Abstract: The present invention relates to a crystalline form of a phenyl carbamate derivative compound and a use thereof, and more particularly, to a more thermodynamically stable crystal, i.e., a Pattern 1 crystalline form, and a preparation method thereof. Amorphous and crystalline forms were prepared using various solvents, and among these, a thermodynamically stable Pattern 1 crystalline form and a pharmaceutical use of this crystalline form are provided.

Abstract: A composition forms a resist underlayer film showing improved adhesiveness to a resist pattern. A resist underlayer film-forming composition for lithography, including: a polymer that has a structure of Formula (1a), Formula (1b), or Formula (2) below on an end of the polymer; and an organic solvent: (where R1 is a hydrogen atom or a methyl group; each of R2 and R3 is independently a hydrogen atom or an organic group such as a hydrocarbon group, etc., the hydrocarbon group optionally has at least one of a hydroxy group and a methylthio group as substituent(s); R4 is a hydrogen atom or a hydroxy group; Q1 is an arylene group; v is 0 or 1; y is an integer of 1 to 4; w is an integer of 1 to 4; x1 is 0 or 1; and x2 is an integer of 1 to 5).

Abstract: The present invention considers derivatized nanomolecules with proven effectiveness to bind to actinides, more specifically uranium, during in vivo, ex vivo, in vitro or in situ assays. When assayed in vivo, the invention showed a reduction in at least kidney damage due to exposition to uranium.

Abstract: A method for the synthesis of an amino acid analogue or a salt, solvate, derivative, isomer or tautomer thereof comprising the steps of: (i) subjecting an amino acid containing a metathesisable group to metathesis with a compound containing a complementary metathesisable group of formula (I) or (II): (Formulae (I), (II)) wherein R1 and R2 are independently selected from H and substituted or unsubstituted C1 to C4 alkyl; each R3 is either absent or independently selected from a heteroatom, a substituted or unsubstituted C1 to C20 alkyl, and a substituted or unsubstituted C1 to C20 alkyl group interrupted by one or more heteroatoms; and each X is independently selected from H and an effector molecule; in the presence of a reagent to catalyse the metathesis to form a dicarba bridge between the amino acid containing a metathesisable group and the compound containing a complementary metathesisable group; and (ii) reducing the dicarba bridge to form a saturated dicarba bridge, wherein the reagent used to catalyse s

Abstract: The invention relates to a process for the aminohydroxylation of alkenes using N-oxycarbamate reagents, e.g. N-acyloxycarbamate, N-alkyloxycarbonyloxycarbamate and N-aralkoxycarbonyloxycarbamate reagents. The invention particularly relates to an intermolecular aminohydroxylation reaction that can be carried out in the absence of added base. The invention also relates to novel N-oxycarbamate reagents that are stable crystalline materials. The process of the invention is useful in the synthesis of compounds having a vicinal amino alcohol moiety, such as biologically active compounds.

Abstract: Alkyl and/or alkenyl glycerol carbamate prepared by reacting a carbonate selected from the group consisting of glycerol carbonate, diglycerol carbonate, polyglycerol carbonate and mixtures thereof, with an amine of the general formula (I): HNR1R2??(I) wherein R1 represents a hydrogen atom or a hydrocarbon group selected from the group consisting of alkyl groups and alkenyl groups having from 1 to 22 carbon atoms and R2 represents a hydrocarbon group selected from the group consisting of alkyl groups and alkenyl groups having from 4 to 22 carbon atoms, and cyclic alkyl groups having 5 or 6 carbon atoms, are described along with methods for their use as pearlizing agents in surface-active preparations.

Abstract: New nitrogen-containing compounds are provided that comprise multiple hydroxyl moieties and photoresist compositions that comprise such nitrogen-containing compounds. Preferred nitrogen-containing compounds comprise 1) multiple hydroxyl substituents (i.e. 2 or more) and 2) one or more photoacid-labile groups.

Abstract: The invention provides poly(ethylene glycol)-lipid conjugates for use in drug delivery.

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: A conjugate comprising L-DOPA covalently linked to at least one ?-aminobutyric acid (GABA) moiety, an ester and/or an addition salt thereof are disclosed, as well as uses thereof for treating a neurodegenerative disease or disorder.

Abstract: Described are alkoxylated urethanes. Specifically, the alkoxylated urethanes are non-isocyanate urethanes (NIUs). The non-isocyanate urethanes that are described can be used as low-foam surfactants and, more particularly, as low-foam wetting agents.

Abstract: The object of the invention are compounds of the formula (2) wherein R1 is H, methyl or ethyl, R2 is C1- to C4 alkyl, A is a C2- to C4 alkylene group, m is number from 10 to 400, n is 1, 2, 3, 4, or 5, a method for their production and their use in the production of polyurethane prepolymers.

Abstract: The invention relates to a process for the preparation of N-protected ?-aminoaldehydes by deacetalization of the acetal functional group of corresponding N-protected ?-aminoacetals using formic acid.

Abstract: The invention relates to a process for the aminohydroxylation of alkenes using N-oxycarbamate reagents, e.g. N-acyloxycarbamate, N-alkyloxycarbonyloxycarbamate and N-aralkoxycarbonyloxycarbamate reagents. The invention particularly relates to an intermolecular aminohydroxylation reaction that can be carried out in the absence of added base. The invention also relates to novel N-oxycarbamate reagents that are stable crystalline materials. The process of the invention is useful in the synthesis of compounds having a vicinal amino alcohol moiety, such as biologically active compounds.

Abstract: The compounds of the invention exhibit antiprotozoal, antimicrobial, and anticancer properties that are useful for the treatment or prevention of infections or cancer in a patient (e.g., a human). For example, the compounds and methods described herein can be used for the treatment or prevention of protozoal infections such as leishmaniasis, malaria, and trypanosoma infections, bacterial infections such as S. aureus and C. albicans, and cancers such as breast, colon, lung, or prostate cancer. The invention further provides methods of synthesizing such compounds as well as kits useful for administering the compounds.

Abstract: The invention relates to addition compounds which are obtainable by reacting a) one or more polyisocyanates containing uretdione groups with b) one or more compounds of the formula (I) Y—(XH)n??(I) with the proviso that at least 50% of the free isocyanate groups of component a) are reacted with the compounds of the formula (I) to give an intermediate which contains uretdione groups, and subsequently the intermediate is reacted with c) one or more compounds of the general formula (II) Z—NHRm??(II) with the proviso that all free NCO groups optionally still present and at least 20% of uretdione groups originally used are reacted with Z—(NHR)m. The invention further relates to the use of the addition compounds as dispersants and dispersion stabilizers, and to a process for preparing them.

Abstract: The present invention relates to compositions comprising certain active compounds which are suitable as repellents, and to their use for preventing an infection of humans or of animals by the infectious states of parasitic flatworms (platyhelminths).

Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of certain cyclohexyl carbamate compounds of formula (I) given below, preferably as skin and/or hair lightening (whitening) actives. The invention further relates to compositions and cosmetic, dermatological or therapeutic products comprising one or more compounds of formula (I) suitable for lightening human skin and/or hair and corresponding methods.

Abstract: A process for manufacturing a compound of Formula (I) which has cis-conformation and wherein R1 represents a 1-phenyl-C1-C4alkyl or 1-naphthyl-C1-C4alkyl group, wherein the phenyl or naphthyl moiety of R1 is unsubstituted or substituted with one or more C1-C4alkoxy groups and the carbon atoms in 2-, 3-, and/or 4-position of the alkyl part of R1 are, independently of the phenyl or naphthyl moiety of R1 and independently of one another, unsubstituted or substituted with C1-C4alkoxy and/or silyloxy or, preferably, are unsubstituted or substituted with one C1-C4alkoxy group and/or silyloxy group per carbon atom, and R2 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, in which process a compound of Formula (II) wherein R3 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, and R1 and R2 have the same meaning as in formula (I); is treated with a base at a temperature of 0° C.

Abstract: The present invention relates to the cosmetic, dermatological or pharmaceutical (therapeutic) use of compounds of formula (I) or a cosmetically acceptable salt of a compound of formula (I) or a mixture containing two or more of these compounds or the salts thereof wherein R1 denotes hydrogen or an organic radical having 1 to 14 carbon atoms, R2 denotes an organic radical having 1 to 14 carbon atoms, and wherein optionally R1 and R2 are covalently bonded to one another, preferably so that a 3 to 8 membered ring is formed, for the lightening of skin and/or hair. The invention further relates to compositions and cosmetic, dermatological or pharmaceutical preparations (compositions) comprising one or more compounds of formula (I) suitable for lightening human skin and/or hair and corresponding methods.

Abstract: The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L3 is a single bond, etc, R3 is alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.

Abstract: The present invention provides addition compounds, which suitable as dispersants and as dispersion stabilizers, and to the salts of the said compounds. The invention further provides processes for preparing these addition compounds, to their use as dispersants and dispersion stabilizers for organic and inorganic pigments and also fillers in organic and aqueous systems, and to pulverous or fibrous solids coated with such dispersants and intended for incorporation into liquid systems.

Abstract: The present disclosure relates to photoactivable protecting groups containing a diarylsulfide chromophore, a method for the synthesis thereof and their use as photoactivable protecting groups using maskless photolithography based array synthesis.

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: Addition-fragmentation agents of the formula are disclosed: wherein R1, R2 and R3 are each independently Z-Q-, a (hetero)alkyl group or a (hetero)aryl group with the proviso that at least one of R1, R2 and R3 is Zm-Q-, Q is a linking group have a valence of m+1; Z is an ethylenically unsaturated polymerizable group, m is 1 to 6; each X1 is independently —O— or —NR4—, where R4 is H or C1-C4 alkyl, and n is 0 or 1.

Abstract: The present invention relates to improved gel masses prepared from a reaction mixture of NCO prepolymers and selected compounds containing groups reactive towards isocyanate groups. This invention is also directed to a process for the production of these gel masses and to the production of pressure-distributing elements comprising these gel masses.

Abstract: There is provided a copolymer and polymeric particle comprising the copolymer, a method of producing a polymeric particle, a copolymeric binder, a method of producing a copolymeric binder, a near infrared radiation-sensitive coating composition, a negative working lithographic offset printing plate, a method of producing a negative working lithographic offset printing plate and methods of imaging the plate and printing with the imaged plate.

Abstract: Novel compounds having the structure (I) are provided, where R1 represents hydrogen, an alkyl group containing 1 to 3 C atoms, or a group R3; R2 represents an alkyl group containing 2 to 22 C atoms, wherein said group can be linear, branched, or cyclic and saturated or olefinically mono- or polyunsaturated; R3 represents a saturated alkyl group containing 1 to 3 C atoms, wherein said alkyl group is substituted by a group —O—(CH2—CHZ—O)p—H at one of the C atoms; X, Y, and Z independently represent hydrogen or a methyl group; and n and m independently represent a number ranging from 1 to 45, and p represents a number ranging from 0 to 45, provided that the sum of n+m+p has to range from 2 to 70. The compounds having structure (I) are excellent low-foaming surfactants.

Abstract: The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.

Abstract: A conjugate comprising L-DOPA covalently linked to at least one ?-aminobutyric acid (GABA) moiety, an ester and/or an addition salt thereof are disclosed, as well as uses thereof for treating a neurodegenerative disease or disorder.

Abstract: Disclosed are new compounds having utility in applications, including as reactants and intermediates in for the formation of polymers and polymeric materials especially useful as hydrogels for ophthalmic lenses.

Abstract: The present invention relates to renin inhibitor compounds having the structure and their use in treating cardiovascular events and renal insufficiency.

Abstract: Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described.

Abstract: This disclosure relates to methods for preparing an enantiomerically enriched N-carboxyanhydride of an amino alpha acid of the formula (IIIa) or (IIIb): from a compound of the formula (IIa) or (IIb), respectively: wherein R1, R2, and R3 are as defined in the disclosure.

Abstract: Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition.

Abstract: 2-Oxo-1,3-dioxolane-4-carboxylic acid and derivatives thereof, according to the following formula, in which R1 represents a negative charge, hydrogen or may be methyl or ethyl or an n-valent radical, which may be substituted with at most n?1 further 2-oxo-1,3-dioxolane-4-carboxyl groups, as well as a process for their preparation by means of carboxylation of the corresponding epoxides, a process for their transesterification and their use for the preparation of hydroxyurethanes and as end groups for the blocking of amines.

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

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 present invention relates to a ruthenium carbonyl complex that is represented by the following Formula (1): RuXY(CO)(L)??(1) (in the Formula (1), X and Y, which may be the same or different from each other, represent an anionic ligand and L represents a tridentate aminodiphosphine ligand which has two phosphino groups and a —NH— group), its production method, and a method for production of alcohols by hydrogenation-reduction of ketones, esters, and lactones using the complex as a catalyst. The ruthenium carbonyl complex of the invention has a high catalytic activity and it can be easily prepared and handled.

Abstract: The present invention relates to a new process for the synthesis of alkyl phosphinic acids, and more particularly to a coupling reaction between an alkylhalide and a hypophosphorous acid derivative in the presence of an amine and an amineoxide.

Abstract: There is provided a compound of Formula and salts thereof wherein R1 is an imine or an alkylated imine, said imine or alkylated imine comprising a linear or branched alkyl group of length C1 to C5; R2 are each independently (a) an unsubstituted or substituted linear or branched alkyl group of chain length C1-7; (b) an aryl substituted alkyl group, wherein said aryl group is substituted, (c) an alkoxy substituted alkyl group, wherein said alkoxy group is substituted by a methoxy group or an alkoxy group substituted with an alkoxy group; or (d) an H atom; wherein said substituents in (a) and (b) are selected from hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, nitro, oxo and fluoro groups. R3 and R4 are linear or branched alkyl groups of length C1 to C6 constituting a ketal or a cyclic ketal. The compounds claimed may be used for the manufacture of a medicament.

Abstract: New nitrogen-containing compounds are provided that comprise multiple hydroxyl moieties and photoresist compositions that comprise such nitrogen-containing compounds. Preferred nitrogen-containing compounds comprise 1) multiple hydroxyl substituents (i.e. 2 or more) and 2) one or more photoacid-labile groups.

Abstract: A compound, composition, method of synthesizing and using the compound of formula 1 are disclosed. The compound of formula I also comprises of salts, polymorphs, 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 hepatic and genetic disorders related to copper overload. Multiple other compounds may be added with the instant claimed compounds and may be delivered as a pharmaceutical dose suitable for treating Wilson's disease.

Abstract: Disclosed are formulation and optimization protocols for delivery of therapeutically effective amounts of biologically active agents to liver, tumors, and/or other cells or tissues. Also provided are compositions and uses for cationic lipid compounds of formula (I). The invention also relates to compositions and uses for stealth lipids of formula (XI). Also provided are processes for making such compounds, compositions, and formulations, plus methods and uses of such compounds, compositions, and formulations to deliver biologically active agents to cells and/or tissues.

Abstract: The present invention relates to compounds of formula (I) below in which: —R1 and R3 represent, independently of one another, a methoxy group optionally substituted by one or more fluorine atoms, —R2 and R4 represent, independently of one another, a hydrogen atom or a methoxy group optionally substituted by one or more fluorine atoms, —A represents a ring chosen from the group comprising aryl and heteroaryl groups, said ring possibly being substituted by or fused to a heterocycle, —X represents a nitrogen atom or a CH group, and —Z1 represents a hydrogen atom or a halogen atom, preferably fluorine, and —Z2 represents a hydrogen atom, a halogen atom, preferably fluorine, a C1 to C4 alkyl group, an aryl group or a —CN, —SO2NR12R13, —SO2R9, —COOR15 or —COR15 group, and also to the pharmaceutically acceptable salts thereof, the isomers thereof and the prodrugs thereof.

Abstract: Disclosed are fluorinated acrylate compounds.

Abstract: Prodrugs of alpha-2-delta ligands, pharmaceutical compositions of prodrugs of alpha-2-delta ligands, methods of making prodrugs of alpha-2-delta ligands, and methods of using prodrugs of alpha-2-delta ligands and pharmaceutical compositions of prodrugs of alpha-2-delta ligands to treat various diseases are disclosed.

Abstract: Prodrugs of alpha-2-delta ligands, pharmaceutical compositions of prodrugs of alpha-2-delta ligands, methods of making prodrugs of alpha-2-delta ligands, and methods of using prodrugs of alpha-2-delta ligands and pharmaceutical compositions of prodrugs of alpha-2-delta ligands to treat various diseases are disclosed.

Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.

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.