Abstract: The invention concerns additive compositions obtained by mixing at least two thermoassociative and exchangeable compounds and at least one boronic ester compound that enables the association of these two copolymers to be controlled; a lubricating composition obtained by mixing at least one lubricating base oil, at least two thermoassociative and exchangeable compounds, and at least one boronic ester compound that enables the association of these two copolymers to be controlled; a method for adjusting the viscosity of a lubricating composition obtained by mixing at least one lubricating base oil and at least two thermoassociative and exchangeable compounds; and the use of a boronic ester compound to adjust the viscosity of a lubricating composition.

Abstract: 18F-labeled 4-boronophenylalanine (BPA) can be produced by preparing and further processing a precursor of 18F-labeled BPA represented by the following formula: in which R1 represents a bromo group, an iodo group, a fluoro group, a diazaborinane derivative, BX3? or BX3?M+ (wherein X represents a halogen atom; and M+ represents a monovalent monoatomic cation, a polyatomic cation or a complex cation).

Abstract: A Cu(I)-catalyzed 1,3-halogen migration reaction effectively recycles an activating group by transferring a halogen from an sp2 to a benzylic carbon with good enantioselectivity and concomitant borylation of the Ar-halo bond. The resulting enantio-enriched benzyl halide can be reacted in the same vessel under a variety of conditions to form an additional carbon-heteroatom or carbon-carbon bond while maintaining high ee. The reaction can be used to efficiently prepare novel compounds and intermediates for the preparation of therapeutics and ligands for catalysis.

Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: The invention relates to new compounds containing alkyl-alkoxy-cyano-borate anions, their preparation and their use, in particular as part of electrolyte formulations for electrochemical or optoelectronic devices.

Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: A method of the present invention for treating malaria includes the step of administering, to a human or an animal, a therapeutically effective amount of drug for suppressing calcium ion exit from an intracellular organelle of the malaria parasite to an outside of the intracellular organelle and/or calcium ion entry from an outside of a cell of the malaria parasite into the cell.

Abstract: The invention concerns processes for the synthesis of a compound of the formula: wherein: R1 and R2 are each, independently, C1-C12 alkyl, CO2R3, OR4, R5(OR6), or C6-C18 aryl; R3-R6 are each, independently, C1-C12 alkyl or C6-C12 aryl; and n and m are each, independently, O or an integer from 1-5; said process comprising:—contacting a compound of the formula H0-R7-0H with BH3 and a compound of the formula in the presence of a nickel-containing catalyst to produce a first product, where R7 is a C2-C12 hydrocarbon group and X is a halogen, OMs or OTs;—contacting the first product in situ with a compound of the formula: in the presence of a nickel-containing catalyst to produce a compound of formula I, where Z is a halogen.

Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.

Abstract: Provided is a method for producing a difluorocyclopropane compound under milder reaction conditions and with high selectivity and high yield. The method for producing a difluorocyclopropane compound of the present invention is characterized by using sodium bromodifluoroacetate as a difluorocyclopropanation agent. With the disclosed method, a difluorocyclopropane compound can be produced under milder reaction conditions and with a higher conversion rate and a higher yield compared to conventional art. Further, by-products can be reduced significantly, thus allowing waste to be greatly reduced. Accordingly, the production method of the present invention is easy to implement industrially (can be employed on an industrial scale) and is thus extremely practical and useful.

Abstract: The present invention relates to functionalizing agents that are particularly useful for functionalizing living rubbery polymers to make the polymer more compatible with fillers, such as carbon black and silica. These functionalizing agents are comprised of a boron containing compound having a structural formula selected from the group consisting of: wherein R is selected from the group consisting of hydrogen atoms, alkyl groups and aryl groups, wherein R1, R2, and R3 can be the same or different and are selected from the group consisting of alkyl groups, and aryl groups, and wherein R4 represents an alkylene group or a bridging aromatic group.

Abstract: The present invention relates to novel tricyanoborates of the general formula Catn+ [B(CN)3(XR1)]—n, wherein R1 is C1-6 alkyl, C2-6 alkenyl, C6-10 aryl or benzyl; X is oxygen or sulfur; and Catn+ is a cation with n being 1 or 2, which is selected from the group consisting of an inorganic cation and an organic cation; and also their preparation and use.

Abstract: The present invention provides a protein cross-linking inhibitor containing a compound represented by any of the following formulas (1)-(13), or a pharmaceutically acceptable salt thereof: R3—[—X—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(1) R3—[—X—B(ZR1)—Y—]n—R4,??(2) R3—[—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(3) R3—[—X—B(ZR1)—]n—R4,??(4) R3—[—B(ZR2)—W—]n—R4,??(5) R3—X—B(ZR1)-T[B(ZR2)—W—R4]2,??(6) R3—B(OH)2,??(7) R3—B(ZR1)—X—B(ZR2)—R4,??(8) R3—B(R1)—O—B(R2)—R4,??(9) R3—[—X—B(ZR1)—Y—B(ZR2)—]n—R4,??(10) R3—[—X—B(ZR1)—Y—B(ZR2)—W-Q-]n—R4,??(11) R3—[—P—X—B(ZR1)—Y—B(ZR2)—W—]n—R4,??(12) [R3—X—B(ZR1)—Y]2B(ZR2),??(13) wherein each symbol is as defined in the DESCRIPTION.

Abstract: In accordance with aspects of the invention methods of using rhodium hydroquinone catalysts for the conjugate addition of boronic acids are disclosed.

Abstract: Borate salts, a method for the production thereof and methods of their use.

Abstract: Monomers having the formula X1—Ar1-[triarylamine]—Ar2-X2 wherein the triarylamine unit comprises at least one nitrogen atom in the backbone of the monomer and at least three substituted or unsubstituted aryl or heteroaryl groups and wherein X1 and X2 are the same or different polymerizable groups and wherein Ar1 and Ar2 are the same or different substituted or unsubstituted aryl or heteroaryl groups. Polymers and copolymers comprising such monomers are also described. The polymers have particular application in organic optoelectronic devices such as organic electroluminescent devices and organic photovoltaic devices.

Abstract: A process for preparing bisallylboranes of the formula (I) by reacting a diene with sodium borohydride in the presence of an oxidant: in an inert solvent, with the borane generated in situ reacting selectively with the diene to form the bis(allyl)borane of the formula (I) and the substituents R1 to R6 having the following meanings: R114 R6 are H, aryl or substituted or unsubstituted C1-C4-alkyl or two radicals R may be closed to form a cyclic system. As oxidant, it is possible to use, for example, alkyl halides or dialkyl sulfates. In a particularly preferred embodiment, the diene used is 2,5-dimethylhexa-2,4-diene (R1, R2, R5, R6=methyl, R3, R4=H).

Abstract: Disclosed are internally blocked borates useful for polymerizable compositions, and polymerizable adhesives made therewith. The internally blocked borates have general structures: wherein X represents —CHR6—, oxygen or sulfur; n is an integer; R1, R2, R3, R4, R5, and R6 are independently selected, for example, from unsubstituted and substituted C1-C10 alkyl, alkylene groups, or aryl groups, including other embodiments further defined, and M is a counter ion with positive charge m.

Abstract: After a fluoroaryl borane derivative is precipitated from a solution containing the fluoroaryl borane derivative, a bis (fluoroaryl) borane derivative, and a hydrocarbon solvent and is subjected to first filtration so that the fluoroaryl borane derivative is isolated, a filtrate that has been obtained by the first filtration is cooled and the bis (fluoroaryl) borane derivative is separated and is subjected to second filtration so that the bis (fluoroaryl) borane derivative is isolated. In a case where the solution contains fluorobenzene, the solution is concentrated, so that the fluorobenzene is removed. Thus, it is possible to provide the high-purity fluoroaryl borane derivative and bis (fluoroaryl) borane derivative having no impurity with ease and at a low cost.

Abstract: The invention pertains to the use of Group 8 transition metal alkylidene complexes as catalysts for olefin cross-metathesis reactions. In particular, ruthenium and osmium alkylidene complexes substituted with an N-heterocyclic carbene ligand and at least one electron donor ligand in the form of a heterocyclic group are used to catalyze cross-metathesis reactions to provide a olefin products that are directly substituted with an electron-withdrawing group.

Abstract: A novel process for preparing perhalogenated monoorganoboranes or diorganoboranes which makes it possible to obtain these compounds under conditions which can readily be implemented in the industry is described.

Abstract: The present invention relates to a novel class of &agr;-aminoboronic acids of Formula (V), which are useful as intermediates in synthetic processes for inhibitors of the serine proteases, leukocyte elastase, pancreatic elastase, cathepsin G, and chymotrypsin. More specifically, the &agr;-aminoboronic acids are useful as intermediates for the synthesis of Hepatitis C Virus (HCV) protease inhibitors. This invention also generally relates to novel methods for the preparation of &agr;-aminoboronic acids.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: This invention describes a process for covalently coupling organic compounds which comprises reacting an olefinic compound having a halogen or halogen-like substituent at a coupling position with a diboron derivative in the presence of a Group VIII metal catalyst and a suitable base. The invention also describes a process for preparing alkene borate intermediates comprising reacting an olefinic compound having a halogen or halogen-like substituent with a diboron derivative in the presence of a Group VIII metal catalyst and a suitable base.

Abstract: The invention provides a process for covalently coupling organic compounds which comprises reacting an aromatic ring compound having a halogen or halogen-like substituent at a coupling position with a diboron derivative in the presence of a Group VIII metal catalyst and a suitabIe base. The invention also provides useful arylboron intermediates.

Abstract: The invention relates to processes for preparing a compound of the formula and the enantiomer of said compound, wherein the benzoic acid moiety is attached at position 6 or 7 of the chroman ring, and R1, R2, and R3 are as defined herein. The invention further relates to intermediates that are useful in the preparation of the compound of formula X above.

Abstract: The present invention relates to rubber compositions containing borate compounds of the formula wherein R1 and R2 are independently selected from the group consisting of alkoxy radicals having from 1 to 8 carbon atoms; R3 is selected from the group consisting of alkylene groups having from 1 to 15 carbon atoms and arylene and alkyl substituted arylene groups having from 6 to 10 carbon atoms; X is selected from the group consisting of —SH, —SCN, and —NH2; and Y is selected from the group consisting of Sx and Sex where x is an integer of from 1 to 8.

Abstract: The present invention relates to rubber compositions containing borate compounds of the formula wherein R1 and R2 are independently selected from the group consisting of alkoxy radicals having from 1 to 8 carbon atoms; R3 is selected from the group consisting of alkylene groups having from 1 to 15 carbon atoms and arylene and alkyl substituted arylene groups having from 6 to 10 carbon atoms; X is selected from the group consisting of and Y is selected from the group consisting of Sx and Sex where x is an integer of from 1 to 8.

Abstract: Resins and carbon--carbon composites are formed from di(alken-1-yl) borinic acids and borinates, either as monomers or as nonpolymerizing additives in a monomer mixture, with the effect of sharply increasing the oxidative stability of the cured product. The compounds have the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.5 -C.sub.7 cycloalkenyl, aryl, (C.sub.1 -C.sub.6 alkyl)-substituted aryl, (C.sub.2 -C.sub.6 alkenyl)-substituted aryl, or (C.sub.2 -C.sub.6 alkynyl)-substituted aryl, at least one of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 being other than H.

Abstract: Reagents suitable for the modification of a bioactive species for the purpose of incorporating a bifunctional boronic compound complexing moiety for subsequent conjugation to a different (or the same) bioactive species having pendant phenylboronic acid moieties of General Formula 1, ##STR1## wherein group R is an electrophilic or nucleophilic moiety suitable for reaction of the putative bifunctional boronic compound complexing reagent with a bioactive species, wherein group R.sub.2 is selected from one of H and OH moieties, and wherein group R.sub.3 is selected from one of an alkyl and a methylene bearing an electronegative substituent. Group Z is a spacer selected from (CH.sub.2).sub.n and CH.sub.2 O(CH.sub.2 CH.sub.2 O).sub.n.sbsb.2, wherein n is an integer of from 1 to 5, and wherein n.sub.2 is an integer of from 1 to 4. Each of group Z.sub.2 and Z.sub.3 is a spacer selected from CH.sub.2 Ar, CH.sub.2 CONHCH.sub.2 Ar, CH.sub.2 CONH(CH.sub.2).sub.n.sbsb.3 CO--NHCH.sub.2 Ar, and (CH.sub.2).sub.n.sbsb.

Abstract: The present invention relates to rubber compositions containing borate compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of alkoxy radicals having from 1 to 8 carbon atoms; R.sup.3 is selected from the group consisting of alkylene groups having from 1 to 15 carbon atoms and arylene and alkyl substituted arylene groups having from 6 to 10 carbon atoms; X is selected from the group consisting of ##STR2## and Y is selected from the group consisting of S.sub.x and Se.sub.xwhere x is an integer of from 1 to 8.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: This invention relates to electrophilic dipeptide analogs conjugated to an N,N-disubstituted .alpha.-amino acid as inhibitors of trypsin-like serine protease enzymes.

Abstract: The present invention relates to the field of nucleic acid immobilization, purification and detection and, more particularly, to boronic acid modified oligonucleotides and polynucleotides useful in bioconjugation reactions. The modified oligonucleotides and polynucleotides are useful in reactions for the immobilization and purification of macromolecules.

Abstract: A novel process for making compounds of Formula I, ##STR1## wherein X is a leaving group selected from the group Br, Cl, TsO, MsO, and TfO and R is a 1,2-diol, from a compound of Formula II: ##STR2## is described.

Abstract: Compound of formula (I) ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, represent hydrogen or alkyl or alternatively R.sub.1 and R.sub.2 form, with the carbon atom which bears them, cycloalkyl,R.sub.3 represents hydrogen or alkyl, phenyl or benzyl,R.sub.4 represents:optionally substituted amino, optionally substituted amindino, optionally substituted guanidino, optionally substituted isothioureido, optionally substituted iminomethylamino, mercapto substituted with heterocyclic, or heterocyclic,R.sub.5 and R.sub.6 each represent hydrogen or alkyl, or ##STR2## forms a boronic ester of pinanediol, m represents an integer such that 0.ltoreq.m.ltoreq.6,n represents an integer such that 1.ltoreq.n.ltoreq.6,A represents any one of the following groups:* optionally substituted bicycloalkyl (C.sub.5 -C.sub.10)phenyl,* or a group of formula: ##STR3## A.sub.1 represents --CO--, --CS--, --SO.sub.

Abstract: Novel boronic acid and ester and carboxyl-modified amino acid compounds of the Formula I, which are inhibitors of trypsin-like enzymes, are disclosed :R.sup.1 --Z--CHR.sup.2 --A,where R.sup.1, Z, R.sup.2 arid A are defined within.

Abstract: Procedures are disclosed which preclude significant safety hazards in the production of bulk quantities pentafluorophenyl lithium. A pentafluorophenyl compound is reacted with an alkyl lithium compound in a reaction zone, preferably temperature controlled, under conditions such that only a small amount of a predetermined quantity of pentafluorophenyl lithium product is present in the reaction zone at any time. The product may be directly discharged from the reaction zone for combination with another reactant.

Abstract: Novel compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, whereinA is --O--, --S-- or --CR.sup.2 R.sup.8 --;R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, X and Y are specifically defined; andup to one combination of (a) R.sup.2 and R.sup.5, (b) R.sup.5 and R.sup.6, (c) R.sup.5 and R.sup.7, (d) R.sup.6 and R.sup.7, and (e) R.sup.7 and Y, taken together with the atoms to which they are attached, may form a ring, the compounds being useful for treating dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of cognitive impairment, attention deficit disorder, and substance abuse and other addictive behavior disorders.Also disclosed are intermediates and processes useful in the preparation of the above compounds.

Abstract: Novel compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, whereinA is --O--, --S-- or --CR.sup.2 R.sup.8 --;R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, X and Y are specifically defined; andup to one combination of (a) R.sup.2 and R.sup.5, (b) R.sup.5 and R.sup.6, (c) R.sup.5 and R.sup.7, (d) R.sup.6 and R.sup.7, and (e) R.sup.7 and Y, taken together with the atoms to which they are attached, may form a ring, the compounds being useful for treating dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of cognitive impairment, attention deficit disorder, and substance abuse and other addictive behavior disorders.Also disclosed are intermediates and processes useful in the preparation of the above compounds.

Abstract: A process for the preparation of 5-(2,4-difluorophenyl)-salicylic acid comprising the reaction of an organometallic derivative with a suitable substituted benzene in the presence of a transition-metal based catalyst is described.

Abstract: A method for the removal of ester protecting groups from .alpha.-amino boronic acid is disclosed for the preparation of compounds of formula (II) belowR.sup.1 -X.sub.n -NHCH (R.sup.2)-B(OH).sub.

Abstract: The invention relates to a process for the reaction of fluorinated or chlorinated aromatics with electrophiles at the ortho position relative to the fluorine or chlorine atom, characterized in that a strong base is added to a mixture of the fluorinated or chlorinated aromatic and the electrophile.

Abstract: An improved process for preparation of compounds of the formula ##STR1## as disclosed. These compounds are useful as intermediates in the preparation of boronic acid adducts of technetium 99m dioxime complexes of the formula.sup.99m Tc X(Y).sub.3 Zwhich are useful as imaging agents.

Abstract: Improved processes for liberating boronic, RB(OR').sub.2, and borinic, RR'BOR', esters from their "ate" complexes, free of alcohol are provided. Pyrolysis of lithium organylborates LiRB(OR').sub.3 and LiRR'BOR', wherein R is an organyl group and R' is straight or branched-chain lower alkyl, directly yields the relatively volatile boronic and borinic esters in high purity, leaving behind a residue of lithium alkoxide. Treatment of the lithium organylborates with an appropriate acid halide cleanly liberates either volatile or non-volatile boronic or borinic esters, readily separated from the lower alkyl ester produced as a by-product. The novel compound lithium dimethylborohydride is also provided.

Abstract: A process for synthesizing an optically pure ketone comprising the steps of: treating an appropriate optically pure boronic ester with an organolithium compound at -78.degree. C. to obtain the "ate" complex, separating the optically pure borinic ester from the complex and converting said borinic ester into an optically pure ketone represented by the formulae:R*COR.sup.1 and R*COC.tbd.CR.sup.1wherein R* is a chiral organyl moeity and R.sup.1 is an achiral organyl moeity.

Abstract: Sulfur containing diols are reacted with hydroxy boron compounds resulting in the formation of symmetrically balanced compounds which are useful as additives for lubricating oil compositions.

Abstract: Heterocyclic boron compounds of the formula IR.sup.1 --A.sup.1 --Z.sup.1 --A.sup.2 --R.sup.2 (I)can be used as components of liquid-crystal phases. A.sup.1 is --A--, --A.sup.4 --A--, or --A--A.sup.4 -- and A is ##STR1## .