Abstract: The present disclosure relates to novel compounds having vitamin D receptor agonist and histone deacetylase inhibitory efficacy as well as methods for reducing or inhibiting the proliferation of cancer cells or for treating cancer.

Abstract: Three unique subtypes of N-hydroxyamides and N-hydroxycarbamates containing both the vanilloid moiety (4-hydroxy-3-methoxybenzyl) and a lipophilic aliphatic moiety. Also disclosed are direct syntheses of these vanilloid fatty hydroxamates. The compounds possess inhibitory activity against the enzymes fatty acid amide hydrolase (FAAH) and matrix metallo-proteinase 9 (MMP-9). In addition, these substances bind to the calcium channel protein TRPV1 and inhibit vesicant-induced inflammation in skin and cornea. The compounds have utility in treating topical or systemic inflammatory processes in the skin and/or eye.

Abstract: Compositions and methods for inhibiting translation initiation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using N,N?-diarylureas and/or N,N?-diarylthiourea compounds are described.

Abstract: The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C disorders, including diseases and disorders mediated by GPCRs.

Abstract: Novel compounds of the general formula: in which X represents a polymer, Q represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; each of R1 and R2 independently represents a hydrogen atom or a C1-4alkyl group; and either Z1 represents a protein or a peptide linked to CR2 via a nucleophilic moiety, and Z2 represents a molecule linked to CR2 via a nucleophilic moiety, or Z1 and Z2 together represent a single group derived from a protein or peptide linked to CR2 via two nucleophilic moieties.

Abstract: A compound comprising: (a) a drug carrier comprising coumarin-labeled-cysteine tethered mesoporous silica nanoparticles (MSNs) loaded with a pharmaceutically active agent, and (b) a fluorescein isothiocyanate-?-cyclodextrin (FITC-?-CD) covalently linked to said cysteine and blocking the release of said pharmaceutically active agent from said nanoparticles, wherein cleavage of said covalent linkage removes said cyclodextrin and releases said pharmaceutically active agent, and said coumarin and said fluorescin form a donor-acceptor pair so that said drug carrier has a first emission wavelength when the covalent linkage is intact and the cyclodextrin said present and a second emission wavelength after cleavage of said covalent linkage to remove said cyclodextrin and release said pharmaceutically active agent.

Abstract: The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.

Abstract: Provided are compounds according to the following Formula I: The Formula I compounds are activated in the presence of reactive oxygen species (ROS) and are therefore selective anti-cancer therapeutics for cancers associated with elevated ROS. Also provided are methods and pharmaceutical compositions for treating cancers associated with increased ROS.

Abstract: The present invention provides a new class of peptides related to rapid replication and high human mortality, and their use in diagnosing, preventing and treating disease including vaccines and therapeutics for emerging viral diseases and methods of identifying the new class of peptides and related structures.

Abstract: The present invention relates to identification of a compound which inhibits the enzyme NMPRTase and glioma cancer cell growth and further used for glioma therapy. Pre-B-cell colony enhancing factor 1 gene (PBEF1) encodes nicotinamide phosphoribosyltransferase (NMPRTase), which catalyzes the rate limiting step in the salvage pathway of NAD metabolism in mammalian cells. PBEF1 transcript and protein levels have been shown to be elevated in glioblastoma and a chemical inhibitor of NMPRTase has been shown to specifically inhibit cancer cells. Here a structure based drug discovery approach has been reported with an aim to develop novel inhibitors for glioblastoma therapy. Present invention relates to virtual screening using docking of ligands from a large library of 13,000 compounds against NMPRTase as the macromolecular target resulting in short listing of 34 possible ligands, of which six were tested experimentally, using the NMPRTase enzyme inhibition assay and further with the glioma cell viability assays.

Abstract: The invention discloses novel 42-0-(heteroalkoxyalkyl) rapamycin compounds of formula (1) and process for preparation thereof. These compounds are useful in the treatment of hyperproliferative vascular diseases such as restenosis and atherosclerosis Wherein, R denotes 3, 4 and 5 membered 3-hydroxy heteroalkoxyalkyl compounds selected from Tetrahydrofuran-3-ol, Oxetan-3-ol, Tetrahydropyran-3-ol, Tetrahydro-4- methyl furan-3-ol, Tetrahydro-2,5,5-trimethyl furan-3-ol, Tetrahydro-2,5-diethyl-2-methyl furan-3-ol, Tetrahydro-6-methoxy-2-methyl 2H-Pyran-3-ol and Tetrahydro-2,2-dimethyl-6-phenyl 2H-Pyran-3-ol.

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 kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.

Abstract: The invention relates to pharmaceutical compositions comprising: (a) at least one angiotensin receptor blocker or a pharmaceutically acceptable salt thereof, and (b) at least one chemokine receptor pathway inhibitor or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising: (a) at least one angiotensin receptor blocker or a pharmaceutically acceptable salt thereof; and (b) at least one chemokine receptor pathway inhibitor or a pharmaceutically acceptable salt thereof which inhibits a component of the chemokine receptor pathway other than the chemokine receptor. Oral sustained release pharmaceutical compositions comprising the pharmaceutical composition, as well as injectable sustained release pharmaceutical compositions comprising the pharmaceutical composition are described. The invention further relates to tablets, capsules, injectable suspensions, and compositions for pulmonary or nasal delivery comprising the pharmaceutical composition.

Abstract: The present invention relates to combination therapy using compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein and an additional pharmaceutically active agent. The invention also relates to pharmaceutical compositions comprising these combinations, and methods of using these combinations in the treatment of various diseases and disorders.

Abstract: A biometric mobile device is capable of interacting with existing cellular, wireless, and wired telecommunication and other communication networks to support intelligence gathering, human body identification, special operations and other applications. A method of collecting biometric data at an accident or crime scene may comprise, for example, utilizing a camera to photograph the accident scene, collecting key entered data that may not be otherwise obtainable, using a fingerprint scanner to collect, digitize and store fingerprint data, using a lab-on-a-chip DNA profile device for collecting and analyzing a DNA specimen and generating identification and DNA profile data for bar code entry and other means for collecting any known form of biometric data including, but not limited to, vascular facial structure, dental structure, cornea, iris or other data which may be unique or limiting for identification purposes.

Abstract: A measurement and testing system comprising a plurality of measurement assemblies and a data acquisition and processing device is disclosed. Each of the plurality of measurement assemblies includes a measurement surface for receiving at least one portion of a body of a subject; and at least one measurement device configured to sense one or more measured quantities and output one or more signals that are representative of the one or more measured quantities. In one embodiment, the data acquisition and processing device is configured to determine whether a load is being applied to a particular one of the plurality of measurement assemblies by a first or second body portion of the subject. In another embodiment, the data acquisition and processing device is configured to construct a first virtual measurement assembly from a first subset of measurement assemblies and a second virtual measurement assembly from a second subset of measurement assemblies.

Abstract: Provided herein, generally, are pharmaceutical formulations, e.g., injectable pharmaceutical formulations with improved stability, comprising morphine sulfate or a hydrate thereof, and methods of producing and using the same. Also provided herein are kits comprising the formulations, e.g., injectable morphine formulations.

Abstract: Presented herein are methods and compositions for determining haplotypes in a sample. The methods are useful for obtaining sequence information regarding, for example, HLA type and haplotype. Also presented herein are methods of determining haplotypes in a sample based on a plurality sequence reads.

Abstract: The present invention provides a piperidine compound represented by Formula (I) (wherein X1, X2, X2, A, B and N are as defined in the Description); or a salt thereof.

Abstract: Methods of determining levels of unbound metabolites are disclosed. Probes derived from fatty acid binding protein muteins are described that bind preferentially to a number of unbound metabolites including oleate, stearate, linoleate, palmitate, arachidonate and unconjugated bilirubin. A profile for a patient is determined using one or more of the described probes. The profile is useful in diagnosis of disease, particularly myocardial infarction, non-alcoholic fatty liver disease (NAFLD), diabetes, stroke, sepsis and neonatal jaundice. The responses of multiple probes to a test sample are used to classify the degree of acute coronary syndrome by comparison to multi-probe profiles generated from unstable angina, non ST elevation myocardial infarction, and ST elevation myocardial infarction.