Abstract: The present invention relates to photosensitizer compounds based on functionalized fullerenes useful in targeted photodynamic therapy (PDT), and methods of use thereof.

Abstract: The present invention relates to novel amide compounds of formula I, and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC6 is responsive, and the pharmaceutical composition containing such compounds.

Abstract: Dynamic colorectal PDT methods, devices and photosensitizer compositions to treat abnormal cell growth in anal tissue such as perianal and intra-anal intraepithelial neoplasia grade III are presented. Dynamic colorectal PDT method comprises the steps of administering topically, intravenously or orally a photosensitizer composition; irradiating; monitoring treatment parameters before, during and/or after irradiation. Photosensitizer composition comprises Temoporfin and excipients/carriers, appropriate for the application method. An applicator is provided for colorectal PDT treatments enhancing irradiation delivery and monitoring treatment parameters. Preferably, applicator is made of a material, used to monitor the fluence rate simultaneously while doing optical spectroscopy. Measurement probe devices are provided for monitoring PDT treatment parameters in-vivo.

Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).

Abstract: Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2?-diindolylmethane, 2?,3-diindolylmethane, and 3,3?-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.

Abstract: The present invention provides compounds of the general Formula DI: along with methods of making such compounds, formulations containing the same, and methods of using the same (e.g., in photodynamic therapy, for the production of solar cells, etc.).

Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.

Abstract: The invention refers to the use of androgen receptor antagonists for the treatment and/or prevention of fibroids, also known as uterine leiomyoma, leiomyomata. Particularly, the invention refers to the use of an androgen receptor antagonist being any one of the compounds according to the following list: cyproterone acetate, oxendolone, chlormadinone acetate, spironolactone, osaterone acetate, dienogest, flutamide, hydroxyflutamide, nilutamide, bicalutamide, RU 58841, LGD-2226, MDV3100, BMS-641988, BMS-779333, or 4-(3-{[6-(2-hydroxy-2-methylpropoxy)pyridin-3-yl]methyl}-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile (thioxoimidazolidine derivative) for the treatment of fibroids.

Abstract: The present invention provides a formulation comprising asenapine hemipamoate suspended particles, which formulation can be administered via a Depot provided by an IM injection of the formulation, and which depot does not display a particle-size dependent release rate. The present invention provides also methods of treatment using the same.

Abstract: The present invention embraces methods for the diagnosis and treatment of learning or mental disorders, as well as the identification of agents useful in the treatment of such disorders based upon the identified involvement of Sarcoplasmic Ca2+-ATPase type 2 Protein in synaptic plasticity and neurotransmitter release in 22q11 deletion/DiGeorge Syndrome.

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: 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: Described are methods of improving insulin sensitivity, and treating fatty liver disease (including non-alcoholic steatohepatitis (NASH)), by administering specific inhibitors of PKC delta.

Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

Abstract: Aromatic molecules that can be used as sensors are described. The aromatic sensors include a polycyclic aromatic hydrocarbon core with a five-membered imide rings fused to the core and at least two pendant aryl groups. The aromatic sensor molecules can detect target analytes or molecular strain as a result of changes in their fluorescence, in many cases with on-off behavior. Aromatic molecules that fluoresce at various frequencies can be prepared by altering the structure of the aromatic core or the substituents attached to it. The aromatic molecules can be used as sensors for various applications such as, for example, the detection of dangerous chemicals, biomedical diagnosis, and the detection of damage or strain in composite materials. Methods of preparing aromatic sensor molecules are also described.

Abstract: Treatments for conditions involving detrimental activity of the enzyme core 2 GlcNAc-T are provided using compounds of the formula I wherein R1 is H, —OH, C1-6 alkoxy, —NR5R6, or Sac 1; R2 is H, —OH, C1-6 alkoxy or Sac 2; R3 is H, —OH, C1-6 alkoxy or Sac 3; R4 is H, C1-6 alkyl, C1-6 hydroxyalkyl or C1-6-alkoxy-C1-6-alkyl; R5 is H, C1-6 alkyl or C1-6 acyl; R6 is H, C1-6 alkyl or C1-6 acyl; Sac 1 Sac 2 and Sac 3 are independently selected saccharide moieties; and Z is a steroid moiety; or a pharmaceutically acceptable salt, ether or ester form thereof

Abstract: The present invention relates to novel catecholamine derivatives of Formula I, to processes for their preparation, pharmaceutical compositions containing them and to their use in therapy.

Abstract: Peptides and compounds are provided that function as EWS-FLI1 protein inhibitors. The peptides and compounds have utility in the treatment of Ewing's sarcoma family of tumors. Also provided are methods of preparing the compounds and assays for identifying inhibitors of EWS-FLI1 protein.

Abstract: This invention provides a novel class of substituted macrocyclic porphyrin compounds. The compounds are useful as peroxynitrite decomposition catalysts. Pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable salt, hydrate, or prodrug thereof are also described.

Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).

Abstract: A pharmaceutical composition for treating, inhibiting, or preventing cancer can include an indole-3-carbinol derivative compound in a pharmaceutically acceptable carrier that is configured for oral administration. The indole-3-carbinol derivative compound can have antitumor activity, and oral administration can provide blood bioavailability of about 0.5% to about 25%. The pharmaceutically acceptable carrier can include a hydroxyl-fatty acid PEG monoester and/or diester. The carrier can be a hydroxyl-fatty acid PEG ester that includes 12-hydroxy stearate. The carrier can be a hydroxyl-fatty acid PEG ester that includes a PEG having from about 100 MW to about 200,000 MW. The indole-3-carbinol derivative can be 2,10-dicarbethoxy-6-methoxy-5,7-dihydro-indolo-(2,3-b)carbazole.

Abstract: The present invention relates, in general, to pattern-recognition receptors (PRRs), including toll-like receptors (TLRs), and, in particular, to a method of inhibiting nucleic acid-induced activation of, for example, endosomal TLRs using an agent that binds to the nucleic acid (“nucleic acid binding agent”), preferably, in a manner that is independent of the nucleotide sequence, the chemistry (e.g., DNA or RNA, with or without base or sugar modifications) and/or the structure (e.g., double-stranded or single-stranded, complexed or uncomplexed with, for example protein) of the nucleic acid(s) responsible for inducing TLR activation. The invention also relates to methods of identifying nucleic acid binding agents suitable for use in such methods.

Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.

Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).

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 compound of formula (I) and compositions thereof, methods of their production as well as methods for treating bacterial infection.

Abstract: The invention relates to topical pharmaceutical compositions comprising a phthalocyanine, wherein a diamagnetic metal ion moiety is either coordinated or covalently bound to the phthalocyanine core. The invention also relates to methods for destroying cancer tissue, precancerous cells, photo-aged cells, damaged cells, or otherwise pathologic cells, or activated cells, such as lymphocytes or other cells of the immune system, or activated or inflamed tissue cells comprising topically administering to the cancer tissue or surrounding tissue an effective amount of a phthalocyanine composition.

Abstract: A method for treating cancer, preventing cancer or delaying the progression of a cancer in an animal or human comprising the step of: administering to the animal or the human having a cancer a composition in an amount effective to treat cancer, prevent cancer or delay the progression of cancer in the animal or the human. The composition comprises a pharmaceutically acceptable excipient, and ascorbate which is joined to a carrier structure containing an anti-cancer active agent, said carrier structure being capable of releasing the anti-cancer agent in the presence of a reactive oxygen species.

Abstract: The invention provides cationic tetracyclic and pentacyclic bacteriochlorophyll derivatives (Bchls) containing at least one positively charged group and/or at least one basic group that is converted to a positively charged group under physiological conditions, preferably Bchls having an onium group derived from a N-containing aliphatic or heterocyclic radical such as ammonium, guanidinium, imidazolium, pyridinium, and the like or a phosphonium, arsonium, oxonium, sulfonium, selenonium, telluronium, stibonium, or bismuthonium group, or a basic group that is converted to such onium groups under physiological conditions, said groups being bound to one or more of the positions 17<3>, 13<3> and 3<2> of the Bchl molecule by ester or amide bond. The Bchls are useful for photodynamic therapy and diagnosis.

Abstract: This invention is directed to methods of preventing or treating neurological or neuropathic diseases or conditions associated with excessive inflammation, neurodegeneration, neuro-remodeling, and axonal/neurite retraction. Particularly, this invention relates to methods treating neurological or neuropathic diseases such as cerebral ischemia, stroke, neuropathic pain, spinal cord injury, Alzheimer's disease, and multiple sclerosis, using novel rho kinase inhibitor compounds. The method comprises identifying a subject in need of the treatment, and administering to the subject an effective amount of a novel rho kinase inhibitor compound to treat the disease.

Abstract: Methods for preventing damage to the epidermis during PDT induced using a pre-photosensitizing agent are provided. The methods of the present invention utilize spatial confinement to control formation of a photoactive species from a topically-applied pre-photosensitizing agent. In one embodiment, thermal inhibition is used to prevent the metabolism of a pre-photosensitizing agent in epithelial tissue surrounding a treatment site. In another embodiment, a chemical inhibitor can be applied to the epithelial tissue to inhibit the conversion of a pre-photosensitizing agent into a phototoxic species.

Abstract: The present invention relates to photosensitizer compounds based on functionalized fullerenes useful in targeted photodynamic therapy (PDT), and methods of use thereof.

Abstract: A composition of matter of an anhydride of formula 1 below and an improved two stage reaction process for production of mono-L-aspartyl chlorin e6, utilizing the anhydride:

Abstract: The present application describes deuterium-enriched ruboxistaurin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).

Abstract: Diseases and conditions associated with tissues of the body, including but not limited to tissues in the eye, can be effectively treated, prevented, inhibited, onset delayed, or regression caused by administering therapeutic agents to those tissues. Described herein are ophthalmic formulations that deliver a variety of therapeutic agents, including but not limited to rapamycin (sirolimus), analogs thereof (rapalogs) or other mTOR inhibitors, to a subject for an extended period of time. The ophthalmic formulations may be placed in an aqueous medium of a subject, including but not limited to intraocular or periocular administration, or placement proximate to a site of a disease or condition to be treated in a subject. A method may be used to administer a therapeutic agent to treat or prevent age-related macular degeneration, macular edema, diabetic retinopathy, uveitis, dry eye, or a hyperpermeability disease in a subject.

Abstract: A pharmaceutical composition that contains an atypical antipsychotic drug and succinic acid, fumaric acid or a mixture of succinic acid and fumaric acid.

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: 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: The present invention provides novel drug formulations for oral administration for diverse medical applications including anticancer, antimetastatic, antibacterial, antifungal, antiprotozoic, antiviral, antiprionic and PDT treatments for diagnostic and therapeutic purposes. In a preferred embodiment the oral drug formulation comprises a photosensitizer and suitable excipients and may be administered in multiple doses over an extended period of time with exposure to activating radiation occurring generally between individual doses or in a light-independent manner. In another preferred embodiment PDT methods for treating hyperplasia and neoplasia, for localizing hyperplasic and neoplasic tissues and pathogen bacteria by fluorescence, for treating infections caused by pathogen bacteria in complex body fluids and for fat reduction, skin disorders and vascular diseases are provided.

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

Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.

Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).

Abstract: The invention provides compounds of Formula (I): wherein b, D, R1, R2, G, Ra and Rb have meanings given in the description, or pharmaceutically-acceptable salts or solvates, or pharmaceutically functional derivatives thereof. The invention further provides process for conjugating the compounds to carrier molecules and uses of such compounds and conjugates in the treatment of disease.

Abstract: The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.

Abstract: The invention relates to substituted heteroaryl derivatives, to methods for the production thereof, to medicaments containing said compounds and to the use of substituted heteroaryl derivatives for producing medicaments.

Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

Abstract: Synthesis of novel substituted indeno[1,2-b]indole derivatives of the type of 5,6,7,8-tetrahydroindeno[1,2-b]indole-9,10-diones and 5H-indeno[1,2-b]indole-6,9,10-triones, which show pronounced inhibition of the human protein kinase CK2, and the use thereof as active ingredients in medicaments and/or drug products in particular for the treatment of neoplastic diseases.

Abstract: The composition for the alkylation according to the present disclosure is characterized in that the composition contains the following cobalt complex. The method of detoxifying the harmful compound according to the present disclosure is characterized in that a harmful compound containing at least one element selected from the groups comprising arsenic, antimony and selenium is detoxified by the alkylation of the harmful compound, in the presence of the composition according to the present disclosure.

Abstract: The present invention provides a polymeric agent which can incorporate a large amount of a drug, accumulate selectively in a tumor site, and has a molecular size of more than that for renal excretion. A metalloporphyrin derivative (such as zinc protoporphyrin) is associated with a styrene-maleic acid copolymer via non-covalent bond to give a SMA micelle complex, allowing provision of a polymeric pharmaceutical agent for treatment of cancer with a large amount of the drug incorporated. The SMA micelle complex can be produced by a method, wherein the metalloporphyrin derivative reacts with the styrene-maleic acid copolymer in the absence of a condensation agent under an alkaline condition, solubilized, adjusted to have a pH of 6-8, and subjected to a procedure for separating a polymer component to recover the micelle complex component for the polymeric pharmaceutical agent.