Abstract: 4-Amino-5-fluoro-3-chloro-6-(substituted)picolinates are prepared from trifluoroacetic acid, p-methoxyaniline, a C1-C4 alkyl propiolate and a substituted methylene amine by a series of steps.

Abstract: A curing resin composition that cures in two stages: photo cure and thermal cure, hardly contaminates a liquid or liquid crystals when in contact with, and provides high adhesive strength, particularly a curing composition that photocures sufficiently even when shadowed by TFT wires, a black matrix, etc. in photocuring; and a sealant, a sealant for ODF (one-drop-fill), and an LCD containing the curing resin composition.

Abstract: An isoxazoline-substituted benzamide compound of formula (1) or a salt thereof: wherein A1, A2 and A3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., W is oxygen atom or sulfur atom, etc., X is halogen atom, C1-C6haloalkyl, etc., Y ia halogen atm, C1-C6alkyl, etc., R1 is —CH?NOR1a, —C(O)OR1c, —C(O)NHR1d, phenyl substituted with (Z)p1, D-14, D-52, D-53, D-55 to D-59, etc., R1a is C1-C6alkyl, etc., R1c is C1-C6alkyl, etc., R1d is hydrogen atom, —C(O)R15, —C(O)OR15, etc., R2 is C1-C6alkyl, —CH2R14a, C1-C6alkynyl, —C(O)R15, —C(O)OR15, etc., further when R1 is —CH?NOR1a, —C(O)OR1c or —C(O)N(R1e)R1d, R2 may be hydrogen atom, R3 is C1-C6haloalkyl, etc., R14a is cyano, —OR25, etc., R15 is C1-C6alkyl, C1-C6haloalkyl, C1-C4alkoxy C1-C4alkyl, C1-C4alkylthio C1-C4alkyl, C3-C6cycloalkyl, C2-C6alkenyl, etc., R25 is C1-C4alkyl, C1-C4haloalkyl, —C(O)R32 or —C(O)OR32, etc., R32 is C1-C6alkyl or C3-C6cycloalkyl, etc., Z is halogen atom, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, etc.

Abstract: The present invention provides a method for producing asymmetrical mono-substituted alkylated compounds of ?-amino acids that are represented by a specific formula, using an aldimine-type Schiff base. In the method of the present invention, the process of alkylating an aldimine-type Schiff base in a medium in the presence of an optically-active quaternary ammonium salt phase-transfer catalyst and an inorganic base is initiated, and subsequently the reaction is quenched at a time earlier than a time for completion of the stoichiometric reaction of the alkylation reaction, so that a mono-substituted alkylated product with high optical purity can be obtained.

Abstract: The present invention relates to a cellulose acetate film used for optical compensation and a retardation enhancer used therein, and relates to a cellulose acetate film which has a high retardation value in the thickness direction (Rth).

Abstract: Compounds of formula (I): wherein R1 to R8, and X? are defined herein. Also disclosed are methods of making and using these compounds.

Abstract: Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.

Abstract: The present invention relates to a process for producing 2-halogenomethylphenyl acetic acid derivatives.

Abstract: The present invention relates to non-steroidal compounds useful in the treatment of inflammatory conditions and pharmaceutical compositions comprising them.

Abstract: Compounds of formula (I): wherein R1 to R8, and X? are defined herein. Also disclosed are methods of making and using these compounds.

Abstract: The disclosure relates to a process for preparing benzofuran derivatives of general formula I: in which R, R1, and R2 are as defined in the disclosure; by coupling the hydroxylamine with a diketone of general formula III: in order to form an oxime that is then cyclized by heating in order to form the desired compound.

Abstract: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as pro-cymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.

Abstract: Compounds of the formula I in which the substituents have the meaning given in the description, processes for preparing these compounds, compositions comprising them and their use for controlling harmful fungi.

Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides a methoxyimino compound, and a fungicide composition comprising same as an active ingredient. The methoxyimino compound of the present invention, which has an excellent antifungal activity against a wide spectrum of fungi even at a low application rate, can be used to protect various crops.

Abstract: The invention relates to the field of pharmaceutical chemistry, specifically to processes for preparing biologically active substances (BAS), in particular creatine amides. What is proposed is a process for preparing creatine amides which comprises treating creatine with para-toluenesulfonic acid in an organic solvent with subsequent reaction of the resultant complex with compounds comprising a primary or secondary amino group in the presence of a condensing agent and a base which are introduced subsequently. The claimed process makes it possible to increase the yield of the end product by 2-5 times in comparison with analogs and also to extend the range of the compounds prepared.

Abstract: The present invention discloses processes for the preparation and isolation of [1,2,4]oxadiazo-3-yl derivatives of carboxylic acids. The derivatives are useful in the treatment of inflammatory diseases and conditions.

Abstract: A curing resin composition that cures in two stages: photo cure and thermal cure, hardly contaminates a liquid or liquid crystals when in contact with, and provides high adhesive strength, particularly a curing composition that photocures sufficiently even when shadowed by TFT wires, a black matrix, etc. in photocuring; and a sealant, a sealant for ODF (one-drop-fill), and an LCD containing the curing resin composition. The curing resin composition contains (A) an oxime ester radical initiator represented by general formula (I), where symbols are as defined in the description, (B) a radical curing resin, (C) a latent epoxy curing agent, and (D) an epoxy resin.

Abstract: The present invention discloses an optically active quarternary ammonium salt having axial asymmetry and a method for producing an ?-amino acid and a derivative thereof using the same. The optically active quarternary ammonium salt having axial asymmetry of the present invention is a chiral phase-transfer catalyst that has a simple structure and that can be produced in a smaller number of process steps. The compound of the present invention is very useful as a phase-transfer catalyst in the synthesis of an ?-alkyl-?-amino acid and a derivative thereof as well as an ?,?-dialkyl-?-amino acid and a derivative thereof. Therefore, the compound of the present invention can be used in the development of novel foods and pharmaceuticals.

Abstract: The present invention relates to non-steroidal compounds useful in the treatment of inflammatory conditions and pharmaceutical compositions comprising them.

Abstract: The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta (TR-Beta). Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them.

Abstract: The present invention relates to a process for producing 2-halogenomethylphenyl acetic acid derivatives.

Abstract: The present invention relates to a product of reaction between a primary and/or secondary amine and one or more active ingredients. By the present invention, there is provided a release of the active component over a longer period of time than by the use of the active itself.

Abstract: Iodylbenzene derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are used as precursors in aromatic nucleophilic substitution reactions. The iodyl group (IO2) is regiospecifically substituted by nucleophilic fluoride to provide the corresponding fluoroaryl derivatives. No-carrier-added [F-18]fluoride ion derived from anhydrous [F-18](F/Kryptofix, [F-18]CsF or a quaternary ammonium fluoride (e.g., Me4NF, Et4NF, n-Bu4NF, (PhCH2)4NF) exclusively substitutes the iodyl moiety in these derivatives and provides high specific activity F-18 labeled fluoroaryl analogs. Iodyl derivatives of a benzothiazole analog and 6-iodyl-L-dopa derivatives have been synthesized as precursors and have been used in the preparation of no-carrier-added [F-18]fluorobenzothiazole as well as 6-[F-18]fluoro-L-dopa.

Abstract: The present invention provides a compound of the following formula (I) below. This compound (I) can be produced by reacting a 2,2?-dimethylene bromide-1,1?-binaphthyl derivative, which can be produced by a relatively small number of processes, with an easily available secondary amine. This compound (I) is useful as a chiral phase-transfer catalyst.

Abstract: Provided herein are compositions including diastereomers in substantially diastereomerically pure form and enantiomers in substantially enantiomerically pure form, and processes for preparing them and converting them to metyrosine.

Abstract: The present invention relates to a product of reaction between a primary and/or secondary amine and one or more active ingredients. By the present invention, there is provided a release of the active component over a longer period of time than by the use of the active itself.

Abstract: In one aspect, the present invention provides a protected ligand precursor having structure XX wherein R8 is independently at each occurrence a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R9-R11 are independently at each occurrence hydrogen, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R8-R11 is a protected hydroxy group or a protected C1-C3 hydroxyalkyl group; and R12 and R13 are independently at each occurrence a protecting group is selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, and C2-C30 aromatic radicals.

Abstract: The present invention relates to benzyloxy- and phenethyl-substituted phenyl-amidine derivatives of formula (I) wherein the substituents are as in the description, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions.

Abstract: Compounds of the formula I in which the substituents have the meaning given in the description, processes for preparing these compounds, compositions comprising them and their use for controlling harmful fungi.

Abstract: The present invention provides 2-azetidinone derivatives, or pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof, comprising formula (I): wherein the substituents are as herein defined. The compounds possess cholesterol absorption inhibitory activity and are accordingly of value in the treatment of disease states associated with hyperlipidaemic conditions.

Abstract: The present invention provides a methoxyimino compound, and a fungicide composition comprising same as an active ingredient. The methoxyimino compound of the present invention, which has an excellent antifungal activity against a wide spectrum of fungi even at a low application rate, can be used to protect various crops.

Abstract: The invention relates to substituted enaminones of Formula I and their derivatives and the discovery that these compounds modulate the effect of ?-aminobutyric acid (GABA) on the GABAA receptor complex in a therapeutically relevant fashion and may be used to ameliorate CNS disorders amenable to modulation of the GABAA receptor complex.

Abstract: The invention describes phenyl-substituted pyridazinones of the formula (I) as herbicides and insecticides. In this formula (I), A, B, G, X, Y and Z are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen, nitro and cyano.

Abstract: This invention relates to a process for preparing R-gossypol L-phenylalaninol dienamine using non-chromatographic purification methods. In particular, the invention is directed to resolution of R- and S-gossypol L-phenylalaninol dienamine by crystallization. R-gossypol L-phenylalaninol dienamine is a useful intermediate for the preparation of R-(?)-gossypol and R-(?)-gossypol acetic acid co-crystal. R-(?)-Gossypol acetic acid and its co-crystal is useful for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.

Abstract: Disclosed are: a method for production of a polyisocyanide derivative having a stable helical main chain structure with a right-handed or left-handed helix or a mixture thereof from a single type of monomer by polymerizing an aromatic isocyanate having a substituent harboring a structure —CONH in the aromatic ring and a hydrophobic moiety having 6 or more carbon atoms in a polymerization solvent, wherein the direction of the helix depends on the polarity of the polymerization solvent; a poly(aromatic isocyanide) derivative produced by the method; and an aromatic isocyanide which is useful as a monomer for use in the production of the poly(aromatic isocyanide) derivative.

Abstract: The present invention provides a chiral phase-transfer catalyst of the following formula (I): The compound (I) can be produced by reacting a 2,2?-dimethylene bromide-1,1?-biphenyl derivative, which can be produced through comparatively small number of steps, with an easily available secondary amine.

Abstract: A process for preparing 2-(chloromethyl)phenylacetic acid derivatives of the formula I, where X is C1-C4-alkoxy or methylamino, by ether cleavage of compounds of the formula II, where R is C1-C4-alkyl, C1-C4-alkoxy, C1-C2-haloalkyl, C1-C4-alkylcarbonyl, C1-C4-alkylcarbonyloxy, halogen, nitro or cyano; n is 2 to 5; and X is as defined above comprises carrying out the reaction in the presence of hydrogen chloride and an inert solvent, and adding a catalyst to the reaction mixture selected from the group consisting of iron, indium and halides, oxides and triflates, thereof.

Abstract: The invention relates to a method for producing 2-chloromethylphenyl acetic acid derivatives of formula (I), in which X represents C1-C4 alkoxy or methylamino, by cleaving the ether bonds in compounds of formula (II), in which R represents C1-C4 alkyl, C1-C4 alkoxy, C1-C2 alkyl halide, C1-C4 alkylcarbonyl, C1-C4 alkylcarbonyloxy, halogen, nitro or cyano, and X has the above-mentioned meaning. The inventive method is characterized in that the transformation takes place in the presence of hydrogen chloride and of an inert solvent, and in that a catalyst selected from the group comprised of: iron, indium or halogenides, oxides or triflates thereof is added to the reaction mixture.

Abstract: There is provided a combination product comprising; (A) melagatran or a pharmaceutically acceptable derivative thereof; and (B) dexamethasone or a pharmaceutically acceptable derivative there of, wherein each of components (A) and (B) is formulated in admixture with a pharmaceutically-acceptable adjuvant, diluent or carrier, as well as the use of such a combination product in the treatment of conditions including disseminated intravascular coagulation.

Abstract: The present invention relates generally to substituted acetic acid derivatives and methods of using them.

Abstract: The invention relates to substituted para-trifluoromethyl phenyl ether compounds and its preparation and use thereof especially. The substituted para-trifluoromethyl phenyl ether compounds of the invention having general formula (I): The substitutes see Description. The compounds of present invention have broad-spectrum activity, and may be used to control diseases in all sorts of plants caused by oomycete, basidiomycete, ascomycete pathogens and deuteromycete, and it may also provide good control efficacy at very low dosage because of the high activity. The compounds of the invention have good insecticidal activity and have good activity against many pests, especially for Carmine spider mite. The compounds are fit for synthetical control against many kinds of pests.

Abstract: There is provided compounds of formula I, R1O(O)C—CH2—(R)Cgl-Aze-Pab-R2I wherein R1 and R2 have meanings given in the description, which are useful as prodrugs of inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (eg thrombosis) or as anticoagulants.

Abstract: Compound of formula (I): wherein: R1 represents aryl, heteroaryl or alkyl which is optionally substituted, or a group of formula —(CO)—CR6R7NR8R9 wherein R6, R7, R8 and R9 are as defined in the description, R2 represents hydrogen or alkyl, R3 represents hydrogen or optionally substituted alkyl, R4 represents a saturated or unsaturated, 7- to 15-membered bicyclic system or optionally substituted alkyl, or R3 and R4, together with the carbon atom carrying them, form a saturated or unsaturated, 3- to 18-membered, mono-, bi- or tri-cyclic system optionally containing one or more hetero atoms selected from O, S and N and optionally substituted, n represents 1 or 2, Ar represents aryl or heteroaryl, R5 represents amino, guanidino, cyano or amidino which is optionally substituted, its optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in pathological conditions involving activated protein C.

Abstract: The present invention relates to the use of amidine compounds in the treatment of amyloid-related diseases. In particular, the invention relates to a method of treating or preventing an amyloid-related disease in a subject comprising administering to the subject a therapeutic amount of an amidine compound.

Abstract: The subject invention provides compounds which are easily metabolized by the metabolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.

Abstract: Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.

Abstract: Novel urea and urethane derivatives of general formula (I) in which R1, R2, R3, R5, R5?, X, Y, B, m, n and o are as defined in Patent Claim 1, and physiologically acceptable salts or solvates thereof are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumors. Osteoporosis, infections and restenosis after angioplasty or in pathological processes maintained or propagated by antiogenesis.

Abstract: A process for preparing xanthine phosphodiesterase V inhibitors, and compounds utilized in said process.

Abstract: A kit of parts containing (a) a pharmaceutical formulation including a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative thereof, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier, and (b) a pharmaceutical formulation including a prodrug of a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative of that prodrug, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier. Components (a) and (b) are each provided in a form that is suitable for administration in conjunction with the other. The kit is useful in the treatment of conditions in which inhibition of thrombin is required or desired.