Eisai Company, Limited

Eisai R&d Management Co., Ltd.

Mercian Corporation

Manabu Sasho

Shigeto Negi

Isao Sugiyama

Nobuaki Sato

Takaaki Suzuki

Atsushi Kamada

Kanemasa Katsu

Hiroshi Kuroda

Naoyuki Shimomura

Takaharu Nakamura

Hiroshi Yamauchi

Yuuki Komatu

Kazuhide Ashizawa

Akio Kayano

Mamoru Miyazawa

Keizo Sato

Manabu Kubota

Takeshi Suzuki

Keisuke Matsuyama

Motosuke Yamanaka

Kenji Hayashi

Jun Niijima

Yorihisa Hoshino

Masanobu Shinoda

Fumiyoshi Matsuura

Toshihiko Naito

Toshikazu Shimizu

Takashi Kamiya

Ken Furukawa

Masahiko Tsujii

Hiroshi Ishihara

Masashi Yoshida

Kazuhiro Yoshizawa

Hiroyuki Chiba

Taiju Nakamura

Atsushi Kamata

Kaoru Murata

Yasunobu Kai

Katsutoshi Nishiura

Naoki Ozeki

Susumu Inoue

Masaharu Gotoda

Hiroyuki Saito

Teiji Takigawa

Shin Sakurai

Yuuki Komatsu

Hiroyuki Ishizuka

Takashi Kamahara

Yoshihiko Hisatake

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 provides the compound of formula (I) in a solid form which, as a bulk medicament for pharmaceutical manufacture, is uniform, has a high purity, and is easy to work with. The invention further provides a process for preparing this compound, and pharmaceutical compositions containing the same. A solid form of (8E,12E,14E)-7-{(4-cycloheptylpiperazin-1-yl)carbonyl}oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide which has uniform specifications and is easy to work with was developed.

Macrolide compound in solid form, process for preparation thereof, and pharmaceutical composition containing the same

In the present invention, the methods of producing a fluorinated cyclic benzamidine derivative (A), or a salt thereof, comprise the step of reacting a specific novel compound with ammonia or imide. The methods of this invention for producing a morpholine-substituted phenacyl derivative (B), or a salt thereof, comprise reaction of a specific novel compound with morpholine, reaction of the product with a halogenating reagent, and deketalization of the product. The methods of this invention for a producing cyclic benzamidine derivative (C), or a salt thereof, comprise the step of coupling compound (A), or a salt thereof, with compound (B), or a salt thereof, in the presence of an ether or a hydrocarbon. The methods of this invention for recrystallizing a cyclic benzamidine derivative (C), or a salt thereof, comprise the steps of dissolving compound (C), or the salt thereof, in a mixed solvent comprising an alcohol and water, or a mixed solvent comprising an ether and water, and after dissolution, adding additional water to precipitate crystals of compound (C), or the salt thereof.

Methods for producing cyclic benzamidine derivatives

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

Intermediates useful for the manufacture of carbapenem and a stereoselective manufacturing method therefor

Carbapenem derivatives

3-Substituted vinyl cephalosporin derivatives represented by the following formula: ##STR1## wherein R.sup.1 represents a hydroxyl or lower alkoxyl group, X represents a nitrogen atom or a group represented by the formula --CH.dbd., R.sup.2 represents a carboxyl group or a carboxyl group protected with a protecting group, and R.sup.3 is as defined herein, and pharmaceutically acceptable salts thereof are potent antibacterial agents. Processes for their preparation, intermediates in such processes, and antibacterial compositions containing them as active ingredients are also described.

3-substituted vinyl cephalosporin derivatives

A cephem derivative represented by the following formula: ##STR1## wherein R.sub.1 means a fluorine-substituted lower alkyl and A.sub.1 denotes a cyclic or acyclic ammonio group, or a non-toxic salt thereof, is prepared by reacting a compound represented by the following formula: ##STR2## wherein A.sub.1 has the same meaning as defined above, with another compound represented by the following formula: ##STR3## wherein R.sub.1 has the same meaning as defined above, and if necessary, removing the protecting groups.

Process for the preparation of cephem derivatives and intermediates

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Tokyo, Japan

Manabu Sasho