Abstract: The present invention relates to the discovery of a method to provide stabilized transglutaminase 1 enzyme, involucrin, and other molecules necessary for the assembly of the cell envelope to skin cells. Novel biological tools, prophylactics, therapeutics, cosmetics, and methods of use of the foregoing for study, prevention, and treatment of skin disorders are also disclosed.

Abstract: Novel ceramide compounds, compositions containing them and the use of these compounds, in particular for strengthening the lipid barrier of the epidermis.

Abstract: The present invention provides an aliphatic compound represented by the following formula (I) or pharmacologically acceptable salts thereof: where n denotes an integer of 1 to 11, and 1 denotes an integer of 1 to 16, the aliphatic compound being an optical isomer of the (2R,3S,2′S) configuration when the 8-position thereof is a double bond, or an optical isomer of the (2S,3R,2′RS) configuration when the 8-position is a single bond; methods for producing the compound or pharmacologically acceptable salts thereof; and uses of the compound in the treatment of cardiovascular diseases (e.g. arteriosclerosis, cardiac diseases), cancer, rheumatism, diabetic retinopathy, and respiratory diseases.

Abstract: A drug complex useful as a DDS compound, which is represented by the following formula: A-R—NH—Y—CH2—O—CO-Q, wherein A is a polymer as a drug carrier; R is a spacer, wherein the spacer is an amino acid or an oligopeptide comprising 2 to 8 amino acids; Y is phenylene group which may be substituted; and Q is a residue of a drug compound such as antineoplastic agents. The complex provides rapid and site-selective release of a drug compound such as antineoplastic or anti-inflammatory agents and surely exhibits expected efficacy.

Abstract: Described in the present invention are a dispersion which comprises, as a dispersoid, (a) 5 to 40 wt. % of an amphipatic lipid containing, in the molecule thereof, at least one hydroxy and amide group, and (b) 2 to 55 wt. % of a surfactant in an aqueous medium; a washing-away type cosmetic composition comprising the dispersion; and a washing-away type cosmetic composition comprising (A) 0.01 to 10 wt. % of an amphipatic lipid which contains, in the molecule thereof, at least one hydroxy and amide group and having a melting point not less than 30° C. and (B) 5 to 95 wt. % of a surfactant. The dispersion according to the present invention is useful as a component of a washing-away type cosmetic composition having both an emulsion-like or pearl-lustrous appearance and low skin irritation.

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; 1

Abstract: Methods and kits for regulating arterial microvascular tone in which a COX-2 inhibitor and a cannabinoid receptor agonist are co-administered to a subject.

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

Abstract: The present invention relates to compounds of the formula I in which A1, A2, R2 and R3 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular disorders such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance. The invention relates to the use of compounds of the formula I for the therapy and prophylaxis of the designated disease states and for the production of pharmaceuticals therefor, novel compounds of the formula I, pharmaceutical preparations comprising them and processes for their preparation.

Abstract: N-(imino)amines and their preparation and their use as NO synthase inhibitors and selective or non-selective traps for a reactive oxygen species.

Abstract: The present invention relates to the use of compounds of formula (I) 1

Abstract: The present invention relates to the use of compounds of formula (I) 1

Abstract: A compound of formula (I) is provided which is able to interact with &bgr;-catenin/TCF-4 binding site, having a structure essentially equivalent to a pharmacophore (IA), as herein described.

Abstract: Compounds having quinone and quinone analogs useful for pharmaceutical preparations have now been found which inhibit cysteine proteases, in particular, caspases and 3C-cysteine proteases. The cysteine protease inhibitors of the present invention can be identified by their mode of action in disrupting the ability of cysteine proteases and, in particular, caspases to cleave a peptide chain. These compounds are useful in inhibiting cysteine protease or cysteine protease-like proteins and for treating infections diseases or physiopathological diseases or disorders attributed to the presence of excessive or insufficient levels of cysteine proteases.

Abstract: Disclosed are compounds having the formula: where R1=H, C1-C6 alkyl, cycloalkyl, R2=H, C1-C6 alkyl, cycloalkyl W=CnH2n-m—NH (n=1-6, m=0, 2, or 4), Z=CONR8(CH2)n, CONR8(CH2)nCO, P(CH3)OCHR8OCOR9, SO2, SO2(CH2)n, SO2(CH2)nCO, SO2NR8(CH2)n, SO2NR8(CH2)nCO, n=1-4 R4=H, (CH2)nOH, (CH2)nOCOR10, (CH2)nNR10R11, (CH2)nCONR10R11, n=0-4 R5=H, (CH2)nNR12R13, n=0-4 R6=H, (CH2)nNR14R15, n=0-4 R7=H, C1-C6 alkyl, cycloalkyl; R8=H, C1-C6 alkyl, cycloalkyl; R9=H, C1-C6 alkyl, cycloalkyl; R10=H, C1-C6 alkyl, cycloalkyl; R11=H, C1-C6 alkyl, cycloalkyl; R12=H, C1-C6 alkyl, cycloalkyl; R13=H, C1-C6 alkyl, cycloalkyl; R14=H, C1-C6 alkyl, cycloalkyl; R15=H, C1-C6 alkyl, cycloalkyl Dashed lines: optional; conformational constraint by (CH2)n, n=1-3, R′=H or O(═) as well as pharmaceuticals c

Abstract: A prodrug composition containing a cinnamate moiety and a biologically active molecule moiety which can be released by hydrolysis or activated by light is disclosed. The cinnamate moiety can have substituents of various electronically donating or electronically withdrawing groups to modify the cinnamate moiety's electric properties as well as photo reactivities for the purpose of achieving a proper hydrolysis rate of the acyl bond between the biologically active molecule moiety and the cinnamic acid backbone. The biologically active molecule can be any biologically active agent or diagnostic, for example, a chemotherapeutic such as a paclitaxel, campotothecin, doxorubicin, amethopterin, etoposide, or fluconazole. The prodrug composition can be modified to add a carrier moiety on the prodrug composition for targeting or to facilitate uptake of the drug. The prodrug compositions can be activated with an energy source to release the drug at the desired site.

Abstract: Compounds are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.

Abstract: The present invention describes rapid noninvasive methods for measuring vasodilation or changes in blood flow in a patient following administration of at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent. The method comprises the administration of at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent to the patient followed by monitoring the temperature change of an area of interest using infrared thermography.

Abstract: A cell adhesion inhibitor of the general formula:

Abstract: Compounds of general formula (I), wherein R1, R2, R3, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.

Abstract: The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxycyclopentyl(enyl)]heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.

Abstract: Compounds of formula I: 1

Abstract: The present invention relates to solid phase or solution phase combinatorial libraries of autoinducer analogs. The present invention also relates to autoinducer agonists and antagonists. In addition, the present invention relates to methods for identifying autoinducer agonists and antagonists, as well as methods for regulating the activity of an autoinducer receptor, regulating biofilm formation, regulating growth or virulence of an organism in a subject, inhibiting the quorum sensing mechanism of an organism, and treating an infection in a subject caused by an organism possessing a quorum sensing mechanism which use the autoinducer analogs of the present invention.

Abstract: The present application describes modulators of MCP-1 of formula (I): 1

Abstract: The invention provides novel &bgr;2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with &bgr;2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: The present invention relates to the use of an amino compound, which is an esteramine or an amidoamine surfactant with improved biodegradability, as an adjuvant for agrochemically active compounds such as pesticides or fertilizers. The adjuvant has Formula (I) where R1 is an aliphatic group containing 7-22 carbon atoms; EO is an ethyleneoxy group; Y is 0 or NH; R2 and R3 is independently CH2CH2OH or an alkyl group with 1-5 carbon atoms, preferably 1-3 carbon atoms; n is a number between 0-10; x is a number 0-1 provided that when Y is O, then x is 1, and when Y is NH, then x is O; and m is a number 2-6, preferably 2-3, provided that when Y is NH, then m is 3-6, preferably 3; or an adduct obtained by reacting one mole of the compound with 1-5 moles of an alkylene oxide having 2-3 carbon atoms.

Abstract: The present invention provides a therapeutic agent for bladder hypersensitivity comprising, as an active ingredient, a tricyclic compound represented by formula (I): 1

Abstract: The present invention provides a visual function disorder improving agent containing a compound having Rho kinase inhibitory activity, particularly (R)-(+)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)-4-(1-aminoethyl)benzamide, as an effective component. This agent has axon of the retinal ganglion cellal extension promoting action and optic nerve cell regeneration promoting action, and is useful for the treatment of a visual function disorder associated with various eye diseases caused by damage, defects, degeneration and the like in the retinal or optic nerve.

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound which is a EP4 agonist.

Abstract: Methods for inhibiting cancer, scar formation, disrupting the cellular cytoskeleton, and conferring resistance from infection are disclosed. Such methods comprise the administration of oleuropein and/or the products of its hydrolysis in therapeutically effective amounts. To that end, a variety of pharmaceutical formulations and routes or administration are disclosed and may be utilized to treat a wide variety of diseases.

Abstract: Methods of treating a bacterial infection and of killing or inhibiting bacteria are disclosed. The methods use derivatives of triterpenes that are abundant in birch bark and other plants. The triterpenes include betulin, allobetulin, and lupeol.

Abstract: Analogs related to oleamide are employed for potentiating the 5-HT2A and 5-HT1A responses to serotonin (5-HT). With respect to the potentiation of the 5-HT2A receptor response, it is disclosed that, of the naturally occurring fatty acids, the primary amide of oleic acid (oleamide) is the most effective potentiating agent of serotonin and that the potentiating activity of oleamide analogs is highly dependent upon their structural features. In particular, the presence, position, and stereochemistry of the 9-cis double bond is required and even subtle structural variations reduce or eliminate activity. Secondary or tertiary amides may replace the primary amide but follow a well-defined relationship requiring small amide substituents suggesting that the carboxamide serves as a hydrogen bond acceptor but not donor. Alternative modifications at the carboxamide as well as modifications of the methyl terminus or the hydrocarbon region spanning the carboxamide and double bond typically eliminate activity.

Abstract: Disclosed are retiferol derivatives of formula (I): wherein X is >C═CH2 or —CH2—; Y and Z are independently of each other hydrogen, fluorine or hydroxy; A is —O(CH2)3—, —(CH2)2-(1,2-C6H4)—, —CH═CH—(1,2-C6H4)—, —C═C—(1,2C6H4)—, —(CH2)2—CO—, —CH2—O—CO—, —CH2NHCO—, or —CH2NHCOCH2—; R1 is C1-C5-alkyl; R2 and R3 are independently of each other alkyl or perfluoroalkyl; and R4 is hydrogen, hydroxy, C1-C5-alkyl or C1-C5-alkyl or C1-C5-alkoxy; the use of such compounds to treat or present hyperproliferative skin diseases such as psoriasis, basal cell carcinomas, disorders of keratinization and keratosis; neoplastic diseases; disorders of the sebaceous glands such as acne and seborrhoic dermatitis; the use of these compounds in reversing the conditions associated with photodamage, particularly for the oral or topical treatment of the skin damaged through sun exposur

Abstract: The present invention relates to the use of compounds of formula (I) 1

Abstract: The present disclosure describes novel compounds of formula (A), wherein R1-R12, X and Y have the meanings given in the specification and compositions containing them which are particularly useful for treating hair loss in mammals, including arresting and/or reversing hair loss and promoting hair growth. The compounds described herein are cardiac-sparing.

Abstract: The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxy-cyclopentyl(enyl)] heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.

Abstract: An enhancer composition for agricultural chemicals which can enhance the effectiveness of an agricultural chemical without causing any phytotoxicity to various crops, which comprises at least one nitrogen-containing compound selected from the group consisting of a tertiary amine, a tertiary amine salt and a quaternary ammonium salt and a chelating agent, wherein the content of the chelating agent ranges from 0.01 to 30 mol per mol of the nitrogen-containing compound.

Abstract: Methods for inhibiting angiogensis are disclosed the comprise administering oleouropein and/or the products of its hydrolysis in therapeutically effective amounts. The methods and compositions of the present invention are particularly effective in inhibiting the vascularization of endothelial cells, and may be utilized to treat a wide variety of cancers, ocular diseases, and inflammatory conditions.

Abstract: Objects of the present invention are to provide an oxidative stress inhibitor which is capable of suppressing the expression of a cytotoxic protein and the activation of a gene transcriptional regulatory factor taking part such expression of a cytotoxic protein and exhibits good feeling upon use and safety; to provide a method for preventing, retarding, alleviating or treating a skin change due to aging or an undesirable aesthetic skin change, both caused or promoted by an oxidative stress; and to provide a cosmetic composition or dermatologic preparation for external use comprising the oxidative stress inhibitor as an effective ingredient, and for those purposes are employed an oxidative stress inhibiting agent which comprises, as an effective ingredient, at least one selected from cysteine or cystine derivatives and the salts thereof.

Abstract: Novel amidino-urea 5-HT7 receptor ligands, methods of preparing such ligands, intermediate compounds useful in the preparation of the receptor ligands, pharmaceutical compositions comprising the receptor ligands, and methods of treating sleep disorders, pain, depression, and schizophrenia employing the receptor ligands are disclosed. The receptor ligands have formula (1): wherein the formula variables are as defined herein, and pharmaceutically acceptable salts, solvates, active metabolites, or prodrugs thereof.

Abstract: Novel amides of polyunsaturated fatty acids with cysteamine-S-phosphate have been synthesized. Combinations of the all-trans-retinoic acid and/or amides of the 13-cis-retinoic acid with O-phospho-L-tyrosine, and N-docosahexaenoyl-cysteamine-S-phosphate, N-eicosapentaenoyl-cysteamine-S-phosphatee, N-arachidonoyl-cysteamine-S-phosphate, N-&agr;-linolenoyl-cysteamine-S-phosphate, and N-&ggr;-linolenoyl-cysteamine-S-phosphate and their analogues N-docosahexaenoyl-O-phospho-2-aminoethanol, N-eicosapentaenoyl-O-phospho-2-aminoethanol, N-arachidonoyl-O-phospho-2-aminoethanol, N-&agr;-linolenoyl-O-phospho-2-aminoethanol, N-&ggr;-linolenoyl-O-phospho-2-aminoethanol in different compositions exhibit a marked cell-growth inhibiting effect and display anti-tumor activity.

Abstract: Amino acid derivative as carrier compounds and compositions which are useful in the delivery of active agents are provided. The active agents can be a peptide, mucopolysaccharide, carbohydrate, or lipid. Methods of administration, including oral administration, and preparation are provided as well.

Abstract: Cosmetic or pharmaceutical compositions comprising compounds of formula (I) and the corresponding salts thereof: 1

Abstract: The present invention relates to a composition having effective insect repellent characteristics comprising as an active ingredient an N-substituted p-menthane carboxamide, which has little or no odor and which is substantially non-toxic for human, pet and livestock.

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-chalcogenmethylcarbonyl group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.

Abstract: The present invention relates to a dermatologic preparation containing a diamide derivative represented by the following formula (1): (wherein, R1 represents a linear or branched hydrocarbon group having 1 to 22 carbon atoms which may be substituted by one or more hydroxy and/or alkoxy groups, R2 represents a linear or branched divalent hydrocarbon group having 1 to 12 carbon atoms, and R3 represents a linear or branched divalent hydrocarbon group having 1 to 42 carbon atoms). This diamide derivative (1) is capable of fundamentally improving the water retention capacity and barrier functions of the horny layer, is excellent in miscibility and mixing stability and can be prepared efficiently at a low cost.

Abstract: The invention relates to surfactant-free cosmetic, dermatological and pharmaceutical compositions, comprising at least one copolymer consisting essentially of a1) 1 to 50% by weight of the repeat structural unit of the formula (1)  where n is an integer from 2 to 9, or a2) 1 to 50% by weight of a mixture of the repeat structural unit of the formula (1) and the repeat structural unit of the formula (2)  where R, R1 and R2 may be identical or different and are hydrogen or a linear or branched alkyl or alkenyl group having in each case 1 to 30 carbon atoms and b) 49.99 to 98.99% by weight of the repeat structural unit of the formula (3)  in which R3 is hydrogen, methyl or ethyl, Z is (C1-C8)-alkylene, n is an integer from 2 to 9 and X is an ammonium, alkali metal or alkaline earth metal ion and c) 0.01 to 8% by weight of crosslinking structures which originate from monomers having at least two olefinic double bonds.

Abstract: Novel active compound combinations of compounds of the formula (I) 1

Abstract: Cosmetic or pharmaceutical compositions comprising compounds of formula (I) and the corresponding salts thereof: 1

Abstract: Novel pharmaceutical therapeutic compositions and methods for using same for the treatment of pain experienced by an individual are provided. The compositions contain at least one member selected from among anandamide and palmitylethanolamide.