Abstract: The present invention provides novel antiviral naphthoquinone compounds, which may be isolated from plants of the genus Conospermum or synthesized chemically, in accordance with the present inventive methods. The antiviral naphthoquionone compounds, derivatives thereof, and prodrugs thereof, may be used alone or in combination with other antiviral agents in compositions, such as pharmaceutical compositions, to inhibit the growth or replication of a virus, such as a retrovirus, in particular a human immunodeficiency virus, specifically HIV-1 or HIV-2, in the treatment or prevention of viral infection.

Abstract: Azatoxin and derivatives thereof are illustrative of a new class of antitumor drugs that are topoisomerase II (top 2) inhibitors. The pharmacophore inhibits the catalytic activity of the purified enzyme but does not unwind relaxed or supercoiled DNA. It is nonintercalative and has at least two domains: a quasi-planar polycyclic ring system, which may bind between DNA base pairs, and a pendant substituent thought to interact with the enzyme, with the DNA grooves or with both. In SV40 and c-myc DNA, azatoxin induces numerous double-strand breaks according to a cleavage pattern which differs from those of known top 2 inhibitors. Azatoxin also is a potent inhibitor of tubulin polymerization.

Abstract: The present invention relates to a group of organic chelators whose affinity for calcium ion in solution is decreased by electromagnetic radiation. Specifically, the chelators are related to fura-2 and utilize the addition of an azide group to the 3-position of the benzofuron ring of a fura-2 type structure. Photolysis of the azide group causes the calcium ion affinity to decrease 100 to 1000 fold. These chelators when incorporated into rat fibroblasts either by microinjection or by incubation as the membrane-permeable, enzymatically-labile esters and flash-photolyzed cause large increases in intracellular free calcium ion. These chelators are used to generate controlled fast elevation of intracellular free calcium ion concentration to mimic or modulate a number of important cellular responses, especially in nerve or muscle.

Abstract: Novel aminediol compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds in inhibiting retroviral protease, particularly useful in the treatment and/or prevention of HIV infection (AIDS).

Abstract: A solids-free, essentially all-oil wellbore fluid comprises (a) an organic fluid having (i) a melting point less than about 20.degree. C. (about 68.degree. F.), (ii) a flash point greater than about 54.4.degree. C. (about 130.degree. F.), and (iii) a dipole moment greater than 0 debye (D), and (b) a salt dissolved in the organic fluid. The wellbore fluid is employed in well drilling, completion, and work-over operations.

Abstract: Novel substituted 2,4-imidazolidinediones are prepared either by reaction of .alpha.-aminocarboxylic acid derivatives with appropriately substituted biphenylmethyl halides and subsequent cyclization with isocyanates or by reaction of N-benzyl-substituted .alpha.-aminocarboxylic acid derivatives with tetrazolylphenylboronic acids or by reaction of sulphonyl-substituted benzyl halides with .alpha.-aminocarboxylic acid derivatives and subsequent cyclization with isocyanates. The compounds according to the invention can be employed as active compounds in medicaments, preferably for the treatment of arterial hypertension and arteriosclerosis.

Abstract: New D-homo-(16-ene)-11.beta.-aryl-4-estrenes of general formula I ##STR1## as well as their pharmaceutically compatible addition salts with acids are described in whichX stands for an oxygen atom, the hydroxyimino grouping >N.about.OH or two hydrogen atoms,R.sup.1 stands for a hydrogen atom or a methyl group,R.sup.2 stands for an hydroxy group, a C.sub.1 -C.sub.10 alkoxy or C.sub.1 -C.sub.10 acyloxy group,R.sup.11 stands for a fluorine, chlorine or bromine atom, and then R.sup.12 and R.sup.13 together mean an additional bond orR.sup.11 stands for a straight-chain or branched-chain C.sub.1 -C.sub.4 -alkyl radical or a hydrogen atom, and then R.sup.12 and R.sup.13 each mean a hydrogen atom or together mean an additional bond,and R.sup.3 and R.sup.4 have the usual meanings indicated in the description for competitive progesterone antagonists.

Abstract: The present invention relates to new bisquinolines useful in the treatment of malaria and to processes for the production thereof. The invention also relates to methods for the treatment of malaria and, in particular, to the treatment of chloroquine-resistant strains of malaria. The compounds of the invention have the following formula: ##STR1## wherein R is a bivalent radical derived from an acyclic or cyclic hydrocarbon by removal of one hydrogen atom from each of two different carbon atoms. R' is hydrogen or lower alkyl (generally containing between about 1 and about 4 carbon atoms). X is hydrogen (--H), fluoro (--F), chloro (--Cl), bromo (--Br), trifluoromethyl (--CF.sub.3), cyano (--CN), or methylsulfoxide (--SOCH.sub.3). In its acyclic form, R generally contains at least two, and no more than about 12, carbon atoms and, preferably, is an unsubstituted straight or branched alkane.

Abstract: Disclosed are amino substituted steroids (XI) which contain an imidazolylpiperazinyl group attached to the terminal carbon atom of the C.sub.17 -side chain which are useful as pharmaceutical agents for treating a number of conditions.

Abstract: A pharmaceutical composition useful to treating dementia which comprises a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which p is 1 and either m is 0 and n is 2 or 3 or m is 1 and n is 2, or p is 2, m is 0 and n is 2, and Z is a heterocyclic group ##STR2## in which Q represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises one or two heteroatoms selected from oxygen, nitrogen and sulphur, or three nitrogen atoms, any amino nitrogen being substituted by a C.sub.1-2 alkyl, cyclopropyl or propargyl group, and any ring carbon atom being optionally substituted by a group R.sub.1 ; or a group ##STR3## which A.sub.1, A.sub.2 and A.sub.3 complete a 5-membered aromatic ring and A.sub.1 is oxygen or sulphur, one of A.sub.2 and A.sub.3 is CR.sub.2 and the other is nitrogen or CR.sub.3, or A.sub.2 is oxygen or sulphur, one of A.sub.1 and A.sub.3 is CR.sub.2 and the other is CR.sub.3 ; and R.sub.1, R.sub.2 and R.sub.

Abstract: Disclosed are imidazonaphthyridine derivatives represented by formula (I) ##STR1## wherein: R.sup.1 represents lower alkyl or substituted or unsubstituted aryl; andX--Y--Z represents ##STR2## wherein R.sup.2 represents hydrogen, lower alkyl, alkenyl, aralkenyl, or --C (R.sup.5)H--(CH.sub.2).sub.n --R.sup.4 (wherein R.sup.4 represents substituted or unsubstituted aryl, substituted or unsubstituted pyridyl, substituted or unsubstituted furyl, hydroxy-substituted lower alkyl, lower alkanoyloxy, morpholino, lower alkanoyl, carboxy, lower alkoxycarbonyl, cycloalkyl, hydroxy, lower alkoxy, halogen or NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 independently represents hydrogen or lower alkyl; R.sup.5 represents hydrogen, lower alkyl, or phenyl; and n represents an integer of 0 to 3); and R.sup.3 represents hydrogen, mercapto, hydroxy, lower alkyl, or aryland pharmaceutically acceptable salts thereof.The compounds show a potent anti-inflammatory, anti-allergic and broncho-dilative activity.

Abstract: Pergolide is produced from 8,9-dihydroelymoclavine by a one-pot process in which it is reacted successively with 1-iodopropane, with a sulfonyl halide, and with an alkali metal thiomethoxide without isolation of intermediate products.

Abstract: SUBSTITUTED-4-FLUORO-1,4-DIAZONIABICYCLO[2.2.2]OCTANE SALTS AND THEIR APPLICATION AS FLUORINATING AGENTS The present invention relates to the preparation and uses of 1-substituted-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts, specifically 1-hydroxyl-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts as reagents for the introduction of fluorine in organic compounds.

Abstract: Novel azabicyclo amides and esters as antagonists at the 5-HT.sub.3 receptor and useful as anti-emetic agents.

Abstract: An aminoalkoxyphenyl derivative of general formula:Cy--B--Ph--O--A--Am (1)as well as a pharmaceutically acceptable salt thereof in whichB represents a --S--, --SO-- or --SO.sub.2 -- group,Ph represents an optionally substituted phenyl radical,A denotes a straight or branched alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxy propylene radical in which the hydroxy is optionally substituted by a C.sub.1 -C.sub.4 alkyl radical.Am represents a group: ##STR1## and Cy is a cyclic group, provided that when Cy represents either a benzo[b]furyl group substituted at position 4 by a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or a benzo[b]thienyl group substituted at position 4 by a halogen atom or by a C.sub.1 -C.sub.4 alkyl group and when B represents a --SO.sub.2 -- group, R.sub.3 represents a --Alk--Ar radical.

Abstract: This invention relates to compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom or an alkyl or alkoxycarbonyl radical or an unsubstituted or substituted phenyl radical,R.sub.2 represents an alkyl (1-8 C) or polyfluoroalkyl radical or an unsubstituted or substituted cycloalkyl radical,R.sub.3 represents an unsubstituted or substituted phenyl radical, a naphthyl, indolyl, quinolyl or phenylamino radical in which the phenyl ring is optionally substituted, or a quinolylamino radical, andm is 0 or 1, the process for preparing them and the medicaments containing them.

Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.

Abstract: Indane-1, 3-dione derivatives of the following general formula [I]: ##STR1## and herbicidal compositions containing them as an active ingredient are provided. The derivatives are highly valuable in exhibiting excellent herbicidal activity while causing markedly low damage on crops.

Abstract: A compound that is 3,6-Bis-(2'-methoxyphenyl)-2,5-dihydro-2, 5-dimethyl-pyrrolo-(3,4-c)-pyrrole-1,4-dione for the formula III ##STR1##

Abstract: The invention relates to a novel process for the preparation of (-) -1.beta.-ethyl-1.alpha.-(hydroxymethyl) - 1,2,3,4,6,7,12,12b.alpha.-octahydro-indolo[2,3-a]quinolizine of the formula (I) ##STR1## and to novel intermediates obtained in this process. The compound of the formula (I) prepared by the process of the invention possesses a peripheral vasodilator effect.