Abstract: The invention relates to a novel process for the preparation of an aminoalcohol of the formula racemically or optically active, starting from 2-azabicyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)— or (1R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulae In the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl)formamide of the formula to give (1S,4R)— or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulae and then cyclized to give the end compounds.

Abstract: A process is provided for stabilizing and/or lowering the color number of alkenyl compounds containing a divalent or trivalent heteroatom in the &agr;-position to the double bond, wherein an oxidizing agent is added to the alkenyl compounds.

Abstract: The present invention relates to a cyclic tertiary amine compound represented by a formula (1) and an organic luminescent device.

Abstract: A composition comprises organoborane amine complex and 1,4-dioxo-2-butene-functional material. The composition can form a part of a polymerization initiator system that also includes a compound that is reactive with the amine portion of the complex. The system can be used to initiate polymerization of acrylic monomer and to form an acrylic adhesive that has exceptionally good adhesion to low surface energy polymers.

Abstract: A composition comprises organoborane amine complex and 1,4-dioxo-2-butene-functional material. The composition can form a part of a polymerization initiator system that also includes a compound that is reactive with the amine portion of the complex. The system can be used to initiate polymerization of acrylic monomer and to form an acrylic adhesive that has exceptionally good adhesion to low surface energy polymers.

Abstract: An organic light emitting device material comprises at least one compound having at least two asymmetric carbon atoms per a molecule.

Abstract: Amide compounds of formula (I), combinatorial libraries of amide compounds and methods of preparing the same are provided. Libraries of the invention are useful for screening in biological assays in order to identify pharmaceutically useful compounds.

Abstract: Three processes are described for preparing (hetero)aromatic substituted benzene derivatives which comprise aromatization of cyclohexenone derivatives via (chloro)cyclohexadiene derivatives.

Abstract: Novel compounds are provided having the structural formula R[—N(NO2)—L—R1]n wherein R, L, R1 and n are defined herein. The compounds are useful in a variety of contexts, but are primarily to be used as high energy oxidizing agents in explosive compositions, propellant formulations, gas-generating compositions and the like. The compounds are also useful as pharmaceutical agents. Compositions containing the compounds are also provided, including energetic compositions, as are methods for using the novel compounds and compositions.

Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be colorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.

Abstract: Three processes are described for preparing (hetero)aromatic substituted benzene derivatives which comprise aromatization of cyclohexenone derivatives via (chloro)cyclohexadiene derivatives.

Abstract: A composition comprises organoborane amine complex and 1,4-dioxo-2-butene-functional material. The composition can form a part of a polymerization initiator system that also includes a compound that is reactive with the amine portion of the complex. The system can be used to initiate polymerization of acrylic monomer and to form an acrylic adhesive that has exceptionally good adhesion to low surface energy polymers.

Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be calorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.

Abstract: The present invention describes methods for the detoxification of a mixture of nitrile compounds, or a mixture of nitrile and amide compounds by conversion of the nitrile compound(s) to the corresponding amide or acid compounds using a pure culture of an induced microorganism strain capable of converting a nitrile moiety to an amide or acid moiety. If an amide is formed or is present in the mixture, the amide can be further converted, using the present methods for detoxification, to the corresponding acid. The acid can then, if desired, be further degraded to CO.sub.2, H.sub.2 O and biomass. The induced pure cultures are able to detoxify a mixture of nitriles or a mixture of nitrites and amides which are typically present, in high concentration(s), in nitrile production waste streams.

Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic chiral catalyst to produce a stereoisomerically or regioselectively enriched product.

Abstract: A method of identifying highly fecund males in which an isotonic, buffered liquid test specimen of semen is layered on top of a barrier medium that inhibits net movement (migration) of less mobile sperm into the barrier medium. Differences in mobility of populations of sperm among test subjects have been found to predict whether a male will be highly fecund or not. Sperm migration into the barrier medium is quantitated, for example by analyzing the barrier medium in a spectrophotometer or a photometer after sperm migration is allowed to occur. Alternatively, a collection member coated with a sperm binding protein may be placed below the barrier medium, and the number of sperm that bind to the collection member quantitated after incubation. The invention also includes a device for incubating the barrier medium at a physiologic temperature for a sufficient period of time to allow the highly mobile sperm to migrate into the barrier medium.

Abstract: The present invention describes methods for the detoxification of a mixture of nitrile compounds, or a mixture of nitrile and amide compounds by conversion of the nitrile compound(s) to the corresponding amide or acid compounds using a pure culture of an induced microorganism strain capable of converting a nitrile moiety to an amide or acid moiety. If an amide is formed or is present in the mixture, the amide can be further converted, using the present methods for detoxification, to the corresponding acid. The acid can then, if desired, be further degraded to CO.sub.2, H.sub.2 O and biomass. The induced pure cultures are able to detoxify a mixture of nitrites or a mixture of nitriles and amides which are typically present, in high concentration(s), in nitrile production waste streams.

Abstract: Reagents and methods for multi-step labeling of nucleic acids allow the addition of relatively insoluble or unstable labels to nucleic acid in the final step. Nucleic acids can be stored as a stable intermediate capable of reacting with a label conjugated to a thiol-reactive group.

Abstract: The present invention relates to advanced glycosylation endproducts, and particularly to the use of novel cyclopentenone aminoreductones, 3-alkylamino-2 -hydroxy-4-hydroxymethyl-2-cyclopenten-1-ones. Such AGEs can be used in various diagnostic and therapeutic methods.

Abstract: The invention is directed to synthetic receptor(s) which comprises a polyfunctional organic template covalently linked to two or more oligomers which may independently be the same or different and may independently be straight chain or branched. The template may be linked to an identifier which uniquely defines the synthetic receptor. The identifier is a stable chemical molecule or a plurality of stable chemical molecules distinguishable and detectable to picomolar levels or may be an oligonucleotide. In an preferred embodiment, the template is covalently linked to a solid support which is linked to an identifier.

Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.

Abstract: A process for the preparation of cyclopropanamine by Hofmann degradation of cyclopropanecarboxamide, comprising the following steps:(1) suspending cyclopropanecarboxamide, either (A) in 1.1 to 4 mol of sodium hydroxide, in solution whose concentration is 10 to 50%, per mol of amide, or (B) in a sparing amount of water,(2) adding 1 to 1.5 mol of hypochlorite, per mol of amide, from a 5 to 15% strength hypochlorite solution at a temperature of 0.degree. to 20.degree. C.,(3) adding 1.1 to 4 mol of sodium hydroxide, in solution whose concentration is 10 to 50%, per mol of amide, in the case where a suspension has been formed according to step (1)(B),(4) reacting the amide, hypochlorite, and sodium hydroxide for 10 to 60 minutes to form a homogeneous reaction mixture,(5) continuously passing the homogeneous reaction mixture through a tubular reactor at a temperature of 45.degree. to 260.degree. C.

Abstract: The present invention is directed to the process of preparing a peptide comprising reacting a first amino acid or peptide with an amino acid fluoride of the formula: ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting groupAA is an amino acid residue andX is H or a protecting group useful,and the first amino and peptide have a free amino group and a blocked carboxy end.

Abstract: Substituted sulfonimidamides, processes for their preparation, their use as a medicament or diagnostic, and medicament comprising themSulfonimidamides of the formula I ##STR1## in which at least one of the three substituents R(1), R(2) and R(3) is a benzoylguanidine, and in which the other substituents have the meanings indicated in the claims, are outstandingly suitable as medicaments having action on the cardiovascular system; that is as antiarrhythmic pharmaceuticals having a cardioprotective component as well as for treating ischemically induced damage; also in operative interventions, such as organ transplantation.

Abstract: The present invention relates to certain purine nucleoside analogues containing a carbocyclic ring in place of the sugar residue, salts, esters and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and to the use of such compounds in therapy, particularly the treatment or prophylaxis of certain vital infections.

Abstract: The invention is the use of nitronyl substituted hindered phenols as antioxidants in therapeutic applications. In the preferred embodiment the compositions have the general formula: ##STR1## Wherein R1 is hydrogen, an alkyl or an aryl and R2 is an alkyl or an aryl; R.sub.3 is an alkyl; and R.sub.4 is an alkyl. Further, the invention relates to novel compositions useful as antioxidants. The novel compounds include: 2,6-di-tert-butyl-4-(N-tert-octyl) nitronyl phenol (DBONP); 2,6-dimethyl-4-(N-tert-octyl) nitronyl phenol (DMONP); N-tert -octylC-phenyl nitrone (OPN).

Abstract: The invention is the use of nitronyl substituted hindered phenols as antioxidants in therapeutic applications. In the preferred embodiment the compositions have the general formula: ##STR1## Wherein R1 is hydrogen, an alkyl or an aryl and R2 is an alkyl or an aryl; R.sub.3 is an alkyl; and R.sub.4 is an alkyl. Further, the invention relates to novel compositions useful as antioxidants. The novel compounds include: 2,6-di-tert-butyl-4-(N-tert-octyl) nitronyl phenol (DBONP); 2,6-dimethyl-4-(N-tert-octyl) nitronyl phenol (DMONP); N-tert-octylC-phenyl nitrone (OPN).

Abstract: A two-step process for the conversion of a trans-1-amino-2-hydroxycycloalkane stereoselectively to a cis-1-amino-2-hydroxycycloalkane is disclosed. The novel step, a one-step hydrolysis with formal inversion, can be used to convert an amide of a trans-1-amino-2-hydroxycycloalkane to a cis-1-amino-2-hydroxycycloalkane. Methods for obtaining the trans-1-amino-2-hydroxycycloalkanes and their amides from alkenes are also disclosed. A preferred process converts indene to cis-1-amino-2-indanol.

Abstract: The invention is the use of nitronyl substituted hindered phenols as antioxidants in therapeutic applications. In the preferred embodiment the compositions have the general formula: ##STR1## Wherein R1 is hydrogen, an alkyl or an aryl and R2 is an alkyl or an aryl; R.sub.3 is an alkyl; and R.sub.4 is an alkyl. Further, the invention relates to novel compositions useful as antioxidants. The novel compounds include: 2,6-di-tert-butyl-4-(N-tert-octyl)nitronyl phenol (DBONP); 2,6-dimethyl-4-(N-tert-octyl)nitronyl phenol (DMONP); N-tert-octyl-C-phenyl nitrone (OPN).

Abstract: Process for preparing amines by reacting amides in aqueous-alkaline solutions and/or suspensions with halogens or hypohalites in the presence of alcohols, and converting the reaction products into the amines by hydrolysis, hydrogenation or reductive methods.

Abstract: The present invention is directed toward artionic polymerization employing lithio amines mixed with an organic alkali metal compound and optionally, a chelating reagent. The lithio amines have the general formula (A)Li(SOL)y, where SOL is a solubilizing component, A is an alkyl, dialkyl, cycloalkyl or dicycloalkyl amine radical or a cyclic amine, and y is 0 or is from about 0.5 to about 3. The invention is also directed toward polymers and other products made using the initiator, and methods therefor. Further, the invention contemplates a polymer, a polymer composition and products therefrom, which include a functional group from the reaction product of an amine and an organolithium compound. The resulting polymers may be terminated with a terminating, coupling or linking agent, which may provide the polymer with a multifunctionality.

Abstract: The present invention is directed toward anionic polymerization initiators which are soluble in acyclic alkane solvents. The initiators include a solubilized lithio amine having the general formula (A)Li(SOL).sub.y. SOL is a solubilizing component and A is an alkyl, dialkyl or cycloalkyl amine radical or a cyclic amine and y is from about 1 to 4. The invention is also directed toward polymers and other products made using the initiator, and methods therefore. Further, the invention contemplates a polymer, a polymer composition and products therefrom, which include a functional group from the reaction product of an amine and an organolithium compound. The resulting polymers may be terminated with a terminating, coupling or linking agent, which may provide the polymer with a multifunctionality.

Abstract: 4-amino-2-buten-1-ol is formed by the regioselective addition of primary amines or ammonia to 3,4-epoxy-1-butene. A quantity of a the primary amine or ammonia is reacted with 3,4-epoxy-1-butene in a reaction medium in the presence of a catalyst. The reaction medium is a liquid which has an E.sub.T (30) no less than about 32. The catalyst is a complex of palladium and phosphine ligands.

Abstract: 5-Amino-1-(hydroxymethyl)cyclopentane-1,2,3,4-tetraol and 2-amino-4-(hydroxymethyl)-3a,5,6,6a-tetrahydro-4H-cyclopent[d]oxazole-4,5, 6-triol, which have the ability to inhibit the activity of sugar hydrolases, especially .beta.-glucosidase and sucrase and can thus be used for the treatment and prophylaxis of tumorous conditions, AIDS, diabetes and obesity, can be prepared by hydrolysis of trehazolin. 2-Amino-4-(hydroxymethyl)-3a,5,6,6a-tetrahydro-4H-cyclopent[d]oxazole-4,5, 6-triol can also be prepared by fermentation using newly isolated strains Micromonospora sp. SANK 62390, FERM BP-3521 and Amycolatopsis sp. SANK 60791, FERM BP-3513.

Abstract: The compound (-)-N-t-butyl-4,4-diphenyl-2-cyclopentenylamine, or its hydrochloride salt has anticholinergic activity, and thus has a variety of pharmaceutical utilities.

Abstract: Pharmacologically active compounds corresponding to the formula I ##STR1## in which n represents 2-5,m represents 2-6,R.sup.1 denotes hydrogen or lower alkyl,R.sup.2 represents an OR.sup.4 group in which R.sup.4 denotes lower alkyl or a phenyl or phenyl-lower alkyl group which is optionally substituted in the phenyl ring, orR.sup.2 represents a ##STR2## group in which R.sup.5 and R.sup.6 independently of one another each denote hydrogen, lower alkyl or a phenyl or phenyl-lower alkyl group which is optionally substituted in the phenyl ring, orR.sup.5 and R.sup.6, together with the nitrogen atom to which they are bonded, represent a saturated 5- or 6-membered heterocycle,R.sup.3 represents a saturated monocyclic or bicyclic hydrocarbon group which is derived from terpenes and has 10 or 11 carbon atoms, andZ represents oxygen or, if R.sup.3 is a dihydronopyl group, Z may also represent sulfur,and salts thereof.

Abstract: The present invention relates to 6-substituted purine carbocyclic nucleosides and their use in medical therapy particularly in the treatment of HIV and HBV infections. The invention also relates to pharmaceutical formulations and processes for the preparation of compounds according to the invention.

Abstract: The present invention arises from the discovery of an endogenous malignancy-associated catabolite characterized by (i) a molecular weight of about 135 daltons as determined by mass spectrum analysis; (ii) a UV absorption maximum at 237 nm; (iii) a 15 centimeter C18 HPLC column retention time of from about 1.00 to about 2.00 minutes as compared to a retention time at a 1 ml/minute flow rate of about 2.5 to about 3.0 minutes for an internal standard marker; (iv) containing no aromatic ring structures, containing one methyl group at the 1-position and one methyl group at the 6-position of an alpha carbon chain, and containing at least one nitrogen moiety as determined by nuclear magnetic resonance; and (v) being present in elevated amounts in the urine substantially exclusively of individuals suffering from malignant conditions.

Abstract: Herbicidal substituted 4-amino-5-alkylthio-1,2,4-triazol-3-ones of the formula ##STR1## in which R.sup.1 represents in each case straight-chain or branched alkyl, alkenyl or alkinyl, each of which has up to 4 carbon atoms, andR.sup.2 represents sec-butyl, tert.-butyl or optionally substituted C.sub.5 -C.sub.10 -alkyl, alkenyl or alkinyl, or piperidyl- or morpholinyl-alkyl, optionally substituted C.sub.3, C.sub.4, C.sub.5 and C.sub.7 -cycloalkyl, substituted cyclohexyl, or optionally substituted benzyl, phenethyl, naphthylmethyl or naphthylethyl.

Abstract: The present invention relates to a process for the production of primary amines containing aliphatically or cycloaliphatically bound amino groups, characterized in that the isocyanate groups of organic isocyanates containing aliphatically and/or cycloaliphatically bound isocyanate groups are formylated with formic acid in a first reaction step and the N-formyl groups are subsequently converted into amino groups.The present invention also relates to polyamine mixtures obtained by this process and containinga) about 40 to 90% by weight, based on the total weight of components a) and b), of N,N',N"-tris-(6-aminohexyl)-isocyanurate andb) about 10 to 60% by weight, based on the total weight of components a) and b), of higher homologs of this triamine containing more than one isocyanurate ring.Finally, the present invention relates to the use of these polyamine mixtures as hardeners for polymer precursors containing epoxide or isocyanate groups.

Abstract: The present invention relates to novel fluorinated alkoxyimines having the formula:R.sub.x --CF.dbd.N--O--CZ.sub.1 Z.sub.2 --CF.sub.3 (I)wherein:R.sub.x is either F or a perhalogenated alkyl group containing from 1 to 3 carbon atoms, andZ.sub.1 and Z.sub.2, either equal to, or different from, each other, are F, Cl, Br, H or a perfluorinated alkyl group containing from 1 to 3 carbon atoms.They are prepared by reacting a fluorinated alkoxyamine haivng the formula:R.sub.x --CF.sub.2 --NH--O--CZ.sub.1 Z.sub.2 --CF.sub.3 (V)with KF at a temperature comprised within the range of from 0.degree. C. to 100.degree. C.The present invention relates furthermore to the N-chloro- and N-bromo-derivatives of said fluorinated alkoxyimines (I), which derivatives have the formulae:R.sub.x --CF.sub.2 --NCl--O--CZ.sub.1 Z.sub.2 CF.sub.3 (VII)andR.sub.x --CF.sub.2 --NBr--O--CZ.sub.1 Z.sub.2 --CF.sub.3 (VIII).

Abstract: A perfluoroalkyl halogenide represented by the formula: ##STR1## wherein X stands for one element selected from the group consisting of iodine and bromine, R.sub.f for a perfluorohydrocarbon group, n for an integer in the range of 1 to 3, and m for an integer in the range of 1 to 3, provided that n and m satisfy the relationship, n.gtoreq.m, is produced by a method which consists essentially in subjecting a perfluorocarboxylic acid fluoride represented by the formula, ##STR2## wherein R.sub.f and n have the same meanings as defined above, to a thermal reaction with a lithium halogenide represented by XI, wherein X has the same meaning as defined above.

Abstract: 3-Hydroxy-2-cyclobuten-1-one salts of the general formula: ##STR1## wherein R is an ammonium group of the general formula: ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different in meaning and each is a hydrogen atom, a lower alkyl group or a cycloalkyl group or R is an alkali metal atom. The salts according for formula I are obtained by the reaction of pure 3-acetoxy-2-cyclobuten-1-one, or 1,3-cyclobutanedione or a distillation residue of the diketene production containing 3-acetoxy-2-cyclobuten-1-one, with a base. The base can be an amine of the general formula: ##STR3## wherein R.sub.1, R.sub.2 , and R.sub.3 have the above-mentioned meaning, or an alkali metal alcoholate or an alkali metal hydroxide. The salts according to formula I are suitable for the production of squaric acid, by their being halogenated in a first step and then being hydrolyzed to squaric acid in a second step.

Abstract: A soil disease controlling agent for preventing and controlling diseases caused by pathogenic fungi living in soil, which comprises an effective amount of at least one of a 2-cycloalkenylamine derivative and its salts as an active ingredient, and at least one inert carrier or diluent.

Abstract: Compounds of the formula ##STR1## wherein Ar, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X and n have the meanings mentioned in the description, processes and intermediates for their preparation, pharmaceutical compositions which contain them and their use in therapy in the treatment of cardiovascular diseases.

Abstract: The present process for the preparation of cyclopropylamine by the so-called Hofmann degradation of cyclopropanecarboxamide is characterized in that the cyclopropanecarboxamide is employed in the form of a solution. The new process can be carried out at 5.degree.-35.degree. C. The cyclopropylamine is obtained after introducing the reaction mixture into a concentrated alkali metal hydroxide solution.

Abstract: Addition salts of cysteamine with acids are prepared by reacting aziridine with an organic sulfur compound of oxidation state -2 and with a ketone and then subjecting the thiazolidine formed as an intermediate to acid hydrolysis, by a process in which aziridine and the ketone are reacted with ammonium hydrogen sulfide or with a metal hydrogen sulfide with the addition of a moderately strong or strong acid at from -10.degree. to +100.degree. C. and a pH which is greater than or equal to 8.5 is maintained.

Abstract: An antiviral compound of the formula: ##STR1## wherein A is selected from a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group and a heterocyclic isostere of a pyrimidin-1-yl group; andG and D are independently selected from hydrogen, C.sub.1 to C.sub.10 alkyl and substituted derivatives thereof, --OH, --C(O)H, --CO.sub.2 R.sub.1 l wherein R.sub.1 is hydrogen or C.sub.1 to C.sub.10 alkyl and --OCH.sub.2 PO.sub.3 H.sub.2, with the proviso that one of D or G is other than hydrogen or C.sub.1 to C.sub.10 alkyl; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to novel intermediates of the formula ##STR1## wherein R is lower alkyl or cyclohexyl, and X is hydroxy or a conventional leaving group, and the use thereof in a process for the preparation of certain histamine H.sub.2 -antagonists.

Abstract: The invention is the use of nitronyl substituted hindered phenols as antioxidants in therapeutic applications. In the preferred embodiment the compositions have the general formula: ##STR1## Wherein R1 is hydrogen, an alkyl or an aryl and R2 is an alkyl or an aryl; R.sub.3 is an alkyl; and R.sub.4 is an alkyl. Further, the invention relates to novel compositions useful as antioxidants. The novel compounds include: 2,6-di-tert-butyl-4-(N-tert-octyl)nitronyl phenol (DBONP); 2,6-dimethyl-4-(N-tert-octyl)nitronyl phenol (DMONP); N-tert-octyl-C-phenyl nitrone (OPN).