Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: Novel bisamidate phosphonate prodrugs of FBPase inhibitors of the Formula IA: and their use in the treatment of diabetes and other conditions associated with elevated blood glucose.

Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.

Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.

Abstract: The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, 1

Abstract: The present invention relates to novel aryl-substituted S(O)m cycles of the formula (I) 1

Abstract: The present invention relates to novel &agr;-substituted-&bgr;-aminoethylphosphonate and &agr;-substituted-&bgr;-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low density lipoproteins and very low density lipoproteins) and for lowering plasma levels of total cholesterol.

Abstract: This invention provides compounds having the structure wherein A is OR5, or R1 is alkyl, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, pyridyl, R2 is H, alkyl, or aryl; R3 and R4 are halo, H, alkyl, aryl, trifluoromethyl, alkoxyaryl, nitro, amino, carboalkoxy, carbamide, carbamate, urea, alkylsulfonamide, —NR7(CH2)mCO2H, arylsulfonamide, cycloalkyl, or a heterocycle; R5 is H, alkyl, —CH(R8)R9, —CH2(CH2)nCO2R10, —C(CH3)2CO2R10, —CH(R8)(CH2)nCO2R10, —CH(R8)C6H4CO2R10, or —CH2-tetrazole; R6 is H, alkyl, halo, alkoxy, trifluoroalkyl or trifluoroalkoxy; R7 is H or alkyl; R8 is H, alkyl, aryl, arylalkyl, cycloalkyl, phthalic acid, R9 is CO2R12, CONHR12, tetrazole, or PO3R12; R10 is H, alkyl, aryl, or aralkyl; R11 is alkyl; R12 is H, alkyl, aryl, or aralkyl; X is O, or S; Y is O, N, or S; Z is C, or N; Q is O, N, or S; m=1-3; n=1-6, or a pharmaceutically acceptable salt thereof, which

Abstract: Die invention relates to the use of compounds of the general formula (I) 1

Abstract: The present invention provides medicinal compositions characterized by containing as the active ingredient either a compound represented by a general formula (1) or a pharmaceutically acceptable composite thereof, 1

Abstract: The invention provides compounds of formula 1,

Abstract: Compounds of formula (I) or pesticidally acceptable salts thereof, compositions containing them and methods of use.

Abstract: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.

Abstract: Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading enzymes is involved.

Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes.

Abstract: The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and conditions related to diabetes.

Abstract: The present invention is directed to compounds, compositions and methods of inhibiting and treating HIV and related viruses, and methods for cocrystallizing reverse transcriptase in vitro, inhibition of the replication of HIV and related viruses thereof.

Abstract: The present invention provides novel compounds represented by the general 1

Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme.

Abstract: The present invention relates to novel antioxidative Vitamin B6 analogs and their use in the cosmetic, dermatological, pharmaceutical and/or nutritional fields. Analogs can be provided in suitable formulations intended in particular for caring for the skin, make up for the skin, protection from the sun of the skin, as well as for the treatment of diseases of the skin and bone, and viral, parasitic and fungal infections.

Abstract: Novel FBPase inhibitors of the formula I 1

Abstract: The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities.

Abstract: A highly reliable method of measuring an analyte in a sample using a redox reaction. In this method, a tetrazolium compound is added to a sample prior to the redox reaction so as to eliminate the influence of any reducing substance in the sample, then a reducing substance or an oxidizing substance derived from the analyte is formed, the quantity of the formed substance derived from the analyte is measured by the redox reaction, and the quantity of the analyte is determined from the quantity of the formed substance derived from the analyte. As the tetrazolium compound, for example, 2-(4-iodophenyl)-3-(2,4-dinitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium salt can be used.

Abstract: Angiotensin II receptor antagonists are useful for decreasing QT dispersion or inhibiting the progression of QT prolongation in patients. Also disclosed is a method for monitoring the reduction in die risk of experiencing an adverse cardiac event, such as sudden cardiac death, myocardial infarction or arrhythmias, using QT dispersion in patients treated with a therapeutically effective amount of an angiotensin II antagonist.

Abstract: The present invention relates to processes for the conversion of nitrites to amidines in the preparation of compounds which are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex. The compounds described herein are potent thrombolytics and useful for the inhibition of platelet aggregation in the treatment of thromboembolic disorders.

Abstract: A compound of formula and salts and solvates thereof, wherein R0, R1, and R2 are defined in the specification. A compound of the present invention is a potent and selective inhibitor of cGMP-specific PDE and has utility in a variety of therapeutic areas where such inhibition is beneficial.

Abstract: A low volatile organic compound co-solvent system is disclosed for preparing emulsion concentrates of low melting organophosphorous insecticides wherein the bioefficacy of the insecticide active is significantly enhanced. The co-solvent system comprises a water-soluble ethoxylated fatty acid/rosin acid-nonionic surfactant composition.

Abstract: A method and composition for the treatment of HIV infection, HBV infection, or abnormal cellular proliferation in humans and other host animals is disclosed that includes the administration of an effective amount of a 1,3-oxaselenolane nucleoside or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

Abstract: A method is provided for treating schizophrenia in a mammalian species by administering an ACE inhibitor, such as captopril, alone or with a neuroleptic such as cholecystokinin, fluphenazine or haloperidol.

Abstract: The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases.

Abstract: A compound of formula ##STR1## and salts and solvates thereof, wherein R.sup.0, R.sup.1, and R.sup.2 are defined in the specification. A compound of the present invention is a potent and selective inhibitor of cGMP-specific PDE and has utility in a variety of therapeutic areas where such inhibition is beneficial.

Abstract: The present invention is concerned with compounds of formula I ##STR1## wherein Z, R.sup.1 and R.sup.2 are as defined herein, as well as their pharmaceutically acceptable salts as therapeutically active substances against central nervous system disorders and for the production of corresponding medicaments.

Abstract: A phosphonic diester derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents a cycloalkyl group; a phenyl group which may have 1 to 3 substituents selected from the group consisting of a lower alkoxy group, a lower alkyl group, a halogen atom, a halogen-substituted lower alkyl group, a lower alkanoyl group, a nitro group, a benzoyl group, a cyano group, an N-lower alkylcarbamoyl group, an N-phenyl-lower alkylcarbamoyl group, an N-(halogen-substituted phenyl)carbamoyl group and an N,N-di-lower alkylcarbamoyl group; a 1,3,4-thiadiazol-2-yl group having a halogen-substituted lower alkyl group as a substituent; a thiazolyl group; a pyridyl group which may be substituted by a halogen atom; a benzothiazol-2-yl group having 1 to 2 lower alkoxy groups on the phenyl ring; or a 4,5-dihydrothieno[3,2-e]benzothiazol-2-yl group; R.sup.2 represents a hydrogen atom or a phenyl lower alkyl group; R.sup.3 and R.sup.

Abstract: A pesticide comprising an active ingredient combination consisting ofa) tetrahydro-3,5-dimethyl-1,3,5-thiadiazine-2-thione of the formula ##STR1## and b) O-(O-ethyl-S-n-propylphosphoryl)-O-(N-methylcarbamoyl)pyrocatechol of the formula ##STR2## and/or c) O-ethyl S,S-dipropyl phosphorodithioate of the formula ##STR3## and/or d) 2-methyl-2-methylthiopropionaldehyde O-methylcarbamoyloxime of the formula ##STR4## and/or e) N,N-dimethyl-2-methylcarbamoyloximino-2-methylthioacetamide of the formula ##STR5## and/or f) ethyl-4-methylthio-m-tolylisopropylphosphoramide of the formula ##STR6## and/or g) (RS)-S-sec-butyl O-ethyl 2-oxo-1,3-thiazolidin-3-ylphosphono-thioate of the formula ##STR7## and/or h) 2,3-dihydro-2,2-dimethylbenzofuran-7-yl methylcarbamate of the formula ##STR8## and/or i) S-tert-butylthiomethyl O,O-diethyl phosphorodithioate of the formula ##STR9## and/or j) S,S-di-sec-butyl O-ethyl phosphorodithioate of the formula ##STR10## and/or k) (RS)-O-1-(4-chlorophenyl)pyrazol-4-yl O-ethyl S-propyl phosphoro

Abstract: Phosphoramidates and phosphinic amides and related compounds are provided. Also provided are methods that use the compounds for modulating the activity of the endothelin family of peptides are provided. In particular, compounds having formula: ##STR1## in which A, B, R.sup.1 and R.sup.2 are as described are provided. Also provided are methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these compounds or prodrugs thereof. Methods for elucidating the physiological and pathophysiological roles of endothelin, as well as isolating endothelin receptors are also provided.

Abstract: The present invention provides novel phosphate derivatives having the general formula wherein A, R.sup.1 and R.sup.2 are as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of potassium channels.

Abstract: A method for the protection of trees of the families Musaceae or Plantanginaceae from destructive pests whereby the trees to be protected share a common root system.

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: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.

Abstract: The present invention relates to thio-substituted, nitrogen-containing heterocyclic phosphonate compounds, including bisphosphonates, phosphonoalkylphosphinates, phosphonocarboxylates, and phosphonosulfonates, and the pharmaceutically-acceptable salts and esters thereof useful for the treatment and prevention of osteoporosis and arthritis. These compounds have the general structure: ##STR1## (a) Z is a monocyclic or polycyclic heterocyclic ring moiety containing one or more heteroatoms selected from O, S, or N, at least one of which is N;(b) Q is covalent bond; O, S, N, or NR.sub.1 ;(c) R is COOH, SO.sub.3 H, PO.sub.3 H.sub.2, or P(O)(OH)R.sup.4, wherein R.sup.4 is substituted or unsubstituted C.sub.1 -C.sub.8 alkyl;(d) each R1 is independently selected from --SR.sup.6 ; --R.sup.8 SR.sup.6 ; nil; hydrogen; unsubstituted or substituted C.sub.1 -C.sub.8 alkyl; unsubstituted or substituted aryl; hydroxy; --CO.sub.2 R.sup.3 ; --O.sub.2 CR.sup.3 ; --NR.sup.3.sub.2 ; --OR.sup.3 ; --C(O)N(R.sup.3).sub.2 ; --N(R.sup.

Abstract: There are provided arylthio, -sulfinyl and -sulfonyl pyrrole compounds having the structural formula I ##STR1## Further provided are compositions and methods comprising those compounds for the control of insects.

Abstract: The present invention relates to quaternary nitrogen-containing phosphate compounds, and the pharmaceutically-acceptable salts and esters thereof having the general structure: ##STR1## wherein: Z is a saturated, unsaturated, or aromatic, monocyclic or polycyclic carbocycle or monocyclic or polycyclic heterocycle containing one or more heteroatoms selected from O, S, or N;Y is N.sup.+ (R.sup.8).sub.2 or C(R.sup.1).sub.2 and when Y is C(R.sup.1).sub.2, at least one R.sup.2 must be N.sup.+ (R.sup.8).sub.3 ;R.sup.1, R.sup.2, R.sup.5, and R.sup.8 are defined in claim 1, m and n are integers from 0 to 10; m+n is from 0 to 10;R is COOH; PO.sub.3 H.sub.2 ; SO.sub.3 H; or P(O)(OH)R.sub.4, wherein R.sub.4 is substituted or unsubstituted alkyl of 1-8 carbons atoms.The present invention further relates to pharmaceutical compostions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients.

Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; ....... represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## ,or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.

Abstract: The present invention relates to phosphonsulfonates and the pharmaceutically-acceptable salts and esters thereof, having the following structure according to formula (I): ##STR1## The present invention further relates to pharmaceutical compositions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients. Finally, the present invention relates to methods for treating or preventing pathological conditions characterized by abnormal calcium and phosphate metabolism in humans or other mammals, including treating or preventing osteoporosis and arthritis, especially rheumatoid arthritis and osteoarthritis. This method comprises administering to a human or other mammal in need of such treatment of a safe and effective amount of a compound or composition of the present invention.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and n have the meanings reported in the description are described.The compounds of formula I are endowed with a dual ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.