Abstract: A novel class of cationic phospholipids and novel method for their synthesis are disclosed. The class of phospholipids comprises phosphotriester derivatives of phosphoglycerides and sphingolipids. It has been unexpectedly found that liposomes comprising one or more of these cationic phospholipids are effective in the lipofection of nucleic acids. These novel phospholipids are particularly attractive because of they are not only effective in lipofection, but are extremely cheap and easy to make.

Abstract: This invention relates to 3-aryl-2-isoxazoline compounds which are selective inhibitors of phosphodiesterase type IV (PDE.sub.IV). The 3-aryl-2-isoxazolines are useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease, psoriasis, allergic rhinitis, dermatitis, shock, atopic dermatitis, rheumatoid arthritis and osteoarthritis. This invention also relates to pharmaceutical compositions useful therefor.

Abstract: A class of novel 1-indole-3-acetamides represented by the formula; ##STR1## is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids.

Abstract: The invention relates to new anellated (oxa) hydantoins, and herbicidal compositions containing same. The invention also relates to methods for controlling noxious plants using the anellated (oxa) hydantoins of the invention.

Abstract: The invention relates to new substituted benzimidazoles of the general formula (I) ##STR1## in which R.sup.1 represents hydrogen, alkyl, alkoxy or optionally substituted aryl,R.sup.2 represents hydroxyl, cyano or in each case optionally substituted alkyl, alkenyl, alkinyl, alkoxy, alkenyloxy, alkinyloxy, alkylthio, amino, aminocarbonyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonyloxy, dialkoxyphosphonyl, (hetero)aryl, (hetero)arylcarbonyl, (hetero)aryloxycarbonyl, (hetero)arylcarbonyloxy or (hetero)arylaminocarbonylaminocarbonyloxy, andR.sup.3 represents fluoroalkyl,X.sup.1, X.sup.2, X.sup.3 and X.sup.

Abstract: A class of novel 1H-indole-1-functional compounds is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock. The compounds are 1H-indole-1-acetamides, 1H-indole-1-acetic acid hydrazides, and 1H-indole-1-glyoxylamides.

Abstract: The invention relates to new 1H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A, B, X, Y and G have the meanings given in the description, to a plurality of processes for their preparation, and to their use as pesticides.

Abstract: Compounds of Formula I are disclosed which are useful for controlling undesired vegetation ##STR1## wherein Q is ##STR2## and W, R.sup.A.sub.m, R.sup.4 -R.sup.8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I.

Abstract: The bisphosphonates of formula (III)R.sub.2 --X--(CW).sub.m1 --CR.sub.3 R.sub.4 --CH.sub.2 --CM[PO--(OR.sub.1).sub.2 ].sub.2 (III)bicyclic bisphosphonates (V), and cyclic bisphosphonates (VII) are useful as antiarthritic agents and do not have the side effects of anti-arthritic agents which are prostaglandin synthetase inhibitors.

Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; .multidot..multidot..multidot..multidot..multidot. represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.

Abstract: Compounds of the formula ##STR1## in which the variables are as defined in the claims and which are suitable diazo components for the synthesis of fibre-reactive dyes are described.

Abstract: .alpha.-Phosphonosulfonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is H, alkyl, arylalkyl or aryl; R.sup.4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.

Abstract: Compounds useful in the treatment of inflammation structurally represented as Formula I ##STR1## one of X or Y is H and the other is selected from the group consisting of: ##STR2## or X and Y are taken together to form a ring selected from the group consisting of: ##STR3## as herein defined. The compounds are useful as anti-inflammatory and anti-arthritic agents.

Abstract: This invention relates to a class of novel phosphonate derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis aryl cycloalkylamino and azacycloalkyl phosphonates. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

Abstract: Novel tethered hapten intermediates and related conjugates based on carbazole and/or dibenzofuran, as well as methods for making and using such conjugates. Haptens based on the above core structures may be substituted at any position on the aromatic rings with a wide variety of substituents. Using tethered intermediates, immunogens, tracers, solid supports and labeled oligonucleotides are all described; as are methods for using the intermediates to prepare the conjugates, methods of using the conjugates to make and purify antibodies, as assay tracers, and in nucleic acid hybridization assays. Kits containing haptenated oligonucleotides and anti-hapten conjugates are also described.

Abstract: A method for assaying nucleic acids or similar compounds comprises binding a sample such as a nucleic acid to phosphatase; reacting the phosphatase with a 3-hydroxy-2-naphthoic acid-2'-phenyl anilide phosphate; irradiating the reaction product with an excited light; and detecting fluorescence emitted therefrom.

Abstract: A phenylalkyl derivative of the formula ##STR1## wherein R.sub.a to R.sub.f, A and B are substituents and n is the number 0 or 1.These phenylalkyl derivatives possess angiotensin antagonist activity.

Abstract: This invention relates to antimicrobial compounds of formula I, II, or III ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, or (C.sub.1 -C.sub.4)alkyl;R.sub.1 and R.sub.2 may be taken together with the carbons to which they are attached to form a 5 to 7-membered carbocyclic ring and the ring may be aromatic;R.sub.3 is hydrogen, (C.sub.1 -C.sub.8)alkyl, (C.sub.2 -C.sub.8)alkenyl, (C.sub.5 -C.sub.8)alkynyl, (C.sub.5 -C.sub.7)cycloalkyl or cycloalkenyl, phenyl or substituted phenyl, (C.sub.7 -C.sub.10)aralkyl or substituted (C.sub.7 -C.sub.10)aralkyl, or a 5 to 8-membered heteroaryl having one or more heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen;R.sub.4 is an electron-withdrawing group selected from CN, NO.sub.2, P(O)(OR.sub.7).sub.2, P(S)(OR.sub.7).sub.2, COOR.sub.6, COR.sub.6, CONHR.sub.6, SOR.sub.6, SO.sub.2 R.sub.6, where R.sub.6 is hydrogen, (C.sub.1 -C.sub.8)alkyl, phenyl or substituted phenyl, (C.sub.7 -C.sub.

Abstract: The pharmaceutically active bicyclic heterocyclic amines (XXX) ##STR1## where W.sub.1 is --N.dbd. or --CH.dbd.; W.sub.3 is --N.dbd. or --CH.dbd.; W.sub.5 is --N.dbd. or --CR.sub.5 -- with the proviso that W.sub.5 is --CR.sub.5 -- when both W.sub.1 and W.sub.3 are --N.dbd. which are useful as pharmaceuticals in treating mild and/or moderate to severe head injury, subarachnoid hemorrhage and subsequent ischemic stroke, asthma and reduction of mucous formation/secretion in the lung and other diseases and injuries.

Abstract: Intermediates of structural formula ##STR1## can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.

Abstract: Methods for detecting nucleic acids in a sample, using naphthol derivative phosphates, are provided. Nucleic acids present in a sample are contacted with phosphatase, producing a modified phosphatase. A naphthol derivative phosphate is contacted with the modified phosphatase to produce a reaction product. Any reaction product formed is detected by irradiating it with an excited light and detecting a fluorescence emitted from the reaction product. Naphthol derivative phosphates useful in these methods are also provided. Methods for production of naphthol derivative phosphates are also provided.

Abstract: The invention provides a phosphonic diester derivative of the formula: ##STR1## wherein the variables are as defined in the specification. The derivative of the invention has excellent hypolipidemic and hypoglycemic activities and little side effects and hence is useful as therapeutic and prophylactic agents for hyperlipidemic diseases and diabetes and as a therapeutic agent for cataract.

Abstract: Compounds of formula (I) ##STR1## in which A is (CH.sub.2).sub.n in which n is 1-10, preferably 3 or 5, and R is the acyl group from a known anti-inflammatory agent, exhibit high anti-inflammatory activity. The mechanism of action is novel because they do not release the anti-inflammatory agent in the body but exhibit an activity superior to the activity of the known anti-inflammatory agent. The compounds are also active in combating bone calcium loss.

Abstract: A new method for the treatment of ischemia conditions and arrhythmia is disclosed. The method uses compounds of the formula ##STR1## wherein A can be --CH.sub.2 --, --O--, --NR.sub.9 --, --S--, --SO--, --SO.sub.2 --; X can be oxygen or sulfur; Y can be --NR.sub.8, --O--, --S--, --CH.sub.2 -- and the R groups are as defined herein. Novel compounds within the definition of formula I are also disclosed.

Abstract: Intermediates of structural formula ##STR1## can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.

Abstract: This invention relates to substituted aryl indazoles, a process for producing them and their use as herbicides. In particular this invention relates to substituted aryl indazoles of the formula ##STR1## wherein all variables are as defined in the specification.

Abstract: The heterocyclic iminobismethylenebisphosphonic acid derivatives of the general formula (I) ##STR1## wherein n is an integer of 0-5 and the group of the formula ##STR2## represents a 4-7 membered monocyclic or 7-11 membered condensed heterocyclic ring group which may be substituted by a halogen atom or a lower alkyl group and contains 1-2 nitrogen atoms their esters and salts thereof are described. The said compounds are useful as a bone resorption inhibitor, a dental calculus formation inhibitory agent or a polyvalent metal ion complex salt forming agent.

Abstract: This invention relates to a class of novel phosphonate derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis aryl cycloalkylamino and azacycloalkyl phosphonates. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

Abstract: Triggerable dioxetanes with a fluorescent molecule containing group bonded or tethered in the dioxetane so as to produce fluorescence from the group are described. The compounds are useful in immunoassays and in probes using enzymes or other chemicals for triggering the dioxetanes to produce light from the fluorescent molecule in the group as a signal.

Abstract: Hypotensive activity is exhibited by new phosphonate substituted amino or imino acids of the formula ##STR1## isomeric mixtures thereof and pharmaceutically acceptable salts thereof, wherein:X is an imino or amino acid of the formula ##STR2##

Abstract: The present invention relates to novel aminophosphonate derivatives substituted in .alpha. position by phenol groups, of formula (I): ##STR1## in which: X.sup.1, X.sup.2, X.sup.3, R.sup.1, R.sup.2, A, B, Z and n are defined in claim 1, as well as their preparations and the pharmaceutical compositions comprising them.

Abstract: The bisphosphonates of formula (III)R.sub.2 --X--(CW).sub.m1 --CR.sub.3 R.sub.4 --CH.sub.2 --CM[PO--(OR.sub.1).sub.2 ].sub.2 (III)bicyclic bisphosphonates (V), and cyclic bisphosphonates (VII) are useful as anti-arthritic agents and do not have the side effects of anti-arthritic agents which are prostaglandin synthetase inhibitors.

Abstract: The invention provides a phosphonic diester derivative of the general formula ##STR1## The phosphonic diester derivative of the invention has hypoglycemic and hypolipidemic activities, for instance, and is of value as an antidiabetic or anti-hyperlipidemic agent.

Abstract: Rhizoxin and rhizoxin-2-ene derivatives of formula ##STR1## in which: n is 1 to 25; A is an extra bond or oxygen, X is oxygen, sulfur, nitrogen or carbonyl; and R is hydrogen, carboxylic acyl having from 1 to 25 carbon atoms, alkoxycarbonyl group having from 2 to 26 carbon atoms, phosphono, alkylphosphono group in which the alkyl part has from 1 to 25 carbon atoms, dialkylphosphono group in which each alkyl part has from 1 to 25 carbon atoms, alkyl group having from 1 to 25 carbon atoms, aralkyl, cycloalkyl, heterocyclic, alkylthio group in which the alkyl part has from 1 to 25 carbon atoms, aralkylthio, or heterocyclylthio, or when X represents a nitrogen atom, R is R.sup.1 and R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, acyl, alkoxycarbonyl, phosphono, alkylphosphono or dialkylphosphono, have valuable anti-tumor activity. They may be prepared by acylation of rhizoxin or rhizoxin-2-ene.

Abstract: Compounds of general formula I: ##STR1## wherein: each of R.sup.1 -R.sup.8, k, and V represent disclosed functional groups that have been chosen such that all disclosed variations of compound I and their pharmaceutically and veterinarily acceptable acid addition salts and hydrates are antagonists of platelet activating factor (PAF) and as such are useful in the treatment or amelioration of various diseases or disorders mediated by PAF.

Abstract: 4-R.sup.4 -R.sup.5 -Saccharinylmethyl aryl carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an arylcarboxylic acid in the presence of an acid-acceptor.

Abstract: A derivative of tryptophan is provided wherein the NH-group of the tryptophan indole nucleus is protected with tert.-butyloxycarbonyl (BOC) and the .alpha.-amino group is protected by 9-fluorenyl-methyloxy-carbonyl (FMOC). The carboxylic acid group of the tryptophan derivative may comprise a free COOH group, may be modified with a protecting or activating group, or may comprise an acyl group bonded to another chemical moiety, such as a polymer, another amino acid, a dipeptide, a polypeptide, or a protein. The tryptophan derivative is useful in the preparation of dipeptides, polypeptides or proteins containing at least one tryptophan-derived amino acid residue.

Abstract: An agent for inhibiting bone resorption comprising an indole derivative of the formula (I): ##STR1## wherein each ring of A and B is optionally substituted, R is a hydrogen atom, a lower alkyl group or an acyl group, and A is a hydroxymethyl group or an esterified or amidated carboxyl group; or its pharmaceutically acceptable salt and a pharmaceutically acceptable carrier, diluent or excipient.

Abstract: The invention describes tautomeric compounds of the formula Ia, Ib or Ic ##STR1## and/or their physiologically tolerable salts, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are a hydrogen atom, substituted (C.sub.1 -C.sub.7)-alkyl, (C.sub.3 -C.sub.10)-cycloalkyl, substituted phenyl or (C.sub.1 -C.sub.4)-alkylphenyl, R.sup.2 is substituted phosphoric acid, R.sup.2 and R.sup.3, R.sup.2 and R.sup.5 or R.sup.4 and R.sup.5 form a monocyclic 5- to 7-membered saturated or unsaturated heterocyclic ring which is mono- or polysubstituted, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 are a hydrogen atom or (C.sub.1 -C.sub.5)-alkyl, X is a hydrogen atom, hydroxyl or halogen, l and n are an integer from 0 to 7, m is an integer from 0 to 2, and the sum of the numbers l, m and n is less than or equal to 10, a process for the preparation of the compounds of the formula Ia, Ib or Ic, pharmaceuticals and their use for the prophylaxis or treatment of osteoporosis.

Abstract: Imidazoles of the formula ##STR1## are prepared by treating a ketone ##STR2## with a nitrogenic acid, nitrite or nitrate in the presence of an acid to form a hydroxynitrile ##STR3## which is treated with R.sup.2 --CHO and an ammonium to form an N-hydroxyimidazole ##STR4## which is reduced in the presence of a buffer. In these compounds, R.sup.1 is hydrogen, alkyl, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl;R.sup.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, cycloalkylalkenyl, cycloalkylalkynyl, or --(CH.sub.2).sub.m Z(CH.sub.2).sub.n R.sup.3, each of which is optionally substituted with F or --CO.sub.2 R.sup.1 ; or aryl or aralkyl, each of which is optionally substituted with 1 or 2 groups selected from halogen, lower alkoxy, lower alkyl, or nitro;R.sup.3 is hydrogen, alkyl, cycloalkyl, lower alkenyl, or lower alkynyl;and the remaining symbols are as defined in the specification.

Abstract: A compound of the formula (I): ##STR1## wherein W is a group of the formula:A--O--(CH.sub.2 .sub.n --wherein A is a cyclic group which may be substituted, n is an of 2 to 10, or W is a group of the formula:R.sup.1 --X--(CH.sub.2).sub.n' --wherein R.sup.1 is an alkyl group which may be substituted, X is an oxygen atom or a sulfur atom which may be oxidized, n' is an integer of 4 to 10; R.sup.2 is a hydrogen atom or a lower alkanoyl group; R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different and are a hydrogen atom or a lower alkyl group, or a salt thereof, is useful as a bone resorption inhibitor.

Abstract: Indazole arthropodicides, compositions containing them and a method for controlling arthropods employing these indazoles as the active ingredient. The indazoles have the following general formula wherein Q, X, Y, R.sub.

Abstract: A phosphorylating agent represented by the following general formula [1]: ##STR1## wherein R represents a protective group of the phosphoric acid; and X represents a heterocyclic residue represented by the following general formula [2]: ##STR2## wherein Y represents a single bond or an oxygen or sulfur atom; Z represents a heterocyclic nucleus comprising at least one nitrogen atom as a ring-forming element and may be condensed with another aromatic ring; and W represents one or more substituents other than a hydrogen atom. The phosphorylating agent is stable, can rapidly proceed phosphodiester bond-forming reactions in good selectivity under mild conditions and thus makes it possible to perform a reaction even in a relatively large scale.

Abstract: Substituted imidazoles such as ##STR1## which are useful as angiotensin II receptor inhibitors. These compounds have activity in treating hypertension and congestive heart failure.

Abstract: Processes for the preparation of biotinylated polynucleotides and analogues thereof and protected intermediate products for use in such processes are described and claimed. The processes may be conveniently used in the automated synthesis of biotinylated polynucleotide on a DNA synthesizer. The polynucleotides so prepared may be used as labelled probes e.g. as diagnostic tools for clinical and research uses.

Abstract: Phosphine oxide-terminated allene-ene-yne compounds are disclosed that possess DNA-cleaving, antimicobial and tumor growth-inhibiting properties. Methods of making and using those compounds are also disclosed.

Abstract: The present invention is directed to a fluorescence polarization method for monitoring fetal lung maturity, to various components needed for preparing and carrying out such monitoring, and to methods of making these components.

Abstract: A class of diacid-containing benzimidazole compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## wherein Y.sub.m is --CH.sub.2 -- or --CH.sub.2 --CH.sub.2 --; wherein m is one; wherein X is one or more groups attachable at one or more of the 4-, 5-, 6- and 7-ring positions not occupied by the phosphonoalkyl moiety; wherein each X is independently selected from hydrido, halo, alkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, alkenyl, alkynyl, phenyl, benzyl, hydroxy, hydroxyalkyl, alkoxy, phenoxy, alkoxyalkyl, benzyloxy, cyano, alkanoyl, alkylthio, arylthio and amino; wherein each of R.sup.10, R.sup.13 and R.sup.

Abstract: Chiral phosphorus-containing ligands comprising at least one amine radical and at least one dihydrocarbylphosphinoxy radical of the formula W=OP (R).sub.

Abstract: Novel compounds having the formula ##STR1## where X R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore for example, as antihypertensive agents.