Abstract: The invention provides a method for synthesizing a compound of formula wherein each R independently represents an optionally substituted aryl, heteroaryl, alkyl, perfluoroalkyl, cycloalkyl, alkoxy, aryloxy, acyl, carboxyl, hydroxyl, halogen, amino, nitro, cyano, sulfo or sulfhydryl group, in ortho, meta or para position to the cycloalkylamine moiety; R1 and R2 each independently represents a hydrogen atom, a lower alkyl group or a cycloalkyl group; R3 represents a hydrogen group, substituted aryl, heteroaryl, alkyl, perfluoroalkyl, cycloalkyl, alkoxy, aryloxy group; Y represents an oxygen atom, a sulfur atom, a NH group, a NR4 group or a CH2 group; R4 represents a hydrogen atom or an alkyl, aryl or a heteroaryl group; and n and m each independently represents an integer from 1 to 5; or a pharmaceutically acceptable salt thereof; or a precursor thereof; wherein the method comprises one or more of the following steps: (a) reacting a compound of formula (II) wherein R, R3, Y, n and m are as defined abo

Abstract: Provided is a small molecule compound as represented by structural formula (I). The product of the present invention in various concentrations and dosages can achieve an obvious change in the growth period of hairs, promoting the growth of the hairs, thus exhibiting an obvious effect of promoting hair growth. In addition, changes in the weight of a mouse in each group are slow, indicating that the test compound does not cause weight loss in an animal.

Abstract: This invention relates to novel 1-cycloalkyl- or 1-heterocyclyl-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.

Abstract: Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. The halogenated stilbene analogs include nitrogen heteroaryl groups and/or amino groups on the stilbene ring.

Abstract: Embodiments of the present disclosure provide compositions including ketamine analogues, salts, and disalts, pharmaceutical compositions including ketamine analogues, salts, or disalts, methods of treatment of a condition or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.

Abstract: There is provided a process for the preparation of a compound of formula (I), wherein R1, R2, R3, R4, X and Y are as described in the description. Such compounds may, for example, be useful intermediates in the synthesis of drugs such as Dronedarone.

Abstract: Novel compounds generally referred to herein as cationic oligomeric phenylene ethynylenes (OPEs), methods of synthesizing OPEs and various uses for the OPEs are described. The compounds can be synthesized in both symmetrical (S-OPE) and non-symmetrical (N-OPE) forms. Suitable uses include sensor and biocidal applications. Reusable structures incorporating the OPEs that are able to capture and release biological species of interest are also described.

Abstract: The present invention relates to a pharmaceutical formulation comprising: a) one or more NO-releasing NSAID(s) of formula (I); b) one or more surfactants; c) a carbonyl scavenger compound selected from free acid forms, salts, carboxylic acid esters derivatives of a compound of formula (II) H2N—(CH2)m—(C6H4)—COOH??(II) wherein m=0-10; and d) optionally an oil or semi-solid fat and/or a short-chain alcohol.

Abstract: Disclosed is a process of enantioselectively forming an aminoxy compound of Formula (3) In formula (3) R1 is one of an aliphatic group and an alicyclic group. R2 is one of hydrogen, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group and an arylalicyclic group. R3 is one of hydrogen, halogen, hydroxyl, and an aliphatic group with a main chain having 1 to about 10 carbon atoms. The respective aliphatic, alicyclic, aromatic, arylaliphatic or arylalicyclic groups of R1, R2, and R3 comprise 0 to about 3 heteroatoms independently selected from the group consisting of N, O, S, Se and Si. The process includes contacting a carbonyl compound of Formula (1) and a nitroso compound of Formula (2) in the presence of a chiral catalyst.

Abstract: There is provided a process for the preparation of a compound of formula (I), wherein R1, R2, R3, R4, X and Y are as described in the description. Such compounds may, for example, be useful intermediates in the synthesis of drugs such as Dronedarone.

Abstract: An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases. The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].

Abstract: The disclosed is a comb-shaped graft copolymer, including a back bone of PMMA and side chains of a random copolymer, a block copolymer, or a homopolymer polymerized of a monomer having a carbon-carbon double bond. The monomer can be alkyl acrylate, styrene, and the likes. The side chains terminal is grafted to a nitro-oxy compound.

Abstract: Compounds of Formula (I) wherein R1 is C1-C4alkyl or C1-C4 haloalkyl; R2 is C1-C4alkyl; R3 is hydrogen or halogen; R4 is hydrogen, C1-C4alkyl or C1-C4halogenalkyl; R5 is hydrogen, halogen, C1-C4alkyl or C1-C4halogenalkyl; R6 is hydrogen, halogen, C1-C4alkyl, C2-C6alkenyl or C3-C6alkinyl; R7 is hydrogen, halogen, C1-C6alkyl, C2-C6alkenyl, C3-C6alkinyl, C3-C6cycloalkyl-C3-C6alkinyl, halophenoxy, halophenyi, C1-C6haloalkyl, C1-C6haloakoxy, C2-C6haloalkenyl, or C2-C6haloalkenyloxy; R8 is hydrogen, halogen, C1-C4alkyl, C2-C6alkenyl or C3-C6alkinyl; with the provisio that at least one of R6, R7 and R8 is different from hydrogen; n is 0 or 1, are suitable for use as microbriocides.

Abstract: The inventions disclosed include methods of treating cancers and related neoplasias, especially prostate cancer, with pharmaceutically acceptable salts comprising lipophilic cation moieties linked to nitroxide or linked to hydroxylamine anti-oxidant groups.

Abstract: The invention provides a method for producing an arylhydroxylamine compound efficiently and safely under mild conditions. The method involves contacting a nitroaryl compound with a hydrogen source in the presence of a platinum catalyst supported on amino group-coordinated silica and a poisoning agent.

Abstract: Disclosed is a core-shell microparticle (10) which is produced by heating a mixture of a crosslinked microparticle (11) having an alkoxyamine group (12) and a monomer to 100 to 180° C. to cause graft polymerization. The crosslinked microparticle (11) is produced by allowing a seed particle to absorb a monomer mixture comprising 15 to 99% by mass of a crosslinkable monomer and 1 to 85% by weight of a monomer having an alkoxyamine group, and then adding a polymerization initiator to the resulting product to cause the polymerization of the monomer mixture.

Abstract: Compounds of Formula (I) wherein R1 is C1-C4alkyl or C1-C4 haloalkyl; R2 is C1-C4alkyl; R3 is hydrogen or halogen; R4 is hydrogen, C1-C4alkyl or C1-C4halogenalkyl; R5 is hydrogen, halogen, C1-C4alkyl or C1-C4halogenalkyl; R6 is hydrogen, halogen, C1-C4alkyl, C2-C6alkenyl or C3-C6alkinyl; R7 is hydrogen, halogen, C1-C6alkyl, C2-C6alkenyl, C3-C6alkinyl, C3-C6cycloalkyl-C3-C6alkinyl, halophenoxy, halophenyi, C1-C6haloalkyl, C1-C6haloakoxy, C2-C6haloalkenyl, or C2-C6haloalkenyloxy; R8 is hydrogen, halogen, C1-C4alkyl, C2-C6alkenyl or C3-C6alkinyl; with the provisio that at least one of R6, R7 and R8 is different from hydrogen; n is 0 or 1, are suitable for use as microbriocides.

Abstract: This invention relates to a process for producing an oxime comprising reacting a ketone and hydroxylamine in the presence of a carboxylic acid and/or its salt in a system consisting of an aqueous phase and a hydrophobic solvent phase.

Abstract: The present invention is directed to a process of making ?-aminooxyketone and ?-hydroxyketone compounds. The synthetic pathway generally involves reacting an aldehyde or ketone substrate and a nitroso substrate in the presence of a catalyst of the formula (IV): wherein Xa-Xc represent independently nitrogen, carbon, oxygen or sulfur and Z represents a 4 to 10-membered ring with or without a substituent and optionally a further step to convert the ?-aminooxyketone compound formed to the ?-hydroxyketone compound. The present invention results in ?-aminooxyketone and ?-hydroxyketone compounds with high enantioselectivity and high purity. The present invention is also directed to a catalytic asymmetric O-nitroso Aldol/Michael reaction. The substrates of this reaction are generally cyclic ?,?-unsaturated ketone substrate and a nitroso substrate.

Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.

Abstract: The present invention provides a novel oxime ether derivative represented by the following formula (I), or salt thereof, that can be industrially produced advantageously, and can function as a fungicide for agricultural and horticultural use that has reliable effects and can be used safely, and a fungicide for agricultural and horticultural use that contains at least one of these compounds as an active ingredient thereof. In addition, the present invention provides a novel ketone derivative that is a production intermediate of the oxime ether derivative.

Abstract: Compounds of formula (I), in which the substituents are as defined in claim 1, are suitable for use as microbiocides.

Abstract: Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. The halogenated stilbene analogs include nitrogen heteroaryl groups and/or amino groups on the stilbene ring.

Abstract: Compounds of formula (I) in which the substituents are as defined in claim 1, are suitable for use as microbiocides.

Abstract: There is provided a process for the preparation of a compound of formula II, wherein R1, R2, R3 and R4 are as described in the description. Such compounds may, for example, be useful intermediates in the synthesis of drugs such as Dronedarone.

Abstract: The present invention provides an efficient method for preparing atomoxetine in high yield. (R)-methylhydroxylaminopropanol compound of formula (II) in the present invention is used as an intermediate without the need for resolution processes.

Abstract: A compound of the present invention, or a pharmaceutically acceptable salt thereof is indicated by formula (1) below: wherein, R1, R2, R3, R4, R5, R6, Q, R8, and R9 have the same meanings as R1, R2, R3, R4, R5, R6, Q, R8, and R9 in the specification.

Abstract: The invention provides compounds that inhibit protein kinases, prodrugs of the compounds, intermediates and methods of synthesizing the compounds and/or prodrugs, pharmaceutical compositions including the compounds and/or prodrugs and methods of using the compounds and/or prodrugs in a variety of contexts, including, for example, in the treatment and/or prevention of various diseases that are responsive to protein kinase inhibition and/or that are mediated, at least in part, by inappropriate kinase activity.

Abstract: Disclosed is a process of enantioselectively forming an aminoxy compound of Formula (3) In formula (3) R1 is one of an aliphatic group and an alicyclic group. R2 is one of hydrogen, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group and an arylalicyclic group. R3 is one of hydrogen, halogen, hydroxyl, and an aliphatic group with a main chain having 1 to about 10 carbon atoms. The respective aliphatic, alicyclic, aromatic, arylaliphatic or arylalicyclic groups of R1, R2, and R3 comprise 0 to about 3 heteroatoms independently selected from the group consisting of N, O, S, Se and Si. The process includes contacting a carbonyl compound of Formula (1) and a nitroso compound of Formula (2) in the presence of a chiral catalyst.

Abstract: The present invention relates to a process for the preparation of a compound of formula wherein R1 is selected from C1-6-alkyl, C3-6-cycloalkyl and aralkyl, and wherein R2 at each occurrence independently is halogen or C1-6-alkyl, and m is an integer from 0 to 4, Q is selected from halogen, —NO2 and —NR3R4, wherein R3 and R4 are independently selected from hydrogen, C1-6-alkyl, C3-6-cycloalkyl, aryl, aralkyl, mesyl and tosyl, or wherein R3 and R4 together form a C4-6-alkylene group, Y at each occurrence is hydrogen or a hydroxy protection group W that can be hydrolytically cleaved under acidic conditions, and n is an integer from 1 to 3, and n is an integer from 1 to 3, with the proviso that n and m together are not greater than 5.

Abstract: The invention relates to a process for preparing aminoglycol by reacting ketoximes with ethylene oxide under basic conditions to give a substituted 2-hydroxyethyl ketoxime and subsequently reacting the latter with an acid to give aminoglycol.

Abstract: An oxylamino group-containing compound represented by the following formula: R1—B-A-B—R2, wherein R1 represents a polymerizable group, R2 represents an oxylamino group-containing group or an oxylamino derivative-containing group, B represents an ester linkage or an amide linkage, and A represents an optionally substituted alkylene group having 2 to 12 carbon atoms.

Abstract: Provided is a process for the formation of nitrated compounds by the nitration of hydrocarbon compounds with dilute nitric acid. Also provided are processes for preparing industrially useful downstream derivatives of the nitrated compounds, as well as novel nitrated compounds and derivatives, and methods of using the derivatives in various applications.

Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect choline acetyltransferase; a method for assaying pesticidal activity of a test substance, which comprises measuring the activity of a choline acetyltransferase in a reaction system in which the choline acetyltransferase contacts with a test substance, and the like.

Abstract: A compound having the general formula shown below: where R1-6 are independently selected from the group consisting of an electron withdrawing group, an alkyl group, an aryl group, hydrogen, a heteroaryl group, and a five or six member ring structure formed from the R1 and R2 pair, the R3 and R4 pair, the R4 and R5 pair, or the R5 and R6 pair; R7 is a substituted or unsubstituted aryl group; and Y is a nucleophile.

Abstract: There is provided a process for the preparation of a compound of formula (I), wherein R1, R2, R3, R4, X and Y are as described in the description. Such compounds may, for example, be useful intermediates in the synthesis of drugs such as Dronedarone. Intermediate steps of the process comprise formulae according to (II) and (III).

Abstract: A subject-matter of the invention is alkoxyamines resulting from ?-phosphorated nitroxides corresponding to the formula: in which R represents an alkyl radical having a number of carbon atoms ranging from 1 to 3, R1 represents a hydrogen atom or a residue: in which R3 represents an alkyl radical having a number of carbon atoms ranging from 1 to 20, and R2 represents a hydrogen atom, an alkyl radical having a number of carbon atoms ranging from 1 to 8, a phenyl radical, an alkali metal, such as Li, Na or K, H4N+, Bu4N+ or Bu3HN+, exhibiting a kinetic dissociation constant kd, measured at 120° C. by EPR, of greater than 0.05 s?1. These compounds can be used as initiators for the (co)polymerizations of at least one monomer which can be polymerized by the radical route.

Abstract: This invention is related to hydroxylamino derivatives of the following 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 the compounds and to pharmaceutical compositions containing them.

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: An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases. The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].

Abstract: An indene derivative for selectively modulating the activities of peroxisome proliferator activated receptors (PPARs) having the following formula (I): wherein, R1 is C1-6 alkyl, C1-6 alkenyl, or C3-6 cycloalkyl, each of which is unsubstituted or substituted with one or more phenyl groups; R2 is H, CN, CO2Ra, CH2CO2Ra, CONRbRc, or phenyl; R3 is C1-6 alkyl, C3-6 cycloalkyl, naphthyl, phenyl, being each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, CN, NH2, NO2, ORa, phenyloxy, C1-6 alkyl, and C3-6 cycloalkyl; and R4, R5, R6, and R7 are each independently H, OH, OSO2CH3, O(CH2)mRe, CH2Rf, OCOCH2ORg, OCH2CH2ORg, OCH2CH?CHRg, or pyridine-2-yloxy, or R5 and R6 together form OCH2O.

Abstract: Problem To provide a method for producing an arylhydroxylamine compound efficiently and safely under mild conditions. Means for Solving the Problem The present invention relates to a method for producing anarylhydroxylamine compound, which comprises contacting a nitroaryl compound with a hydrogen source in the coexistence of a platinum catalyst supported on amino group-coordinated silica and a poisoning agent.

Abstract: The present invention is directed to a process of making ?-aminooxyketone and ?-hydroxyketone compounds. The synthetic pathway generally involves reacting an aldehyde or ketone substrate and a nitroso substrate in the presence of a catalyst of the formula (IV): wherein Xa—Xc represent independently nitrogen, carbon, oxygen or sulfur and Z represents a 4 to 10-membered ring with or without a substituent and optionally a further step to convert the ?-aminooxyketone compound formed to the ?-hydroxyketone compound. The present invention results in ?-aminooxyketone and ?-hydroxyketone compounds with high enantioselectivity and high purity. The present invention is also directed to a catalytic asymmetric O-nitroso Aldol/Michael reaction. The substrates of this reaction are generally cyclic ?,?-unsaturated ketone substrate and a nitroso substrate.

Abstract: A process is described for preparing isoxazoles of the formula I where the substituents are as defined below: R1 is hydrogen, C1-C6-alkyl, R2 is C1-C6-alkyl, R3, R4, R5 are hydrogen, C1-C6-alkyl, or R4 and R5 together form a bond, R6 is a heterocyclic ring, n is 0, 1 or 2; which comprises preparing an intermediate of the formula VI where R1, R3, R4 and R5 are as defined above, followed by halogenation, thiomethylation, oxidation and acylation to give compounds of the formula I. Also novel intermediates for preparing the compounds of the formula I and novel processes for preparing the intermediates are described.

Abstract: The invention at hand provides at least dinitroxylated diamantanes. In addition, it provides methods for producing substituted diamantanes with high yields and selectivity. According to the invention, dinitroxylated diamantanes are suitable for being reacted with nucleophiles to form the corresponding disubstituted diamantanes. Surprisingly, it was discovered that at least dinitroxylated or hydroxylated diamantanes are rearranged in the presence of a strong acid, creating at least 4,9-nitroxylated or hydroxylated diamantanes. On the basis of this, 4,9-substituted diamantanes are able to be produced in a targeted manner by reaction with further nucleophiles.

Abstract: Acylfulvene analogs, which inhibit tumor growth, especially solid tumor growth, and which have an adequate therapeutic index to be effective for in vivo treatment are provided herein. The compounds described herein are useful as anti-neoplastic agents, i.e., to inhibit tumor cell growth in vitro or in vivo, in mammalian hosts, such as humans or animals, e.g., domestic animals, and are effective against solid tumors, hematologic malignancies and multi-drug resistant cancers/tumors. The present compounds can be used alone or they can be used in combination with one or more anti-cancer or anti-tumor agents.

Abstract: This invention provides a catalyst composition for preparing hydroxylamine, which comprises palladium, a platinum compound, a germanium compound and a carrier, wherein a halogen concentration of the composition is no more than 10 ppm. The catalyst composition is prevented from poisoning by halogens, and therefore the catalyst composition has high selectivity and catalytic activity. Further, the weight ratio of palladium and platinum in the catalyst composition ranges from 100:1 to 1000:1, such that the catalyst composition can be used to solve the commonly observed problem, i.e., decreased selectivity due to the excessive amount of platinum.

Abstract: The present invention provides new chemically modified 4-dedimethylaminotetracycline compounds that can be substituted with aryl, alkenyl, or alkynyl groups. The 7, 8, and/or 9 positions and methods for preparing such compounds. Other tetracycline compounds include the 4-dedimethylaminotetracycline derivatives with an oxime group, NH-Alkyl, or N—NH-Alkyl group substituted at the C4 position as well as C2 Mannich derivatives. The present invention also provides a method of treating a mammal suffering from conditions or diseases by administering to the mammal an effective amount of the new chemically modified tetracycline compounds.

Abstract: A stabilized hydroxylamine solution is disclosed. The stabilized solution comprises a selected stabilizer, which can be added during manufacture and/or storage of the hydroxylamine solution.

Abstract: It is an object of the present invention to provide a process for producing a hydroxylamine by reacting a salt of hydroxylamine with an alkali compound, where the yield reduction due to formation of a complex between the produced hydroxylamine and a salt produced as a by-product or adsorption of the hydroxylamine to the by-product salt is decreased, and a high-concentration and high-purity hydroxylamine is safely produced at a high yield. The process for producing a hydroxylamine of the present invention comprises a reaction step of reacting a salt of hydroxylamine with an alkali compound to obtain a hydroxylamine while keeping the reaction solution at a pH of 7 or more, a purification step of purifying the hydroxylamine by ion exchange, and a concentration step of concentrating the hydroxylamine by distillation at the column bottom.