Abstract: More efficient and/or economical methods for synthesizing heptapeptide alcohol analogs of oxytocin are provided along with novel intermediates which are useful in synthesizing such oxytocin analogs. Efficient and economical methods for synthesizing intermediates useful in synthesizing these oxytocin analogs are also provided.

Abstract: An amino-acid iodine complex, viz. amino-acid amino-carboxyl iodine complex, was provided wherein its coordinate center is iodine molecule, complex reagent is amino-acid, sites of complexing reaction are amino and carboxyl groups of amino-acid. The complex can be used for the production of feedstuff, food additive, disinfectant, antiseptic and medicament. Also provided is a method for the production of said complex comprising opening the inner-complex ring of amino-acid by acid catalysis and allowing the amino-acid to combine with iodine molecule to form an amino-acid amino-carboxyl iodine complex; because amino-acid is a nutriment and amino-carboxyl complex is achieved, their introduction not only increases the nutritional function of the complex and improves the stability of iodine, but also is beneficial to the environment protection and enhances the disinfecting activity against viruses and bacteria.

Abstract: The present invention provides illudin analogs of the general formula (I): where R1 is (CH2)n—X—Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C1-C8)alkyl, (C6-C10)aryl, (C6-C10)aryl(C1-C4)alkyl or cyclo(C3-C6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; R2 is absent; or R1 and R2 together comprise a 5-7 membered cyclic ring; R3 is (C1-C4)alkyl or H; R4 is H, SCH2CO2 (C1-C4)alkyl, O—(C5-C12)aryl or —S—(C5-C12)aryl; R5 is H, OH or absent; R6 is (C1-C4)alkyl or absent; R7 is OH or OSi((C1-C4)alkyl)3; or R6 and R7 together are ethylenedioxy; R8 is optionally substituted (C1-C4)alkyl; and the bonds represented by ----- are individually present or absent. The invention further provides dimers comprising analogs of formula (I).

Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.

Abstract: The synthesis of peptides comprising disulphide bridges is challenging since it is difficult to ensure that the correct cysteine residues combine to form the desired disulphide bridges. The present invention describes novel protection techniques useful in the preparation of peptides. Described is a process for the deprotection of an Acm-, MBzl- and/or tBu-protected thiol which comprises reacting said protected thiol with an acid in the presence of an oxidising agent at a temperature sufficient to effect deprotection and generation of disulphide bonds.

Abstract: Thio-alpha-amino acids of general formula (I), wherein R1, R2 and R3 have the meanings given in the description, methods for producing them, and medicaments containing these compounds. The invention also provides methods for treating pain and other diseases using the pharmaceutical compositions comprising the thioamino acids.

Abstract: Form II crystalline maleate salt of S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine is disclosed. The Form II crystalline salt is a channel hydrate, with a melting point of about 77.69° C.

Abstract: A crystalline maleate salt of S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine is disclosed. The crystalline salt has absorption of less than one percent water by weight at 90% R.H. at 25° C., a melting point of 123° C., and aqueous solubility in excess of 230 mg ml−1.

Abstract: The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

Abstract: Compounds having therapeutic utility are of formula (I)

Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.

Abstract: The invention relates to a novel acylate which is the reaction product of (a) a substance which is selected from the group consisting of naturally occuring alpha-aminocarboxylic acids, neurotransmitters other than such acids, and central or peripheral nervous system pharmacologically active compounds, and containing a functional group including an acylatable hydrogen atom, or a reactive derivative thereof; and (b) an essential fatty acid or a reactive derivative thereof; and including the pharmaceutically acceptable salts of such acylates possessing a basic and (or) acidic function; and to their functional derivatives. The acylates and their functional derivatives may be used for treatment of a disease or condition related to a neurotransmitter defector deficiency, or to another central or peripheral nervous system defect or deficiency, and in particular Parkinson's disease.

Abstract: Perfluoroalkyl-substituted amines, acids, amino acids and thioether acid compounds containing a perfluoroalkyl-iodoalkyl or perfluoroalkyl-alkene group as well as derivatives thereof, are described. They are useful as surfactants in a variety of applications where low surface tensions are required, including coating formulations for glass, wood, metal, cement, paper, textiles, as foam control agents in polyurethane foams and especially in aqueous fire-fighting formulations.

Abstract: The present invention provides a compound for chelating a metal or a metal complex, characterized in that it consists of a bis-dithiocarbamate structure (F) having the formula below: 1

Abstract: A method for preparing S-alkyl and S-aryl thiocarbamates comprising reacting a precursor thiol reagent with trichloroacetyl chloride to produce an S-alkyl and S-aryl trichloroacetyl thioester intermediate, which is reacted with an amine to yield the corresponding thiocarbamate product. Also disclosed is the method for preparing S-alkyl and S-aryl thiocarbamates comprising reacting an amine with trichloroacetyl chloride to produce a trichloroacetamide intermediate, which is then reacted with the precursor thiol to yield the corresponding thiocarbamate product.

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

Abstract: Thio-alpha-amino acids of general formula (I), wherein R1, R2 and R3 have the meanings given in the description, methods for producing them, and medicaments containing these compounds. The invention also provides methods for treating pain and other diseases using the pharmaceutical compositions comprising the thioamino acids.

Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkylcysteine involves condensing cysteine with an aryl nitrile to form a 2-arylthiazoline-4-carboxylic acid, followed by alkylating the 2-arylthiazoline-4-carboxylic acid at the 4-position. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine or a 2-alkyl cysteine.

Abstract: the present invention provides novel compounds represented by formula I: 1

Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves reacting cysteine (or a salt or an ester thereof) and an aryl carboxylic acid to form a thiazoline ring, stereospecifically alkylating the thiazoline ring, and hydrolyzing the thiazoline ring to obtain a 2-alkylcysteine (or related compound). The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.

Abstract: The present invention provides illudin analogs of the general formula (I): where R1 is (CH2)n—X—Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C1-C8)alkyl, (C6-C10)aryl, (C6-C10)aryl(C1-C4)alkyl or cyclo(C3-C6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; R2 is absent; or R1 and R2 together comprise a 5-7 membered cyclic ring; R3 is (C1-C4)alkyl or H; R4 is H, SCH2CO2 (C1-C4)alkyl, O—(C5-C12)aryl or —S—(C5-C12)aryl; R5 is H, OH or absent; R6 is (C1-C4)alkyl or absent; R7 is OH or OSi((C1-C4)alkyl)3; or R6 and R7 together are ethylenedioxy; R8 is optionally substituted (C1-C4)alkyl; and the bonds represented by—are individually present or absent. The invention further provides dimers comprising analogs of formula (I).

Abstract: A method of making an alpha-amino acid compound having the structure of Formula 32: 1

Abstract: Objects of the present invention are to provide an oxidative stress inhibitor which is capable of suppressing the expression of a cytotoxic protein and the activation of a gene transcriptional regulatory factor taking part such expression of a cytotoxic protein and exhibits good feeling upon use and safety; to provide a method for preventing, retarding, alleviating or treating a skin change due to aging or an undesirable aesthetic skin change, both caused or promoted by an oxidative stress; and to provide a cosmetic composition or dermatologic preparation for external use comprising the oxidative stress inhibitor as an effective ingredient, and for those purposes are employed an oxidative stress inhibiting agent which comprises, as an effective ingredient, at least one selected from cysteine or cystine derivatives and the salts thereof.

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

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: A process is described for the preparation of R or S aminocarnitine, R or S phosphonium aminocarnitine and R and S 3,4 diaminobutanoic acid, and their derivatives with the following formula: 1

Abstract: A process is described for the preparation of R or S aminocarnitine, R or S phosphonium aminocarnitine and R and S 3,4 diaminobutanoic acid, and their derivatives with the following formula: 1

Abstract: An enzymatic synthesis and composition of &agr;-hydroxy carboxylic acid and &agr;-amino acid or peptide co-oligomers is disclosed wherein a residue of the &agr;-hydroxy carboxylic acid is linked to a residue of the &agr;-amino acid or peptide by an amide linkage. Proteolytic enzyme papain catalyzes co-oligomerization of the &agr;-hydroxy carboxylic acid and &agr;-amino acid. The degree and distribution of oligomerization varies upon the type and concentrations of different reaction mixtures utilized and upon the length of allowed reaction time. The resultant oligomers may be provided to ruminants as bioavailable amino acid supplements that are resistant to degradation in the rumen.

Abstract: The synthesis of N-methyl-homocysteines and their use are described.

Abstract: A compound selected from the group consisting of a compound of formula I 1

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 present invention relates to novel cysteine protease inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.

Abstract: A process for the preparation of racemic amino acids, characterized in that an acylamino acid of the formula R1—CH(NH—CO—R2)COOH wherein R1 is hydrogen, a linear, branched or cyclic alkyl that has from 1 to 7 carbon atoms and that may contain substituents such as a hydroxyl, alkyloxy or alkylthio group; and R2 is a hydrogen atom or an alkyl having from 1 to 3 carbon atoms; is heated in the presence of water, in a pressure-resistant vessel, to a temperature in the range from 110° C. to 220° C. and is hydrolyzed.

Abstract: A process for precipitating cystine from a solution in sulfuric acid, includes forming a mixture of a solution of cystine in aqueous sulfuric acid and of an aqueous solution of a base by simultaneous metering the cystine solution and the aqueous base solution into a mixing container. The metering takes place in such a way that the mixture in the container has a pH between 1.0 and 7.0 and a temperature between 30° C. and the boiling point of the mixture.

Abstract: A process for the production of methionine which comprises (a) hydrolyzing the methionine amide in the presence of a catalyst comprising titanium to produce ammonium methioninate, said catalyst having a porosity of from 5 to 1000 nm, a total pore volume of from 0.2 to 0.55 cm3/g and a surface area of from 30 to 150 m2/g, and (b) a second step of recuperating methionine from the ammonium methioninate salt by removing ammonia. Also claimed is an industrial process for the production of methionine incorporating the aforementioned hydrolysis.

Abstract: R or S aminocarnitine and their derivatives with formula (I) where Y is as described in the description, starting with aspartic acid with the same configuration as the aminocarnitine desired. This process has advantage in the type of reactants used, reduced volumes of solvents and the possibility of avoiding purification of intermediate products.

Abstract: This invention relates to a compound that is represented by the following Structure I: R1—SO2—C(R2)R3—(CO)m—(L)n—SG  I wherein R1 is an aliphatic or cyclic group, R2 and R3 are independently hydrogen or bromine as long as at least one of them is bromine, L is an divalent linking group, m and n are independently 0 or 1, SG is a solubilizing group with a pKa of 8 or less, with the proviso that when m and n are both 0, SG is not a sulfo (or salt thereof) or a sulfonamido (or salt thereof) and when m is 0 and n is 1, either L is not an alkylene group or SG is not a carboxy (or salt thereof).

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 synthesis of peptides comprising disulphide bridges is challenging since it is difficult to ensure that the correct cysteine residues combine to form the desired disulphide bridges. The present invention describes novel protection techniques useful in the preparation of peptides. Described is a process for the deprotection of an Acm-, MBzl- and/or tBu-protected thiol which comprises reacting said protected thiol with an acid in the presence of an oxidising agent at a temperature sufficient to effect deprotection and generation of disulphide bonds.

Abstract: Compounds, compositions and methods are provided that are useful in the treatment and prevention of certain viral infections and associated diseases. In particular, the compounds of the invention inhibit the activity of a viral RNA polymerase. The subject methods are particularly useful in the treatment of diseases causes by hepatitis C virus infection.

Abstract: It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are useful in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (I BD).

Abstract: A preparation for oral administration which comprises S-(3-hydroxypropyl)-L-cysteine and one or more excipients, where the excipients do not cause discoloration of S-(3-hydroxypropyl)-L-cysteine is disclosled. According to an embodiment of the invention, the excipient may comprise a starch and/or a cyclodextrin. Typical starches used in the invention include corn starch, potato starch, wheat starch, and rice starch. Typical cyclodextrins used in the invention include &agr;-cyclodextrin, &bgr;-cyclodextrin, and &ggr;-cyclodextrin. Other excipients, such as saccharides, sugar alcohols and cellulose are not present in amounts that cause discoloration of the HPCY.

Abstract: The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.

Abstract: Novel brain targeted low molecular weight, hydrophobic antioxidants and use of antioxidants in treatment of central nervous system neurodegenerative disorders such as Parkinson's, Alzheimer's and Creutzfeldt-Jakob's diseases and in treatment of conditions of peripheral tissues, such as acute respiratory distress syndrome, amyotrophic lateral sclerosis, atheroscierotic cardiovascular disease and multiple organ dysfunction, in which oxidants are overproduced.

Abstract: A method for enhancing the purity of a desired compound comprising: Step (a) treating a crude reaction product which contains at least one desired compound, unreacted starting materials and/or byproducts with at least one bifunctional quenching agent that is capable of selective covalent reaction with unwanted byproducts, or excess reagents; Step (b) allowing the quenching agent to covalently react with unreacted starting materials and/or byproducts to afford a derivatized compound of the quenching agent: and Step (c) isolating the desired compound is described as well as novel quenching agents and methods for their use in the rapid purification of synthetic intermediates and products in synthesis, combinatorial chemistry, and automated organic synthesis.

Abstract: The present invention provides illudin analogs of the general formula (I): where R1 is (CH2)n—X—Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C1-C8)alkyl, (C6-C10)aryl, (C6-C10)aryl(C1-C4)alkyl or cyclo(C3-C6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; R2 is absent; or R1 and R2 together comprise a 5-7 membered cyclic ring; R3 is (C1-C4)alkyl or H; R4 is H, SCH2CO2 (C1-C4)alkyl, O—(C5-C12)aryl or —S—(C5-C12)aryl; R5 is H, OH or absent; R6 is (C1-C4)alkyl or absent; R7 is OH or OSi((C1-C4)alkyl)3; or R6 and R7 together are ethylenedioxy; R8 is optionally substituted (C1-C4)alkyl; and the bonds represented by ----- are individually present or absent. The invention further provides dimers comprising analogs of formula (I).

Abstract: An article suitable for use as a biosensor includes a molecule of a formula X—R—Ch adhered to a surface of the article as part of a self-assembled monolayer. X is a functionality that adheres to the surface, R is a spacer moiety, and Ch is a chelating agent. A metal ion can be coordinated by the chelating agent, and a polyamino acid-tagged biological binding partner of a target biological molecule coordinated to the metal ion. A method of the invention involves bringing the article into contact with a medium containing or suspected of containing the target biological molecule and allowing the biological molecule to biologically bind to the binding partner. The article is useful particularly as a surface plasmon resonance chip.

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: The present invention concerns an enzymatic oxidative deamination process of a dipeptide monomer to prepare an intermediate useful to prepare compounds having endopeptidase and angiotensin converting enzyme inhibition activity.

Abstract: A compound of formula (I) wherein R1 is a C1-6 straight or branched chain alkyl group, a C2-6alkenyl group, a C2-6 alkynyl group, a C3-6cycloalkyl group or a C3-6cycloalkylC1-6alkyl group, each optionally substituted by one to three groups independently selected from: —CN; —NO2; a group —COR2 wherein R2 is hydrogen, C1-6 alkyl, —OR3 wherein R3 is hydrogen or C1-6alkyl or NR4R5 wherein R4 and R5 are independently selected from hydrogen or C1-6 alkyl; a group —S(O)mR6 wherein m is 0, 1 or 2, R6 is hydrogen, C1-6 alkyl, hydroxy or NR7R8 wherein R7 and R8 are independently hydrogen or C1-6 alkyl; a group PO(OR9)2 wherein R9 is hydrogen or C1-6 alkyl; a group NR10R11 wherein R10 and R11 are independently selected from hydrogen, C1-6 alkyl, —COR12 wherein R12 is hydrogen or C1-6 alkyl, or —S(O)m?R13 wherein m? is 0, 1 or 2 and R13 is hydrogen or C1-6 alkyl; halo; or a group —OR14 wherein R14 is hydrogen, C1-6 alkyl optionally substituted by one to three halo atoms, C6-10 aryl or —COR15 wherein R15 is hydroge