Abstract: Potent dopamine-.beta.-hydroxylase inhibitors having the Formula ##STR1## that are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.

Abstract: Fungicidally active novel piperazinylmethyl-1,2,4-triazolylmethyl-carbinols of the formula ##STR1## in which R represents optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkinyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted aryloxyalkyl or optionally substituted arylthioalkyl,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents optionally substituted alkyl, optionally substituted alkenyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl,Z represents the ##STR2## group and p represents the number 0 or 1,or addition products thereof with acids and metal salts.

Abstract: Novel compounds including 1-aryl-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofurans such as 1-(4-chlorophenyl)-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofuran, and 1-aryl-1-(1H-1,2,4-trizazol-1-ylmethyl)-1,3-dihydroisobenzofurans are disclosed. The corresponding benzo[c]thiopenes, isochromans, and isothiochromans and antifungal pharmaceutical compositions containing same, and methods of using said pharmaceutical compositions to elicit an antifungal response in warm blooded animals having a susceptible antifungal infection are also disclosed.

Abstract: Substituted [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3 dioxolan-2-yl]methyl]-1H-imidazoles and 1H-1,2,4-triazoles having antimicrobial properties and being particularly useful in the treatment of vaginal candidosis.

Abstract: New 1,2,4-triazolo-carbamates of general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings given in the specification, are acetylcholinesterase inhibitors and may be used as drugs for the treatment of senile dementia.

Abstract: 2-Alkyl-, 2-alkenyl- and 2-alkynyl-2,3-dihydro-2-(1H-azolyl(C.sub.1 -C.sub.2)alkyl)benzo[b]thiophenes especially 2-alkyl-, 2-alkenyl- and 2-alkynyl-2,3-dihydro-3-hydroxy-2-(1H-1-imidazolylmethyl)-4-,5-,6- and 7-halobenzo[b]thiophenes and related derivatives having antifungal activity are disclosed. Pharmaceutical compositions comprising compounds of the invention and their use in treating fungal infections in susceptible hosts such as humans are also disclosed.

Abstract: 3,4-Diazole derivatives corresponding to the general formula I ##STR1## which exert a highly selective action on histamine-H.sub.2 receptors are described. Processes for the preparation of these compounds and pharmaceutical preparations containing these compounds are also described.

Abstract: Triazole compounds of the formula: ##STR1## in which: X and X', which are the same or different, each represents hydrogen, halogen, trifluoromethyl, C.sub.1 -.sub.5 alkyl, or C.sub.1 -.sub.5 alkoxy, orX and X' together represent methylenedioxy,n is an integer of from 1 to 6,a is 0, 1 or 2;b is 0, 1, 2 or 3;c is 0, 1 or 2 andd is 2, 3, 4 or 5 such that a+b+c+d is equal to 4, 5, 6 or 7.These compounds and physiologically tolerable acid addition salts thereof may be used as medicines especially in the treatment of pain and anxiety.

Abstract: A process for preparing a compound of formula (I) ##STR1## wherein X phenyl optionally substituted by one halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy; or pyridyl; R.sup.1 is hydrogen or C.sub.1-6 alkyl; and n is an integer of from 1 to 6; which process comprises, cyclizing a compound of formula (II): ##STR2## wherein X, R.sup.1 and n are as defined in relation to formula (I); Y is an hydroxy or an acid activating group and R.sup.x is hydrogen or an N- protecting group and thereafter if desired carrying out one or more of the following steps: (i) removing any protecting group R.sup.x, (ii) preparing a salt of the compound of formula (I).

Abstract: The present invention relates to indane derivatives with the following formula: ##STR1## wherein R.sub.1 is H, Halogen, an alkyl group having from one to three carbon atoms inclusive, methoxy, a methylthio-group, or a trifluoromethyl group,n is 2-4X is O or S,Y is O, CH.sub.2 or N--R.sub.2, where R.sub.2 is hydrogen or an (1-6 C) alkyl, (2-6 C) alkenyl or cycloalkyl-methyl group having from three to six carbon atoms,Z is --(CH.sub.2).sub.n --, n is 2 or 3 or Z is 1,2-phenylene optionally substituted with halogen or trifluoromethyl or Z=1,2--C.sub.6 H.sub.4 CO-- (to form a quinazolidinone or -thione ring system). U=N or C.Each compound exists as geometric isomers and each of these as a pair of optical isomers; and the separation and isolation of these are also within the scope of the invention.Moreover, pharmaceutically acceptable acid addition salts of the compounds of Formula I are within the scope of the present invention.

Abstract: Tetrazole derivatives of the formula: ##STR1## wherein R.sup.1 is an optional defined substituent; A is sulfur or a lower alkylene-thio, l is 0 or 1; B is a lower alkylene; R.sup.2 is hydroxy, a lower alkoxy, or a group: ##STR2## wherein R.sup.3 and R.sup.4 are optional defined substituents, or the R.sup.3 and R.sup.4 may combine together with the nitrogen atom to which they are joined to form a defined heterocyclic group, and a pharmaceutically acceptable salt thereof, which have prophylactic or therapeutic activities against peptic and/or duodenal ulcers and also anti-inflammatory activity and are useful as an anti-ulcer or anti-inflammatory drug; processes for the preparation of the tetrazole derivatives; and pharmaceutical composition containing said tetrazole derivatives.

Abstract: Alkanol derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--CH.sub.2 X--CH.sub.2 --Y--(CH.sub.2).sub.n --NHR.sup.3 (I)which have a highly selective action on histamine-H.sub.2 receptors are described. Due to this action, these compounds may advantageously be used for treatment of diseases caused by raised gastric secretion.

Abstract: 1,3-Dioxolanyl derivatives corresponding to the general formula I ##STR1## are described. These compounds have an antimicrobial activity and may therefore advantageously be used in chemotherapy.

Abstract: Novel phenylpiperazinylpropane and -butane derivatives of hetarylphenols and hetarylanilines of the formula ##STR1## where R.sup.1 is hydrogen or alkyl of 1 to 4 carbon atoms, R.sup.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms or alkoxy where alkyl is of 1 to 3 carbon atoms, the phenyl ring can be monosubstituted or disubstituted by R.sup.2, X is oxygen or an NH group, and the heterocyclic structure Het. is 1,3,4-oxadiazolyl, triazolyl, imidazolyl or pyrazolyl, and their physiologically tolerated addition salts with acids, processes for their preparation, and pharmaceutical formulations which contain these compounds and exhibit predominantly sedative, neuroleptic and hypotensive properties.

Abstract: Substituted [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]methyl]-1H -imidazoles and 1H-1,2,4-triazoles having antimicrobial properties and being particularly useful in the treatment of vaginal candidosis.

Abstract: Novel tertiary aminohydroxypropoxy substituted aryl compounds exhibit .alpha..sub.1 -adrenoceptor and serotonin antagonism and are also useful as antihypertensive agents.

Abstract: Benzodioxine compounds of the formula: ##STR1## in which Het is a five- or six-membered heterocyclic radical containing from one to three hetero atoms, and from one to three double bonds, optionally substituted by one or more alkyl or alkoxy radicals each from C.sub.1 to C.sub.5.These compounds and physiologically tolerable acid addition salts thereof may be used as medicines, especially in the treatment of psychoses.

Abstract: 2-[3-[4-(3-Halophenyl)-1-piperazinyl]propyl]-5-(1-hydroxyethyl)-2,4-dihydro -[4-phenoxyalkyl-3H-1,2,4-triazol-3-ones and closely related compounds are psychotropic agents having promise as antidepressants by virtue of their receptor site binding affinity profiles and animal pharmacology.

Abstract: The new azolylmethylamines can be prepared by reaction of amines and azoles with formaldehyde. They can be used in microbicidal agents.

Abstract: A dibenz[b,e]oxepin compound having an antiallergic activity is represented by the following general formula: ##STR1## wherein R.sub.1 represents a cyano group, a 5-tetrazolyl group, a carbamoyl group or --CO.sub.2 R.sub.3 wherein R.sub.3 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms or a 1-(ethoxycarbonyloxy)ethyl group, and R.sub.2 represents a 4-alkylpiperazino group wherein the alkyl group has 1 to 5 carbon atoms, a 3-quinuclidinylamino group or --X--(CH.sub.2).sub.n --NR.sub.4 R.sub.5 wherein X represents --NH--, --S -- or --O--, R.sub.4 and R.sub.5 are same or different and each represents an alkyl group having 1 to 5 carbon atoms and n represents 2 or 3; and the pharmaceutically acceptable acid addition salts or metal salts thereof.

Abstract: Described are 5-diazacycloalkyltriazolo[2,3-c][1,3]benzodiazepines, for example compounds of the formula ##STR1## wherein R.sub.1 represents hydrogen, halogen, trifluoromethyl, lower alkylthio, lower alkoxy or lower alkyl; R.sub.2 represents hydrogen, lower alkyl or hydroxy-C.sub.2 -C.sub.7 alkyl wherein the hydroxy group is separated from the nitrogen atom by at least 2 carbon atoms; R.sub.3 represents hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen or trifluoromethyl; and C.sub.n H.sub.2n represents ethylene. The synthesis, pharmaceutical compositions and methods of use as neuroleptic and/or antihistaminic agents are given.

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: Antibacterial activity is exhibited by .beta.-lactams having a ##STR1## substituent in the 1-position and an acylamino substituent in the 3-position wherein Z is oxygen or sulfur, and R is alkyl, alkenyl, alkynyl, substituted alkyl, phenyl, substituted phenyl, a 5,6 or 7-membered heterocycle (R.sub.c), phenylalkyl, (substituted phenyl)alkyl, R.sub.c -alkyl or --NR.sub.a R.sub.b wherein R.sub.a and R.sub.b are the same or different and each is hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, phenylalkyl, or (substituted phenyl)alkyl or one of R.sub.a and R.sub.b is hydrogen, alkyl, phenyl, substituted phenyl, phenylalkyl or (substituted phenyl)alkyl and the other is amino, alkanoylamino, arylcarbonylamino, alkoxycarbonylamino, alkylsulfonylamino, alkylamino, dialkylamino, phenylamino, (substituted phenyl)amino, hydroxy, cyano, alkoxy, phenyloxy, (substituted phenyl)oxy, phenylalkoxy, (substituted phenyl)alkoxy, R.sub.c, R.sub.c -alkyl, R.sub.

Abstract: A compound having the formula ##STR1## can be prepared by heating an anion having the formula ##STR2## with a cation having the formula ##STR3## or a cation having the formula ##STR4##

Abstract: This disclosure describes novel 2-(4-substituted-1-piperazinyl)[1,2,4]triazolo[1,5-a]pyrimidines useful as hypotensive agents.

Abstract: There is disclosed a process for preparing a 1,2,4-triazole-3-carboxamide represented by the formula: ##STR1## wherein, R.sup.1 and R.sup.2 represent independently a hydrogen atom, an alkyl group, a cycloalkyl group or an aryl group, or both R.sup.1 and R.sup.2 represent an alkylene group linked with each other directly or through an oxygen atom or a nitrogen atom to form a ring together with the nitrogen atom to which they are attached,which comprises subjecting an oxamohydrazide represented by the formula: ##STR2## wherein R.sup.1 and R.sup.2 have the same meanings as defined above,to reaction with formamidine or a salt thereof.

Abstract: Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and a 1-substituent of the formula ##STR1## (or a salt or ester thereof).

Abstract: The present invention provides certain aminoalkyl and aminoalkenyl triazoles which are useful as anti-psychotics. Certain of these aminoalkyl triazoles were previously known as anti-allergy agents.

Abstract: The invention relates to novel intermediates for preparing novel cephem compounds of high antimicrobial activity, the intermediates being of the formula: ##STR1## wherein A is lower alkylene which may have an oxo group;R.sup.3 is carboxy, protected carboxy, lower alkyl, lower alkenyl, hydroxy(lower)alkyl, phenyl(lower)alkyl or aryl; andR.sup.7a is hydrogen or a mercapto-protective group, or a salt thereof.

Abstract: This disclosure describes novel pyrazolylpiperazines useful as hypotensive agents in mammals and as intermediates for the preparation of certain pyrazolo[1,5-a]pryrimidines.

Abstract: There are disclosed compounds having the formula ##STR1## wherein X is a group selected from ##STR2## Y represents a single or double bond; R.sup.1 is hydrogen or lower alkyl;n is an integer 2-4;n' is an integer 1-2; andR is 2-pyrimidinyl, 2-pyridinyl, 2-pyrazinyl, halo-substituted 2-pyrazinyl, 5-tetrazolyl, phenyl or phenyl substituted by halo, lower alkyl or lower alkoxy;and the pharmacologically acceptable salts thereof, which exhibit anti-hypertensive activity.

Abstract: 4-Cyano-2-azetidinone derivatives represented by the formula ##STR1## wherein R.sup.1 is an amino group which may be acylated or protected, X is a hydrogen atom or a methoxy group and W is a hydrogen atom or a sulfo group, and methods of producing the same, for example, as represented by ##STR2## wherein R.sup.2 is an acylated or protected amino group, Y is a halogen atom or a group having the formula --OCOR.sup.3, --SCOR.sup.3 or --S(O).sub.n --R.sup.3 (R.sup.3 being a hydrocarbyl group and n an integer 1 or 2), R.sup.4 is an amino group which may be acylated or protected and X is as defined above. Compounds [I] are useful as advantageous intermediates for the synthesis of optically active 4-substituted-2-azetidinone derivatives, and, when W=SO.sub.3 H, [I] are also useful as antimicrobial agents and as beta-lactamase inhibitors.

Abstract: Isochromans, isothiochromans, 2-benzoxepins, and 2-benzothiepins are described. The compounds possess hypotensive and anti-psychotic properties; methods and compositions using them are described.

Abstract: Disclosed are compounds of the general formula: ##STR1## wherein R.sub.1 is amino, an acylated amino or a protected amino group, X is hydrogen or methoxy, and R' is hydrogen, R or R.sup.4 wherein R is an organic residue attached to the azetidine ring through a carbon atom therein and R.sub.4 is azido, a halogen, an amino group which may optionally be acylated or a group of the formula --OR.sub.5, ##STR2## or --S--S--R.sub.5 wherein R.sub.5 is an organic residue and n is 0, 1 or 2, and pharmaceutically acceptable salts and esters thereof.The compounds have antimicrobial and/or .beta.-lactamase-inhibitory activity and are of value as drugs for human beings and domesticated animals.

Abstract: A class of bicyclic benzenoid aminoalkylene ether and thioether compounds exhibiting pharmacological activity including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions are disclosed.

Abstract: Novel derivatives of 4-(piperazin-1-yl-phenyloxymethyl)-1,3-dioxolan-2-ylmethyl-1H-imidazoles and 1H-1,2,4-triazoles, useful as antifungal and antibacterial agents.

Abstract: The compounds of the formula ##STR1## in which R is hydrogen, halogen, alkyl, alkoxy, hydroxyl, nitro or cyano; andR.sup.2 is .dbd.O, .dbd.S, H.sub.2, --SCH.sub.3, or an amino group; with the proviso that when R is chloro in 8-position, R.sup.2 must be other than oxygen or sulfur; or a pharmaceutically acceptable salt thereof.

Abstract: Novel heterocyclic derivatives of (4-phenylpiperazin-1-yl-aryloxymethyl-1,3-dioxolan-2-yl)methyl-1H-imidazol es and 1H-1,2,4-triazoles, useful as intermediates and as antifungal and antibacterial agents.

Abstract: Phenoxyalkyl substituted-1,2,4-triazolones having anti-depressant properties typified by 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-4-(2-phenoxyethyl)- 2H-1,2,4-triazol-3(4H)-one are disclosed.

Abstract: Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 where Q.sub.

Abstract: A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and an acid addition salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.

Abstract: A 2-azolylmethyl-1,3-dioxolane or -dioxane derivative of the formula ##STR1## in which Az is imidazol-1-yl or 1,2,4-triazol-1-yl,R.sup.1, R.sup.2, R.sup.3 and R.sup.5 each independently is hydrogen or alkyl, orR.sup.1 and R.sup.3 together are an optionally substituted multi-membered methylene bridge,R.sup.4 is hydrogen, optionally substituted alkyl, optionally substituted aryl or optionally substituted aralykyl,m is 0 or 1,R.sup.6 is hydrogen, halogen, cyano, alkyl, optionally substituted aryl, --X--R.sup.7, --COOR.sup.8 or --CONHR.sup.9,X is oxygen, sulphur, SO, or SO.sub.2,R.sup.7 is alkyl, halogenoalkyl, cyano, optionally substituted aralkyl or optionally substituted aryl,R.sup.8 is alkyl,R.sup.9 is alkyl or optionally substituted aryl, andn is 0 or 1, or a plant-tolerated acid addition salt or metal salt complex thereof which possesses fungicidal activity.

Abstract: 3-Aralkyloxy-2,3-dihydro-2-(triazolylmethyl)benzo(b)thiophenes and related derivatives having antifungal, antibacterial, and antiprotozoal activity are prepared by the reaction of the corresponding 2,3-dihydro-3-hydroxy-2-(triazolylmethyl)benzo(b)thiophene or related derivative and an aralkyl halide.Preferred compounds are those where the aralkyl function is a hetercyclic aromatic, particularly 2-chloro-3-thenyl, and where the benzene nucleus is substituted by chlorine or fluorine.Pharmaceutical formulations comprising compounds of this invention are described, as well as the method for their use in treating microbial infections.

Abstract: The present invention relates to new 6-substituted 6H-dibenzo [b,d]pyran derivatives, to a process for their preparation and pharmaceutical and veterinary compositions containing them.

Abstract: A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and an acid addition salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.

Abstract: There are disclosed piperidinio, piperazino and homopiperazino derivatives wherein there is N-substitution by a heterocyclic compound taken from the group benzimidazole, indole, purine or benzotriazole and to the organic or mineral acid addition salts of these derivatives. The process for preparation of such compounds and their use is also disclosed.

Abstract: A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and a salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.

Abstract: Novel heterocyclic derivatives of [4-(piperazin-1-yl-phenoxymethyl)-1,3-dioxolan-2-ylmethyl]-1H-imidazoles and 1H-1,2,4-triazoles, useful as antifungal and antibacterial agents.

Abstract: Physiologically-acceptable 3-aminosydnonimines of the formula ##STR1## and their pharmacologically-acceptable acid-addition salts, when formulated into medicament dosage forms, are useful for reducing systemic blood pressure, pulmonary artery pressure and left ventricular end diastolic pressure when orally administered to patients in need of such pressure reduction. These compounds are prepared by cyclizing a compound which, in its free-base state, is of the formula ##STR2## to a corresponding product which, in its free-base state, is of the formula ##STR3## and, when R.sup.2 is other than -H, acylating that product.