Abstract: The invention relates to methods for detecting inactivation of the DNA Homologous Recombination pathway in a patient, and in particular for detecting BRCA1 inactivation.

Abstract: The present invention relates to a series of new drugs which refer to chemical series capable of catalyzing the decomposition of H2O2 to generate singlet oxygen (1O2). The drugs relate to therapeutic mechanisms, different from traditional photodynamic therapy, in which the specific affinity of photofrin to focus, such as tumors, vascular plaques and skin diseases is utilized. The activation of photofrin is carried out by specific protein binding or by electron beam, x-ray, r-ray, or other means, to focus, catalyze the decomposition reaction of H2O2 to generate 1O2 in the focus, 1O2 further induces apoptosis and necrosis of cells with pathological changes. The drugs are useful in tumors, vascular plaques and skin diseases, and cosmetic effects on skin are prompted. The drugs obtained via the screening and studying of the present invention are used for chemodynamic therapy (CDT), or for radiochemodynamic therapy (RCDT) carried out via radioactive rays.

Abstract: The invention relates to pharmaceutically acceptable salts of amphiphilic photosensitizing agents which have a water solubility of at least 0.5 mg/ml and to their use in methods of photochemical internalization. Such salts may be formed from a pharmaceutically acceptable base, for example an organic amine such as an amino alcohol, or from a pharmaceutically acceptable acid, for example a sulphonic acid or a sulphonic acid derivative. Due to their increased water solubility, such salts are particularly suitable for use in the preparation of parenteral pharmaceutical preparations, e.g. for use as solutions for injection or infusion.

Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.

Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.

Abstract: Provided is a sensitizing detection agent of an oral or intravenous administration type which enables the detection of bladder cancer with a higher sensitivity without causing pain to the patient. A sensitizing detection agent for bladder cancer comprising 5-aminolevulinic acid (ALA), a derivative thereof, or a salt of these is orally or intravenously administered, and a video camera system is inserted via the urethra and a blue light at 380-440 nm is irradiated to observe the red fluorescent part. Further, VLD-M1 is inserted and a blue light at 405 nm is irradiated to observe fluorescence intensity (relative intensity) of the red light part. For oral administration, 20 mg/kg (maximum of 1 g) of ALA is dissolved in 50 mL of a 5% glucose solution prior to the administration.

Abstract: The invention describes methods that are useful for treating cancer by administering a Chk1 inhibitor which can induce apoptosis in p53-defective cells when combined with a chemotherapy and/or radiotherapy. Methods for screening candidates for a Chk1 inhibitor-based cancer treatment regimen are also described.

Abstract: The use, as a dermatological or cosmetic medicament, of compounds capable of transiently interacting with the AhR receptor (aryl hydrocarbon receptor) as agents for modulating skin functions such as sebaceous function, skin healing, skin atropy termed “dermatoporosis”, estrogen deprivation and defense against infection, without inducing other toxic effects of the TCDD type. The compounds that interact with the AhR receptor are chosen in that they have a metabolism favorable to the dissociation of these effects, in particular by virtue of in situ production from a precursor and/or metabolization modulated in situ.

Abstract: There are provided compounds of the formula wherein X, Y, Z, R1, R2, R3 and R4 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.

Abstract: Methods and devices related to the treatment of diseases using phototherapy are described. Some embodiments provide an organic light-emitting diode device, such as a light-emitting device for phototherapy, comprising Ring System 1, Ring System 2, Ring System 3, Ring System 4 or Ring System 5. Methods of treating disease with phototherapy are also described.

Abstract: Mechanisms for complications of renal failure and processes for treating the same are disclosed. They include contacting a biological fluid (e.g. blood) with a filter body, the filter body having immobilized thereon either a CD36 receptor or a CD36 receptor fragment or a SCARB1 receptor or a SCARB1 receptor fragment, the blood having a reduced quantity of oxidatively modified proteins after contacting the filter body. They also include administering an antagonist drug to a patient that blocks the binding activity of the RAGE receptor or the CD36 receptor or the SCARB1 receptor. Diagnostic methods are also provided.

Abstract: The invention is generally related to the field of photodynamic therapy by use of photosensitizers and stabilized formulations of the photosensitizers. These formulations may be used to deliver a photosensitizer as a pharmaceutical, agricultural, or industrial agent. The photosensitizer containing formulations and compositions of the invention comprise one or more block copolymers. Furthermore, the invention relates to processes for the production of, and application of, said formulations and compositions as photosensitizer drug delivery systems.

Abstract: A method of synthesizing cycloalkanyl[b]indoles, as well as related cycloalkanyl[b]benzofurans and cycloalkanyl[b]benzothiophenes is provided. The method is a single, multicomponent reaction that combines (1) an indole, benzofuran, or benzothiopene, (2) an aldehyde, ketone, or ketal, and (3) a diene in the presence of an acid, in particular a Ga(III) or In(III) salt. Compositions and methods of using these compounds to stimulate secretion and/or production of glucagon-like peptide-1 or inhibit the activity of Calcitonin Gene-Related Peptide receptor are also provided.

Abstract: The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain.

Abstract: The present invention provides pharmaceutical photosensitizer-loaded nanoparticle formulations and their methods of preparation for photodynamic therapy, comprising a hydrophobic or hydrophilic photosensitizer, nanoparticulate calcium phosphate and in certain cases auxiliary reagents such as stabilizers. The calcium phosphate-based nanoparticle formulations of the present invention provide excellent storage stability and therapeutically effective amounts of photosensitizer for intravenous or topical administration. In a preferred embodiment, tetrapyrrole derivatives such as porphyrins, chlorins and bacteriochlorins, are the preferred hydrophobic photosensitizers to be formulated in calcium phosphate nanoparticle formulations for photodynamic tumor therapy. Additionally, 5,10,15,20-tetrakis(4-phosphonooxyphenyl)porphine (pTPPP) is a preferred hydrophilic photosensitizer for photodynamic tumor therapy.

Abstract: The present invention relates, in general, to a method of modulating physiological and pathological processes and, in particular, to a method of modulating cellular levels of oxidants and thereby processes in which such oxidants are a participant. The invention also relates to compounds and compositions suitable for use in such methods.

Abstract: The present invention relates to a pheophorbide-? conjugate or its salt, solvate or hydrate. The pheophorbide-? conjugate of the present invention exhibiting fluorescence upon its introduction into cells and degradation inhibits the survival of various cancer cells. Especially, the conjugate of pheophorbide-? (1) and doxorubicin shows higher fluorescence intensity at lower pH (cancer environment). Therefore, the present composition for photodynamic therapy (PDT) of cancers is also very useful in detecting cancers. Interestingly, the anticancer effects of the present composition are dually exerted with help of both the photosensitizer and the anticancer drug of the present conjugates.

Abstract: The invention relates to the use of 20-(4-carboxyphenyl)-2,13-dimethyl-3,12-diethyl-[22] pentaphyrine as antibacterial agent in photodynamic treatment. This expanded porphyrin derivatized in position 4 with a carboxyphenyl group proved very active after photo-oxidation both against S. aureus and E. hirae. Its high antibacterial activity and its low toxicity make this pentaphyrine particularly useful as antimicrobial agent both for photodynamic therapy against bacterial infections and in the disinfection of microbiologically contaminated liquids.

Abstract: Leucine-rich repeat kinase-2 (LRRK2) mutations are a common cause of Parkinson's disease. Inhibitors of LRRK2 kinase that are protective in in vitro and in vivo models of LRRK2-induced neurodegeneration were identified. The presently disclosed subject matter establishes that LRRK2-induced degeneration of neurons in vivo is kinase dependent and that LRRK2 kinase inhibition provides a potential new neuroprotective paradigm for treating Parkinson's disease.

Abstract: Are disclosed new crystalline forms of asenapine maleate, useful in the production of pharmaceutical formulations for the treatment of diseases of the central nervous system, in particular schizophrenia; processes for the production of these new crystalline forms are also disclosed.

Abstract: This invention relates to the use sigma-2 receptor antagonists, and of pharmaceutical compositions comprising such compounds, in methods for inhibiting Abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology and more broadly treating with such compounds and compositions neurodegenerative diseases and disorders associated with Abeta pathology. This invention also relates to methods for screening compounds for activity in inhibiting cognitive decline on the basis of their ability to bind to a sigma-2 receptor.

Abstract: The present invention relates to novel fusarisetin compounds separated from Fusarium sp. FN080326 and having an anticancer activity, and to the use thereof. In detail, novel fusarisetin compounds separated and purified from Fusarium sp. FN080326, which is in turn separated from a soil sample, have an inhibitory activity on the proliferation and transfer of cancer cells such as breast cancer cells, liver cancer cells or myeloid leukemic cells. Therefore, the compounds can be effectively used for anticancer compositions containing the compounds as active ingredients.

Abstract: A method of making a bacteriochlorin is carried out by condensing a pair of compounds of Formula II to produce the bacteriochlorin, wherein R is an acetal or aldehyde group. The condensing may be carried out in an organic solvent, preferably in the presence of an acid. The bacteriochlorins are useful for a variety of purposes such as active agents in photodynamic therapy, luminescent compounds in flow cytometry, solar cells, light harvesting arrays, and molecular memory devices.

Abstract: Lipidated micro- or macroparticles are prepared by covalently linking a glycoprotein, typically collagen, with at least one lipid. An amino group in the glycoprotein is joined with a primary amine in the lipid. These particles can be used to encapsulate active ingredients, such as drugs.

Abstract: Solid forms of (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine hydrochloride, in particular crystalline forms and/or amorphous forms thereof, pharmaceutical compositions and medicaments containing these solid forms, the use of these solid forms, and a process for obtaining such solid forms.

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: This documents provided methods and materials involved in treating bladder cancer. This document also provides methods and materials involved in identifying bladder cancer patients likely or unlikely to respond to treatment (e.g., BCG therapy).

Abstract: The present invention provides methods of treating cancer, particularly cancers that are null or have decreased expression or activity of the Lkb1 gene. Also included are methods of identifying therapeutic targets for the treatment of cancer.

Abstract: The invention relates generally to macrocyclic compounds and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of inhibitors of apoptosis (IAPs) and/or are useful in the treatment of medical conditions, such as cancer.

Abstract: The present invention describes an improved photodynamic treatment to treat subfoveal choroidal neovascularization (CNV).

Abstract: Described herein are methods and compositions for killing or preventing the growth of microbes. It has been discovered that a class of porphyrins can kill or prevent the growth of microbes. The porphyrins can be used in a number of different applications where microbes grow.

Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?2B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.

Abstract: Compositions comprising microaggregates containing hydrophobic drugs, as well as methods for their production, are described. Such microaggregates may include micelle structures or combinations thereof with liposomes, and constitute an effective delivery vehicle for a hydrophobic agent. Methods for microaggregate production include the use of preferred lipid compounds and processing conditions favoring the production of small aggregates for improved filter sterilization.

Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?1B—The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.

Abstract: Provided are a tumor proliferation inhibitor and a method for inhibiting tumor proliferation both of which can be applied to a minimally invasive cancer treatment using low-intensity pulsed ultrasound. The present invention provides a tumor proliferation inhibitor containing an ultrasound-sensitive substance and an acoustic cavitation phenomenon-enhancing substance, and provides a method for inhibiting tumor proliferation that can exhibit a tumor proliferation-inhibitory effect using the tumor proliferation inhibitor in combination with low-intensity pulsed ultrasound of a degree that is used in ultrasound diagnosis, and that can be applied to a minimally invasive cancer treatment using low-intensity pulsed ultrasound.

Abstract: The present invention relates to the use of avermectin derivative as a drug for the treatment of parasitic infections. The avermectin derivative is represented by the formula (I) wherein: (i) R1 is chosen from the group constituted of —CH(CH3)2, —CH(CH3)CH2CH3, or cyclohexyle, (ii) X represents —CH2CH2—, or —CH?CH—, (iii) R2 is chosen from the group constituted of or —OH group, (iv) R3 is OH or NOH, (v) represents a single bond when R3 is OH, or a double bond when R3 is NOH, as an inhibitor of a membrane-bound protein which transports exogenous compounds out of target cells.

Abstract: Methods of treating renal cancers and other kidney-related inflammatory disorders with a bioabsorbable polymer scaffold (such as a stent) are described. The treatments are provided as alternative to complete or partial surgical removal of a diseased kidney.

Abstract: Oral formulations and method of formulating photosensitive agents for oral administration during photodynamic therapy (PDT) and Antimicrobial photodynamic therapy (APDT) treatment are presented. The oral formulated photosensitizers show increased solubility and permeability, thus improving the bioavailability of photosensitizers at the treatment site. An orally administered photosensitizer is suitably formulated for mucosal adhesion and absorption via gastrointestinal mucosal membranes. Oral formulation provided herein use lipids and known proteins as carriers for photosensitizers by oral route. Carriers for encapsulating preselected photosensitizers include conventional liposomes, pegylated liposomes, nanoemulsions, nanocrystrals, nanoparticles, fatty emulsions, lipidic formulations, hydrosols, SMEDDS, Alpha-Feto protein (AFP), and Bovine-Serum-Albumin (BSA), fatty emulsions, hot-melt-extrudates and nanoparticles.

Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.

Abstract: In one aspect, the invention relates to methods for treating muscle atrophy by providing to an animal in need thereof an effective amount of a compound. The compound can modulate the expression levels of multiple mRNA of a muscle atrophy signature. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.

Abstract: A nano-carrier comprising an antiproliferative drug encapsulated by a lipophilic enhancement agent.

Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.

Abstract: This invention relates to the targeted delivery of hydrophobic drugs or combinations of hydrophobic drugs with photodynamic therapy agents to vascular lesions by complexation of the drugs to blood serum lipoproteins, which have an affinity for and accumulate in such vascular lesions.

Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

Abstract: The invention relates to methods and compositions for treating schizophrenia or bipolar disorder (in particular, mania) by using a combination of a synaptic vesicle protein 2A (SV2A) inhibitor and an antipsychotic or their pharmaceutically acceptable salts, hydrates, solvates, polymorphs thereof. In some embodiments, the methods and the compositions are for treating one or more positive and/or negative symptoms, as well as cognitive impairment, associated with schizophrenia or bipolar disorder (in particular, mania).

Abstract: The present invention discloses a class of novel macro-heterocyclic compounds represented by the formula Ia or Ib, and their intermediates, preparation methods and the uses. The macro-heterocyclic compounds of the present invention have good inhibitory activities against hepatitis C virus (HCV), and can be used to treat HCV infection effectively by its excellent inhibition against HCV, low toxicity and side effects.

Abstract: The present invention relates to methods for treating cancer by administering a therapeutically effective amount of compound of formula (I), such as selective NPY5R antagonist MK-0557 (trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H), 1?-cyclohexane]-4?-carboxamide), or a pharmaceutically acceptable salt thereof, to a subject in need thereof The methods can further comprise administering a chemotherapeutic agent to the subject in need thereof.

Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, R3, Z and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

Abstract: Compounds of the general structural formula (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents are disclosed. Treatable diseases and conditions include cancers, inflammatory diseases and conditions, and immunodeficiency diseases.