Abstract: A method of the invention industrially produces heterocyclic mercapto compounds useful as raw materials or intermediates in the synthesis of medicaments or pesticides, or as permanent wave agent, with a high yield and high productivity using easily available starting materials. A heterocyclic mercapto compound represented by Formula (1) (wherein X represents any structure of —O—, —S—, —NH—, and —NR1—; R1 represents any of an alkyl group, alkoxy group and alkoxyalkyl group each having 1 to 6 carbon atoms; Y represents an oxygen atom, a sulfur atom or —NR2—; R2 represents a hydrogen atom or alkyl group having 1 to 6 carbon atoms; and Z1 represents a divalent organic residue having at least one mercapto group) is produced by reacting a metal sulfide or a metal hydrosulfide with a compound represented by Formula (2) (wherein X and Y are as defined in Formula (1); and Z2 represents a divalent organic residue having at least one halogen group) in the presence of a solvent at a pH of 7.0 to 11.0.

Abstract: The present invention relates to stable salts of pyridoxine and ?-hydroxyisocaproic acid (HICA) endowed with enhanced nutritional and/or therapeutical efficacy in respect to their individual effects and to solid compositions containing such salts, particularly suited to oral administration. A method of preparation is also provided.

Abstract: The present invention relates to the o-pyridinequinone disubstituted derivatives, the composition containing the derivatives, the process for preparation of the derivatives and the use of the derivatives. The o-pyridinequinone disubstituted derivatives of the present invention have action of selectivity inhibiting COX-2 and they can be made into pharmaceuticals. The o-pyridinequinone disubstituted derivatives of the present invention have no acute toxicities and are a safe pharmaceutical.

Abstract: The present invention relates to a radiotherapy enhancer that can reduce the radiation dose and adverse drug reactions when used in combination with a cancer radiotherapy. There is provided a radiotherapy enhancer comprising, as an active ingredient, a pyridine derivative represented by general formula (1): wherein R1, R2, and R4 may be the same or different from one another and represent a hydrogen atom, hydroxy group, or protected hydroxy group, excluding the case where R1, R2, and R4 are all a hydrogen atom, and R3 represents a halogen atom, amino group, carboxyl group, carbamoyl group, cyano group, nitro group, alkyl group having 1 to 6 carbon atoms, alkenyl group having 2 to 6 carbon atoms, or carbonyl group containing an alkoxy group having 1 to 6 carbon atoms).

Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: An electron transport system complex II inhibitor comprising 2-pyridinol derivative represented by the general formula [I] wherein R is alkyl or alkenyl optionally having substituent containing halogen, or its tautomer 2-pyridone derivative represented by the general formula [II] wherein R is alkyl or alkenyl optionally having substituent containing halogen, or salt thereof as an active ingredient. The compound inhibits the complex II strongly with nM order activity. Consequently, 2-pyridinol derivative or its tautomer, 2-pyridone derivative, are useful as the complex II inhibitor.

Abstract: The instant invention provides for compounds which comprise substituted 3-aryl-4-hydroxyquinolin-2(1H)-ones that inhibit FAS activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting FAS activity by administering the compound to a patient in need of treatment of cancer.

Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomers of those compounds, are suitable for use as herbicides.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.

Abstract: 4-Aminopicolinic acids having alkyl or alkenyl substituents in the 6-position and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.

Abstract: The present invention relates to novel derivatives of deferiprone. In particular, the present invention relates to fluorinated derivatives of deferiprone or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, processes for the manufacture thereof and their use in the treatment of neurodegenerative diseases caused by the presence of free iron or iron accumulation in neural tissues and in diseases wherein excess iron must be removed or redistributed.

Abstract: Iron modulator compounds of formula (I) are provided for treating amyloidoses wherein R1 is selected from H, C1-6 alkyl, C1-6 alkenyl, C1-6 hydroxyalkyl, C1-6 hydroxyalkenyl, R2 is selected from H, C1-6 alkyl, C1-6 alkenyl, C1-6 hydroxyalkyl, C1-6 hydroxyalkenyl and C6-10 aralykyl in which the aryl group of the aralkyl group is optionally substituted by hydroxy, halo or C1-4 alkyl R3 is selected from H, C1-6 alkyl, C1-6 alkenyl and C1-12 acyl; R4 is selected from H and C1-3 alkyl R5, R6 and R7 are independently selected from H, C1-6 alkyl, C3-7 aryl, and C1-10 aralkyl; the alkyl, aryl and aralkyl groups being optionally substituted by one or more halo, hydroxy and nitro groups or R5 and R7 together with the nitrogen atom to which they are bonded form a heterocyclic ring optionally substituted by one or more hydroxyl groups or a pharmaceutically acceptable tautomer, ester or addition salt thereof.

Abstract: The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula (I); wherein R1 is X with the proviso that R2 is Y; or R1 is T with the proviso that R2 is W; or R1 is X with the proviso that R2 R5 N when taken together form a heterocyclic ring selected from piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl, wherein the group piperidinyl, morpholinyl, pyrrolidinyl or piperazinyl is either unsubstituted or substituted with one to three C1 to C6 alkyl groups.

Abstract: This invention is directed generally to processes for the preparation of compounds of Formula I: wherein R2, R3, R4, R5, X1, X2, X3, X4, X5, X6 are as defined in the specification.

Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.

Abstract: The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.

Abstract: The present invention provides a novel epoxy compound, which can be converted into a cured epoxy resin product having liquid crystal properties by curing with a curing agent. Since the cured epoxy resin product of the present invention exhibits good heat conductivity, it is also useful as an insulating material requiring high heat releasability such as a printed circuit substrate and the like.

Abstract: A compound represented by formula (I); a multifunctional isocyanate composition, containing an adduct formed by treating the compound represented by formula (I) with a compound represented by formula (II); and a microcapsule using the multifunctional isocyanate composition: wherein, in formula (I), R1 represents -L1-X1 or X1; R2 represents a hydrogen atom or -L2-X2; L1 and L2 each independently represent a divalent linking group; X1 and X2 each independently represent a nucleophilic substituent; n represents an integer of 1 to 4; and when n is 2 or more, R1s may be the same or different; and R3—(NCO)m??Formula (II) wherein, in formula (II), R3 represents an arbitrary m-valent linking group; and m represents an integer of 2 or above.

Abstract: The present invention is directed to a 2,4-bis(trifluoroethoxy)pyridine compound represented by formula (1): (wherein X1 represents a fluorine atom or a hydrogen atom) or a salt thereof, and to a drug containing the compound or the salt as an active ingredient. The compound has metabolic resistance in human liver microsome, good absorbability upon oral administration, and excellent ACAT inhibitory activity.

Abstract: 3-Phenoxy-2-pyridone compound can be produced by making the amide compound of the formula (1): wherein R is optionally substituted phenyl; react with a malonoaldehyde derivative such as 3-alkoxypropenal and the like in the presence of a protonic acid.

Abstract: Disclosed are novel compounds useful for the control of harmful organisms, harmful organism control agents using the same, and processes for producing the novel compounds. The useful novel compounds according to the present invention include compounds represented by formula (1).

Abstract: N-substituted carbamoyloxyalkyl-azolium derivatives which have antifungal activity and are useful for the treatment of fungal diseases.

Abstract: 2-(6-Cyano-1-hexyn-1-yl)adenosine, 2-(6-cyano-1-hexyn-1-yl)adenosine 5?-monophosphate, or salts thereof; and drugs containing the same as an active ingredient. The compounds have excellent effects of lowering ocular tension, promoting blood flow in retina, and protecting optic nerve failure and are highly soluble in water. Owing to these characteristics, the compounds are useful as drugs such as remedies for glaucoma and ocular hypertension.

Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for, and intermediates used in, their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.

Abstract: Thiocarbonate and thiocarbamate derivatives of 4-demethylpenclomedine are provided along with pharmaceutical compositions containing them and use for treating cancer. A method for preparing the derivatives is also provided.

Abstract: A catalyst of the invention includes an imide compound having a N-substituted cyclic imide skeleton represented by following Formula (I): wherein R is a hydroxyl-protecting group. Preferred R is a hydrolyzable protecting group. R may be a group obtained from an acid by eliminating an OH group therefrom. Such acids include, for example, carboxylic acids, sulfonic acids, carbonic acid, carbamic acid, sulfuric acid, nitric acid, phosphoric acids and boric acids. The catalyst may include the imide compound and a metallic compound in combination. In the presence of the catalyst, (A) a compound capable of forming a radical is allowed to react with (B) a radical scavenging compound and thereby yields an addition or substitution reaction product of the compound (A) and the compound (B) or a derivative thereof. This catalyst can produce an organic compound with a high selectivity in a high yield as a result of, for example, an addition or substitution reaction under mild conditions.

Abstract: The present invention is directed to substituted N?-(arylcarbonyl)-benzhydrazides, N?-(arylcarbonyl)-benzylidene-hydrazides and analogs thereof, represented by the Formulae I and II: wherein Ar1, Ar2, and R1–R2 are defined herein. The present invention also relates to the discovery that compounds having Formulae I and II are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.

Abstract: The present invention relates to bottom antireflective coating compositions and polymers useful in making such compositions.

Abstract: Pharmaceutical nitrone comprise condensates of an N-hydroxylamine and a physiological aldehyde, providing improved delivery and absorption, enhanced stability and reduced toxicity. Preferred physiological aldehydes are subject to endogenous cellular uptake transport, and include pyridoxal, pyridoxal phosphate, and heme-A. Essentially any physiologically compatible and pharmaceutically active hydroxylamine moiety may be incorporated, such as hydroxylamine moieties of prior pharmaceutical nitrones, and known pharmaceutically active hydroxylamines.

Abstract: The present invention relates to a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-?-D-ribofuranosyluronamide)-N-(2-{N?-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide and to a process for the preparation of, compositions containing and the uses of such a crystalline form.

Abstract: Selective MMP-13 inhibitors are pyridine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is an integer of from 0 to 6.

Abstract: A method for preparing pyridine-2,3-dicarboxylic acid esters of the general formula: wherein R is C1-6-alkyl, C3-6-cycloalkyl, aryl or arylalkyl, and R1 to R3, independently of one another, represent hydrogen, C1-6-alkyl, fluorinated C1-6-alkyl, C1-6-alkoxy, (C1-6-alkoxy)-C1-6-alkyl or (C1-6-alkoxy)carbonyl. These esters are obtained from the corresponding 2,3-dichloropyridine, the corresponding alcohol ROH and carbon monoxide in the presence of a palladium-diphosphine complex and a weak base. Pyridine-2,3-dicarboxylic acid esters are herbicides or intermediates for the preparation of herbicides.

Abstract: The present invention relates to novel compounds that are novel adenosine receptor analogues. Specifically, the compounds of the present invention preferably function as both adenosine receptor agonists and ganglionic blocking agents. To achieve this functionality, the compounds of the present invention, preferably contain a ganglionic blocking motif, is inserted into the adenosine molecule. The ganglionic blocking motif preferably includes an elongated carbon chain that, in a particularly preferred embodiment, contains two terminal amino groups. The ganglionic blocking motif preferably includes a carbon along the elongated carbon chain that is integral to a cyclic ketal that is part of the adenosine molecule. In presently-preferred embodiments, the elongated carbon chain ranges from two to sixteen carbons in length. The compounds of the present invention will be useful for treatment of a variety of conditions including, but not limited to, hypertension, vasodilation, and ischemia.

Abstract: The present invention relates to novel compounds of the formula (I) in which W, X, Y, Z, G, A, B, Q1, Q2 and D are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.

Abstract: A process for preparing 4-haloalkylnicotinic esters of the formula (I), where RF is (C1-C4)-haloalkyl and R is (C1-C6)-alkyl; which comprises a) reacting an aminoketone of the formula (II), RF—C(O)—CH?CH—NH2 ??(II) ?in a condensation reaction under reduced pressure with a compound of the formulae (III) to (V), (R1Z)CH?CH—COOR??(III), (R1Z)2CH—CH2—COOR??(IV), HC?C—COOR??(V), where R1 is (C1-C6)-alkyl and Z is O, S, NR1 or C(O)O, ?to give a compound of the formulae (VI) and/or (VII), RF—C(O)—CH?CH—NH—CH?CH—COOR??(VI) RF—C(O)—CH?CH—NH—CH(ZR1)—CH2—COOR??(VII) b) and subjecting the reaction product to a ring closure reaction.

Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.

Abstract: 2-(6-Cyano-1-hexyn-1-yl)adenosine, 2-(6-cyano-1-hexyn-1-yl)adenosine 5?-monophosphate, or salts thereof; and drugs containing the same as an active ingredient. The compounds have excellent effects of lowering ocular tension, promoting blood flow in retina, and protecting optic nerve failure and are highly soluble in water. Owing to these characteristics, the compounds are useful as drugs such as remedies for glaucoma and ocular hypertension.

Abstract: N-substituted 3-hydroxy-4-pyridinones and metal chelates, methods of preparing N-substituted 3-hydroxy-4-pyridinones and metal chelates, and pharmaceutical compositions containing new N-substituted 3-hydroxy-4-pyridinones and/or their metal chelates. Use of N-substituted 3-hydroxy-4-pyridinones and their metal chelates as pharmaceutical agents for the treatment of diseases, such as parasitic and viral infections, conditions associated with inflammation and infection, and conditions mediated by cell-proliferation or collagen formation.

Abstract: Compounds of Formula (I) are effective in the treatment of a microbial infection.

Abstract: The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.

Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomer of those compounds, are suitable for use as herbicides.

Abstract: This invention relates aryl substituted pyridines, pyrimidines, pyrazines and triazines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein A1, A2, A3, R1-R4, X and Y are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

Abstract: The novel compounds of formula I: wherein R, A, X1, X2, X3, Z and m have the meaning given in claim 1, and the agronomically acceptable salts or N-oxides thereof, and herbicidal compositions containing such compounds as active ingredients.

Abstract: The present invention relates to a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-?-D-ribofuranosyluronamide)-N-(2-{N?-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide and to a process for the preparation of, compositions containing and the uses of such a crystalline form.

Abstract: An electron transport system complex II inhibitor comprising 2-pyridinol derivative represented by the general formula [I] 1

Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.

Abstract: There are described benzoylcyclohexanediones of the formula I, their preparation, and their use as herbicides and plant growth regulators. In this formula (I), C1, C2, C3 are cyclic radicals, X1 is a hetero atom, X2 is a chain of carbon atoms, L is a chain-like element, R1, R2, R3, R4, R5 are various radicals, and Y and Z are monoatomic bridge elements.

Abstract: Compounds of formula (I) and salts thereof as phytopathogenic fungicides wherein A1 is substituted 2-pyridyl; A2 is optionally substituted phenyl; L is —(C═O)—, —SO2— or —(C═S)—; R1 is hydrogen, optionally substituted alkyl or acyl; and R2 is hydrogen or optionally substituted alkyl are useful phytopathogenic fungicides.

Abstract: There is disclosed substituted thiocarboxamides of the general formula (I) useful as herbicides.