Eisai Company, Limited

Takeo Kanai

Shigeto Negi

Seiichiro Nomoto

Eiichi Morita

Yoshimasa Machida

Isao Saito

Isao Sugiyama

Hiroshi Yamauchi

Keizo Takayanagi

Yasuhide Tanaka

Hironori Ikuta

Kyosuke Kitoh

Fujio Nakamura

Takeshi Nagasu

Kanemasa Katsu

Yuuki Komatu

Yukio Ohya

Atsushi Koiwa

Yukio Morita

Tasuke Kawabata

Shinichi Endoh

A novel 4-cyanopiperidine derivative, which is represented by the following general formula (I): ##STR1## wherein X means a halogen atom, or an acid addition salt thereof, is prepared by reacting N-(2-hydroxyethyl)-4-carbamoylpiperidine or an acid addition salt thereof with a dehydrating and halogenating agent; or by reacting 4-cyanopiperidine or a salt thereof with a compound represented by the following general formula (IV):

4-cyanopiperidine derivatives

Improved process for the preparation of 7-(2-amino-2-phenyl-acetamido)cephem derivatives of the general formula (I): ##STR1## wherein R.sub.1 is a hydrogwn atom or hydroxyl group, n stands for 0, 1 or 2, and A denotes a nitrogen-containing heterocyclic group or a direct bond coupling directly the sulfur atom and the --(CH.sub.2).sub.n COOH group together, as well as pharmaceutically acceptable salts thereof. The process is not only simple and easy to carry out, but also provides as crystalline precipitate the intended products with a high yield. The 7-(2-amino-2-phenyl-acetamido)cephem derivatives are useful as intermediates for syntheses of antibacterial agents.

Process for the preparation of 7-(2-amino-2-phenylacetamido) cephem

N-(Substituted chromone-3-carbonyl)phenylglycine derivatives. These derivatives are useful intermediates for cephem compounds which are excellent as antibacterial agents.

N-(Substituted chromone-3-carbonyl)-phenylglycine derivatives

Novel cephalosporin compounds of the general formula: ##STR1## wherein R.sub.1 represents a substituted or unsubstituted nitrogen-containing heterocyclic-thio group, R.sub.2 represents hydrogen or hydroxy, and R.sub.3, R.sub.4 and R.sub.5 each represents hydrogen, hydroxy or acyloxy, and their salts, and processes for the preparation thereof. The novel compounds and their salts have antibacterial activity.

Cephalosporin compounds and antibacterial drugs containing the same

New propiophenone derivatives prepared by the reaction of propiophenone, formaldehyde and piperidine, as well as pharmacologically acceptable acid-addition salts thereof are provided, which possess improved pharmacological activities such as anti-tramorine and anti-nicotine activities superior to those of the known analoguous compound. The new compounds are useful for the therapeutic treatment of human patient suffering from pathological muscular contracture, spastic paralysis due to cerebral apoplexy, spinal and cerebral palsies and the like.

Propiophenone derivatives and preparation thereof

New propiophenone derivatives prepared by the reaction of propiophenone, formaldehyde and piperidine, as well as pharmacologically acceptable acid-addition salts thereof are provided, which possess improved pharmacological activities such as anti-tremorine and anti-nicotine activities superior to those of the known analogous compound. The new compounds are useful for the therapeutic treatment of human patient suffering from pathological muscular contracture, spastic paralysis due to cerebral apoplexy, spinal and cerebral palsies and the like.

Propiophenone derivatives in the treatment of pathological muscular

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Honjo, Japan

Takeo Kanai