Abstract: The invention discloses novel compounds of the pyridinium series useful for the management of diabetes and aging-related vascular complications, including kidney disease, nerve damage, atherosclerosis, retinopathy, dermatological disorders and discoloration of teeth, by breaking preformed AGE, of the general formula I, or pharmaceutically acceptable salts thereof, wherein, R1, R2, R3, X and m are as defined in the specification.

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: This invention relates to compounds which are IP receptor antagonists and which are represented by Formula (I): wherein G2 is a heteroaryl group containing one or two nitrogen atoms substituted with a carboxylic acid group, said heteroaryl ring containing one or two nitrogen atoms, and G1 is as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: Compounds of the formula wherein R1, R2, R3, R4, X and n are defined in the specification, are useful for the treatment of anxiety, depression and related CNS disorders, and other related conditions such as the treatment of alcohol and drug withdrawal, sexual dysfunction and Alzheimer's disease.

Abstract: Compounds of formula (I) may be useful in treating diseases prevented by or ameliorated with potassium channel openers.

Abstract: Compounds having a selective N-type calcium channel antagonistic activity are provided.

Abstract: Dihydropyridine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type calcium channel. They are used as remedies for various diseases relating to the N-type calcium channel such as encephalopathies caused by the ischemia in the acute phase after the onset of cerebral infarction, cerebral hemorrhage or the like, Alzheimer's disease, etc.

Abstract: Compounds antagonistic of the pain enhancing effects of prostaglandins are disclosed. The compounds comprise an optionally-substituted A ring with a —CH(R3)N(R2)B—R1 and —OD groups positioned in a 1,2 relationship to one another on ring carbon atoms. The 3-position ring-atom is not substituted. B is an optionally-substituted pyridyl ring and the group R1 is positioned on B in a 1,3 or 1,4 relationship with the —CH(R3)N(R2)B- linking group. R1, R2 and R3 and D can be a number of different organic or halogen moieties. N-oxides of —NR2 and S-oxides of sulphur containing rings are disclosed as are processes for the preparation of the compounds, intermediates in their preparation, pharmaceutical compositions containing them, and their use as therapeutic agents.

Abstract: The present invention relates to novel tocotrienols and tocotrienol-like compounds displaying biological activity. The tocotrienols and tocotrienol-like compounds of this invention may be conveniently obtained from biological sources or by chemical synthesis and may be used in pharmaceutical compositions, foodstuffs and dietary supplements. This invention also relates to the use of tocotrienols, tocotrienol-like compounds, and mixtures thereof, as hypocholesterolemic, antithrombotic, antioxidizing, antiatherogenic, antiinflammatory and immunoregulatory agents, or as agents useful to decrease lipoprotein (a) concentration in the blood or to increase feed conversion efficiency.

Abstract: Optically active 1,4-dihydropyridine derivatives represented by general formula (I) and anion salts thereof and a production method therefor: ##STR1## (wherein R.sup.1 represents a C.sub.1-6 alkyl group, R.sup.2 represents a nitrogen-containing heterocyclic group forming a quaternary ammonium which may be substituted, and n is an integer of 1, 2 or 3). The optically active 1,4-dihydropyridine derivatives represented by general formula (I) have vasodilating activity and hypotensive activity and are excellent in water solubility so that they are useful as a drug for circulatory system such as a hypotensor or vasodilator.

Abstract: 4-Phenyl-3-substituted 1,4-dihydropyridine esters are prepared by reaction of benzaldehydes with ketoesters and enamines, if appropriate with isolation of the ylidene intermediate products, or by esterification of corresponding dihydropyridinecarboxylic acids with alcohols.The new 4-phenyl-3-substituted 1,4-dihydropyridine esters can be employed as active compounds in medicaments for the treatment of the central nervous system, in particular as cerebral therapeutics.

Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: An (N-(pyridinylmethyl)-heterocyclic)ylideneamine compound of the formula ##STR1## wherein R.sup.3, A, and B are as described below, and its pharmaceutically acceptable salts and prodrugs. Compounds of the formula I and their pharmaceutically acceptable salts and prodrugs are useful in the treatment of addictive disorders, such as the use of tobacco or other nicotine containing products, neurological and mental disorders such as senile dementia of the Alzheimer's type, Parkinson's disease, attentional hyperactivity disorder, anxiety, obesity, Tourette's Syndrome and ulcerative colitis.

Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of cyanoguanidine derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I). ##STR1## As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Abstract: Corticotropin-releasing factor (CRF) antagonists having formulae (I), (II) or (III) wherein the dashed lines, A, B, Y, Z, G, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.16 and R.sub.17 are as defined in the description, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment of CNS and stress-related disorders.

Abstract: New seco-D steroid derivatives, processes for their preparation and pharmaceutical compositions are provided, which are active on the cardiovascular system.

Abstract: A 1,4-dihydropyridine compound having the formula (I): ##STR1## wherein, R.sup.1 indicates --COO--A--(3-pyridyl), A indicates a C.sub.3 -C.sub.6 straight chain alkylene group in which one piperazine may be interposed; R.sup.2 indicates a C.sub.2 -C.sub.10 alkyl group, alkenyl group or alkynyl group; a lower alkyl group or lower alkenyl group having a substituent; or a cycloalkyl group which may have a substituent; R.sup.3 indicates the same group as R.sup.1 or --COO--R.sup.4 ; and R.sup.4 indicates a lower alkyl group which may have a substituent or its pharmacologically acceptable salt and an anti-allergenic drug, antiphlogistic, drug for overcoming resistance to anti-cancer drugs, or drug for reinforcing the effect of anti-cancer drugs containing the same as effective ingredients.

Abstract: Novel compounds of Formula ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the above formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.

Abstract: A compound in metal-free or metal complex form of formula (1) to (3) in which R is hydrogen or C.sub.1-30 alkyl; X is hydrogen, halogen (preferably Cl or Br) or C.sub.1-30 alkyl.

Abstract: A polymer containing a recurring unit of a conjugated N-fluoropyridinium salt and an active material for a positive electrode, an electrolyte, a battery material for the positive electrode and a battery which use such a polymer. That polymer provides a battery material and a primary battery or a secondary battery which have high electromotive force, high energy density, high environmental acceptability, a low internal resistance in charging and discharging and strong recoverability of the electromotive force, and can be useful as a fluorinating agent.

Abstract: A method for producing chromium picolinate complex by the reaction of picolinic acid with chromium, wherein the reaction is carried out under the conditions of temperature of 70.degree. C. and pH of 3.5 to 4.2.

Abstract: The present invention relates to the field of immunoassays for metal ions. The invention presents: metal ion-ligand coordination complexes ("MLC"), novel ligands, antibodies specific for MLC, immunoassays utiliizing the foregoing, and methods for selecting said antibodies.

Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of piperidine and tetrahydropyridine derivatives of 4-phenyl-1,4-dihydropyridines of Formula I. ##STR1## As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Abstract: Leukotriene-B.sub.4 analogs of formula I ##STR1## in which R.sup.1 means radical COOR.sup.2 with R.sup.2 meaning a hydrogen atom or a (C.sub.1 -C.sub.4)-alkyl group or R.sup.1 means radical CH.sub.2 OH,B means an alkylene group with 1-3 C atoms in the chain, a radical ##STR2## or a radical ##STR3## with R.sup.3 meaning a hydrogen atom, a carboxy or methoxycarbonyl group, A means groups ##STR4## --NH--CO--, --CO--NH--, --OCH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --COCH.sub.2 -- or --CHOH--CH.sub.2 --,X means N or CH,D means groups or ##STR5## and . . . . . means a single or double bond, as well as optionally their salts with physiologically harmless bases, process for their production and their pharmaceutical use.

Abstract: The invention relates to the compounds of formula I ##STR1## wherein R is lower alkyl or hydrogen; R.sub.1 is hydrogen, lower alkyl or aryl-lower alkyl; R.sub.2 is hydrogen, nitro, cyano trifluoromethyl, halo, lower alkoxy, lower alkyl, lower alkoxycarbonyl, aminocarbonyl or mono- or di-lower alkylaminocarbonyl, amino or mono- or di-lower alkylamino; and pharmaceutically acceptable salts thereof when R.sub.1 is hydrogen; which are useful as endothelin antagonists.

Abstract: Imidazolyl and pyridyl derivatives of phenyl substituted 1,4-dihydropyridines of formula (I) ##STR1## wherein Het is ##STR2## A represents a direct linkage, --CH.sub.2 --, CH.sub.2 --CH.sub.2 -- or, when Het is ##STR3## A may also represent --CH.dbd.CH--; R is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy; each of R.sub.3 and R.sub.4 is a C.sub.1 -C.sub.3 alkyl group; one of R.sub.1 and R.sub.2 is a group --OR' wherein R' is a C.sub.1 -C.sub.6 alkyl either unsubstituted or omega substituted by C.sub.1 -C.sub.3 alkoxy or cyano, and the other is, independently,a) a group --OR";b) a group ##STR4## or c) a group --OR.sup.IV wherein R.sup.IV is hydrogen or a substituent selected from:(i) --(CH.sub.2).sub.m --CH.dbd.CH--Ph, ##STR5## are useful as Thromboxane A.sub.2 (TxA.sub.2) Synthase inhibitors and as calcium antagonists.

Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.

Abstract: The invention relates to nicotinic acid hydrazone derivatives of formula I: ##STR1## in which the various symbols are as defined in the description, and their use as herbicides or as intermediates in the synthesis of herbicides.

Abstract: The compounds are 2,4-disubstituted 3-ethoxycarbonyl 5-methoxycarbonyl 6-methyl 1,4-dihydropyridines in their dextrorotatory form, useful to potentiate the activity of cytotoxic agents and to increase the sensitivity of tumor cells to antitumor agents.A compound disclosed is d-2-{[2-(2-(N-p-nitrobenzylamino)ethoxy)ethoxy]methyl}-4-(2,3-dichlorophen yl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine.

Abstract: Addition-curable platinum group metal catalyzed silicone compositions are provided which utilize an N-heterocyclic adhesion promoter, such as bis(trimethoxysilyltrimethylene) 2,6 pyridine dicarboxylate. Cohesive bonding is effected on both plastic and metal substrates at temperatures of less than 100.degree. C. and in less than 1 hour.

Abstract: The invention relates to substituted pyridine-2,4-dicarboxylic acid derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings given. The invention also relates to a process for the preparation of the abovementioned compounds and to their use as medicaments, in particular as fibrosuppressants and immunosuppressants.

Abstract: Use of optically active carboxylic esters of oxygen-containing heterocycles as doping substances in liquid crystal mixtures and liquid crystal mixtures containing them.Optically active 1,3-dioxolane-4-carboxylic esters and oxirane-2-carboxylic esters of the general formula (I)R(--A.sup.1).sub.j (--M.sup.1).sub.k (--A.sup.2).sub.l (--M.sup.2).sub.m (--A.sup.3).sub.n --X--Acin whichR.sup.1 is, for example, (C.sub.1 -C.sub.16)-alkyl or (C.sub.1 -C.sub.16)-alkoxy,A.sup.1, A.sup.2, A.sup.3 are, for example, phenyl or pyrimidine-2, 5-diyl,M.sup.1, M.sup.2 are, for example, CO--O, CH.sub.2 --CH.sub.2,j, l are 0, 1, 2,k, m are 0, 1,n is 0, 1, 2,X is O, S andAc is ##STR1## in which R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 for example, H or methyl, are particularly suitable doping substances for liquid crystalline mixtures, since they induce a high spontaneous polarization and effect a substantial decrease in the melting point.

Abstract: Thioformamide derivatives of formula (I): ##STR1## wherein R represents alkyl; A represents optionally substituted pyrid-4-yl; Y represents ethylene or methylene or a direct bond and X represents an optionally substituted phenyl, pyridyl, furyl or thienyl group or optionally substituted alkyl, alkenyl or cycloalkyl, and salts thereof possessing useful pharmacological properties.

Abstract: A solvent soluble heterocyclic o-hydroxy thione carrying a lipophilic group and the process for the selective extraction of gallium, and certain other related metals, especially from solutions containing excess aluminium.

Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.

Abstract: The present invention relates to a novel and efficient process for the preparation of 8-hydroxybicyclo[7.3.1]tridec-4-ene-2,6-diyne ring system which is part of the aglycone of esperemicin and to novel cytotoxic antitumor agents having said bicyclic ring system. The present invention also provides a method for treating mammalian malignant tumors by administering to an animal in need of such treatment an antitumor effective amount of a compound of the present invention.

Abstract: 1,4-dihydropyridine derivatives of Formula 1 or pharmaceutically acceptable salts thereof: ##STR1## wherein the substituents are disclosed herein and which are useful against tumor cells which have acquired resistance to one or more drugs used as chemotherapeutic agents.

Abstract: Dihydrocaffeic acid derivatives are here disclosed which are applicable as medicines having excellent absorbency in the case of oral administration and good concentration retention in blood.The disclosed compounds have the function to induce the production and secretion of a nerve growth factor (NGF) in the brain tissue, and therefore they are effective as medicines for the progression inhibition and therapy of regressive disorders of the central nervous system.

Abstract: A pyridine compound of the formula ##STR1## wherein X is a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxyl group having 1 to 4 carbon atoms, a haloalkyl group having 1 to 4 carbon atoms or a haloalkoxyl group having 1 to 4 carbon atoms, n is 1 to 5, and when n is 2 or more, Xs may be identical to or different from each other, A is an alkyl residue or alkene residue in which a portion connecting the aryl group with the 4-position of the pyridyl group has 3 to 8 carbon atoms, or an alkapolyene residue in which said portion has 4 to 8 carbon atoms and 2 to 4 double bonds; the alkyl residue, alkene residue, and alkapolyene residue may have an alkyl side chain having 1 to 4 carbon atoms, an alkylidene side chain having 1 to 4 carbon atoms or 1 to 16 halogen atoms, and when there are 2 or more side chains, the side chains may be identical to or different from each other, and R.sup.1 and R.sup.

Abstract: 2,4- and 2,5-substituted pyridine-N-oxides are provided which are effective as fibrosuppressives and immunosuppressives. Said compounds are also suitable for the treatment of disorders of the metabolism of collagen and collagen-like substances or the biosynthesis of Clq.

Abstract: Compounds of the following formula (I): ##STR1## where R.sup.1 and R.sup.2 are alkyl or cycloalkyl, which may be substituted, R.sup.4 is aryl such as phenyl which may be substituted, L is a direct bond or an oxygen containing linking group, R is a hydrogen, alkyloxy, alkyl, halogen or haloalkyl and Het is a pyridinyl or pyridazinyl group. The compounds can be used antihypertensives or myocardial relaxants. Also part of the invention are pharmaceutical compositions, intermediates and methods of synthesis.

Abstract: An imidazolidine derivative having the formula (I) or its salt: ##STR1## wherein X is an alkyl group which may be substituted, an alkenyl group which may be substituted, an alkynyl group which may be substituted, ##STR2## (in which each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently a hydrogen atom or an alkyl group, R.sup.5 is an alkyl group which may be substituted with a halogen atom, a cycloalkyl group which may be substituted or a phenyl group which may be substituted, W is an oxygen atom or a sulfur atom, and each of k, l, m and n is independently 0 or 1, provided that (a) case where all of k, l and m are 0 at the same time and (b) case where m and n are 0 at the same time and R.sup.5 is an alkyl group which may be substituted with a halogen atom, are excluded), or ##STR3## group (in which each of R.sup.6 and R.sup.7 is independently a hydrogen atom or an alkyl group, each of R.sup.8 and R.sup.9 is independently an alkyl gorup, R.sup.

Abstract: A class of fluorescent rare earth chelates and the ligands upon which they are based whose molecular structure incorporates a plurality of substituted arylpyridine diacid units attached to a central template structure is disclosed. These ligands function as efficient energy transfer groups in fluorescent tagging reagents and tracers.

Abstract: Thioformamide derivatives of the formula (I) ##STR1## wherein R represents an alkyl group; A represents either:(1) a phenyl group which is optionally substituted; or(2) heteroaromatic group (e.g. pyrid-3-yl, quinolin-3-yl);Y represents:an ethylene or methylene group or a direct bond; and B represents either:a) a phenyl, pyridyl, furyl or thienyl group, each of which may be optionally substituted, orb) a straight- or branched-chain alkyl, alkenyl, or cycloalkyl group, each of which may be optionally substituted.These compounds may be formulated into pharmaceutical preparations and have utility in the treatment of disorders associated with smooth muscle contraction.

Abstract: A class of fluorescent rare earth chelates and the ligands upon which they are based whose molecular structure incorporates a plurality of substituted arylpyridine diacid units attached to a central template structure is disclosed. These ligands function as efficient energy transfer groups in fluorescent tagging reagents and tracers.

Abstract: .alpha.-Arylacrylates substituted by a heterocyclic radical and of the general formula I ##STR1## where R.sup.1 is alkoxy or alkylthio, R.sup.2 is alkyl, Het is pyridyl, pyridone, quinolyl, pyrimidinyl, pyrimidinone, the heterocyclic ring system being unsubstituted or substituted, A is carbonyloxy, oxygen or sulfur, and n is 0 or 1, and their plant-tolerated acid addition salts and metal complexes, and the N-oxides of the heterocyclic compounds, and fungicides containing these compounds.

Abstract: Therapeutically useful thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Het represents pyrid-3-yl, isoquinolin-4-yl, tetrahydroquinolin-3-yl, quinolin-3-yl, pyridazin-4-yl, pyrimid-5-yl, thiazol-5-yl, thieno[2,3-b]-pyridin-5-yl, pyrazin-2-yl, indol-3-yl and thieno[3,2-b]-pyridin-6-yl, Y represents ethylene, methylene or a valency bond, and X represents carbonyl, hydroxymethylene, >C.dbd.NOR.sup.1, >C.dbd.NN(R.sup.1).sub.2 or >C.dbd.NN(R.sup.1)CON(R.sup.1).sub.2 in which R.sup.1 represents hydrogen or optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl, or two R.sup.1 substituents on the same nitrogen atom may together form an optionally substituted alkylene radical chain and salts thereof, processes for their preparation and compositions containing them are described.

Abstract: The invention relates to substituted pyridine-2,4-dicarboxylic acid derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings given. The invention also relates to a process for the preparation of the abovementioned compounds and to their use as medicaments, in particular as fibrosuppressants and immunosuppressants.

Abstract: Dihydropyridine derivatives and salts thereof represented by the general formula, ##STR1## which possess excellent calcium antagonist effect, hypotensive effect, platelets aggregation inhibitory effect, phosphodiesterase inhibitory effect, calmodulin inhibitory effect and peroxidized lipid lowering effect, and thus dihydropyridine derivatives and salts thereof are useful as a coronary blood flow improving agent such as coronary vasodilator, hypotensive agent, prophylaxis and treating agents for thrombosis, phosphodiesterase inhibitory agent, peroxidized lipid metabolism lowering agent, anti-inflammatory agent and others.

Abstract: A dihydropyridine.revreaction. pyridinium salt type of redox, or chemical, delivery system for the site-specific and/or site-enhanced delivery of a radionuclide to the brain is provided. A chelating agent capable of chelating with a radionuclide and having a primary, secondary or tertiary amino function can be converted to the corresponding analogue in which said function is replaced with a dihydropyridine.revreaction. pyridinium salt redox system and then complexed with a radionuclide to provide a new radiopharmaceutical that, in its lipoidal dihydropyridine form, penetrates the blood-brain barrier ("BBB") and allows increased levels of radionuclide concentration in the brain, particularly since oxidation of the dihydropyridine moiety in vivo to the ionic pyridinium salt retards elimination from the brain while elimination from the general circulation is accelerated. This radionuclide delivery system is well suited for use in scintigraphy and similar radiographic techniques.