Eisai Company, Limited

Takaharu Nakamura

Hachiro Sugimoto

Norio Karibe

Kunizou Higurashi

Atsuhiko Kubota

Yoshiharu Yamanishi

Hiroo Ogura

Hiroyuki Sugumi

Yutaka Tsuchiya

Shin Araki

Kiyomi Tamatsu

Michiko Ohtake

Shigeto Negi

Isao Sugiyama

Hiroshi Yamauchi

Kanemasa Katsu

Yuuki Komatu

Toshihiko Naito

Takashi Kamiya

Yasunobu Kai

Yoshimasa Machida

Kyosuke Kitoh

Isao Saito

Seiichiro Nomoto

Kiyomi Yamatsu

Masahiro Yonaga

Takeru Kaneko

Masataka Ueno

Takahiro Nakazawa

Kohshi Ueno

Sachiyuki Hamano

Yoshiharu Daiku

Manabu Sasho

Masuhiro Ikeda

Kunizo Higurashi

Sachiyuki Hamazo

Tetsuya Nakamura

Shizumasa Kijima

Motosuke Yamanaka

Toshiji Igarashi

Kimio Hamamura

Noriyasu Hirose

Hidetoshi Kawashima

Takashi Banba

Kiiti Ema

Noritoshi Sano

Yuko Miyauchi

Yuuichi Inai

A piperdine derivative having the formula (I) or a pharmacologically acceptable salt thereof:

Piperidine derivative and pharmaceutical composition

A cyclic amine is defined by the formula: ##STR1## in which A is naphthyl, phenyl, quinolyl or alkyl, X is a group containing carbonyl, n is 2 or 3 and B is alkyl, halogen, phenyl or --YZ, Y being --0--, --CO-- or --NH--, Z being phenyl, naphthyl, pyridyl, alkyl or cycloalkyl. It is useful to treat a mental symptoms associated with a cerebrovascular disease.

Cyclic amine and pharmacological composition

A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes anthraquinone, X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR5## (in all the above formulas, n is an integer of 1 through 7 and R.sup.3 represents a lower alkyl group or a benzyl group), a group of the formula ##STR6## a group of the formula ##STR7## a group of the formula --O--CH.sub.2 CH.sub.2 CH.dbd. or a group of the formula ##STR8## the ring A denotes a group of the formula ##STR9## a group of the formula ##STR10## a group of the formula ##STR11## or a group of the formula ##STR12##

A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from substituted or unsubstituted quinazolinedione,

A cyclic amine is defined by the formula: ##STR1## in which A is naphthyl, phenyl, quinolyl or alkyl, X is a group containing carbonyl, n is 2 or 3 and B is alkyl, halogen, phenyl or --YZ, Y being --O--, --CO-- or --NH--, Z being phenyl, naphthyl, pyridyl, alkyl or cycloalkyl. It is useful to treat mental symptoms associated with a cerebrovascular disease.

Piperidine compounds useful to treat cerebrovascular diseases

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

A novel piperidine derivative is defined by the formula (I), including a slt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,

Piperdine derivative and pharmaceutical composition

The novel vitamin E derivative provides an excellent antihyperlipemic effect and is defined by the formula (I): ##STR1## wherein R represents a nicotinoyl group; and m is an integer of from 2 to 5 while n is an integer of from 3 to 6, provided that n is larger than m.

Novel vitamin E derivatives and process for the production thereof

A 3-propenylcephem derivative of the following formula: ##STR1## wherein R.sub.1 represents a fluoro-substituted lower alkyl group or a cyano-substituted lower alkyl group, and A represents a cyclic or an acylic ammonio group, or a pharmaceutically acceptable salt thereof, exhibiting excellent anti-bacterial activities against both Gram-positive bacteria and Gram-negative bacteria; Process for the preparation thereof; Anti-bacterial composition; Intermediate for the 3-propenylcephem derivative; and Process for the preparation of the intermediate.

3-propenylcephem derivative

A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,

A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2.] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,

Novel thiadiazolylacetamide cephem derivatives of the following formula are described. ##STR1## wherein A represents a quaternary ammonio group; or a pharmaceutically acceptable salt thereof. These novel compounds are useful as antibacterial agents, because they have a broad antibacterial spectrum ranging from gram-negative bacteria to gram-positive bacteria. Processes for the preparation of these novel compounds are also described.

Thiadiazolylacetamide cephem derivatives

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Abiko, Japan

Takaharu Nakamura