Abstract: The present application describes novel amides and derivatives thereof of formula 1

Abstract: Fuel additives comprise a compound having a group represented by the formula >C═=N—  (1). Also disclosed are fuel compositions containing such additives. The additives have a superior detergent effect to conventional gasoline detergents and an excellent detergency of the injection nozzles of a diesel engine and is free from being sludge.

Abstract: This invention provides compounds of Formula (I): wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, CORC; RC is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 and containing one or two independent substituents from the group including H, halogen, CN, N02, amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 a

Abstract: Novel compounds, pharmaceutical compositions and methods are disclosed for producing local anesthesia of long-duration. The compounds of this invention are multibinding compounds that comprise from 2 to 10 ligands covalently attached to a linker or linkers, each ligand being capable of binding to a ligand binding site in a voltage-gated Na+ channel to modulate the biological processes/functions thereof.

Abstract: Disclosed are compounds of the formula: wherein Ar, R1, R2, R3, W, X, Y, and Z are substituents as defined herein, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.

Abstract: Disclosed are compounds of formula wherein Ar represents an aryl or heteroaryl group; and R1, R2, R3, R4 and R5 represent organic or inorganic substituents, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and, thus, are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.

Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.

Abstract: Novel compounds, pharmaceutical compositions and methods are disclosed for producing local anesthesia of long-duration. The compounds of this invention are multibinding compounds that comprise from 2 to 10 ligands covalently attached to a linker or linkers, each ligand being capable of binding to a ligand binding site in a voltage-gated Na+ channel to modulate the biological processes/functions thereof.

Abstract: A ferulic acid derivative represented by the general formula: 1

Abstract: The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is or and where m is 1 or 4-6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R5, R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and A is a substituent of its ring and is selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.

Abstract: The invention relates to tuned multifunctional linker molecules for charge transport through organic-inorganic composite structures. The problem underlying the present invention is to provide multifunctional linker molecules for tuning the conductivity in nanoparticle-linker assemblies which can be used in the formation of electronic networks and circuits and thin films of nanoparticles.

Abstract: This invention is directed to novel local anesthetic compounds, pharmaceutical compositions containing these compounds, methods of use and methods of preparing these compounds.

Abstract: In a compound of the formula I (reactive polymer), L is a, polymer, XY is a reactive radical which is inert toward NCO groups and splits off one or more protective groups Y under acidic, neutral or basic conditions and the radical X bears, after Y has been split off, at least two groups which are reactive toward isocyanates. Also provided are processes for preparing such a polymer and for preparing V a polymer polyol which is obtainable by reacting a polymer of the formula I with an acid or base. A polymer polyol as is obtainable by treatment of a reactive polymer according to the present invention in the neutral, acidic or basic range can be used to produce a polyaddition product or polycondensation product.

Abstract: Amines are prepared by reacting aldehydes or ketones at elevated temperature under elevated pressure with nitrogen compounds selected from the group of ammonia, primary and secondary amines, and with hydrogen in the presence of a catalyst containing copper, wherein the catalytically active mass of the catalyst contains, before the reduction with hydrogen, 20 to 85% by weight of oxygen-containing compounds of zirconium, calculated as ZrO2, 1 to 30% by weight of oxygen-containing compounds of copper, calculated as CuO, 14 to 70% by weight of oxygen-containing compounds of nickel, calculated as NiO, 0 to 5% by weight of oxygen-containing compounds of molybdenum, calculated as MoO3, and 0 to 10% by weight of oxygen-containing compounds of aluminum, calculated as Al2O3.

Abstract: The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV- or FIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.

Abstract: Novel methods, processes and metal complexes attached to a hypoxia-localizing moiety comprising

Abstract: The present invention describes an isolated macrocycle having the formula: where d is an integer from 0 to about 100; A, B, and each D are the same or different and are selected from the group consisting of each R1 is the same or different and is a bivalent alkylene moiety; each R2 is the same or different and is a bivalent alkylene moiety; and each R3 is the same or different and is selected from the group consisting of a hydrogen atom and an alkyl moiety. Methods for producing these macrocycles are also described. The macrocycles of the present invention can be used as arthropod repellents.

Abstract: Disclosed herein are compounds of Formula I and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation.

Abstract: The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.

Abstract: This invention provides novel quinazolinone compounds and pharmaceutically acceptable salts thereof, which are useful as local anesthetics. This invention also provides pharmaceutical compositions containing such compounds; methods for producing local anesthesia in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

Abstract: The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.

Abstract: The invention relates to compounds of the formulae: processes for their preparation, polymers, co-polymers or block co-polymers containing them or their use as monomers or co-monomers in free radical polymerisation and in the manufacture of adhesives, dental composites or optical lenses.

Abstract: The present invention is a fluorine-containing compound having i) a perfluoropolyoxyalkyl or -alkylene chain having an average molecular weight of 800 or more and ii) a cyclic or non-cyclic polyether atomic group. Its use as a low-scattering lubricant or surface modifier (water repellent) brings about an improvement in sliding durability of magnetic recording media.

Abstract: The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.

Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas 1

Abstract: The present invention relates to a novel pyrimidinone compounds and the pharmaceutical acceptable salts thereof having remarkable antagonistic action against angiotensin II receptor, thereby, being useful in treating cardiovascular disease caused by binding angiotensin II to its receptor.

Abstract: A ferulic acid derivative represented by the general formula: 1

Abstract: The invention relates to new compounds of general formula I or the pharmaceutically acceptable salts thereof, wherein X=N—R3 or CH—R4, Y=CH2 or (CH2)2, Z=O or H2; and R1, R2, R3, R4 and Ar have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.

Abstract: Provided are methods of purification of an organic lithium salt comprising the steps of: (a) dissolving an impure organic lithium salt in a solution comprising an organic complexing solvent; (b) crystallizing from said solution a solid solvate complex comprising said lithium salt and said organic complexing solvent; (c) separating said solid solvate complex from said solution; (d) dissociating said solid solvate complex to yield: (i) said lithium salt in a solid form, and, (ii) a volatile composition comprising said organic complexing solvent; and, (e) removing said volatile composition to yield said lithium salt in a solid form of purity greater than the purity of said impure lithium salt. The present invention also pertains to electrolytes for electric current producing cells comprising such purified lithium salts.

Abstract: The invention relates to a triaza-cryptand of the general Formula I wherein a is selected from the group consisting of 0 and 1, b and c independently are selected from the group consisting of 0 and 1, with the proviso that not both of b and c are 0, d is selected from the group consisting of 1, 2 and 3, e and f independently are selected from the group consisting of 0 and 1, with the proviso that not both of e and f are 0, R1 and R2 are either hydrogen or form an alkyl(C1-C4) benzene ring or an alkoxy(C1C4) benzene ring together with C1 and C2, wherein C2 is the para position, R3 and R2 are either hydrogen or form an alkyl(C1-C4) benzene ring or an alkoxy(C1-C4) benzene ring together with C3 and C4, wherein C3 is the para position, R5 and R6 are either hydrogen or form a benzene ring or a naphtalene ring together with C5 and C6, R7 and R8 are either hydrogen or form an alkyl(C1-C4) benzene ring or an alkoxy(C1-C4) benzene ring together with C7 and C8, wherein C8 is the para position,

Abstract: This invention encompasses compounds of the formula wherein Ar represents a mono- , di- or trisubstituted aryl group where at least one position on Ar ortho to the point of attachment to the pyrazole ring is substituted; and R1 represents lower alkyl; R2 is hydrogen or lower alkyl; and R3 and R4 independently represent organic and inorganic substituents, which compounds are highly selective partial agonists or antagonists or human CRF1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.

Abstract: Method for recovering oxygen from a medium containing O.sub.2 using polynitrogenated compounds that have five coordinating functions which are capable of binding a metal atom, particularly a cobalt atom. In the recovery method, oxygen is first absorbed by the metal complex and then desorbed from the complex and recovered in an appropriate vessel.

Abstract: The invention relates to new compounds of general formula I ##STR1## or the pharmaceutically acceptable salts thereof, wherein X=N--R.sup.3 or CH--R.sup.4,Y=CH.sub.2 or (CH.sub.2).sub.2,Z=O or H.sub.2 ;and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Ar have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.

Abstract: A robust chelate complex is provided having the formula: ##STR1## wherein: M is a metal, preferably a transition metal; Z is an anionic donor atom, three of which are nitrogen, and the other is oxygen; L.sub.1 is a labile ligand;Ch.sub.1, Ch.sub.2 and Ch.sub.3 are oxidation resistant chelate groups which are the same or different and which form 5 or 6 membered rings with the metal, and Ch.sub.4 is a chelate group having the structure ##STR2## wherein R.sub.1 and R.sub.2 are the same or different and are preferably selected from the group consisting of hydrogen, halogen, methyl, and CF.sub.3 or when linked, a five or six membered ring cyclo substituent. The complex provides a stable, long-lived oxidation catalyst or catalyst activator.

Abstract: The present invention relates to compounds selected from the group consisting of the compounds of formula (I): ##STR1## X is a halogen atom, A is --CH.sub.2 --, --CH(OH)--, --CH(NH--COCH.sub.3)-- or S, R is H, CO.sub.2 H, CO.sub.2 --B--R.sub.1 or CO--N(R.sub.2)--B--R.sub.1, B is linear, branched or cyclic C.sub.1 -C.sub.10 -alkylene, R.sub.1 is H, CH.sub.2 OH, CH.sub.2 --O--CH.sub.3, CH.sub.2 --NR.sub.3 R.sub.4 or phenyl, R.sub.2 is H or C.sub.1 -C.sub.4 -alkyl, R.sub.3 is H or linear, branched or cyclic C.sub.1 -C.sub.10 -alkyl, R.sub.4 is H or linear or branched C.sub.1 -C.sub.10 -alkyl, it being possible for NR.sub.3 R.sub.4 to be a saturated heterocyclic radical having from 5 to 8 ring members and containing at least one nitrogen atom, and the carbon carrying the substituent R, when Q is saturated, can be of indeterminate (R,S) configuration or of determinate (R) or (S) configuration; and their addition salts.

Abstract: Compounds of formula (I) ##STR1## wherein n, V, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification are matrix metalloproteinase inhibitors.

Abstract: This invention provides novel bis-indolylmaleimide macrocycle derivatives of the formula: and solvates thereof. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.

Abstract: The current invention discloses useful amidino derivative useful as nitric oxide synthase inhibitors.

Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: The invention relates to a compound having the general Formula I ##STR1## in which one of the groups R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 represents an ionophoric moiety and the remaining groups each independently are hydrogen, a lipophilic or hydrophilic group or a reactive group for coupling to a polymer or a biomolecule, or R.sub.2 forms an aromatic ring system together with R.sub.3 and R.sub.5 forms an aromatic ring system together with R.sub.6.The compound of the invention is useful as a luminescence indicator for alkali ions.

Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, x and y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.

Abstract: Derivatives of glutamic and aspartic of formula (I) are described ##STR1## where the compounds are potent receptor antagonists of gastrin at the peripheral level and of cholecystokinin at the level of the central nervous system.

Abstract: The invention relates to a method of determining an alkali ion in a sample, wherein the alkali ion is contacted with a compound having a luminophoric moiety and an ionophoric moiety, which ionophoric moiety reacts with the alkali ion present in the sample, wherein the luminophoric moiety changes its luminescence properties, after which the luminescence is measured and the alkali ion determined utilizing the test reading,which method is characterized in that the compound utilized is a monoaza-crown ether of the general Formula I ##STR1## in which X is the luminophoric moiety, m is the number 0, 1 or 2, and r and s independently mean the numbers 0, 1 or 2.

Abstract: The invention discloses fluorescent chelator compounds that are especially useful to monitor and measure cytosolic concentrations of alkali metal cations such as Na.sup.+, K.sup.+, and Li.sup.+. The new compounds are comprised of: (1) crown ethers (that may or may not have substituent groups attached to the core carbons, but will always contain at least one core nitrogen) that are linked via the core nitrogen(s) to at least one (2) fluorophore that contains an additional heteroaromatic liganding center. In the currently preferred dye, SBFI, the core compound is crown ether 1,7-diaza-4,10,13-trioxacyclopentadecane and the heteroaromatic fluorophores are benzofurans that are linked to isophthalate groups. Selectivities for Na.sup.+ over K.sup.+ of about 20 are observed, resulting in effective dissociation constants for Na.sup.+ of about 20 mM against a background of 120 mM K.sup.+. Increasing ?Na.sup.

Abstract: The present invention is directed to novel halo-substituted bis-indolemaleimide compounds of the formula: ##STR1## The invention further provides a method of preparing the disclosed compounds and the preparation of pharmaceutical formulation for use in inhibiting Protein Kinase C in mammals.

Abstract: The invention concerns an improved process for the preparation of macrocyclic products with 12 or more ring atoms containing one or more polar functional groups on the ring and/or one or more heteroatoms within the ring by ring closing metathesis (RCM) of suitably substituted diene precursors even if the substrates are devoid of any kind of conformational preorganization. Metal carbene complexes of Ru, Mo, W, Re, Os, which are tolerant towards the respective functional group and can either be isolated or prepared in situ are used as catalysts or catalyst precursors. Preferred catalysts or catalyst precursors are ruthenium complexes of the general type XX.sub.1 LL.sub.1 Ru.dbd.CRR.sub.1, wherein X, X.sub.1 =halogen, L, L.sub.1 =trialkylphosphine, R, R1=H, Ph, CH.dbd.CPh.sub.2 denote the most preferred embodiment. The process can be applied to the synthesis of olfactory compounds, perfumary ingredients, pheromones, crown ethers, antibiotics and pharmaceuticals for human and veterinary medicine.

Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.

Abstract: The current invention discloses useful pharmaceutical compositions containing azepine derivatives useful as nitric oxide synthase inhibitors.

Abstract: A method for imaging mammalian tissue utilizing a non-ionic complex of a paramagnetic ion of lanthanide element and a macrocyclic chelating agent.

Abstract: Therapeutic compounds have the formula:(X)j-(core moiety),j being an integer from one to three, the core moiety comprising a core moiety, the core moiety being a heterocycle having one ring or two-fused rings, each ring having five or six ring atoms, A being a carbon atom of the core moiety and attached to a terminal carbon atom of (CH.sub.2).sub.m, and X has a structure and X being a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkyl or alkenyl of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.