Abstract: The present invention is directed generally to pharmaceutical compositions, methods, and kits for improving side effects associated with aromatase inhibitor treatment in a subject diagnosed with breast cancer. More specifically, the present invention provides compositions, methods, and kits comprising an aromatase inhibitor and an androgenic agent.

Abstract: This invention relates to new water-soluble solid pharmaceutical inclusion complexes and their aqueous solutions for oral, ophthalmic, topical or parenteral use containing a macrolide and certain cyclodextrins. More particularly the invention relates to new water-soluble solid pharmaceutical inclusion complexes and their solutions in aqueous solvents, said compositions containing a) as an active ingredient a macrolide such as Rapamycin, Pimecrolimus, Temsirolimus, Everolimus or Tacrolimus in an amorphous form and optionally in the form of their polymorphic hydrates or solvates e.g. solvates formed with acetone or ethanol. b) a large surface cyclodextrin, such as gamma cyclodextrin—whereby the weight ratio of said macrolide to said cyclodextrin ranges between 1:111 and 1:333.

Abstract: Pharmaceutical formulations exhibit a desirably low Cmax, among other properties, that contain particles of amorphous bardoxolone methyl, either in pure form or in the form of a solid dispersion, admixed with particles of a hydrophilic binding agent. Such formulations possess the advantage of higher oral bioavailability, relative to formulations based on the crystalline form of bardoxolone methyl.

Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of psoriasis.

Abstract: A method and composition for reducing the cholesterolemic effect in mammals of ingesting a blended nutritional fat composition containing a palm mid-fraction (PMF) hardstock fat combined with an unsaturated vegetable oil. The composition is solid or semi-solid at 20° C. and fluid at 35° C., and includes between 15% and 45% by weight linoleic acid. The weight ratio of disaturated triglyceride (DST) molecules to trisaturated triglyceride (TST) molecules is greater than 10:1, and the PMF hardstock fat contains approximately 50% to 95% by weight DST molecules, the majority of which contain either palmitic acid or a combination of palmitic and stearic acids at the sn-1 and sn-3 triglyceride positions and either oleic acid or linoleic acid at the sn-2 molecular position.

Abstract: The invention relates to a method for cosmetically treating oily skin, including the topical application onto the skin of a composition containing a jasmonic acid compound in a physiologically acceptable medium.

Abstract: Compounds for use in the treatment or prophylaxis of an affective disorder, which compound is represented by formula I: in which: the dotted line represents a single or a double bond; and R5 and R5? are independently —H, —OH or —OR6, where R6 is a linear or branched C1-C4 alkyl; X is —CH2O—; Z is —CH2CH2O—, —CH(CH3)CH2O— or —CH2CH(CH3)O—; m is 1; and n is an integer of 1-5; or a pharmaceutically acceptable salt, prodrug, metabolite, or hydrate thereof.

Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.

Abstract: HslVU is the proteasome-related system composed of HslV peptidase and HslU chaperone. It is involved in intracellular proteolysis. The presence of HslVU homologs in pathogenic microbes and its absence in human makes it an antimicrobial drug target. The functional HslVU complex forms when HslV dodecamer is flanked at both ends by HslU hexamers. In the HslVU complex, intercalation of C-termini residues of HslU subunits into the clefts between adjacent HslV subunits results in allosteric activation of HslV. We identified small molecules capable of activating HslV peptidase in the absence of its natural activator HslU. Quinazoline and chromone derivatives were suggested by ligand docking to bind at the HslU C-termini intercalation pockets in the HslV. This was confirmed by HslV activation assays with these compounds that gave ED50 in sub-micromolar range. The results showed that small, extracellular non-peptidic molecules can activate the HslV peptidase which in turn would initiate intracellular proteolysis.

Abstract: Tricyclic indazole compound and its pharmaceutically acceptable salts of acid addition, use thereof, method and intermediates for preparing them, and a pharmaceutical composition containing them. The tricyclic indazole compound has the following general Formula (I): in which R1, R2, L1, L2, X1, X2, X3, X4, X5, Y, W, m, and n have the meanings stated in the description.

Abstract: The present invention relates to the field of medical treatments for diseases and disorders. More specifically, the present invention relates to the use of the lanthionine synthetase component C-like (LANCL) proteins as therapeutic targets for novel classes of anti-inflammatory, immune regulatory and antidiabetic drugs.

Abstract: The invention relates to improved and stable pharmaceutical formulations of phenylalanine derivatives and the use thereof as urokinase inhibitors, particularly for the treatment of malignant tumors and tumoral metastases.

Abstract: Compositions and methods for inhibiting sulfide biogeneration from biofilms are described, as well as methods for preparing the compositions. The compositions comprise anthrahydroquinone and a biocide. The compositions may also include anthraquinone.

Abstract: Agri-horticultural pest control compositions having outstanding control effect on pests, in particular, agri-horticultural pests, which comprise as active ingredients one or more 4-(3-butynyl)aminopyrimidine derivatives represented by the general formula [I], namely, where R1 is typically selected from among: a) phenyl c) —SiR5R6R7 (R5, R6, and R7 which may be the same or different represent a linear or branched alkyl having 1-6 carbon atoms, a linear or branched haloalkyl having 1-3 carbon atoms which is substituted by one halogen atom, a linear or branched cyanoalkyl having 1-3 carbon atoms which is substituted by one cyano group, and phenyl); d) hydropgen atom; R2 typically represents a hydrogen atom; R3 typically represents a hydrogen atom; R4 represents a hydrogen atom and one or more agri-horticultural pest control compounds selected from among agri-horticultural antimicrobial compounds, say, multi-site contact active compounds, nucleic acids synthesis inhibitory active compounds, mitosis and cell

Abstract: There is provided the use of a methylxanthine derivative such as theophylline and a steroid in a synergistic combination for the treatment of chronic obstructive pulmonary disease, wherein the combination is administered by the inhaled route for pulmonary delivery.

Abstract: A pharmaceutical composition for treating diabetes is provided in this invention. The composition contains a lanostane compound as a potent component. A suitable source of the lanostane compound is a Poria extract from metabolite, sclerotium, or fermentation product of Poria cocos (Schw) Wolf. The Poria extract contains 1-60% of the lanostane compounds by weight of the extract, and is devoid of secolanostane.

Abstract: Provided is a pharmaceutical composition for the treatment and prevention of obesity, diabetes, metabolic syndromes, degenerative diseases and mitochondrial dysfunction-related diseases, comprising: a therapeutically effective amount of a compound represented by Formula I below, or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and a pharmaceutically acceptable carrier, a diluent or an excipient, or any combination thereof. wherein R1 through R8 and n are as defined in this disclosure.

Abstract: Sustained-release vaginal ring for comprising dehydroepiandrosterone (DHEA), dehydroepiandrosterone sulfate (DHEA-S) or pharmaceutically acceptable thereof as active principle, and optionally a release-modulating agent of the active principle, wherein the amount of active principle is between 1% to 32% by weight, relative to the total weight of the formulation, and the modulator is selected from: polyvinylpyrrolidone K-30, lactose, microcrystalline cellulose and sodium lauryl sulfate. The vaginal ring of the present invention can be used to increase ovarian reserve in women, to be used as drug in assisted reproduction programs, and to relieve symptoms associated with menopause, such as symptoms of vulvar and vaginal atrophy and sexual dysfunction in postmenopausal women.

Abstract: Disclosed are small molecule inhibitors of the formula (I): and the pharmaceutical compositions thereof and processes of making the same. The compounds are useful in treating various diseases and conditions involving chymase.

Abstract: Cosmetic compositions comprising substituted amino heterocyclic carbamoyl analogs and methods of using such compositions to impart anti-aging benefits to the skin are disclosed. The substituted amino heterocyclic carbamoyl analogs are believed to have modulatory activity against one or more biochemical pathways implicated in skin aging.