The Green Cross Corporation

The Green Cross Company

Chikara Fukaya

Kazumasa Yokoyama

Tadakazu Suyama

Taizo Ono

Yoshio Arakawa

Yoshio Tsuda

Youichiro Naito

Yoshihisa Inoue

Masanori Sugiura

Masakazu Iwai

Kanemichi Okano

Takehiro Okada

Atsuyuki Ashimori

Toshiaki Akira

Masahiro Watanabe

Norifumi Nakamura

Yoshiro Iga

Masahiro Eda

Yusei Shiraga

Yasumi Uchida

Hiroshi Sakashita

Shigeki Kuwahara

Mamoru Tabata

Hiroshi Fukui

Masahiko Kajii

Shigeo Tanaka

Hitoshi Yasuda

Sumio Matzno

Miyuki Eiraku

Mitsuyoshi Hihara

Tadahiro Takemoto

Maki Goda

Tsutomu Mimura

Fumihiko Akahoshi

Yasuhiro Kohama

Koichi Yamauchi

Naoki Sugiyama

Fumihiko Akaboshi

Haruko Yakumaru

Tomokazu Gotoh

Yoshiko Tanaka

Yasunari Yamaura

Takao Kondoh

Shinji Takeda

Hiroko Nishimura

Yoshio Isuda

Youichiro Nishida

Shuichi Hanada

Triazole derivative and pharmaceutical use thereof

An aminopyridine compound represented by the formula: ##STR1## wherein n represents 0 or 1; Z represents .dbd.S, .dbd.NCN or .dbd.CHNO.sub.2 ; R.sub.1 represents --NR.sub.3 R.sub.4, --NHNR.sub.3 R.sub.4, --NHCONHR.sub.3 or --NHSO.sub.2 R.sub.3 ; R.sub.2 represents H, or substituted or unsubstituted alkyl; R.sub.3 and R.sub.4, which may be the same or different, represent H, substituted or unsubstituted alkyl, aryl, substituted or unsubstituted acyl or alkoxycarbonyl group; and R.sub.3 and R.sub.4 may form a heterocyclic ring together with a nitrogen atom to which R.sub.3 and R.sub.4 are bound, through another heteroatom or without it; an optical isomer thereof or art acid salt thereof, which is excellent in pharmacological effect and repressed in side effects as a drug for circulatory diseases.

Aminopyridine compounds

Aminophenol derivatives of the following formula (I) ##STR1## wherein X is hydrogen atom, lower alkyl or a protecting group for phenolic hydroxy, Y is hydrogen atom or lower alkyl, Z is hydrogen atom, lower alkyl, halogen atom or trifluoromethyl, A is hydrogen atom or lower alkyl, t is an integer of 1 to 5, l and m are respectively an integer of 2 to 4, E and W are nitrogen atoms, F is a direct bond or oxygen atom, P and Q are each hydrogen atom, halogen atom, lower alkyl or lower alkoxy, and R.sup.8 is hydrogen atom, hydroxy or a hydroxy-protecting group, and their pharmcologically acceptable salts. Since the aminophenol derivatives (I) of the present invention have excellent antioxidative action and antiinflammatory and antiallergic action in mammalian animals including human, they are extremely useful as pharmaceuticals such as an antiinflammatory or an antiallergic.

Substituted or unsubstituted benzhydryl heteroalkyl-substituted

An aminopyridine compound represented by the formula: ##STR1## wherein n represents 0 or 1; Z represents .dbd.S, .dbd.O, .dbd.NCN or .dbd.CHNO.sub.2 ; R.sub.1 represents --CN, --NR.sub.3 R.sub.4, --CONR.sub.3 R.sub.4, --NHNR.sub.3 R.sub.4, --NHCONHR.sub.3, --NHSO.sub.2 R.sub.3 or --SR.sub.3 ; R.sub.2 represents H, or substituted or unsubstituted alkyl; R.sub.3 and R.sub.4, which may be the same or different, represent H, substituted or unsubstituted alkyl, aryl, substituted or unsubstituted acyl or alkoxycarbonyl group; and R.sub.3 and R.sub.4 may form a heterocyclic ring together with a nitrogen atom to which R.sub.3 and R.sub.4 are bound, through another heteroatom or without it; or an acid salt thereof, which is excellent in pharmacological effect and repressed in side effects as a drug for circulatory diseases.

A therapeutic and prophylactic agent for peptic ulcers which contains as an active ingredient a compound of the general formula (I): ##STR1## wherein R.sub.1 represents hydrogen or .dbd.O; R.sub.2 represents hydrogen or --OR.sub.5 ; R.sub.3 represents hydrogen or --OR.sub.5 ; R.sub.4 represents --OR.sub.7 in the case of the absence of double bond; R.sub.5, R.sub.6 and R.sub.7 each represents hydrogen or an organic residue;

Therapeutic and prophylactic agents for peptic ulcer

A cycloalkane derivative represented by the formula (I): ##STR1## wherein A, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, Z, and n are as defined in the specification. The compounds of formula (I) exhibit activities against peptic ulcers and are useful as therapeutic and prophylactic agents for peptic ulcers.

Cycloalkane derivatives

A therapeutic and prophylactic agent for peptic ulcers comprising as an effective ingredient a cyclohexane derivative represented by general formula (I): ##STR1## wherein A represents a group shown by formula, &gt;CH.sub.2, ##STR2## wherein X represents ethynylene, vinylene or ethylene, Y represents oxo or a hydroxy group; R.sup.1, R.sup.3, R.sup.4 and R.sup.5 each represents a hydrogen atom or alkyl; R.sup.2 represents a hydrogen atom, alkyl or a group shown by --OR.sup.8 ;

Therapeutic and prophylactic agents for peptic ulcers

Novel bis-S-alkylbenzene derivatives capable of inhibiting lipoxygenase, inparticular, 5-lipoxygenase are disclosed. It is expected that the compounds, which are hardly metabolized in vivo, are highly useful in the treatment and/or prevention of various diseases, including allergic diseases such as asthma, inflammation, myocardial infarction, nephritis, scabies and gout.

Bis-S-alkylbenzene derivatives

An antithrombotic composition containing an amide derivative which is obtained by binding a sulfur-containing amine to an unsaturated fatty acid having 4 to 13 carbon atoms through an amide bond and which exerts a high platelet agglutination-inhibiting effect.

Platelet agglutination-inhibiting agent

Dihydropyridine derivatives represented by formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.6, which may be the same or different, each represents an alkyl group, a cycloalkyl group or an alkoxyalkyl group; R.sub.4 and R.sub.5, which may be the same or different, each represents a hydrogen atom, a halogen atom, a nitro group, a halogenated alkyl group, an alkylsulfonyl group, a halogenated alkoxy group, an alkylsulfinyl group, an alkyl group, a cycloalkyl group, an alkxoy group, a cyano group, an alkoxycarbonyl group or an alkylthio group (provided that R.sub.4 and R.sub.5 are not hydrogen atoms at the same time); X represents a vinylene group or an azomethine group; A and B are each an alkylene group or an alkenylene group; R.sub.7 and R.sub.8, which may be the same or different, each represents a hydrogen atom, an alkyl group, an alkenyl group, an aralkyl group, an aryl group, or a heterocyclic group (provided that R.sub.7 and R.sub.8 may combine with the adjacent nitrogen atom to form a heterocyclic ring), and acid addition salts of the dihydropyridine derivatives of formula (I).

Dihydropyridine derivatives

A therapeutic and prophylactic agent for peptic ulcers which contains as an active ingredient a compound of the general formula (I): ##STR1## wherein R.sub.1 represents hydrogen or =O; R.sub.2 represents hydrogen or --OR.sub.5 ; R.sub.3 represents hydrogen or --OR.sub.6 ; R.sub.4 represents --OR.sub.7 in the case of the absence of double bond; R.sub.5, R.sub.6 and R.sub.7 each represents hydrogen or an organic residue;

Dihydropyridine derivatives of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, A, B are defined as in the specification and nontoxic acid-addition salts thereof, have an excellent calcium blocking action (Ca-antagonist), and antihypertensive action, a platelet aggregation-inhibiting action, a phosphodiesterase-inhibiting action and the like, and thus are useful as a medicine, such as a coronary vasocilator, a cerebral hyperkinemic, antihypertensive, thrombosis-preventing or -treating agents, phosphodiesterase-inhibitor or the like. Pharmaceutical compositions and methods of use are also disclosed.

Dihydropyridine derivatives and pharmaceutical composition thereof

1-(fluoro- or perfluoro lower alkyl-substituted benzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic acid carboxymethyl ester is found to have antiinflammatory and analgestic activity with less side effects on gastrointestinal traces than its homologue, acematacin or indometacin.

Indoleacetic acid derivatives used as anti-inflammatories

There is provided a dihydropyridine derivative having the formula ##STR1## wherein R'.sub.1 denotes methyl, chlorine, bromine, fluorine, trifluoromethyl, nitro, cyano or methoxy, R.sub.7 denotes benzyl; and the dihydropyridine links to the 2-, 3-, or 4-position of the pyridine. The compound has an activity as a Ca-antagonist, and is useful for treating vascular disorders such as coronary artery disease, celebral artery disease, hypertension and the like.

Certain 1,4-dihydro-2,6-dilower-alkyl-4-(mono-substituted pyridyl)

New peptide derivatives represented by the following general formula

Peptide derivatives

Growing community of inventors

Osaka, Japan

Chikara Fukaya