Abstract: A new compound is provided, which is used for preparing lacosamide. A novel method for preparing lacosamide is also provided. During the reaction, iodomethane and silver oxide that are cost expensive are not used, nor a Pd-c catalyst is used, so the production cost is low, the raw materials and accessory materials are cheap and easily available, and the process is simple, so that industrial production is easy to realize; and moreover, the yield is high, and good economic efficiency can be achieved.

Abstract: Methods for increasing athletic performance, preventing paresthesia, increasing beta alanine absorption and cell membrane permeability through both passive diffusion and active transport, and increasing the half-life of beta alanine present in a blood stream in a human or animal are disclosed. Each method includes administering to the human or animal a pharmaceutically effective amount of N-Acetyl Beta Alanine or an N-Acetyl Beta Alanine composition.

Abstract: The invention provides methods and compositions for preparing lisdexamfetamine and salts thereof. More particularly, the invention provides, for example, methods of preparing lisdexamfetamine from D-amphetamine.

Abstract: An oxygen absorber is provided that contains at least one of compounds each having a particular structure, and the oxygen absorber exhibits an oxygen absorbing capability without a metal contained, and is suitable for removing oxygen inside a packaging material packaging foods or the like.

Abstract: Combinations of charged local anesthetics with chemical permeation enhancers have been developed to give long duration block which is selective for sensory block over motor block. The duration of block is greatly prolonged by combining the local anesthetic with a permeation enhancer. The selectivity of sensory over motor block is provided by selecting the concentration of the local anesthetic and the permeation enhancer to provide selective permeability of the sensory and motor neurons to the enhancer.

Abstract: This invention relates to processes and intermediates for the preparation of an alpha-amino beta-hydroxy acid of Formula 1 wherein the variables R1, R?1 and R2 are defined herein and the compound of Formula 1 has an enantiomeric excess (ee) of 55% or greater.

Abstract: The present invention is directed to a process for preparing ?-amino-?-hydroxycarboxamides. The process works with epoxycarboxamides of the formula 2 which are reacted with ammonia or other amines.

Abstract: The present invention relates to a process for the preparation of (2S,3S)-3-amino-N-cyclopropyl-2-hydroxyalkanamides, and their use in the preparation of HCV inhibitors and cathepsin inhibitors.

Abstract: A new compound is provided, which is used for preparing lacosamide. A novel method for preparing lacosamide is also provided. During the reaction, iodomethane and silver oxide that are cost expensive are not used, nor a Pd-c catalyst is used, so the production cost is low, the raw materials and accessory materials are cheap and easily available, and the process is simple, so that industrial production is easy to realize; and moreover, the yield is high, and good economic efficiency can be achieved.

Abstract: This invention relates to processes and intermediates for the preparation of an alpha-amino beta-hydroxy acid of Formula 1 wherein the variables R1, R?1 and R2 are defined herein and the compound of Formula 1 has an enantiomeric excess (ee) of 55% or greater.

Abstract: A process for producing an enantiomerically enriched compound of Formula I: where the R-configuration, or S-configuration at the stereogenic center is marked with an *; by hydrogenating an enamide of formula III: in an organic solvent in the presence of a catalyst comprising a transition metal selected from rhodium or iridium, complexed to a chiral diphosphine ligand; Ar is optionally substituted phenyl; Z is OR1, SR1 or NR1R2; and P is R3, OR3 or NR3R4; R1 and R2 are selected from H, C1-8 alkyl, C5-12 cycloalkyl, aryl and aryl-C1-2-alkyl; or R1 and R2 together with the nitrogen atom form a C4-7-membered heterocyclic ring optionally fused with a 5- to 6-membered carbocyclic or heterocyclic ring; and R3 and R4 are selected from H, C1-8 alkyl, aryl, C5-12 cycloalkyl and aryl-C1-2-alkyl; or R3 and R4 together with the nitrogen atom form a C4-7-membered heterocyclic ring.

Abstract: Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed.

Abstract: Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders.

Abstract: The present invention relates to a process for the preparation of (2S,3S)-3-amino-N-cyclopropyl-2-hydroxyalkanamides as well as novel compounds prepared or used in the process.

Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.

Abstract: Provided are syntheses of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin via a chiral intermediate of the following formula 4 wherein Ar is a C6-10 aromatic group, R is a straight or branched C1-4 alkyl, ester, or carboxylic acid, and R1 is a straight or branched C1-5 alkyl, aralkyl, or substituted aralkyl.

Abstract: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.

Abstract: This invention concerns compounds of adamantanamines and neramexane, including their pharmaceutically-acceptable salts, diesterioisomers, and formulations for treating Alzheimer's related dementias, depression, AIDS related dementias, as antivirals, inflammatory diseases such as rheumatoid arthritis, and cerebral ischemia, hyperlipidemia, and diabetes.

Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

Abstract: The present disclosure relates to specific dimercaptoamides, reducing compositions for permanently reshaping keratin fibers comprising the dimercaptoamides, for instance, human keratin fibers such as the hair; and processes for reshaping keratin fibers comprising the application of said reducing compositions. The present disclosure also relates to processes for preparing the dimercaptoamides.

Abstract: This invention relates to processes and intermediates for the preparation of an alpha-amino beta-hydroxy acid of Formula 1 wherein the variables R1, R?1 and R2 are defined herein and the compound of Formula 1 has an enantiomeric excess (ee) of 55% or greater.

Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

Abstract: Combretastatin derivatives of formula (I), preparation and use thereof are disclosed, wherein: Rf is alkyl with 1-8 carbon atoms and 1-17 fluorine atoms, R is amino, substituted amino, hydroxyl, nitro, halo, alkyloxy, phosphate or amino acid side chain. Said derivatives have a capability to inhibit the polymerization of microtubules and are useful in treatment against tumor and neovascularization.

Abstract: The present invention provides a technique for crystallizing a desired protein at a high probability; namely, a protein crystallizing agent and a method of crystallizing protein. The present invention also provides a technique for determining the conditions for protein crystallization easily with high efficiency; namely, a method of screening the conditions for protein crystallization and a protein crystallization screening reagent. As the protein crystallizing agent, at least one compound selected from the group consisting of a basic amino acid, acidic amino acid, ester derivative of amino acid and amide derivative of amino acid is used, or at least one of these compounds is used in combination with another protein crystallizing agent.

Abstract: The present invention provides compounds of formula (I), wherein k, Ar, R2, R3, R4, R5, R4?, R5?, R6, R7, A, D, m and E are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: An amphiphilic dendritic dipeptide, comprises a dipeptide(s) comprising one or more of a naturally occurring or synthetic amino acids and a dendron. These are suitable for use in various formulations, films, coatings, membranes and sensors, among other applications.

Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.

Abstract: The present invention provides compounds, pharmaceutical compositions, and methods that can be used to treat pathologies that are due to copper overload or to the presence of reactive oxygen species.

Abstract: The present invention relates to a process for the preparation of (2S,3S)-3-amino-N-cyclopropyl-2-hydroxyalkanamides as well as novel compounds prepared or used in the process.

Abstract: The present invention provides a compound of the formula (I): in which R1, R2, R3, A and n are described and set forth more fully herein. Also provided are their preparation and their application in therapy.

Abstract: The present invention is directed to a process for preparing ?-amino-?-hydroxycarboxamides. The process works with epoxycarboxamides of the formula 2 which are reacted with ammonia or other amines.

Abstract: The present invention relates to a process for the preparation of (2S,3S)-3-amino-N-cyclopropyl-2-hydroxyalkanamides, and their use in the preparation of HCV inhibitors and cathepsin inhibitors.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: The present invention describes a synthetic non-viral vector composition for gene therapy and the use of such compositions for in vitro, ex vivo and/or in vivo transfer of genetic material. The invention proposes a pharmaceutical composition containing 1) a non-cationic amphiphilic molecule or macromolecule and its use for delivery of nucleic acids or 2) a cationic amphiphilic molecule or macromolecule that transforms from a cationic entity to an anionic, neutral, or zwitterionic entity by a chemical, photochemical, or biological reaction and its use for delivery of nucleic acids. Moreover this invention describes the use of these non-viral vector compositions in conjunction with a surface to mediate the delivery of nucleic acids. An additional embodiment is the formation of a hydrogel with these compositions and the use of this hydrogel for the delivery of genetic material. A further embodiment of this invention is the use of a change in ionic strength for the delivery of genetic material.

Abstract: Universal supports for oligonucleotide synthesis include a support material represented by the following formula: In this formula, substituent A is selected from H, alkyl, aryl, or a polymeric or silica base material; substituent B is selected from acyl, aroyl, or a polymeric or silica base material; and substituent C is selected from a dimethoxytrityl group or a protecting group removable under acidic or neutral conditions. For the supports, one of substituents A or B constitutes the polymeric or silica base material. In use, an oligonucleotide is attached to the support at substituent C.

Abstract: Combretastatin derivatives of formula (I), preparation and use thereof are disclosed, wherein: Rf is alkyl with 1-8 carbon atoms and 1-17 fluorine atoms, R is amino, substituted amino, hydroxyl, nitro, halo, alkyloxy, phosphate or amino acid side chain. Said derivatives have a capability to inhibit the polymerization of microtubules and are useful in treatment against tumor and neovascularization.

Abstract: This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders.

Abstract: Processes for the preparation of 4-aminopyrazole and derivatives thereof, such as those of formula (C), which are useful as intermediates in the preparation of pharmaceutical compounds; to certain compounds used in these processes; and to processes for the preparation of said compounds.

Abstract: The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.

Abstract: The present invention is directed to nitrile-oxide precursor compounds, and their preparation and use as an irreversible cross-linking agent in polymers having appropriate functionality, i.e., alkenes, alkynes nitriles, and isocyanates. The present invention is also directed to the use of nitrile oxide compound in filled or unfilled applications such as pressure sensitive adhesives, reactive hot melts, polyurethane dispersions, thermosetting adhesives, thermoplastic adhesives or coatings.

Abstract: This invention relates to synthetic excitatory amino acid prodrugs according to formula (I) and processes for their preparation.

Abstract: The present invention provides novel heterobifunctional and monobifunctional polyethylene glycol derivatives for the pegylation of therapeutically active proteins. The heterobifunctional PEGs which bear two different functional groups as well as the monobifunctional PEGs which contain two similar functional groups, may be used for cross-linking purposes. The cross-linking may be intramolecular between two areas within the same molecule or intermolecular between two separate molecules. The pegylated protein conjugates that are produced, retain a substantial portion of their therapeutic activity and are less immunogenic than the protein from which the conjugate is derived. New syntheses for preparing such bifunctional derivatives are described.

Abstract: A process for producing a 2-alkylcysteinamide, which comprises hydrolysis of a 4-alkylthiazolidine-4-carboxamide represented by the general formula (2) or a salt thereof: wherein R represents a lower alkyl group having 1–4 carbon atoms; and each of R1 and R2 independently represents hydrogen or a lower alkyl group having 1–4 carbon atoms, or R1 and R2 are linked together to form an alicyclic, structure having 4–7 carbon atoms, excluding the case where both R1 and R2 are hydrogen, to give a 2-alkylcysteinamide represented by the general formula (1) or a salt thereof wherein R represents a lower alkyl group having 1–4 carbon atoms. Cells of a microorganism or treated products thereof having activity of stereoselective hydrolysis of a 2-alkyl-L-cysteinamide are allowed to act on the compound represented by the general formula (1) to yield a 2-alkyl-L-cysteine.

Abstract: Novel analogs of arachidonylethanolamide are presented which have higher affinities for the cannabinoid CB1 and/or CB2 receptor sites. Further, most of the analogs exhibit greater metabolic stability than arachidonylethanolamide. The improved receptor affinity and selectivity and/or greater metabolic stability make these analogs therapeutically useful as medications for relief of pain caused by cancer and nausea caused by chemotherapy, as well as for peripheral pain. The compounds may also be useful as oral and topical contraceptives, in suppression of the immune system, enhancement of appetite and in treatment of psychomotor disorders, multiple sclerosis and hypertension.

Abstract: Disclosed are compounds of formula X, which are useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions comprising compounds of formula X and methods of preparing the compounds of formula X are also disclosed.

Abstract: Colchicine derivatives represented by the formula (I) with a halogen or nitric ester group, or pharmaceutically acceptable salts thereof, are described. Pharmaceutical compositions containing the same as effective components are also described. The colchicine derivatives were found to have anticancer, anti-proliferous and immunosuppressive function. Methods for preparing the colchicines derivatives are also provided.

Abstract: The present invention relates to synthetic cationic lipids, liposome formulations and the use of such compounds to introduce functional bioactive agents into cultured cells.

Abstract: The present invention provides novel monofunctional polyethylene glycol aldehydes for the pegylation of therapeutically active proteins. The pegylated protein conjugates that are produced, retain a substantial portion of their therapeutic activity and are less immunogenic than the protein from which the conjugate is derived. New syntheses for preparing such aldehydes are described.

Abstract: Compositions including a conjugate of ?-difluoromethylornithine can be applied topically to reduce hair growth.

Abstract: The present invention provides a process for efficiently producing an optically active ?-amino acid and an optically active ?-amino acid amide. After contacting with cells or processed cells thereof having an ability to asymmetrically hydrolyse, a water solvent is substituted with at least one solvent selected from the group consisting of linear, branched, or cyclic alcohol having 3 or more carbon atoms and the optically active ?-amino acid is preferentially precipitated from the alcohol solution. The addition of basic compounds, particularly potassium compounds to the alcohol solution containing the optically active ?-amino acid amide, which is obtained after the separation of the optically active ?-amino acid, enables the purification of the amide without the inclusion of amino acid into amino acid amide. Thus, the amide is subjected to the step of racemization and then recycled.