Abstract: Anti-viral compounds with low cytotoxicity are identified from screening of products found in Red Sea sponges, including the sponge Stylissa carteri. The identified compounds can be brominated pyrrole-2-aminoimidazole alkaloids and derivatives thereof. Specific examples of identified compounds include oroidin, hymenialdisine, and debromohymenialdisine, as well as derivatives thereof. The compounds also can be useful scaffolds or pharmacores for further chemical modification and derivatization. Selected compounds, particularly oroidin, show selective anti-viral HIV-1 activity coupled with reduced cytotoxicity. The compounds can function as HIV reverse-transcriptase inhibitors, and molecular modeling can be used to confirm inhibition.

Abstract: The current invention concerns an innovative treatment for mitochondrial disorders and diseases or conditions associated with mitochondrial dysfunction. In particular, effective and safe dosages of compounds suitable for the treatment of mitochondrial disorders have been established, providing for new treatment regimens and patient populations.

Abstract: The present disclosure is directed, among other things, to the surprising and unexpected efficacy provided by select V2R antagonists in significantly reducing the cell proliferation levels of clear cell renal cell carcinoma. Thus, the present disclosure provides methods, uses, and medicaments that include such select V2R antagonists for utility in treating clear cell renal cell carcinoma.

Abstract: The present invention relates to oral administration of water soluble cannabinoid and terpenoid concentrates on a flavored fibrous carrier. The compositions described herein provide an alternative to smoked cannabis that also avoid the slow action and unpredictable dosing of edible cannabis preparations. Water soluble concentrates of cannabinoids and terpenoids may be produced by derivatization reactions which are known in the art. Such water soluble concentrates enjoy significantly increased absorption by mucosal membranes of the mouth and may therefore be experienced by the consumer more quickly. Water soluble cannabinoid and terpenoid concentrates may be used in combination with each other and in combination with non-derivatized molecules which provides the user with fast and slow acting components in a single delivery vehicle.

Abstract: This application describes a compound represented by Formula (I): YZX1—S(O)(X2)F)m]n??(I) wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X1 is a covalent bond or —CH2CH2—, X2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.

Abstract: Anti-viral compounds with low cytotoxicity are identified from screening of products found in Red Sea sponges, including the sponge Stylissa carteri. The identified compounds can be brominated pyrrole-2-aminoimidazole alkaloids and derivatives thereof. Specific examples of identified compounds include oroidin, hymenialdisine, and debromohymenialdisine, as well as derivatives thereof. The compounds also can be useful scaffolds or pharmacores for further chemical modification and derivatization. Selected compounds, particularly oroidin, show selective anti-viral HIV-1 activity coupled with reduced cytotoxicity. The compounds can function as HIV reverse-transcriptase inhibitors, and molecular modeling can be used to confirm inhibition.

Abstract: The present invention relates to chemical compounds of formula (I), with the substituents as described in the specification, useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7 nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of ?7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases.

Abstract: Compounds which inhibit the small G protein Rho GTPase cell division cycle protein Cdc42 are provided. Morphological analyzes of filopodia, western blots of Ccd42 phosphorylation, and effects on cellular wound healing and on growth cone formation all demonstrate that the described compounds are able to inhibit all tested Cdc42-mediated processes. The compounds effectively inhibit the effects of Cdc42 and effectively inhibit Cdc42-related cellular functions involving actin, such as Golgi organization and cell movement. Furthermore, the described Cdc42 inhibitor compounds may be provided as a medicament for the treatment of various conditions.

Abstract: It relates to spirocyclic compounds of formula (I), or pharmaceutically or veterinary acceptable salts thereof, or any stereoisomers either of the compounds of formula (I) or of their pharmaceutically or veterinary acceptable salts, wherein A and B form a spirocyclic ring system wherein the spiro atom connecting A and B is a carbon atom and wherein A is a known 3- to 8-membered carbocyclic or heterocyclic monocyclic ring or a known 6- to 18-membered carbocyclic or heterocyclic polycyclic ring system; B is a known 4- to 7-membered carbocyclic or heterocyclic monocyclic ring; C is phenyl or a known 5- to 6-membered heteroaromatic ring; and R1-R7 are as defined herein. It also relates to a process for their preparation, as well as to the intermediates used in this process; to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular as antifibrinolytic and antihemorragic agents.

Abstract: Anthranilic acid derivatives are used to inhibit the formation of advanced glycation end products to reduce complications in diabetes.

Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of respiratory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of cough caused by minor throat and bronchial irritation (such as commonly accompanies the flu and common cold), as well as those resulting from inhaled particle irritants, upper respiratory infections, (pseudobulbar affect) in patients with amyotrophic lateral sclerosis and multiple sclerosis, neuropathic pain and pain associated with fibromyalgia.

Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.

Abstract: A system is described for long-term controlled release delivery of a drug or a therapeutic agent. According to the invention, one or more drugs or therapeutic agents contained in microspheres are mixed with a temperature sensitive hydrogel which is then introduced directly to the desired situs of the drug or therapeutic agent. The temperature sensitive hydrogel may also contain a drug or a therapeutic agent, for example, a pain relieving drug, for a short-term controlled release. The temperature sensitive hydrogel is in liquid state at room temperature, but upon injection, shortly becomes gelatinous. This system is particularly suitable for treatment of diseases, disorders, or conditions, for example, tumors, discogenic back pain, or arthritis, warranting localized administration of a drug or a therapeutic agent. In addition, the specification provides a method for production of a drug- or therapeutic agent-containing microspheres.

Abstract: The present application relates methods for treating a depressive symptom comprising administering an effective amount of a ? opioid receptor agonist or a pharmaceutically acceptable salt thereof to a subject in need thereof. Non-limiting examples of such agonist include the compounds of Formulas I, II, III, and IV, as well as the compounds of Table A.

Abstract: Disclosed herein are methods of treating a patient at risk of developing or having a neurofibromatosis or a sporadic schwannoma. In exemplary embodiments, the method involves administering to a subject in need an effective amount of a modulator of a target related to neurofibromatosis. Also disclosed are screening assays involving the implementation of Merlin-null Schwann cells, and to compounds identified using same.

Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.

Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.

Abstract: This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.

Abstract: An apparatus to apply antiseptic treatment while providing the benefits of a moisturizer. A method for using the apparatus whereby the antiseptic treatment is applied to a body orifice via a squeeze tube, a twist up stick tube or by using a finger to retrieve the antiseptic treatment from a small jar with a twist-off top to help provide a protectant that reduces a body's intake of harmful microbes.

Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.

Abstract: The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.

Abstract: Compounds of the general structure S-1, wherein X and R1-R5 are defined in the specification, are capable of abrogating the deubiquitinating (DUB) activity of the 19S RP DUBs and are useful in methods and compositions for treating cancer, in particular, cancer tumors refractory to treatment by state-of-the-art chemotherapy.

Abstract: Compounds that are central nervous system drug candidates for the treatment of cognitive decline and, more particularly, Alzheimer's disease are provided. Methods of treating, inhibiting, and/or abatement of cognitive decline and/or Alzheimer's disease with a compound or pharmaceutically acceptable salt of the invention are also provided. Also provided are methods of preparing the compounds/compositions of the invention.

Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.

Abstract: The present invention relates to novel vanilloid receptor ligands, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use of these compounds for the production of pharmaceutical preparations.

Abstract: The present invention provides a compound which is an inhibitor of sphingolipid biosynthesis for use in the treatment of a disease which has a secondary Niemann-Pick type C disease like cellular phenotype.

Abstract: A 2,3-dihydro-1H-indene-2-yl urea represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:

Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.

Abstract: Benzamide derivatives of formulae I and II, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof, and pharmaceutical compositions comprising the same, are described and have therapeutic utility, particularly in the treatment of diabetes, obesity, and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined as provided herein.

Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.

Abstract: A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.

Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.

Abstract: Compounds according to formula (I) are effective for the treatment of broncho-obstructive and inflammatory diseases.

Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.

Abstract: The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.

Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Tip-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.

Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.

Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.

Abstract: The present invention relates to methods of reducing cardiotoxicity and/or improving survival from treatment with anthracycline agents comprising administering a therapeutically effective amount of a composition comprising a vasopressin antagonist compound or a pharmaceutically acceptable salt thereof as an active ingredient, administered simultaneously or prior to the anthracycline administration.

Abstract: Pharmaceutical compositions and dosage forms comprising an adsorbent, and an adverse agent, such as an opioid antagonist. In one embodiment, at least a portion of the adverse agent is on the surface or within the micropore structure of an adsorbent material. The pharmaceutical compositions and dosage forms comprising the adsorbent and the adverse agent are useful for preventing or discouraging tampering, abuse, misuse or diversion of a dosage form containing an active pharmaceutical agent, such as an opioid. The present invention also relates to methods for treating a patient with such a dosage form, as well as kits containing such a dosage form with instructions for using the dosage form to treat a patient. The present invention further relates to process for preparing such pharmaceutical compositions and dosage forms.

Abstract: Compounds of the formula (I) are provided: wherein V, W, X, Y, Z, R3, R4, R5, R6, R7 and m are as defined in the specification; and pharmaceutically acceptable salts and prodrugs thereof. The compounds may be useful in the treatment or prevention of various diseases and conditions in which dipeptidylpeptidase-IV (DPP-IV) is implicated.

Abstract: Carbamate linked prodrugs of meptazinol and other opioid analgesics are provided. The prodrug moiety may comprise a single amino acid or short peptide. Additionally, the present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid pro-drug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a prodrug moiety, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.

Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.

Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that a compound of the present invention or a salt thereof exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. The present invention further relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound of the present invention or a salt thereof, and an excipient.

Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.

Abstract: The present invention relates to salts of meptazinol carbamate prodrugs, and to their synthesis and use.

Abstract: A method for repelling arthropods involving treating an object or area with an arthropod repelling effective amount of at least one compound having the formula wherein X is O, S, NH, N-NH2, N-CH3 or CH2, R? is H or alkyl, R? is alkyl, n is 0, 1, 2, 3 or 4, and mixtures thereof, optionally including a carrier material or carrier. The compound is preferably selected from homopiperazine, 1-methylhomopiperazine, 1-methylpyrrolidine, (R)-(?)-2-methylpiperazine, (S)-(+)-2-methylpiperazine, 2-methylpiperazine, 1-methylpiperazine, pyrrolidine, 1-methylpiperidine, piperidine, 1-ethylpiperazine, 1-methylimidazolidine, 1-methylthiomorpholine, 1,4-dimethylpiperazine, homopiperidine, imidazolidine, 4-methylpiperidine, thiomorpholine, 1-amino-4-methylpiperazine, 4-methylmorpholine, azocane, 2,6-dimethylpiperazine, 2,5-dimethylpiperazine, piperazine, 1-methlyhomopiperidine, or mixtures thereof.

Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.

Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.