Abstract: The present invention relates to an isoquinoline compound represented by the following formula (I), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water adduct thereof, a hydrate thereof and a solvate thereof, as well as an agent for the prophylaxis and/or treatment of a disease caused by hyperreactivity of poly(ADP-ribose)polymerase, containing the compound, and a poly(ADP-ribose)polymerase inhibitor containing the compound. In addition, this compound is useful as an agent for the prophylaxis and/or treatment of cerebral infarction, particularly as an agent for the prophylaxis and/or treatment of acute cerebral infarction. Furthermore, this compound is useful as a prophylactic and/or therapeutic agent that improves neurological symptoms associated with cerebral infarction, particularly acute cerebral infarction. wherein the symbols are the same as defined in the description.

Abstract: The invention provides epoxy and oxetane compositions including the novel acyloxy and N-acyl curing agents described herein. Use of invention curing agents result in cured adhesive compositions with remarkably increased adhesion and reduced hydrophilicity when compared to resins cured with other types of curing agents. Furthermore, the curatives of this invention do not interfere with free-radical cure and are thus suited for use in hybrid cure thermoset compositions.

Abstract: The invention provides improved crosslinkers which permit more efficient determination of protein interactions in biological samples.

Abstract: Devices, compositions, and methods are described which provide a tubular nanostructure targeted to a lipid bilayer membrane. The targeted tubular nanostructure can have a surface region configured to pass through a lipid bilayer membrane of a cell, a hydrophobic surface region flanked by two hydrophilic surface regions configured to form a pore in a lipid bilayer membrane of a cellular organelle, and at least one ligand configured to bind one or more cognates on the lipid bilayer membrane of the cellular organelle. The target cell can be, for example, a tumor cell, an infected cell, or a diseased cell in a subject. The tubular nanostructure can form a pore in the lipid bilayer membrane of the cellular organelle, e.g., mitochondria, which can permit transit or translocation of at least one compound across the membrane and cause cell death of the target cell.

Abstract: An oil-soluble lubricating oil additive composition prepared by the process which comprises (A) reacting a copolymer of an (i) an unsaturated acidic reagent; and (ii) a mono-olefin, with at least one linking hydrocarbyl di-primary amine, thereby producing a hybrid succinic anhydride copolymer having from about 10% to about 90% unreacted anhydride groups; and subsequently (B) reacting the hybrid succinic anhydride copolymer with a second amine compound, thereby producing the succinimide.

Abstract: The invention includes methods of processing an initial di-carbonyl compound by conversion to a cyclic compound. The cyclic compound is reacted with an alkylating agent to form a derivative having an alkylated ring nitrogen. The invention encompasses a method of producing an N-alkyl product. Ammonia content of a solution is adjusted to produce a ratio of ammonia to di-carboxylate compound of from about 1:1 to about 1.5:1. An alkylating agent is added and the initial compound is alkylated and cyclized. The invention includes methods of making N-methylpyrrolidinone (NMP). Aqueous ammonia and succinate is introduced into a vessel and ammonia is adjusted to provide a ratio of ammonia to succinate of less than 2:1. A methylating agent is reacted with succinate at a temperature of from greater than 100° C. to about 400° C. to produce N-methyl succinimide which is purified and hydrogenated to form NMP.

Abstract: The present invention relates to novel compounds from Antrodia camphorata and the use thereof.

Abstract: The present disclosure relates to a compound of the formula I or a tribologically acceptable salt, solvate, hydrate, or proadditive thereof, wherein R1, R2 and R4 are as defined herein. Such novel pyrrolidine, or succinimide, derivatives may be useful as friction modifiers in lubricant compositions. This disclosure also relates to a method of using such friction modifier compounds in lubricating fluid formulations to lubricate machine parts, including gear, axle, engine, and transmission parts, and to lubricant compositions containing such friction modifier compounds.

Abstract: Compounds isolated from the fruiting body of A. camphorata in a solid culture or pharmaceutically acceptable salts thereof, which exhibit immunostimulatory or anti-inflammatory effects. Also disclosed are methods of stimulating immune responses and/or treating an inflammatory disorder with these compounds or pharmaceutically acceptable salts thereof.

Abstract: To provide a compound which has a higher vulcanization efficiency and superior heat aging resistance compared to conventional compounding agents for rubber compositions and which is environmentally friendly. An amine salt compound of a carboxylic acid containing a thermal dissociation portion having the Formula (I): wherein R represents an organic group selected from a C1 to C20 alkyl group, a C3 to C10 cycloalkyl group, a C6 to C20 aryl group and a C7 to C30 alkaryl group, R1, R2 and R3 independently represent a hydrogen atom or a C1 to C20 organic group which may have a heteroatom and/or a substituent group and X represents a C2 to C20 organic group which may have a heteroatom and/or a substituent group and a compounding agent for rubber vulcanization and a rubber composition containing the same.

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

Abstract: This invention provides a method for preparing, in high purity and high yield, heterobifunctional derivatives of poly(ethylene glycol) or related polymers. A chromatographic purification step is not necessary in the method. In accordance with the method of the invention, an intermediate polymer having a formula of W-Poly-OH is provided bearing a removable group W at one terminus. The intermediate polymer W-Poly-OH is first altered by modifying the OH group to a first functional group X, followed by the removal of W to generate a second hydroxyl group. The latter hydroxyl group may then be further converted to a second functional group Y, thus providing the desired heterobifunctional derivative.

Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.

Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: The present invention is directed to the preparation of novel compounds useful in the treatment of hyperlipidemia, arteriosclerosis, hypercholesterolemia, and other related metabolic disorders. More specifically, the present invention is a novel process for the preparation of 1,4-diphenylazetidinone derivatives from ?-substituted amino amides which are protected in the presence of silylating agents and at least one cyclization catalyst whose structural formula is represented by one of the general formula: wherein the various R-groups are defined herein.

Abstract: Disclosed herein is a compound having a structure Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: Coupling reactions, suitable for use in organic or aqueous media, are performed by contacting a 1,2,4,5-tetrazine with a dienophile. The dienophile may be covalently bonded to a protein, and the coupling reaction may be performed in biological media such as those containing cells or cell lysates. The reactions may be performed in the presence of primary amines, thiols, acetylenes, azides, phosphines, and products of Staudinger and/or Sharpless-Huisgen reactions Novel 3-substituted cyclopropene compounds and trans-cyclooctenes are exemplary dienophiles for these reactions.

Abstract: A compound comprising or a pharmaceutically acceptable salt, prodrug, or a metabolite thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed.

Abstract: The present invention provides a novel ?-sulfonimide compound having at least one imide group and at least one sulfonyl group and a method for preparing the same.

Abstract: A monomer with a chromophore group represented by Formula (I): wherein AR1 represents a substituted or unsubstituted aromatic group; AR2 represents a substituted or unsubstituted aromatic group or a substituted or unsubstituted alkyl group; and R represents a substituted or unsubstituted alkyl group, with the proviso that one of R, AR1, and AR2 has a substituent with a polymerizable functional group. The monomer can be advantageously used to prepare polymeric dispersants for pigment dispersion, especially inkjet inks.

Abstract: To provide a compound which has a higher vulcanization efficiency and superior heat aging resistance compared to conventional compounding agents for rubber compositions and which is environmentally friendly. An amine salt compound of a carboxylic acid containing a thermal dissociation portion having the Formula (I): wherein R represents an organic group selected from a C1 to C20 alkyl group, a C3 to C10 cycloalkyl group, a C6 to C20 aryl group and a C7 to C30 alkaryl group, R1, R2 and R3 independently represent a hydrogen atom or a C1 to C20 organic group which may have a heteroatom and/or a substituent group and X represents a C2 to C20 organic group which may have a heteroatom and/or a substituent group and a compounding agent for rubber vulcanization and a rubber composition containing the same.

Abstract: The invention relates to compounds of formula (I): wherein substituents are as defined.

Abstract: Compounds of methamphetamine derivatives having a meta-substituted alkyl linker on the benzene ring and a protective group on the nitrogen of the methamphetamine hapten. Such compounds have the structure wherein R1 is an alkyl linker comprising 2-15 carbon atoms and 0-6 heteroatoms, R2 is a leaving group, and R3 is a protecting group.

Abstract: A novel cationic bleach activator having an enhanced hydrolytic stability is provided. The novel cationic bleach activator also leads to a reduction in strength loss of cotton fibers compared to conventional hot peroxide bleaching, and achieves this reduction in strength loss without a loss of whiteness. Bleaching compositions and detergent compositions comprising the novel cationic bleach activator also are provided. A method of bleaching cellulosic fibers, such as cotton fibers, and a method for removing a stain or discoloration from an article are further provided.

Abstract: Multi-armed functional polyethylene glycol polymers with active terminal groups may be used in conjugation with small molecule pharmaceuticals, proteins and peptides to enhance half-life and bioavailability of the drug and improve solubility, stability and immunological competence.

Abstract: A reaction product comprising an adduct of a mid-range vinylidene content PIB polymer composition and maleic anhydride, a phenolic compound or a compound having a reactive site for subsequent amination. The PIB composition comprises a relatively low molecular weight, mid-range vinylidene content PIB polymer product wherein at least about 90% of the PIB molecules present in the product comprise alpha or beta position isomers. The vinylidene (alpha) isomer content of the product may range from 20% to 70% thereof and the content of tetra-substituted internal double bonds is very low, preferably less than about 5% and ideally less than about 1–2%. The mid-range vinylidene content PIB polymer products may be prepared employing a liquid phase polymerization process conducted in a loop reactor at a temperature of at least 60° F. using a BF3/methanol catalyst complex and a contact time of no more than 4 minutes.

Abstract: This invention relates to novel N-linked sulfonamides of N-heterocyclic carboxylic acid and carboxylic acid isosteres, their preparation, and use for treating neurological disorders including physically damaged nerves and neurodegenerative diseases, and for treating alopecia and promoting hair growth.

Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.

Abstract: This invention relates to a process for producing 5-methyl-N-alkyl-2-pyrrolidone by a) reacting ?-angelica lactone with alkyl amines and b) hydrogenating the products of step (a) in the presence of a metal catalyst, which is optionally supported.

Abstract: The present invention describes carbamic acid ester-derived and valeric acid ester-derived polyfunctional cross-linker molecules, and methods for their synthesis and use. The inclusion of polymeric moieties such as poly(alkylene oxide) in the cross-linkers of the present invention can provide advantageous solubility properties in aqueous environments. Such cross-linkers may be used to form conjugates for use in a variety of assay formats.

Abstract: The present invention is directed to maleimides and preparation of compounds of the formula I wherein R1 and R2 independently from each other stand for variously substituted, and R3 stands for allyl, variously substituted, with the proviso, that R1 and R2 not simultaneously stand for phenyl.

Abstract: Novel compounds of the formula I in which X, Y, Z, R, R1, R2 and R3 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of tromboembolic diseases and for the treatment of tumors

Abstract: Method for separating reaction product from imide compound catalyst represented by Formula (1) or derivative thereof in reaction mixture obtained by reaction in presence of imide compound catalyst: wherein R1 and R2 are each, for example, a hydrogen atom or an alkyl group, where R1 and R2 may be combined to form a double bond, an aromatic ring, or a non-aromatic ring, and X is an oxygen atom or a hydroxyl group. The method includes an extraction process using two organic solvents separable from each other to thereby separate the reaction product into one organic solvent layer and the imide compound catalyst component into the other organic solvent layer. The disclosed method efficiently and simply separates the reaction product from the catalyst component.

Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.

Abstract: The present invention describes carbamic acid ester-derived and valeric acid ester-derived polyfunctional cross-linker molecules, and methods for their synthesis and use. The inclusion of polymeric moieties such as poly(alkylene oxide) in the cross-linkers of the present invention can provide advantageous solubility properties in aqueous environments. Such cross-linkers may be used to form conjugates for use in a variety of assay formats.

Abstract: The present invention relates to novel hexa-arm polyethylene glycol (6-arm PEG) and its derivatives. The core of 6-arm PEG derivatives is sorbitol and the end groups can be derivatized into many different reactive functionalities that are useful in conjugating with many different targets. The present invention also provides a biodegradable polymeric hydrogel-forming composition comprising the 6-arm PEG and its derivatives, and methods of using such 6-arm PEG derivatives as surgical or biological implants or sealants.

Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.

Abstract: The invention relates to compounds of Formula (I), to processes for their preparation and pharmaceutical compositions thereof, that inhibit the Ras farnesyl-protein transferase enzyme (FPTase), and may be used as an alternative to, or in conjunction with, traditional cancer therapy for the treatment of ras oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.

Abstract: The invention relates to compounds of Formula (I), to processes for their preparation and pharmaceutical compositions thereof, that inhibit the Ras farnesyl-protein transferase enzyme (FPTase), and may be used as an alternative to, or in conjunction with, traditional cancer therapy for the treatment of ras oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.

Abstract: Imido and Amido substituted alkanohydroxamic acids reduce the levels of TNFa and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.

Abstract: Compounds of general formula (I): 1

Abstract: In accordance with the present invention, there are provided thermosetting resin compositions with a reduced propensity to shrink in volume upon cure and methods of use therefor. The compositions of the present invention include compounds having aromatic, rigid-rod like spacer groups between the crosslinkable moieties. As such, these compounds impart a degree of liquid crystal-like character to the thermosetting resin composition which results in lower shrinkage upon cure. This effect follows from the well-known expansion that occurs when liquid crystal-like materials pass from a nematic liquid crystal-like state to an isotropic state. Further provided by the present invention are low shrinkage die attach pastes and methods of use therefor.

Abstract: The invention provides heterobifunctional cross-linking reagents and methods of using the cross-linking reagents. The cross-linking reagents of the invention combine a nucleophilic hydrazide residue with an electrophilic maleimide residue allowing coupling of aldehydes to free thiols. In the methods of the invention, human immunodeficiency virus (HIV) infected cells can be detected using conjugates that include CD4 molecules conjugated to detectable markers via the disclosed cross-linking reagents.

Abstract: Processes for preparing N-methyl-L-alanine derivatives and novel intermediates of the process. The derivatives and intermediates are useful for preparing cell-binding agent/maytansinoid complexes.

Abstract: The invention relates to compounds of Formula (I), to processes for their preparation and pharmaceutical compositions thereof, that inhibit the Ras farnesyl-protein transferase enzyme (FPTase), and may be used as an alternative to, or in conjunction with, traditional cancer therapy for the treatment of ras oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.

Abstract: Phenoxy- and thiophenoxyacrylic acid compounds of the formula I in which Het, R1, R2, R3, V, W and Z are as defined in claim 1 and processes for their preparation, intermediates for their preparation, herbicidally active compositions comprising the compounds of the formula I and a method for controlling harmful fungi are described.

Abstract: There is disclosed substituted thiocarboxamides compounds of the formula (I): wherein R1, R2, R3 and Z are as defined in the specification. The compounds are useful as herbicides.

Abstract: This invention provides water-based compositions, particularly coating, ink, fountain solution, adhesive, agricultural and electronics cleaning compositions, manifesting reduced equilibrium surface tension by the incorporation of a surface tension reducing amount of an N-alkylimide of tartaric acid and/or an N-alkylimide of malic acid of the following structures, respectively: where R1 is a C5 to C10 alkyl group.

Abstract: A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I with an alkylating agent of structure III in the presence of a basic catalyst in an aprotic reaction medium. The ureide may be a 5,5-disubstituted barbituric acid, or it may be phenytoin, glutethimide, and ethosuximide. The alkylating agent is an ester of a sulfonic acid. The base may be a hydride or amine. A preferred process comprises N-alkoxyalkylating 5,5-diphenyl-barbituric acid with methoxymethyl methanesulfonate in the presence of di-isopropyl ethyl amine and isolating the resultant N,N?-bismethoxymethyl-5,5-diphenyl-barbituric acid. The invention also contemplates the novel compounds N-methoxymethyl-5,5-diphenylbarbituric acid, N-methoxymethyl ethosuximide, and N-methoxymethyl glutethimide, and a method comprising administering them to a patient.

Abstract: In the presence of an imide compound (e.g., N-hydroxyphthalimide) shown by the formula (2): wherein R1 and R2 independently represents a hydrogen atom, a halogen atom, an alkyl group, an aryl group, a cycloalkyl group; or R1 and R2 may bond together to form a double bond or an aromatic or non-aromatic ring; Y is O or OH and n=1 to 3; or the imide compound and a co-catalyst (e.g., a transition metal compound), an adamantane derivative having a functional group such as a nitro group, an amino group, a hydroxyl group, a carboxyl group, a hydroxymethyl group and an isocyanato group is oxidized with oxygen. According to the above method, an adamantane derivative having a hydroxyl group together with a functional group such as a nitro group, an amino group, a hydroxyl group, a carboxyl group, a hydroxymethyl group and an isocyanato group is efficiently obtained.