Abstract: Methods of making phosphite-borane compounds of the formula ##STR1## wherein: each R.sub.1 is independently selected from: H; C.sub.1 -C.sub.10 alkyl; alkylaryl; aralkyl; aryl; monovalent metal ions; nucleosides; and quaternary ammonium ions, (R.sub.4).sub.4 N.sup.+, in which the substituents R.sub.4 of the ammonium nitrogen atom are H or C.sub.1 -C.sub.10 alkyl;R.sub.2 is H or C.sub.1 -C.sub.10 alkyl; andR.sub.3 is CNCH.sub.2 CH.sub.3.sup.+ BF.sub.4.sup.-, COOH, carboxyl salts, COOR.sub.5, or CONHR.sub.5, wherein R.sub.5 is C.sub.1 -C.sub.10 alkyl, alkylaryl, aralkyl, or aryl;with the proviso that if at least one of the R.sub.1 substituents is H, nucleoside, monovalent metal ion, or quaternary ammonium ion, then R.sub.3 may also be CN,via synthetic routes comprising hydrolysis. The phosphorous-boron adducts of the invention are bioactive in character, variously exhibiting anti-tumor, anti-inflammatory, and hypolipidemic activity.

Abstract: Process for the production of 5,6-dihydroxyindolines by ether cleavage of corresponding ether procursors with aqueous hydrogen bromide and subsequent direct crystallization from the aqueous reaction mixture.

Abstract: An isoxazole derivative represented by the general formula (1) or a salt thereof: ##STR1## a method for preparing the same; compositions for inhibiting lipoxygenase and cyclooxygenase comprising an effective amount of the derivative and a pharmaceutically acceptable carrier therefor; and a method for inhibiting lipoxygenase and cyclooxygenase which comprises administering to a patient the derivative.

Abstract: The invention relates to a novel process for the preparation of compounds of formula I ##STR1## wherein R is straight-chain C.sub.2 -C.sub.4 alk-1-en-1-yl, and salts thereof, and to a novel starting material and the use thereof.

Abstract: Compounds of the formula: ##STR1## wherein the substituents are as defined herein, and enantiomers, diastereomers, racemates and salts with pharmaceutically acceptable bases, antagonize LTD.sub.4 action and thus, are useful in treating bronchial asthma, pulmonary anaphylaxis, cystic fibrosis, chronic bronchitis, bronchiectasis, respiratory distress syndrome and pulmonary oedema.

Abstract: Compositions useful in methods of disinfecting contain azoic compounds of the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different and each represents an atom of hydrogen or an aliphatic or aromatic hydrocarbon radical comprising from 1 to 6 carbon atoms; X.sup.1 and X.sup.2 are identical or different and each represents an oxygen atom or an NR.sup.5 group, wherein R.sup.5 is a hydrogen atom, an aliphatic or aromatic hydrocarbon radical comprising from 1 to 6 carbon atoms, or a nitro group; and wherein when two NR.sup.5 groups are simultaneously present each R.sup.5 may be identical to or different from the other. Compositions containing the azoic compounds in a liquid medium at concentrations of from 35 .mu.gr/ml to 2 mgr/ml are sufficient to impede replication and proliferation of viruses of the retrovirus group yet they are insufficiently toxic to destroy sound human or animal cells which come in contact with the compositions.

Abstract: The invention relates to fungicidal compositions which comprise a carrier and, as active ingredient, an indole derivative of the formula ##STR1## in which R is a substituted phenyl group; R.sup.3 and R.sup.4 independently are hydrogen or halogen or an optionally substituted alkyl, alkoxy, cycloalkyl, phenyl or phenoxy group; R.sup.5 and R.sup.6 independently are hydrogen atom or an optionally substituted alkyl, alkoxy, cycloalkyl, phenyl or heterocyclyl group or R.sup.5 and R.sup.6 together with the interjacent nitrogen atom represent a heterocyclyl group; and R.sup.7 is hydrogen or alkyl group; and their use as fungicides. Certain of the above mentioned indole derivatives are novel and a process for the preparation of these compounds is also provided.

Abstract: An improved process for the preparation of trans-6-[2-(substituted-pyrrole-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where .alpha.-metalated N,N-disubstituted acetamide is converted in seven operations to the desired products, and specifically, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl) -N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyr role-3-carboxamide, as well as other valuable intermediates used in the processes and prodrugs which are bioconverted to hypolipidemic and hypocholesterolemic agents and pharmaceutical compositions of the same.

Abstract: The present invention provides novel benzamides and sulfonamides, formulations thereof, and intermediates thereto. The benzamides and sulfonamides of the present invention are useful as hypoglycemic agents and, accordingly, a method of using such compounds to lower a mammal's blood glucose level is also provided.

Abstract: The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.

Abstract: Crystalline 4-(di-n-propyl)amino-6-aminocarbonyl-1,3,4,5-tetrahydrobenz[cd]indole hippurate and its method of preparation and use are provided.

Abstract: The compound, 3,3-dinitroazetidine, and a process of preparing 3,3-dinitroazetidine including reacting a mixture of 1-tertiary-butyl-3,3-dinitroazetidine and benzyl chloroformate to form 1-(benzyloxycarbonyl)-3,3-dinitroazetidine, reacting the 1-(benzyloxycarbonyl)-3,3-dinitroazetidine and trifluoromethanesulfonic acid to form 3,3-dinitroazetidinium trifluoromethanesulfonate, and neutralizing the 3,3-dinitroazetidinium trifluoromethanesulfonate with a base to form 3,3-dinitroazetidine are provided. Salts of the 3,3-dinitroazetidine and preparation of such salts are also disclosed.

Abstract: The invention provides a method of purifying 2-alkyl-4-halo-5-formylimidazoles, which comprises dissolving an 2-alkyl-4-halo-5-formylimidazole in an aqueous solution of a sulfonating agent, adjusting the solution to pH 1-6, and removing the impurity 2-alkyl-4,5-dihaloimidazole by filtration or extraction.

Abstract: The present invention provides novel antitumor agents which are hybrid molecules consisting of a cyclic enediyne unit attached to a DNA-binding unit via a linker unit, and having the general formula (I)D--(OCH.sub.2).sub.m --O--(CH.sub.2).sub.n --Ar--Y--CONH--B(I)wherein D is a cyclic enediyne; B is a residue capable of binding to the minor groove of DNA; n is 0 and m is 1, is or n is 1 and m is 0 or 1; Ar is an aromatic residue selected from the group consisting of phenyl, naphthyl, pyridyl, quinolinyl and indolyl; and Y is a direct bond, --CH.sub.2 -- or --CH.dbd.CH--; or a pharmaceutically acceptable salt thereof.

Abstract: A process is disclosed for the preparation of .sup.1 H-pyrazo [1,5-b][1,2,4]triazole magenta couplers represented by formula (I): ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 each independently represents a hydrogen or a substituted or unsubstituted alkyl group, provided that R.sup.1 and R.sup.2 are not simultaneously a hydrogen atom; R.sup.6 represents a substituted alkyl, aryl, alkoxy, aryloxy or other organic functional group; L represents a substituted or unsubstituted alkylene; m is an integer greater than zero; n, y, and z each represents an integer of zero to five; and X is a coupling off group.The process comprises employing a nitrile compound of formula (II): ##STR2## as an intermediate to obtain the compounds of formula (I).

Abstract: Compounds of the formula ##STR1## wherein D is the residue of a metal-free azo dye free of fiber-reactive groups and containing 2 to 4 sulfo groups,D' is the residue of a metal-free azo dye free of fiber-reactive groups and containing 2 to 4 sulfo groups, with the proviso that D and D' are different,each R.sub.1 is independently hydrogen or C.sub.1-4 alkyl,each of R.sub.2 and R.sub.3 is independently hydrogen, C.sub.1-4 -alkyl or 2-, 3- or 4-hydroxy(C.sub.2-4 alkyl),X is linear or branched C.sub.2-10 alkylene or linear or branched C.sub.3-10 alkylene monosubstituted or disubstituted by hydroxy which optionally contains one or two radicals selected from --O-- and --NRa--, wherein Ra is hydrogen or C.sub.

Abstract: Two types of structural analogues of D-myo-inositol 1,4,5-trisphosphate [Ins(1,4,5)P.sub.4 ] are prepared by a chemo-enzymatic route. These 6-O-substituted analogues retain the biological activity of Ins(1,4,5)P.sub.3 and are able to elicit Ca.sup.2+ release from porcine brain microsomes. Moreover, these analogues allow the preparation of Ins(1,4,5)P.sub.3 -based immunogens and affinity matrix which are successfully applied to the preparation and purification of antibodies against Ins(1,4,5)P.sub.3. These antibodies display discriminative affinity toward Ins(1,4,5)P.sub.3, and provide a useful tool to study intracellular Ca.sup.2+ mobilization.

Abstract: Copolymerizable oxime ethers of the general formula ##STR1## where A is a divalent linking member, R.sup.1 and R.sup.2 independently of one another are each C.sub.1 -C.sub.10 -alkyl, C.sub.1 -C.sub.10 -alkoxy, C.sub.5 -C.sub.10 -cycloalkyl or C.sub.5 -C.sub.10 -aryl, each of which may furthermore contain 1-3 nonadjacent nitrogen, oxygen or sulfur atoms as heteroatoms in the carbon chain or in the carbon ring and may be substituted by from one to three C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy groups, R.sup.1 or R.sup.2 may be hydrogen or R.sup.1 and R.sup.2 together form a bridge of 3 to 14 carbon atoms, where some of the carbon atoms may furthermore be part of an aromatic ring, Z is an n-valent organic radical which contains a copolymerizable ethylenically unsaturated group and n is an integer of from 1 to 3.

Abstract: Disclosed are fluorobenzene derivatives, which are important intermediates for producing herbicidal oxazolidinedione derivatives, and methods of producing them. The fluorobenzene derivatives include compounds of a formula (11): ##STR1## where X is a halogen atom, R.sup.3 is a nitro, amino or isocyanato group or R.sup.1 OCONH, and R.sup.1 is an alkyl or phenyl group. Via the intermediates of the invention, oxazolidinedione derivatives can be produced with high yield.

Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.