Abstract: The present invention provides processes and synthetic intermediates for the synthesis of 4-substituted ((1S,2S,4R)-2-hydroxy-4-{7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentyl)methyl sulfamates, which are E1 activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with E1 activity.

Abstract: The present invention relates to compounds of Formula I, IA, II, HA, III, or IHA and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, IA, II, IIA, III, or IIIA are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases).

Abstract: The present invention relates to a method of increasing the chlorine fastness of dyed synthetic polyamide fibre materials, which comprises treating the fibre material after dyeing with an aqueous liquor comprising a thiourea/formaldehyde/bisphenol condensate or a thiourea/polyisocyanate adduct.

Abstract: The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo.

Abstract: What is described are the compounds and the synthesis of [F-18]-labelled L-glutamic acid, [F-18]-labelled L-glutamate, their derivatives of the formula (I) and their use.

Abstract: The present invention concerns new thiolysine and selenolysine compounds that can be used as building blocks for peptides and proteins, providing ligation handles for site- and chemoselective modification of said peptides and proteins. In particular, the invention provides. In particular, the invention provides (the use of) the compounds 5-thiolysine (also referred to as ?-thiolysine); 4-thiolysine (also referred to as ?-thiolysine); 5-selenolysine (also referred to as ?-selenolysine) and 4-selenolysine (also referred to as ?-selenolysine). The positioning of the thiol or selenol group at the respective carbon atom allows for a very efficient intramolecular transfer reaction to take place after conjugation with a selected ligand, and the thiol or selenol group may subsequently be removed using reported procedures, thereby restoring the native lysine structure, or be used as an additional conjugation handle. The methodology is fast and gives well-defined material.

Abstract: The present invention relates to chiral ligands deriving from ?- and ?-amino acids, and from metal complexes formed from the same. The ligands are useful with catalytic gold complexes, particularly Au(I) complexes.

Abstract: A resist composition including a base component (A) which exhibits changed solubility in a developing solution, and an acidic compound component (J) which is decomposed by exposure to exhibit decreased acidity, wherein the acidic compound component (J) contains a compound represented by formula (J1) [in the formula, R1 represents H, OH, halogen atom, alkoxy group, hydrocarbon group or nitro group; m represents 0-4; n represents 0-3; Rx represents H or hydrocarbon group; X1 represents divalent linking group; X2 represents H or hydrocarbon group; Y represents single bond or C(O); A represents alkylene group which may be substituted with oxygen atom, carbonyl group or alkylene group which may have fluorine atom; Q1 and Q2 represents F or fluorinated alkyl group; and W+ represents primary, secondary or tertiary ammonium coutercation which exhibits pKa smaller than pKa of H2N+(X2)—X1—Y—O-A-C(Q1)(Q2)—SO3? generated by decomposition upon exposure].

Abstract: Polyplex formulations were prepared using p(TETA/CBA), its PEGylated analog, p(TETA/CBA)-g-PEG2k, and mixtures of the two species at 10/90 and 50/50 wt %, respectively. Increasing PEG wt % inhibited polyplex formation. This work demonstrates the feasibility of preparing homogenous polyplexes by altering the PEG wt % using a mixture of p(TETA/CBA) and p(TETA/CBA)-g-PEG2k products. Further, a single-step method of making p(TETA/CBA)-g-PEG2k is disclosed.

Abstract: The present invention relates to an improved method for the preparation of 13-cyclohexyl-3-methoxy-6-[methyl-(2-{2-[methyl-(sulphamoyl)-amino]-ethoxy}-ethyl)-carbamoyl]-7H-indolo-[2,1-a]-[2]-benzazepine-10-carboxylic acid. The present invention also relates to a new compound, namely tert-butyl (methyl-{2-[2-(methylamino)-ethoxy]-ethyl}-sulphamoyl)-carbamate, used in this improved method.

Abstract: The present invention provides, among other things, segmented, degradable polymeric reagents suitable for reaction with biologically active agents to form conjugates, the polymeric reagents comprising one or more polymer chains divided or separated by one or more degradable linkages into polymer segments having a molecular weight suitable for renal clearance. The polymeric reagents can have a substantially linear structure, a branched structure, or a multiarm structure. Each structure includes one or more linkages capable of degradation in vivo.

Abstract: The present invention provides a method of measuring an endogenous low-molecular-weight compound specifically and conveniently with high sensitivity. Using the particular sulfur-containing amino acid derivative, a method of measuring an endogenous low-molecular-weight compound specifically and conveniently with high sensitivity can be provided.

Abstract: The present invention provides an efficient and scalable process to prepare the compound of formula 4 by reduction of the corresponding ?-acyloxy sulfides.

Abstract: The present invention relates to the use of a compound comprising a moiety of formula (I) as a reagent for protecting a thiol group in a thiol compound wherein X, X? and Y are as defined herein. The protecting group methodology of the present invention allows straightforward and selective protection of thiol groups. Cleaving of the thiol group to regenerate the thiol functional group is also facile and controllable. The present invention further provides an analogous protecting group methodology directed to protection of disulfide groups.

Abstract: The present invention concerns new thiolysine and selenolysine compounds that can be used as building blocks for peptides and proteins, providing ligation handles for site- and chemoselective modification of said peptides and proteins. In particular, the invention provides. In particular, the invention provides (the use of) the compounds 5-thiolysine (also referred to as ?-thiolysine); 4-thiolysine (also referred to as ?-thiolysine); 5-selenolysine (also referred to as ?-selenolysine) and 4-selenolysine (also referred to as ?-selenolysine). The positioning of the thiol or selenol group at the respective carbon atom allows for a very efficient intramolecular transfer reaction to take place after conjugation with a selected ligand, and the thiol or selenol group may subsequently be removed using reported procedures, thereby restoring the native lysine structure, or be used as an additional conjugation handle. The methodology is fast and gives well-defined material.

Abstract: The present invention relates to a method of making asymmetrical bis(thiosemicarbazones), compounds useful as synthetic intermediates in the method, new bis(thiosemicarbazones) that can be readily accessed by use of the method and methods of treatment and imaging utilising some of the new bis(thiosemicarbazones).

Abstract: The disclosure herein provides a compound of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, and hydrates thereof. The steps of synthesis of compound of formula I is described. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, transdermal administration, or injection. Such compositions may be used to treatment of metabolic condition or neurodegenerative disorders or its associated complications.

Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.

Abstract: The invention relates to propionic acids, propionic acid esters, and related compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds for the treatment of various diseases or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).

Abstract: A compound, composition and method of making and using a compound of formula 1 are disclosed. The compound of formula I also comprises of salts, polymorphs, solvates, mesylates, hydrochloric salt, solvates and hydrates thereof. The compound may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for peroral, topical, transmucosal, inhalation, targeted delivery and sustained release formulations. Such compositions may be used to treat metal accumulation in blood, organs and due to genetic complications.

Abstract: A compound, composition and method of making and using a compound of formula 1 are disclosed. The compound of formula I also comprises of salts, polymorphs, solvates, mesylates, hydrochloric salt, solvates and hydrates thereof. The compound may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for peroral, topical, transmucosal, inhalation, targeted delivery and sustained release formulations. Such compositions may be used to treat metal accumulation in blood, organs and due to genetic complications.

Abstract: The invention relates to feed additives containing dipeptides or salts thereof, in which one amino acid residue of the dipeptide is a DL-methionyl residue and the other amino acid residue of the dipeptide is an amino acid in the L-configuration selected from lysine, threonine, tryptophan, histidine, valine, leucine, isoleucine, phenylalanine, arginine, cysteine and cystine; feed mixtures containing these additives and method of producing the dipeptides.

Abstract: Novel Amino Acid Derivatives and Pharmaceutical Uses Thereof Provided are novel compounds of Formula I: wherein ‘X’ represents an amino acid group, ‘n’ is an integer between 1 and 4, ‘R1’ represents benzyl, t-butyl or 9-fluorenylmethyl and ‘R2’ represents a tetramethylmercaptoimidazole derivative or —S+R3R4, wherein R3 and R4 each independently represent lower alkyl, or a pharmaceutically and/or veterinarily acceptable derivative thereof. Further provided are pharmaceutical formulations of the compounds and the use thereof in the preparation of a medicament for inhibiting diseases in which transglutaminase has been implicated. Advantageously, the medicament is for treating fibrosis, scarring and/or cancer. Additionally provided are methods, of inhibiting autoimmune diseases such as coeliac disease, neurodegeneration and chronic inflammatory diseases (e.g.

Abstract: The present invention relates to carbamoylation of amines, mercaptanes, thiophenols and phenols employing organic azides. More specifically, the invention relates to a method for generating urea derivatives, thiocarbamate derivatives and carbamate derivatives, and is based on the intermediate formation of isocyanate, starting from an organic azide. The reaction as described is useful in applications for modified nucleoside synthesis, oligonucleotide synthesis, as well as modification, labeling and conjugation of polymers and biomolecules.

Abstract: The present invention provides polymeric conjugates containing positively charged moieties. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.

Abstract: Acyloxyalkyl carbamate prodrugs of 3-aminopropylsulfinic acid and analogs thereof, pharmaceutical compositions of 3-aminopropylsulfinic acid and analogs thereof, methods of making prodrugs of 3-aminopropylsulfinic acid and analogs thereof, methods of using prodrugs of 3-aminopropylsulfinic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing diseases or disorders such as spasticity or gastroesophageal reflux disease are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylsulfinic acid and analogs thereof and sustained release oral dosage forms thereof, which are suitable for oral administration, are also disclosed.

Abstract: A compound of formula (I): namely (2S)-2-amino-4-{[2-(ethanimidoylamino)ethyl]thio}butanoic acid, compound with phosphoric acid, or a solvate or physiologically functional derivative thereof, is useful as a relatively non-hygroscopic selective inhibitor of inducible nitric oxide synthase.

Abstract: Dithiocarbamate derivative compounds, useful as multifunctional additives for lubricating oils and fuels, are provided and are derived from a reaction product obtained from (a) a di(hydrocarbyl)thiocarbamate intermediate derived from the reaction of a dihydrocarbylamine and carbon disulfide; (b) an amide of the general formula R7CONH2 wherein R7 is an alkylene group having 2 to about 30 carbon atoms; and (c) an effective amount of a carbonyl-containing compound.

Abstract: Method of making an alpha-amino acid compound having the structure of Formula 32: comprising treating under hydrolyzing conditions a hydantoin compound having the structure of Formula 33: where the substituents are described herein.

Abstract: Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors:

Abstract: Disclosed is a method for synthesizing 1-(acyloxy)-alkyl derivatives of primary or secondary amine drugs from 1-acyl-alkyl derivatives of primary or secondary amine drugs, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amenable to scale-up. For example, 1-acyl-alkyl derivatives of gabapentin and pregabalin are oxidized to yield 1-(acyloxy)-alkyl derivatives of gabapentin and pregabalin, respectively.

Abstract: The present invention provides a process for industrially producing (aminomethyl)trifluoromethylcarbinol derivatives, in particularly, optically active compounds thereof, which are useful as starting compounds for drugs such as protease inhibitors, etc.

Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: The present invention relates to novel amidino compound of formula (I): to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use as selective inhibitors of inducible nitric oxide synthase.

Abstract: Methods of synthesizing pharmacologically useful oxazolidinones are disclosed, and, in particular, a method of manufacturing a 5-(tert-butylcarbamoyl)-aminomethyl-oxazolidinone by condensing a carbamate with a tert-butylcarbamoyl protected derivative of glycidylamine or 3-amino-1-halopropanol.

Abstract: Trisubstituted N-protected guanidines and methods for use as guanidinylating reagents to yield N-protected guanidine derivatives.

Abstract: The present invention relates to novel amidino compound of formula (I). to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use as selective inhibitors of inducible nitric oxide synthase.

Abstract: Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Abstract: The present invention provides a process for making N-alkoxy(or aryloxy)carbonyl isothiocyanate derivatives by reacting a chloroformate with a thiocyanate, in the presence of an aqueous solvent and a catalytic amount of a N,N-dialkylarylamine, to produce a N-alkoxy(or aryloxy)carbonyl isothiocyanate intermediate product, wherein the intermediate product is converted to a N-alkoxy(or aryloxy)carbonyl isothiocyanate derivative in high yield and purity.

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: Dithiocarbamyl derivatives, useful as multifunctional additives for lubricating oils, of the formula ##STR1## wherein Q is ##STR2## R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.30 n-alkyl, C.sub.3 -C.sub.30 branched alkyl, C.sub.3 -C.sub.12 cycloalkyl, C.sub.5 -C.sub.12 aryl, or C.sub.6 -C.sub.12 alkylaryl; R.sup.3 is C.sub.1 -C.sub.20 alkylene; R.sup.4 is --R.sup.3 --C(O)--O--; R.sup.5 and R.sup.6 are each independently hydrogen, C.sub.1 -C.sub.30 n-alkyl, C.sub.3 -C.sub.30 branched alkyl, C.sub.3 -C.sub.12 cycloalkyl, C.sub.5 -C.sub.12 aryl, or C.sub.6 -C.sub.12 alkylaryl; R.sup.7 is C.sub.1 -C.sub.20 alkylene, optionally substituted with --OR.sup.5 or --COOH; R.sup.8 is --R.sup.3 --C(O)--NR.sup.5 --; n is 0, 1, 2 or 3; and y is 0, 1, 2, or 3.

Abstract: Trisubstituted N-protected guanidines and methods for use as guanidinylating reagents to yield N-protected guanidine derivatives.

Abstract: The present invention provides a process for making N-alkoxy(or aryloxy)carbonyl isothiocyanate derivatives by reacting a chloroformate with a thiocyanate, in the presence of an organic solvent and a catalytic amount of a N,N-dialkylarylamine, to produce a N-alkoxy(or aryloxy)carbonyl isothiocyanate intermediate product, wherein the intermediate product is converted to a N-alkoxy(or aryloxy)carbonyl isothiocyanate derivative in high yield and purity.

Abstract: The present invention relates to a compound of the formula wherein R.sup.1 and R.sup.2 are selected from lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms; R.sup.3 is a substituted or unsubstituted lower alkyl group having 1-6 carbons; and R.sup.4 is selected from substituted or unsubstituted lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms. The present invention also relates to a pharmaceutical composition comprising the above compound, as well as a method of treating tumor cells with the compound.

Abstract: Derivatives of gamma-amino-alpha,beta-unsaturated sulfonic acids, a process for the preparation of the same and their utilization in the synthesis of pseudopeptides characterized by the presence of at least a sulfonamide type bond conjugated to a double bond are described.

Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.

Abstract: Diethylenetriaminepentaacetic acid monoamide derivatives, their complexes and complex salts, containing an element of atomic numbers 21-29, 31, 32, 39, 42-44, 49 or 57-83, pharmaceutical agents containing these compounds, their use as contrast media and process for their production.

Abstract: A composition comprisinga) a lubricant or a hydraulic fluid andb) at least one compound of the general formula I ##STR1## in which x=1 or 2 and,if x=1,R is as defined for R.sup.1 or R.sup.3 --O-- or,if x=2,R is as defined for R.sup.8, andR.sup.1 and R.sup.3 are, for example, alkyl, cycloalkyl, alkenyl, phenyl, naphthyl, aralkyl or alkaryl, or alkyl, cycloalkyl, alkenyl, phenyl, naphthyl, aralkyl or alkaryl, which are monosubstituted or polysubstituted by groups from the series comprising halogen, cyano, nitro, e.g. --OCH.sub.3 or e.g. --COOCH.sub.3, or alkyl, cycloalkyl, alkenyl, aralkyl or alkaryl which are interrupted by one or more groups from the series comprising --O--, --S--, --NH--, ##STR2## or alkyl, cycloalkyl, alkenyl, aralkyl or alkaryl which are monosubstituted or polysubstituted by groups from the series comprising halogen, cyano, nitro, e.g. --OCH.sub.3 or e.g. --COOCH.sub.3 and interrupted by one or more groups from the series comprising --O--, --S--, --NH--, ##STR3## and R.sup.2 is NR.sup.4 R.

Abstract: A process for the manufacture of N-protected .alpha.-aminoketones and N-protected .alpha.-aminoalcohols of the formula ##STR1## wherein X is halogen, one of Q.sup.1 and Q.sup.2 is hydrogen and the other is hydroxy or Q.sup.1 and Q.sup.2 together are oxo, R.sup.1 is an amino protecting group and R.sup.2 is hydrogen or the characterizing group of an .alpha.-aminocarboxylic acid,starting from the corresponding lower alkyl N-protected .alpha.-aminocarboxylates via corresponding lower alkyl N-silyl protected .alpha.-aminocarboxylates.

Abstract: Hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.