered parenterally, and which show excellent water solubility and small interspecies or individual differences and are rapidly converted to the active form by chemical conversion. This invention provides water-soluble prodrugs represented by formula (1), or pharmaceutically acceptable salts, or hydrates or solvates thereof, (wherein,

Water-soluble prodrugs

An apparatus for forming ultrafine particles, including: a light source generating a laser beam to be irradiated at an organic substance; at least one microflow channel capable of passing therethrough a suspension containing the organic substance; and a flow device for allowing the suspension containing the organic substance to continuously or intermittently pass through the microflow channel, the organic substance present in the microflow channel being irradiated with the laser beam at least once within a predetermined period, thereby forming ultrafine particles of the organic substance.

Apparatus for forming ultrafine particles

A method of producing a medicinal nanoparticle suspension is provided, wherein a medicinal ingredient added in a suspending solution is ground to form nanoparticles of the medicinal ingredient by irradiating the suspending solution with a laser. The process is implemented after adding a poorly water-soluble or water-insoluble medicinal ingredient of a drug in a poor solvent to form the suspending solution.

Method of producing medicinal nanoparticle suspension

N-substituted carbamoyloxyalkyl-azolium derivatives which have antifungal activity and are useful for the treatment of fungal diseases.

N-substituted carbamoyloxyalkyl-azolium derivatives

N-substituted carbamoyloxyalkyl-azolium derivatives Which have antifungal activity and are useful for the treatment of fungal diseases.

N-phenyl substituted carbamoyloxyalkyl-azolium derivatives

Intermediates for N-substituted carbamoyloxyalkyl-azolium derivatives

Azoles for treatment of fungal infections

N-Benzylazolium derivatives of the general formula (I), ##STR1## wherein Q is the remainder of an azole compound of the formula II ##STR2## possessing antifungal activity; Z is nitrogen or methine;

N-benzylazolium derivatives

Compounds of the formula ##STR1## which have antifungal activity.

Cyclohexane derivatives

The invention relates to N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives which are useful as an agent for treating tumors, pharmaceutical compositions including the same, a method of treating tumors and a method of preparing N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine derivatives for treating tumors. Compounds of formula (I), ##STR1## wherein R.sup.1 is a saturated or unsaturated, straight or branched hydrocarbon radical wherein the number of carbon atoms in the longest straight chain of this hydrocarbon radical ranges from three to seven, or is a radical of the formula --(CH.sub.2)n--.sup.Y wherein Y is a cyclohexyl radical, a C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical and wherein when Y is a cyclohexyl radical n is an integer from 0 to 4, and when Y is C.sub.1 -C.sub.4 alkoxy radical or a phenyl radical n is an integer from 2 to 4, and R.sup.2 is a hydrogen atom or a radical easily hydrolyzable under physiological conditions, or a hydrate or solvate thereof. Compounds of formula (I) are useful in the treatment of tumors.

N.sup.4 -(substituted-oxycarbonyl)-5'-deoxy-5-fluorocytidine compounds,

The novel 5'-deoxy-5-fluorocytidine derivatives of formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are hydrogen or an easily hydrolyzable radical under physiological conditions, with the proviso that, at least one or R.sup.1, R.sup.2 and R.sup.3 is an easily hydrolyzable radical under physiological conditions, as well as hydrates of solvates of these compounds have antitumor properties. They can be prepared from compounds of formula I, wherein R.sup.1 is hydrogen or an amino-protecting radical and R.sup.2 and R.sup.3 are hydrogen or a hydroxy-protecting radical or taken together are a cyclic hydroxy-protecting radical.

Fluorocytidine derivatives

Growing community of inventors

Yokohama, Japan

Isao Umeda