Abstract: Novel quinolinecarboxylic derivatives of the formula: ##STR1## wherein Z is ##STR2## in which R.sup.1 is hydrogen atom or a lower alkyl, R.sup.2 is hydrogen atom, hydroxyl or a lower alkyl and R.sup.3 is hydrogen atom, hydroxyl or an amino, and a pharmaceutical salt thereof have excellent antibacterial activities and are useful as an antibacterial agent.

Abstract: Novel quinolinecarboxylic derivatives of the formula: ##STR1## wherein Z is ##STR2## in which R.sup.1 is hydrogen atom or a lower alkyl, R.sup.2 is hydrogen atom, hydroxyl or a lower alkyl and R.sup.3 is hydrogen atom, hydroxyl or an amino, and a pharmaceutical salt thereof have excellent antibacterial activities and are useful as an antibacterial agent.

Abstract: Novel benzylpiperazine compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof, which has excellent hypolipidemic activity without undesirable side effect, and a pharmaceutical composition containing the compound as an active ingredient suitable for the prophylaxis and treatment of hyperlipidemia.

Abstract: A 1-benzhydryl-4-cinnamylpiperazine derivative represented by the following formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a methoxy group, and R.sup.2 represents a hydrogen or fluorine atom, or a pharmaceutically acceptable acid addition salt thereof. The compound (I) is prepared by selectively reducing the corresponding 1-benzhydryl-4-cinnamoylpiperazine derivative and optionally converting the product into its acid addition salt. The compound (I) is useful for treatment of cerebrovascular disease in a human.

Abstract: Novel compounds of the formula: ##STR1## wherein R is ethyl, 2-fluoroethyl or cyclopropyl, and X is hydrogen atom or fluorine atom, and a pharmaceutically acceptable salt thereof, which have excellent antimicrobial activities in vivo and hence are useful as an antimicrobial agent, and an antimicrobial composition containing said compound as an active ingredient, and processes for the preparation of the compounds.

Abstract: Novel N-phenyl-trans-4-guanidinomethylcyclohexanecarboxamide compounds of the formula: ##STR1## wherein R is hydrogen atom or a lower alkyl group, or a pharmaceutically acceptable salt thereof, which have excellent anti-ulcer activities and hence are useful as an anti-ulcer drug, and a pharmaceutical composition useful for the treatment and prophylaxis of peptic ulcers which comprises as an active ingredient the compound as set forth above in admixture with a conventional pharmaceutically acceptable carrier or diluent.

Abstract: A 1-benzyl-4-benzhydrylpiperazine derivative represented by the following general formula (I) ##STR1## wherein R.sup.1 represents a hydrogen atom or a methoxy group, andR.sup.2 represents a hydrogen or fluorine atom,or a pharmaceutically acceptable acid addition salt thereof.The 1-benzyl-4-benzhydrylpiperazine derivative or an acid addition salt thereof is prepared by reductively condensing a benzaldehyde derivative with a fluorobenzhydrylpiperazine, or condensing a benzyl halide derivative with a fluorobenzhydrylpiperazine optionally in the presence of an acid acceptor, or condensing a benzylpiperazine with a fluorobenzhydryl halide derivative and, optionally converting the product to its acid addition salt.The 1-benzyl-4-benzhydrylpiperazine derivative is useful for improving a cerebrovascular disease.

Abstract: Novel 4,5-bis(4-methoxyphenyl)-2-(pyrrol-2-yl)-thiazoles of the formula: ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, 2,2,2-trifluoroethyl, a group of the formula: --CH.sub.2 COOR.sup.2 R.sup.2 is C.sub.1-8 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, or phenyl-C.sub.1-2 alkyl), or a group of the formula: --(CH.sub.2).sub.n --A--R.sup.3 (A is oxygen or sulfur, R.sup.3 is C.sub.1-4 alkyl or C.sub.2-4 alkenyl, and n is 1, 2 or 3), a process for the preparation of the compounds, and a pharmaceutical composition useful as a platelet aggregation inhibitor which comprises as an active ingredient the above 4,5-bis(4-methoxyphenyl)-2-(pyrrol-2-yl)thiazole compound in admixture with a conventional pharmaceutically acceptable carrier or diluent.

Abstract: An ethyl benzylphosphinate derivative represented by the general formula (I) ##STR1## wherein Y represents a hydrogen or fluorine atom, X represents a methylene group or an oxygen atom, and n is 2, 3 or 4.The said compounds can be produced by reacting a compound represented by the following formula (II) ##STR2## wherein Y is as defined above, with a compound represented by the following formula (III) ##STR3## wherein X and n are as defined, and M is an alkali metal atom, in an inert medium. These compounds are useful as a calcium antagonist.

Abstract: Novel benzimidazole derivatives of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group, a lower alkenyl group or a lower alkynyl group, R.sup.2 is hydrogen atom, a lower alkyl group or a lower hydroxyalkyl group, and n is 2 or 3, or a pharmaceutically acceptable acid addition salt thereof, which have potent antihistaminic activity with less toxicity and hence are useful as an antihistaminics, and a process for the preparation of the compounds, and a pharmaceutical composition useful as antihistaminics containing the compound as an essential active ingredient.

Abstract: 4-Chloro-4-methyl-5-methylene-1,3-dioxolane-2-one is useful as an intermediate for the synthesis of 4-chloromethyl-5-methyl-1,3-dioxolene-2-one which, in turn, finds use as a modifying agent for making various prodrugs.Said intermediate compound gives said objective compound in a good yield by a rearrangement reaction.

Abstract: 1-Ethyl-6,8-difluoro-1,4-dihydro-7-(1-imidazolyl)-4-oxoquinoline-3-carboxyl ic acid derivative of the formula: ##STR1## wherein R is hydrogen atom or an alkyl group having 1 to 3 carbon atoms, which have excellent anti-microbial activities and are useful as an anti-microbial agent for the treatment of infectious diseases in warm-blooded animals including human beings, and an anti-microbial composition containing said compound as an active ingredient.

Abstract: A novel quinolinecarboxylic acid derivative of the formula ##STR1## or a pharmaceutically acceptable salt thereof. These compounds are useful as antibacterial agents, and are prepared by a process which comprises reacting a compound of the formula ##STR2## with a compound of the formula ##STR3##wherein X represents a halogen atom, and thereafter, as required, converting the resulting compound to a pharmaceutically acceptable salt thereof.

Abstract: A 1,1-dioxopenicillanic acid ester represented by formula (I) ##STR1## wherein R represents a methyl or phenyl group. The ester of formula (I) may be prepared by reacting 1,1-dioxopenicillanic acid or its salt with a compound represented by formula (III) ##STR2## wherein R is as defined above, and X represents a halogen atom, or by oxidizing a compound of formula (V) ##STR3## wherein R is as defined above. The ester of the formula (I) is useful as a .beta.-lactamase inhibitor and may be used in association with a .beta.-lactam antibiotic.

Abstract: A phosphonic acid ester of the formula ##STR1## exhibits calcium-antagonistic, coronary vasodilating and hypotensive activities. Pharmaceutical compositions containing the same are useful for the prophylaxis and treatment of circulatory organ diseases such as angina pectoris, hypertension and the like.

Abstract: Novel benzimidazole derivatives of the formula: ##STR1## wherein R.sup.1 is an alkyl group having 1 to 3 carbon atoms, allyl group, propargyl group, or phenyl group; R.sup.2 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms; and n is 2 or 3, or pharmaceutically acceptable acid addition salts thereof, which have excellent antihistaminic activities and are useful as antiallergics for various allergic diseases, and a process for the preparation thereof, and an antihistaminic composition containing the compound as an active ingredient.

Abstract: A process for producing a brominated 1,3-dioxolen-2-one of the following general formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom, a methyl group, or an aryl group, and R.sub.2 represents a hydrogen atom, or R.sub.1 and R.sub.2 may be bonded together to form --(CH.sub.2).sub.n -- in which n represents an integer of 3 to 5, which comprises reacting a compound of the following formula (II) ##STR2## wherein R.sub.1 and R.sub.2 are as defined, with bromine under radical generating conditions.

Abstract: (5-Methyl-2-oxo-1,3-dioxolen-4-yl)methyl 6-[(hexahydro-1H-azepin-1-yl)methyleneamino]penicillanate of the following formula (I) ##STR1## or its pharmaceutically acceptable acid addition salt. The compound is useful as an antibacterial agent and may be prepared by reacting (5-methyl-2-oxo-1,3-dioxolen-4-yl)-methyl 6-aminopenicillanate of the following formula (II) ##STR2## or its acid addition salt with chloro-N,N-hexamethyleneformiminium chloride, and as required, converting the resulting compound to its pharmaceutically acceptable acid addition salt.

Abstract: A novel Ampicillin ester of the general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, a methyl group or an aryl group, and R.sub.2 represents a hydrogen atom or may be taken together with R.sub.1 to form a divalent carbon chain residue, or its acid addition salt.The novel Ampicillin ester or its acid addition salt is prepared by (1) reacting a corresponding 6-N-acylamino penicillanic acid (II) or its salt with a compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 are as defined above, and X is a halogen atom, or reacting a compound of the formula ##STR3## wherein R.sub.1 and R.sub.

Abstract: A 1,3-dioxolen-2-one derivative of the general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, a methyl group, or an aryl group, R.sub.2 represents a hydrogen atom, or may be taken together with R.sub.1 to form a divalent carbon chain residue, and x represents a halogen atom.The above compounds can be prepared by reacting a compound of the general formula ##STR2## with a halogenating agent, and are useful as protective group-introducing reagents for introducing protective groups into reagents in various chemical reactions, or as modifiers for prodrug preparation in medicine.