Eisai Company, Limited

Shin Araki

Yutaka Tsuchiya

Hachiro Sugimoto

Atsuhiko Kubota

Yoshiharu Yamanishi

Norio Karibe

Hiroo Ogura

Kunizou Higurashi

Takaharu Nakamura

Hiroyuki Sugumi

Kiyomi Tamatsu

Michiko Ohtake

Kiyomi Yamatsu

Atsushi Sasaki

Takashi Kosasa

Youichi Iimura

Michiko Kosasa

Hiroshi Yoshino

Takeru Kaneko

Shinro Tachibana

Takahiro Nakazawa

Masuhiro Ikeda

Yoshihiro Arakawa

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

Piperidine derivative and pharmaceutical 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 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

A cyclic amine compound is defined by the formula: ##STR1## in which J is indanyl, indanonyl, indenyl, indenonyl, indanedionyl, tetralonyl, benzosuberonyl, indanolyl or a divalent group thereof, K is phenyl, an arylalkyl or cynnamyl, B is --(CHR22) r--, R22 being H or methyl, --CO-- (CHR22)r--, .dbd.(CH--CH.dbd.CH)b--, .dbd.CH--(CH2)c-- or .dbd.(CH--CH)d.dbd. and the ring including T and Q is piperidine. The compound is useful to treat senile dementia.

Cyclic amine compounds and pharmaceutical use

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,

A cyclic amine compound is defined by the formula: ##STR1## in which J is indanyl, indanonyl, indenyl, indenonyl, indanedionyl, tetralonyl, benzosuberonyl, indanolyl or a divalent group thereof, K is phenyl, an arylalkyl or cynnamyl, B is --(CHR22)r--, R22 being H or methyl, --CO--(CHR22)r--, .dbd.(CH--CH.dbd.CH)b--, .dbd.CH--(CH2)c-- or .dbd.(CH--CH)d.dbd. and the ring including T and Q is piperidine. The compound is useful to treat senile dementia.

Cyclic amine compounds with activity against acetylcholinesterase

A novel piperidine derivative or a pharmacologically acceptable salt thereof is used in the treatment and prevention of dementias and sequelae of cerebrovascular diseases. These compounds also exhibit strong, highly selective anticholinesterase activity and may be orally or parenterally administered.

A novel polypeptide is defined by the below shown formula and is useful as an analgesic. ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and each represents a hydrogen atom or a lower alkyl or lower alkenyl group, A represents a D-amino acid, Gly or Sar provided that when the D-amino acid is D-Cys, it is bonded with L-Cys or D-Cys in position 5 through a S--S bond to effect intramolecular ring closure, B represents L-Phe or D-Phe in which the benzene ring may be substituted or an .alpha.-N-alkyl derivative thereof, C represents an L-amino acid, D-Cys or an .alpha.-N-alkyl derivative thereof, D and E each represent an L- or D-basic amino acid or an .alpha.-N-alkyl derivative thereof, F represents a group of the formula --OR.sup.3 (in which R.sup.3 is H or a lower alkyl group), a group of the formula: ##STR2## (in which R.sup.4 and R.sup.5 are the same or different and each represents H or a lower alkyl group), a group of the formula: --G--OR.sup.6 (in which G is an L- or D-amino acid or Gly or an .alpha.-N-alkyl derivative thereof and R.sup.6 represents H or a lower alkyl group), a group of the formula: ##STR3## (in which G is as defined above and R.sup.7 and R.sup.8 may be the same or different and each represents H or a lower alkyl group), a group of the formula: --G--L--Arg--OR.sup.9 or --G--D--Arg--OR.sup.9 (in which G is as defined above and R.sup.9 represents H or a lower alkyl group or a group of the formula: ##STR4## (in which G is as defined above and R.sup.10 and R.sup.11 may be the same or different and each represents H or a lower alkyl group), a group of the formula: --G--J--OR.sup.12 in which G is defined as above, J is a neutral amono acid group or an acidic amino acid group and R.sup.12 is hydrogen or a lower alkyl group; or a group of the formula: --G--Arg--M--OR.sup.13 in which M is D-amino acid group and R.sup.13 is hydrogen or a lower alkyl group, provided that all of the amino acids constituting the polypeptide of the above formula do not represent at the same time an L-amino acid of the general formula: ##STR5## (in which R represents a group corresponding to a structural formula of an amino acid deprived of a group of the formula: ##STR6## or pharmacologically acceptable salts of them.

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Sakuramura, Japan

Shin Araki