Abstract: The present invention relates to certain ester and nitrile derivatives of formula (I): wherein one dotted line represents a carbon-carbon single or double bond and the other dotted lines each represent a carbon-carbon single bond; R1 is a hydrogen atom or a methyl group, R2 is a methyl or ethyl group, R3 is a hydrogen atom or a methyl group, R4 is a hydrogen atom or a methyl group or said R4 taken together with the bond between carbon atom 2 and 3 form a cyclopropane; and X represents a CN or a COOR5 group, R5 representing a C1-5 alkyl group; with the compound being in the form of any one of its pure stereoisomers or mixtures thereof. These compounds are useful perfuming ingredients.

Abstract: To provide a novel polyimide precursor or polyimide which can provide a liquid crystal alignment film having a low volume resistivity, a liquid crystal aligning agent containing these polymers, a liquid crystal alignment film and a novel diamine which is useful as the starting material of these polymers.

Abstract: Prodrugs of guanfacine, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for improving the pharmacokinetics of guanfacine or minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration are provided herein.

Abstract: It is reported herein that certain muscle diseases and conditions, including forms of muscular dystrophy, are characterized by impaired insulin-dependent signaling in the muscle tissue, in essence, a form of insulin resistance. The present disclosure relates to therapeutic agents, compositions and methods for treating a muscle disease or condition characterized by impaired insulin-dependent signaling by targeting components of the defective insulin signaling pathway. The disease or condition may be treated by administering a therapeutic agent that activates the insulin signaling pathway, in particular, therapeutic agents that act post-insulin receptor to modulate intracellular effector molecules. An exemplary modulator is metformin. Metformin may be administered alone or may be co-administered with another therapeutic agent for treating the muscle disease or condition, such as a corticosteroid.

Abstract: The invention relates to the production of carbamates in a single reactor (one-pot) using solid catalysts, involving the reaction between at least one nitro compound, an organic carbonate of formula (OR)(OR?)C?O, a gas selected from hydrogen gas and a mixture of gases containing hydrogen and hydrogen precursor compounds, and a catalyst that has at least one metallic oxide and can also contain an element of groups 8, 9, 10 and 11 of the periodical table. The carbonates obtained can be transformed into their corresponding isocyanates.

Abstract: The present invention provides methods of forming carbamates, ureas, and isocyanates. In certain embodiments these methods include the step of reacting an amine with an ester-substituted diaryl carbonate to form an activated carbamate which can be further derivatized to form non-activated carbamate or a urea. The urea or carbamate can be subjected to a pyrolysis reaction to form isocyanate.

Abstract: The invention is directed to a process for preparing aromatic carbamates which comprises the reaction of an aromatic amine with an organic carbonate in the presence of a catalyst characterized in that Zn4O(OAc)6 is used as catalyst.

Abstract: Reaction products prepared from reactants including: (a) at least one compound of structural Formula (I): wherein R1 is selected from aryl and heteroaryl; X is selected from a direct bond, —O—, —S—, —NH—, alkylene, cycloalkylene, heterocyclylene, arylene, alkarylene, and heteroarylene; Y is a substituted alkylene group having at least two contiguous carbon atoms and which can be interrupted by one or more —O—, —S—, or —NH— moieties as defined herein, wherein the alkylene group of Y has substituents independently selected from —OH, —NH2, —SH, cycloalkyl, heterocyclyl, aryl, and heteroaryl, or two hydrogen atoms on the same carbon atom of Y are replaced by carbonyl, and wherein at least two substituents of Y are each independently selected from —OH, —NH2, and —SH, as defined herein; and (b) at least one isocyanate functional material.

Abstract: A method for the production of N-aryl carbamates (urethanes) and N-aryl isocyanates is described in which aromatic nitro compounds are subjected to a reductive carbonylation in the presence of carbon monoxide and organic compounds carrying hydroxyl groups, wherein the carbonylation is carried out in the presence of metal complex catalysts, for which anionic N,O chelate ligands of the general type [M(N˜O)?2] and [M(O˜N˜N˜O)2?] containing a bi- or trivalent transition metal of the groups 5 to 11 are used.

Abstract: The invention relates to the field of antibiotic compositions, both inside and outside the medical field. Presented is a new class of antibiotic compounds around the lead compound (3,4-dichloro-phenyl)-carbamic acid 2-isobutoxycarbonylamino-1-methyl-ethyl ester, which are especially useful for combating infections with gram-positive bacteria and especially MRSA.

Abstract: An improved process for preparing dabigatran etexilate, as well as analogous compounds of formula 7, is described.

Abstract: The invention relates to a method for producing enantiomers form of 2,3-diaminopropionic acid derivatives of formula (I) by asymmetric hydrogenation from compounds of formula (II).

Abstract: A continuous process for the production of an aromatic urethane from the reaction of an aromatic amine and an organic carbonate comprising the steps of passing the aromatic amine and the organic carbonate through a fixed bed reactor containing a zinc carbonate catalyst to produce the aromatic urethane and collecting the aromatic urethane.

Abstract: Embodiments of this disclosure, among others, encompass methods for generating alkenes under mild thermolytic conditions that can provide almost total conversion of a precursor compound to an alkene without isomerization or the need to chromatographically purify the final product By selectively blocking the amino and carboxy groups of the de?vatized amino acid, the methods of the disclosure provide for the synthesis of a peptide having the vinylglycine moiety at either the carboxy or the amino terminus of the peptide The mild conditions for the thermolytic removal of an o-NO2-phenyl substituted aryl group ensure that there is minimal if any damage to thermally sensitive conjugates such as a peptide bearing the vinylglycine The methods of the present disclosure have practical applications for the preparation of unsaturated compounds under mild, thermolytic conditions.

Abstract: Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

Abstract: A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: a method for producing the same, and a pharmaceutical composition useful for the prevention or treatment of diseases, in which chymase is involved, including the compound of having the formula (I), or its pharmaceutically acceptable salt, or a solvate thereof are provided.

Abstract: The invention encompasses processes for the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.

Abstract: The invention encompasses processes for the synthesis of (S)-(+)-3-(aminomethyl) -5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.

Abstract: Disclosed is a process for preparing single enantiomers of beta-amino phenylbutyric acid derivatives and pharmaceutically acceptable salts thereof, which affords the desired compounds having special optical configuration. The process comprises a step of chemical synthesis and a step of resolving the optical isomers of beta-amino phenylbutyric acid derivatives with a resolving agent. The resolving step comprises reacting the optical isomers with resolving agents, such as di-para-toluoyl-L-tartaric acid and di-para-toluoyl-D-tartaric acid. The obtained R-beta-amino phenylbutyric acid derivatives (I) have high optical purity, and the total yield of the accumulative resolution of the laevo and the dextro isomer is up to above 70%.

Abstract: Carbamate preparation process comprising, the reaction between at least: an amine or polyamines, an organic carbonate of formula (OR)(OR?)C?O, a catalyst which is formed by at least a support selected from at least a metal oxide, a microporous material, a mesoporous material, an anionic laminar compound of hydrotalcite type or their derivatives or an organic polymer and which may further contain a metal from groups 8, 9, 10 and 11 of the periodical system. The carbonates obtained can be transformed in their corresponding isocyanates.

Abstract: The present invention provides a photoresist composition comprising a resin, an acid generator and a compound represented by the formula (I): wherein R1 represents a C2-C12 alkyl group which can have one or more hydroxyl groups, etc., R2 and R3 each independently represent a hydrogen atom, etc., R4, R5 and R6 each independently represent a hydrogen atom, etc., A1 represents a single bond or a C1-C2 alkylene group in which one or more —CH2— can be replaced by —O—.

Abstract: The present invention provides a compound represented by the formula (C1): wherein Rc2 represents a C6-C10 aromatic hydrocarbon group having at least one nitro group and Rc1 represents a group represented by the formula (1): wherein Rc4 represents a hydrogen atom etc., Rc5 represents a C1-C30 divalent hydrocarbon group, and Rc3 represents a group represented by the formula (3-1), (3-2) or (3-3): wherein Rc6, Rc7, Rc8, Rc9, Rc10, Rc11, Rc12, Rc13 and Rc14 each independently represent a C1-C30 hydrocarbon group, and a photoresist composition comprising a resin, an acid generator and the compound represented by the formula (C1).

Abstract: The present invention relates to a process for preparing aldehydes by reacting an ?,?-unsaturated carboxylic acid or a salt thereof with carbon monoxide and hydrogen in the presence of a catalyst comprising at least one complex of a metal of transition group VIII of the Periodic Table of the Elements with at least one compound of the formula (I), where Pn is pnicogen; W is a divalent bridging group having from 1 to 8 bridge atoms between the flanking bonds; R1 is a functional group capable of forming at least one intermolecular, noncovalent bond with the —X(?O)OH group of the compound of the formula (I); R2, R3 are each in each case optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl or hetaryl or together with the pnicogen atom and together with the groups Y2 and Y3 if present form an optionally fused and optionally substituted 5- to 8-membered heterocycle; a, b and c are each 0 or 1; and Y1,2,3 are each, independently of one another, O, S, NRa or SiRbRc, where Ra,b,c are each H or in each c

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: The present invention relates to a novel catalyst for producing N-substituted carbamates, the preparation of the catalyst and an improved method for producing N-substituted carbamates from these novel catalysts. The active component of the catalyst is a heteropoly acid and the catalyst support comprises a metal oxide or a metalloid oxide. The catalyst can be used to promote the reaction of carbamate and amine, thereby generating N-substituted carbamates with high yield. In the presence of the catalyst, the reaction conditions are relatively mild, the catalytic activity and selectivity of the reaction are high, and the reaction time is relatively short. Furthermore, the catalyst can be conveniently separated from the reaction system and recycled. therefore, the catalyst can be used to facilitate the further scale-up test and commercial application.

Abstract: Compounds of the formula I: wherein R1, R2, X and N are as defined in the specification; E is N, CH; A? and A? are terminal groups as defined in the specification. The compounds have utility as HIV-1 protease inhibitors.

Abstract: The present invention provides for reagents for the introduction of colorimetric-oxycarbonyl protecting groups, compounds bearing colorimetric-oxycarbonyl protecting groups, and the use thereof in solid-supported organic syntheses of oligonucleotides, polypeptides, polysaccharides, and combinatorial libraries.

Abstract: The ring-containing modified resin is represented by the following chemical formula (1) R1[—(—O—CO—NH—R2—NH—CO—O—R3—)p—O—R4]q??(1) (in the chemical formula (1), R1 is a dehydroxyl residue of a resin having a benzene ring and/or a condensed ring and hydroxyl group: —R2— is deisocyanate group derived from an organic diisocyanate: —R3— is a dehydroxyl residue of polyol having number-average molecular weight of 200 to 30000: p is 1 to 3: —R4 is a hydrogen atom, alkyl group having 1 to 18 carbons, phenyl group: q is the same number as the number of the dehydroxyl residue of R1).

Abstract: The invention relates to a method for producing N-aryl carbamates (urethanes) and N-aryl isocyanates. According to said method, aromatic nitro compounds are subjected to a reductive carbonylation in the presence of carbon dioxide and organic compounds that bear hydroxyl groups and the carbonylation is carried out in the presence of metal complexing catalysts. Anionic N,O-chelate ligands of the general formulae [M(N˜O)?2] and [M(O˜N˜N˜O)2?], containing a divalent or trivalent transition metal of groups 5-11 are used for the catalysts.

Abstract: The present invention relates to novel compounds, methods of preparing these compounds, and pharmaceutical compositions comprising these compounds. These compounds are carbamate prodrugs that convert to active inhibitors of the IMPDH enzyme in vivo. The compounds and pharmaceutical compositions of this invention are particularly well suited for activation and subsequent inhibition of the IMPDH enzyme activity. Consequently, these prodrugs may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds and compositions of this invention.

Abstract: This invention is related to hydroxylamino derivatives of the general formula (I) wherein n is 0, 1 or 2; R1 and R2, independently of each other, are H, OH or OCH3; R3 is H or CH3; R4 is H, C1-C3 straight or branched alkyl or, together with R3, forms a five to seven-membered carbocyclic ring; and R5 and R6, independently of each other, are H or C1-C5 straight or branched alkyl and the pharmaceutically acceptable salts or prodrug thereof, for the preparation of medicaments useful for the prevention, treatment and diagnosis of CNS degenerative disorders related to protein misfolding and/or misaggregation. The invention also relates to novel compounds included in formula (I), to a method for preparing said compounds and to pharmaceutical compositions containing them.

Abstract: A process for the preparation of a nonnatural amino acid represented by the following formula (C): which is characterized by reacting a compound represented by the following formula (A1), a compound represented by the following formula (A2) and a compound represented by the following formula (A3) (step 1): to form a compound represented by the following formula (B): and then subjecting the compound (B) to deprotection of protective groups of carboxyl groups and to decarboxylation (wherein X1 and X2 are a leaving group, R1 is an aromatic group, an unsaturated heterocyclic group, or R6CO group, R2 and R3 are a protected carboxyl group, R4 is a protected amino group, R5 is hydrogen atom, an aliphatic hydrocarbon group, an aromatic group, or a heterocyclic group, R6 is an aromatic group or an unsaturated heterocyclic group, etc., and p, q and r are an integer of 0 to 10).

Abstract: The present invention is directed to D-homoandrosta-17-yl-carbamate derivatives as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.

Abstract: In one aspect, the present invention provides a composition of a covalent conjugate of a GABA analog with a drug. In another aspect, the present invention provides methods for treating pain and neurological disorders using the conjugates of GABA analogs.

Abstract: The present invention provides methods of forming carbamates, ureas, and isocyanates. In certain embodiments these methods include the step of reacting an amine with an ester-substituted diaryl carbonate to form an activated carbamate which can be further derivitized to form non-activated carbamate or a urea. The urea or carbamate can be subjected to a pyrolysis reaction to form isocyanate.

Abstract: Methods of preparing a class of oxazolidinones useful to impede bacterial growth are disclosed.

Abstract: The invention encompasses processes for the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.

Abstract: The present invention relates to aniline derivatives of formula I: wherein R1, R2, R3, R4, Z and q are as defined herein; or salts thereof and their use.

Abstract: Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

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: An efficient new route for the preparation of dihydroeponemycin, an active eponemycin derivative, is provided, which includes the synthesis of the intermediate compound, a hydroxymethyl-substituted enone. In addition, a method is provided for synthesizing inhibitors, which includes PI?-modified analogues. These analogues selectively bind to a major immunoproteasome catalytic subunit LMP2 and inactivate its proteolytic activity in a method of treating diseases, including myeloma and other cancers, Huntington's disease and Alzheimer's disease.

Abstract: The present invention relates to compounds which are derivatives of cytisine or acetylcholine which exhibit activity as agonists, partial agonists or antagonists of nicotinic acetylcholine receptors and may be used in modulating these receptors and in treating mood disorders in patients in need of therapy.

Abstract: Disclosed is a method for preparing a compound of Formula 1 by contacting compound of Formula 2 with R1—NH2 in the presence of a carboxylic acid and a method for preparing a compound of Formula 2 by contacting a compound of Formula 4 with phosphorus tribromide. wherein R1 is H, C1-C4 alkyl, cyclopropyl, cyclopropylmethyl or methylcyclopropyl; R2 is CH3 or Cl; R3 is C1-C6 alkyl or C3-C6 alkenyl, each optionally substituted with up to 3 halogen and up to 1 phenyl; and X is Cl or Br. Also disclosed is a method for preparing a compound of Formula 5 wherein R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 that is characterized by preparing the compound of Formula 1 by the method above.

Abstract: Disclosed is a method for producing aminocarbonyl compounds of the general formula (I) wherein R1 and R2 can be identical or different and represents hydrogen, alkyl, alkenyl, alkynyl, or aryl, X represents hydrogen, alkyl, alkenyl, alkynyl, aryl, or OR3, R3 representing hydrogen, alkyl, alkenyl, alkynyl, or aryl. According to said method, an aldehyde of the general formula (II) R1CO??(II) wherein R1 has the meaning indicated above, is reacted with an imine of the general formula (III) wherein R2 and X have the meaning indicated above, in the presence of a catalyst. Aminocarbonyles are obtained by means of catalyzed Mannich reactions with aldehydes. For example, if ?-unbranched aldehydes are reacted with previously formed N-Boc imines in the presence of (S)-proline as a catalyst, the desired ?-amino aldehydes are obtained at excellent yields, diastereoselectivities and enantioselectivities.

Abstract: Urethanes are prepared by oxidative carbonylation of at least one amino compound in the presence of carbon monoxide, oxygen and organic, at least one hydroxyl-group-carrying compound. The carbonylation is carried out in the absence of halogen-containing promoters. The carbonylation is also carried out in the presence of a metal complex catalyst which contains neutral bidentate N-chelate ligands of the (N˜N) type, two monoanionic N,O-chelate ligands of the general type (N˜O)? or tetradentate dianionic chelate ligands (O˜N˜N˜O)2?.

Abstract: The present invention relates to a method of treating pain using a compound of formula wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to certain novel derivatives of formula (I).

Abstract: The invention encompasses the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, via the intermediate, (3R)-5-methyl-3-(2-oxo-2{[(1R)-1-phenylethyl]amino}ethyl)hexanoic acid.

Abstract: The invention relates to the use of piperazine compounds of formula (I) or the agriculturally useful salts of piperazine compounds of formula (I) as herbicides, the variables in formula (I) being defined as cited in the claims and the description.

Abstract: The present invention provides a compound of the general formula (I), wherein X is the connection between the CO-hydrazine and the NR1-oxalic acid or ester group, and uses and synthesis methods. These compounds represent amino acid derivatives, wherein the amine group is turned into an acidic group by the oxalic acid group and the carboxylic acid is turned into an amine functionality by the hydrazine group; as well as peptidomimetics comprising the compound and methods for their synthesis.

Abstract: The invention relates to the inhibition of histone deactylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.