Abstract: Novel aminomethylphosphine ligands have particular substituents on the central carbon atom. Such ligands form coordination complexes that may be catalysts for the polymerization of monomers or other catalytic induced reactions.

Abstract: Novel aminomethylphosphine ligands have particular substituents on the central carbon atom. Such ligands form coordination complexes that may be catalysts for the polymerization of monomers or other catalytic induced reactions.

Abstract: Novel soluble polyester-supported chiral phosphines have been prepared and have been used in the preparation of rhodium and ruthenium catalysts. Such polymer-supported catalysts show high catalytic activities and enantioselectivities. In the case of Ru(BINAP) catalyst supported on soluble polyester, the resulting catalysts were found to be more active than those of the corresponding homogeneous Ru(BINAP) catalysts in the asymmetric hydrogenation of 2-arylpropenoic acids. These soluble polyester-supported catalysts can be easily separated from the reaction mixture and then be reused without loss of activity and selectivity.

Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalyzed reactions.

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: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: The invention is an improved method for the preparation of tertiary phosphines by way of cross-coupling of aryl, alkenyl, cycloalkenyl or aralkyl halides or aryl, alkenyl, cycloalkenyl or aralkyl sulfonate esters with chlorophosphines in the presence of a catalyst and a reductant. The general reaction scheme is shown below: ##STR1## wherein R.sup.1 is aryl, alkenyl, cycloalkenyl or aralkyl, any of which may be substituted by one or more of the following: alkyl, aryl, aralkyl, alkoxy, alkanoyl, chloro, fluoro, alkoxycarbonyl, cyano, trifluoromethyl, cycloalkyl, or CONR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently hydrogen, alkyl, aryl or aralkyl; R.sup.2 and R.sup.3 are independently aryl, alkyl, aralkyl, any of which may be substituted by one or more of the following: alkyl, aryl, aralkyl, alkoxy, alkanoyl, chloro, fluoro, alkoxycarbonyl, cyano, trifluoromethyl, cycloalkyl or CONR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently hydrogen, alkyl, aryl or aralkyl; and n is 2 where R.

Abstract: Cationic phospholipids and their use in treating pathogen-associated disease are disclosed. The class of phospholipids comprises the phosphotriester derivatives of phosphoglycerides and sphingolipids. Liposomes comprising one or more of the cationic phospholipids are effective in the lipofection of nuclidic acids and are therefore useful in methods of treating disease.

Abstract: The invention relates to novel calixarenes of formula: ##STR1## in which m is equal to 0 or 1, n is an integer from 2 to 8, with 4.ltoreq.n(m+1).ltoreq.8,R.sup.1 and R.sup.2, which can be the same or different, are alkyl or O-nitrophenoxyalkyl groups andR.sup.3 and R.sup.4, which can be the same or different, are alkyl or aryl groups.The calixarenes can be used for extracting actinides and lanthanides from aqueous solutions from spent fuel reprocessing.

Abstract: A process for recovery of solid and reusable urea from the urea adduction process. Refinery streams are subjected to a step of urea adduction for removal of unwanted branched products, aromatics and sulphur. The adduct is purified, dried and then subjected to the step of mechanical shearing.

Abstract: A method and composition for enhancing the biodegradation of hydrocarbon contaminated soil, water, and/or sludge are disclosed. The composition comprises an adduct of urea with a non-ionic surfactant and a phosphorous source. The disclosed method provides for the application of a degradation effective amount of a composition which comprises a N:P ratio which ranges from 10:2 to about 10:0.5 and the urea and non-ionic surfactant are present in the adduct in a weight ratio ranging from 98:2 to 75:25. Further, the method of biodegradation is carried out by the application of the composition to provide for a C:N:P ratio of 100:10:1 to 100:1:001. The C:N:P ratio is based on the weight percent of the hydrocarbon contaminate in the soil, water and/or sludge sites to be treated.

Abstract: The present invention provides novel compounds represented by the general formula I: ##STR1## wherein R.sub.1 is a straight or branched lower alkyl, a cycloalkyl-lower alkyl, an aryl-lower alkyl, a cycloalkyl, an aryl an aryl-cycloalkyl, lower alkoxy, an aryloxy, or a heteroaryl;R.sub.2 is hydrogen, a straight or branched lower alkyl, a cycloalkyl, or a cycloalkyl-lower alkyl;R.sub.3 and R.sub.3 ' are each the same or different and each is hydrogen atom, a straight or branched lower alkyl, a cycloalkyl, an aryl-lower alkyl, an aryl, or a heteroaryl; orR.sub.3 and R.sub.3 ' together form a ring structure;R.sub.3 " is hydrogen, lower alkyl or an aryl; orR.sub.2 and R.sub.3 " together form a lower alkylene group --(CH.sub.2).sub.n -- wherein n is an integer of 1, 2 or 3; orR.sub.2 and R.sub.3 " together form a group represented by the formula: --(CH.sub.2).sub.p --Ar-- or --Ar--(CH.sub.2).sub.p --, respectively, wherein p is zero or an integer of 1 or 2, and Ar is an arylene or heteroarylene;C(.dbd.X) is C(.dbd.

Abstract: Ligands useful for transition metal catalyzed bond forming reactions are provided with a metal binding portion having at least one metal binding moiety ##STR1## wherein Ar and Ar' each is an aryl or a heteroaryl. These ligands may be prepared by providing an aromatic carboxylic acid having a diarylphosphino or diheteroarylphosphino substituent on the aromatic ring, and forming an ester or an amide derivative of the carboxylic acid by coupling with a chiral diol or a chiral diamine. The ligands facilitate, for example, flexible strategies for enantiocontrolled construction of five membered carbocyclic rings with varying substitution patterns and high enantioselectivity.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalysed reactions.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: One embodiment of the present invention provides compounds comprising an adduct of urea with a non-ionic surfactant. Another embodiment of the present invention, there is provided a composition suitable for enhancing the bioremediation of contaminated soils and water which comprises at least one adduct of urea with a non-ionic surfactant, preferably in combination with a phosphorous source.

Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: Improved solvent systems for the formulation of N-alkyl thiophosphoric triamide urease inhibitors. These formulations enable the preparation of stable concentrated solutions of N-alkyl thiophosphoric triamides for storage, transportation, and eventual impregnation onto solid urea containing fertilizers and incorporation into liquid urea containing fertilizer compositions. These formulations are comprised primarily of a solvent selected from the group consisting of glycols and glycol derivatives. Optionally, in addition to the glycol base solvent, the formulations can contain a co-solvent selected from the group consisting of liquid amides, 2-pyrrolidone and N-alkyl 2-pyrrolidones, and/or a nonionic surfactant selected from the group consisting of alkylaryl polyether alcohols. The presence of the co-solvent and/or surfactant has been found to impart desirable properties to the formulations under certain conditions.

Abstract: The present invention provides a method for producing novel optically active diphosphine compounds ?2,2'-bis(di-substituted phosphino)-1,1'-binaphthyl compounds! having a selectivity (chemoselectivity or enantioselectivity) and catalytic activity different from those of conventional BINAP compounds. In a method of the present invention for producing an optically active diphosphine compound (i.e., 2,2-bis(di-substituted phosphino)-1,1'-binaphthyl), 2,2'-bis(trifluoromethanesulfonyloxy)-1,1'-binaphthyl is reacted, in the presence of a transition metal-phosphine complex, with a phosphineoxide compound represented by the following general formula:A.sub.

Abstract: Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.3 ' and R.sub.4 ' are as defined in claim 1. The compounds are in part novel and are suitable for use as light stabilizers for organic materials.

Abstract: The preparation of .alpha.-carbonylphosphine oxides by oxidizing an .alpha.-hydroxyalkyl phosphine oxide with an organic hydroperoxide or of an organic peroxy acid in the presence of a compound of a Group IV to Group VIII metal in the periodic table, and novel .alpha.-hydroxybenzyl phosphine oxides. .alpha.-Carbonylphosphine oxides are used as photoinitiators for polymerizable compositions.

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: A dicationic surfactant for enhancing the chemiluminescence of chemiluminescent compounds particularly dioxetanes which are triggerable is described. The surfactant has the formulaX.sup.- (R.sub.1).sub.3 A.sup.+ CH.sub.2 -Link-CH.sub.2 A.sup.+ (R.sub.2).sub.3 X.sup.-wherein A is selected from the group consisting of phosphorus and nitrogen atoms separately or together, wherein X is an anionic counterion and R.sub.1 and R.sub.2 are selected from the group consisting of unsubstituted and substituted alkyl and aralkyl groups containing 1 to 20 carbon atoms and R.sub.1 and R.sub.2 can be the same or different, and wherein Link is a carbon chain group selected from the group consisting of dialkylenearyl, aryl, alkylene, alkenylene and alkynylene groups containing 4 to 20 carbon atoms. The surfactants are particularly useful in Western and Southern blot assays.

Abstract: New lipopolyamines of general formula (I), their salts, their preparation and their use. ##STR1## n=1 to 5 and m=2 to 6 R represents a radical ##STR2## (R.sub.1 and R.sub.2 : aliphatic radical containing 12 to 22 carbon atoms; R: hydrogen atom or alkyl radical optionally substituted with phenyl), or a radical ##STR3## (X=CH.sub.2, CO; R.sub.3 and R.sub.4 aliphatic radical containing 11 to 21 carbon atoms), their preparation and their use.The lipopolyamines of general formula (I) are especially useful as vectors for the transfection of eukaryotic cells.

Abstract: Multifunctional additives having a variety of advantageous properties are described. They are formed by a process which comprises heating concurrently or in any sequence a) an oil-soluble ashless dispersant containing basic nitrogen with b) an alkoxylated alcohol of at least 8 carbon atoms c) a borating agent and optionally d) an inorganic oxyacid or anhydride of phosphorous. The reactants are in proportions on an active ingredient basis of about 0.03 to about 0.35 part by weight of b) per part by weight of a), and about 0.005 to about 0.06 part by weight of boron as c) per part by weight of a). The reaction temperature can range from about 50.degree. to about 150.degree. C. Water and/or solids present in the resultant mixture can be removed. Preferably, the optional phosphorous component is used in the formation of these additives. This phosphorous component can be an inorganic oxyacid or anhydride of phosphorous.

Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT).

Abstract: A crosslinking agent suitable for acrylic rubbers, particularly for acrylic rubbers containing units of a cyanoacetic acid comonomer or a malonic acid comonomer for imparting a crosslinkability, which comprises a reaction product of formaldehyde or a polymerized formaldehyde with urea or thiourea in the presence of an acidic catalyst.

Abstract: A method for incorporating novel phosphine containing amino acids into peptide sequences is provided. The resulting phosphine-containing peptides can be used to bind a transition metal between two phosphine moieties presented on an amino acid in a peptide. The resulting phosphine-containing peptide metal complex is useful as a stereoselective catalyst of a chemical reaction or as a means for delivering a metal selectively to a target tissue or organ for medical uses.

Abstract: Novel benzylphosphonate compounds of the general formula I: ##STR1## are disclosed as useful in treating bone wasting diseases including postmenopausal osteoporosis in increasing in mammals bone formation and bone mass.

Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

Abstract: Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalyzed reactions.

Abstract: Novel mordants based upon a polyethyleneimine backbone and either pendant phosphonium or quaternized-nitrogen compounds are disclosed. The mordants find use in stopping or controlling ink-bleeding into ink-jet receptors and photographic films.

Abstract: A process for separation of aliphatic straight-chain compounds having terminal functional groups from mixtures containing isomers thereof branched in the .alpha.-position by precipitating the aliphatic, straight-chain compounds as their clathrates.

Abstract: Reaction of amine-containing substrates with hydrogen peroxide can suffer from certain problems, especially in the presence of transition metals. These problems include both in situ generation of impurities and particularly nitrosamines, which are allegedly carcinogenic, and also impaired product formation. The problems can be ameliorated by employing in the reaction mixture free radical scavengers, including in particular phenols and polyhydroxy-substituted aromatic compounds. The scavengers are advantageously employed in conjunction with a metal chelating agent such as polycarboxylic acid or an organopolyphosphonic acid.

Abstract: Organophosphorus dihalides can have one of their halogen substituents substituted with an alkyl group from a trialkylaluminum by gradual addition of the latter reagent to the former.

Abstract: Novel benzylphosphonate compounds of the general formula I: ##STR1## are disclosed as useful in treating bone wasting diseases including postmenopausal osteoporosis in increasing in mammals bone formation and bone mass.

Abstract: The present invention relates to novel preorganized hexadentate ligands suitable for complexing with a radionuclide to form imaging agents for diagnostic purposes. The ligands have the formula: ##STR1## wherein a) R.sub.2 is hydrogen and R.sub.3 is methyl; or R.sub.2 and R.sub.3 together form a methoxy benzene ring.

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: Process for the preparation of phosphino compounds Phosphorus-containing compounds of the formula (I)(R.sup.1)(R.sup.2)P(O)--CR.sup.3 R.sup.4 --CHR.sup.5 R.sup.6 (I)in whichR.sup.1 and R.sup.2 are alkyl, alkoxy or optionally substituted phenyl,R.sup.3 and R.sup.5 are H, R, optionally substituted phenyl, ROCO--, RO--CO--RO--, halogen, CN, RO--, RO--RO--R-CO--, H.sub.2 NCO--, RNHCO-- or RRNCO--, in which R is alkyl,R.sup.4 and R.sup.6 have the same meaning as defined for R.sup.1 and R.sup.2 or are a divalent radical--CO--R.sup.7 --COin whichR.sup.7 is oxygen, NR* or sulfur, and R* is H, optionally substituted phenyl or alkyl,are precursors for plant protection agents and fire retardants. According to the invention they can be prepared in high yields and high purity by reacting a compound (R.sup.1)(R.sup.2)P--OR.sup.8, in which R.sup.8 is alkyl or optionally substituted phenyl, with an alkene of the formula R.sup.3 R.sup.4 C.dbd.CR.sup.5 R.sup.

Abstract: .alpha.-Chloro phosphorus ylides of the formula I ##STR1## where the Ar radicals are identical or different aryl groups, and E is a substituent which stabilizes the ylide (I), are prepared by reacting a phosphonium salt of the formula II ##STR2## where Hal is chlorine, bromine or iodine, with a chlorinating agent, using bleaching powder as chlorinating agent.

Abstract: Lubricant additives are producd by reacting an alkoxplated amine with phosphorous acid. The additives preferably also contain a boron moiety which is reacted with the phosphorous acid and amine, preferably in a one step reaction. More preferably, a mono-functional alcohol or a long-chain aliphatic carboxylic acid is added to this mixture. The additives are particularly useful in metalworking oils and particularly as extreme pressure additives to replace the currently used chlorinated paraffin additives.

Abstract: Crude organic solutions of N,N-dialkylcarbamoylmethylphosphine oxide compounds can be purified by treatment with a first row transition metal salt to form a complex which can be treated to regenerate a purified solution of the compound. The first row transition metal can be selected from the monobasic acid salts of zinc, for example.

Abstract: A process is disclosed for preparing biaryl, bidentate ligands comprising:(1) contacting a biaryl compound having the structural formula: ##STR1## with a proton abstracting agent under conditions suitable to form a biaryl dianion, which is then(2) contacted with a Group V compound of the formula: ##STR2## where X' is halogen or a suitable leaving group.

Abstract: Reaction of amine-containing substrates with hydrogen peroxide can suffer from the problems of in situ generation of nitrosamines, which are allegedly carcinogens, as impurities and impaired product formation, especially in the presence of transition metals.The problems can be ameliorated by employing a selected range of alkyleneaminopoly(methylenephosphonic acid) compounds such as cyclohexane-1,2-diaminotetra(methylenephosphonic acid).

Abstract: The content of hydrogen chloride and phosphorous acid of crude amino organic phosphonic acids, especially diethylenetriaminepentakis (methylene phosphonic acid) is reduced by solvent extraction into an alcoholic phase leaving purified phosphonic acid behind.

Abstract: Crude N,N-dialkylcarbamoylmethylphosphonates and phosphine oxide extractants, and particularly crude dihexyl N,N-diethylcarbamoylmethylphosphonate and octylphenyl N,N-diisobutylcarbamoyl phosphine oxide, are purified by distilling the crude materials in a thin film evaporator. Preferably, the crude dihexyl N,N-diethylcarbamoylmethylphosphonate is reacted with concentrated hydrochloric acid and subsequently reacted with aqueous sodium hydroxide prior to distillation in the thin film evaporator to hydrolyze impurities contained in the crude product. The purified extractants are useful for extracting actinides and lanthanides from liquid waste streams.

Abstract: Novel nucleophilic tertiary organophosphines and the specific cleavage of peptide bonds by nucleophilic tertiary organophosphines. This invention is of particular utility in providing chemical agents for use in the cleavage of proteins and the determination of the amino acid sequence of proteins.

Abstract: A process for the production of a blocked urea group-containing polyisocyanate from a partially blocked polyisocyanate and polyamine, comprising the steps of:(i) reacting a partially blocked polyisocyanate, said polyisocyanate being made substantially free of monomeric polyisocyanate, by vacuum thin layer evaporation with a primary polyamine, secondary polyamine, or mixtures thereof, in relative proportions such that the ratio of isocyanate groups to amino groups is in the range from about 1:1 to 1.3:1, and(ii) isolating said urea group-containing polyisocyanate by wherein the vacuum boiling point of said polyisocyanate is lower than the deblocking temperature of said urea group-containing polyisocyanate.