Abstract: A process suitable for industrially preparing 2,3-trans-1,4-bridged cyclohexane sulfonamide derivatives, especially useful as an intermediate for the synthesis of a trans bicyclo[2,2,1] heptane carboxylic acid derivative, a clinically important thromboxane A.sub.2 antagonist, comprising: allowing to react corresponding a cis/trans mixture of sulfonamide derivatives with an anionoid or water-soluble carbonyl reagent at pH 3-7 so that the trans isomer may form a water-soluble adduct with the anionoid or carbonyl reagent, separating the resulting adduct dissolved in an aqueous layer, and recovering the trans isomer by treating the adduct with a base or an acid. Also provided is an alkali metal hydrogen sulfite adduct of 2,3-trans 1,4-bridged cyclohexane sulfonamide derivative.

Abstract: A process suitable for industrially preparing 2,3-trans-1,4-bridged cyclohexane sulfonamide derivatives, especially useful as an intermediate for the synthesis of a trans bicyclo[2,2,1] heptane carboxylic acid derivative, a clinically important thromboxane A.sub.2 antagonist, comprising: allowing to react corresponding a cis/trans mixture of sulfonamide derivatives with an anionoid or water-soluble carbonyl reagent at pH3-7 so that the trans isomer may form a water-soluble adduct with the anionoid or carbonyl reagent, separating the resulting adduct dissolved in an aqueous layer, and recovering the trans isomer by treating the adduct with a base or an acid. Also provided is an alkali metal hydrogen sulfite adduct of 2,3-trans 1,4-bridged cyclohexane sulfonamide derivative.

Abstract: 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.

Abstract: There is provided 5(Z)-7-(endo-3-benzenesulfonamidobicyclo[2.2.1]hept-exo-2-yl)-5-heptenoic acid, sodium salt which is useful as an antithrombotic, anti-vasoconstricting and anti-bronchoconstricting agent.

Abstract: A process for preparing a compound of Formula (I): ##STR1## wherein R is phenyl or phenyl substituted with hydroxy, lower alkoxy, halogen or lower alkyl; Y is unsubstituted or substituted methylene, ethylene, vinylene or oxygen; m is 0 or 1; n is 0, 1 or 2; and q is 1, 2, 3 or 4; with the limitation that when m is 0, n is not 0, and when m is 1, n is not 2, which process comprises:(a) reacting an aldehyde of Formula (II); ##STR2## wherein R, Y, m and n are as defined above, under reaction conditions for the Wittig Reaction with a ylide of Formula (III):(R.sup.1).sub.3 P.dbd.CH(CH.sub.2).sub.q COOM (III)wherein R.sup.1 is C.sub.1 -C.sub.

Abstract: Pharmaceutical compounds and compositions for injectable use in the treatment of thromboxane A.sub.2 mediating diseases, comprising a pharmaceutical carrier and a pharmacologically effective amount of a compound of the formula: ##STR1## wherein R.sup.1 is carboxyl or 5-tetrazolyl; R.sup.2 is hydrogen, methyl, hydroxy, chloro, or bromo; or a pharmaceutically acceptable ester or salt thereof, together with one or more non-toxic pharmaceutically acceptable carriers; and methods for treating thromboxane A.sub.2 mediating diseases.

Abstract: Bicyclic sulfonamido derivatives represented by the formula: ##STR1## wherein R.sub.1 is a hydrogen or lower alkyl; R.sub.2 is an alkyl, substituted or unsubstituted arly, aralkyl or hetelocycle; R.sub.3 is hydrogen or methyl; X is an alkylene or alkenylene which may be substituted by a fluorine atom or atoms and may contain an oxygen, sulfur and/or phenylene in the chain; Y is straight or branched alkylene or alkeneylene, oxygen, or sulfur; m is 0 or 1; and n is 0, 1 or 2, or their salt, said derivatives being useful as antithrombotic, anti-vasoconstricting, and anti-bronchoconstricting drugs.

Abstract: Bicyclic sulfonamido derivatives represented by the formula: ##STR1## wherein R.sub.1 is a hydrogen or lower alkyl; R.sub.2 is an alkyl, substituted or unsubstituted aryl, aralkyl or hetelocycle; R.sub.3 is a hydrogen or methyl; X is an alkylene or alkenylene which may be substituted by a fluorine atom or atoms and may contain an oxygen, sulfur and/or phenylene in the chain; Y is straight or branched alkylene or alkenylene oxygen, or sulfur; m is 0 or 1; and n is 0, 1 or 2, or their salt, said derivatives being useful as antithrombotic, anti-vasoconstricting, and anti-bronchoconstricting drugs.

Abstract: (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.

Abstract: Tetrazole derivatives represented by the formula: ##STR1## wherein R is naphthyl or phenyl optionally substituted by phenyl, lower alkyo, halogen, lower alkoxy, hydroxy or acetoxy; X is methylene, dimethylmethylene or oxygen; n is an integer of 0 or 1; and p and r each is an integer of 0 or 1 and q is an integer of 1 or 2 provided that p+q+r=2; or a tautomer in tetrazole ring and a pharmaceutically acceptable salt thereof, which are useful as TXA.sub.2 receptor antagonist.

Abstract: Bicyclic sulfonamido derivatives represented by the formula: ##STR1## wherein R.sub.1 is a hydrogen or lower alkyl; R.sub.2 is an alkyl, substituted or unsubstituted aryl, aralkyl or heterocycle; R.sub.3 is a hydrogen or methyl; X is an alkylene or alkenylene which may be substituted by a fluorine atom or atoms an may contain an oxygen, sulfur and/or phenylene in the chain; Y is straight or branched alkylene or alkenylene, oxygen, or sulfur; m is 0 or 1; and n is 0, 1 or 2, or their salt, said derivatives being useful as antithrombotic, anti-vasoconstricting, and anti-bronchoconstricting drugs.

Abstract: Intermediates of the following formula are useful for the synthesis of 1-oxacephalosporins. Their preparation from penicillins and the transformation process to make 1-oxacephalosporins are disclosed. The compounds are of the formula: ##STR1## wherein A is amino or a selected acylamino;COB is carboxy or a selected protected-carboxy;X is halogen or the group ORin which R is a group represented by following formulas: ##STR2## wherein Nu is a selected nucleophilic group; R.sup.1 is a group of the following formula: ##STR3## in which Hal is halogen or alkylsulfonyloxy and R.sup.2 is alkyl or aryl; andY is hydrogen or methoxy; with the proviso that when R is propargyl or 2-oxopropyl andR.sup.1 is ##STR4## A is in the 3.alpha.-configuration and Y is 3.beta.-hydrogen or A is in the 3.beta.-configuration and Y is 3.alpha.-methoxy.

Abstract: An antibacterial 7beta-substituted malonamido-7alpha-methoxy-3-tetrazolylthiomethyl-1-dethia-1-oxa-3-cephem-4 -carboxylic acid and its derivative represented by the following formula: ##STR1## (wherein R.sup.1 is alkyl, hydroxyaryl, or thienyl;R.sup.2 and R.sup.4 each is hydrogen, light metal or a carboxy-protecting group; andR.sup.3 is optionally protected hydroxyalkyl, carbamoylalkyl, dialkylaminoalkyl, or sulfamoylalkyl)are disclosed.

Abstract: A 7.beta.-ureidoacetamido-7.alpha.-methoxy-3-[1-(2-hydroxyethyl)-1H-tetrazol -5-yl]thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acid derivative represented by the following formula: ##STR1## wherein R is aryl or heteroaryl; R.sup.1 is hydrogen or alkyl optionally substituted by halogen or pyridinium; R.sup.2 is hydrogen or a hydroxy-protecting group; and R.sup.3 is hydrogen, a light metal, or a carboxy-protecting group.

Abstract: A 7.beta.-ureidoacetamido-7.alpha.-methoxy-3-(1-carbamoylmethyl-1H-tetrazol- 5-yl)thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acid derivative represented by the following formula: ##STR1## wherein Ar is phenyl, hydroxyphenyl, or thienyl and R is hydrogen, a light metal, or a carboxy-protecting group.

Abstract: A compound represented by the formula (II) epimerizes by the action of a base and the product is precipitated for shifting the equilibrium to yield the corresponding epimer represented by the formula (I). ##STR1## wherein Ar is an optionally substituted aryl or heterocyclic group;Tet is an optionally substituted tetrazolyl group andB.sup.1 and B.sup.2 are each ester forming group in the field of penicillin or cephalosporin chemistry.

Abstract: An intermediate represented by following formula for synthesizing 3-hydroxy-3-cephem compounds. ##STR1## wherein A and B each is a hydrogen or amine substituent; R is a hydrogen or thiol substituent; Nal is a halogen; X is a hydroxy or carboxy protecting group; the broken line between A and R shows that when R and B are hydrogens, and A is a carboxylic acyl, the substituents can be combined to form an azetidimethiazoline bicyclic ring; and the enamine derivatives thereof.

Abstract: 7.beta.-(2-Cyano-aliphatic acylamino)-7.alpha.-methoxy-3-heterocyclic thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acids and salts or pharmacologically acceptable esters generically represented by the following formula are potent antibacterials and esters are prospective oral drugs: ##STR1## (wherein A is a lower alkyl, lower alkenyl or lower alkynyl group;B is a hydrogen atom, salt forming atom, salt forming group or physiologically hydrolyzable ester group; andHet is a heterocyclic group).

Abstract: An antibacterial compound represented by the following formula: ##STR1## (wherein R is a hydrogen atom or a lower alkyl, lower alkenyl, lower alkynyl or lower alkylthio-lower alkyl group;B.sup.1 and B.sup.2 each is a hydrogen atom or an ester or salt forming group or atom same or different for each; andHet is a monocyclic hetero-cyclic group)showing strong antipseudomonal activity, process for preparing the same, pharmaceutical preparation containing the same and method for combating bacterial infection by applying the same.

Abstract: An intermediate represented by following formula for synthesizing 3-hydroxy-3-cephem compounds ##STR1## wherein A and B each is a hydrogen or amino substituent; R is a hydrogen or thiol substituent; Hal is a halogen; X is a hydroxy or carboxy protecting group; the broken line between A and R shows that when R and B are hydrogens, and A is a carboxylic acyl, the substituents can be combined to form an azetidinothiazoline bicyclic ring; and the enamine derivatives thereof.