Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Other

Shigeto Negi

Yoshimasa Machida

Isao Sugiyama

Seiichiro Nomoto

Isao Saito

Hiroshi Yamauchi

Kanemasa Katsu

Kyosuke Kitoh

Yuuki Komatu

Takashi Kamiya

Hironori Ikuta

Motosuke Yamanaka

Toshihiko Naito

Takaharu Nakamura

Manabu Sasho

Akihiko Tsuruoka

Atsushi Kamata

Yasunobu Kai

Takeo Kanai

Shigeru Souda

Naoyuki Shimomura

Kenji Hayashi

Kazutoshi Miyake

Masayuki Matsukura

Toshiaki Ogawa

Naoki Yoneda

Yoshiharu Daiku

Kenichi Nomoto

Toshikazu Shimizu

Masanori Mizuno

Taiju Nakamura

Makoto Kaino

Tadanobu Takamura

Akio Kayano

Naoki Ozeki

Yukio Ohya

Mamoru Miyazawa

Koichi Nose

Naoya Kishi

Fusayo Yoshida

Keizoh Satoh

Mikio Tomimatsu

Kenro Nakatsuka

Toyokazu Haga

Hiroshi Kuroda

Manabu Kubota

Takeshi Suzuki

Seiichi Kobayashi

Keisuke Matsuyama

Hiroyuki Naka

Osamu Asano

Nobuaki Sato

Jun Niijima

Manabu Murakami

Nobuhisa Watanabe

Yorihisa Hoshino

Fujio Nakamura

Tsutomu Kawata

Takeshi Nagasu

Masanobu Shinoda

Hitoshi Harada

Fumiyoshi Matsuura

Takashi Inoue

Atsushi Kamada

Nobuyuki Yasuda

Junsaku Nagaoka

Seiji Yoshikawa

Kazuhiro Yoshizawa

Tatsuo Horizoe

Isao Tanaka

Hiroyuki Chiba

Kaoru Murata

Eiichi Morita

Keizo Takayanagi

Katsutoshi Nishiura

Susumu Inoue

Tamio Kawamura

Hiroe Minami

Kaya Ohashi

Yasuhide Tanaka

Masaharu Gotoda

Teiji Takigawa

Keizo Sato

Shin Sakurai

Yukio Morita

Hiroyuki Ishizuka

Hiroyuki Saito

Yuuki Komatsu

Yoshihiko Hisatake

Kyoko Koizumi

Yoshikazu Hasagawa

Tasuke Kawabata

Hiroshi Akamatsu

Manabu Sasyou

Hirofumi Noda

Ken-ichi Sakai

Manabu Kuboto

Intermediates useful for the synthesis of pyrazole-fused ring derivatives, such as 7-phenylpyrazolo [1,5-a]pyridine derivatives, and method for producing the same. Method for producing compound represented by the general formula (II), wherein Zand Zeach independently represents a methine group or a nitrogen atom; Rrepresents an ethyl group or the like; Rrepresents a hydrogen atom or the like; Rand Reach independently represents a Calkyl group or the like, salts thereof, or solvates of both, comprising the step of: reacting a compound represented by the general formula (I), wherein Z, Z, R, R, Rand Reach has the same definition as described above, with an organometallic reagent; and then reacting the resulting product with pentafluoroiodobenzene. 

Process for production of pyrazole-fused ring derivatives

The present invention relates to calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy) -2-fluoropropoxy]phenyl]-2-isopropoxypropionate] represented by formula (I), a hydrate thereof, a crystal of the compound of formula (I), and a crystal of the hydrate of the compound of formula (I) which are useful as pharmaceuticals, and to processes for producing the same, and intermediates therefore, and processes for production thereof. There is need for (2S)-3-[3-[(2S)-3-(4 -chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, in the form of a drug substance, purified so as to minimize a residual solvent content and having a uniformized specification and a highly favorable workability, and a process for producing the same. Crystalline calcium bis[(2S)-3-[3-[(2S)-3-(4 -chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate], a calcium salt of (2S) -3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, solves the above problem.

Calcium bis [(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl ]-2-isopropoxypropionate] and intermediate thereof

An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group)in the presence of a carbocation scavenger.

Process for preparation of water-soluble azole prodrugs

The present invention relates to a method for producing an isoindole derivative (compound (II)) with the following general formula (II): (wherein Rand Reach independently represents a Calkyl group) or a salt thereof, comprising the step of cyclizing, in a solvent, compound (I) with the following general formula (I): (wherein Rand Rhave the same meanings as Rand Rin formula (II) above) or a salt thereof, or their hydrate or solvate in the presence of a base (Step 1).

Methods for producing isoindole derivatives

The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action. That is, it provides a novel condensed imidazole compound which has an adenosine A2 receptor antagonist action, is effective for preventing or treating diabetes mellitus and diabetic complications, and is represented by the formula (I);(wherein Rrepresents e.g. an amino group which may be substituted with an alkyl group; Rrepresents e.g. hydrogen atom, an alkyl group, a cycloalkyl group or an alkyl group, alkenyl group or alkynyl group which may be substituted with hydrox etc.; Rrepresents e.g. an optionally substituted alkyl group, alkenyl group, alkynyl group, aryl group, heteroaryl group, pyridinone group, pyrimidinone group or piperadinone group; Ar represents e.g. an optionally substituted aryl or heteroaryl group; and Q and W are the same as or different from each other and each represents N or CH), a pharmacologically acceptable salt or hydrates thereof.

Condensed imidazole compounds and a therapeutic agent for diabetes mellitus

Process for the preparation of basic antibiotic-inorganic acid addition salts and intermediate oxalates

Process for producing stereoisomer of pyrrolidine derivative

A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH.dbd. or --N.dbd. group; R.sup.1 denotes a hydroxyl, lower alkoxyl, fluorine-substituted lower alkoxyl or protected hydroxyl group; R.sup.2 and R.sup.3 are the same or different and individually represent a lower alkyl, hydroxyl-substituted lower alkyl, a carbamoyl-substituted lower alkyl group or cyano-substituted lower alkyl group, R.sup.2 is a hydrogen atom and R.sup.3 is a lower alkoxyl or alkyl group optionally substituted by one or more halogen atoms, or the group ##STR2## means a 4-6 membered heterocyclic group, which contains one nitrogen atom, or a morpholino group, said heterocyclic group or morpholino group being optionally substituted by one or more lower alkyl, hydroxyl and/or hydroxyl-substituted lower alkyl groups; and R.sup.4 denotes a carboxyl or protected carboxyl group; or a pharmaceutically acceptable salt thereof; and a process for the preparation thereof; as well as an antibacterial composition containing the above cephem compound.

7-acyl-3-(substituted carbamoyloxy) cephem compounds and process for

Propenoic acid derivatives of the formula: ##STR1## where R.sup.15 and R.sup.17 are aryl or heteroalkyl groups and R.sup.16 and R.sup.18 are hydrogen, a lower alkyl or the like are intermediates used to prepare pharmaceutically active diazole propenoic acid compounds.

Diazole-propenoic acid compounds

A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH.dbd. or --N.dbd. group; R.sup.1 denotes a hydroxyl, lower alkoxyl, fluorine-substituted lower alkoxyl or protected hydroxyl group; R.sup.2 and R.sup.3 are the same or different and individually represent a lower alkyl, hydroxyl-substituted lower alkyl, a carbamoyl-substituted lower alkyl group or cyano-substituted lower alkyl group, R.sup.2 is a hydrogen atom and R.sup.3 is a lower alkoxyl or alkyl group optionally substituted by one or more halogen atoms or the group ##STR2## means a 4-6 membered heterocyclic group, which contains one nitrogen atom, or a morpholino group, said heterocyclic group or morpholino group being optionally substituted by one or more lower alkyl, hydroxyl and/or hydroxyl-substituted lower alkyl groups; and R.sup.4 denotes a carboxyl or protected carboxyl group; or a pharmaceutically acceptable salt thereof; and a process for the preparation thereof; as well as an antibacterial composition containing the above cephem compound.

7-acyl-3-(substituted carbamoyloxy) cephem compounds

A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH.dbd. or --N.dbd. group; R.sup.1 denotes a hydroxyl, lower alkoxyl or protected hydroxyl group; R.sup.2 and R.sup.3 are the same or different and individually represent a lower alkyl, hydroxyl-substituted lower alkyl, a carbamoyl-substituted lower alkyl group or cyano-substituted lower alkyl group, R.sup.2 is a hydrogen atom and R.sup.3 is a lower alkoxyl or alkyl group optionally substituted by one or more halogen atoms, or the group ##STR2## means a 4-6 membered heterocyclic group, which contains one nitrogen atom, or a morpholino group, said heterocyclic group or morpholino group being optionally substituted by one or more lower alkyl, hydroxyl and/or hydroxyl-substituted lower alkyl groups; and R.sup.4 denotes a carboxyl or protected carboxyl group; or a pharmaceutically acceptable salt thereof; and a process for the preparation thereof; as well as an antibacterial composition containing the above cephem compound.

7-acyl-3-(substituted carbamoyloxy) cephem compound

A novel propenoic acid derivative which exhibits adenosine A1 antagonism is defined by the general formula (I): ##STR1## (wherein A represents an aromatic ring; R.sup.1 represents aryl or the like; R.sup.2, R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like; and R.sup.7 and R.sup.8 each represent lower alkyl or the like) or a pharmacologically acceptable salt thereof.

Propenoic acid derivatives diazole propenoic acid compounds which have

A cephalosporin derivative represented by the formula: ##STR1## wherein R.sub.1 represents a lower alkyl group, and A is selected from: a group of the following formula: ##STR2## where R.sub.2 and R.sub.3 are the same or different lower alkyl group, R.sub.4 represents a substituted lower alkyl or amino group; a group which may be substituted and which is represented by the following formula: ##STR3## where R.sub.5 represents a lower alkyl group; or a group of the following formula: ##STR4## where R.sub.5 is as defined above, R.sub.6 represents a hydroxyl lower alkyl or carboxyl group, or its pharmacologically acceptable salt, and a process for preparing the same, as well as an antibacterial agent containing the same.

7Beta-(thiadiazolyl)-2-iminoacetamido-3cephem compounds

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Ibaraki, Japan

Shigeto Negi