Torii & Co., Ltd.

Taiho Pharmaceutical Company Limited

Otsuka Pharmaceutical Company, Limited

Kowa Company Limited

Ono Pharmaceutical Co., Ltd.

Taisho Pharmaceutical Co., Ltd.

Maruho Co., Ltd.

Funai Pharmaceutical Ind., Ltd.

Funai Yakuhin Kogyo Kabushiki Kaisha

Otsuka Pharmaceutical Factory, Inc.

Sanwa Kagaku Kenkyusho Co., Ltd.

Otsuka Kagaku Yakuhin Kabushiki Kaisha

Toho Pharmaceutical Industries Co., Ltd.

Funai Kakuhin Kogyo Kabushiki Kaisha

Otsuka Pharmaceutical

Setsuro Fujii

Norio Unemi

Takashi Yaegashi

Setsuo Takeda

Toyoo Nakayama

Toshiyuki Okutome

Yojiro Sakurai

Kimio Sudo

Shigeki Nunomura

Toshihiro Hamakawa

Kazuo Ogawa

Mitsuteru Hirata

Masateru Kurumi

Yoshiyuki Muranaka

Sadao Hashimoto

Koichiro Watanabe

Eizou Hattori

Hiroshi Ishikawa

Hidetsugu Tsubouchi

Masahiko Nagakura

Koichi Yasumura

Hiroyuki Kawamura

Takuo Aoyama

Koichiro Jitsukawa

Sachio Toyama

Mitsuru Hirohashi

Mamoru Sugimoto

Hiroshi Ishihama

Masahiro Kawasaki

Kenji Kitazato

Yoshihito Yamamoto

Nobuo Yokoo

Tomohisa Miyamoto

Bompei Yasui

Tsuyoshi Watanabe

Naohiro Kayama

Ryoji Matsui

Iwao Hashimoto

Kazuko Ando

Nobumoto Chikazawa

Kouichi Tsuji

Mitsugi Yasumoto

Yutaka Kojima

Hiroshi Matsumoto

Hisashi Kunieda

Naoki Umeda

Tadafumi Terada

Masashi Shiota

Jun-ichi Yamashita

Mitsuo Nakamura

Eiichi Sakakibara

Toshiharu Muraoka

Kouji Ikegaya

Touru Yokoyama

Mitugi Yasumoto

Shin-ichi Watanabe

Junichi Yamashita

Ichiro Yamawaki

Satoshi Yamada

Kazuhiro Onogi

Hiroshi Terashima

Masatoshi Inai

Tomio Ohta

Fumio Shimizu

Masayasu Kurono

Hiroshi Kiyokawa

Shinichi Watanabe

Itsuo Okumoto

Hideki Aishita

Koichi Tsuji

Satoshi Sugiyama

Seizo Taira

Takashi Suzue

Yoshiaki Uegai

Takeshi Chiba

Kiyoaki Noda

Akio Yokoshima

Yoneichi Sawai

Mamoru Sugimito

Masatomi Otsuka

Yoshiyasu Osaki

Yasumichi Kajita

Heizo Kira

Masatoshi Shiga

Yoichiro Kawai

Yuji Mino

Seizi Hiraku

Teruo Arima

Masakazu Fukushima

Keiko Muryobayashi

Takuo Sato

Ken Taniguchi

Minoru Wada

Isao Nakagawa

Seiichiro Yamasaki

Akira Akimoto

Syouzou Sawai

Motoyoshi Kajihara

Toshiaki Shibata

Okumoto Itsuo

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

Novel synthetic polypeptide derivatives, i.e., novel calcitonin derivatives, having improved basic physiological activities of the corresponding natural calcitonins, i.e., the activity for lowering the blood level of calcium, the activity as an analgesic, as well as the activity for inhibiting the secretion of the gastric juice. Thus these synthetic calcitonins are effective as agents for curing hypercalcemia, analgetic agents, anti-ulcerative agents and the like.

Polypeptide derivatives

A composition for increasing the anti-cancer activity of an anti-cancer compound selected from among 5-fluorouracil and a compound capable of producing 5-fluorouracil in vivo, the composition comprising an effective amount of a pyridine derivative represented by the formula ##STR1## wherein R.sup.1 is hydroxy or acyloxy, R.sup.2 and R.sup.4 are each hydrogen, halogen, amino, carboxyl, carbamoyl, cyano, nitro, lower alkyl, lower alkenyl or lower alkoxycarbonyl, R.sup.3 and R.sup.5 are each hydrogen, hydroxy or acyloxy; when at least one or R.sup.1, R.sup.3 and R.sup.5 is hydroxy, the structure of 1-position on the pyridine ring can be ##STR2## due to the keto-enol tautomerism, said hydrogen attached to nitrogen being optionally substituted with a substituent selected from the group consisting of lower alkyl, tetrahydrofuranyl, tetrahydropyranyl, lower alkoxy-lower alkyl, phthalidyl, carbamoyl, lower alkoxycarbonyl-lower alkylcarbamoyl, phenyl-lower alkoxy-lower alkyl, phenylcarbamoyl which may have a substituent on the phenyl ring, lower alkylcarbamoyl, carboxy-lower alkylcarbamoyl, lower alkylthio-lower alkyl and lower alkenyl, provided that the compound having the following formula is excluded, ##STR3## wherein .alpha. is hydrogen, lower alkyl, tetrahydrofuranyl, tetrahydropyranyl, lower alkoxy-lower alkyl, lower alkylcarbamoyl, lower alkylthio-lower alkyl or lower alkenyl.

Composition for increasing the anti-cancer activity of an anti-cancer

5-fluorouracil derivatives

A 2-oxa-isocephem compound of the formula (1): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined, pharmaceutically acceptable salts thereof, composition containing the same and processes for preparing the same are disclosed. The compound is useful as an antimicrobial agent.

2-oxa-isocephem compounds

Phenylcarboxylic acid derivatives having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each H, halogen, alkyl, haloalkyl, alkanoyl, cycloalkyl, nitro, amino, --O--D--R.sup.5 (D is alkylene, R.sup.5 is H, amino, morpholino, carboxyl, phthalimido, phenyl, epoxy), substituted or unsubstituted phenoxy, substituted or unsubstituted phenylalkylamino, carboxylalkenyl, or both form alkylenedioxy; R.sup.3 is H, --E--R.sup.6 (E is alkylene, R.sup.6 is H, carboxyl, cyano, OH, phenylalkoxy, or halogen-substituted phenyl, or phenylcarbamoyl), --CO--G--R.sup.7 (G is alkylene, R.sup.7 is H, substituted or unsubstituted phenylcarbamoyl), substituted or unsubstituted benzoyl, alkenyl, carbamoyl, phenyl, or halophenyl; R.sup.4 is H or alkyl; A is alkylene, alkylene condensed with cycloalkyl ring, or alkenylene; B is alkylene or alkenylene; l is 0 or 1. Said compounds have fatty acid synthesis-inhibitory activity, cholesterol synthesis-inhibitory activity and are useful as antilipidemic agent, prophylactic and treating agent of artherosclerosis, prophylactic and treating agent of obesity, antidiabetics.

Phenylcarboxylic acid derivatives

Derivatives of 5-deoxy-fluorouridine are disclosed of formula (1) ##STR1## in which one of R and R is a substituted furanylmethyl or thienylmethyl group; and the other R and R is a lower alkanoyl group with one free amino substituent or a salt thereof.

3'-O-,5'-O-derivatives of 2'-deoxy-5-fluorouridine

An anticancer compound is disclosed which is represented by the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is a phenyl-lower alkyl optionally having a substituent, phenyl-lower alkenyl or naphthyl-lower alkyl, the other of R.sup.1 and R.sup.2 is hydrogen or acyl, and R.sup.3 is hydrogen, acyl or tetrahydrofuranyl, or represented by the formula ##STR2## wherein R.sup.x is an optionally substituted pyridyl, Y is arylene and .alpha. is a known 5-fluorouracil derivative residue which can be converted to 5-fluorouracil in vivo and which is linked to the carbonyl by an ester or amide linkage.

There is described a 2-oxa-isocephem compound of the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.4 are as defined, and R.sup.3 is a group of the formula: ##STR2## wherein n, m, R.sup.6, R.sup.7, B.sup.- and l are as defined, or pharmaceutically acceptable salt thereof. The compound has antimicrobial activity.

2-oxa-isocephem compounds, compositions containing the same and

2-Oxa-isocephem compounds and compositions containing same

A benzopylpiperazine ester of the following formula: ##STR1## wherein A represents a single bond or an alkylene group, vinylene group, --O--alkylene group or methine group, R.sub.1 represents a bicyclic carbon ring residue which may be substituted with a lower alkyl group, lower alkoxy group, oxo group or nitro group or a halogen atom, or may be partially saturated; a fluorene residue which may contain an oxo group; a fluorenylidene group; an anthracene residue; a phenanthrene residue which may be substituted with a lower alkyl group, or may be partially saturated; a benzofuran residue or thianaphthene residue which may be substituted with a lower alkyl group or lower alkoxy group; a benzopyran residue or benzoazine residue which may be substituted with an oxo group or phenyl group and partially saturated; a phthalimide residue; a benzodiazine residue; an isozazole residue which may be substituted with a lower alkyl group or phenyl group; or an alkylene dioxybenzene residue or xanthene residue; and R.sub.2 represents an alkyl group, cycloalkyl group, cycloalkylalkyl group or aralkyl group, excepting the case where A is a single bond, R.sub.1 is ##STR2## and R.sub.2 is a methyl group, exhibits excellent chymotrypsin inhibitive activity.

Benzoylpiperazine esters and a process for their production

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

A 2-oxa-isocephem compound of the formula (1): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined, pharmaceutically acceptable salts thereof, esters of the carboxy group in the 4-position thereof and quaternary ammonium salts thereof, composition containing the same and processes for preparing the same are disclosed. The compound is useful as an antimicrobial compound.

2-oxa-isocephem compounds, compositions containing same and processes of

Pyrazolotriazine compounds of the formula: ##STR1## wherein R.sup.1 is OH or alkanoyloxy; R.sup.2 is H, OH, or SH; R.sup.3 is (1) unsaturated N- or S-containing heterocyclic group optionally having 1-2 substituents of halogen, nitro or phenylthio, (2) naphthyl, (3) phenyl optionally having 1-3 substituents of (i) alkyl, (ii) phenyl, (iii) alkoxycarbonyl, (iv) cyano, (v) nitro, (vi) alkoxy, (vii) phenylalkoxy (viii) phenylthio-alkyl, (ix) phenoxy, (x) ##STR2## R is alkyl, halo-substituted alkyl, phenyl optionally having 1-3 substituents, or pyridyl, and l is 0, 1 or 2, (xi) halogen, (xii) phenylalkyl, (xiii) carboxy, (xiv) alkanoyl, (xv) benzoyl optionally having 1-3 substituents, (xvi) amino, (xvii) OH, (xviii) alkanoyloxy, (xix) ##STR3## or (xx) ##STR4## (A is alkylene), said compounds having a xanthine oxidase inhibitory activity and are useful for the prophylaxis and treatment of gout.

Pyrazolotriazine compounds

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Toyonaka, Japan

Setsuro Fujii