Meiji Seika Kaisha, Ltd.

Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai

Meiji Seika Kabushiki Kaisha

Meuji Seika Kaisha Ltd.

Mitsugu Hachisu

Yasuharu Sekizawa

Takaaki Aoyagi

Seiji Shibahara

Tomio Takeuchi

Shunzo Fukatsu

Hamao Umezawa

Yasuo Sato

Takashi Tsuruoka

Shigeharu Inouye

Taro Niida

Kunio Atsumi

Kiyoaki Katano

Uichi Shibata

Takemi Koeda

Shinichi Kondo

Keiichi Ajito

Dai Kubota

Shoichi Murakami

Mikio Yamamoto

Kenji Kawamura

Hiroyasu Asaoka

Osamu Itoh

Minoru Ishikawa

Shinsuke Kato

Takako Taniguchi

Masaji Sezaki

Tsuneo Okonogi

Shuichi Gomi

Shigeharu Inoue

Yoshiyuki Koyama

Yuji Matsuhashi

Kazuyuki Fujishima

Kazuko Mizutani

Shinjiro Murata

Naoko Kamitoh

Masashi Miyamoto

Keizo Shimomura

Hiroko Kawashima

Keiko Shitoh

Masao Hirayama

Yukiko Takahashi

Takahiko Satoh

Tomoko Soneda

Shinsuke Katoh

Phenylpiperazine derivatives as integrin &agr;v&bgr;3 antagonists

Aminopiperidine derivates as integrin &agr;v&bgr;3 antagonists

An objective of the present invention is to provide a compound that has antiarrhythmic activity. The present invention provides a compound of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 each represent H, halogen or lower alkyl which may be substituted by halogen; A represents H, C3-6 cycloalkyl, phenyl which may be substituted by halogen, nitro, or lower alkoxy, a 5-membered or 6-membered heterocyclic ring which may contain N and/or S, --NR.sup.3 R.sup.4 (wherein R.sup.3 and R.sup.4 each represent H or lower alkyl which may be substituted by phenyl), or COR.sup.5 (wherein R.sup.5 represents OH, amino or lower alkoxy); Q represents S or O; m represents 0-18; and n represents 0-2, and pharmaceutically acceptable salts and solvates thereof.

5-(4-piperidinyl)dibenzothiazepine derivatives and

New N,N-di-alkyl- or alkenyl-substituted derivatives of oxamic acid of which the two alkyl or alkenyl groups are different from each other are now produced and found to exhibit the cerebral protective effect against cerebral anoxia in the brain of a mammalian animal, including human, and to be useful as an agent for improving or ameliorating the damaged or disturbed functions of the brain. Some known N,N-di-alkyl-substituted derivatives of oxamic acid or which the two alkyl groups are identical to each other are now also found to have similar, cerebral protective effect against cerebral anoxia and to be useful as an agent for improving the damaged functions of the brain.

Oxamic acid compounds and pharmaceutical composition for use in

A novel actinonin derivative and a salt thereof are provided, which are useful as enzyme inhibitors and particularly have strong inhibitory activities against enkephalinase and angiotensin-converting enzymes. This actinonin derivative is represented by general formula (I): ##STR1## wherein R.sup.1 is sulfoxymethyl or carboxyl or a substituted carboxyl group selected from carboxamide, hydroxyaminocarbonyl and alkoxycarbonyl groups; and R.sup.2 is hydroxyl, alkoxy, hydroxyamino or sulfoxyamino group.

Actinonin derivatives and pharmaceutically acceptable salts thereof

A method of inhibiting the abnormal postnatal axial growth of the eye of a maturing animal during conditions ordinarily leading to said abnormal growth, which comprises (1) determining the neurochemical present in the retina of said eye, e.g., dopamine, the concentration of which is reduced during said conditions, and (2) administering to said eye during postnatal maturation effective amounts of said neurochemical, its agonist or its antagonist.

Oxamic acid compounds and pharmaceutical compositions for use in

Novel N-(dialkylaminoalkyl)-substituted derivatives or N-(dialkylaminoalkyl)-N-alkyl-substituted derivatives of oxamic acid are now synthetized and found to exhibit the cerebral protective effect against cerebral anoxia in brain of a mammalian animal, including human, and to be useful as an agent for improving or ameliorating the damaged or disturbed functions of the brain.

Novel oxamic acid compounds and pharmaceutical composition for use in

As new compounds are provided a class of derivatives of actinonin represented by the general formula ##STR1## where R is a hydrogen or a lower alkyl group, which can exhibit the enzyme-inhibitory activities to a limited range of peptidases and show a remarkable enzyme-specificity, and which are effective to treat a cycloheximide-induced experimental amnesia in mice and are expectable to be useful to treat an amnesia in a mammalian animal, including human.

Actinonin derivatives having physiological activities

New 3-[N-(mercaptoacyl)]amino-4-arylbutanoic acid derivatives are now provided, which exhibit analgesic activity and are effective to enhance the analgesia induced by a known analgesic compound, ]D-ala.sup.2,met.sup.5 ]-enkephalin (DAME).

3-[N-(mercaptoacyl)]amino-4-arylbutanoic acid derivatives and an

New 3-N-acyl derivatives of 3-amino-2-hydroxy-4-phenylbutanoic acid are provided, which exhibit analgesic activity and are affective to enhance the morphine analgesia.

3-Amino-2-hydroxy-4-phenylbutanoic acid derivatives and pharmaceutical

A 5-phenylthiazole derivative represented by the formula: ##STR1## wherein R represents a hydrogen atom, a lower alkyl group, a hydroxyl group, an amino group or a mercapto group, or a pharmaceutically acceptable salt thereof shows a cardiac effect and a low toxicity to a human or animal with little influence on atrium rhythms.

Cardiotonic agents

A new analgesic agent is now provided, which comprises as the active ingredient 3-amino-2-hydroxy-4-phenylbutanoic acid and some related compounds thereof. These compounds have now found to be effective as inhibitor against enkephalinase and as an agent for enhancing analgesic activity of morphine.

Analgesic agent

5-Substituted picolinic acid derivatives represented by the formula (I): ##STR1## wherein R.sub.1 represents a straight or branched chain halogen-substituted alkyl group having 2 to 6 carbon atoms or a substituted phenyl group having the formula ##STR2## wherein R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, an amino group, an N-alkyl-substituted amino group, an acylamino group, an acetyl group, an acyloxy group, a hydroxy group or a halogen-substituted alkyl group or R.sub.3 and R.sub.4, when taken together, represent a polymethylene chain; and R.sub.2 represents an --OM group wherein M represents a hydrogen, sodium, potassium, calcium, aluminium or magnesium atom, a straight or branched chain or cyclic alkoxy group having 1 to 6 carbon atoms, an aminoalkoxy group, a phenoxy group, a substituted phenoxy group, a 5-indanyloxy group, an acyloxyalkyloxy group having the formula ##STR3## wherein R.sub.5 represents a hydrogen atom or a methyl group and R.sub.6 represents a lower alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group, or an amino group represented by the formula ##STR4## wherein R.sub.7 and R.sub.8, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a phenyl group which are useful as anti-hypertensive agents, a process for preparing the above 5-substituted picolinic acid derivatives, and anti-hypertensive compositions containing the same.

5-Substituted picolinic acid derivatives and an anti-hypertensive

5-Alkoxy-picolinic esters represented by the formula (I): ##STR1## wherein R represents an alkyl group having 1 to 6 carbon atoms and R.sub.1 represents an unsubstituted phenyl group; a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms or an acetyl group; a phthalidyl group; an alkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; an alkoxyalkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; an indanyl group; or an acyloxyalkyl group having the formula ##STR2## wherein R.sub.2 represents a hydrogen atom or a methyl group and R.sub.3 represents an alkyl group having 1 to 5 carbon atoms (such as a methyl, n-propyl, isobutyl, t-butyl, etc., group), an alkoxy group having 1 to 4 carbon atoms, a phenyl group, a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as chlorine, bromine, iodine, etc., atom) or an aralkyl group wherein the alkyl moiety has 1 to 3 carbon atoms, which are useful as anti-hypertensive agents, a process for preparing 5-alkoxy-picolinic esters, and anti-hypertensive compositions containing the 5-alkoxy-picolinic esters.

5-Alkoxy-picolinic esters and anti-hypertensive composition containing

5-Alkoxy-picolinic acids and the salts and the esters thereof represented by the formula (I): ##STR1## wherein R represents an alkyl group having 1 to 6 carbon atoms and M represents a hydrogen atom; a calcium atom; a sodium atom; a potassium atom; an aluminum atom; an unsubstituted phenyl group; a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as a chlorine, bromine, iodine, etc., atom); a phthalidyl group; an alkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; or an acyloxyalkyl group having the formula ##STR2## wherein R.sub.2 represents a hydrogen atom or a methyl group and R.sub.3 represents an alkyl group having 1 to 5 carbon atoms (such as a methyl, n-propyl, isobutyl, t-butyl, etc., group), an alkoxy group having 1 to 4 carbon atoms, a phenyl group, a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as a chlorine, bromine, iodine, etc., atom) or an aralkyl group wherein the alkyl moiety has 1 to 3 carbon atoms, which are useful as anti-hypertensive agents, a process for preparing 5-alkoxy-picolinic acids and the salts and the esters thereof, and anti-hypertensive compositions containing the 5-alkoxy-picolinic acids and the salts and the esters thereof.

5-Alkoxy-picolinic acid calcium salts and anti-hypertensive composition

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Yokohama, Japan

Mitsugu Hachisu