Shionogi Company Limited

Masami Doteuchi

Kentaro Hirai

Shigeru Matsutani

Saichi Matsumoto

Takuji Mizui

Koichi Otani

Teruyuki Ishiba

Itsuo Makino

Masayuki Narisada

Toshio Fujishita

Shuh Narumiya

Toru Kita

Yukio Mizushima

Fumihiko Watanabe

Teruo Yamamori

Ikuo Adachi

Motohiko Ueda

Yasunobu Ishihara

Fumrhio Watanabe

Haruhiko Tada

Fumio Yasuda

(Di-tert-butylhydroxyphenyl)thio substituted hydroxamic acid derivatives of the formula: ##STR1## wherein X is straight or branched C.sub.1 to C.sub.15 alkylene which may be attached to Y through phenylene, provided that X is not n-butylmethylene; Y is CO--N(OH) or N(OH)--CO; and R is hydrogen or straight or branched C.sub.1 to C.sub.9 alkyl, C.sub.3 to C.sub.9 cycloalkyl, aryl, or aralkyl, provided that R is not hydrogen when Y--R is N(OH)--CO--R; or a pharmaceutically acceptable salt thereof; useful in treating arteriosclerosis, ulcer, inflammation, allergy, or the like.

Di-tert-butyl(hydroxy)phenylthio substituted hydroxamic acid derivatives

Phenolic thioethers of the formula: ##STR1## wherein R is a hydrogen atom or a protective group for carboxyl, X is a straight or branched C.sub.4 -C.sub.15 alkylene group, a straight or branched C.sub.1 -C.sub.15 alkylene group having a phenylene group or a straight or branched C.sub.2 -C.sub.15 alkenylene group, and their salts, which inhibit the denaturation of low density lipoproteins (LDL) and the incorporation of LDL by macrophages and are useful as anti-arteriosclerosis agents.

Phenolic thioethers, and their production and use

Novel isoprenoidamine compounds (I) which show antiulcer activity are provided. ##STR1##

Isoprenoidamine compounds which are useful antiulcer agents

(Di-tert-butylhydroxyphenyl)thio derivatives of the formula: ##STR1## wherein R is cyano, carbamoyl, or 5-tetrazolyl; n is an integer of 2 to 6; provided that when R is cyano, n is not 2; or a pharmaceutically acceptable salt thereof; useful in treating arterioschlerosis, ulcer, inflammation, allergy, or the like.

(Di-tert-butylhydroxyphenyl)thio derivatives and antiarterioschlerosis

Isoprenoidamine compounds useful as antiulcer agents

9-(Substituted thio)-4H-pyrido[1,2-a]pyrimidin-4-one derivatives of the formula: ##STR1## wherein n is 0 or 1, R is --COR.sup.1, --CONR.sup.4 R.sup.5 or --CH.sub.2 R.sup.6, R.sup.1 is C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl, allythio, styryl, phenoxymethyl, thienylmethyl, C.sub.6 -C.sub.10 aryl optionally substituted, benzyl optionally substituted or 5- or 6-membered heterocyclic group optionally substituted, R.sup.2 and R.sup.3 each is hydrogen, C.sub.1 -C.sub.5 alkyl, carboxy, C.sub.2 -C.sub.5 alkoxycarbonyl or benzyloxycarbonyl optionally substituted, R.sup.4 and R.sup.5 each is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl optionally substituted, and R.sup.8 is pyridyl or phenyl optionally substituted) being useful as antiulcer agents are provided through several routes.

9-(Substituted thio)-4H-pyrido[1,2,-A]pyrimidin-4-one derivatives

A compound of the formula: ##STR1## (wherein R.sup.1 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkoxycarbonyl, or trifluoromethyl; R.sup.2 is hydrogen, C.sub.1 -C.sub.5 alkoxycarbonyl, C.sub.6 -C.sub.12 aryloxycarbonyl, C.sub.1 -C.sub.5 alkanoyloxy-C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxycarbonyloxy-C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 acylamino-C.sub.1 -C.sub.5 alkyl, 2-hydroxy-1-C.sub.2 -C.sub.5 alkenyl, phthalimido-C.sub.1 -C.sub.5 alkyl, halogeno-C.sub.1 -C.sub.5 alkoxycarbonyl-C.sub.1 -C.sub.5 alkyl, hydroxy-C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkylthio-C.sub.1 -C.sub.5 alkyl, or C.sub.1 -C.sub.5 alkylsulfinyl-C.sub.1 -C.sub.5 alkyl; ##STR2## m is an integer of 0 or 1; R.sup.3 and R.sup.4 each is hydrogen, halogen, cyano, C.sub.1 -C.sub.5 alkyl, amino, C.sub.1 -C.sub.5 alkoxy, C.sub.6 -C.sub.12 aryl-C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkoxycarbonyl, fluoro-C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkanoylamino, or carbamoyl) or its salt, being useful as antiulcer agents, is provided.

Thienopyridine derivatives useful in treating gastric ulcers

Highly effective anti-ulcer agents, i.e. Quassinoids of the following formula: ##STR1## wherein R is hydrogen or hydroxy;

Novel anti-ulcer agents and quassinoids

An aminoalkylbenzene derivative of the formula: ##STR1## [wherein A is oxygen or sulfur;

Aminoalkylbenzene derivatives

1,6-Dialkyl-3-substituted-4-nitrophenyl-4,7-dihydropyrazolo[3,4-b]pyridine- 5-carboxylic acid esters as Ca blocker having potent antihypertensive and coronary vasodilating actions and useful in treatment of diseases in circulatory system such as angina pectoris, hypertension, cerebrovascular dysfunction, arrhythmia, etc. with no systole inhibitory action, prepared from nitrobenzylideneacetoacetic acid esters on reaction with 3-substituted-5-amino-1-alkylpyrazoles.

1,6-Dialkyl-3-su

A compound of the formula: ##STR1## [wherein R is dimethylamino or 1-pyrrolidinyl;

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Osaka, Japan

Masami Doteuchi