Eisai Company, Limited

Masuhiro Ikeda

Kiyomi Yamatsu

Takeru Kaneko

Takahiro Nakazawa

Isao Saito

Hachiro Sugimoto

Takaharu Nakamura

Norio Karibe

Kohshi Ueno

Masahiro Yonaga

Masataka Ueno

Shinro Tachibana

Kunizo Higurashi

Yoshihiro Arakawa

Hiroshi Yoshino

Yutaka Tsuchiya

Shin Araki

Shizuko Ohya

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 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

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.

Polypeptide

A novel peptide having the primary structure: N-Me-Tyr-Gly-Gly-Phe-Leu-Arg-Arg-D.Ile-Arg-Pro-Lys-D.Leu-Lys-Trp-NH.sub.2 (in which D.Ile and D.Leu represent a D-Ile and a D-Leu residue respectively, other abbreviations of amino acids represent each an L-amino acid residue and Me represents a methyl group), which exhibits a remarkable analgesic effect when administered peripherally. A process for the preparation thereof by a solid phase method is also disclosed.

Analgesic peptide and process for the preparation thereof

Growing community of inventors

Tsukuba, Japan

Masuhiro Ikeda