Abstract: Novel alkylenediamine derivatives effectively employable glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5 R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.

Abstract: A stabilized physiologically active benzimidazole derivative having the formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a fluoroalkyl group having 1 to 6 carbon atoms, a cycloalkyl group, phenyl group or an aralkyl group, R.sup.2 is hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom form a ring, and each of R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b and R.sup.4c independently is hydrogen atom, a halogen atom, a fluoroalkyl group having 1 to 6 carbon atoms, a lower alkyl group, a lower alkoxy group, a lower alkoxycarbonyl group or an amino group. The stabilized benzimidazole derivative is in amorphous form or present in contact with a basic material.

Abstract: Amino-alcohol derivatives of the formula, ##STR1## where R.sub.1 is a straight or branched alkyl group having 3 to 8 carbon atoms, R.sub.2 and R.sub.3 are each a lower alkyl group, or R.sub.2 and R.sub.3 form a 5- to 7-membered ring together with the adjacent nitrogen atom which may have an oxygen atom attached thereto, R.sub.4 is a hydrogen atom or a lower alkyl group, R.sub.5 is a hydrogen atom or a lower alkyl group, X is a hydrogen or halogen atom or a lower alkyl or lower alkoxy group, and n is an integer of 2 or 3, and acid addition salts thereof, are effectively useful as medicines and agricultural chemicals. Processes are also disclosed for preparing such compounds.

Abstract: A novel glycerol derivative which is effective to reduce blood pressure has the formula: ##STR1## wherein R.sup.1 is an alkyl group having 10-22 carbon atoms, R.sup.2 is lower acyl, benzoyl, aryl, mono-, di- or triarylalkyl, alkyl, cycloalkyl, or cycloalkylalkyl; Q is substituted or unsubstituted alkylene containing 1-4 carbon atoms, l is 0 or 1; Y is a nitrogen-containing heterocyclic group or a nitrogen-containing bridged heterocyclic group (--(Q).sub.l -- is attached to a carbon atom contained in a hetero-ring of the heterocyclic group) in which Y is the bridged heterocyclic group where l is 0; and each of R.sup.5, R.sup.6 and R.sup.7 is hydrogen, lower alkyl, aryl or aralkyl.

Abstract: A peptide having one of the following formulae (I), (II), (III) and (IV): ##STR1## or its functional derivatives, and a pharmaceutically acceptable salt thereof are disclosed. These peptides have a nootropic effect and are effective as antidementia agents.

Abstract: 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.

Abstract: Disclosed is a novel peptide having one of the formulae: ##STR1## (A and B are the amino acids: wherein if A is D- or L-Pro, B is Har or Cit;if A is D-Pro, B is D-Arg, andif B is D- or L-Arg, A is Sar, Pip, Aze or Arg)Asn-A-L-(D-)Pro-Arg-(Gly).sub.n(A is Ser, Thr or Ala, n is 1 or 0)A-Ser-Pip-Arg(A is Pro-Asn-, Asn- or Pro-) ##STR2## (A is cyclopentylcarbonyl, Pro or pGlu; B is Gly or .beta.-Ala, W is a hydrogen atom or a group having the formula: or a peptide having the formula: ##STR3## wherein A and B have the same meanings as mentioned above, respectivelypGlu-Asn-Ser-A-B-(Gly).sub.n(A is Aze, D- or L-Pro, Pip or Sar, B is D- or L-Arg, Cit, Har, Lys or Orn, n is 1 or 0) andPro-(Asn).sub.m -Ser-L-(D-)Pro-Arg-(Gly).sub.n(m and n are independently 0 or 1)their functional derivatives, and pharmaceutically acceptable salts thereof.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: Novel alkylenediamine derivatives effectively employable as glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5, R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.

Abstract: A therapeutic agent for liver disease containing as an active ingredient a piperazine derivative having the formula: ##STR1## wherein, A represents a phenyl, p-benzoquinonyl or cumarinyl group which may have at least one substituent selected from the group consisting of halogen, alkyl, fluoroalkyl, formyl, alkoxycarbonyl, acyl, hydroxy, alkoxy, acyloxy, glycosyloxy, amino, alkylamino, mercapto, alkylthio and nitro; B represents a single bond or a straight chain alkylene group containing 1-4 carbon atoms which may have at least one substituent selected from the group consisting of alkyl, aryl, aralkyl, hydroxy and oxo; R represents an atom or a group selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, alkyl, cycloalkyl, aralkyl and aryl; and n is 2 or 3, or its pharmaceutically acceptable salt is disclosed.

Abstract: A glycerol derivative which is effective to reduce blood pressure and has the formula: ##STR1## wherein R.sup.1 is an alkyl group having 10-22 carbon atoms, R.sup.2 is a lower acyl group or benzoyl, each of R.sup.3 and R.sup.4 independently is hydrogen or a straight or branched chain alkyl group having 1-6 carbon atoms; each of R.sup.5, R.sup.6 and R.sup.7 independently is hydrogen, a straight or branched chain alkyl group having 1-6 carbon atoms, an aryl group or an aralkyl group; and each of m and n independently is 0 or a positive integer under the condition of m+n=2-8.

Abstract: A novel (-)-optically active piperazine derivative of the formula: ##STR1## (wherein the mark of * indicates an optically active carbon) shows an increased cerebral circulation-improving effect as well as an enhanced safety.

Abstract: A novel glycerol derivative which is effective to reduce blood pressure has the formula: ##STR1## wherein R.sup.1 is an alkyl group having 10-22 carbon atoms, R.sup.2 is lower acyl, benzoyl, aryl, mono-, di- or triarylalkyl, alkyl, cycloalkyl, or cycloalkylalkyl; Q is substituted or unsubstituted alkylene containing 1-4 carbon atoms, l is 0 or 1; Y is a nitrogen-containing heterocyclic group or a nitrogen-containing bridged heterocyclic group (--(Q).sub.l -- is attached to a carbon atom contained in a hetero-ring of the heterocyclic group) in which Y is the bridged heterocyclic group where l is 0; and each of R.sup.5, R.sup.6 and R.sup.7 is hydrogen, lower alkyl, aryl or aralkyl.

Abstract: 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.

Abstract: A novel process for the preparation of 2-(10,11-dihydro-10-oxodibenzo[b, f]thiepin-2-yl)propionic acid which shows high anti-inflammatory and analgetic action is disclosed. The process starts from a propiophenone derivative having the formula (II): ##STR1## wherein R.sup.1 is hydrogen or a lower alkyl group, which is once converted into a haloacetal compound via a halo-ketone compound, and then converted into the desired dibenzothiepin derivative through a combination of rearrangement, hydrolysis and ring closure in variable sequences.

Abstract: A process for protection of brain cells comprises orally or parenterally administering into a man suffering from ischemia or being susceptable to ischemia a piperazine derivative having the formula: ##STR1## wherein R.sup.1 is hydrogen or a lower alkyl group, R.sup.2 is hydroxyl, an aralkyloxy group, a lower alkoxy group having 1-5 carbon atoms or a lower alkenyloxy group having 3-5 carbon atoms, R.sup.3 is hydrogen, an aralkyloxy group, a lower alkoxy group having 1-5 carbon atoms or a lower alkenyloxy group having 3-5 carbon atoms and R.sup.4 is hydrogen or a lower alkoxy group having 1-5 carbon atoms.

Abstract: 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.

Abstract: A process for protection of brain cells which comprises orally or parenterally administering into a man suffering from ischemia or being susceptible to ischemia a 1,3-oxazolidin-2-one derivative having the formula: ##STR1## wherein R is a straight or branched chain alkyl having 3-8 carbon atoms, X is hydrogen, halogen, a lower alkyl or alkoxy, and n is 4, 5 or 6. Representative examples of the active component are (4S,5R)-4-(2-methylpropyl)-5-phenyl-3-(3-piperidinopropyl)-1,3-oxazolidin- 2-o ne and (4S,5R)-4-(2-methylpropyl)-3-[3-(perhydroazepin-1-yl)-propyl]-5-phenyl-1,3 -oxazolidin-2-one.