Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

Abstract: There are disclosed compounds of formulae (I) or (II) in which A is selected from the group consisting of (1), (2), (3) and (4); OH, and one of R1 and R2 is selected from H, OH and OCH3, and the other of R1 and R2 is selected from OH and OCH3; one of R3 and R4 is selected from H, OH and OCH3, and the other of R3 and R4 is selected from OH and OCH3; provided that at least one of the pairs R1, R2 and R3, R4 are both OH; R5 is selected from OH and OCH3; and denotes a single or double bond; and pharmaceutically acceptable salts and prodrugs thereof. The compounds of the invention are useful for the treatment of hormone-dependent conditions and cancers.

Abstract: The invention is directed to pharmaceutical compositions useful in the treatment of migraine. The compositions contain metoclopramide and one or more NSAIDs in unit dosage form. By selecting NSAIDs that are non-acidic or segregating the metoclopramide and NSAID, the storage life of the compositions has been increased. Also disclosed are coordinated dosage forms for the sequential release of drugs. The invention encompasses methods of treating migraine using any of these dosage forms.

Abstract: The present invention relates to methods of improving a treatment outcome comprising administering a heat shock protein (HSP) preparation or an ?-2-macroglobulin (?2M) preparation with a non-vaccine treatment modality. In particular, an HSP preparation or an ?2M preparation is administered in conjunction with a non-vaccine treatment modality for the treatment of cancer or infectious diseases. In the practice of the invention, a preparation comprising HSPs such as but not limited to, hsp70, hsp90 and gp96 alone or in combination with each other, noncovalently or covalently bound to antigenic molecules or ?2M, noncovalently or covalently bound to antigenic molecules is administered in conjunction with a non-vaccine treatment modality.

Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

Abstract: The use of benzazepin-N-acetic acid derivatives which contain an oxo group in the a position to the nitrogen atom and are substituted in the 3 position by a 1-(carboxyalkyl)-cyclopentyl-carbonyl-amino radical, and of their salts and biolabile esters, for the prophylaxis and/or treatment of heart damage caused by cardiotoxic doses of medicaments or chemicals, in larger mammals and in particular humans. The invention is particularly applicable to the prophylaxis and/or treatment of heart damage, in particular to the myocardium, which may occur during cytostatic chemotherapy. The invention also includes the use of the afore-mentioned benzazepin-N-acetic acid derivatives for adjuvant treatment in therapies in which medicaments having oxidative-toxic side-effects are used, and the preparation of medicaments suitable for this prophylaxis and/or treatment or adjuvant treatment.

Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

Abstract: This invention provides the methodology and agents for treating any disease or clinical condition which is at least partly the result of endoplasmic reticulum-associated retention of proteins. Thus, the methods and agents of the present invention provide for the release of normally retained proteins from the endoplasmic reticulum. The present invention is particularly useful for treating any disease or clinical condition which is at least partly the result of endoplasmic reticulum-associated retention or degradation of mis-assembled or mis-folded proteins. In certain embodiments of the invention the agents include at least one curcuminoid.

Abstract: This invention provides various biquinone and trimeric quinone derivatives. The invention also provides a method for synthesis of a multi-quinone compound including reacting a hydroxyquinone anion with a first quinone possessing a first directing group at a C-2 of the first quinone and a second directing group at a C-3 of the first quinone and obtaining a biquinone having one of the first and second directing groups at a C-3 of a first quinone monomer and a hydroxyl group at a C-3′ of a second quinone monomer. The biquinone can be further reacted to obtain various biquinone derivatives or with a second hydroxyquinone anion to obtain trimeric quinone derivatives, including trimeric naphthoquinone derivatives. The biquinones and trimeric quinones of this invention demonstrate antiviral activity and can be used to treat viral infections, particularly HIV infections.

Abstract: The use of a pharmaceutical formulation in treating coronary arteriosclerosis and a two-component pharmaceutical formulation. The pharmaceutical formulation contains peroxidic species or reaction products resulting from oxidation of an alkene, such as geraniol, by an oxygen-containing oxidizing agent, such as ozone; a penetrating solvent, such as dimithyl sulfoxide; a dye containing a chelated metal, such as hematoporphyrin; and an aromatic redox compound, such as benzoquinone.

Abstract: Disclosed herein are novel chalcone derivatives of formulas (I), (II) and (III): 1

Abstract: This invention pertains to substituted chalcones, specifically substituted 1-(4-methoxyphenyl)-3-(3,5-dimethoxyphenyl)prop-1-en-3-ones, which have therapeutic application, for example, as potent antiproliferative agents and antiinflammatory agents, and which have the formula (I) wherein: X is —H, —OH, —OC(═O)R3, —OS(═O)2OH, or —OP(═O)(OH)2; Y is —H or a C1-4alkyl group; Z is —H or —OCH3; R1 is —H, a C1-4alkyl group, or C1-4fluoroalkyl group; R2 is —H, a C1-4alkyl group, or C1-4fluoroalkyl group; and, R3 is —H, a C1-6alkyl group, a C3-20 heterocyclyl group, or a C5-20aryl group; and pharmaceutically acceptable salts, esters, and protected forms thereof.

Abstract: The two carbohydrate mixture of this invention utilizes a source of fructose in combination with at least one readily digestible glucose polymer source. The addition of the fructose significantly decreases the glycemic response when compared to the digestible glucose polymer alone. Additional components may be added to the simple two component carbohydrate mixture to form a carbohydrate system suitable for incorporation into an enteral nutritional. This carbohydrate system optionally incorporates nonabsorbent carbohydrates, dietary fiber and indigestible oligosaccharides. The present invention is also directed to an enteral nutritional which incorporates the two component carbohydrate mixture and less than 37% of calories from fat. Additionally, the invention is directed to a method of delivering nutrients to a person with diabetes by feeding the enteral nutritional.

Abstract: The present invention relates to compounds, compositions and methods for the prevention or treatment of mycobacterium infections. The compounds are naturally occurring and synthetic biflavonoids, flavonoids, chalcones and chalcone like compounds. The compounds were screened for anti-mycobacterium activity. Of the compounds showing anti-mycobacterium activity, eight were identified as particularly potent, exhibiting greater than 90% inhibition of the growth of Mtb at a concentration of 12.5 Πg/mL. The actual minimum inhibitory concentrations (MIC), defined as the lowest concentration inhibiting 99% of the inoculum, for the preferred compounds ranged from 6.8 to 48.3 ΠM.

Abstract: All multiple myeloma cell lines examined showed constitutively active I&kgr;B kinase (IKK), I&kgr;B&agr; phosphorylation and constitutively active NF-&kgr;B. Curcumin, a chemopreventive agent, suppressed constitutive I&kgr;B&agr; phosphorylation through inhibition of IKK activity and downregulated NF-&kgr;B. Curcumin also downregulated expression of NF-&kgr;B-regulated gene products such as I&kgr;B&agr;, Bcl-2, Bcl-xL, cyclin D1 and interleukin-6. Consequently, curcumin suppressed multiple myeloma cell proliferation and arrested cells at the G1/S phase of the cell cycle. Curcumin also induced apoptosis and chemosensitivity to vincristine. Overall, results presented herein provide a molecular basis for the treatment of multiple myeloma patients with this pharmacologically safe agent.

Abstract: Anticancer agents containing, as an active ingredient, at least one compound selected from the group consisting of &ohgr;-hydroxy fatty acids and salts or esters thereof, hydroxy oxo-fatty acids and salts or esters thereof, lactones, macrocyclic ketones, and macrocyclic diesters having specific chemical structures.

Abstract: The present invention provides methods of slowing or inhibiting vascular smooth muscle (VSM) cell proliferation to slow the development or recurrence of atherosclerosis by contacting VSM cells with soluble epoxide hydrolase (sEH) inhibitors. Further, the methods of the invention can be used to slow or to inhibit vascular restenosis after angioplasty and the stenosis of vascular stents. Further, the methods of the invention can be used to slow or to inhibit the stenosis of hemodialysis grafts and other natural and synthetic vascular grafts.

Abstract: A compound of formula 1

Abstract: The invention is directed to small organic molecules having the ability to mimic or agonize hepatocyte growth factor/scatter factor (HGF/SF) activity, or inhibit or antagonize HGF/SF activity, the former useful for promoting, for example, vascularization of tissues or organs for promoting wound or tissue healing, or augmenting or restoring blood flow to ischemic tissues such as the heart following myocardial infarction. Inhibition of cellular growth or proliferation is beneficial in the treatment, for example, of inflammatory diseases such as inflammatory joint and skin diseases, and dysproliferative diseases such as cancer.

Abstract: A composition and method of cancer treatment is disclosed. The composition and method utilized the extract of B. papyrifera, or compounds included therein having aromatase inhibition properties, as active cancer chemopreventative and treating agents in mammals, including humans.

Abstract: This invention pertains to substituted chalcones, specifically substituted 1-(4-methoxyphenyl)-3-(3,5-dimethoxyphenyl)prop-1-en-3-ones, which have therapeutic application, for example, as potent antiproliferative agents and antiinflammatory agents, and which have the formula (I) wherein: X is —H, —OH, —OC(═O)R3, —OS(═O)2OH, or —OP(═O)2(OH)2; Y is —H or a C1-4alkyl group; Z is —H or —OCH3; R1 is —H, a C1-4alkyl group, or C1-4fluoroalkyl group; R2 is —H, a C1-4alkyl group, or C1-4fluoroalkyl group; and, R3 is —H, a C1-6alkyl group, a C3-20 heterocyclyl group, or a C5-20aryl group; and pharmaceutically acceptable salts, esters, and protected forms thereof.

Abstract: The present invention relates to formulations in solid or liquid form comprising isoquercitrin as a natural flavonoid, which is present therein as a light protection filter and/or antiviral substance. The invention relates to both cosmetic and medicinal formulations.

Abstract: Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having Ki's below 200 pM and activities 102-103 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, viz.: 1.) an &agr;-keto heterocylic head group; 2.) a hydrocarbon linkage unit employing an optimal C12-C8 chain length; and 3.) a phenyl or other &pgr;-unsaturation corresponding to the arachidonyl &Dgr;8.9/&Dgr;11.12 and/or oleyl &Dgr;9.10 positions. A preferred &agr;-keto heterocylic head group is &agr;-keto N4 oxazolopyridine, with incorporation of a second weakly basic nitrogen. Fatty acid amide hydrolase is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors).

Abstract: The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor/anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, incluidng angiongenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.

Abstract: Compositions and a method of protecting skin from either UV-induced immunosuppression or from UV-induced skin damage using a composition containing an extract of soy or clover, and/or the isoflavone compounds genistein, biochanin, dihydro-diadzein, formonentin, dihydro-geneistein, 2-dehydro-O-desmethyl-angolensin, tetrahydro-daidzein, equol, dehydro-equol, O-desmethyl-angolensin, or 6-hydroxy-O-desmethyl-angolensin.

Abstract: The invention relates to cosmetic or dermatological preparations comprising a) 0.1 to 10% by weight of one or more 3,3-diphenylacrylates of the formula I, and b) 0.1 to 10% by weight of one or more dibenzoylmethane derivatives of the formula II, in which the substituents R1 to R10 independently of one another have the meanings given in the description.

Abstract: Compounds containing two aromatic systems covalently linked through a linker containing one or more atoms, or “linker” defined as including a covalent bond per se so as to space the aromatic systems at a distance 1.5-15 Å, are effective in treating conditions associated with bone deficits. The compounds can be administered to vertebrate subjects alone or in combination with additional agents that promote bone growth or that inhibit bone resorption. They can be screened for activity prior to administration by assessing their ability to effect the transcription of a reporter gene coupled to a promoter associated with a bone morphogenetic protein and/or their ability to stimulate calvarial growth in model animal systems.

Abstract: The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compounds that elevate TGF-beta levels, as well as pharmaceutical compositions comprising compounds that elevate TGF-beta levels, and methods for detecting diseases associated with endothelial cell activation.

Abstract: 2,4,6-trihydroxy-&agr;-p-methoxyphenylacetophenone (also identified herein as “D-58”), or its pharmaceutically acceptable derivatives such as salt and ester forms, is administered for inhibiting inflammatory reactions. The treatment can be remedial or prophylactic. Examples of the conditions that can be treated include acute inflammatory reactions and allergic inflammatory reactions, and specific examples include allergy, asthma, arthritis, psoriasis, skin sunburn, inflammatory pelvic disease, inflammatory bowel disease, urethritis, uvitis, senusitis, pneumonitis, encephalitis, meningitis, myocarditis, nephritis, osteomyelitis, myositis, hepatitis, gastritis, enteritis, dermatitis, gingivitis, appendicitis, pancreatitis, cholocystitis and cholangitis. The 2,4,6-trihydroxy-&agr;-p-methoxyphenylacetophenone can be administered by various routes as needed.

Abstract: The present invention concerns enzymatic aromatic hydroxylation-activated prodrugs, particularly anti-tumour prodrugs and those which are specifically activated by the hydroxylation activity of the enzyme CYP1B1.

Abstract: 2,4,6-trihydroxy-&agr;-p-methoxyphenylacetophenone (also identified herein as “D-58”), or its pharmaceutically acceptable derivatives such as salt and ester forms, is administered for inhibiting inflammatory reactions. The treatment can be remedial or prophylactic. Examples of the conditions that can be treated include acute inflammatory reactions and allergic inflammatory reactions, and specific examples include allergy, asthma, arthritis, psoriasis, skin sunburn, inflammatory pelvic disease, inflammatory bowel disease, urethritis, uvitis, senusitis, pneumonitis, encephalitis, meningitis, myocarditis, nephritis, osteomyelitis, myositis, hepatitis, gastritis, enteritis, dermatitis, gingivitis, appendicitis, pancreatitis, cholocystitis and cholangitis. The 2,4,6-trihydroxy-&agr;-p-methoxyphenylacetophenone can be administered by various routes as needed.

Abstract: 2,4,6-trihydroxy-&agr;-p-methoxyphenylacetophenone (also identified herein as “D-58”), or its pharmaceutically acceptable derivatives such as salt and ester forms, is administered for inhibiting inflammatory reactions. The treatment can be remedial or prophylactic. Examples of the conditions that can be treated include acute inflammatory reactions and allergic inflammatory reactions, and specific examples include allergy, asthma, arthritis, psoriasis, skin sunburn, inflammatory pelvic disease, inflammatory bowel disease, urethritis, uvitis, senusitis, pneumonitis, encephalitis, meningitis, myocarditis, nephritis, osteomyelitis, myositis, hepatitis, gastritis, enteritis, dermatitis, gingivitis, appendicitis, pancreatitis, cholocystitis and cholangitis. The 2,4,6-trihydroxy-&agr;-p-methoxyphenylacetophenone can be administered by various routes as needed.

Abstract: The present invention relates to methods for preventing or treating skin disorders using flavonoid compounds. The present invention also relates to methods for regulating skin condition.

Abstract: A method of reducing hair growth in a mammal includes applying, to an area of skin from which reduced hair growth is desired, a dermatologically acceptable composition containing a suppressor of the metabolic pathway for the conversion of glucose to acetyl-CoA.

Abstract: The present invention concerns enzymatic aromatic hydroxylation-activated prodrugs, particularly anti-tumour prodrugs and those which are specifically activated by the hydroxylation activity of the enzyme CYP1B1.

Abstract: The present invention pertains to a method for healing a wound in a mammal which comprises the steps of (A) providing a therapeutic wound healing composition comprising a therapeutically effective amount of an inhibitor of mono-adenosine diphosphate-ribosyl transferase to inhibit adenosine diphosphate-ribosylation of vascular endothelial growth factor; and (B) contacting the therapeutic wound healing composition with a wound in a mammal. This invention also pertains to wound healing compositions and to methods for preparing and using the wound healing compositions and the pharmaceutical products in which the therapeutic compositions may be used. This invention further pertains to therapeutic dermatological-wound healing compositions useful to minimize and treat diaper dermatitis and to methods for preparing and using the therapeutic dermatological-wound healing compositions.

Abstract: A method of inhibiting an envelope virus selected from the group consisting of influenza bovine diarrheal, hepatitis C and tick borne encephalitis virus that udergoes hemagglutinin-mediated fusion with a host cell is disclosed which comprises administering to a virus-infected cell, a cell susceptible of infection or a mammal in need thereof, an effective amount of a compound as defined by Formula I in the specification.

Abstract: The present invention provides compositions and methods for treatment of human skin. Such methods include those for regulating sebum on facial skin of a human subject, comprising applying to said subject an emulsion composition comprising(a) an anhydrous silicone mixture comprising(i) an ethylene oxide/propylene oxide silicone copolymer;(ii) an ethylene oxide silicone copolymer;(iii) a silicone gum; and(iv) a silicone fluid; and(b) water.

Abstract: The present invention relates to methods for prevention or treating skin disorders using flavonoid compounds. The present invention also relates to methods for regulating skin condition.

Abstract: Quercetin chalcone, an effective, soluble and bioavailable bioflavonoid, is disclosed. Also disclosed are compositions containing quercetin chalcone in combination with an acceptable carrier and/or diluent, as well as methods for administration thereof to warm-blooded animals. Such administration is beneficial in generally maintaining good health of the animal and, more specifically, for the treatment of allergies.

Abstract: The invention relates to the use of .alpha.-hydroxyketoalkyl derivatives as light protection filters for cosmetic or pharmaceutical products, the .alpha.-hydroxyketoalkyl group being linked, if appropriate via a spacer, to a chromophoric group which has an absorption maximum in a wavelength range of between 280 and 400 nm and has a conjugated .pi.-electron system of at least 8 .pi.-electrons, and to new .alpha.-hydroxyalkyl derivatives, processes for their preparation and pharmaceutical and cosmetic formulations comprising these derivatives as light protection substances.

Abstract: A psoriasis treatment composition derived from the plant Asphodelus Microcarpus includes 3-methylanthralin, chrysophanol, aloe-emodin, aloe-emodin monoacetate, and/or derivatives thereof. The composition is prepared by extracting a liquid from the Asphodelus Microcarpus root and mixing the liquid with acetic acid. A method of treatment includes applying the composition to an affected area of skin at a frequency sufficient to effect an alleviation of symptoms, typically once per day for 14-56 days.

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: Use of flavone derivatives and flavanone derivatives, in particular flavonoids for stabilizing cosmetic or dermatologically acceptable substances, the chemical formula of which includes the structural moiety of dibenzoylmethane, against the decomposition caused by UV radiation.

Abstract: The present invention provides methods for treating cancer, particularly malignant tumors, with ketone thyroxine analogues having no significant hormonal activity. A ketone thyroxine analogue is administered to an afflicted mammal in an amount effective to cause depression or regression of malignant tumor growth or to treat cancer. Particularly preferred ketone thyroxine analogues are those capable of causing about 35 percent or more inhibition of initial velocity of microtubule protein assembly in vitro.

Abstract: A method for the prevention and treatment of atherosclerosis and its related diseases in mammals, in which an NADPH oxidase inhibitor is administered, is provided. The NADPH oxidase inhibitor prevents the production of reactive oxygen species upon exposure of endothelial cells to atherogenic LDL levels, thus resulting in decreased endocytosis and vascular hyperpermeability. Preferred NADPH oxidase inhibitors are of the formula: ##STR1## Additionally, there is provided a diagnostic method for predicting risk of a human patient to atherosclerotic-related diseases.

Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.

Abstract: The invention describes a method of killing or inhibiting the growth of the malaria causing pathogen Plasmodium falciparum by exposing the pathogen to a preparation containing methylene-bis-aspidinol, desaspidin, and/or aspidin.

Abstract: Novel pharmaceutically/cosmetically-active adamantyl-substituted biaromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a')-(f'): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

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.