Abstract: Disclosed are compounds which bind &agr;4&bgr;7 integrin. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by &agr;4&bgr;7 integrin. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: A single dosage medication formulation has a beta-adrenergic blocker and a cholesterol lowering agent that is a statin combined in a single oral formulation for treatment of and reducing the risk of cardiovascular disease to enhance simplicity, cost reduction, convenience, and patient compliance with the use of these agents.

Abstract: Use of nordihydroguaiaretic derivatives to suppress CDC-2 and survivin, stimulate apoptosis, and treat tumors.

Abstract: Novel C3-substituted cyclodeca-1,5-diynes can be prepared through novel synthetic procedures using starting (E)-C3-substituted-4-(aryl- or heteroarylmethylidene)cyclodeca-1,5-diynes reagents. Both the C3-substituted cyclodeca-1,5-diyn-3-enes and the starting reagents have improved thermal stability compared to unsubstituted counterparts.

Abstract: A polyunsaturated fatty acid-containing composition for treating hypertriglyceridemia and methods of use thereof are provided.

Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.

Abstract: The present invention relates to the use of D-chiro-inositol (DCI) as a regulator of hypothalamic gene expression and, more particularly, to the use of DCI and derivatives and metabolites thereof to treat neuroendocrine impairments such as obesity, polycystic ovarian syndrome (PCOS), impaired regulation of hormones during aging and to correct such neuroendocrine impairments and associated functions.

Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved

Abstract: This invention relates to the field of therapy and diagnostic methods for ulcerative colitis. Specifically, the method comprises administering a compound or recombinant protein that inhibits interaction between CEP and human tropomyosin. Also included in the invention are methods to screen for drugs useful in treating ulcerative colitis and diagnostic methods for detecting diseases associated with an autoantigen response to hTM in affected tissue.

Abstract: Dictyostatin-1 has been found to stabilize microtubules and prohibit their depolymerization to free tubulin. Because of these activities, the dictyostatin compounds can be used in the treatment of a number of diseases in which aberrant cellular proliferation occurs such as drug-sensitive and drug-resistant cancers, autoimmune disorders, and inflammatory diseases.

Abstract: This invention relates to a compound or group of compounds present in an active principle derived from plants of species Euphorbia peplus, Euphorbia hirta and Euphorbia drummondii, and to pharmaceutical compositions comprising these compounds. Extracts from these plants have been found to show selective cytotoxicity against several different cancer cell lines. The compounds are useful in effective treatment of cancers, particularly malignant melanomas and squamous cell carcinomas (SCCs). In a preferred embodiment of the invention, the compound is selected from the group consisting of jatrophanes, pepluanes, paralianes and ingenanes, and pharmaceutically-acceptable salts or esters thereof, and more particularly jatrophanes of Conformation II.

Abstract: The interconversion of inactive 11-keto steroids with their active 11&bgr;-hydroxy equivalents can be controlled by the use of inhibitors of the 11&bgr;-reductase enzyme, such as carbenoxolone (3&bgr;-(3-carboxypropionyloxy)-11-oxo-olean-2-en30-oic acid). Such inhibitors may be put to a number of therapeutic uses in humans and animals, for instance to inhibit hepatic gluconeogenesis, to lower intracellular cortisol concentration, to increase insulin sensitivity in adipose tissue and muscle, and to prevent or reduce neuronal loss/cognitive impaiment due to glucocorticoid potentiated neurotoxicity or neural dysfunction or damage.

Abstract: The present invention provides an antioxidant carotenoid composition substantially free of lutein comprising lutein esters. This antioxidant composition may readily be formulated into products for administration to humans to provide protection from the harmful effects of free radicals. The invention also provides a method of preventing or inhibiting the harmful effects of free radicals by administering an effective amount of an antioxidant carotenoid composition substantially free of lutein comprising lutein esters.

Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.

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: Glycation, particularly of proteins, notably of the skin and/or nails and/or hair of an individual subject in need of such treatment, especially for combating skin aging, comprises administering thereto, for such period of time as required to elicit the desired cosmetic/therapeutic response, a thus-effective amount of at least one hydroxystilbene compound, e.g., of 3,3′,5,5′-tetrahydroxystilbene or derivative thereof.

Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.

Abstract: Disclosed are methods for increasing the differentiation of mammalian neuronal cells for purposes of treating neurodegenerative diseases or nerve damage by administration of various compounds including alcohols, diols and/or triols and their analogues.

Abstract: A method for suppressing undesired viral growth in a host which comprises administering to the host an effective amount of a compound of the formula: wherein R1, R2, R3 and R4 are independently selected from the group consisting of HO—, CH3O— and CH3(C═O)O—. The method is exemplified by inhibiting Tat transactivation of a lentivirus and in suppressing Herpes simplex virus.

Abstract: A nutritional formulation containing bactericidal amounts of diacetyltartaric acid esters of mono- and diglycerides is provided. A process of inhibiting bacterial infections including the step of feeding the nutritional composition to a subject is also provided.

Abstract: The present invention relates to a compound of the general formula wherein R1, R2, R3 and R4 are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.

Abstract: The present invention relates new use of rhein or the salt thereof, that is new use in preparing medicine for treatment of diabetic nephropathy. A medicine containing rhein or the salt thereof for treatment of diabetic nephropathy may be supplied in aqueous solution or capsula for oral, the dosage is not larger than 200 mg/day. Toxicity of rhein or the salt thereof is low, LD50 is 3.2 g/kg. The concentration of medicine in blood is still higher in 24 hours after administered rhein by oral. Rhein can effectively control or decrease the hyperglycemia, suppress renal hypertrophy and kidney index in experimental diabetic rats. The urinary protein execretion was significantly decreased in the diabetic patients treated by rhein.

Abstract: A compound effect for the treatment of dermatological disorders comprises a mono- or diester of an &agr;,&ohgr;-dicarboxylic acid, wherein the alcohol moiety of the said ester comprises a keratolytically active alcohol. The compound may have the formula, where n is in the range of 6 to 12; m is in the range of 0 to 8; R′ is selected from the group consisting of H, alkyl, aryl, alkenyl, benzyl, OH, NHR″, CONHR″ and COOR″; R″ is selected from the group consisting of alkyl, aryl, alkenyl, and benzyl; and Y is selected from the group consisting of H, alkyl, aryl, alkenyl, benzyl and X.

Abstract: Betulin and dihydrobetulin acyl derivatives according to the present invention have been found to have potent anti-HIV activity. The compounds of the present invention have the following formulae: or pharmaceutically acceptable salts thereof, wherein R1 is a C2-C20 substituted or unsubstituted carboxyacyl, R2 is a C2-C20 substituted or unsubstituted carboxyacyl; and R3 is hydrogen, halogen, amino, optionally substituted mono- or di-alkylamino, or —OR4, where R4 is hydrogen, C1-4 alkanoyl, benzoyl, or C2-C20 substituted or unsubstituted carboxyacyl; wherein the dashed line represents an optional double bond between C20 and C29.

Abstract: The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors.

Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.

Abstract: 2-Deoxystreptamine is an aminocyclitol whose structural stability and abundant functionality make it an attractive scaffold for the combinatorial generation of small molecules. The ability to selectively functionalize the various positions of 2-deoxystreptamine with an almost infinite number of different groups ensures that the libraries so generated will be both spatially and functionally diverse. These compounds can then be screened for biological activity to afford lead compounds for pharmaceutical programs. Additionally, biological ligand mimics based on 2-deoxystreptamine can be readily appended, either directly or through a tether, to solid surfaces or incorporated covalently into gels to afford novel materials useful in separation science.

Abstract: The invention provides a therapeutic method for treating or preventing stroke and other ischemic disorders, as well as novel compounds and pharmaceutical compositions useful for carrying out such methods.

Abstract: New stable derivatives of ubiquinole are described, having general formula (I), along with processes for their production and their pharmaceutical use, in particular in the treatment of intracellular oxidative stress and diseases involving oxidative stress of this kind.

Abstract: Methods and compositions for the control of nematodes are disclosed. Specifically, fatty acid ester compounds have been found to advantageously control nematodes at concentrations which are non-phytoxic. The fatty acid ester compounds can be used in conjunction with other nematicidal agents such as free fatty acids, fatty acid salts, avermectins, ivermectin, and milbemycin. In another embodiment, the subject invention further provides methods for killing the eggs of nematodes. Thus, the subject invention further relates to the surprising discovery that certain fatty acid esters have ovicidal activity against nematode eggs.

Abstract: Provided is a pharmaceutical composition based on rhein or diacerhein. The composition is intended for administration by the oral, rectal or cutaneous (percutaneous or transdermal) route, and comprises rhein or diacerhein, or one of their pharmaceutically acceptable salts or esters, and sodium lauryl sulfate, comicronized, in a weight ratio between 3:1 and 30:1. The composition exhibits improved bioavailability.

Abstract: This invention is a method and composition for the inhibition of VCAM-1, and in particular for the treatment of cardiovascular or inflammatory disease, including atherosclerosis, that includes the administration of an effective amount of an ester of probucol.

Abstract: The present invention relates to colchicine and thiocolchicine derivatives which can be obtained from these molecules by functionalization of the C-7 to ketone or functionalization of the amino group. Said compounds have a marked antiblastic activity both on the normal cancer cells and on the chemoresistant phenotype. The compounds of the invention can be administered both by injection and orally.

Abstract: This invention relates to the novel retinoyloxy(aryl-substituted)-alkylene butyrate compounds of Formula (I) and pharmaceutical compositions containing same, to methods of treating, preventing or ameliorating cancer and other proliferative diseases in a subject in need of such treatment comprising administering a compound of Formula (I) and pharmaceutically-acceptable salts and prodrugs thereof. ##STR1## The compounds of the invention are also useful in methods of inhibiting histone deacetylase, ameliorating wrinkles, treating or ameliorating dermatological disorders, inducing wound healing, treating cutaneous ulcers and treating gastrointestinal disorders.

Abstract: A nutritional formulation containing bacterial amounts of diacetyltartaric acid esters of mono- and diglycerides is provided. A process of inhibiting bacterial infections including the step of feeding the nutritional composition to a subject is also provided.

Abstract: Therapeutic treatment as well as prophylactic measures are provided by topical application of compositions containing an aryl 2-acetoxyethanoic acid to eradicate or prevent the development of axillary foul odor, foot malodor and other body odors, e.g. scalp, and skin, nail and follicular infections caused by microorganisms. The compositions are antimicrobial against several organisms that infect the skin and are specifically effective against P. acnes. The compositions are therapeutically effective against folliculitis and perifolliculitis and are useful for other skin lesions, nail and mucosal infections such as impetigo, seborrheic dermatitis, erythrasma and trichomycosis axillaris, associated with or caused by microorganisms. The therapeutic effect of the composition may be synergized or amplified by incorporating a cosmetic or dermatologic agent into the formulation for topical treatment of cosmetic and dermatologic indications.

Abstract: Therapeutic treatment as well as prophylactic measures are provided by topical application of compositions containing an aryl 2-acetoxyethanoic acid to eradicate or prevent the development of axillary foul odor, foot malodor and other body odors, e.g. scalp, and skin, nail and follicular infections caused by microorganisms. The compositions are antimicrobial against several organisms that infect the skin and are specifically effective against P. acnes. The compositions are therapeutically effective against folliculitis and perifolliculitis and are useful for other skin lesions, nail and mucosal infections such as impetigo, seborrheic dermatitis, erythrasma and trichomycosis axillaris, associated with or caused by microorganisms. The therapeutic effect of the composition may be synergized or amplified by incorporating a cosmetic or dermatologic agent into the formulation for topical treatment of cosmetic and dermatologic indications.

Abstract: This invention relates to the novel compounds of Formula (I) and pharmaceutical compositions containing same, to methods of treating, preventing or ameliorating cancer and other proliferative diseases in a subject in need of such treatment comprising administering a compound of Formula (I) and pharmaceutically-acceptable salts and prodrugs thereof. ##STR1## The compounds of the invention are also useful in methods of ameliorating wrinkles, inducing wound healing, treating cutaneous ulcers and treating gastrointestinal disorders.

Abstract: This invention relates to the novel compounds of Formula (I) and pharmaceutical compositions containing same, to methods of treating, preventing or ameliorating cancer and other proliferative diseases in a subject in need of such treatment comprising administering a compound of Formula (I) and pharmaceutically-acceptable salts and prodrugs thereof. ##STR1## The compounds of the invention are also useful in methods of ameliorating wrinkles, inducing wound healing, treating cutaneous ulcers and treating gastrointestinal disorders.

Abstract: The instant invention provides compositions containing molecules having at least one moiety from .beta.(3,4-dihydroxyphenyl) lactic acid and/or caffeic acid which are found in extracts from genus Salvia, said moieties being of the formula: ##STR1## said active agents having a molecular weight of at least 190 daltons. A class of preferred agents are those which are conjugated to form dimers and larger polymers containing said moieties. The agents of the invention may be administered in pharmaceutically acceptable carriers systemically or locally.

Abstract: Substituted amino compounds of general formula (I) ##STR1## are described, as are a method of preparing them and their use as drugs, especially as analgesics.

Abstract: Methods for inactivating bacteria including bacterial spores using an oil-in-water emulsion are provided. The oil-in-water emulsion comprises an oil, a surfactant and an organic phosphate-based solvent. These methods can be used to inactivate a wide variety of bacteria such as Bacillus.

Abstract: This invention relates to N'-substituted-N,N'-disubstitutedhydrazines of formula I ##STR1## wherein X and X' are independently O, S, or NR; A' and B' are independently substituted or unsubstituted aryl or aromatic heterocycle; wherein F is alkyl, alkenyl, or aralkyl; and wherein E is a tertiary carbon containing organic radical having a total of at least four carbon and halogen atoms but not more than six halogen atoms, or a non-tertiary carbon containing non-haloalkyl organic or organometallic radical having at least five atoms other than hydrogen, oxygen and halogen which are useful as insecticides, compositions containing those compounds, methods of producing the compounds, and methods of their use. More particularly, the invention relates to insect growth regulating compounds and compositions, and methods of using such compounds and compositions. Compounds of the present invention are particularly suitable for controlling plant-destructive insects in crops of cultivated plants, ornamentals and forestry.

Abstract: There are disclosed a controlling agent and an antifouling composition against harmful aquatic organisms, which include a particular N-phenylisothiazolone derivative of the formula: ##STR1## wherein X.sup.1 and X.sup.2 are the same or different and are independently hydrogen, chlorine or bromine; and R is haloalkoxy. Also disclosed is a method for preventing or inhibiting the adhesion of harmful aquatic organisms to water-exposed articles, which includes applying the antifouling composition to the water-exposed articles.

Abstract: The composition for the treatment of poultry litters comprises at least an edible surfactant emulsifying agent, for example an ethoxylate obtained from castor oil. It may also be combined with a mixture of cresols, guaiacol and resorcinol. This composition can be sprayed in liquid form on the litter so as to reduce the effects of coccidiose.

Abstract: Medicinal products for the selective control of tumor tissue and a method for control of such tumor tissue by administration of such product to a host. The products comprise: (a) two different compounds having a pH below 7 when the compounds are present in a protonated form, such compounds having the formula set forth below and (b) a pharmaceutically acceptable inert medicinal product carrier. The compounds have the following ##STR1## wherein R.sub.1 is hydrogen or a moiety which completes an ester group or an ether group, R.sub.2 is independently selected from the group consisting of an amino group, hydroxyl, an ester group, an ether group and a halogen, and n is an integer of 1 to 4.

Abstract: A new salt of a prodrug useful in antibody directed enzyme prodrug therapy (ADEPT) is disclosed. A hydrogen iodide salt of the prodrug N-(4-[N,N-bis(2-iodoethyl)amino]phenoxycarbonyl)-L-glutamic acid is prepared which can be obtained in crystalline form. Preparation of the crystalline form of the prodrug enables preparation of the prodrug in highly pure form.

Abstract: FK506 and geldanamycin promote nerve regeneration by a common mechanism that involves the binding of these compounds to polypeptide components of steroid receptor complexes other than the steroid hormone binding portion of the complex (FKBP52 and hsp90, respectively). These and other agents cause hsp90 dissociation from steroid receptor complexes or block association of hsp90 with steroid receptor complexes.

Abstract: 6,7-disubstituted-2-aminotetralines of general formula (1) ##STR1## and their pharmacologically acceptable salts, wherein X and Y, identical or different are selected from the group consisting of methoxy, acetoxy and fluoro; and R and R.sub.1, identical or different, are selected from the group consisting of hydrogen, ethyl, propyl, cyclopropylmethyl, 2-hydroxy-2-phenylethyl, 2-hydroxy-2-(4-methylphenyl)ethyl and 2-hydroxy-3-(4-methoxyphenoxy)propyl are endowed with immunomodulator activity.

Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formula (II): ##STR1##