Abstract: The invention provides mitochondrially targeted antioxidant compounds. A compound of the invention comprises a lipophilic cation covalently coupled to an antioxidant moiety. In preferred embodiments, the lipophilic cation is the triphenyl phosphonium cation, and the compound is of the formula P(Ph3)+XR.Z? where X is a linking group, Z is an anion and R is an antioxidant moiety. Also provided are pharmaceutical compositions containing the mitochondrially targeted antioxidant compounds, and methods of therapy or prophylaxis of patients who would benefit from reduced oxidative stress, which comprise the step of administering the compounds of the invention.

Abstract: 2-Methylene-19-nor-24(S) and 24(R) derivatives of 1?,25-dihydroxyvitamin D2 are disclosed. These compounds are characterized by minimal bone calcium mobilization activity and relatively high intestinal calcium transport activity. This results in novel therapeutic agents for the treatment of diseases such as renal osteodystrophy, autoimmune diseases, and osteoporosis.

Abstract: Host cells expressing HM74 were used to obtain furosemide-like molecules with agonist activity having the following structure formula:

Abstract: The present invention relates to substituted Azetidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.

Abstract: The invention relates to a novel use of known benzazepine, benzoxazepine, benzo-thiazepine-N-acetic acid and phosphono-substituted benzazepinone derivatives having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity. The compounds of the invention are useful for the preparation of pharmaceutical compositions for prophylaxis and treatment of neurodegenerative disorders. The compounds of the invention are known from the European patents EP 0 733 642 and EP 0 916 679, and can be described by the general formulae (1): wherein the symbols have the meanings as given above in the description.

Abstract: The invention concerns the use for producing of GSK-3? inhibiting medicines from paullone derivatives. The invention is useful for treating pathologies involving GSK-3? and CDK5.

Abstract: The present invention relates to derivatives of 1-oxa-3-aza-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory actions, especially to the inhibition of tumour necrosis factor-? (TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

Abstract: The invention relates to novel substituted pyrazolo[4,3-e]-diazepines of general formula: to pharmaceutical compositions containing them, to their use as medicinal products and to processes for preparing them.

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

Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Abstract: 4,5-Dihydroxypyrimidine-6-carboxamides of formula (I); are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R1, R2, R3 and R4 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract: The present invention relates to compounds of the Formula I wherein R1, R3, R5, R7, X, Y and U are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods of treating diseases and disorders, for example, neurodegenerative and/or neurological disorders, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, R1, R2, Rx, R8, R9 and n are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.

Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.

Abstract: Compounds of Formula (I) or (II) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein

Abstract: Quinazoline derivatives have the formula: or the pharmaceutically acceptable salts thereof; wherein each of Z5, Z6, Z7 and Z8 is N or CH and wherein one or two Z5, Z6, Z7 and Z8 are N and wherein two adjacent Z positions cannot be N; wherein m and n are each independently 0–3; wherein R1 is independently OH, SH, NH2, OR, SR, NHR, halo or R-halide; wherein two adjacent R1 groups may be joined to form an aliphatic hetero cycle ring of 5–6 members; wherein R2 is independently R, halo, R-halide, OR-halide, NH2, CONH2 or CONHR; wherein R is optionally substituted C1–C12 alkyl, C1–C12 alkenyl, C1–C12 alkynyl, or aryl C1–C12 alkyl, containing 0–4 heteroatoms in place of a carbon in the carbon backbone, where the optional substituents are ?O, ?N, or OH; and wherein R3 is H or CH3. Such compounds are useful in pharmaceutical compositions and methods of treating conditions characterized by enhanced TGF? activity.

Abstract: The present invention relates to phenylaminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states such as cancers associated with tyrosine kinases, especially Bcr-Abl, to their use as medicaments and to their use in the manufacture of medicaments for use in the production of inhibition of tyrosine kinase reducing effects in warm-blooded animals such as humans.

Abstract: The present invention provides compounds of Formula I or II that are useful as anti-cancer agents and other diseases that can be treated by inhibiting tyrosine kinase enzymes

Abstract: The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: (I) X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring optionally substituted; R2 represents a heterocyclic bicyclic rings, having 1–4 heteroatoms selected from an oxygen atom, a sulfur atom and a nitrogen atom and having 5–9 carbon atoms, of formula (II) R3 represents a hydrogen atom, a C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R4 represents a hydrogen atom, a C1-6 alkyl group, a C1-4 alkoxy group or a halogen atom.

Abstract: Methods are provided for treating or prophylactically preventing metabolic disorders in humans without causing, promoting, or aggravating fluid retention, peripheral edema, pulmonary edema, or congestive heart failure, by administration of a therapeutically effective amount of a compound sufficient to partially or fully activate peroxisome proliferator activated receptors (PPARs) and partially or fully inhibit, antagonize or block the activity of angiotensin II type 1 receptors. Metabolic disorders that can be treated or prevented include but are not limited to type 2 diabetes, the metabolic syndrome, prediabetes, and other insulin resistance syndromes.

Abstract: The invention provides kappa receptor agonists of formula (I) and delta receptor antagonists of formula (II), wherein R1–R6 X and n have any of the meanings given in the specification, as well as compositions comprising them, methods for their use, and synthetic procedures and intermediates useful for their preparation.

Abstract: A method for treatment of neurodegenerative disease conditions stemming from multiple sclerosis, aging, autoimmune diseases and fibromyalgia. A compound effective to increase neuronal metabolism of histamine to a histamine H2 agonist is administered in an amount sufficient to stimulate production of cyclic AMP at a level which is sufficient to maintain myelin against undergoing self-degeneration. The compound is selected from the group consisting of histamine M-methyltransferase, monoamineoxidase-A, monoamineoxidase-A agonists and histamine H3 antagonists. The histamine M-methyltransferase may be administered to increase neuronal metabolism of histamine to tele-methylhistamine, whereas the monoamineoxidase-A or monoamineoxidase-A agonist may be administered so as to increase neuronal metabolism of telemethylhistamine to an H2 agonist.

Abstract: Tetrahydro-?-carboline compounds represented by the following formulae: wherein x, y and z are each independently an integer of 0 to 4 and R is selected from the group consisting of H, alkyl, aryl and heterocyclic moiety wherein the alkyl, aryl and heterocyclic moiety are optionally substituted with a member selected from the group consisting of halogen, alkoxy and trifluoromethyl; pharmaceutically acceptable salts thereof and prodrugs thereof are provided. The compounds are useful for treating neurological diseases.

Abstract: Quinoline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans.

Abstract: The invention relates to 4-substituted quinoline compounds of general formula: which are active as antimicrobials, in which: X1, X2, X3, X4 and X5 is C—R?1, to C—R?5 respectively, or alternatively at most one represents N, Y represents CHR, CO, CROH, CRNH2, CRF or CF2, R being a hydrogen or alkyl, m is 1, 2 or 3 and n is 0, 1 or 2, Z is CH2 or Z is O, S, SO, SO2 and, in this case, n is equal to 2, R2 is —CO2R, —CH2CO2R, —CH2—CH2CO2R, —CH2OH or —CH2—CH2OH, wherein R is as defined above, R3 represents phenyl, heteroaryl or alk-Ro3, where alk is alkyl and Ro3 represents various groups, where appropriate containing oxygen, sulfur or amine, in their enantiomeric or diastereoisomeric forms or their mixtures, and/or where appropriate in the syn or anti form or their mixtures, and their salts.

Abstract: Quinolylpropylpiperidine derivatives of general formula (I) in which R1 is hydrogen or fluorine, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl substituted either with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino or R3 is propargyl substituted by phenyl or heteroaryl as defined above and R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their preparation process and intermediates and the compositions containing them.

Abstract: This invention relates to derivatives of 3,6-disubstituted azabicyclo compounds. The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to pharmaceutical compositions containing the compounds of the present invention and the methods for treating the diseases mediated through muscarinic receptors.

Abstract: This invention provides compounds of Formula 1, their N-oxides and agriculturally suitable salts wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure. Also disclosed are methods for controlling invertebrate pests comprising contacting the invertebrate pests or their environment with a biologically effective amount of a compound of Formula 1 or a composition comprising a compound of Formula 1.

Abstract: The present invention provides stereoscopically-pure diastereomers of Formula I: In a preferred embodiment, the stereoisomers of the present invention are of Formula II, depicted below: R2, R3 and R4 are independently H, OH, OCH3, CH2OH, NHCONH2, NH2, halogen or CF3, and R1 is pyridine, or an amine which may be substituted with hydrogen, lower alkyl, lower alkylenearyl, lower alkylenephenyl, lower alkylenehydroxyphenyl, lower alkyleneamine, lower alkyleneaminoaryl, lower alkylaminohydroxyphenyl, or a similar functional group. R5 is hydrogen, hydroxyl or methyl; R6 is hydrogen, lower alkyl, lower alkylenaryl, lower alkylenephenyl, lower alkylenehydroxyphenyl, lower alkyleneamine, lower alkyleneaminoaryl, lower alkylaminohydroxyphenyl, and the like. For both Formula I and Formual II, the first carbon on the side chain progressing from the ring is preferably in the R-configuration. The second carbon atom on the side chain of Formula II, which is attached to R5, may or may not be a chiral center.

Abstract: This invention concerns the use of a compound of formula (I?), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxy -carbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(?O)2—; mono- or di(C1-6alkyl)aminoS(?O)2; —C(?N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula (b-1), (b-2), or (b-3), L is optionally subs

Abstract: A composition, suitable for topical application to the skin, containing at least one benzoisothiazolone of formula (I): Novel benzoisothiazolones of formula (I) and a method of caring for dry and/or mature skin.

Abstract: The present invention relates to compositions for controlling plant pests containing the compound of formula (I) in a mixture with fungicidally active compounds, except for cyclopropylcarboxamide derivatives and azolylmethylcycloalkanes.

Abstract: Novel thiazole aniline compounds, pharmaceutical compositions, methods of making them and uses thereof in treating M3 muscarinic acetylcholine receptor mediated diseases are disclosed.

Abstract: The invention provides novel compounds useful as kinase inhibitors or as starting materials And/or intermediates in the synthesis of compounds useful as kinase inhibitors. The compounds have The general structure of formula (I) wherein A is a 3- to 8-membered ring, optionally substituted and/or heteroatom-containing, and R1, R2, R3, R4, R5, R6, X, Y, Z, p, and q are as defined herein. The compounds may also be in the form of a salt, ester, amide, or other analog. In preferred compounds, A is a 5- to 8-membered ring, R1 is hydrogen, q is a bond, X is N, Y is C?O, Z is N, R2 contains a terminal amino moiety, p is 1, and R3 and R4 are linked to form a pyrrole ring fused to a second cyclic group. Pharmaceutical compositions and methods for using the compounds are also provided.

Abstract: Disclosed are methods and compositions for the treatment of a wide array of cancers and tumors. In illustrative embodiments, diindolylmethanes, C-substituted diindolylmethanes, and analogs thereof have been described, which when administered either alone, or in combination with other anti-cancer or anti-tumorigenic compounds, provide new therapies for the treatment of cancer.

Abstract: Dihydronepetalactone, a minor natural constituent of the essential oil of catmints (Nepeta spp.) such as Nepeta cataria, has been identified as an effective insect repellent compound. Synthesis of dihydronepetalactone may be achieved by hydrogenation of nepetalactone, the major constituent of catmint essential oils. This compound, which also has fragrance properties, may be used commercially for its insect repellent properties.

Abstract: The invention relates to novel active compound combinations of certain cyclic ketoenols and certain insecticidally active compounds that together have very good insecticidal and acaricidal properties.

Abstract: The oral administration to genetically alcoholic rats (from the strain UChB of the University of Chile) of a compound selected from endogenic polyamines (putrescine, spermidine, spermine), 1,3-propanediamine, their pharmaceutically acceptable salts and solvates, and their bioprecursor amides, causes a significant reduction in the alcohol consumption. The activity lasts for some time after the treatment period. Besides, there is a virtually null disulfiram-like adverse effect, what constitutes an advantage over the unpleasant use of some anti-alcoholism agents, such as calcium cyanamide or disulfiram itself. Therefore, the compounds of the invention are useful for the preparation of medicaments for the therapeutic and/or prophylactic treatment of alcoholism in human beings.

Abstract: The invention relates to 4-hydroxymethyl-1-aryl-cyclohexylamine compounds, methods for their production, pharmaceutical formulations containing such compounds and the use of 4-hydroxymethyl-1-aryl-cyclohexylamine derivatives for producing medicines which are useful, for example for treating pain. Related methods of treatment are also provided.

Abstract: An apparatus for converting a gaseous and/or liquid feed fluid to gaseous and/or liquid products using a solid catalyst comprises a reactor, a liquid phase disposed within the reactor volume, a fixed catalyst at least partially disposed in the liquid phase, a cooling system having a cooling element in thermal contact with the liquid phase, a feed inlet positioned to feed the feed fluid into the reactor volume, and a fluid outlet in fluid communication with the liquid phase. The catalyst is contained in a catalyst container and the container may be adjacent to said cooling element, extend through said cooling element, or may surround the catalyst container. The catalyst may be a Fischer-Tropsch catalyst.

Abstract: A crosslinked polymeric bead comprising a polymer having from 0.5 mole percent to 2 mole percent crosslinker. The bead has a diameter no greater than 200 ?m, no void spaces having a diameter greater than 5 ?m, and less than 5 weight percent of organic extractables.

Abstract: A photocurable composition comprising cationically curable compound, an acrylate-containing compound; a hydroxyl-containing compound; a cationic photoinitiator; and a free radical photoinitiator; wherein said composition has less than 0.54 equivalents of cationically curable groups, less than 0.10 equivalents of acrylate groups and less than 0.10 equivalents of hydroxyl groups per 100 grams of said composition.

Abstract: An energy curable lithographic ink composition having an asymptotic relative viscosity of about 0.4 to about 1.5 and a water up-take number of at least about 30%. Also disclosed is a method of improving various rheological properties and increasing the water window of an energy curable lithographic ink by varying the composition of the ink in order to result in an asymptotic relative viscosity of about 0.4 to about 1.5 and a water up-take number of at least about 30%. A method of identifying and selecting an energy curable lithographic ink composition having optimal press performance is also disclosed.

Abstract: A visible light cationically photopolymerizable composition is provided. This composition includes an expanding monomer and a dioxirane. More specifically, the expanding monomer used in this composition is one or more dioxiranyl tetraoxaspiro[5.5]undecanes. The composition of the present invention may be used as a matrix resin for dental restorative materials. Another embodiment of the present invention is various novel dioxiranyl tetraoxaspiro[5.5]undecanes.

Abstract: Colored fine particulate resins can each be produced by bringing a colored resin, which comprises a thermally fusible resin and a colorant evenly distributed in the thermally fusible resin, into a molten state; forming the colored resin, which is in the molten state, into droplet-shaped fine particles in a non-dissolving medium which does not dissolve the colored resin; and then cooling and solidifying the droplet-shaped fine particles. The colored fine particulate resins are useful in image recording materials, printing materials and paints. Articles can be colored with the image recording materials, printing materials or paints.

Abstract: Polycarbonate compositions containing a specific combination of additives achieve desirable flame retardance characteristics when used in thin wall polycarbonate articles. These compositions contain a polycarbonate/siloxane component, containing a polycarbonate siloxane copolymer, or a mixture of a polycarbonate siloxane copolymer and polycarbonate resin; a mineral filler; and a flame retardant. The composition contains at least 50% by weight of polycarbonate when the polycarbonate of the polycarbonate siloxane copolymer and any polycarbonate resin (linear or branched) are considered together; and the polycarbonate siloxane copolymer and the mineral filler are present in amounts effective to achieve a flex modulus of 29,000 kg/cm3 or greater, for example 30,000 kg/cm3 or greater, good flex-fold strength and good impact strength, for example a room temperature Notched Izod Impact Strength of 25 kgf-cm/cm or greater.

Abstract: A thermoplastic polymer/elastomer composite composition including one or more thermoplastic polymers, a natural or synthetic rubber, and a long chain cyclic dimerate ester and/or long chain cyclic trimerate ester plasticizer.

Abstract: A flame-retardant compound is disclosed, comprising a polyolefin alloy and a combination of flame-retardant agents. The polyolefin alloy comprises at least one polyolefin and a metallocene-catalyzed olefin copolymer. The flame-retardant agents comprise a nanoclay and at least one inorganic flame-retardant. An essentially halogen-free flame-retardant compound is preferred. Surface coverings for mammalian-occupied spaces benefit from the properties of the flame-retardant compound.

Abstract: An adhesive composition comprising natural rubber based particles uniformly dispersed in a radiation setting compound is cured by radiation to make a pressure-sensitive adhesive layer on a substrate, thereby: sufficient adhesiveness is obtained; different fillers sufficiently charged; drying time after application is short; both overall application and pattern application are readily performed; application can be performed on different substrates; and sufficient adhesive strength between the substrate and the pressure-sensitive adhesive layer can be realizes. This adhesive composition may be manufactured by: mixing aqueous emulsion 31 containing the natural rubber based particles 30 and the radiation setting compound 32; elevating a temperature of the mixture while stirring; removing vaporized water in the aqueous emulsion; and replacing the water as the medium wherein the natural rubber based particles are dispersed with the radiation setting compound.

Abstract: The present invention relates to the thermoplastic hydrophilic adhesive compositions having an increased adhesion capability and stability on moist or wet surfaces. The adhesive compositions comprise a thermoplastic hydrophilic homogeneous polymeric matrix having selected liquid absorption capacity, liquid absorption rate, and rheology. The adhesive compositions of the present invention are particularly suitable as topical adhesives for skin adhesion of articles such as disposable waste management articles, disposable absorbent articles, and personal care articles.