Nippon Chemiphar Co., Ltd.

Kuraray Co., Ltd.

Amano Pharmaceutical Co., Ltd.

Nissin Shokuhin Kabushiki Kaisha

Susumu Okabe

Tomio Yamakawa

Yutaka Nomura

Mitsuo Masaki

Masaru Satoh

Hitoshi Matsukura

Masatoshi Hayashi

Yoshiji Fujita

Yoshiaki Omura

Yoichi Ninagawa

Tomonari Ogawa

Kinya Kariya

Mitsuo Mazaki

Masaru Sato

Takashi Sonehara

Masazumi Ikeda

To provide a medicament that can be used as a drug for the effective treatment of gastric ulcers, duodenal ulcers and like diseases of the digestive tract. The medicament comprises a combination of at least one agent selected from the group consisting of histamine H.sub.2 receptor antagonists and proton pump inhibitors, and a digestive enzyme.

Digestive enzyme-containing medicament

Disclosed are novel imidazole derivatives having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are H, alkyl, cycloalkyl, aryl, aralkyl or halogen-substituted alkyl, or R.sup.1 and R.sup.2 are combined to form a heterocyclic ring; R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are H, halogen, alkoxy, aralkyloxy, alkyl, alkoxycarbonyl, nitro, amino, acyl, fluorine substituted-alkyl, or fluorine substituted-alkoxy, or R.sup.3 is combined with R.sup.2 to form a heterocyclic ring; R.sup.8 and R.sup.9 are H, halogen, alkoxy, alkyl, alkoxycarbonyl, nitro, amino, acyl, fluorine substituted-alkyl, fluorine substituted-alkoxy, or aryl group which may have a substituent, or R.sup.8 and R.sup.9 are combined to form an alicyclic ring; R.sup.7 is, where R.sup.8 and R.sup.9 are not combined, H, and, where R.sup.8 and R.sup.9 are combined, H, alkyl which may have a substituent, aryl which may have a substituent, arylcarbonyl which may have a substituent, or a sulfur-containing heterocyclic group; and n is 0 or 1. The new imidazole derivatives are effective particularly as anti-ulcer agents.

Imidazole derivatives

Novel sulfoxide derivatives having the formula (I) 5 or (V) show a gastric acid-secretion inhibitory effect: ##STR1## wherein each of R.sup.1 and R.sup.2 is hydrogen, lower alkyl, hydroxyalkyl, phenyl, phenylalkyl or cycloalkyl, R.sup.1 and R.sup.2 may form together with the adjacent N atom a heterocyclic group; each of R.sup.3, R.sup.4, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6, and R.sup.7 is hydrogen, halogen, lower alkoxy, lower alkyl, trifluoromethyl, or fluorine atom-containing lower alkoxy; Y is CH or N; and Z is unsubstituted or substituted 2-pyridine or 2-aminophenyl.

Fused pyrazine sulfoxide derivatives for use as antiulcer agents

Disclosed are novel imidazole derivatives having the formula: ##STR1## wherein R.sup.1 is hydrogen or an alkyl group having 1-6 carbon atoms, R.sup.2 is an alkyl group having 2-6 carbon atoms substituted with an alkoxy group having 1-4 carbon atoms, each of R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently is hydrogen, a halogen, an alkyl group having 1-6 carbon atoms, an alkoxy group having 1-6 carbon atoms, a fluorine-substituted alkyl group having 1-6 carbon atoms, or a fluorine-substituted alkoxy group having 1-6 carbon atoms. The new imidazole derivatives are effective particularly as anti-ulcer agents.

Sulfinyl imidazole derivatives and antiulcer agents containing the same

Novel imidazole derivatives

Sulfoxide derivatives having the formula (I) or (V) show a gastric acid-secretion inhibitory effect: ##STR1## wherein each of R.sup.1 and R.sup.2 is hydrogen, lower alkyl, hydroxyalkyl, phenyl, phenylalkyl or cycloalkyl, R.sup.1 and R.sup.2 may form together with the adjacent N atom a heterocyclic group; each of R.sup.3, R.sup.4, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6, and R.sup.7 is hydrogen, halogen, lower alkoxy, lower alkyl, trifluoromethyl, or fluorine atom-containing lower alkoxy; Y is CH or N; and Z is unsubstituted or substituted 2-pyridine or 2-aminophenyl.

Certain gastric acid secretion inhibiting sulfoxides

The present invention relates to novel pyrimidine derivatives of the general formula ##STR1## wherein R.sup.1 represents a pyrazolyl, imidazolyl, or triazolyl group, R.sup.2 represents hydrogen atom or lower alkyl group, R.sup.3 represents a halo, amino, lower alkoxy, pyrazolyl, imidazolyl, triazolyl, piperidinyl, or aryloxy group, one of X or Y represents N and the other of X or Y represents CH, and the salts thereof. These derivatives may be used in the treatment of peptic ulcer disease.

Pyrimidine derivatives

A method of protecting gastrointestinal tract in a mammal from the untoward, non-gastric-acid-induced effects of exposure to gastrointestinally injuruous agents, which comprises administering orally to said mammal a non-antisecretory amount of a benzimidazole derivative having the formula (I): ##STR1## wherein R.sup.1 is the hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a cycloalkyl group, phenyl group or aralkyl group, R.sup.2 is the hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom forms a ring, and each of R.sup.3 and R.sup.4 independently is the hydrogen atom, a halogen atom, the trifluoromethyl group, a lower alkyl group, a lower alkoxy group, a lower alkoxycarbonyl group or an amino group.

Method of protecting gastrointestinal tract

An N-acylcarnosine aluminum salt of the formula, ##STR1## wherein R represents a lower alkyl group having 1 to 6 carbon atoms, a phenyl group or a lower alkoxy group-substituted phenyl group, and n is an integer of 1 to 3 is effective for use as a digestive ulcer-remedying or anti-ulcer agent.

N-Acylcarnosine aluminum salt, its preparation, and a digestive ulcer

Novel farnesylacetic acid amide compounds represented by general formula ##STR1## wherein A is alkylene of at least 2 carbon atoms, R.sup.1 is H or lower alkyl, and R.sup.2 and R.sup.3 are each independently H, alkyl, cycloalkyl, alkenyl, aryl or aralkyl, or either one of R.sup.2 and R.sup.3 is such a group that forms, together with A, a piperidine or pyrrolidine ring which contains as constituent thereof the nitrogen atom lying therebetween, or R.sup.2 and R.sup.3 combinedly represent a group which forms, together with the nitrogen atom to which they are bonded, a piperidine, pyrrolidine or piperazine ring; and salts thereof have antiulcerogenic and antibacterial activities.

Farnesylacetic acid amides

Novel farnesylacetic acid ester derivatives containing an amine nitrogen in the alcohol residue thereof and represented by the following general formula exhibit high levels of antiulcerogenic activity and very low levels of toxicity: ##STR1## wherein A is an alkylene radical containing at least 2 carbon atoms; R.sup.1 is H, alkyl, cycloalkyl, aryl, aralkyl or alkenyl; R.sup.2 and R.sup.3 are independently H, alkyl, aryl, aralkyl or alkenyl or one of R.sup.2 and R.sup.3 forms, together with A, a piperidine, pyrrolidine, tetrahydropyrimidine or piperazine ring which contains the nitrogen atom lying therebetween or R.sup.2 and R.sup.3 combine to form, together with the adjacent nitrogen atom, a piperazine ring; provided that the total number of carbon atoms contained in A, R.sup.1, R.sup.2 and R.sup.3 is at least 5.

Growing community of inventors

Kyoto, Japan

Susumu Okabe