Abstract: The present invention provides methods for labeling One or two oxygen atom(s) in a carboxyl group of a carboxyl-containing compound with an oxygen isotope selected from oxygen-17 (17O) or oxygen-18 (18O). The methods of the present invention are characterized in that an activated ester of the carboxyl-containing compound (carboxylic acid) is reacted with H217O or H218O in the presence of an activator. In the methods of the present invention, the reaction between the activated ester of a carboxylic acid and H217O or H218O can be allowed to proceed without including drastic conditions such as strongly acidic conditions or alkaline hydrolysis because an activator is used.

Abstract: The present invention provides kinase inhibitors of Formula (I)

Abstract: Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.

Abstract: Disclosed are novel colorant compounds which contain one or more ethylenically-unsaturated (vinyl), photopolymerizable radicals which may be copolymewrized (or cured) with ethylenically-unsaturated monomers to produce colored compositions such as colored acrylic coatings and polymers, e.g., coatings and polymers produced from acrylate and methacrylate esters, colored polystyrenes, and similar colored polymeric materials derived from other ethylenically-unsaturated monomers. The present invention also pertains to processes for the preparation of certain of the photopolymerizable colorant compounds.

Abstract: The present invention relates to a maleimide group-containing polymer particle containing a crosslinked polymer particle containing a group represented by the following formula (1) and to a method of producing the maleimide group-containing crosslinked polymer particle by reacting hydroxymethylmaleimide with a hydroxyl group-containing polymer particle obtained by introducing a polyethylene glycol into a crosslinked polymer particle: wherein n denotes an integer of 1 or more.

Abstract: The present invention relates to bottom antireflective coating compositions and polymers useful in making such compositions.

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: The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated by integrin receptors, such as a ?v?3, ?v?5, ?v?6, ?5?1 and the like. The invention encompasses novel compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of such diseases and disorders. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: A method for the treatment of conditions associated with a need for inhibition of GSK-3, such as diabetes, dementias such as Alzheimer's disease and manic depression which method comprises the administration of a pharmaceutically effective, non-toxic amount of a compound of formula (I): or a pharmaceutically acceptable derivative thereof, wherein: R is hydrogen, alkyl, aryl, or aralkyl; R1 is hydrogen, alkyl, aralkyl, hydroxyalkyl or alkoxyalkyl; R2 is substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; R3 is hydrogen, substituted or unsubstituted alkyl, cycloalkyl, alkoxyalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl or aralkyl wherein the aryl moiety is substituted or unsubstituted; or, R1 and R3 together with the nitrogen to which they are attached form a single or fused, optionally substituted, saturated or unsaturated heterocylic ring; to a human or non-human mammal in need thereof, and compounds of formula I.

Abstract: Novel substituted pyrrolidine-2,3,4-trione compounds of formula I and methods for preparing the compounds. Also disclosed are pharmarceutical compositions comprising the compounds and methods of using the compounds for treating pain, anxiety and various other diseases or conditions.

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 present invention provides a thiocarbonylthio compound represented by formula (I) 1

Abstract: Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity.

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: Disclosed is a method of inhibiting anandamide amidase in an individual or animal and novel inhibitors of anandamide amidase. The disclosed method and novel compounds can be used to reduce pain in an individual or animal suffering from pain, reducing nausea in an individual undergoing chemotherapy, for example cancer chemotherapy, suppressing appetite in an individual, reducing intraocular pressure in the eye of an individual or animal suffering from glaucoma and suppressing the immune system in an individual with an organ transplant.

Abstract: The subject matter of the invention are new xanthene derivatives of the formula I, wherein R1,R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and X, Y, are as defined herein. The compounds according to the invention provide molecules that are—due to their spectral properties (absorption maxima in the range of approx. 650 nm and above as well as emission maxima above 670 nm)—very suitable for the use as dyes and in particular as fluorescence dyes. The compounds of the formula I according to the invention are used for the production of fluorescence conjugates, for their application in immunoassays, for DNA analytics, for in-vivo diagnostics or as a laser dye.

Abstract: Succinimide-acid compounds prepared by reaction of hydrocarbyl-substituted succinic acylating agents with alpha-omega amino acids are disclosed, as well as derivatives thereof useful as lubricity additives, lubricant dispersants, friction modifiers, liquid hydrocarbonaceous fuel detergents, antioxidants and alkali and/or alkaline-earth metal detergents.

Abstract: The present invention relates to novel active substances (coniosetin and coniosetin derivatives) of the formula I 1

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: Compounds represented by general formula (1) or salts thereof which have a matrix metalloprotease inhibitory activity and are useful as drugs, wherein the rings A and B represent each an optionally substituted homocycle or heterocycle, etc.; R1s are the same or different and each represents hydrogen, optionally substituted hydrocarbyl, acyl, etc.; X1 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, etc.; X2 represents a bond, optionally substituted divalent aliphatic hydrocarbyl, —O—, etc.; Ys are the same or different represents hydrogen, optionally substituted hydrocarbyl, oxo, etc.; m is 0 or 1; n is an integer of 1 to 3; q1 is an integer of 1 to 2n+4; and q2 is an integer of 0 to 2n+3, provided that q1+q2 is 2n+4.

Abstract: Succinimide-acid compounds prepared by reaction of hydrocarbyl-substituted succinic acylating agents with alpha-omega amino acids are disclosed, as well as derivatives thereof useful as lubricity additives, lubricant dispersants, friction modifiers, liquid hydrocarbonaceous fuel detergents, antioxidants and alkali and/or alkaline-earth metal detergents.

Abstract: New types of hydroxamic acid-based bifunctional chelators are provided. These chelators are designed to chelate metal ions that can be detected either by their paramagnetic or radioactive properties. Conjugation with peptides or protein can be achieved by the presence of a linker moiety in the molecular structure of these chelators.

Abstract: Reactions of ring systems, such as aziridines, oxetanes and oxiranes with carboxylic acids, anhydrides, imides, lactones and carbonate esters are catalyzed by C3-C60, substituted or unsubstituted, straight or branched-chained, alkyl, aryl, or aralkyl carboxylate Cr+3 salts, preferably chromium +3 octoate. The catalysts also accelerate the reaction of hydroxy compounds with anhydrides, and of thiiranes with anhydrides. The catalysts selectively enhance the conversion of ring systems to form monomers, prepolymers, copolymers, functional end-group monomers, functional end-group prepolymers, and functional end-group polymers rather than forming homopolymers. By varying the catalyst concentration, molar ratios, and reaction temperatures, the reaction time required to form the desired product can be controlled.

Abstract: This invention relates to a two-part system useful for treating proteinaceous substrates. The two-part system has a first part comprising a water-soluble/dispersible reactive polyimido compound and a second part comprising a nucleophilic catalytic agent. The polyimido compounds may be selected from the group consisting of polysuccinimide compounds, polyglutimide compounds, and copolymers of thereof. The polyimido compound may also comprise a functionalizing moiety that provides functionality to the polyimido compound and is preferably derived from a nucleophilic moiety selected from the group consisting of amines, alcohols, phenols, thiols, and carboxylates; and a water-solubilizing/dispersing moiety that provides water-solubility and/or water-dispersibility to the polyimido compound and is preferably derived from a nucleophilic moiety selected from the group consisting of amines, alcohols, phenols, thiols, and carboxylates.

Abstract: A surfactant which is the reaction product of a hydrocarbyl-substituted succinic anhydride or a reactive equivalent thereof with at least one water-dispersible amine-terminated poly(oxyalkylene), is effective for use in soil remediation.

Abstract: This invention relates to water-soluble/dispersible reactive functionalized imido and polyimido compounds, wherein the polyimido compounds may be selected from the group consisting of polysuccinimide compounds, polyglutimide compounds, and copolymers of thereof. The polyimido compound comprises a functionalizing moiety F that provides functionality to the polyimido compound and is preferably derived from a nucleophilic moiety selected from the group consisting of amines, alcohols, phenols, thiols, and carboxylates; and a water-solubilizing/dispersing moiety that provides water-solubility and/or water-dispersibility to the polyimido compound and is preferably derived from a nucleophilic moiety selected from the group consisting of amines, alcohols, phenols, thiols, and carboxylates. The invention also pertains to a proteinaceous substrate to which the imido or polyimido compound has been covalently bonded and to a method for treating a proteinaceous substrate with the imido or polyimido compound.

Abstract: This invention relates to water-soluble/dispersible reactive imido and polyimido compounds, wherein the polyimido compounds may be selected from the group consisting of polysuccinimide compounds, polyglutimide compounds, and copolymers of thereof. The polyimido compounds comprise a water-solubilizing/dispersing moiety that provides water-solubility and/or water-dispersibility to the polyimido compound and preferably is derived from a nucleophilic moiety selected from the group consisting of amines, alcohols, phenols, thiols, and carboxylates. The present invention also pertains to a proteinaceous substrate to which the imido or polyimido compound has been covalently bonded and to a method for treating a proteinaceous substrate with the imido or polyimido compound.

Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula (T)xA—B—D—E—G wherein A is an aryl or heteroaryl rings; B is an aryl or heteroaryl ring or a bond; each T is a substituent group; x is 0, 1, or 2; the group D represents the group E represents a two or three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents and with the proviso that when G is each of the substituents on E is an independent substituent; and include pharmaceutically acceptable salts thereof.

Abstract: A novel butadiene derivative of the formula: wherein Ring A is heterocycle, or benzene being optionally substituted by lower alkyl, alkoxy, nitro, hydroxy, substituted or unsubstituted amino or halogen, Ring B is heterocycle, or benzene being optionally substituted by lower alkoxy, lower alkylenedioxy or di-lower alkylamino, R1 and R2 are each H or lower alkyl, one of —COR32 and —COR42 is carboxyl, and the other is carboxyl being optionally esterified, or the corresponding amide or pyrrolidine derivatives, or a pharmaceutically acceptable salt thereof.

Abstract: Provided are methods of purification of an organic lithium salt comprising the steps of: (a) dissolving an impure organic lithium salt in a solution comprising an organic complexing solvent; (b) crystallizing from said solution a solid solvate complex comprising said lithium salt and said organic complexing solvent; (c) separating said solid solvate complex from said solution; (d) dissociating said solid solvate complex to yield: (i) said lithium salt in a solid form, and, (ii) a volatile composition comprising said organic complexing solvent; and, (e) removing said volatile composition to yield said lithium salt in a solid form of purity greater than the purity of said impure lithium salt. The present invention also pertains to electrolytes for electric current producing cells comprising such purified lithium salts.

Abstract: This invention relates to a diamino compound represented by the formula [1]: in which G1 is a trivalent organic group of 2-20 carbon atoms, G2 is independently a single bond, —COO—, —OCO—, —NHCO—, —CONH—, —O—, —O—, or —CO—, G3 is a single bond or an alkylene group of 1-20 carbon atoms, X and Y are each independently a hydrogen atom, a fluorine atom, a chlorine atom, a cyano group, a nitro group, or an alkyl group, a haloalkyl group, an alkoxy group or a haloalkoxy group, each alkyl or alkoxy group having 1-12 carbon atoms, or a cycloalkyl group of 3-8 carbon atoms or a trans-4-alkylcyclohexyl group of 9-14 carbon atoms, and m is an integer of 0-3; a polyamic acid and polyimide using the said diamino compound, an aligning film using the said polyimide and a liquid crystal display device using the said aligning film.

Abstract: A new reagent for preparation of a caged compound in accordance with the present invention is a compound having, as a basic structure, an N-succinimidyl cinnamate structure expressed by the following formula 1: Another reagent for preparation of a caged compound in accordance with the present invention is a compound having, as a basic structure, a p-nitrophenyl cinnamate structure expressed by the following formula 3:

Abstract: The present invention provides a simple and inexpensive method for producing &agr;-hydroxy-&bgr;-aminocarboxylic acids and their esters. An ester of an N-protected &agr;-amino acid ester is converted into a &bgr;-ketosulfoxide, which is then processed with an acid to give an &agr;-ketohemimercaptal. Next, this is acylated and then processed with a base to obtain an N-protected &agr;-acyloxy-&bgr;-amino-thioester, which is then saponified to obtain an intended compound. According to the method of the present invention, it is possible to produce &agr;-hydroxy-&bgr;-aminocarboxylic acid derivatives, which are intermediates in producing various HIV protease inhibitors, renin inhibitors and carcinostatics, from a-amino acids. The method comprises reduced reaction steps, the selectivity in the method to give the intended product is high, and the yield of the product obtained is high.

Abstract: Tosylproline analogs of formula I, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are thymidylate synthase inhibitors; and are useful as anti-tumor agents and as anti-parasitics, anti-bacterials, anti-fungals, and anti-virals.

Abstract: A compound comprising i) 20-80 mol % of at least one monoethylenically unsaturated dicarboxylic acid or anhydride thereof, ii) 5-30 mol % of at least one unsaturated oligomer of an optionally branched olefin having 2 to 20 carbon atoms, having an average molecular weight Mw of 300-5000, iii) 10-60 mol % of an ethylenically unsaturated acid having at least 10 carbon atoms, or a mono-,di- or tri- ester of glycerol (1, 2, 3 propanetriol) in which at least one of the carboxylic acid residues of the ester is derived from said ethylenically unsaturated acid, or an oil, optionally hydrolysed, containing at least 30 wt % of the acid or ester is disclosed, which has both dispersant and VI improving properties in lubricating oils.

Abstract: A compound of formula IV ##STR1## wherein G is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkenyl, C.sub.2 -C.sub.12 alkynyl or Ar;Ar is an aromatic or heteroaromatic group or a substituted aromatic or heteroaromatic group;R.sup.1 is halo, SR, OR, amino, mono or di-(C.sub.1 -C.sub.6 -alkyl)amino, tri (C.sub.1 -C.sub.6 -alkyl)ammonium, C.sub.1 -C.sub.6 -alkylthio, di(C.sub.1 -C.sub.6 -alkyl)sulfonium, C.sub.1 -C.sub.6 -alkylsulfonyl, or C.sub.1 -C.sub.6 -alkylphosphonyl;R.sup.2 is OH or SH; orR.sup.1 and R.sup.2 taken together form a second bond or together form an epoxide, aziridine, episulfide, or cyclopropyl ring;R is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkanoyl or Ar;R.sup.3 is C.sub.1 -C.sub.6 alkyl;R.sup.4 and R.sup.5 are H; orR.sup.4 and R.sup.5 taken together form a second bond;R.sup.24 is a leaving group; andR.sup.26 is an alcohol protecting group;X is O, NH or (C1-C3 alkyl)N--.

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: Ethers of polyalkyl or polyalkenyl N-hydroxyalkyl succinimides having the formula: ##STR1## or a fuel soluble salt thereof. The compounds of formula I are useful as fuel additives for the prevention and control of engine deposits.

Abstract: Fluorinated imides useful for imparting repellency of low surface tension fluids to thermoplastic polymers of formulae ##STR1## wherein R.sub.1 is F(CF.sub.2).sub.x --(CH.sub.2).sub.m, or F(CF.sub.2).sub.x SO.sub.2 N(R.sub.5) (CH.sub.2)p wherein x is from about 4 to about 20, m is from about 2 to about 6, p is from 1 to about 12, and R.sub.5 is an alkyl radical of from 1 to about 4 carbons;R.sub.2 is a linear, branched or cyclic alkylene or poly(oxyalkylene) hydrocarbon group having from about 2 to about 15 carbons;R.sub.3 is selected from the group consisting of F(CF.sub.2).sub.x --(CH.sub.2).sub.m, F(CF.sub.2).sub.x --(CH.sub.2).sub.m --OC(O)--(CH.sub.2).sub.n, and F(CF.sub.2).sub.x SO.sub.2 N(R.sub.5)(CH.sub.2).sub.p OC(O)(CH.sub.2).sub.n wherein x is from about 4 to about 20, m is from about 2 to about 6, n is about 2 to about 12, p is from 1 to about 12, and R.sub.5 is an alkyl radical of from 1 to about 4 carbons;R.sub.4 is an alkyl or alkenyl group of from about 4 to about 20 carbons, andR.sub.

Abstract: Levetiracetam is prepared by optical resolution of etiracetam by means of preparative high performance liquid chromatography or continuous simulated moving bed chromatographic system using silica gel supporting amylose tris(3,5-dimethylphenylcarbamate) as a packing material.

Abstract: A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I ##STR1## with an alkylating agent of structure III ##STR2## 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: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.

Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

Abstract: What is described herein are derivatized polymers of .alpha.-olefin-maleic anhydride alkyl half-ester or full acid, preferably the isobutylene compound, optionally with repeat units of maleamic acid and/or its corresponding maleimide therein. These polymers are useful as fixatives in personal care products, such as hair spray compositions, particularly as one-phase, low VOC formulations in pump and aerosol systems, and in anhydrous, alcoholic, aqueous-alcoholic and in high hydrocarbon tolerant solvent formulations. In use, these hair spray compositions dry down to form clear, continuous and defectless films.

Abstract: Activating groups for cyanine dyes used to label chain terminators in nucleotide sequencing, based on N-hydroxyphthalimide, are disclosed. From these activating groups, activated dyes of the present Invention are prepared which react with the derivitized nucleotide chain terminators to give a labeled chain terminator of the present Invention. The activating groups of the present Invention allow the dye-chain terminator reaction to occur at a much higher yield and with much greater selectivity for the mono-substituted product, compared with the prior art.

Abstract: Esters of polyalkyl or polyalkenyl N hydroxyalkyl succinimides having the formula: ##STR1## or a fuel soluble salt thereof; wherein R is a polyalkyl or polyalkenyl group having an average molecular weight in the range of about 450 to about 5,000;n is an integer from 2 to 5; and Z is a moiety selected from the group consisting of ##STR2## wherein R.sub.1 is a hydroxy, nitro, cyano or --(CH.sub.2).sub.x --NR.sub.3 R.sub.4, wherein R.sub.3 and R.sub.4 are independently hydrogen or lower alkyl of 1 to 6 carbon atoms and x is 0 or 1; and R.sub.2 is hydrogen, hydroxy, nitro, cyano or --(CH.sub.2).sub.y --NR.sub.5 R.sub.6, wherein R.sub.5 and R.sub.6 are independently hydrogen or lower alkyl of 1 to 6 carbon atoms and y is 0 or 1.The compounds of formula I are useful as fuel additives for the prevention and control of engine deposits.

Abstract: The morphology of multidimensional, thermally stable oligomers is combined with the inclusion of charge carrier linkages within the polymer arms to produce thermally stable advanced composites from cured oligomers that are conductive or semiconductive if suitably doped.

Abstract: Provided are methods for the synthesis of N-cyclic maleamic acids and N-cyclic maleimide derivatives, as well as N-cyclic maleamic acids and N-cyclic maleimides synthesized thereby. The method for synthesis of an N-cyclic maleamic acid involves reacting an amino group-containing N-cyclic compound with maleic anhydride in acetic acid to obtain an N-cyclic maleamic acid. An N-cyclic maleimide can be formed by adding hexamethyldisilazane to an N-cyclic maleamic acid prepared according to the above-described method, thereby cyclizing a maleamic acid site of the N-cyclic maleamic acid. The described methods allow for the products to be obtained at high yields.

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: There is disclosed substituted thiocarboxamides of the general formula (I) useful as herbicides.