Shionogi Company Limited

Shionogi Seiyaku Kabushiki Kaisha

Teikoku Hormone Mfg. Co., Ltd.

Kentaro Hirai

Teruyuki Ishiba

Hirohiko Sugimoto

Shigeru Matsutani

Itsuo Makino

Toshio Fujishita

Kazuyuki Sasakura

Masami Doteuchi

Koichi Otani

Haruo Koike

Masamichi Watanabe

Saichi Matsumoto

Takuji Mizui

Yukio Mizushima

Masami Doeteuchi

The compounds of the present invention inhibit the HMG-CoA reductase, and subsequently suppress the biosynthesis of cholesterol. And they are useful in the treatment of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis.

Pyrimidine derivatives

The compounds of the present invention inhibit HMG-CoA reductase, and subsequently suppress the synthesis of cholesterol. And they are useful in the treatment of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis. The compounds have the formula ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 each is independently hydrogen, optionally substituted lower alkyl, or optionally substituted aryl; R.sup.4 is lower alkyl, aralkyl, aryl, or heteroaryl, each of which is optionally substituted; X is vinylene or ethylene; Y is ##STR2## where R.sup.5 is hydrogen, lower alkyl, aryl, aralkyl, or a cation capable of forming a non-toxic pharmaceutically acceptable salt.

Pyrrole derivatives

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

Isoprenoidamine compounds which are useful antiulcer agents

Isoprenoidamine compounds useful as antiulcer agents

A compound of the formula: ##STR1## (wherein R is hydrogen, hydroxy, methoxy, acetoxy, acetoxymethyl or trifluoromethyl;

Substituted isoquinoline derivatives and anti-ulcer agents

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

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

Aminoalkylbenzene derivatives

A compound of the formula: ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.5 alkanoyl or substituted sulfonyl, which is useful as a synthetic intermediate to 2-guanidino-4-[2-(formamido)ethylthiomethyl]thiazole, histamine H.sub.2 receptor antagonist.

2-Guanidino-4-hydroxymethylthiazole and derivatives thereof

Substituted aminoalkylbenzene type lower acylamides

4,1-Benzoxazepines of the following formula are novel central nervous system: ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.5 alkyl;

Triazolo-4,1-benzoxazepines having CNS activity

Bis(carboxamide) derivatives being useful as histamine H.sub.2 receptor antagonists or anti-peptic ulcer agents are provided from certain dicarboxylic acid derivatives.

Bis(carboxamide) derivatives

4,1-Benzoxazepines of the following formula are central nervous system drugs: ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.5 alkyl; X is hydrogen, halogen, or nitro; Y is phenyl, 2-halophenyl, 4-halophenyl, 2-trifluoromethylphenyl, or pyridyl; and ##STR2## is a group of the formula: ##STR3## (wherein Q is oxygen, sulfur, or hydrazono, with a proviso that, when Y is phenyl or 2-halophenyl and R is hydrogen, Q is neither oxygen nor sulfur;

4,1-Benzoxazepines and compositions

4,1-Benzoxazepines and thia analogs thereof of the formula: ##STR1## (wherein --A--B-- is the following group: ##STR2## (wherein R.sup.1 is hydrogen, C.sub.1 to C.sub.3 alkyl, or C.sub.7 to C.sub.9 aralkyl;

4,1-Benzoxazepines and thia analogs thereof

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

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Kyoto, Japan

Kentaro Hirai