Abstract: A method of treating cells that carry at least one APOE4 allele comprises increasing nitric oxide levels in the cells (e.g., by administering an exogenous source of nitric oxide to the cells) by an amount sufficient to combat the decrease of nitric oxide level associated with the presence of the APOE4 allele. Also disclosed is a method of increasing nitric oxide levels in cells in need thereof which comprises administering APOE to the cells in an amount sufficient to increase nitric oxide levels in the cells.

Abstract: The present invention is directed to a pharmaceutical composition comprising a pharmaceutically effective amount of a lipophilic drug, in association with a pharmaceutical carrier, said carrier comprising a lipophilic drug solubilizing effective amount of a propylene glycol monoester of C6-C18 fatty acid having at least 60% by weight monoester based on the total weight of the propylene glycol ester and a non-ionic surfactant.

Abstract: PEG-LHRH analog conjugates, where a PEG moiety is covalently bound to a serine residue of a LHRH analog either directly or via a bifunctional linker molecule, such as an amino acid, and methods for producing these conjugates are provided in the present invention. Also provided are a pharmaceutical composition and a method for treating pathologies in which LHRH analog administration is beneficial.

Abstract: Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.

Abstract: This invention relates to novel compounds of the following formula and a process for the preparation thereof.

Abstract: The present invention generally relates to the field of treating degenerative disease by administering a pharmaceutically effective amount of a compound that elevates glutathione or at least one Phase II detoxification enzyme in diseased tissue. The present invention also relates to a pharmaceutical composition useful for the treatment of degenerative diseases, as well as a method of identifying agents that modulate intracellular levels of glutathione or intracellular levels of at least one Phase II enzyme in neuronal cells.

Abstract: The present invention provides novel hydrogel-forming, self-solvating, absorbable polyester copolymers capable of selective, segmental association into compliant hydrogels upon contacting an aqueous environment. Methods of using the novel polyester copolymers of the invention in humans are also disclosed for providing a protective barrier to prevent post-surgical adhesion, treatment of defects in conduits such as blood vessels, and controlled release of a biologically active agent for modulating cellular events such as wound healing and tissue regeneration or therapeutic treatment of diseases such as infection of the periodontium, dry socket, bone, skin, vaginal, and nail infections.

Abstract: Novel nitric-oxide releasing lipid molecules are provided which comprise a lipid molecule selected from (a) phosphoglycerides, (b) lipids having a sphingosine base as a backbone, (c) monoacylglyerols, (d) diacylglycerols, (e) glycosylacylglycerols, and (f) sterol compounds of the formula: 1

Abstract: The present invention is directed to polymeric-prodrug transport forms of the formula: wherein: E1-4 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy, C1-6 heteroalkoxy, and at least one of E1-4 includes a B moiety, wherein B is a leaving group, OH, a residue of a hydroxyl-or amino-containing moiety or wherein J1 is the same as J, or another member of the group defining J and E5 is the same as E1-4, or another member of the group defining E1-4; Y1-2 are independently O, S or NR9; M is a heteroatom selected from either X or Q; wherein X is an electron withdrawing group and Q is a moiety containing a free electron pair positioned three to six atoms from C(=Y2); R2-5 and R7-9 are independently selected

Abstract: Novel S-nitrosothiols derivatives of penicillamine or glutathione, which correspond to following general formula(I) 1

Abstract: A skin care composition comprising. (a) a silicone-containing phase comprising cross-linked polyorganosiloxane polymer and silicone oil, wherein the composition comprises from about 0.1% to about 20% by weight of the combination of cross-linked polyorganosiloxane polymer and silicone oil, (b) from about 0.1% to about 20% by weight of an organic liquid crystal-forming amphiphilic surfactant, and (c) water; wherein the composition is in the form of an oil-in-water emulsion. The compositions of the invention provide improved skin feel, reduced greasiness/stickiness and faster absorption.

Abstract: The invention relates to the field of antiviral agents, and more specifically to antiviral therapy. The invention provides use of at least one compound or mixture of compounds of the general formula or a functional equivalent or pharmaceutically acceptable salt, ester or hydrate thereof for the treatment of a viral infection.

Abstract: The compounds of formula in which the symbols R1, R2, R3 and R4 represent independently from each other a hydrogen atom or a methyl or ethyl group, the symbol X represents an oxygen atom or an alkylene group of formula in which n is an integer from 1 to 3, the symbols R6 and R7 represent each a hydrogen atom or a methyl or ethyl group, and R5 represents an alkyl or alkoxy group from C1 to C4, linear or branched, an alkenyl group from C2 to C4, linear or branched, or a group of formula in which Y has the same meaning as X and R8 is a linear or branched alkyl group from C1 to C4 or a linear or branched alkenyl group from C2 to C4, are novel compounds showing musky odors and which confer musky-velvety, voluminous and very tenacious notes to the products to which they are added.

Abstract: There is described the use of a compound represented by general formulae (I), (II) or (III), for the inhibition of matrix metalloproteinases (MMP), wherein X1 is oxygen or sulfur, R1 is OH, SH, CH2OH, CH2SH or NHOH, R2 is a residue of 2 to 10 hydrocarbon backbone atoms, which binds to the amino acid 161 of HNC, said residue being saturated or unsaturated, linear or branched, and contains preferably homocyclic or heterocyclic structures, X2 is oxygen or sulfur and binds as hydrogen acceptor on amino acid 160 of HNC, Y is a residue which binds to the S1′ pocket of HNC and consists of at least 4 backbone atoms Z1-Z2-Z3-Z4-R3, and R3 is n-propyl, isopropyl, isobutyl or a residue with at least 4 backbone atoms, which is not larger than a tricyclic ring system. These compounds bind to MMPs in a manner different from the mode of binding of the inhibitors of the state of the art.

Abstract: This invention relates to pharmaceutical compositions and methods for treating alopecia and promoting hair growth using small molecule carbamates and ureas.

Abstract: Composition containing at least one aminophenol derivative and a solubilizing compound which is not in the form of vesicles, chosen from: (a) oxyalkylenated fatty acid esters of sorbitan, (b) oxyalkylenated hydrogenated castor oils, and/or (c) oxyalkylenated fatty alcohols. The invention also relates to a process for dissolving at least one aminophenol derivative by mixing it with a solubilizing agent as defined above.

Abstract: Methods of using prostaglandin agonists for the reduction of intraocular pressure, and accordingly glaucoma.

Abstract: The present invention provides a method to control parasitic and saprophagous mites on beneficial insects such as honeybees via the application of a parasiticidally or saprophagouscidally effective amount of a mitochondrial electron transport inhibitor or a pyrimidine compound of formula I.

Abstract: The present invention relates to novel fungicidal two-component compositions based on metalaxyl having an R-enantiomer content of more than 70% by weight as one essential component and a second fungicidal component, for the treatment of phytopathogenic diseases of crop plants, especially phytopathogenic fungi, and to a method of combating phytopathogenic diseases on crop plants. The metalaxyl component is called active ingredient I.

Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; composition comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.

Abstract: There are described new active compound combinations of a compound of the formula (I) 1

Abstract: This invention is a pharmaceutical composition that inhibits the growth of cancers and tumors in mammals, particularly in human and warm blooded animals. The composition contains N-chlorophenylcarbamates and N-chlorophenylthiocarbamates along with a chemotherapeutic agent and optionally a potentiator. A composition for treating viral infections in animals or humans comprising a safe and effective amount of N-chlorophenylcarbamates and the N-chlorophenylthiocarbamates and a potentiator is also disclosed.

Abstract: The invention provides a drug-oligomer conjugate having the following general formula: wherein D is a therapeutic drug moiety; H and H′ are each a hydrophilic moiety, independently selected from the group consisting of straight or branched PEG polymers having from 2 to 130 PEG subunits, and sugars; L is a lipophilic moiety selected from the group consisting of alkyl groups having 2-26 carbon atoms, cholesterol, adamantane and fatty acids; o is a number from 1 to the maximum number of covalent bonding sites on H; m+n+p together have a value of at least one and not exceeding the total number of covalent bonding sites on D for the —H′, —L and —H—L substituents; the H—L bond(s) are hydrolyzable and the D—L′ bond(s), when present, are hydrolyzable; the conjugate being further characterized by one of the following: (i) m is 0 and p is at least 1; (ii) n is 0 and p is at least 1; (iii) m and n are each 0 and p is at least 1; (iv) p is

Abstract: This invention relates to compounds of general formula (I): in which Ar is a group selected from: A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and Y represents carboxy or an acid bioisostere. These compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.

Abstract: Disclosed are novel compounds and novel pharmaceutical compositions for use in medical therapy, as well as intermediates and processes for preparing such compounds. Therapeutic methods for preventing or treating glutamate-related disorders in a mammal and methods to inhibit or prevent glutamate binding in mammalian tissue are also disclosed.

Abstract: Poly(ethylene glycol) carbamate derivatives useful as water-soluble pro-drugs are disclosed. These degradable poly(ethylene glycol) carbamate derivatives also have potential applications in controlled hydrolytic degradation of hydrogels. In such degradable hydrogels, drugs may be either trapped in the gel and released by diffusion as the gel degrades, or they may be covalently bound through hydrolyzable carbamate linkages. Hydrolysis of these carbamate linkages releases the amine drug at a controllable rate as the gel degrades.

Abstract: An insecticidal and miticidal composition is provided which comprises at least one fatty acid ester selected from the group consisting of glycerin monooleate, glycerin monolinolate, glycerin monocaprylate, glycerin mono/dioleate, glycerin di/trioleate, glycerin mono/dilinolate, glycerin mono/diricinoleate, glycerin diacetomonolaurate, sorbitan laurate, sorbitan oleate, diglycerin laurate, diglycerin oleate, diglycerin monolaurate, diglycerin monooleate, tetraglycerin oleate, hexaglycerin laurate, decaglycerin laurate, propylene glycol monolaurate, and propylene glycol monooleate; and a nonionic surfactant. The insecticidal and miticidal composition does not have phytotoxicity but has satisfactory long lasting effects even if it is used in a lower concentration.

Abstract: Disclosed are methods and compositions for regulating the melanin content of mammalian melanocytes; regulating pigmentation in mammalian skin, hair, wool or fur; treating or preventing various skin and proliferative disorders; by administration of various compounds, including alcohols, diols and/or triols and their analogues.

Abstract: There are described a flowable composition for controlling harmful insects and representatives of the order Acarina, comprising at least one pesticidally active compound, one or more signal substances selected from the group consisting of pheromones, kairomones and attractants, a UV absorber or a UV absorber mixture and, if appropriate, one or more additives selected from the group consisting of viscosity-regulating thickeners, fillers, solvents and other formulation auxiliaries,

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: Multi-layer, time release, anti-acne patches and multi-layer, anti-acne patches for the topical application of an anti-acne effective combination of active agents are provided along with a method for making the same. The multi-layer, anti-acne patches contain an anti-acne effective combination of at least two agents selected from the group of an antimicrobial agent, an antiseptic agent, an anti-irritant, a keratolytic agent, a hormone, a hormone agonist and a hormone antagonist. The individual layers of adhesive polymeric matrix material contained in the multi-layer, anti-acne patches provided, may contain identical or disparate combinations of agents constituting the anti-acne effective combination. The multi-layer, anti-acne patches may further contain enhancing agents which improve the efficacy of the anti-acne effective combination present therein.

Abstract: Compounds of formula 1 1

Abstract: A composition comprising a combination of: (a) at least one film-forming polymer; (b) at least one citric acid ester of formula (I): in which: R1, R2 and R3 independently represent H or a saturated or unsaturated, linear or branched C1-C30 alkyl chain or a saturated or unsaturated cyclic C3-C30 alkyl chain, wherein at least one of R1, R2 and R3 is not a hydrogen atom, R4 represents a hydrogen atom or an R′4—CO— group in which R′4 represents a saturated or unsaturated, linear or branched C1-C8 alkyl group or a saturated or unsaturated cyclic C3-C8 alkyl group; and (c) at least one compound of formula (II): in which &agr; represents an ortho or para position of the phenyl group, and R and R′ independently represent a hydrogen atom or a C1-C6 alkyl group, and cosmetic and/or dermatological compositions comprising such a combination.

Abstract: A (poly)alkylene glycol higher alkyl ether derivative composition characterized by comprising 30-90 mol. % of (B1) (poly)alkylene glycol higher alkyl ether derivative and 70-10 mol.

Abstract: The present invention relates to the use of small organic compounds acting as opioid receptor ligands for the treatment of vasomotor disturbances. In particular the present invention relates to the use of triaza-spiro compounds of formula wherein R1, R2, R3, R4, R5, z and n are defined in the specification, for the treatment of migraine, non-insulin dependent diabetes mellitus (type II diabetes), sepsis, inflammation, incontinence and/or vasomotor disturbances, in particular the peripheral vasomotor effects known as hot flushes or hot flashes.

Abstract: The claimed invention pertains to methods for treating a patient who is at risk for a vascular (e.g., cardiovascular, cerebrovascular) event comprising administering to the patient an effective amount of a lipid-modifying drug. The claimed methods are particularly effective in patients having a lipid profile comprising a low Low Density Lipoprotein and a low High Density Lipoprotein.

Abstract: (4-oxy-3-(aryl)phenyl)pyridine compounds, in free or acid addition salt form, are useful as pharmaceuticals for treatment and prophylaxis of inflammation, particularly inflammatory or obstructive diseases of the airways, e.g. for asthma therapy. Preferred compounds are novel biphenyl pyridines, biphenyl benzamides and biphenyl phenylcarboxy compounds. The compounds are selective inhibitors of PDE 4 isoenzyme activity and also act to down regulate or inhibit TNF-&agr; release.

Abstract: This invention relates to a single phase emulsifiable concentrate composition comprising (a) between about 0.05 and about 25 wt. % of a biologically, fungicidally and/or herbicidally active aza compound; (b) between about 2 and about 40 wt. % of a lactam selected from the group of N-methyl pyrrolidone, N-methyl caprolactam, a C8 to C18 alkyl pyrrolidone, a C8 to C18 caprolactam and a mixture thereof; (c) between about 2 and about 20 wt. % of a moisture scavenging agent selected from the group consisting of a liquid molecularly hindered carbodiimide, a molecular sieve or a mixture thereof and (d) between about 10 and about 80 wt. % of a mixture of at least two non-ionic surfactants having an overall hydrophilic/lipophilic balance (HLB) above 7. The invention also relates to the stable oil-in-water (o/w) miniemulsions prepared from the above by dilution to between about 40 and about 99.99 wt. % water for a “pour on”, dip or spray solution useful in the treatment of animals or plants.

Abstract: The present invention provides novel carbamate-based cationic lipids of the general structure: or a salt, or solvate, or enantiomers thereof, wherein (a) R1 is a lipophilic moiety; (b) R2 is a positively charged moiety; (c) n is an integer from 1 to 8; (d) X is an anion or polyanion; and (e) m is an integer from 0 to a number equivalent to the positive charge(s) present on the lipid. The present invention further provides compositions of these lipids with polyanionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions, and a kit for preparing the same.

Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

Abstract: An ascorbic acid-based composition and related method for the treatment of aging or photo-damaged skin is disclosed. The composition includes water and ascorbic acid, at least a portion of which has generally been pretreated by being dissolved under relatively high temperature and concentration conditions. The composition typically includes at least about 5.0% (w/v) ascorbic acid and may advantageously be formulated to have a pH above 3.5. Generally, the composition also includes non-toxic zinc salt, tyrosine compound, and/or pharmaceutically acceptable carrier. In addition, the composition may include an anti-inflammatory compound, such as aminosugar and/or sulfur-containing anti-inflammatory compound. The topical composition may be in the form of a serum, a hydrophilic lotion, an ointment, a cream, or a gel.

Abstract: The sunscreen or makeup may be applied to a person who is wet, or even underwater, yet it will provide the fill efficacy which it would have had had it been applied to the person when their skin was dry. In addition, it will be effective from the time that it is first applied, so no waiting period is required, as was the case for the so-called “water resistant” and “waterproof” sunscreens of the prior art. A series of test procedures which illustrate the efficacy of the “wet-appliable” sunscreens of the present invention are disclosed.

Abstract: A composition for cosmetics use which comprises a lysophospholipid mixture, wherein 30 mol % or more of fatty acids bonded to said lysophospholipid mixture are monoenoic fatty acids; and a cosmetic composition which comprises a lysophospholipid mixture and a cosmetically acceptable carrier, wherein 30 mol % or more of fatty acids bonded to said lysophospholipid mixture are monoenoic fatty acids. The cosmetic composition having such a lysophospholipid mixture has high storage stability and is excellent in feeling upon use.

Abstract: The invention describes novel compounds derived from pentaerythritol of general formula I, XIV, XVI, XIX and XXII, the substituents being as defined in the description, which can be used as pharmaceutical active substances, especially for the treatment of cardiovascular diseases.

Abstract: Disclosed herein are cardenolides and related compounds covalently linked to phosphocholine moieties and pharmaceutical formulations comprising such compounds. Also disclosed herein are methods for treating hypertension, premenstrual syndrome (PMS), preeclampsia and polycystic kidney disease using the compounds.

Abstract: The present invention concerns new immunosuppressive and antiviral pharmaceutical agents using lipid alcohols of the general formulae I and II in which R1 represents a straight-chained or branched, saturated or unsaturated alkyl chain with 1-30 carbon atoms which can optionally be substituted once or several times by halogen, C1-C6 alkoxy, C1-C6 alkylmercapto, C1-C6 alkoxycarbonyl, carboxy, C1-C6 alkylsulfinyl or C1-C6 alkylsulfonyl groups, R2 represents hydrogen, a straight-chained or branched, saturated or unsaturated alkyl chain with 1-20 carbon atoms which can optionally be substituted once or several times by halogen, C1-C6 alkoxy, C1-C6 alkylmercapto, C1-C6 alkoxycarbonyl or C1-C6 alkylsulfonyl groups, X represents a valency dash, oxicarbonyl, carbonyloxy, amidocarbonyl, carbonylamido, oxygen, sulphur, a sulfinyl or sulfonyl group Y represents a valency dash, oxicarbonyl, carbonyloxy, amidocarbonyl, carbonylamido, oxygen, sulphur, a sulfinyl or sulfonyl group n represents an integ

Abstract: A new method of eradicating an existing infection of powdery mildew on plants using a wax ester emulsion is provided wherein the wax ester emulsion is comprised of wax esters, which are derived from esterification of monoethylenic acids and monoethylenic alcohols having between 18 and 24 carbons, and surfactant at a concentration of between 1% v/v and 10% v/v of the total wax ester component.

Abstract: A pesticidal device which comprises a pesticidal ingredient being volatile at room temperature (e.g. 1-ethynyl-2-methyl-2-pentenyl 3-(2-chloro-2-fluorovinyl)-2,2-dimethylcyclopropanecarboxylate, 1-ethynyl-2-fluoro-2-pentenyl 3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropanecarboxylate), 2,3,5,6-tetrafluoro-4-methylbenzyl 3-(2-methyl-1-propenyl)-2,2-dimethylcyclopropanecarboxylate, 2,3,5,6-tetrafluoro-4-methylbenzyl 3-(2-chloro-2-fluorovinyl)-2,2-dimethylcyclopropanecarboxylate, 2,3,5,6-tetrafluoro-4-methylbenzyl 3-(1-propenyl)-2,2-dimethylcyclopropanecarboxylate) is supported on balloon material, and a method for controlling pests by using the pesticidal device.

Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.

Abstract: 6-dimethylaminomethyl-1-phenyl-cyclohexane compounds, methods of preparing them and the use of these compounds in drugs are described.