Abstract: p38 and JNK mitogen activated protein (MAP) kinase al losteric inhibitors are useful for treatment and/or prophylaxis of degenerative diseases of the nervous system. Compounds are used in a method for treatment and/or prophylaxis of the diseases and for use in therapy in general. The compounds bind to the region composed of amino acids at positions 170-199 of Mitogen-activated protein kinase 14 (Uniprot accession nr Q16539 or SEQ ID No 1) and/or Mitogen-activated protein kinase 11 (Uniprot accession nr Q15759 or SEQ ID No 2), SEQ ID NO.1 and SEQ ID NO.2 being the amino acid sequences of MAPK14 (?38?) and MAPK11 (?38?), respectively. The specific region composed of amino acids at positions 170-199 is herein disclosed as SEQ ID HO.4 for Mitogen-activated protein kinase 14 and SEQ ID NO.5 for Mitogen-activated protein kinase 11 and are believed to be new inhibitory binding sites.

Abstract: A protective film of polarizer comprising an organic acid that has a solubility in water at 25° C. of at most 0.1% by mass and has an acid dissociation constant in a mixed solvent of tetrahydrofuran/water=6/4 by volume at 25° C. of from 2 to 7 can improve polarizer durability.

Abstract: Methods of providing neuroprotection are disclosed comprising administering a non-sedative barbiturate compound in an amount sufficient to achieve neuroprotection in a mammalian subject. Preferred compounds are in the family of diphenylbarbituric acid and analogs. Preferred doses for a neuroprotective effect exceed the dosage of a corresponding sedative barbiturate without sedative side-effects such as anesthesia and death.

Abstract: Phenobarbital derivatives synthesized out of the alkyl chain at the 5-position, particularly with hydrophilic properties, and carrying an active ester at the end, allow formation of aminodextran conjugates that give curves in the desired range of the assay in the ONLINE TDM microparticle assay format when matched against the Roche FPIA antibody specific for phenobarbital (“an antibody specific for phenobarbital”).

Abstract: An exchange membrane containing modified maleimide oligomers comprising sulfonated poly(aryl ether ketone) (S-PAEK) and modified maleimide oligomers. The exchange membrane uses the modified maleimide oligomers having a hyper-branched architecture as matrix, and introduces them into S-PAEK to constitute semi-interpenetration network (semi-IPN), so as to intensify water holding capacity, chemical resistance, the electrochemical stability and thermal resistance of the ionic/proton exchange membrane. The exchange membrane can be used to fabricate the membrane electrode assemblies, fuel cells, and be applied them to the fields of seawater desalination, heavy water and sewage treatment, and biomass-energy resources.

Abstract: The present invention relates to a composition and a method of delivering a barbituric acid derivative to the central nervous system of a mammal in need of treatment for neurological conditions. In particular, the present invention relates to a method of administering an oral dosage form of a sodium salt of 5,5-diphenyl barbituric acid to enhance the bioavailability of 5,5-diphenyl barbituric acid and brain delivery of same.

Abstract: Provided herein are compounds, compositions and methods for treating disorders mediated by abnormal cellular proliferation and processes for identifying such compounds.

Abstract: A method of treating movement disorders comprises administering to a human or animal subject in need of treatment a therapeutically effective amount of at least one compound according to the following formula: wherein R3 and R4 are each independently selected from the group consisting of lower alkyl, phenyl and lower alkyl substituted phenyl, and R1 and R2 are each independently either a hydrogen atom or a radical of the formula wherein R5 and R6 are each independently selected from the group consisting of H, lower alkyl, phenyl and lower alkyl substituted phenyl, its pharmaceutically acceptable salts, prodrugs, and metabolites thereof.

Abstract: Methods of providing neuroprotection are disclosed comprising administering a non-sedative barbiturate compound in an amount sufficient to achieve neuroprotection in a mammalian subject. Preferred compounds are in the family of diphenylbarbituric acid and analogs. Preferred doses for a neuroprotective effect exceed the dosage of a corresponding sedative barbiturate without sedative side-effects such as anesthesia and death.

Abstract: Compounds of formulae: where Ar1, Ar2, R3, R4, and m are disclosed herein, or a pharmaceutically acceptable salt thereof (a “Nitro(cyano)vinylpiperazine Compound”); compositions comprising an effective amount of a Nitro(cyano)vinylpiperazine Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Nitro(cyano)vinylpiperazine Compound are disclosed.

Abstract: Methods of providing neuroprotection are disclosed comprising administering a non-sedative barbiturate compound in an amount sufficient to achieve neuroprotection in a mammalian subject. Preferred compounds are in the family of diphenylbarbituric acid and analogs. Preferred doses for a neuroprotective effect exceed the dosage of a corresponding sedative barbiturate without sedative side-effects such as anesthesia and death.

Abstract: The present invention relates to a composition and a method of delivering a barbituric acid derivative to the central nervous system of a mammal in need of treatment for neurological conditions. In particular, the present invention relates to a method of administering an oral dosage form of a sodium salt of 5,5-diphenyl barbituric acid to enhance the bioavailability of 5,5-diphenyl barbituric acid and brain delivery of same.

Abstract: N-substituted derivatives of 5-oximinobarbituric add of the general formula where X is sulfur; R1 is selected from the group consisting of saturated or unsaturated alkyl, cycloalkyl, aryl and arylalkyl; and R2 is selected from the group consisting of hydrogen, saturated or unsaturated alkyl, cycloalkyl, aryl and arylalkyl possessing a biological activity.

Abstract: A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I: with an alkylating agent of structure III: in the presence of a basic catalyst in aprotic reaction medium. The ureide may be a 5,5-disubstituted barbituric acid, or it may be phenytoin, glutethimide, and ethosuximide. The alkylating agent is an ester of a sulfonic acid. The base may be a hydride or amine. A preferred process comprises N-alkoxyalkylating 5,5-diphenyl-barbituric acid with methoxymethyl methanesulfonate in the presence of di-isopropyl ethyl amine and isolating the resultant N,N′-bismethoxymethyl-5,5-diphenyl-barbituric acid. The invention also contemplates the novel compounds N-methoxymethyl-5,5-diphenylbrbituric acid, N-methoxymethyl ethosuximide, and N-methoxymethyl glutethimide, and a method comprising administering them to a patient.

Abstract: Fungicidal compounds of the formula (I): and stereoisomers thereof, wherein R1 is optionally substituted aryl or optionally substituted heteroaryl; Y is oxygen, sulphur or NR4; R2, R3 and R4, which may be the same or different, are hydrogen, C1-4 alkyl or C2-4 alkenyl; X is halogen, C1-4 alkyl, C2-4 alkenyl, C1-4 alkoxy, nitro or cyano, and n is 0 or an integer of 1 to 4; provided that when Y is oxygen, n is 0 and R1 is unsubstituted phenyl at least one of R2 and R3 is other than hydrogen or methyl.

Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.

Abstract: A compound of formula I wherein R1 is hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryloxy or alkylalkoxy, and R2 is aryloxy, or a pharmaceutically acceptable salt of an acidic compound of formula I, or a prodrug thereof. The compounds of formula I and their aforementioned salts and prodrugs can be used in the treatment or control of cancer associated with overexpresison of gelatinase-A and/or gelatinase-B, particularly skin cancer, breast cancer, prostate cancer, colon cancer, lung cancer, and gastric cancer. The compounds of the invention are also useful for other diseases associated with unregulated degradation of extracellular matrix, including rheumatoid arthritis, osteoarthritis, multiple sclerosis, corneal ulceration, periodontal disease and the like.

Abstract: Cyclic urea derivatives of the formula I ##STR1## in which X, X', Y, Y' and Z can have various meanings, are prepared by a) reacting a urea derivative of the formula II ##STR2## with a diketone of the formula III ##STR3## and b) hydrogenating the product from step a) in the presence of a metal-containing catalyst.

Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein R.sup.1 is optionally substituted aryl or optionally substituted heteroaryl; Y is oxygen, sulphur or NR.sup.4 ; R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, are hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl; X is halogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.1-4 alkoxy, nitro or cyano; and n is 0 or an integer of 1 to 4; provided that when Y is oxygen, n is 0 and R.sup.1 is unsubstituted phenyl at least one of R.sup.2 and R.sup.3 is other than hydrogen or methyl.

Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.

Abstract: The invention relates to optically active compounds represented by the general formula ##STR1## wherein R.sub.1, R.sub.2, Q.sub.1, Q.sub.2, Q.sub.3, ##STR2## and M are defined as in the specification, methods and intermediates for their preparation, liquid crystal compositions comprising at least one optically active compound of formula I and their use in electrooptical display, switching and modulation devices.

Abstract: A compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, halogen, haloalkyl, alkoxy, alkenoxy, alkoxyalkyl, haloalkoxy, alkylthio, cyano, nitro, amino, NR.sup.4 R.sup.5, hydroxy, acylamino, --CO.sub.2 R.sup.3, --O(CH.sub.2).sub.m CO.sub.2 R.sup.3, phenyl, phenoxy, benzyl or benzyloxy, the phenyl group or phenyl moiety of the benzyl group being optionally substituted in the ring; or R.sup.1 and R.sup.2 when taken together form a 5- or 6-membered ring; m is 1 or 2; R.sup.3 and R.sup.5 are hydrogen or C.sub.1-4 alkyl; R.sup.4 is C.sub.1-4 alkyl; n is 0 or 1; X is oxygen or sulphur; Y is hydrogen when n is 0; or Y is oxygen or sulphur when n is 1; are useful as nematicides.

Abstract: The invention relates to optically active compounds represented by the general formula ##STR1## wherein R.sub.1, R.sub.2, Q.sub.1, Q.sub.2, Q.sub.3, ##STR2## and M are defined as in the specification, methods and intermediates for their preparation, liquid crystal compositions comprising at least one optically active compound of formula I and their use in electrooptical display, switching and modulation devices.

Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, halogen, haloalkyl, alkoxy, alkenoxy, alkoxyalkyl, haloalkoxy, alkylthio, cyano, nitro, amino, NR.sup.5 R.sup.6, hydroxy, acylamino, --CO.sub.2 R.sup.4, --O(CH.sub.2).sub.m CO.sub.2 R.sup.4, phenyl, phenoxy, benzyl or benzyloxy, the phenyl group or phenyl moiety of the benzyl group being optionally substituted in the ring; or R.sup.2 and R.sup.3 when taken together form a 5 - or 6-membered ring; m is 1 or 2; R.sup.4 and R.sup.6 are hydrogen or C.sub.1-4 alkyl; R.sup.5 is C.sub.1-4 alkyl; n is 0, 1 or 2; provided that when n is 0, R.sup.1, R.sup.2 and R.sup.3 are not all hydrogen, or when n is 0 and R.sup.2 is hydrogen, R.sup.1 and R.sup.3 are not both methyl, or when n is 0 and R.sup.2 and R.sup.3 are both hydrogen, R.sup.1 is not methyl; are useful as nematicides.

Abstract: The present invention relates to unsaturated carboxylic acid amide derivatives of the formula ##STR1## wherein ring A stands for an optionally substituted aromatic ring; R.sup.1 stands for a hydrogen atom or an optionally substituted hydrocarbon residue or forms an optionally substituted carbocyclic ring with the adjacent group --CH.dbd.C-- together with two carbon atoms constituting the ring A; R.sup.2 stands for a hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group; R.sup.3 stands for an optionally substituted hydrocarbon residue; and n denotes an integer ranging from 2 to 6, and salts thereof, as well as the production thereof.The compounds of the present invention act on the central nervous system of mammals and has a strong anti-cholinesterase activity, which can be used for the prophylaxis and therapy of, for example, senile dementia, Alzheimer's diseases, Huntington's chorea, et., and are useful as medicines.

Abstract: 6-substitutted acyclopyrimidine nucleoside derivatives represented by the following general formula I: ##STR1## wherein R.sup.1 represents a hydrogen or halogen atom or a group of alkyl, alkenyl, alkynyl, alkylcarbonyl, arylcarbonyl, arylcarbonylalkyl, arylthio or aralkyl; R.sup.2 represents a group of arylthio, alkylthio, cycloalkylthio, aryl sulfoxide, alkyl sulfoxide, cycloalkyl sulfoxide, alkenyl, alkynyl, aralkyl, arylcarbonyl, arylcarbonylalkyl or aryloxy; R.sup.3 represents a hydroxyalkyl group of which alkyl portion may contain an oxygen atom; X represents an oxygen or sulfur atom or amino group; Y represents an oxygen or sulfur atom; and A represents .dbd.N-- or --NH-- or pharmaceutically acceptable salts thereof, processes for their preparation and antiviral agents containing them as active ingredients.

Abstract: The present invention provides methods and compositions for assaying biological samples, such as human serum, for barbiturates. In one aspect, analogs of barbiturates derivatized with fluorescein and analogs of barbiturates derivatized with immunogenic polypeptides are provided. The fluorescent analogs are employed as tracers in a competitive homogeneous immunoassay, i.e., a fluorescence polarization immunoassay, for detecting barbiturates. The immunogenic analogs are employed to make anti-barbiturate antiserum of the invention for use in the immunoassay method. Intermediates for preparing the fluorescent and immunogenic analogs are also provided. Further provided are test kits, comprising a fluorescent tracer and an antiserum according to the invention, for analyzing biological samples by fluorescence polarization immunoassay for the presence of a barbiturate.

Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein R.sup.1 is optionally substituted aryl or optionally substituted heteroaryl; Y is oxygen, sulphur or NR.sup.4 ; R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, are hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl; X is halogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.1-4 alkoxy, nitro or cyano; and n is 0 or an integer of 1 to 4; provided that when Y is oxygen, n is O and R.sup.1 is unsubstituted phenyl at least one of R.sup.2 and R.sup.3 is other than hydrogen or methyl.

Abstract: The invention relates to substituted phenylbarbituric acids of the formula ##STR1## wherein R.sup.1 and R.sup.3, independently, are lower-alkoxy or lower-alkylthio; R.sup.2 is lower-alkoxy, hydroxy or amino; and R.sup.4 is hydrogen; or R.sup.1 and R.sup.2 are lower-alkoxy, R.sup.3 is hydrogen and R.sup.4 is lower-alkyl,which are prepared from correspondingly substituted benzene derivatives and alloxan. The compounds of formula I can be converted into substituted benzaldehydes which in turn are known intermediates in the preparation of pharmaceutically valuable benzylpyrimidines.

Abstract: There are disclosed novel oxopyrimidine derivatives of the general formula ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and are each hydrogen or lower alkyl optionally substituted by lower alkoxy, and R.sub.3 and R.sub.4 may be the same or different and are each phenyl optionally substituted by lower alkyl or halogen, provided that when R.sub.1 and R.sub.2 are both hydrogen, R.sub.3 and R.sub.4 are each substituted phenyl. Pharmaceutical compositions containing these compounds and their use as anticonvulsant, antianxiety and muscle relaxant agents are described.

Abstract: A process is herein described for catalytically reducing nitroaromatic compounds by displacement of hydrogen from carbon monoxide and water or from synthesis gas to nitroaromatic compounds, the catalytic reduction being catalyzed by complexes of rhodium, iridium, ruthenium and osmium; said process is characterized in that the CO+H.sub.2 O system or the (CO+H.sub.2)+H.sub.2 O system is caused to react with a nitroaromatic compound of formula:Ar--(NO.sub.2).sub.x (I)wherein Ar is an aryl or hetero-aryl group, also substituted by inert groups; x is an integer from 1 to 3, in the presence of a complex catalyst of formula:[MChel(L).sub.2 ].sup.+ X.sup.- (II)or of a catalyst composed by carbonyl compounds and chelants of formula:Mz(CO).sub.y +nChel (III)wherein M=Rh, Ir, Ru, Os; "Chel" is a bidentate or tridentate aromatic nitrogen chelating compound; "L" is a molecule of carbon monoxide or of an olefin or half a molecule of a diolefin; X.sup.- is an anion selected from Cl.sup.-, Br.sup.-, I.sup.-, PF.sub.6.sup.

Abstract: A process for the preparation of certain 5-substituted dialuric acids, compounds having utility as intermediates for the synthesis of certan hypoglycemic 5-substituted oxazolidine-2,4-diones.

Abstract: Hypoglycemic 5-phenyl and 5-naphthyl oxazolidine-2,4-diones and the pharmaceutically-acceptable salts thereof; certain 3-acylated derivatives thereof; a method of treating hyperglycemic animals therewith; and intermediates useful in the preparation of said compounds.

Abstract: A process of inhibiting the growth of, severely damaging, or killing plants which process comprises applying to the plant or to the growth medium thereof an effective amount of a composition comprising as active ingredient a compound of formula I: ##STR1## wherein A, B and D are independently chosen from the group consisting of hydrogen, halogen, hydroxy, nitro, cyano, thiocyano, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxy, optionally substituted alkenyloxy, optionally substituted alkynyloxy, optionally substituted alkylthio, optionally substituted cycloalkyl, optionally substituted amino, optionally substituted phenyl, carboxy, alkoxycarbonyl, optionally substituted carbamoyl, sulfo, alkylsulfonyl and optionally substituted sulfamoyl; R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.

Abstract: Hypoglycemic 5-phenyl and 5-naphthyl oxazolidine-2,4-diones and the pharmaceutically-acceptable salts thereof; certain 3-acylated derivatives thereof; a method of treating hyperglycemic animals therewith; and intermediates useful in the preparation of said compounds.

Abstract: Chemiluminescent-labeled conjugates of the formula: ##STR1## wherein one of R.sup.1 and R.sup.2 is hydrogen and the other is --NR.sup.3 R.sup.4 ; R.sup.3 is hydrogen or straight chain alkyl containing 1-4 carbon atoms and R.sup.4 isL(CO--HN--CH.sub.2).sub.nwherein n=2-8 and L(CO)-- is a hapten bound through an amide bond. The labeled conjugates are useful as reagents in specific binding assays for determining haptens or their specific binding partners in liquid media.

Abstract: Compounds useful as tracers in the radioimmunoassay of barbiturates: ##STR1## wherein (a) R.sub.1, R.sub.2 and R.sub.4 are identical to the substituents found at these positions in the barbiturate which is to be assayed;(b) at least one R.sub.3 is a radioiodinatable radical; and(c) if only one R.sub.3 is a radioiodinatable radical then the remaining R.sub.3 is identical to the substituent found at this position in the barbiturate which is to be assayed; and the radioiodinated derivatives of said compounds.

Abstract: Racemic and optically active compounds of the formulaQ--C.sub.n H.sub.2n --NH--Rwherein Q is ##STR1## where R.sub.1 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, trifluoromethyl or amino,R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or trifluoromethyl,R.sub.1 and R.sub.2, together with each other, are methylenedioxy or ethylenedioxy, andA is --O--, --CH.sub.2 --CH.sub.2 --, --O--CH.sub.2 -- where the oxygen is bonded to the benzene ring, or --NR.sub.3 -- where R.sub.3 is hydrogen or alkyl of 1 to 4 carbon atoms,N is an integer from 2 to 6, inclusive, andR is hydrogen, benzyl or ##STR2## where R.sub.4 is hydrogen, methyl or ethyl,R.sub.5, r.sub.6 and R.sub.7, which may be identical to or different from each other, are each hydrogen, halogen, hydroxymethyl, trifluoromethyl, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, nitro, cyano, --CONHR.sub.3, --CONHOH, --COOR.sub.3, R.sub.