Abstract: Compounds characterized generally as benzo-fused oxazopinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is a benzo-fused oxazopinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sbsb.q--C.ident.C-Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.

Abstract: Synthetic intermediates of 1-arylethyl-3-substituted piperidines.

Abstract: A class of 6-arylpyrimidines which is useful in the control of weeds is of the general formulae: ##STR1## wherein R.sup.2 is selected from hydrogen, halo, substituted or unsubstituted alkyl, haloalkyl, polyhaloalkyl, haloalkenyl, polyhaloalkenyl, haloalkynyl, polyhaloalkynyl, alkenyl, alkynyl, alkoxy, alkylthio, alkoxycarbonylalkyl, cyano, alkoxyalkyl, alkoxycarbonyl, cycloalkyl, aralkyl, alkylamino, dialkylamino, or dialkylaminocarbonyl group; R.sup.3 is an alkyl, alkenyl, alkynyl, or haloalkyl group; R.sup.5 is an alkyl, alkenyl, alkynyl, alkenynyl, or alkoxyalkyl, group; R.sup.6 is an aryl group (e.g. aromatic ring); and X is oxygen or sulfur. R.sup.2 and R.sup.3 may form a fused ring.

Abstract: The invention provides novel 2,3,6 substituted quinazolinones having the formula: ##STR1## wherein R.sup.6, R and X are as described in the specification, which have activity as angiotensin II (AII) antagonists.

Abstract: Compounds of general formula: ##STR1## are topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and related disorders such as glaucoma.

Abstract: The compounds of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl, biaryl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl-lower alkynyl, aryloxy-lower alkyl, arylthio-lower alkyl; C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, biaryl-lower alkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl or aryloxy-aryl-lower alkyl; and aryl represents carbocyclic or heterocyclic aryl; Z represents C.sub.1 -C.sub.3 -alkylene or vinylene, each unsubstituted or substituted by lower alkyl; Y represents SO.sub.2 or CO; A represents O, S, or a direct bond; B represents lower alkylene; or B represents lower alkenylene provided that A represents a direct bond; X represents oxygen or sulfur; R.sub.

Abstract: Compounds of the formula [I] and salts thereof, which are useful for treatment of liver disorders, ##STR1## wherein X is oxygen or sulfur; andA is straight C.sub.3 -C.sub.4 alkylene which can be substituted by one or more lower alkyl groups.

Abstract: The following cyclic anthranilic acid derivative, their acid addition salts or alkali salts thereof represented by a general formula [I] are useful for antirheumatic drug, autoimmune disease curing drug and metabolic bone disease curing drug. ##STR1## wherein R.sup.1 to R.sup.6 and X are as defined in claim 1.

Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.

Abstract: Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.

Abstract: Insecticidal 1,2,3,4-Tetrahydro-5-nitropyrimidine derivatives, and salts thereof, of the formula ##STR1##

Abstract: Introduction of a fluoro substituent into an aromatic ring adjacent an electron donating group is difficult producing mixed isomers and low yields of desired products.A process for the introduction of a fluoro substituent into a substantially adjacent position to an electron-donating group into an aromatic compound in high yield is disclosed.The fluoroaromatic compounds are useful as synthetic intermediates for example in the manufacture of agrochemicals, pharmaceuticals and dyestuffs.

Abstract: .alpha.-Oxoacetamides of the formula R.sup.1 C(O)C(O)NR.sup.2 R.sup.3 in which R.sup.1 is optionally substituted phenyl, 1-indolyl, 2,3-dihydro-1-indolyl, 1-benzimidazolidinonyl, 3-benzofuranyl, 3-benzothiophenyl, 3-indolyl, and 1,2-alkano-3-indolyl; R.sup.2 is selected from: ##STR1## and R.sup.3 is selected from hydrogen or lower alkyl; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.

Abstract: 5-HT.sub.3 receptor antagonist compounds of the formula ##STR1## in which Z is --O--, --S-- or --N(R.sup.2)--; R.sup.1 and R.sup.2 are independently selected from hydrogen and lower alkyl or are together --(CH.sub.2).sub.n -- wherein n is 2 to 4; and R.sup.3 is selected from ##STR2## and the pharmaceutically acceptable salts, individual isomers, compositions, and methods of use thereof.

Abstract: Antibacterial 5-alkylquinolonecarboxylic acids of the formula ##STR1## in which R.sup.3 is C.sub.1 -C.sub.4 -alkyl,R.sup.1 is optionally substituted alkyl or cycloalkyl, alkenyl, alkoxy, amino or alkylamino or optionally substituted phenyl,R.sup.2 is hydrogen or optionally substituted alkyl,R.sup.4 is a nitrogen-containing heterocyclic radical, andA is hydrogen, halogen, methyl, cyano or nitro, or forms a bridge with R.sup.1.and hydrates and salts thereof.

Abstract: This invention relates to novel tricyclic derivatives of 7-substituted-6-fluoro-1,4-dihydroquinol-4-one-3-carboxylic acids and certain esters and cation salts thereof. The compounds of this invention are substituted at the 7-position by vinyl, W--CH.dbd.CH--, CH.sub.3 C.tbd.C--, W--CH.sub.2 C.tbd.C-- or ##STR1## where W is selected from certain substituted alkyl groups. This invention also relates to antibacterial compositions containing the compounds and methods of using the compounds to treat bacterial disease.

Abstract: Disclosed is a compound represented by the formula (I) or a salt thereof: ##STR1## wherein R.sup.1 represents an aliphatic hydrocarbon, aralkyl or aryl group which may be substituted; R.sup.2 represents hydrogen, an aliphatic hydrocarbon group having one or more substituents, an aryl group which may be substituted, an amino group which may be substituted, a formyl group, a nitro group or a halogeno group; A represents a divalent hydrocarbon chain of 2 to 4 carbon atoms which may be substituted; and m represents an integer of 0 to 2, which is useful for treatment and prevention of diseases induced by abnormalities in regulation of reactions in vivo mediated through endothelin or interleukin 1, and of immune diseases and inflammatory diseases.

Abstract: Novel pyrido[2,3-f] [1,4]thiazepines and novel pyrido[3,2-b] [1,5]benzothiazepines of the formula: ##STR1## These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibronchoconstriction activity. Also described are methods of producing the novel compounds and intermediates thereof.

Abstract: Novel benzoxazine compounds of the structure ##STR1## wherein X and Y are independently selected from the group hydrogen, alkyl, alkoxyalkyl, aminoalkyl, hydroxyalkyl and hydroxyaminoalkyl, each alkyl moiety having 1 to 6 carbons, and m=1, 2 or 3, have been found suitable as hair dyes.

Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl or aryl, m and n are 0 or 1, and A is a divalent organic radical which, with (CR.sup.1 R.sup.2).sub.m NF--SO.sub.2 (CR.sup.3 R.sup.4).sub.n groups, forms a 5- to 8-membered ring, are admirably suitable fluorinating agents for fluorinating carbon atoms, especially as stereospecific fluorinating agents, when the compounds contain a chiral carbon atom and are in optically active form. The compounds of formula I are prepared by reacting the corresponding silated sulfonamides, wherein the NF group is replaced by an N-SiR.sup.7 R.sup.8 R.sup.9 group and R.sup.7, R.sup.8 R.sup.9 are each independently C.sub.1 -C.sub.12 alkyl, cyclopentyl, cyclohexyl, benzyl or phenyl, with a fluorinating agent.

Abstract: The present invention provides compounds of the general formula: ##STR1## wherein R.sub.1 is a straight-chained or branched C.sub.1 -C.sub.12 -alkyl radical which can be substituted by a phenyl, naphthyl or C.sub.3 -C.sub.7 -cycloalkyl radical, a straight-chained or branched C.sub.2 -C.sub.12 -alkenyl radical which can be substituted by a C.sub.3 -C.sub.7 -cycloalkyl, phenyl or naphthyl radical, a C.sub.3 -C.sub.7 -cycloalkyl radical or an unsubstituted or mono- or polysubstituted mono- or bicyclic aromatic radical, in which the substituents can be halogen atoms, carboxyl groups or C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -alkoxycarbonyl radicals, R.sub.2 and R.sub.3, which can be the same or different, are straight-chained, branched, saturated or unsaturated C.sub.1 -C.sub.6 -alkyl radicals or, together with the nitrogen atom to which they are attached, form a saturated or unsaturated ring which can contain further heteroatoms and can possibly be substituted by a C.sub.1 -C.sub.

Abstract: This invention relates to benzoxazine and benzoxazepine carboxamide compounds which exhibit 5-HT.sub.3 antagonist properties including CNS, anti-emetic and gastric prokinetic activity and which are void of any significant D.sub.2 receptor binding affinity. This invention also relates to pharmaceutical compositions and methods for the treatment of gastrointestinal and mental disorders using said compounds.

Abstract: This invention relates to heteroazabenzo-bicyclic substituted carboxamide compounds of the formula: ##STR1## where W is O, S or NR.sub.5 andZ is ##STR2## 3-quinuclidine, 4-quinuclidine,4-(1-azabicyclo[3.3.1]nonane),3-(9-methylazabicyclo[3.3.1]nonane),7-(3-oxo-9-methylazabicyclo[3.3.1]nonane) or4-[3-methoxy-1-(3-[4-fluorophenoxy[propyl)piperidine];which exhibit 5-HT.sub.3 antagonist properties including CNS, anti-emetic and gastric prokinetic activity. This invention further relates to pharmaceutical compositions and methods for the treatment of the above disorders.

Abstract: Fluorinated aniline derivatives of the general formula I are described ##STR1## in which R.sup.1 represents H or (CH.sub.2).sub.n -X, n is a whole number from 1 to 3, X is H, OH, NH.sub.2, CH.sub.3 CONH, CH.sub.3 SO.sub.2 NH, SO.sub.3 H or ArSO.sub.3 H, Ar is optionally substituted arylene radical, R.sup.1 is alternatively also a --(CH.sub.2).sub.3 -- group, which is bonded to the free o-position next to the N-atom, Y is H, --O--, --NH--, --S-- or a C--C single bond, R.sup.2, in the event that Y=H, is the same as or different from R.sup.1 and means one of the radicals shown for R.sup.1, and in the event that Y is a C--C single bond or --O--, --NH-- or --S--, is an alkylene group having 1 to 3 carbon atoms linked with Y, and R.sup.3 =H, alkyl having 1 to 3 carbon atoms, OCH.sub.3, CH.sub.3 CONH, CO.sub.2 H or SO.sub.3 H.

Abstract: The invention relates to chromogenic 3,1-benzoxazines of the formula ##STR1## wherein X.sup.1 denotes hydrogen, C.sub.1 -C.sub.4 -alkyl, chlorine or OY.sup.1,X.sup.2 denotes NY.sup.2 Y.sup.3,X.sup.3 denotes OY.sup.4 or NY.sup.5 Y.sup.6,R.sup.1 -R.sup.3 independently of one another denote hydrogen, C.sub.1 -C.sub.4 -alkyl, chlorine, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -mono- or -dialkylamino, orR.sup.1 together with Y.sup.2,R.sup.2 or R.sup.3 together with Y.sup.4 or Y.sup.5, orR.sup.2 and R.sup.3 simultaneously with Y.sup.5 and Y.sup.6 denote a 2 to 4-membered bridge which can contain one oxygen atom or one nitrogen atom and can carry up to 4 methyl groups, and whereinR.sup.1 and R.sup.3 simultaneously represent hydrogen only if R.sup.2 with Y.sup.4 or Y.sup.5 forms one of the abovementioned bridges,R.sup.4 denotes hydrogen, methyl or chlorine,Y.sup.1 and Y.sup.4 independently of one another denote C.sub.1 -C.sub.4 -alkyl, cyclohexyl or benzyl and Y.sup.2, Y.sup.3, Y.sup.5 and Y.sup.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: j is 0 or 1;q is 0, 1 or 2;p is 0 and r is 2 or 3, orp is 1 and r is 2;X is O, S, SO or NR where R is hydrogen, C.sub.1-6 alkyl or C.sub.1-10 carboxylic acyl;Y is NH; or O when R.sub.1 is hydrogen; either R.sub.1 is C.sub.1-6 alkoxy and one of R.sub.2, R.sub.3 and R.sub.4 is hydrogen and the other two are selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-10 carboxylic acylamino, C.sub.1-6 alkyl S(O) n wherein n is 0, 1 or 2, nitro or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or phenyl C.sub.1-4 alkyl groups any of which phenyl moieties may be substituted by one or two groups selected from halogen, CF.sub.3, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; or R.sub.1 is hydrogen and R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen, C.sub.

Abstract: Disclosed are the compound of the formula ##STR1## wherein n represents zero, 1 or 2; Ar represents a carbocyclic or heterocyclic aryl radical; R and R.sub.1 independently represent hydrogen, lower alkyl or Ar-lower alkyl; R.sub.2 and R.sub.3 independently represent hydrogen, lower alkyl, halogen, trifluoromethyl or lower alkoxy; or R.sub.2 and R.sub.3 together on adjacent carbon atoms represent lower alkylenedioxy; R.sub.4 represents hydroxy or NR.sub.5 R.sub.6 wherein R.sub.5 and R.sub.6 independently represent hydrogen, lower alkyl or AR-lower alkyl,; or R.sub.5 and R.sub.6 together with the nitrogen to which they are attached represent pyrrolidino or piperidino; pharmaceutically acceptable salts thereof; lower alkyl enol ethers and lower alkanoyl enol esters of compounds of formual I wherein R.sub.4 represents hydroxy; as e.g. antiinflammatory agents; methods for preparing said compounds and pharmaceutical compositions comprising said compounds.

Abstract: A new series of 1,5-benzothiazepine analogues are disclosed. These compounds are represented by the following general formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each represent hydrogen, a lower alkyl, nitro, amino, lower-alkyl-oxy or halogen group, X represents O or S. These compounds are useful as anti-hypertensive agents.

Abstract: The invention relates to new benzodisultams of the general formula (I) ##STR1## in which R.sup.1 represents an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aralkyl and aryl,R.sup.2 represents hydrogen or an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl and aralkyl, andR.sup.3 represents an optionally substituted and/or optionally fused six-membered aromatic heterocyclic radical which contains at least one nitrogen atom,a process for their preparation and their use as herbicides.

Abstract: Herbicidal sulfonamides are useful as general or selective herbicides, both pre-emergence and post-emergence.

Abstract: Herbicidally active novel benzodisultams of the formula ##STR1## in which R.sup.1 represents an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aralkyl and aryl,R.sup.2 represents hydrogen, fluorine, chlorine, bromine, hydroxyl, cyclopropyl, C.sub.1 -C.sub.4 -alkyl (which is optionally substituted by fluorine and/or chlorine), C.sub.1 -C.sub.4 -alkoxy [which is optionally substituted by fluorine and/or chlorine], C.sub.1 -C.sub.4 -alkylthio (which is optionally substituted by fluorine and/or chlorine), amino, or C.sub.1 -C.sub.4 -alkyl- or di-(C.sub.1 -C.sub.4 -alkyl)-amino (which is optionally substituted by fluorine) andR.sup.3 represents hydrogen, fluorine, chlorine, bromine, hydroxyl, cyclopropyl, C.sub.1 -C.sub.4 -alkyl (which is optionally substituted by fluorine and/or chlorine), C.sub.1 -C.sub.4 -alkoxy (which is optionally substituted by fluorine and/or chlorine), C.sub.1 -C.sub.

Abstract: This invention is directed to compounds of the formula ##STR1## wherein X is a thiazine or thiazepine of the formula ##STR2## These compounds possess angiotensin converting enzyme inhibition activity and are thus useful as hypotensive agents.

Abstract: 5-alkyl-1-phenyl-2-piperazinoalkylpyrazolin-3-one compounds of the Formula ##STR1## in which R.sub.1 is a straight-chain, branched or cyclic alkyl group with up to 6 carbon atoms, Z is an alkylene chain with 2 to 4 carbon atoms, and 1-phenyl substituent is an optionally substituted phenyl ring, and R.sub.4 is a phenyl or pyridyl group which is optionally substituted and their preparation are described. The compounds have pharmacological, particularly antiallergic, properties.

Abstract: Compounds of formula ##STR1## wherein X is S or SO.sub.2, R.sub.4 is aryl or hetero, and R.sub.1 is hydrogen or ##STR2## are disclosed. These compounds are useful as cardiovascular agents and especially as anti-hypertensive agents.