Fujirebio Kabushiki Kaisha

(Zaidanhojin) Sagami Chemical Research Center

Nippon Chemiphar Co., Ltd.

Toyo Soda Manufacturing Co., Ltd.

Sagami Chemical Research Center

Nitto Boseki Co., Ltd.

Yoshikazu Isowa

Muneki Ohmori

Tetsuya Ichikawa

Kaoru Mori

Yoshiaki Sato

Mitsuo Masaki

Kiyotaka Oyama

Yoshiharu Nakashima

Masaki Uehara

Kenji Hirate

Hideaki Kurita

Yuji Nonaka

Keiichi Kihara

Hajime Matsumoto

Yasuo Sekine

Akihiro Sekine

Heijiro Satoh

Noriaki Kashiwaba

Shigeaki Nishimura

Masanari Sato

Tetsuaki Yamaura

Akihiko Hosoda

Norihisa Miyake

Nobuhiko Hirakawa

Masashi Nishikawa

Takeshi Nagasawa

Seiji Kondo

Katsumasa Kuroiwa

Teruo Kutsuma

Nobuhiro Hirakawa

Koichi Narita

Tetsuaki Yamura

Hisako Harada

Disclosed is a novel peptide having one of the formulae: ##STR1## (A and B are the amino acids: wherein if A is D- or L-Pro, B is Hat or Cit;

Peptides, and antidementia agents containing the same

A novel peptide derivative having the formula: ##STR1## wherein A between Pro and Q.sup.2 is Arg or Lys: Q.sup.1 is pGlu or H; Q.sup.2 is --Gly--OH or OH; Y.sup.1 is H or --CO--T and Y.sup.2 is OH or T; wherein T is a thiamine derivative group is disclosed. The peptide derivative shows a remarkable nootropic effect.

Peptide derivatives and antidemetia agents

A peptide having one of the following formulae (I), (II), (III) and (IV): ##STR1## or its functional derivatives, and a pharmaceutically acceptable salt thereof are disclosed. These peptides have a nootropic effect and are effective as antidementia agents.

Petide antidementia and nootropic agents

Disclosed is a novel peptide having one of the formulae: ##STR1## (A and B are the amino acids: wherein if A is D- or L-Pro, B is Har or Cit;

The compounds of the formulas (VI) and (VII) are useful intermediates in producing pyridyloxy derivatives of the formula (I), such as, for instance, N-{4-[4-(piperidinomethyl)pyridyl-2-oxy]-2-butenyl}-2-(furfurylt hio)acetamide, which are useful as anti-peptic ulcer agents. The compounds of formula (VI) have the formula ##STR1## wherein A represents a formyl group, a protected formyl group, a hydroxymethyl group or a protected hydroxymethyl group. The compounds of formula (VIII) have the formula ##STR2## wherein G represents a formyl group, a protected formyl group, a hydroxymethyl group, a hydroxymethyl group in which the hydroxyl group is protected, or a halogenomethyl group, Y represents --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, and n is 0, 1 or 2.

Intermediates for pyridyloxy compounds having utility as anti-peptic

A compound represented by the following formula or a salt thereof ##STR1## wherein each of R.sub.1 and R.sub.2 represents a lower alkyl group, or R.sub.1 and R.sub.2, together with the nitrogen atom to which they are bonded, may form a substituted or unsubstituted, saturated or partially unsaturated 4- to 8-membered heterocyclic group which may contain a hetero atom selected from N, O and S, Y represents a group of the formula --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, and n is 0, 1 or 2. This compound is useful as anti-peptic ulcer agent.

4-aminomethyl-pyridyl-2-oxy derivatives having anti-ulcer activity

Alkylamide derivatives having the formula, These compounds have a strong antiulcer action depend on histamine H.sub.2 -receptor antagonistic action and a cytoprotective action upon gastric mucous membrance.

Alkylamide derivatives with H.sub.2 -receptor antagonistic and

Addition compounds have the formula ##STR1## wherein R.sub.1 represents an aliphatic oxycarbonyl group, benzyloxycarbonyl group which can have nuclear substituents or benzoyl, aromatic sulfonyl or aromatic sulfinyl group; R.sub.2 represents methyl, isopropyl, isobutyl, isoamyl or benzyl group; R.sub.3 represents a lower alkoxyl, benzyloxy or benzhydryloxy group and n represents 1 or 2. The addition compounds are produced by reacting an N-substituted monoaminodicarboxylic acid having the formula ##STR2## with an amino carboxlic acid ester having the formula in an aqueous medium in the presence of a protease and reacting the resulting dipeptide ester with the amino carboxylic acid ester and separating the addition compound. The addition compounds can be decomposed into the constituent dipeptide esters and amino acid esters by the action of an acid.

Addition compound of dipeptide derivative and amino acid derivative

Addition compounds having the formula ##STR1## wherein R.sub.1 represents an aliphatic oxycarbonyl group, benzyloxycarbonyl group which can have nuclear substituents, or benzoyl, aromatic sulfonyl or aromatic sulfinyl group; R.sub.2 represents methyl, isopropyl, isobutyl, isoamyl or benzyl group; R.sub.3 represents a lower alkoxyl, benzyloxy or benzhydryloxy group and n represents 1 or 2 are produced by reacting an N-substituted monoaminodicarboxylic acid having the formula ##STR2## with an amino carboxylic acid ester having the formula ##STR3## in the presence of a protease.

Addition compounds having the formula ##STR1## wherein R.sub.1 represents an aliphatic oxycarbonyl group, benzyloxycarbonyl group which can have nuclear substituents, or benzoyl, aromatic sulfonyl or aromatic sulfinyl group; R.sub.2 represents methyl, isopropyl, isobutyl, isoamyl or benzyl group; R.sub.3 represents a lower alkoxyl, benzyloxy or benzhydryloxy group and n represents 1 or 2 together with methods for preparing (I) and for decomposing (I) into the constituent dipeptide esters and amino acid esters.

Growing community of inventors

Tokyo, Japan

Yoshikazu Isowa