Abstract: Disclosed is a phenyl boronic acid compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aryl group. Z and Z? are independently —O—, —NH— or —S—. X is an electron withdrawing group. R is a substituted or unsubstituted straight chained hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups and Y is —H, an amine, —[NH—(CH2)q]r—NH2, halogen, —CF3, thiol, ammonium, alcohol, —COOH, —SO3H, —OSO3H or phosphonium group covalently bonded to the terminal position of R. Each —NH— in —[NH—(CH2)q]r—NH2 is optionally N-alkylated or N,N-dialkylated and —NH2 in —[NH—CH2)q]r—NH2 is optionally N-alkylated, N,N-dialkylated or N,N,N-trialkylated. q is an integer from 2 to about 10 and r is an integer from 1 to about 5.

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: Orthoborate salts suitable for use as electrolytes in lithium batteries and methods for making the electrolyte salts are provided. The electrolytic salts have one of the formulae (I). In this formula anionic orthoborate groups are capped with two bidentate chelating groups, Y1 and Y2. Certain preferred chelating groups are dibasic acid residues, most preferably oxalyl, malonyl and succinyl, disulfonic acid residues, sulfoacetic acid residues and halo-substituted alkylenes. The salts are soluble in non-aqueous solvents and polymeric gels and are useful components of lithium batteries in electrochemical devices.

Abstract: The structure and preparation of antibiotics incorporating borinic acid complexes are disclosed, especially hydroxyquinoline, imidazole and picolinic acid derivatives, along with compositions of these antibiotics and methods of using the antibiotics and compositions as bactericidal and fungicidal agents as well as therapeutic agents for the treatment of diseases caused by bacteria and fungi.

Abstract: Compounds having enhanced oxidation stability are disclosed. The compounds have an aryl boronic acid residue having one or more electron withdrawing groups on the aromatic moiety which contains the boronic acid residue, such that the molecule has enhanced oxidation resistance as compared to a corresponding molecule without the one or more electron withdrawing groups.

Abstract: A fluorescent monomer compound represented by the following formula (1) is provided: wherein Q, Q? and D3 may be the same or different, may be combined together into a fused ring, and are each a substituent selected from the group consisting of a hydrogen atom, a halogen atom, a hydroxyl group, and substituted or unsubstituted alkyl, acyl, oxyalkyl, carboxyl, carboxylate ester, carboxamido, cyano, nitro, amino and aminoalkyl groups; and D1, D2 and D4 each represent a substituent, wherein at least one of D1, D2 and D4 is a substituent group comprising a vinyl group at an end thereof, and wherein the substituent group comprising a vinyl group at an end thereof enables the fluorescent monomer compound to be soluble in water.

Abstract: The present invention provides solid-phase saccharide dyes. The dyes are bisboronic acids covalently bonded to a solid substrate. The dyes selectively conjugate with saccharides, particularly glucose, and register a signal. The signal is proportional to the quantity of saccharide. Thus, the dyes of the present invention are useful for measuring and monitoring saccharide levels, particularly in biological fluids such as blood.

Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.

Abstract: A process for producing organic substituted aromatic or heteroaromatic compounds including biaryl and biheteroaryl compounds in a two-step reaction. In the first step, the aromatic or heteroaromatic compound is borylated in a reaction comprising a borane or diborane reagent (any boron reagent where the boron reagent contains a B—H, B—B or B—Si bond) and an iridium or rhodium catalytic complex. In the second step, a metal catalyst catalyzes the formation of the organic substituted aromatic or heteroaromatic compound from the borylated compound and an electrophile such as an aryl or organic halide, triflate (OSO2CF3), or nonaflate (OSO2C4F9). The steps in the process can be performed in a single reaction vessel or in separate reaction vessels. The present invention also provides a process for synthesis of complex polyphenylenes starting from halogenated aromatic compounds.

Abstract: The present invention provides process useful for the preparation of intermediates which are useful in the preparation of amino acids useful in preparing peptide receptor modulators, for example agonists or partial agonists of such peptide receptors. Such peptide receptor modulators include, for example glucagon like peptide-1 receptor modulators which are useful for the amelioration of the diabetic condition.

Abstract: The invention relates to a process for the preparation of organic boronic acid derivatives involving the reaction of an organic compound with diboronic acid in the presence of a Group 8-11 metal catalyst.

Abstract: The liquid ethereal medium or liquid hydrocarbyl medium of a solution or slurry of an alkali metal tetrakis(Faryl)borate is substituted with at least one halogenated hydrocarbon, without isolating the alkali metal tetrakis(Faryl)borate, to form a new slurry or solution. At least a portion of the new solution is mixed together with a salt selected from a) a protic ammonium salt, b) an onium salt, and c) a triarylmethyl salt, to produce a protic ammonium tetrakis(Faryl)borate, an onium tetrakis(Faryl)borate, or a triarylmethyl tetrakis(Faryl)borate.

Abstract: Disclosed is a phenyl boronic acid compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aryl group. Z and Z? are independently —O—. —NH— or —S—. X is an electron withdrawing group. R is a substituted or unsubstituted straight chained hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups and Y is —H, an amine, —[NH—(CH2)q]r—NH2, halogen, —CF3, thiol, ammonium, alcohol, —COOH, —SO3H, —OSO3H or phosphonium group covalently bonded to the terminal position of R. Each —NH— in —[NH—(CH2)q]r—NH2 is optionally N-alkylated or N,N-dialkylated and —NH2 in —[NH—(CH2)q]r—NH2 is optionally N-alkylated, N,N-dialkylated or N,N,N-trialkylated. q is an integer from 2 to about 10 and r is an integer from 1 to about 5.

Abstract: The invention relates to processes for preparing a compound of the formula (V) and alkyl boronic esters thereof wherein R1 is attached at the 2 or 3 position of the benzene ring, R2 is attached at the 5 or 6 position, and R1, R2 and G are as defined herein. Said compound is a key synthetic intermediate in the preparation of 2-amino-6-(substituted-4-phenoxy)-substituted-pyridines useful as nitric oxide synthase (NOS) inhibitors in a mammal.

Abstract: Disclosed are derivatives of 2-{[N-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl]-amino}-alkylboronic acid, processes for the preparation of such compounds, pharmaceutical preparations, and the use of such derivatives in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans

Abstract: The present invention relates to halo sulfonyl aryl boronates of the general formula (I): wherein Arylene designates a carbocyclic or heterocyclic, aromatic ring system comprising 1-3 rings; R1, R2 and R3 are, independently, hydrogen, C1-6alkyl, C1-6alkoxy, halogen, nitro, cyano or phenyl; X is fluoro, chloro or bromo; and Y is a boroxine moiety attached via a bond from Arylene to one of the boron atoms of a boroxine ring which ring has a group of the formula -Arylene(R1)(R2)(R3)SO2X, wherein Arylene, R1, R2, R3 and X are as defined above, at each of the other two boron atoms of the boroxine ring, or Y is a boronic acid group or a boronic ester group. The invention also relates to the preparation of the compounds of formula (I) and to their use in organic synthesis.

Abstract: A process for producing organic substituted aromatic or heteroaromatic compounds including biaryl and biheteroaryl compounds in a two-step reaction. In the first step, the aromatic or heteroaromatic compound is borylated in a reaction comprising a borane or diborane reagent (any boron reagent where the boron reagent contains a B—H, B—B or B—Si bond) and an iridium or rhodium catalytic complex. In the second step, a metal catalyst catalyzes the formation of the organic substituted aromatic or heteroaromatic compound from the borylated compound and an electrophile such as an aryl or organic halide, triflate (OSO2CF3), or nonaflate (OSO2C4F9). The steps in the process can be performed in a single reaction vessel or in separate reaction vessels. The present invention also provides a process for synthesis of complex polyphenylenes starting from halogenated aromatic compounds.

Abstract: Disclosed is a phenyl boronic acid compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aryl group. Z and Z? are independently —O—. —NH— or —S—. X is an electron withdrawing group. R is a substituted or unsubstituted straight chained hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups and Y is —H, an amine, —[NH—(CH2)q]r—NH2, halogen, —CF3, thiol ammonium, alcohol, —COOH, —SO3H, —OSO3H or phosphonium group covalently bonded to the terminal position of R. Each —NH— in —[NH—(CH2)q]r—NH2 is optionally N-alkylated or N,N-dialkylated and —NH2 in —[NH—(CH2)q]r—NH2 is optionally N-alkylated, N,N-dialkylated or N,N,N-trialkylated. q is an integer from 2 to about 10 and r is an integer from 1 to about 5.

Abstract: A process for preparing formylphenylboronic acids of the formula (I) by reaction of protected chlorobenzaldehydes of the formula (II) with lithium in an inert solvent to form compounds of the formula (III) and subsequent reaction with a boron compound of the formula BY3 to give compounds of the formula (I).

Abstract: The liquid ethereal medium or liquid hydrocarbyl medium of a solution or slurry of an alkali metal tetrakis(Faryl)borate is substituted with at least one halogenated hydrocarbon, without isolating the alkali metal tetrakis(Faryl)borate, to form a new slurry or solution. At least a portion of the new solution is mixed together with a salt selected from a) a protic ammonium salt, b) an onium salt, and c) a triarylmethyl salt, to produce a protic ammonium tetrakis(Faryl)borate, an onium tetrakis(Faryl)borate, or a triarylmethyl tetrakis(Faryl)borate.

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 relates to a process for the preparation of an organic boronic acid derivative comprising reacting a penta- or hexa-substituted diboron derivative with an organic compound having a halogen or halogen-like substituent at a coupling position in the presence of a Group VIII metal catalyst, such that a direct carbon to boron bond is formed between said coupling position and a boron-containing residue of the penta- or hexa-substituted diboron derivative.

Abstract: This invention provides novel compounds derived from a marine sponge, Adocia sp., that specifically modulat kinesin activity by targeting the kinesin motor domain and mimicking the activity a microtubule. The compounds act as potent anti-mitogens are useful in a wide variety of in vitro and in vivo applications.

Abstract: The present invention relates to therapeutically active novel aminoindanes of formula (I). Also provided is a method of preparing compounds of formula (I), and pharmaceutical compositions comprising the compounds. The novel compounds act as modulators of metabotropic glutamate receptors and, as such, are useful in treating diseases of the central nervous system related to the metabotropic glutamate receptor system.

Abstract: Thee present invention relates to therapeutically active cubane compounds, a method of preparing the same, and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in creating diseases of the central nervous system related to the metabotropic glutamate receptor system.

Abstract: The invention relates to a method for producing 2- and 2,5-substituted derivatives of 4-(trifluoromethyl)-phenol and 4-(2-trifluoromethyl)-phenyl)-2-tetrahydropyranyl) ether and to novel derivatives. Said method is characterised in that a compound of formula (2) 4-(trifluoromethylphenyl)-2-(tetrahydropyranyl) ether is reacted with an electrophile E-X or a combination of electrophiles E-X and E-Y in the presence of a base, X and Y having the meanings given in the description.

Abstract: The present invention relates to therapeutically active novel spiro[2,4]heptane amino carboxy compounds and derivatives thereof. Also provided is a method of preparing compounds of Formula (I), and pharmaceutical compositions comprising the compounds. The novel compounds act as modulators of metabotropic glutamate receptors and, as such, are useful in treating diseases of the central nervous system related to the metabotropic glutamate receptor system.

Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.

Abstract: Compositions and methods for inhibiting arginase activity, including arginase activity in a mammal, are provided. Methods of making the compositions of the invention are also provided as are methods of using the compositions therapeutically. The compositions described herein are useful for alleviating or inhibiting a variety of arinase- and NO synthase-related disorders, including heart disease, gastrointestinal motility disorders, and penile erectile dysfunction in humans.

Abstract: The present invention provides stable compounds prepared from boronic acid and lyophilized compounds thereof of the formula (1): in which Z1 and Z2 are moieties derived from sugar. The invention also provides methods for preparing such compounds. Lyophilizing a mixture comprising a boronic acid compound and a moiety derived from sugar produces a stable composition that readily releases the boronic acid compound upon reconstitution in aqueous media.

Abstract: A process for preparing formylphenylboronic acids of the formula (I) by reaction of protected chlorobenzaldehydes of the formula (II) with lithium in an inert solvent to form compounds of the formula (III) and subsequent reaction with a boron compound of the formula BY3 to give compounds of the formula (I).

Abstract: The invention relates to processes for preparing a compound of the formula (V) 1

Abstract: The invention relates to a process for the preparation of organic boronic acid derivatives involving the reaction of an organic compound with diboronic acid in the presence of a Group 8-11 metal catalyst.

Abstract: A reagent having the general formula of General Formula I: wherein group Z comprises a spacer selected from an aliphatic chain up to about 6 carbon equivalents in length, an unbranched aliphatic chain of from about 6 to 18 carbon equivalents in length with at least one of an intermediate amide and a disulfide moiety, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; wherein group R is an electrophilic or nucleophilic moiety suitable for reaction of the reagent with a biologically active species; and wherein group Q is one of nothing at all, an amide, a methyl amide, a methylene, an ether, a thioether, a methyl ether, and a methyl thioether moiety. Also, a conjugate, a bioconjugate and a method of conjugating.

Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and and methods for their use.

Abstract: The invention relates to a process for the preparation of organic boronic acid derivatives involving the reaction of an organic compound with diboronic acid in the presence of a Group 8-11 metal catalyst.

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 related to heterobifunctional cross-linkers substituted by a cell surface binding group or a cell recognising group, and also by a bio-active group, the bio-active group attached to a carbonyl of the cross-linker by an acid labile bond. Examples of suitable bio-active groups include an immunomodulator and an anti-neoplastic group. The conjugate enables, for example, the coupling of immunomodulators ex vivo to a target cell, for example a tumor antigen presenting cell. The conjugate can act as a non-toxic prodrug carrying a cytotoxin, for example, to a target tissue site, where the pH-dependency of the labile amide bond provides for cell selectivity of the masked cytotoxin. The invention further relates to a method for producing the cross-linkers, their use in treating disease, and ex-vivo cell labeling.

Abstract: A process for producing organic substituted aromatic or heteroaromatic compounds including biaryl and biheteroaryl compounds in a two-step reaction. In the first step, the aromatic or heteroaromatic compound is borylated in a reaction comprising a borane or diborane reagent (any boron reagent where the boron reagent contains a B—H, B—B or B—Si bond) and an iridium or rhodium catalytic complex. In the second step, a metal catalyst catalyzes the formation of the organic substituted aromatic or heteroaromatic compound from the borylated compound and an electrophile such as an aryl or organic halide, triflate (OSO2CF3), or nonaflate (OSO2C4F9). The steps in the process can be performed in a single reaction vessel or in separate reaction vessels. The present invention also provides a process for synthesis of complex polyphenylenes starting from halogenated aromatic compounds.

Abstract: Compounds of the formula (I) in which Q1 and Q2 are each OH or form a trimeric boric anhydride, Z is CHO, CH2Y, X or a protected aldehyde group, and X is CN, COOH, COCl, CONH2 or C(OR)3, and Y is OH or NH2, and Z is in the o-, m- or p-position to the boronic acid radical, are prepared by a) reacting a compound of the formula (II)  with Mg in the presence of an anthracene compound and, if desired, a transition-metal halide and, if desired, an Mg halide or in the presence of a transition-metal halide and, if desired, an Mg halide, to give the corresponding arylmagnesium chloride, b) reacting the latter with a borate of the formula B(OR′)3 and hydrolyzing the product, with removal of the aldehyde protecting group, c) and, if desired, oxidizing or reducing the free aldehyde group.

Abstract: Process for preparing arylboron and alkylboron compounds of the formulae (II) and (III) by reacting arylmagnesium and alkylmagnesium halides of the formula (I) with boron compounds in microreactors in accordance with equation I or equation II, 1

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 process for purifying formylphenylboronic acids of the formula (I) 1

Abstract: The invention provides novel solid supports comprising dihydroxyalkyl aminoalkyl and dihydroxyalkylaminobenzyl groups, and methods for making and using them. The supports are particularly useful for immobilizing and derivatizing functionalized boronic acids for use in solid phase synthesis, such as those used in combinatorial chemistries. The compositions and methods of the invention are also useful as scavenger solid supports, e.g., in solution-phase parallel synthesis of small molecule libraries, and for use in resin-to-resin transfer reactions via phase transfer of solid supported boronic acids under both aqueous and anhydrous conditions. The methods of the invention provide convergent solid-phase synthesis of symmetrically or unsymmetrically functionalized compounds, such as biphenyl compounds. Also provided are synthesizer devices, e.g., semiautomated parallel synthesizers.

Abstract: Compositions and methods for inhibiting arginase activity, including arginase activity in a mammal, are provided. Methods of making the compositions of the invention are also provided as are methods of using the compositions therapeutically. The compositions described herein are useful for alleviating or inhibiting a variety of arinase- and NO synthase-related disorders, including heart diseae, gastrointestinal motility disorders, and penile erectile dysfunction in humans.

Abstract: The invention relates to a process for the preparation of an organic boronic acid derivative comprising reacting a penta- or hexa-substituted diboron derivative with an organic compound having a halogen or halogen-like substituent at a coupling position in the presence of a Group VIII metal catalyst, such that a direct carbon to boron bond is formed between said coupling position and a boron-containing residue of the penta- or hexa-substituted diboron derivative.

Abstract: A process for preparing boronic acids of the formula (I) and borinic acids of the formula (II), 1

Abstract: The invention relates to a process for the preparation of organic boronic acid derivatives involving the reaction of an organic compound with diboronic acid in the presence of a Group 8-11 metal catalyst.

Abstract: Reagents suitable for the modification of a bioactive species for the purpose of incorporating one or more phenyldiboronic acid (PDBA) moieties for subsequent conjugation to a different (or the same) bioactive species having one or more pendant boronic compound complexing moieties of the general formula of General Formula I, wherein group R is a reactive electrophilic or nucleophilic moiety suitable for reaction of the PDBA reagent with a bioactive species. Group Z is a spacer selected from a saturated or unsaturated chain up to about 0 to 6 carbon equivalents in length, an unbranched saturated or unsaturated chain of from about 6 to 18 carbon equivalents in length with at least one intermediate amide or disulfide moiety, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length. Group Q is a linkage that includes one of amide, ether and thioether moieties.

Abstract: The invention relates to a process for the preparation of organic boronic acid derivatives involving the reaction of an organic compound with diboronic acid in the presence of a Group 8-11 metal catalyst.