Abstract: Squaric acid Derivatives of formula (1) are described: wherein R1 is an integrin binding group; R2 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic chain; R3 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group: and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune of inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.

Abstract: The invention relates to novel heteroethynylenic compounds having the general formula (I): 1

Abstract: Novel imides are inhibitors of tumor necrosis factor alpha and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is (R)-2 -Phthalimido-3-(3′,4′-dimethoxyphenyl)propane.

Abstract: A pharmaceutical composition comprising idebenone in synergistic combination with nimodipine for the treatment of cognitive disorders of cerebrovascular origin.

Abstract: A method of sensitizing tumor cells to radiation thereapy, chemotherapy and immunomodulatory thereapy, comprising the step of exposing the tumor cell to an effective amount of at least one monoterpene or sesquiterpene and treating the tumor cell is disclosed.

Abstract: A method of controlling target aquatic microorganism pest populations by exposing the target population to an effective amount of an aquacidal compound. The aquacidal compounds are selected from the group consisting of quinones, anthraquinones, naphthalenediones, quinine, warfarin, coumarins, amphotalide, cyclohexadiene-1,4-dione, phenidione, pirdone, sodium rhodizonate, apirulosin and thymoquinone. The method is particularly effective for treating ballast water of ships or other enclosed volumes of water subject to transport between or among geographic areas to control the relocation of plants, toxic bacteria, and animals contained in the water.

Abstract: A method of controlling target aquatic microorganism pest populations by exposing the target population to a toxic amount of an aquacidal compound comprising an anthraquinone. The method is particularly effective for treating ballast water of ships or other enclosed volumes of water subject to transport between or among geographic areas to control the relocation of plants, toxic bacteria, and animals contained in the water.

Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.

Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z),14(Z)-dienoic acid and 20-,21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z),15(Z)-dienoic acid.

Abstract: A method is described for using a combination of ubiquinone 10 and succinic acid in the treatment of human patients afflicted with fibromyalgia to alleviate one or more symptoms associated with that disease state. Fibromyalgia positive patients treated buccally, sublingually or by oral ingestion administration of ubiquinone 10 and succinic acid enjoy a reduction in clinical symptoms of the disease.

Abstract: The present invention provides new methods for the treatment of viral hepatitis C involving the administration of vitamin E and other compounds with antioxidant properties. Treatment with high doses of vitamin E is effective in treating chronic hepatitis C in patients refractory to interferon. In addition, new methods are described for the treatment of hepatic fibrosis and hepatic conditions manifesting hepatic fibrosis involving the administration of butylated hydroxytoluene and a metabolite of pentoxifylline, 1-[3-carboxypropyl]-3, 7-dimethylxanthine. Furthermore, new methods are described for the treatment and prevention of hepatic disorders involving the use of 2,6-di-tert-butylphenol derivatives.

Abstract: A method is described for using a combination of ubiquinone 10 and succinic acid in the treatment of human patients afflicted with fibromyalgia to alleviate one or more symptoms associated with that disease state. Fibromyalgia positive patients treated buccally, sublingually or by oral ingestion administration of ubiquinone 10 and succinic acid enjoy a reduction in clinical symptoms of the disease.

Abstract: 4-phenyl-4-oxo-butanoic acid derivatives for use in the treatment of the human or animal body by therepy; particularly as kynurenine-3-hydroxylase inhibitors, in the prevention and/or treatment of a neurodegenerative disease wherein the inhibition of such an enyzme is needed. The present invention further comprises a selected class of the above mentioned 4-phenyl-4-oxo-butanoic acid derivatives, their pharmaceutically acceptable salts, a process for their preparation and pharmaceutical compositions containing them.

Abstract: A method for increasing the effectiveness of a biocide is described. In the method, at least one biocide and at least one diethanolamide are applied to a substrate or aqueous system subject to the growth of microorganisms. The diethanolamide is applied in an amount effective to increase the biocidal activity of the biocide. Biocidal compositions are described where the biocide and the diethanolamide are present in a combined amount effective to control the growth of at least one microorganism. Methods for controlling the growth of microorganisms on various substrates and in various aqueous systems are also described. The combination of the biocide and the diethanolamide is particularly useful as a biocide in the leather industry, the lumber industry, the papermaking industry, the textile industry, the agricultural industry, and the coating industry, as well as in industrial process waters.

Abstract: The present invention relates to compounds that are two-part molecules, and compositions containing such compounds, in which one part is designed to become covalently bonded to the skin (bonding agent) and the other part (a characteristic use agent) is designed to impart some characteristic use, such as emolliency, moisturizing effect, anti-acne, anti-wrinkle, anti-pain, antimicrobial, antifungal, antiviral, anti-irritation, skin tanning and skin lightening effects, extended protection of the skin (e.g., from ultraviolet light, by incorporation of a sunscreen component; from toxic and/or irritating substances; from insects and skin parasites, by incorporation of insecticides and/or insect repellants; from free radicals or other agents, as in aging, by incorporation of antioxidants), or dyeing of hair, skin nails, wool or fuir. The covalently bonded part may also be useful to impart skin strengthening effect (e.g., from shear forces) or as wound healing agents.

Abstract: A compound of the formula: wherein R1 represents a lower alkyl; R2 represents H, an optionally substituted alkyl or an optionally substituted alkenyl; R3 and R4 each represents an optionally substituted lower alkyl or a lower alkoxy, or R3 and R4 form, taken together, an optionally substituted butadienylene; and X1 and X2 each represents an optionally esterified or etherified hydroxy, or a salt thereof is useful for protecting cells from the cytotoxicity of &bgr;-amyloid protein.

Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.

Abstract: The invention discloses ketones of formula I: wherein, Y is an optionally substituted alkyl, cycloalkyl, or cycloalkylalkyl, wherein each alkyl group is straight or branched and each alkyl and cycloalkyl group is saturated or unsaturated; R1 is hydrogen or a C1-6 alkyl group that is substituted, saturated or unsaturated, straight or branched; A is a chromophoric substituted aromatic ring or ring system; n is an integer; and with the proviso that formula I is not 2-ethoxy-1-phenyl-ethanone. These compositions are useful for the delivery of organoleptic compounds, especially of flavors, fragrances, masking agents and antimicrobial compounds.

Abstract: This invention relates to a process for separating one or more cyclic products from a reaction product fluid comprising one or more cyclic reactants, a metal-organophosphorus ligand complex catalyst, optionally free organophosphorus ligand, a non-polar solvent and said one or more cyclic products, wherein said process comprises: (1) reacting said one or more cyclic reactants in the presence of said metal-organophosphorus ligand complex catalyst, optionally free organophosphorus ligand and non-polar solvent to form a multiphase reaction product fluid; and (2) separating said multiphase reaction product fluid to obtain a non-polar phase comprising said one or more cyclic reactants, metal-organophosphorus ligand complex catalyst, optionally free organophosphorus ligand and non-polar solvent and a polar phase comprising said one or more cyclic products.

Abstract: A method of inhibiting the growth of tumor cells is disclosed. In one embodiment, this method comprises the step of exposing tumor cells to an effective amount of a composition comprising at least two compounds selected from the group consisting of tocotrienols, statins and ionones.

Abstract: A method of treating or preventing a disorder resulting from a mitochondr dysfunction induced by an iron overload including Friedreich Ataxia, hypertrophic cardiomyopathy, Hallervorden-Spatz disease, sideroblastic anemia by administering an effective amount of an ubiquinone derivative such as idebenone, decylubiquiqnone, coenzyme Q2, coenzyme Q4, and coenzyme Q6, either alone or in conjunction with a second therapeutic agent or a non-reducing antioxidant.

Abstract: The present invention relates to a foam composition for killing dust mites comprising an acaricidal agent, polymer, ether solvent, perfume, surfactant and water.

Abstract: This invention is a novel treatment for sexual dysfunctions by administering to a subject exhibiting a sexual dysfunction compounds that upmodulate the AMPA receptor. Methods and compositions for treating sexual dysfunction are provided. Kits containing the compositions in appropriate form for administration are also provided.

Abstract: The present invention relates to a foam composition for killing dust mites comprising an acaricidal agent, polymer, ether solvent, perfume, surfactant and water.

Abstract: A method of preventing and treating a viral condition caused by an enveloped virus is described, comprising using a therapeutically effective amount of a compound selected from the group consisting of a substituted hydroquinone and the corresponding benzoquinone, wherein said hydroquinone comprises a 2-R.sup.1, 3-R.sup.2 -1,4-hydroquinone where at least one of R.sup.1 and R.sup.2 include a carbon linkage to the benzene ring of the hydroquinone. Particularly useful compounds include 5,8-dihydro-5,8-methano-1,4-naphthalenediol, 1,4-naphthoquinone, 3', 6'-dihydroxybenzo-norbornane, tert-butylhydroquinone, other diols, e.g. 1,5-naphthalenediol, and alkylated diols, e.g. 4-methoxy-1-naphthol.

Abstract: A compound comprising a non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO group, a pharmaceutical composition including the compounds and methods of treatment of pain and/or inflammation using the compounds and compositions are disclosed. Also disclosed is a composition comprising a non-steroidal antiinflammatory agent and a compound that donates, transfers or releases nitric oxide.

Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.

Abstract: The present invention relates to healthy foods and cosmetics. More particularly, it relates to healthy foods and cosmetics containing a polyisoprenylated benzophenone derivatives as effective ingredients and having a variety of functions for maintaining health such as anti-ulcer activity, the Maillard reaction inhibiting activity, anti-oxidation activity, reactive oxygen species scavenging activity, and anti-tumor promotion activity.

Abstract: Topically applicable, stable, UV-photoprotective cosmetic/dermatological compositions well suited for the photoprotection of human skin and/or hair against the damaging effects of UV-A and UV-B irradiation, comprise (a) an effective UV-photoprotecting amount of at least one dibenzoylmethane UV-sunscreen compound and (b) an effective dibenzoylmethane compound (a) photostabilizing amount of at least one benzalmalonate silane having the structural formula (I): ##STR1##

Abstract: The present invention pertains generally to the field of Public Health, including the prevention and treatment of coronary heart disease which is currently the first cause of death in the American population. More specifically, the present invention concerns a total modular system of multivitamin and mineral supplementation composed of 7 distinct modules for improving public health by insuring adequate intake of micronutrients needed for disease prevention and protection against nutritional losses and deficiencies due to, for example, lifestyle factors and common inadequate dietary patterns. A module, as used herein throughout, is defined as a separate and distinct combination of vitamin-mineral and other health promoting compounds which are directed to specific target populations. The formulations of the present invention which, when combined in one capsule or tablet or as separate modules, exert a joint and enhancing effect on the major pathogenetic factors involved in the atherosclerotic process.

Abstract: The present invention are for emulsion compositions and the process for making such compositions containing biological and cosmetic actives subject to hydrolysis of actives during processing and storage of the emulsion composition. Buffers are incorporated into emulsion at a point wherein the acidic and basic conditions created during processing have little effect on compositions.

Abstract: The present invention provides illudin analogs of the general formula (I): ##STR1## where R.sub.1 is (CH.sub.2).sub.n --X--Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C.sub.1 -C.sub.8)alkyl, (C.sub.6 -C.sub.10)aryl, (C.sub.6 -C.sub.10)aryl(C.sub.1 -C.sub.4)alkyl or cyclo(C.sub.3 -C.sub.6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; R.sub.2 is absent; or R.sub.1 and R.sub.2 together comprise a 5-7 membered cyclic ring;R.sub.3 is (C.sub.1 -C.sub.4)alkyl or H; R.sub.4 is H, SCH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4)alkyl, O--(C.sub.5 --C.sub.12)aryl or --S--(C.sub.5 -C.sub.12)aryl; R.sub.5 is H, OH or absent; R.sub.6 is (C.sub.1 -C.sub.4)alkyl or absent; R.sub.7 is OH or OSi((C.sub.1 -C.sub.4)alkyl).sub.3 ; orR.sub.6 and R.sub.7 together are ethylenedioxy;R.sub.8 is optionally substituted (C.sub.1 -C.sub.4)alkyl; andthe bonds represented by -- are individually present or absent.

Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor .alpha., nuclear factor .kappa.B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.

Abstract: A pharmaceutical composition comprising idebenone of the present invention is useful for prevention of the progression of dementia.

Abstract: Use of topical formulations having a content of one or more compounds from the group consisting of ubiquinones and derivatives thereof for treatment of senile xerosis and/or exogenous ageing of the skin.

Abstract: The present invention relates to a foam composition for killing dust mites comprising an acaricidal agent, polymer, ether solvent, perfume, surfactant and water.

Abstract: Substituted triols are prepared by reducing appropriately substituted carboxylic esters. The substituted triols can be used as active substances in medicaments.

Abstract: Disclosed is a method of inhibiting the growth of marine organisms on a marine structure, by applying diphenyldiones. These compounds may be directly incorporated into the marine structure during manufacture, directly applied to the structure, or applied to the structure by means of a coating.

Abstract: A class of 1,2-diarylcyclopentenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from alkyl, hydrido, hydroxyalkyl, halo, haloalkyl, alkoxycarbonyl and carboxyl; wherein R.sup.5 is selected from alkylsulfonyl, haloalkylsulfonyl and sulfamyl; and wherein B is phenyl or pyridyl, wherein B is optionally substituted at a substitutable position with alkyl, halo, alkylthio, cyano, haloalkyl, alkoxy, hydroxyalkyl and alkoxyalkyl; or a pharmaceutically-acceptable salt thereof.

Abstract: Fouling of marine structures such as boats by shell bearing sea animals which attach themselves to such structures, such as barnacles, is inhibited by coatings containing lipid soluble, non-toxic, biodegradable substances which prevent the animals from sitting down on the structures. These substances attack the nervous system of the barnacle, neutralize the glue extruded by the barnacle, and otherwise prevent the barnacles from attaching themselves to surfaces immersed in the aqueous marine environment while being benign to the environment. A preferred inhibitor is pepper containing capsaicin. The inhibitor is incorporated into standard marine paints, impregnants, varnishes and the like.

Abstract: This invention relates to benzyl and naphthalenylmethyl thiophenones and cyclopentenones, some of which are novel, which have oral antihyperglycemic activity in diabetic mice, a genetic animal model of non-insulin dependent diabetes mellitus. These compounds are represented by the formula ##STR1## wherein: R.sup.2 and R.sup.3 are independently selected from hydrogen, C.sub.1-6 alkyl, halogen, C.sub.1-6 alkoxy, thio-C.sub.1-6 alkyl, or trifluoromethyl or R.sup.2 together with R.sup.3 forms a benzo ring fused to the phenyl ring and optionally substituted with one or two substituents independently selected from C.sub.1-6 alkyl, halogen, C.sub.1-6 alkoxy, thio-C.sub.1-6 alkyl, or trifluoromethyl;R.sup.1 is selected from hydrogen, C.sub.1-6 alkyl, halogen, C.sub.1-6 alkoxy, thio-C.sub.1-6 alkyl, or trifluoromethyl; andR.sup.4 is selected from the group consisting of: ##STR2## wherein R.sup.5 is H or C.sub.1-6 alkyl or a pharmaceutically acceptable salt thereof.

Abstract: This invention relates to ortho substituted phenyl compounds as inhibitors of prostaglandin synthase, to pharmaceutical compositions comprising such compounds and to methods of using such compounds as antiinflammatory and antipyretic agents.

Abstract: A method has been discovered for repelling ants by treating objects or areas with effective amounts of compositions that include (a) one or more C.sub.6 to C.sub.8 carboxylic acids; (b) one or more C.sub.6 to C.sub.14 alcohols; (c) one or more esters which are reaction products of (a) and (b) or an ester which is a reaction product of the repellents and other carboxylic acids or alcohols; (d) one or more C.sub.6 to C.sub.11 carboxylic acid esters; (e) one or more C.sub.6 to C.sub.14 ketones; or (f) mixtures thereof.

Abstract: A cosmetic treatment for inducing upper and lower lip augmentation in humans, wherein an active ingredient encouraging vasodilatation, preferably an ultra highly diluted homeopathic, ultra highly diluted element, local irritant or direct local vasodilator or a combination of two or more is administered by topical application or sublingually or gum by chewing. The vasodilators singly or in combinations of preferably ultra highly diluted elements, homeopathics, local irritant or vasodilators are diluted to preferably ten to fifteen percent for topical administration in a cosmetic cream or cosmetic gel or oral sublingual drops diluted in a 2% alcohol base or a five percent fructose-coated chewing gum. The treatment results in a significant non-invasive augmentation of both the upper and lower lip that onsets within a few moments and is effective for a duration on an average of four and one half hours.

Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: The subject invention relates to pharmaceutical compositions comprising a safe and effective amount of a compound having the structure: ##STR1## wherein n is 3 or 4; each R is independently alkyl or alkoxy; and R' is C.sub.1 C.sub.20 alkyl; and a pharmaceutically-acceptable topical carrier.The subject invention also relates to methods for preventing damage to skin, without markedly sensitizing the skin, by topically applying a safe and effective amount of such compounds to the skin.

Abstract: Known and new catechol derivates may be used as medicinal antioxidants in the prevention or treatment of tissue damage induced by lipid peroxidation. The conditions and diseases to be treated are for example heart disease, rheumatoid arthritis, cancer, inflammatory disease, a rejection reaction in organ transplants, ischemia, cancer and aging.

Abstract: The present invention relates to derivatives of cyclic phenolic thioethers of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, which are inhibitors or stimulators of superoxide generation, and which may also inhibit cyclooxygenase and/or 5-lipoxygenase, to pharmaceutical compositions containing one or more of these compounds in combination with a pharmaceutically-acceptable carrier, and to medical methods of treatment employing these compounds.

Abstract: Amino derivatives represented by the following general formula (1): ##STR1## and external skin care preparations containing such an amide derivative, are useful for preventing or curing skin roughness. Intermediates useful for the preparation of such amides are also disclosed.

Abstract: A therapeutic method is provided to inhibit tumor cell growth in a subject in need of said therapy is provided, comprising parenterally administering a therapeutic amount of a compound in a pharmaceutically acceptable carrier, wherein said compound has the structure: ##STR1## wherein R is selected from the group consisting of: ##STR2## and wherein said tumor cell is sensitive to inhibition by said compound and is selected from the group consisting of a myeloid leukemia cell, a T-cell leukemia cell, a lung carcinoma cell, an ovarian carcinoma cell, and a breast carcinoma cell.