Abstract: Methods of making sequence-defined polymers and sequence-defined polymers. The methods are based on the orthogonal reactivity of monomers having at least two different functional groups. The sequence-defined polymers can be used in various applications. For example, the SDPs (e.g., pH sensitive SDPs) are used in cell lysis methods or as molecular vehicles to transport drug cargo into cells.

Abstract: A composition comprising an acrylamide compound (A1) having an ester structure and a molecular weight of from 150 to 200 and an acylphosphine oxide polymerization initiator (B1) is provided.

Abstract: The invention provides compounds and methods, for example, to carry out organocatalytic Michael additions of aldehydes to cyclically constrained nitroethylene compounds catalyzed by a proline derivative to provide cyclically constrained ?-substituted-?-nitro-aldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96 to >99% e.e.). The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to cyclically constrained protected ?-amino acid residues, which are essential for systematic conformational studies of ?-peptide foldamers. New methods are also provided to prepare other ?-amino acids and peptides. These new building blocks can be used to prepare foldamers, such as ?/?-peptide foldamers, that adopt specific helical conformations in solution and in the solid state.

Abstract: Chiral amino compounds, methods of preparation and uses thereof. Tamiflu can be obtained from the said compounds. Multi-substituted chiral tetrahydropyrrolyl amine which can be used as intermediate compounds of medicament can also be produced by the said compounds.

Abstract: Provided are novel processes for the preparation of Saxagliptin and novel intermediates employed in the process for preparing Saxagliptin.

Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.

Abstract: The present invention relates to the field of perfumery. More particularly, it concerns compounds comprising at least one ?-thio carbonyl or nitrile moiety capable of liberating an active molecule selected from an ?,?-unsaturated ketone, aldehyde or nitrile. The present invention concerns also the use of said compounds in perfumery as well as the perfuming compositions or perfumed articles comprising the invention's compounds. (I) wherein: a) m represents an integer from 1 to 6; b) Pro represents a hydrogen atom or a group susceptible of generating an odoriferous ?,?-unsaturated ketone, aldehyde or nitrile and is represented by the formulae (II) or (II?) in which the wavy line indicates the location of the bond between said Pro and the sulfur atom S; and at least one of the Pro groups is of the formula (II) or (II?).

Abstract: The present invention relates to a chemocatalytic liquid-phase process for the direct one-stage amination of alcohols to primary amines by means of ammonia in high yields using a catalyst system containing at least one transition metal compound and a xantphos ligand.

Abstract: The present invention provides triterpenoids produced from natural compounds such as oleanolic acid, ursolic acid, betulinic acid, and hederagenin.

Abstract: The present invention relates to a cationic lipid of formula (I) having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

Abstract: The present invention relates to a novel process for the preparation of 1-H-pyrrolidine-2,4-dione derivatives and to novel intermediates and to a process for their preparation.

Abstract: The present invention provides novel human anti-influenza antibodies and related compositions and methods. These antibodies are used in the diagnosis and treatment of influenza infection.

Abstract: The present invention relates to cosmetic and/or personal care formulations and/or compounds. In one embodiment, the present invention relates to ester compounds that can be used in various personal care formulations and/or compounds. In another embodiment, the present invention relates to branced ester compounds having a molecular weight of at least about 1,500 daltons that can be used in various personal care formulations and/or compounds.

Abstract: The invention pertains to a new route to prepare ?-functionalized carboxylic acid esters in a one-pot reaction, by reacting an olefinic acid ester in the presence of a catalyst system, comprising a Rh(I)-complex, together with an aryl boron or a diamine as nucleophilic compounds, and under oxygen-free conditions and elevated temperatures.

Abstract: A process provides for producing chiral prostacyclin derivatives of Formula (I) in high yield from meso anhydrides.

Abstract: A method for preparing a trans-{4-[(alkylamino)methyl]cyclohexyl}acetic acid, which is useful as a raw material compound for manufacture of medicaments and the like, comprising the step of reducing amide group of a compound represented by the following general formula (6) (R1 represents hydrogen atom or a C1-6 alkyl group, and R2 represents a C1-6 alkyl group, a C3-6 cycloalkyl group, a (C3-6 cycloalkyl)(C1-6 alkyl) group, a C6-10 aryl group, or a C7-12 aralkyl group).

Abstract: Pleuromutilin derivative compounds of the following formula, and uses thereof for the treatment of diseases mediated by microbes, are disclosed:

Abstract: Surface-modified zirconia nanoparticles and methods for making and using the same are provided. The surface-modifiers include non-metallic organic derivatives, comprising at least one hydroxamate functionality, wherein at least some of the non-metallic organic derivatives are attached to at least some of the zirconia nanoparticles.

Abstract: Methods of halogenating a carbon containing compound having an sp3 C—H bond are provided. Methods of fluorinating a carbon containing compound comprising halogenation with Cl or Br followed by nucleophilic substitution with F are provided. Methods of direct oxidative C—H fluorination of a carbon containing compound having an sp3 C—H bond are provided. The halogenated products of the methods are provided.

Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”).

Abstract: A polymer for resist use is obtainable from a monomer having formula (1) wherein R1 is H, CH3 or CF3, R2 and R3 are a monovalent hydrocarbon group, R4 to R9 are hydrogen or a monovalent hydrocarbon group, R10 is a monovalent hydrocarbon group or fluorinated hydrocarbon group, A1 is a divalent hydrocarbon group, k1 is 0 or 1, and n1A is 0, 1 or 2. A resist composition comprising the polymer displays a high dissolution contrast during organic solvent development.

Abstract: The present invention discloses high yielding enantioselective process for synthesis of Oseltamivir from readily available starting material, cis-1,4-butene diol. The process features incorporation of chirality using sharpless asymmetric epoxidation (AE) and diastereoselective Barbier allylation and construction of cyclohexene carboxylic acid ester core through a ring closing metathesis (RCM) reaction. Further also disclosed herein is synthesis of (?)-methyl 3-epi-shikimate.

Abstract: The invention relates to a process for the preparation of trans 4-amino-cyclohexil ethyl acetate HCl wherein d) hydrogenating 4-nitrophenyl acetic acid in a protic solvent at a temperature between 40-50° C. in the presence of Pd/C under 0.1-0.6 bar overpressure, and e) further hydrogenating the 4-aminophenyl acetic acid obtained in situ in step a) at a temperature between 50-60° C. under 1-4 bar overpressures, then f) heating to reflux the 4-aminocyclohexil acetic acid obtained in step b) for 1-3 hours in hydrochloric ethanol, and if desired after removing the solvent acetonitrile was added to the residue obtained and distilled off.

Abstract: Chiral amino compounds, methods of preparation and uses thereof. Tamiflu can be obtained from the said compounds. Multi-substituted chiral tetrahydropyrrolyl amine which can be used as intermediate compounds of medicament can also be produced by the said compounds.

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: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also provides selective herbicidal compositions comprising, firstly, geminally alkoxy/alkylspirocyclically substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.

Abstract: Disclosed are neuraminidase inhibitor compounds and pharmaceutical compositions with improved bioavailability and/or improved efficacy and methods of treating influenza using the compounds and pharmaceuticals compositions.

Abstract: A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.

Abstract: Suggested are biocide compositions, comprising (a) esters based on ketocarboxylic acids, (b) biocides, and optionally (c) oil components or co-solvents and/or (d) emulsifiers. The compositions exhibit an improved stability even if stored at temperatures between 5° and 40° C. over a longer period.

Abstract: The present application relates to processes for the preparation of intermediates useful in the manufacture of oseltamivir and the H3PO4 salt of oseltamivir, Tamiflu®. The application further relates to novel intermediate and compounds and oseltamivir analogs and to pharmaceutical compositions comprising said analog compounds. The application further relates to a method of using the novel analogs of oseltamivir to treat or prevent influenza.

Abstract: The invention provides compounds and methods, for example, to carry out organocatalytic Michael additions of aldehydes to cyclically constrained nitroethylene compounds catalyzed by a proline derivative to provide cyclically constrained ?-substituted-?-nitro-aldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96 to >99% e.e.). The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to cyclically constrained protected ?-amino acid residues, which are essential for systematic conformational studies of ?-peptide foldamers. New methods are also provided to prepare other ?-amino acids and peptides. These new building blocks can be used to prepare foldamers, such as ?/?-peptide foldamers, that adopt specific helical conformations in solution and in the solid state.

Abstract: A biobased plasticizer and a surface covering are disclosed. The biobased plasticizer includes an ester formed as a reaction product of a furan derivative selected from the group consisting of furoic acid, furfural and furfuryl alcohol reacted with a carboxylic acid or an alcohol, or includes an ester formed as a reaction product of a biobased aromatic compound and a biobased aliphatic compound. The surface covering is plasticized with a composition comprising an ester formed as a reaction product of a functionalized aromatic heterocyclic compound reacted with a carboxylic acid or an alcohol.

Abstract: The present invention relates to a chemocatalytic liquid-phase process for the direct one-stage amination of alcohols to primary amines by means of ammonia in high yields using a catalyst system containing at least one transition metal compound and a xantphos ligand.

Abstract: Disclosed are a process suited to large scale synthesis with high yield for producing oseltamivir phosphate, in which a preparation of oseltamivir phosphate which is highly safe as a pharmaceutical product can be produced, and an intermediate compound for producing oseltamivir phosphate. In this production process, an intermediate compound represented by general formula (V) is synthesized by employing Michael reaction/Michael reaction/Horner-Wadsworth-Emmons reaction, and oseltamivir phosphate is produced by converting the substituent groups in this intermediate compound.

Abstract: The present disclosure relates to surface-modified zirconia nanoparticles, methods for making and using the same, and high index of refraction films made therefrom. The provided zirconia nanoparticles are surface modified with ligands that include N-hydroxyurea functionalities. The provided ligands also can contain compatibilizing groups that allow the provided surface-modified zirconia nanoparticles to be incorporated into an organic matrix. High index of refraction films can be made using these organic matrices.

Abstract: To provide a method for recovering a precious metal from a solution containing precious metal ions, an extracting agent or adsorbent used therefor, and a back-extracting agent or desorbent. An extracting agent or adsorbent in which precious metal ions are extracted or adsorbed, is brought into contact with a back-extracting agent or desorbent containing a sulfur-containing amino acid derivative represented by the following formula (I): wherein R1 is a methyl group, an ethyl group, a vinyl group, a C3-8 linear, branched or cyclic hydrocarbon group, or a C6-14 aromatic hydrocarbon group, R2's are each independently a hydrogen atom, a methyl group, an ethyl group, a vinyl group, a C3-8 linear, branched or cyclic hydrocarbon group or a C6-14 aromatic hydrocarbon group, and n is 0 or 1, to obtain a solution containing the precious metal ions, which is subjected to a reduction treatment to obtain a precious metal.

Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”).

Abstract: It is possible to produce oseltamivir safely and stably in large quantities by using as a starting material tartaric acid, mannitol or arabinose, via dihydroxyhexenoic acid ester of the formula (4c): (wherein R1, R2 and R6 are same or different and are each alkyl, aryl, substituted aryl, aralkyl, substituted aralkyl or aromatic heterocyclic group, and R1 and R2 are not methyl simultaneously).

Abstract: The invention pertains to a new route to prepare ?-functionalized carboxylic acid esters in a one-pot reaction, by reacting an olefinic acid ester in the presence of a catalyst system, comprising a Rh(I)-complex, together with an aryl boron or a diamine as nucleophilic compounds, and under oxygen-free conditions and elevated temperatures.

Abstract: The present invention relates to compound of formula I, which are functionalized, non-phenolic amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.

Abstract: The present invention provides synthetic routes for preparing various isomers of cyclohexane-based coolants, such as menthyl esters and menthanecarboxamide derivatives, in particular those substituted at the amide nitrogen, for example with an aromatic ring or aryl moiety. Such structures have high cooling potency and long lasting sensory effect, which make them useful in a wide variety of consumer products. One synthetic route involves a copper catalyzed coupling of a primary menthanecarboxamide with an aryl halide, such reaction working best in the presence of potassium phosphate and water. Using this synthetic route, specific isomers can be prepared including the menthanecarboxamide isomer having the same configuration as l-menthol and new isomers such as a neoisomer having opposite stereochemistry at the carboxamide (C-1) position. The neoisomer unexpectedly has potent and long lasting cooling effect.

Abstract: The present disclosure relates to surface-modified zirconia nanoparticles, methods for making and using the same, and high index of refraction films made therefrom. The provided zirconia nanoparticles are surface modified with ligands that include N-hydroxyurea functionalities. The provided ligands also can contain compatibilizing groups that allow the provided surface-modified zirconia nanoparticles to be incorporated into an organic matrix. High index of refraction films can be made using these organic matrices.

Abstract: A salt represented by the formula (X): wherein Q1 and Q2, L1 and L2, ring W1, R5, w, v, Z+ and W10 are defined in the specification.

Abstract: One aspect of the present invention provides a compound represented by formula (I), wherein, R1 is hydrogen or an acetyl group and R2 is a C1-3 straight chain or branched alkyl group. Another aspect of the present invention provides flavor or fragrance compositions comprising at least one compound of formula (I).

Abstract: An initiator for the terminal group of the polymer product of an atom or group radical transfer polymerisation has an activated carboxyl or an amine group which is reacted with an amine or carboxyl (respectively) group containing biologically active compound. The initiator is preferably 4-(3-(2-bromo, 2-methyl-propionate)phenyl)-propionic acid N-hydroxysuccinimide ester or 2-bromo, 2-methyl-propionic acid N-hydroxysuccinimide ester. The monomers preferably comprise a zwitterionic monomer such as 2-methacryloxyethyl-2?-trimethyl ammoniumethyl phosphate inner salt.

Abstract: The present invention relates to compound of formula I, which are functionalized, non-phenolic amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.

Abstract: Process for the preparation of a compound of formula I in the form of a single stereoisomer in crystalline form, comprising deprotecting the amine group in a compound of formula IIa or in a mixture of a compound of formula IIa with a compound of formula IIb and isolating a compound of formula I from the reaction mixture; compounds and salts of compounds of formula I in crystalline form; pharmaceutical compositions comprising such salts; processes for the preparation of intermediates and intermediates in a process for the preparation of a compound of formula I.

Abstract: Pleuromutilin derivative compounds of the following formula, and uses thereof for the treatment of diseases mediated by microbes, are disclosed:

Abstract: Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid, pharmaceutical compositions thereof, methods of making prodrugs of trans-4-(aminomethyl)-cyclohexane-carboxylic acid, and methods of using prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof to treat or prevent various diseases or disorders are disclosed. Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof suitable for oral and topical administration and for administration using sustained release dosage forms are also disclosed.

Abstract: Disclosed are neuraminidase inhibitor compounds and pharmaceutical compositions with improved bioavailability and/or improved efficacy and methods of treating influenza using the compounds and pharmaceuticals compositions.