Abstract: A pharmaceutical composition is provided which includes a pharmaceutically acceptable excipient and a pharmaceutically and physically acceptable amount of a compound selected from the group consisting of Chemical Formulas I-IV as described herein, or a pharmaceutically acceptable salt thereof. Also provided are methods of increasing a level of a defined neurotrophic peptide in an organism or tissue comprising the administration of a pharmaceutically and physically acceptable amount of one or more of the compositions described above, and a method for treating a neurodegenerative disease in a subject in need thereof, the method comprising administering a therapeutically effective amount of the pharmaceutical composition of claim 1.

Abstract: Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.

Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.

Abstract: The present invention provides a pest control composition having an excellent controlling effect on pests, which comprises a combination of an ester compound represented by the formula (1): and a cyclic compound represented by the formula (2a) and/or a cyclic compound represented by the formula (2b).

Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

Abstract: The present invention concerns a method for identifying a compound which inhibits the activation of RAC GTPase by DOCK5 protein comprising the steps of (i) coexpressing the DOCK5 and the RAC proteins in a cell, wherein said DOCK5 protein induces the conversion of inactive RAC, which inactive RAC is bound to GDP, to active RAC, which active RAC is bound to GTP, (ii) contacting or not said cell with said compound, (iii) determining the conversion of inactive RAC to active RAC in the presence or absence of said compound, and (iv) selecting the compound inhibiting the conversion of inactive RAC to active RAC. Said compound is useful for treating disease-associated bone loss.

Abstract: The present invention is directed to novel sulfamide derivatives, pharmaceutical compositions comprising said compounds and methods for the treatment of epilepsy and related disorders comprising administering to a subject in need thereof, said compounds, either alone or as co-therapy with one or more anticonvulsant and/or anti-epileptic agents.

Abstract: N-Substituted sulfoximines are effective at controlling insects.

Abstract: The present invention relates to inhibiting angiogenesis with sulfur- or selenium-containing compounds, and polymeric forms thereof, in mammals including animals and humans. Sulfur- or selenium-containing compounds, and polymeric forms thereof, can be used alone or in combination with standard therapies to inhibit angiogenesis-mediated disorders. The present invention also relates to the combined use of sulfur- or selenium-containing compounds, and polymeric forms thereof, with other anti-angiogenesis agents, with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer, and with laser, photodynamic therapy for ocular-related disorders such as diabetic retinopathy or age-related macular degeneration.

Abstract: The present invention relates to sulfonamide derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are useful in the treatment of neuronal disorders, autoimmune diseases, cancer and cardiovascular diseases. Furthermore, said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and -3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. Formula (I) IAr1 is a substituted or unsubstituted aryl or heteroaryl group; X is O or S, preferably O; Ar2 a substituted or unsubstituted arylene or heteroarylene group; R1 and R2 are independently selected from the group consisting of hydrogen and a C1-C6-alkyl group.

Abstract: N-Substituted sulfoximines are effective at controlling insects.

Abstract: N-Substituted sulfoximines are effective at controlling insects.

Abstract: A method of treatment of hyperproliferative disorders comprises a step of administering an effective amount of a compound represented by

Abstract: The present invention relates to sulfamate benzothiophene compounds of the formula: (I) wherein R1, R2, R3, m and n are as defined in the specification. The invention also relates to pharmaceutical compositions containing these compounds and to methods of using them.

Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13 SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.

Abstract: Compounds of formula (I): wherein: X is a group of formula (B): and R1, R2, R4, n, x, y and z are as defined within are described. Processes for their preparation and their use in the treatment of disorders mediated by the neuropeptide Y5 receptor in a warm-blooded animal, such as a human being, are also described.

Abstract: Therapeutic substituted cyclopentane compounds, and compositions, medicaments, and therapeutic methods related thereto are disclosed herein.

Abstract: Novel pyraole derivatives of formula (I), wherein: X is oxygen or sufu, R1 is C1–C3alkyl, C1–C3haloalkyl, C1–C3alkoxy-C1–C3alkyl or C1–C3haloalkoxy-C1–C3alkyl; R2 is C1–C3haloalkyl; and R3 is halogen. The novel compounds have plant-protective properties and are suitable for protecting plants against infestations by phytopathogenic microorganisms.

Abstract: A method of treatment of hyperproliferative disorders comprises administering an effective amount of a compound represented by Formula II: or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides compounds of formula (I) the prodrugs thereof, and the pharmaceutically acceptable salts of the compounds and prodrugs, wherein R?, R?, R??, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof in treating diabetes, insulin resistance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, cataracts, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis, and tissue ischemia.

Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1 is R2 is and R3 is C0-4alkyl, are useful in the treatment of cancer.

Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.

Abstract: Compounds represented by Formula (I): 1

Abstract: Compounds of formula I: [wherein: X represents —CH═CH—, —CH═CR—, —CR═CR—, —CO—, —O—, —NH—, —NR—, S—, —SO—, —SO2—, —CH═N—, —CR═N—, —CH═N(O)—, —CR═N(O)— or any other atom or group of atoms capable of forming a S— or 6-membered heterocyclic ring; Y1, Y2 and Y3 independently represent hydrogen or halogen; R1, R2 and R3 are independently represent hydrogen, halogen, hydrocarbyl (—R), hydroxyl (—OH), hydrocarbyloxy (—O—R), mercapto (—SH), hydrocarbylthio (—S—R), hydrocarbylsulfinyl (—SO—R), hydrocarbylsulfonyl (—SO2—R), nitro (—NO2), amino (—NH2), hydrocarbylamino (—NHR), bis(hydrocarbyl)amino (—NR2), hydrocarbylcarbonylamino (—NH—CO—R), cyano (—CN), carbamoyl (—CONH2), hy

Abstract: &bgr;-lactamases are the most widespread resistance mechanism to &bgr;-lactam antibiotics, such as penicillins and cephalosporins. In response to these enzymes, inhibitors have been introduced. Unfortunately, these inhibitors are also &bgr;-lactams, and resistance to them has developed rapidly. Consequently, the present invention provides a novel structure-based approach to inhibitors of these enzymes.

Abstract: Tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.

Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.

Abstract: &agr;, &bgr;-Unsaturated sulfones of the following formulae are provided, which are useful as antiproliferative agents, including, for example, anticancer agents:

Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2  I  in which A, R1 and R2 are as defined in the description, and b) compounds of the formula II, their N-oxide or one of their salts  where the substituents R12 to R18 are as defined in the description, and/or c) compounds of the formula III  where the substituents X1 to X5 and R19 to R22 are as defined in the description, in a synergistically effective amount.

Abstract: Compounds of formula (I) 1

Abstract: This invention provides methods which are useful for the inhibition of the various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of formula I:

Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula 1

Abstract: Methods for treating diseases associated with toxicity of Apolipoprotein E (“apoE”). Specifically, the present invention relates to new methods for treating a mammal having a condition associated with toxicity of apolipoprotein E cleavage fragments containing residues 130-169, comprising administering to said mammal a pharmacologically effective amount of compound or a pharmaceutically acceptable sale, derivative or fragment thereof to interfere with the receptor-binding site associated with residues 130-169 of the apolipoprotein E molecule in said mammal.

Abstract: A mixed micellar pharmaceutical formulation includes a micellar proteinic pharmaceutical agent, an lkali metal C8 to C22 alkyl sulphate, alkali metal salicylate, a pharmaceutically acceptable edetate and at least one absorption enhancing compounds. The absorption enhancing compounds are selected from the group consisting of lecithin, hyaluronic acid, pharmaceutically acceptable salts of hyaluronic acid, octylphenoxypolyethoxyethanol, glycolic acid, lactic acid, chamomile extract, cucumber extract, oleic acid, linolenic acid, borage oil, evening of primrose oil, trihydroxy oxo cholanylglycine, glycerin, polyglycerin, lysine, polylysine, triolein and mixtures thereof. The amount of each absorption enhancing compound is present in a concentration of from 1 to 10 wt./wt. % of the total formulation, and the total concentration of absorption enhancing compounds are less than 50 wt./wt. % of the formulation.

Abstract: Compounds related to lactacystin and lactacystin &bgr;-lactone, pharmaceutical compositions containing the compounds, and methods of use.

Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds having the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## which are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders are provided. In particular, based on their RXR-agonist activity, these compounds may be used to treat noninsulin-dependent diabetes mellitus (NIDDM) and obesity.

Abstract: An intimal thickening inhibitory agent comprising, as an active ingredient, a compound represented by formula (1): ##STR1## wherein X represents an oxygen atom or a group of formula (2): ##STR2## wherein n represents an integer of from 0 to 2, R.sub.1 represents a hydrogen atom or an acyl group; R.sub.2 represents a hydrogen atom, a lower alkyl group or a lower alkenyl group; R.sub.3 represents a lower alkyl group; and R.sub.4, R.sub.5, and R.sub.6, which may be the same or different, each represent a hydrogen atom or a substituted or unsubstituted alkyl group; or R.sub.3 and R.sub.4 may be taken together to form a 5-membered ring; or R.sub.5 and R.sub.6 may be taken together to form a cycloalkyl group; provided that R.sub.6 is nil when R.sub.3 and R.sub.4 are taken together to form benzofuran or benzo[b]thiophene.

Abstract: This invention provides methods which are useful for the inhibition of the various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of formula I: ##STR1##

Abstract: Tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.

Abstract: The present invention relates to the derivatives of formula: ##STR1## and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.

Abstract: A compound of the formula ##STR1## wherein R is a) phenyl; phenyl(C.sub.1 -C.sub.4 alkoxy); phenoxy; or benzyl; the phenyl ring of each substituent being optionally substituted with one or more of halogen, nitro, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 haloalkyl, C.sub.1 -C.sub.8 haloalkoxy, di(C.sub.1 -C.sub.8 alkyl)amino, phenyl or phenoxy; or b) a 5- or 6-membered heterocyclic group comprising 1-3 heteroatoms selected from the group consisting of N, O or S, optionally substituted with one or more of halogen, nitro, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 haloalkyl, C.sub.1 -C.sub.8 haloalkoxy, or di-(C.sub.1 -C.sub.8 alkyl)amino. These compounds and pesticidal compositions prepared therefrom, are useful as plant protecting agents for the control of insects, nematodes, and mites.

Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.

Abstract: Tetrahydrofurans tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.

Abstract: The present invention provides a compound of formula (1) ##STR1## in which: R.sub.4 represents a hydrogen atom, a halogen atom or a nitro group;R.sub.6 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.6) alkyl group;R.sub.7 represents a chlorine atom or a hydroxyl group; andZ represents: a phenyl group optionally substituted with one or more halogen atoms, straight or branched (C.sub.1 -C.sub.4)alkyl groups, straight or branched (C.sub.1 -C.sub.4)alkoxy groups, or trifluoromethyl, formyl, --CH.sub.2 OR, --CH.sub.2 OCOR, --CH.sub.2 CONRR', --CH.sub.2 ONCOR, --COOR, nitro, --NHR, --NRR' or --NHCOR groups, wherein R and R' are each, independently, a hydrogen atom or a (C.sub.1 -C.sub.7) alkyl group; a heterocyclic group optionally substituted as defined above for phenyl; or a cyclo(C.sub.5 -C.sub.8)alkyl group; additionally, when R.sub.

Abstract: Nitroxyalkylamide compounds having the formula: R.sup.1 --(A).sub.n --CONH--B'--ONO.sub.2 wherein R.sup.1 is an optionally substituted furyl, furyloxy, thienyl, thienyloxy, isoxazolyl, phenoxy, phenylthio or 1,4-dibenzodioxanyl, A is a C.sub.1 -C.sub.4 alkylene group; B' is a C.sub.1 -C.sub.4 alkylene group; and n is 0 or 1. The compounds of the present invention have a desirable vasodilator action for collateral vessels and an anti-anginal action, and are useful as therapeutic agents for treating angina pectoris.

Abstract: This invention is directed to 1-alkoxy-2-(alkoxy- or cycloalkyloxy-)-4-(cyclothioalkyl- or cyclothioalkenyl-)benzene compounds that inhibit cyclic AMP phosphodiesterase or tumor necrosis factor (TNF) and are useful in treating patients suffering from disease state capable of being modulated by inhibiting production of cyclic AMP phosphodiesterase or TNF by administering the compound to the patient. The invention is also directed to the preparation of these compounds, pharmaceutical compositions containing these compounds and methods for their pharmaceutical use.

Abstract: HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.

Abstract: The present invention relates to a method of treating urinary incontinence in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, azanorbornane derivatives of azabiaglo and related compounds.

Abstract: Benzylidene derivatives having anti-inflammatory activities, are shown by the following formula I: ##STR1## wherein A is -CH.sub.2 - or -CH.sub.2 CH.sub.2 -; B is a bond or -CH.sub.2 -, -CHOH-, -CO-, -O-, or A and B may taken together form -CH=CH-; D is >N- or >CH-; R.sup.1 and R.sup.2 each independently is hydrogen, lower alkyl or lower alkoxy; R.sup.3 is hydrogen, lower alkyl, cycloalkyl, lower alkoxy, arylalkyloxy, heteroarylalkyloxy, lower alkylcarbonyl, arylcarbonyl, substituted or unsubstituted carbamoyl, or a group of the formula:-(CH.sub.2).sub.n -R.sup.4wherein R.sup.4 is hydrogen, hydroxy, substituted or unsubstituted amino, aryl, heteroaryl, hydroxycarbonyl or lower alkyloxycarbonyl; n is an integer of 0-3.

Abstract: The invention concerns benzenesulphonamide derivatives of the formula I ##STR1## wherein R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; R.sup.2 and R.sup.3 together form -A.sup.2 -X.sup.2 -A.sup.3 - which defines a ring having 5 or 6 ring atoms, wherein A.sup.2 and A.sup.3 each is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl; A.sup.1 is a direct link to X.sup.1 or is (1-3C) alkylene; X.sup.1 is oxy, thio or imino; Ar is optionally substituted phenylene; R.sup.4 is (1-4C)alkyl, fluoro-(2-4C)alkyl or optionally substituted phenyl or a heterocyclic moiety; R.sup.5 is hydrogen or (1-4C)alkyl; and R.sup.6 is hydrogen, halogeno, trifluoromethyl, (1-4C)alkyl or (1-4C)alkoxy; or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.