Abstract: There is provided a prodrug of a pharmaceutically active agent, such prodrug comprising a beta-keto carboxylic acid, a beta-keto carboxylic acid salt or a beta-keto carboxylic acid ester functional group, a pharmaceutical composition comprising the prodrug, and to the use of the prodrug or composition for treatment of a mammalian subject suffering from a condition which can be cured or alleviated by administration of the pharmaceutically active agent. There is further provided a method of inhibiting decarboxylation of a compound comprising a beta-keto carboxylic acid or a salt thereof with a monovalent cation, characterized in that a dry salt of the beta-keto carboxylic acid with a divalent or polyvalent cation is prepared.

Abstract: A composition comprising an inorganic particulate material in an amount of about 20 wt % to about 70 wt %, a carrier for the particulate material comprising a compound of formula (I) in an amount of about 1 wt % to about 70 wt %, a particulate material coating material in an amount of about 0 wt % to about 5 wt %, and a dispersing agent for the particulate material in an amount of about 0 wt % to about 5 wt %, based on the total weight of the composition, wherein one of R1 and R2 is a straight or branched chain C1-C30 alkoxy radical, and the non-alkoxy R1 or R2 is hydrogen; and R3 is a straight or branched chain C1-C30 alkyl radical.

Abstract: Adapalene or a pharmaceutically acceptable salt thereof formulated into a pharmaceutical composition is useful for reducing the number of acne lesions, via daily topical application, in combination or in association with benzoyl peroxide (BPO); such treatment may be via administration of a pharmaceutical composition combining adapalene and BPO or by a concomitant application of two pharmaceutical compositions, one containing adapalene and the other containing BPO.

Abstract: A buccal and/or sublingual formulation comprising one or more active compounds; and a buccal matrix which releases the active compounds at a predetermined rate for transport across the buccal and/or sublingual membranes, wherein the rate of release of the active compounds is either (A) the same or substantially the same rate at which the active compounds are transported across the buccal and/or sublingual membranes; or (B) a rate which releases the active compounds over an extended period as required by the therapeutic affect or treatment window for those active compounds.

Abstract: Uncoated particles of reversed cubic phase or reversed hexagonal phase material containing an active disposed within are provided. The uncoated particles have an ionic charge that is sufficient to stabilize them in dispersion in a liquid, e.g. a polar solvent. The active that is disposed within the particles may be, for example, a pharmaceutical or nutriceutical compound.

Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein X, Q, and R1-R6 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.

Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.

Abstract: A composition is provided which comprises an acidic component, generally fulvic acid, having a molecular weight not exceeding 20,000 Daltons and a low content of the elements aluminum, mercury, cadmium, chromium and lead. The acidic component is preferably carbohydrate derived and preferably using a wet oxidation process.

Abstract: [Problem] The present invention has an object to provide a compound having a GPR40 agonistic activity, which is useful as a pharmaceutical composition, an insulin secretion promoter, or an agent for preventing/treating diabetes. [Means for Solution] The present inventors have extensively studied a compound having a GPR40 agonistic activity, and as a result, they have found that the compound (I) of the present invention or a pharmaceutically acceptable salt thereof, in which a carboxylic acid is bonded to a bicyclic or tricyclic moiety through methylene, and further, a benzene ring substituted with a monocyclic 6-membered aromatic ring is bonded to a bicyclic or tricyclic moiety through —O-methylene or —NH-methylene, has an excellent GPR40 agonistic activity. They have also found that the compound has an excellent insulin secretion promoting action and strongly inhibits increase in the blood glucose after glucose loading, thereby completing the present invention.

Abstract: A composition containing 1,4-dihydroxy-2-naphthoic acid at a high concentration is obtained by intracellularly and extracellularly producing 1,4-dihydroxy-2-naphthoic acid using a bacterium belonging to the genus Propionibacterium and collecting it. This composition is efficacious in improving intestinal flora, alleviating abdominal ailments in association with the intake of milk, and preventing metabolic bone diseases.

Abstract: A method of treating cancer is disclosed comprising administering to a patient in need of such treatment a RXR agonist at a level below the RAR activating threshold and at or above the RXR effective dose.

Abstract: Provided are compounds for inhibiting Snail-p53 binding and therapeutic agents for cancer including the compounds as an effective component. The Snail-p53 binding inhibitors induce expression of p53 in K-Ras mutant cell lines, thereby enabling effective treatment or prevention of K-Ras mutant cancer, such as, pancreatic cancer, lung cancer, cholangioma, and colon cancer, of which diagnosis or treatment is not easy.

Abstract: Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, or NHSO2X, wherein X is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, heterocycle, or substituted heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.

Abstract: Biphenyl compounds having the formula (I): are useful for preventing/treating pathologies linked to a deficiency of the activation of the RAR gamma receptor, e.g., for treating a pathology linked to a cell differentiation and/or proliferation disorder, for treating acne, for treating psoriasis.

Abstract: The present invention provides liposomes that are useful for delivery of bioactive agents such as therapeutics. Among others, the liposomes of the invention are capable of delivering their payload at sites of increased secretory phospholipase A2 (sPLA2) activity, because phospholipase A2 (PLA2) will hydrolyse lipids of the liposome. Thus, the liposomes of the invention may e.g. be used in relation to cancer therapy. Another aspect of the invention is a liposomal formulation comprising the liposome of the invention. Still another aspect is a method of producing a liposomal formulation of the invention.

Abstract: The inventors have found that vitamin K3 and vitamin K5 which may be used in pharmaceuticals and foods or ACNQ, DHNA, or the like which can stimulate the growth of bifidobacteria can inhibit degranulation of basophil-like cells, exhibit a potent degranulation-inhibiting effect, and are useful anti-allergic agents or foods. The present invention provides an anti-allergic agent containing, as an active ingredient, one or more species selected from among 2-amino-3-carboxy-1,4-naphthoquinone, 1,4-dihydroxy-2-naphthoic acid, 1,4-naphthoquinone, 4-amino-2-methyl-1-naphthol, 2-methyl-1,4-naphthoquinone, 2-amino-3-chloro-1,4-naphthoquinone, and a salt thereof.

Abstract: Provided are methods of orally treating ischemic diseases and conditions, such as digital ulcers, associated with or caused by the ischemic diseases.

Abstract: The invention provides compositions for the diagnosis or treatment of neoplasias, including lymphomas, leukemias, brain cancers (e. glioblastomas, medulloblastomas), breast cancer, colon cancer, and pancreatic cancer, and methods of use therefor.

Abstract: The present invention describes a novel retinoid-responsive nucleic acid, and a novel protein. Further, the invention describes the use of such a nucleic acid or protein in various diseases, and for the treatment, the diagnosis and prognosis of various diseases, and also for a method for the prognosis of responsiveness to retinoids.

Abstract: The present invention relates to a controlled release pharmaceutical or food formulation comprising at least one active pharmaceutical or food ingredient dispersed in a mixture of a glycogen with a polysaccharide, and the process for its preparation. The invention also relates to a slow release system represented by a mixture of a glycogen with a polysaccharide, and its use for the preparation of slow release pharmaceutical or food formulations.

Abstract: Novel anhydrous dermatological depigmenting compositions, especially for topical application, contain, within the fatty phase thereof, as pharmaceutical active agents, a dissolved phenolic compound and a retinoid.

Abstract: An external preparation containing the following components (A) and (B): (A) a non-steroidal analgesic/anti-inflammatory agent, and (B) an organic amine. The external preparation of the present invention has improved skin permeation and excellent stability of a non-steroidal analgesic/anti-inflammatory agent in the external preparation. The external preparation of the present invention also has excellent appearance.

Abstract: Dermatological/cosmetic compositions contain, in a physiologically acceptable medium, at least one retinoid, dispersed benzoyl peroxide and a gelling system comprising at least two categories of compounds.

Abstract: The present invention is directed to a compound of formula (I), its diastereoisomers, its enantiomers or its pharmaceutically acceptable salts or solvates, formula (I), to procedures of obtaining the same, to intermediates thereof, and use as competitive inhibitors of the third enzyme of the shikimic acid pathway, the type II dehydroquinase.

Abstract: The present invention provides a controlled release pharmaceutical composition which exhibits reduced food effect.

Abstract: Small molecule inhibitors of Stat3 and their derivatives are disclosed. Also described are methods to inhibit cell growth by use of Stat3 inhibitors, and the use of Stat3 inhibitors for the prevention and/or treatment of cancer. Further, inhibitors of Stat3 that also do not inhibit Stat1 are described as well as their derivatives. Methods of screening additional compounds for Stat3 inhibition activity and/or non-inhibition of Stat1 activity are also described herein.

Abstract: Described herein are methods for enhancing engraftment of hematopoietic stem and progenitor cells using compounds identified using a zebrafish model of hematopoietic cell engraftment. The compounds can be used to treat hematopoietic stem cells ex vivo prior to transplantation of the cells. Alternatively, the compounds can be administered to an individual undergoing cell transplantation.

Abstract: A composition suitable for topical application that contains at least two active ingredients, one of these being dapsone and one selected from the group consisting of adapalene, tazarotene and treinion for the effective treatment of acne and other dermatological conditions.

Abstract: This disclosure ascribes new functions to derivatives of tetralin, anthraquinone, naphthylamine, tri-amino-pyrimidine, xanthen-3-one, and/or cinnamic acid (including, for example, NSC270718R, NSC117285R, NSC170008Y, NSC306711P, NSC119913X, NSC119915Z, NSC119911V, NSC119910U, NSC128437O, NSC125908P, NSC9600Q, or NSC13778J, each obtained from the Structure Diversity Set, National Institutes of Health, National Cancer Institute, Developmental Therapeutics Program). These compounds are shown to be effective inhibitors of viral essential protein kinases (such as poxvirus B1 and/or F10 protein kinases). Exemplary chemical structures for viral protein kinase (VPK) inhibitors are provided, as are methods of using such compounds, for instance, to inhibit VPK activity and/or poxvirus growth, and/or for the treatment of poxvirus infection. Also provided are pharmaceutical compositions including disclosed VPK inhibitors.

Abstract: The invention discloses an implant suitable for delivery of at least one drug, the implant comprising a fibrillar collagen matrix having, as measured in Example 1, a viscosity of greater than 100 mPas, optionally greater than 103 mPas, further optionally greater than 106 mPas, still further optionally greater than 109 mPas when a collagen dispersion formed from 140 mg of the fibrillar collagen matrix is dispersed in 25 ml of 2 mM HCl at a pH of less than 3.5 and at a temperature of 30.0+/?0.5° C.

Abstract: The photostabilizing electronic excited state energy—particularly singlet state energy from retinoid compounds—has been found to be readily transferred to (accepted by) ?-cyanodiphenylacrylate compounds having an alkoxy radical in the four (para) position (hereinafter “alkoxycrylenes”) on one of the phenyl rings having the formula (I): wherein one of R1 and R2 is a straight or branched chain C1-C30 alkoxy radical, preferably C1-C8, more preferably methoxy, and the non-alkoxy radical R1 or R2 is hydrogen; and R3 is a straight or branched chain C1-C30 alkyl radical, preferably C2-C20. The alkoxycrylene compounds of formula (I) significantly increase the photostability of retinoid compounds in a composition by at least 3-fold and as much as 10-fold or greater. The ability of the alkoxycrylene compounds to stabilize the retinoid compound is concentration dependent, with the amount of retinoid photostabilization increasing with the concentration of the alkoxycrylene compound.

Abstract: This invention relates to novel prostacyclin analogs and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel prostacyclin analogs that are derivatives of treprostinil. This invention also provides compositions comprising a compound of this invention and a carrier and the use disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering analogues of prostacyclin, such as treprostinil.

Abstract: The invention provides for the use of carbonic anhydrase activators; protein kinase C activators and FGF-18 to treat depressive disorders. The invention also relates to improved animal models and methods for screening and identifying compounds the treatment of depressive disorders.

Abstract: An improved excipient comprising substantially homogeneous particles of a compressible, high functionality granular microcrystalline cellulose based excipient is provided. The improved excipient comprises microcrystalline cellulose and a binder, and optionally a disintegrant, and is formed by spraying a homogeneous slurry of the components. The excipient provides enhanced flowability/good flow properties, excellent/high compactibility, and increased API loading and blendability as compared to the individual components, and as compared to conventional excipients formed from the same materials. The improved excipient has strong intraparticle bonding bridges between the components, resulting in a unique structural morphology including significant open structures or hollow pores. The presence of these pores provides a surface roughness that is the ideal environment for improved blending with an API.

Abstract: The present invention relates to chronotherapeutic pharmaceutical compositions and a method of preparing the same. The composition comprises of at least one active ingredient, a pH independent agent and a hydrophilic agent. The active ingredient in the composition is coated with the pH independent agent. The composition provides a dual controlled release system, which aids in an initial lag time of 4-6 hours and controlled release of the active ingredient up to 24 hours.

Abstract: The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.

Abstract: The invention relates to the use of calixarenes for preventing or limiting the transfer of an actinide in the body from a site of skin contamination.

Abstract: This invention provides a method for inhibiting pancreatic islet ?-cell dysfunction, comprising administering to a subject in need thereof an inhibitory effective amount of a rhein compound having the general formula (I) or a pharmaceutically acceptable salt thereof,

Abstract: The present invention provides sustained-release oral pharmaceutical compositions and methods of use. The sustained-release oral pharmaceutical compositions include an opioid (including salts thereof) and a salt of a non-steroidal anti-inflammatory drug (NSAID).

Abstract: Dermatological/cosmetic gel compositions suited for preventing or treating cell differentiation and/or proliferation and/or keratinization disorders, including preventing or treating common acne, comprise (i) at least one retinoid, (ii) dispersed benzoyl peroxide and (iii) at least one pH-independent gelling agent, formulated into (iv) a physiologically acceptable medium therefor.

Abstract: The invention is directed to methods and compositions that can be used in the treatment of headaches. In particular, methods and compositions are described involving the combination of a long-acting NSAID and a 5-HT1B/1D agonist.

Abstract: A method of treating cancer in a subject comprising the step of administering to the subject in need thereof an effective amount of a combination of a compound that binds a nuclear export signal (NES inhibitor) on topoisomerase II? and a topoisomerase inhibitor. Twenty small molecule inhibitors (SMI) that bind to the two nuclear export sequences (NES) topo II? have been identified from the NCI database using computer-generated molecular modeling. These SMI will improve the effectiveness of topo II directed therapeutics, particularly in the treatment of diseases such as multiple myeloma (MM). In vitro apoptosis assays indicate that these drugs may be effective as single agents or in combination with currently used cancer drugs that target topo II.

Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype.

Abstract: The invention relates to novel spill resistant formulations comprising either a weak base or a weak acid as the pharmaceutical ingredient, a liquid base, a clay and a water soluble cellulose ether. The clay and cellulose ether allow for a broader pH range into which the pharmaceutically active agent may be dispersed or dissolved, and therefore allows for easier preparation and formulation of the pharmaceutical composition.

Abstract: Orally deliverable dual-release pharmaceutical suspensions, having a first portion comprising an immediate release form of the active in the solution form or granules or suspended form in the vehicle/medium preferably in the solution form and a second portion comprising a sustained-release form of active in the form of microgranules/microparticles suspended in the immediate release fraction of the solulabilised active agent which comprise a core and at least one coat suitable for liquid dosage forms for the administration of the active ingredients, wherein the core comprises at least one active agent(s) or its pharmaceutically acceptable salts, derivatives, isomers, polymorphs, solvates, hydrates, analogues, enantiomers, tautomeric forms or mixtures thereof; optionally at least one water insoluble, and optionally one or more pharmaceutically acceptable excipient(s); and at least one coat comprising at least one pH independent water-insoluble polymer(s) along with one or more pharmaceutically acceptable excipi

Abstract: We describe methods and compositions for treating a patient suffering from a hyperproliferative disorder or photoageing. Our methods involve blocking the activity of a retinol binding protein receptor (RBPr) in cells of the patient, and/or administering to the patient an antagonist of a retinol binding protein receptor (RBPr) and/or lowering the endogenous level of retinoic acid (RA) in cells of said patient.

Abstract: Based on the discovery that celastrol and gedunin are Hsp90 inhibitors, the present invention provides novel inhibitors of Hsp90. and pharmaceutically acceptable salts, derivatives, and compositions thereof. The invention provides two classes of compounds. One class includes celastrol and its derivatives. The other class includes gedunin and its derivatives. The present invention further provides methods for treating disorders wherein Hs?90 inhibition is desired (e.g., proliferative diseases, cancer, inflammatory diseases, fungal infections, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. Celastrol, gedunin, and derivatives thereof are particularly useful in the treatment of prostate cancer, breast cancer, ovarian cancer, lung cancer, and leukemia.

Abstract: The present invention provides the use of pelorol analogs of Formula, (I) and pharmaceutical compositions thereof as modulators of SHIP 1 activity. A compound or a pharmaceutical composition of the present invention may be used for the treatment or prophylaxis of an inflammatory, neoplastic, hematopoetic or immune disorder or condition in addition to other disorders and conditions.

Abstract: Bifunctional molecules and methods for their use are provided. The subject bifunctional molecules are conjugates of a drug moiety and a pharmacokinetic modulating moiety, where these two moieties are optionally joined by a linking group. The bifunctional molecules are further characterized in that they exhibit at least one modulated pharmacokinetic property upon administration to a host as compared to a free drug control. The subject bifunctional molecules find use in a variety of therapeutic applications.

Abstract: The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs, processes for preparation of the same, their uses in pharmaceutical formulations, and for the treatment of various disorders, including pain.