Taiho Pharmaceutical Company Limited

Taisho Pharmaceutical Co., Ltd.

Kuraray Co., Ltd.

Synphar Laboratories, Inc.

Taiho Pharmaceutical

Norio Unemi

Setsuro Fujii

Setsuo Takeda

Mitsugi Yasumoto

Kenji Kitazato

Hiroshi Matsumoto

Sadao Hashimoto

Tadafumi Terada

Hitoshi Saito

Jun-ichi Yamashita

Mitugi Yasumoto

Junichi Yamashita

Ichiro Yamawaki

Fumio Mori

Tetsuji Asao

Kazuo Ogawa

Yuji Yamada

Dai Q Nguyen

Jehangir Khan

Yukio Tada

Mohsen Daneshtalab

Ronald J Micetich

Chan M Ha

Inderjit Sidhu

Tsutomu Kawai

Yoshikazu Sugimoto

Toshiyuki Toko

Atsuhiko Uemura

Yadagiri Bathini

Mark Abel

Tetsuo Furukawa

Sameeh Salama

A compound of formula I, or an optical isomer or pharmaceutically acceptable salt thereof, ##STR1## is disclosed as well as a pharmaceutical composition and a method of treating or preventing a fungal infection using the compound.

Triazoles as therapeutic agents for fungal infections

Novel 2'-deoxy-5-substituted uridine derivative represented by the general formula, ##STR1## wherein R.sub.1 is a hydrogen atom, a benzoyl group or a tetrahydrofuranyl group; R.sub.2 is a fluorine atom or a trifluoromethyl group; and any one of R.sub.3 and R.sub.4 is a hydrogen atom and the other one is an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, a benzyl group having as the substituents selected from the group consisting of a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms and a nitro group, or an alkyl group having 1 to 3 carbon atoms having one or two phenyl groups as the substituents. The novel 2'-deoxy-5-substituteduridine derivative possesses excellent antitumor activity with less toxicity, thus it is useful as antitumor agent.

2'-deoxy-5-substituted uridine derivatives

2'-Deoxy-5-fluorouridine derivatives of the formula ##STR1## wherein, R.sup.1 is hydrogen atom or an acyl group and R.sup.2 and R.sup.3 are respectively hydrogen atom, an acyl group or a group of the formula ##STR2## wherein X.sup.1 and X.sup.2 are respectively oxygen atom or sulfur atom; R.sup.4 is a phenyl group, a benzyl group or a naphthyl group each of which may be substituted by an alkyl group, an alkoxyl group, an alkoxycarbonyl group, an alkylthio group, and acyl group, a halogen atom, trifluoromethyl group, nitro group, cyano group, carboxyl group and/or methylenedioxy group and R.sup.5 is an alkyl group, an alkenyl group or one of the groups represented by R.sup.4 which is the same as or different from R.sup.4, at least one of R.sup.2 and R.sup.3 being a group of the formula ##STR3## which exhibit excellent antitumour activities and have lower toxicity, methods of the production thereof and antitumour compositions containing said 2'-deoxy-5-fluorouridine derivatives.

2'-deoxy-5-fluorouridine derivatives

Disclosed is a 2'-deoxy-5-fluorouridine derivative of the formula ##STR1## wherein one of R.sub.1 and R.sub.2 is a benzyl group which may optionally have substituent selected from the group consisting of C.sub.1 -C.sub.6 alkyl group, C.sub.1 -C.sub.6 alkoxy group, C.sub.1 -C.sub.3 halogenated alkyl group, halogen atom, hydroxyl group and nitro group on the phenyl ring, and the other constitutes an amino acid residue, or a salt thereof. The compounds are useful for treating cancer.

1,1,2-triaryl-1-alkene derivatives

Novel 2'-deoxy-5-substituted uridine derivatives, processes for

An anti-cancer composition for delivering a 5-fluorouracil to cancer tissues in a warm-blooded animal, wherein the cancer is a cancer sensitive to 5-fluorouracil. The composition comprises uracil or a pharmaceutically acceptable salt thereof, and a 5-fluorouracil pro drug selected from the group consisting of 1, 3-bis (2-tetrahydrofuryl)-5-fluorouracil and 3-(2-tetrahydrofuryl)-5-fluorouracil in a small amount of about 0.1 to less than 0.1 mole per mole of uracil or salt thereof.

Anti-cancer composition for delivering 5-fluorouracil

An anti-cancer composition for treating cancers sensitive to 5-fluorouracil therapy in warm-blooded animals, comprising 5-fluorouracil and uracil.

An anti-cancer composition for delivering 5-fluorouracil to cancer tissues which comprises at least one 5-fluorouracil derivative, and a uracil derivative.

Anti-cancer compositions for delivering 5-fluorouracil

An anti-cancer composition for delivering 5-fluorouracil to cancer tissues in a warm-blooded animal, wherein the cancer is a cancer sensitive to 5-fluorouracil, comprising 1-n-hexylcarbamoyl-5-fluorouracil and uracil (or salt there-of), wherein the composition contains less than 0.1 mole of the 5-fluorouracil per mole of the uracil.

An anti-cancer composition comprising a 5-fluorouracil (including derivatives thereof) and uracil (or salt thereof), is disclosed, wherein the composition contains less than 0.1 mole of the 5-fluorouracil per mole of the uracil.

A composition for delivering 5-fluorouracil to cancer tissues, of a cancer sensitive to 5-fluorouracil, in warm blooded animals, comprising effective amounts of 1-(n-hexylcarbamoyl)-5-fluorouracil and uracil in a molar ratio of 1:0.1-10, respectively.

Composition containing 1-(n-hexylcarbamoyl)-5-fluorouracil and uracil

A composition containing a pharmacologically effective amount of 1,3-bis(2-tetrahydrofuryl)-5-fluorouracil and an excipient for delivering 5-fluorouracil to cancer cellular tissue of a cancer sensitive to 5-fluorouracil therapy.

Method of and composition for delivering 5-fluorouracil to tumors

An anti-cancer composition comprising a 5-fluorouracil and uracil.

Anti-cancer composition for delivering 5-fluorouracil to cancer tissues

A 5-fluoropyrimidin-4-one derivative represented by the formula ##STR1## wherein R is straight-chain or branched-chain alkyl having 4 to 18 carbon atoms, straight-chain or branched-chain alkenyl having 2 to 18 carbon atoms, alkylene oxido having 3 to 10 carbon atoms, aryl or aralkyl;

Growing community of inventors

Tokushima, Japan

Norio Unemi