Abstract: Dioxetanes which couple with organic and biological molecules of the formula: ##STR1## wherein X is a leaving group which is removed by an `activating agent to produce light, wherein A is a coupling substituent, Ar is a substituent selected from the group consisting of phenyl and naphthyl to provide a label are described. R.sub.1 is an optional linker substituent and can have between 1 and 30 carbon atoms with some of the carbon atoms being oxygen, sulfur, nitrogen or phosphorus. Ar as phenyl is preferred. The dioxetane coupled molecules are useful in assays of all types where luminescence can be used as an indicator.

Abstract: Kits comprising 1,2-dioxetanes which can be cause to chemiluminesce by contact with an enzyme, and the enzyme, are provided for use in optically detectable assays. The assay calls for binding the enzyme to the substance to be detected in a sample, removing any unbound enzyme, and then combining the treated sample with the dioxetane. If the substance to be detected is present, enzyme bound thereto will cleave the protecting group of the dioxetane, causing the dioxetane to decompose and chemiluminescence. The intensity of luminescence is indicative of the concentration of the substance in the sample. The substance to be detected may be an enzyme, in which case no binding group is necessary.

Abstract: The invention relates to a steroid derivative which steroidal skeleton is bound at carbon atom 17 to a spiromethylene ring of the formula: ##STR1## wherein R.sub.a and R.sub.b are independently selected from the group consisting of hydrogen, methyl, and halogen; m is 1 or 2; and the asterisk denotes carbon atom 2 of the spiromethylene ring which is carbon atom 17 (or carbon atom 17.alpha. of a homosteroid skeleton) of the steroid. The steroids have progestational or antiprogestational activity.

Abstract: Spiroadamantyl dioxetanes bearing an alkoxy substituent, and an aromatic substituent of phenyl or naphthyl on the dioxetane ring can be activated to chemiluminesce if the aromatic substituent bears a moiety designated OX, wherein the X is cleaved by an enzyme with which the dioxetane is permitted to come in contact with. The T.sub.1/2 kinetics of the chemiluminescent reaction, as well as the signal intensity, or quantum yield of the chemiluminescent reaction, can be altered by selection of an electron-withdrawing or an electron-donating group Z, at positions on the aromatic substituent other than those adjacent the point of attachment to the dioxetane. Signal strength can further be enhanced by recognized chemiluminescent enhancers.

Abstract: A method of detecting the presence of a substance being monitored in a medium, selected from the group of substances including organophosphorus compounds and the metal ions Zn, Be and Bi, including the steps of: providing a 1,2-dioxetane phenyl phosphate compound; providing a phosphatase that catalytically degrades the 1,2-dioxetane phenyl phosphate compound to produce light, the catalytic activity of the phosphatase toward 1,2-dioxetane phenyl phosphate compound being altered by the substance being monitored; exposing the 1,2-dioxetane phenyl phosphate compound and the phosphatase together to a medium which may contain the substance being monitored; detecting light produced after the exposing step; and determining, from the detected light, the presence and concentration in the medium of the substance being monitored.

Abstract: A new class of stable dioxetanes bears a polycyclic stabilizing group and aryloxy moiety, the oxygen atom of which is provided with a protective group which can be removed by an enzymatic or chemical trigger admixed with the dioxetane. The polycyclic stabilizing group is preferably spiroadamantane. The group further bears an alkoxy, aryloxy, aralkyloxy or cycloalkyloxy moiety which is partially or completely substituted with halogens, particularly fluorine and chlorine. Proper selection of electron active groups on the stabilizing moiety, the aryl group and the OR group yields enhanced enzyme kinetics, superior light intensity and excellent detection sensitivity in various assays.

Abstract: 1, 2-dioxetane compounds bearing a proteolytic enzyme specific amino acid or peptide are provided, which amino acid or peptide can be removed by action of the corresponding protease. When the amino acid or peptide is removed, the 1,2-dioxetane decomposes with chemiluminescence, the generation of light providing a rapid, ultra-sensitive and convenient means for detecting the presence of the protease in the sample being inspected. The amount of light generated, or degree of chemiluminescence, can be correlated with the amount of protease present. Immunoassays, as well as DNA hybridization and DNA probe assays are provided.

Abstract: Novel 1,2-dioxetanes with improved chemiluminescent properties, such as signal intensity, S/N ratio, T1/2, etc. are provided by spiroadamantyl 1,2-dioxetanes, wherein the remaining carbon atom of the ring bears an alkoxy, aryloxy, or arylalkoxy substituent, and either a phenyl or naphthyl ring, this aromatic ring bearing, at the meta position on the phenyl group, or a non-conjugated position on the naphthyl ring, a OX moiety wherein X is an enzyme-cleavable group, which when removed from the dioxetane, leaves the oxyanion which decomposies with chemiluminescence, the aryl ring further bearing an electron active substituent Z. The nature and placement of the Z substituent, at a position not adjacent the point of attachment to the dioxetane ring, strongly influences the properties of the dioxetane. Assays, as well as kits for the performance of those assays, include the dioxetane, an enzyme capable of cleaving the X group, and in certain cases, membranes and chemiluminscent enhancement agents.

Abstract: Enzymatically cleavable chemiluminescent 1,2-dioxetane compounds capable of producing light energy when decomposed, substantially stable at room temperature before a bond by which an enzymatically cleavable labile substituent thereof is intentionally cleaved, are disclosed. These compounds can be represented by the formula: ##STR1## wherein: X and X.sup.1 each represent, individually, hydrogen, a hydroxyl group, a halo substituent, an unsubstituted lower alkyl group, a hydroxy (lower) alkyl group, a halo (lower) alkyl group, a phenyl group, a halophenyl group, an alkoxyphenyl group, a hydroxyalkoxy group, a cyano group or an amide group, with at least one of X and X.sup.1 being other than hydrogen; andR.sub.1 and R.sub.2, individually or together, represent an organic substituent that does not interfere with the production of light when the dioxetane compound is enzymatically cleaved and that satisfies the valence of the dioxetane compound's 4-carbon atom, with the provisos that if R.sup.1 and R.sub.

Abstract: New antibacterial agents produced by fungal culture 07F275, of which the compound designated 07F275 alpha having the following structure: ##STR1## is representative. Methods for the fermentation, recovery and purification from crude solutions are also disclosed.

Abstract: An oxaspiro ?2,5!octane derivative of the formula: ##STR1## useful in inhibiting angiogenesis in solid tumors.

Abstract: A peroxygen bleaching composition which comprises approximately by weight a mixture of about 1 to about 75% of an inorganic peroxygen bleaching compound; and about 1 to about 75% peroxygen ketalcycloalkanedione bleachant activator.

Abstract: Stable, enzymatically triggered chemiluminescent 1,2-dioxetanes with improved water solubility are provided. Dioxetanes further instituted with two or more water-solubilizing groups disposed on the dioxetane structure provide superior performance by eliminating the problem of reagent carryover when used in assays performed on capsule chemistry analytical systems. Compositions comprising a dioxetane with two or more water-solubilizing groups, a non-polymeric cationic surfactant enhancer and optionally a fluorescer, for providing enhanced chemiluminescence are also provided.

Abstract: Compounds having the formula: ##STR1## wherein T is a polycycloalkylidene group (e.g., adamant-2-ylidene); R is a C.sub.1-20 alkyl, aralkyl or cycloalkyl group; and Y is a fluorescent chromophore (eg., m-phenylene), produced by reacting a compound having the formula: ##STR2## with an R-ylating agent (e.g., R.sub.2 SO.sub.4) in the presence of an alkali metal alkoxide in a polar aprotic solvent. Also, compounds having the formula: ##STR3## are produced by reacting a compound having the formula: ##STR4## wherein X is an electronegative leaving group (e.g., a halogen anion such as chloride ion) in the presence of a Lewis base (e.g., a trialkyl-amine) dissolved in an aprotic organic solvent (e.g., benzene or toluene). Also, compounds having the formula ##STR5## are produced by reacting a compound of the formula ##STR6## with a tetra-O-acylated-O-hexopyranoside halide, then hydrolyzing off the protective acyl groups.

Abstract: A chemiluminescent assay method and compositions are described which use a haloalkoxy group-substituted dioxetane which is deprotected by a hydrolytic enzyme to undergo a chemiluminescent reaction. Chemiluminescent 1,2-dioxetane compounds substituted on the dioxetane ring with a haloalkoxy group which can be triggered by a reagent to generate light are disclosed. Haloalkoxy group-substituted dioxetanes are useful for the detection of triggering agents including enzymes. The enzyme may be present alone or linked to a member of a specific binding pair in an immunoassay, DNA probe assay or other assay where the enzyme is bound to a reporter molecule.

Abstract: Dioxetanes which couple with organic and biological molecules of the formula: ##STR1## wherein X is a leaving group which is removed by an activating agent other than an enzyme which is removed by an activating agent to produce light, wherein A is a coupling substituent, Ar is a substituent selected from the group consisting of phenyl and naphthyl to provide a label are described. R.sub.1 is an optional linker substituent and can have between 1 and 30 carbon atoms with some of the carbon atoms being oxygen, sulfur, nitrogen or phosphorus. Ar as phenyl is preferred. The dioxetane coupled molecules are useful in assays of all types where luminescence can be used as an indicator.

Abstract: Oxaspiro?2,5! octanes of the formula ##STR1## inhibit angiogenesis and are particularly suitable for the treatment of solid tumors. In preferred embodiments, R.sup.1 is a carbamoyl derivative, R.sup.2 is an alkoxy substituent and R.sup.3 is ##STR2## Pharmaceutical salts of these compounds, such as methyl, amonium and organic amine salts also exhibit desirable properties.

Abstract: Stable, enzymatically triggered chemiluminescent 1,2-dioxetanes with improved water solubility and storage stability are provided. Dioxetanes further substituted with two or more water-solubilizing groups disposed on the dioxetane structure and an additional fluorine atom or lower alkyl group provide superior performance by eliminating the problem of reagent carryover when used in assays performed on capsule chemistry analytical systems. These dioxetanes display substantially improved stability on storage. Compositions comprising these dioxetanes, a non-polymeric cationic surfactant enhancer and optionally a fluorescer, for providing enhanced chemiluminescence are also provided.

Abstract: Compounds of the formula ##STR1## which have antifungal activity.

Abstract: Novel light producing 1,2-dioxetanes are described of the formula ##STR1## wherein ArOX is an aryl ring substituted with an X oxy group and A are passive organic groups which allow the 1,2-dioxetane to produce light when triggered by removing X. X is a chemically labile group which is removed by an activating agent. The 1,2-dioxetane compounds can be triggered to produce light at room temperatures.

Abstract: O-substituted fumagillol derivatives and its salts have an angiogenesis inhibiting activity and are useful for prophylaxis and treatment of diseases induced by abnormally stimulated neovascularization.

Abstract: The invention recites a process for preparing 9,10-secocholesta-5,7,10(19)-trienes of formula (I) ##STR1## where R.sup.1 is hydrogen or a hydroxy-protecting group and R.sup.2 and R.sup.3 are independently hydrogen or OR.sup.1. The compounds are prepared from epoxides of the following formulas ##STR2## by reaction with a low-valent metal reagent formed by reducing a metal halide, M(z)X.sub.z, preferably WCl.sub.6.

Abstract: A new class of stable dioxetanes bears a polycyclic stabilizing group and aryloxy moiety, the oxygen atom of which is provided with a protective group which can be removed by an enzymatic or chemical trigger admixed with the dioxetane. The polycyclic stabilizing group is preferably spiroadamantane. The group further bears an alkoxy, aryloxy, aralkyloxy or cycloalkyloxymoiety which is partially or completely substituted with halogens, particularly fluorine and chlorine. Proper selection of electron active groups on the stabilizing moiety, the aryl group and the OR group yields enhanced enzyme kinetics, superior light intensity and excellent detection sensitivity in various assays.

Abstract: A compound of the formula ##STR1## where n, Q, and Z are as defined useful in chemiluminescent immunoassays.

Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is hydrogen or straight, branched or cyclic alkyl, aryl, hydroxy or alkoxy; and(f) R.sub.1 and R.sub.2 are independently hydrogen or straight, branched or cyclic alkyl having from one to 10 carbon atoms, aryl, heterocyclyl, heteroaryl, hydroxy, or alkoxy; or R.sub.1 and R.sub.2 are bonded together to form a ring having from from 3 to about 7 atoms wherein one to three atoms may be heteroatoms.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.

Abstract: The present invention provides new sources of taxanes and other metabolites from members of the order Coniferales that are not in the genus Taxus.

Abstract: Compounds represented by the general formula (I), as well as intermediates for the synthesis of thereof: ##STR1## where R.sup.1 is a hydrogen atom or an acyl group; R.sup.2 is a lower alkyl group; R.sup.3 is a hydrogen atom or a lower alkyl group; R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl or aryl group; R.sup.2 and R.sup.4, when taken together, may form a 5-membered ring; R.sup.5 and R.sup.6, when taken together, may form a cycloalkyl group or a heterocyclic group in which at least one methylene on the ring of a cycloalkyl group is substituted by an oxygen atom, a sulfur atom or an alkyl-substituted nitrogen atom, provided that R.sup.6 is not present if the ring formed by R.sup.2 and R.sup.4 taken together is a benzofuran ring.

Abstract: 4-(3-beta-D-galactopyranosylphenyl)-4-methoxyspiro[1,2-dioxetane-3,2'-adama ntane] which is useful in various chemiluminescent assays.

Abstract: Compounds of formula (I): ##STR1## wherein: R is selected from the radicals: ##STR2## Y is selected from ##STR3## R.sub.1 represents the radical ##STR4## and A, B, C, D, R.sub.2, R.sub.3 and R.sub.4 are as defined in the description, and also the possible geometric isomers and/or diastereoisomers and/or enantiomers thereof in pure form or in the form of a mixture. The compounds of the present invention have a therapeutic use as a result of their angiogenesis-inhibiting activity.

Abstract: (Benzylidene)-azolylmethylcycloalkane or -alkene of formula ##STR1## in which: A and A.sub.1 are hydrocarbon chains of 1 to 3 carbon atoms,R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are hydrocarbon radicals,X is halogen,Y is H or halogen,n=1, 2 or 3,W is --CH.dbd. or --N.dbd..Use as a fungicide.

Abstract: Alkene adamantane compounds useful as intermediates for producing the corresponding 1,2-dioxetanes which are useful in chemiluminescent assays.

Abstract: A compound having the formula ##STR1##

Abstract: Triggerable dioxetanes with a fluorescent substituent bonded or tethered in the dioxetane so as to produce fluorescence from the group are described. The compounds are of the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are carbon containing groups and wherein one of R.sub.1, R.sub.2 and R.sub.3 is a tethered fluorescent substitutent. 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: Novel cyclohexane-ylidene derivatives of formula (I) are described. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production. These compounds are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.

Abstract: 1,2-dioxetane compounds bearing a proteolytic enzyme specific amino acid or peptide are provided, which amino acid or peptide can be removed by action of the corresponding protease. When the amino acid or peptide is removed, the 1,2-dioxetane decomposes with chemiluminescence, the generation of light providing a rapid, ultra-sensitive and convenient means for detecting the presence of the protease in the sample being inspected. The amount of light generated, or degree of chemiluminescence, can be correlated with the amount of protease present. Immunoassays, as well as DNA hybridization and DNA probe assays are provided.

Abstract: Spiroadamantyl dioxetanes bearing an alkoxy substituent, and a phenyl substituted on the dioxetane ring can be activated to chemiluminesce if the aromatic substituent bears a meta-substituted moiety designated OX, wherein the X is cleaved by an enzyme with which the dioxetane is permitted to come in contact with. The T.sub.1/2 kinetics of the chemiluminescent reaction, as well as the signal intensity and/or quantum yield of the chemiluminescent reaction, can be altered by addition of a chlorine substituent at position 4 on the phenyl ring. Signal strength can further be enhanced by recognized chemiluminescent enhancers.

Abstract: Chemiluminescent bioassays for the presence or concentration of an analyte in a sample use 1,2-dioxetanes as substrates for the enzyme of an enzyme complex that bind to the analyte. The chemiluminescence obtained from the decomposition of the dioxetane triggered by the enzyme through the formation of the corresponding 1,2-dioxetane oxyanion of the enzyme complex is enhanced by the addition of TBQ as an enhancement agent. Other polymeric quaternary onium salts can be used as enhancement agents in conjunction with enhancement additives which improve the ability of the enhancement agent to form hydrophobic regions in the aqueous sample, in which regions the 1,2-dioxetane oxyanion and its chemiluminescent decomposition products can be sequestered. A kit for performing such assays is also provided.

Abstract: Spiroadamantyl dioxetanes bearing an alkoxy substituent, and an aromatic substituent of phenyl or naphthyl on the dioxetane ring can be activated to chemiluminesce if the aromatic substituent bears a moiety designated OX, wherein the X is cleaved by an enzyme with which the dioxetane is permitted to come in contact with. The T.sub. 1/2 kinetics of the chemiluminescent reaction, as well as the signal intensity, or quantum yield of the chemiluminescent reaction, can be altered by selection of an electron-withdrawing or an electron-donating group Z, at positions on the aromatic substituent other than those adjacent the point of attachment to the dioxetane. Signal strength can further be enhanced by recognized chemiluminescent enhancers.

Abstract: Process for preparing highly pure enantiomers of oxirane alcohols, which comprises recrystallizing a mixture of the isomeric oxirane alcohols, in which the desired enantiomer is present in an excess of at least 60% ee, in a solvent or solvent mixture at a temperature just below the melting point of the oxirane alcohol.Oxirane alcohols prepared according to the invention are distinguished by high enantiomer purity. Ferroelectric liquid crystals, which contain highly pure enantiomers of oxirane alcohols according to the invention and/or derivatives derived therefrom, have particularly short switching times.

Abstract: A process for the production of ambergris-type labdane spiroketals of general formulae I and II ##STR1## where R represents oxygen or sulphur, useful in the perfumery industry, the said process being characterized by the intramolecular cyclisation of the epoxyketone or its thio analog of general formula III ##STR2## where R.sub.1 represents COCH.sub.3 and R.sub.2 oxygen or sulphur.

Abstract: Methods are disclosed for purifying chemiluminescent water-soluble 1,2-dioxetane derivatives suitable for use as reporter molecules in a variety of biological analytical systems, including enzyme-linked immunoassays, nucleic acid probe techniques, and structural determinations. The methods are based upon high pressure, medium pressure or low pressure liquid chromatography using as the stationary phase alkaline pH-stable compositions with the chromatographic characteristics of reversed-phase adsorbents, at alkaline pH values, and in the absence of acid-forming compounds or compounds with an unshared pair of electrons. Desalting of substantially pure water soluble 1,2-dioxetane derivatives may be accomplished by the same chromatographic systems or by molecular sieve chromatography systems, but in the absence of salt buffers. Under some circumstances, purification and desalting may be combined in a single chromatographic step.

Abstract: This invention relates to the field of immune therapy of cancer, more specifically to immunoconjugates of a cytotoxic moiety with a targeting moiety, more specifically to immunoconjugates of antibodies or fragments or functional derivatives of antibodies coupled to a cytotoxic substance such as drugs, toxins or radioisotopes. It especially relates to the release of substances bound to a targeting moiety through the use of acid-cleavable linker molecules.

Abstract: The present invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is 2-methyl-1-propenyl group or isobutyl group; R.sup.2 and R.sup.3 are each hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group or R.sup.2 and R.sup.3 may form a ring together with the adjacent nitrogen atom; and the bonding mark .about. represents an .alpha.-linkage or .beta.-linkage, or a salt thereof. The compound (I) of the present invention has, among others, angiogenesis inhibiting activity, cell-growth inhibiting activity and immune reaction inhibiting activity, thus being useful as medicines, etc.

Abstract: The present invention concerns novel dioxolane containing fluoroepoxides that are useful as curing materials, adhesives lubricants and coatings.

Abstract: Novel assay methods employing compounds which are chemically or enzymatically cleavable and which give rise to an intermediate which further decomposes by an intramolecular anchimeric displacement reaction which releases a signal producing species are disclosed. Also disclosed are probe hybridization assays employing the compounds of the invention employing thermostable enzymes which are not denatured by the hybridization conditions. Such signal producing species may include chemiluminescent dioxetanes and other colored products.

Abstract: Disclosed herein are an azole derivative represented by the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 respectively represent a (C.sub.1 -C.sub.5) alkyl group or a hydrogen atom; X represents a halogen atom, a (C.sub.1 -C.sub.5) alkyl group or a phenyl group; n represents an integer of from 0 to 2 and A represents a nitrogen atom or a CH, provided that R.sup.1 is not a hydrogen atom when R.sup.2 is a hydrogen atom, a process for producing the azole derivative represented by the formula(I),and an agricultural and horticultural composition containing the azole derivative represented by the formula(I).

Abstract: A novel synthesis of compounds having the formula: ##STR1## wherein T is a stabilizing spiro-linked polycycloalkylidene group, R.sup.3 is a C.sub.1 -C.sub.20 alkyl, aralkyl or heteroatom containing group, Y is an aromatic fluorescent chromophore, and Z is a cleavable group which, when cleaved, induces decomposition of the dioxetane ring and emission of optically detectable light, is disclosed. A tertiary phosphorous acid alkyl ester of the formula:(R.sup.1 O).sub.3 Pwherein R.sup.1 is a lower alkyl group, is reacted with an aryl dialkyl acetal produced by reacting a corresponding aryl aldehyde with an alcohol of the formula:R.sup.3 OHwherein R.sup.3 is as defined above, to produce a 1-alkoxy-1-arylmethane phosphonate ester of the formula: ##STR2## reacting the phosphonate with base to produce a phosphonate-stabilized carbanion, reacting the carbanion with a ketone of the formula:T.dbd.

Abstract: Dioxetane compounds reactable with an enzyme to release optically detectable eneregy are disclosed. These compounds have the formula: ##STR1## wherein T is a carboxylic acid or methoxy substituted adamantyl group bound to the ring through a spiro bond, Y is phenoxy or napthyloxy and X is methoxy, ethoxy or propoxy. Z is an enzyme cleavable group such that when cleaved by an enzyme, an electron rich moiety is left bound to the dioxetane ring.

Abstract: The present invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is 2-methyl-1-propenyl group or isobutyl group; R.sup.2 is hydrogen atom, an optionally substituted aliphatic hydrocarbon residue or an optionally substituted acyl group, or a salt thereof.The compound (I) of the invention has, among others, angiogenesis inhibiting activity, cell-proliferation inhibiting activity and immune reaction inhibiting activity, thus being useful as medicines, etc.

Abstract: The invention relates to a new process for the reduction of 15-keto carbacyclin intermediates in the presence of cerium(III) Salts.