Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less that 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposes are also disclosed.

Abstract: The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives.

Abstract: A method of treating a subject with a cytokine-mediated inflammatory disorder comprising administering to the subject an effective amount of a pharmaceutically acceptable cholinesterase inhibitor, provided that the inhibitor is not galantamine.

Abstract: The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.

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: The invention relates to compounds of Formula (1) for use in modulating potassium channel activity in cells.

Abstract: The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.

Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

Abstract: The present application provides compositions and methods using bioorthogonal inverse electron demand Diels-Alder cycloaddition reaction for rapid and specific covalent delivery of a “payload” to a ligand bound to a biological target.

Abstract: The embodiments provide compounds of the general Formulae I, II, III, IV, V, VI, VII, and X, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Abstract: The present invention relates to the field of cardiology. More specifically, the present invention relates to the use of ?3 adrenoreceptor agonists to treat cardiac hypertrophy and heart failure. In a specific embodiment, a method for treating cardiac hypertrophy comprises the step of administering a therapeutically effective amount of a ?3 adrenoreceptor agonist to a patient diagnosed with cardiac hypertrophy. In a more specific embodiment, the method for treating cardiac hypertrophy comprises the step of administering a therapeutically effective amount of the ?3 adrenoreceptor agonist BRL 26830A to a patient diagnosed with cardiac hypertrophy. In a further embodiment, the present invention provides a method for treating a cardiovascular disease or condition associated with cardiac hypertrophy comprising the step of administering a therapeutically effective amount of a ?3 adrenoreceptor agonist to a patient diagnosed with cardiac hypertrophy.

Abstract: Luminescent and/or electroactive nanoparticles suitable for MRI (Magnetic Resonance Imaging) and/or PET (Positron Emission Tomography) are prepared by mixing luminescent or electroactive compounds and ethyl oxide/propyl oxide block-copolymers in an organic solvent, which is thereafter evaporated in order to obtain a residue; and by hydrolyzing-condensating tetraalkoxysilanes in an aqueous solution in the presence of the residue; the obtained nanoparticles show no or a negligible release of the luminescent or electroactive compounds and are useful for bio-analytic and bio-medic applications.

Abstract: The present invention provides methods to reduce or inhibit weight gain by administering inhibitors of the SirT1 protein to a subject. Methods to identify such inhibitors are also disclosed.

Abstract: This invention relates generally to cyanine-containing compounds; pharmaceutical compositions comprising cyanine-containing compounds; and methods of using cyanine-containing compounds for cancer cell imaging, cancer cell growth inhibition, and detecting cancer cells, for example. Compounds of the invention are preferentially taken up by cancer cells as compared to normal cells. This allows many uses in the cancer treatment, diagnosis, tracking and imaging fields.

Abstract: The present invention provides hepatoprotectant acetaminophen mutual prodrugs, which have an acetaminophen moiety covalently linked to a second moiety that may act as a hepatoprotectant against acetaminophen hepatotoxicity. Additionally, acetaminophen mutual prodrugs may have improved water solubility which may provide better suitability for parenteral and other dosage forms relative to administration of acetaminophen. Also provided are methods of treating a disease or condition that is responsive to acetaminophen (such as fever, pain and ischemic injury) using hepatoprotectant acetaminophen mutual prodrugs, as well as kits and unit dosages.

Abstract: Compositions comprising a (A) dithiino-tetracarboximide of formula (I) and at least one agriculturally beneficial biological control agent (B) are disclosed. A method for curatively or preventively controlling phytopathogenic fungi of plants or crops is disclosed. A method for treating seed and a method for protecting seed are disclosed.

Abstract: Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.

Abstract: The present disclosure relates to aqueous liquid pharmaceutical compositions comprising a) at least one triptan compound, pharmaceutically acceptable salts or hydrates thereof, and b) xylitol.

Abstract: The invention relates to novel tetrahydro-1H-carbazole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and methods of treatment comprising administration of said compounds to patients.

Abstract: A formulation or preparation for treating and preventing arterial and venous thrombi is provided. This preparation includes a non-metal containing photodynamic dye and a fat soluble vitamin. A method of administration for treatment and prophylaxis of arterial and venous thrombi is also provided. This method includes steps of: combining a non-metal containing photodynamic dye and a fat soluble vitamin; combining the non-metal containing photodynamic dye and fat soluble vitamin with a sodium solution; and administering the combination of non-metal containing photodynamic dye, fat soluble vitamin, and sodium solution as an intravenous drip.

Abstract: The present invention relates to compositions comprising a combination of PKC activators and PKC inhibitors and methods to modulate ?-secretase activity; improve or enhance cognitive ability; and/or reduce neurodegeneration in individuals suffering from diseases that impair cognitive ability, particularly Alzheimer's Disease. The invention also relates to methods for improving or enhancing cognitive ability. The present invention also provides methods for increasing the generation of non-amyloidogenic soluble APP (sAPP) comprising the activation of protein kinase C (PKC) in the brain and inhibiting PKC in peripheral tissues. Macrocyclic lactones (i.e. bryostatin class and neristatin class) are preferred PKC activators and Vitamin E is a preferred PKC inhibitor for use in the inventive composition.

Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.

Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.

Abstract: The present invention related to the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with critical buccal condition, leading to difficulties in swallowing oral medicine forms and thus difficulties in treating said illnesses. Particularly, the present invention discloses the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with dysphagia and/or odynophagia and/or aspiration risk. Another aspect of the present invention is the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for the treatment of dysphagia and/or odynophagia and/or aspiration risk.

Abstract: The present invention relates to naphthalene derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine.

Abstract: The invention encompasses isoindoline compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel disease and myelodysplastic syndrome.

Abstract: The present invention relates to the synthesis of a series of ionone and curcumin derivatives as multi-targeting agents effective against both hormone-sensitive and hormone-independent cancers. In particular, the present invention is directed to a distinct class of bifunctional antiandrogens, which inhibit both AR and IKBkinases (IKK). A series of ionone-based chalcones were synthesised and their in vitro cytotoxicity against prostate cancer cell lines were demonstrated. A series of derivatives formed by reacting ionone-based chalcones and hydrazines demonstrate substantial antiproliferative activities in prostate cancer, breast cancer and lung cancer cell lines.

Abstract: The present invention relates provides pharmaceutical compositions comprising an amorphous carvedilol salt and one or more pharmaceutically acceptable excipients, wherein the amorphous carvedilol salt is formed in situ during the preparation of the pharmaceutical composition. The amorphous carvedilol salt is preferably an amorphous carvedilol phosphate salt. The pharmaceutical compositions can be prepared by providing one or more inert cores; contacting the core or cores with a solution or a dispersion comprising carvedilol, an acid component and optionally a binder, in a solvent; removing the solvent; and optionally coating the core or cores with an extended release composition. Preferred pharmaceutical compositions contain both immediate-release pellets and at least one population of extended-release pellet.

Abstract: Described herein are peptide derivatives and peptidomimetics as inhibitors for transglutaminases, methods for their preparation, pharmaceutical compositions containing said compounds as well as uses of said transglutaminase inhibitors in particular for the treatment of coeliac disease and transglutaminase dependent diseases.

Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.

Abstract: The invention encompasses novel amorphous and crystalline forms of carvedilol phosphate, carvedilol hydrogen phosphate, and carvedilol dihydrogen phosphate as well as methods of making the novel amorphous and crystalline forms. Also disclosed are pharmaceutical compositions comprising the novel amorphous and crystalline forms and uses thereof.

Abstract: Methods for reducing or preventing the effects of ionizing radiation in healthy cells arc provided. The methods relate to the use of selective cyclin-dependent kinase (CDK) 4/6 inhibitors to induce transient quiescence in CDK4/6 dependent cells, such as hematopoietic stem cells and/or hematopoietic progenitor cells. Radioprotection can be effected in mammals by treatment with selective CDK4/6 inhibitor compounds either before, at the same time as, or after exposure to the ionizing radiation.

Abstract: The invention features methods, compositions, and kits useful for the treatment of muscular dystrophy, e.g., Duchenne muscular dystrophy, in a patient.

Abstract: Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R1 preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which C is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumors. The prodrug is expected to be activated preferentially in tumor cells, which it will act as a DNA alkylating agent preventing cell division.

Abstract: A method of reducing the virulence of a bacterium that expresses accessory gene regulator A (AgrA) includes administering to the bacterium an amount of AgrA antagonist effective to inhibit the synthesis of one or more virulence factors by the bacterium.

Abstract: The present invention provides prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group containing a sulfonic acid containing phenyl carbamate, in which the protecting group confers enhanced water solubility upon the prodrug, and in which the prodrug also has a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody, and for the therapeutic use of such prodrug and conjugates, and for processes for preparing such prodrugs and conjugates.

Abstract: The invention relates to methods and compositions for improving cognitive function by using a combination of a synaptic vesicle protein 2A (SV2A) inhibitor and an acetylcholinesterase inhibitor (AChEI) or their pharmaceutically acceptable salts, hydrates, solvates, polymorphs thereof. In particular, it relates to the use of a combination of an SV2A inhibitor and an AChEI in treating a central nervous system disorder with cognitive impairment in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, amyotrophic lateral sclerosis (ALS), and cancer-therapy-related cognitive impairment.

Abstract: This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.

Abstract: Administration of sPLA2 inhibitors has been found to decrease cholesterol levels, atherosclerotic plaque formation and aortic aneurysm in mice, and to decrease cholesterol and triglyceride levels in humans. Interestingly, administration of sPLA2 inhibitors was found to decrease cholesterol levels even when the inhibitors were administered only once per day. Therefore, provided herein are methods of treating dyslipidemia, CVD, and conditions associated with CVD such as atherosclerosis and metabolic syndrome, by administering one or more sPLA2 inhibitors. Significantly, administration of sPLA2 inhibitors and various compounds used in the treatment of CVD, such as for example statins, resulted in greater decreases in LDL and LDL particle levels in a synergistic manner. In addition, administration of sPLA2 inhibitors and statins resulted in a synergistic decrease in plaque content.

Abstract: The invention is directed to naphthalene and quinoline sulfonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.

Abstract: The present invention is directed to compounds of Formula I: (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: The present invention relates to method for the treatment or prevention and of proliferative eye diseases including but not limited to: age related macular degeneration associated proliferative retinopathy, proliferative diabetic retinopathy, proliferative vitreoretinopathy, posterior capsular opacification, scaring and fibrosis after glaucoma filtration surgery, uveal melanoma, and retinoblastoma. The method comprises contacting cells in the eye by means of intra-ocular injection or infusion, with a drug that irreversibly inhibits cellular proliferation without causing extensive tissue necrosis or cytotoxicity. In a preferred embodiment the drug is bizelesin.

Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1 R2 R3, R4, R5, R6, X and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.

Abstract: This invention relates to novel macrocyclic protease inhibitors and their pharmaceutically acceptable salts thereof. This invention also provides compositions comprising at least one compound of this invention and the use of such compositions in methods of treating a flavivirus infection or liver fibrosis in a patient in need thereof.

Abstract: There is provided amino acid ester compounds comprising at least one nitric oxide releasing group, pharmaceutically acceptable salts thereof and compositions thereof. These compounds involve an amino acid side-chain or an amino acid derivative thereof and a nitric oxide releasing group as depicted in the following structures: wherein R1 is either an ethyl or an amino acid side-chain group or an amino acid derivative thereof and R2 is an amino acid side-chain group or an amino acid derivative thereof and n is an integer from 1 to 10.

Abstract: The disclosure provides that components of a PTEN cell signaling pathway may be utilized as therapeutic targets for treating, preventing, slowing the progression of or delaying the onset of a neurodegenerative disease or disorder. Such components that may be targeted include, phosphatase and tensin homologue (PTEN), glycogen synthase kinase 3 beta (GSK3?), and AKT. The subject matter disclosed herein relates to the therapeutic use of inhibitors of PTEN, inhibitors of GSK3?, or activators of AKT to treat a neurodegenerative disease or disorder in a subject. Compounds are disclosed which may be used in the methods provided.

Abstract: A controlled release dosage form has a coated core with the core comprising a drug-containing composition and a water-swellable composition, each occupying separate regions within the core. The drug-containing composition comprises a low-solubility drug and a drug-entraining agent. The coating around the core is water-permeable, water-insoluble and has at least one delivery port therethrough. A variety of formulations having specific drug release profiles are disclosed.

Abstract: This invention is directed to indolone derivatives which are antagonists for the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.

Abstract: Oral pharmaceutical form containing microgranules for the sustained release of at least one active principle, including a neutral carrier that is insoluble in water or in an alcohol solution, or a neutral carrier rendered insoluble in water or an alcohol solution, comprising at least one first mounting layer containing at least one active principle and optionally a pharmaceutically acceptable binding agent, wherein the whole comprises at least one coating based on at least one hydrophobic polymer.

Abstract: Compounds of the general formula I wherein rings B, C, D and E may be present or not and, when present, are combined with A as A+C, A+E, A+B+C, A+B+D, A+B+E, A+C+E, A+B+C+D or A+B+C+D+E, rings B, C and E being aliphatic whereas ring D may be aliphatic or aromatic/heteroaromatic, and wherein X is —(CH2)m—, in which m is an integer 1-3, to form a ring E or, when E is absent, a group R1 bound to the nitrogen atom, wherein R1 is selected from the group consisting of a hydrogen atom, alkyl or haloalkyl groups of 1 to 3 carbon atoms, cycloalkyl(alkyl) groups of 3 to 5 carbon atoms (i.e.