Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.

Abstract: The invention provides compositions and methods for wound healing and scar reduction. The compositions and methods of the invention include at least one EP4 agonist set forth herein. Wounds and or scars that can be treated by the compositions and methods of the invention can arise from events such as surgery, trauma, disease, mechanical injury, burn, radiation, poisoning, and the like.

Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula I, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.

Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables RA, RAA, subscript n, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, R5, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

Abstract: The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.

Abstract: The present invention relates to indolizine compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of P2X7, and for the treatment of P2X7-related disorders.

Abstract: This disclosure relates to a one-step method for preparing the tau radiopharmaceutical, [18F]T807, using an unprotected or protected precursor (e.g., tert-butyl 7-(6-nitropyridin-3-yl)-5H-pyrido[4,3-b]indole-5-carboxylate).

Abstract: Disclosed are the ERK inhibitors of formula (1.0) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0). This invention provides compounds that are ERK inhibitors (i.e., ERK2 inhibitors). This invention also provides a pharmaceutical composition comprising an effective amount of at least one (e.g., 1) compound of formula (1.0) and a pharmaceutically acceptable carrier.

Abstract: A redox-active triangular prism is provided. The redox-active triangular prism includes a plurality of pure enantiomers selected from a group consisting of (?)-NDI-? and (+)-NDI-?. Methods for their preparation as solvent-templated supramolecular structures and a characterization of their redox-active behavior are provided.

Abstract: The disclosure relates to Compounds of Formula (1) : and pharmaceutically acceptable salts thereof wherein Z1, Z2, Z3, Xa, Xb, Xc, Y, X2, and X4 are as defined herein, compositions comprising an effective amount of a Compound of Formula (1) or a pharmaceutically acceptable salt thereof, and methods to treat or prevent a condition, such as cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (1) or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to the preparation of compounds, in particular to the preparation of compounds which may be used as intermediates for the preparation of antibiotics, preferably carbapenem antibiotics, more preferably ertapenem, and salts thereof.

Abstract: Disclosed herein are compounds such as those of Formula (I) that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Abstract: The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof; as further described herein. The present invention further provides pharmaceutical compositions comprising these compounds, and combinations comprising these compounds combined with or used with a therapeutic co-agent, as well as therapeutic uses of these compounds and compositions. These are useful in the treatment of diseases such as cancer that are associated with activation of ERK1 and/or ERK2, and especially for MAPK pathway dependent cancers showing resistance to Raf and/or MEK inhibitory cancer therapeutics.

Abstract: Provided herein are compounds that modulate the activity of inhibitor of apoptosis proteins (IAPs), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

Abstract: The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.

Abstract: Novel CFTR corrector compounds that are effective in rescuing halide efflux, delF508-CFTR protein processing, and apical functional chloride ion transport in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of rescuing halide efflux in a cell, correcting a processing defect of a delF508-CFTR protein in a cell, and correcting functional delF508-CFTR chloride channels in a cell are also provided.

Abstract: The present invention is directed to an improved process to convert morphine into noroxymorphone having economic and ecological advantages.

Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: Heterocycle amino alkyloxy substituted quinazoline derivatives as represented by the structural Formula (I) and pharmaceutically acceptable salts thereof, capable of inhibiting the activity of receptor tyrosine kinase EGFR, and being used to treat cancers related to the expression of the receptor tyrosine kinase of the ErbB family are provided.

Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.

Abstract: The subject is to provide a liquid crystal compound satisfying at least one of physical properties such as a high stability to heat or light, a high clearing point (or a high maximum temperature), a low minimum temperature of a liquid crystal phase, a small viscosity, a suitable optical anisotropy, a large dielectic anisotropy, a suitable elastic constant and an excellent compatibility with any other liquid crystal compound, a liquid crystal composition including this compound and a liquid crystal display device including this composition. The compound is represented by the following formula (1a): wherein R1 is alkyl having 1 to 15 carbons or the like; ring A1, ring A2, ring A3 and ring A4 are independently 1,4-phenylene, naphthalene-2,6-diyl or the like; Z1 and Z2 are independently a single bond or the like; o and p are independently 0, 1 or 2; and n is an integer from 2 to 10.

Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

Abstract: The present invention relates to Rifaximin polymorphic forms, to their use in medicinal preparations and to therapeutic methods using them.

Abstract: Thiazoloquinolines and thiazolonaphthyridines with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.

Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Abstract: The present invention is directed to novel non-invasive diagnostic tools to image cancers, especially, leukemia and non-Hodgkin's lymphomas (NHL) with minimal toxicity in vivo. The present invention represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these cancers. The novel imaging probe is capable of detecting precancerous cells, as well as their metastatic spread in tissues. This represents a quantum step forward in the diagnosis and staging of NHL using non-invasively molecular imaging techniques. This novel probe will also be useful to monitor patients response to chemotherapy treatments and other interventions or therapies used in the treatment of NHL. Compounds according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.

Abstract: Provided are a nano structure, a fabrication method thereof, and an application device using the same. The nano structure includes: a substrate; a plurality of linkers formed over the substrate; and one or more metallic nanoparticles grown from a plurality of metal ions bonded to the linkers. In the nano structure, metallic nanoparticles may have an average particle diameter of about 0.5 to 3.0 nm.

Abstract: The invention relates to complexes of germanium with amino acids and carboxylic acids of the general formula Ge[OH]a[AA]b[CA]c (I), where AA is an amino acid, CA is a carboxylic acid, a=0÷3, b=1÷3, c=0÷3, and 1?b+c?4, wherein AA and AC in the complex can be identical or different, and to a method for preparing same. The method consists in preparing an aqueous suspension of germanium dioxide, adding an amino acid and a carboxylic acid to the aqueous suspension of germanium oxide produced, heating the mixture produced with agitation at a temperature of 40-100° C. for 2-14 hours with subsequent filtering, removal of the water and production of a complex in solid form. The method makes it possible to prepare stable complexes with a controllable composition and a controllable ratio of germanium to amino acid and carboxylic acid which are stable in solid form and can be used in medicine.

Abstract: A surface modified lithium titanate and preparation method thereof is provided. In the surface modified lithium titanate, the deactivating groups distributed on the surface of the lithium titanate are —O—P—RR?R?, —O—P—(OR)R?R?, —O—P—(OR)(OR?)R?, and —O—P—(OR)(OR?)(OR?), where R, R? and R? are identical or different C1˜C8 alkyl or alkenyl groups. The deactivating groups are bonded to the lithium titanate via a bond or a bridge. The exemplary surface modified lithium titanate can effectively lower its catalytic activity, reduce the gassing of lithium ion batteries, and therefore improve the high temperature storage and high temperature cycle performance of lithium titanate batteries. The exemplary preparation method is simple, has great repeatability, a low cost, low pollution to the environment, and is suitable for industrial production.

Abstract: A simple, commercially viable process for the preparation of phosphonic acid monomers containing essentially no diester or inorganic phosphorous acid compounds is disclosed.

Abstract: A palladium(II) complex which catalyzes the Sonogashira coupling reaction efficiently under aerobic condition and a method of employing the palladium(II) complex to synthesize internal alkynes. The palladium(II) complex is an effective catalyst for the coupling reactions of aryl iodo and diiodo compounds with unactivated alkyl alkynes and terminal dialkynes to produce various novel symmetrical dialkynes and disubstituted internal alkynes in excellent yields.

Abstract: A novel ligated reagent complex is provided. The ligated reagent includes at least one zero-valent atom, whether metal, metalloid, or non-metal, in complex with at least one hydride molecule and at least one nitrile compound. The ligated reagent complex can be useful in the synthesis of nanoparticles. Also provided is a method for preparing a ligated reagent complex. The method includes a step of ball-milling a mixture that includes a preparation containing a zero-valent element, a hydride molecule, and a nitrile compound.

Abstract: Various compositions and methods for Quasi-Amadori products and derivatives thereof are contemplated in which a halogenated carbohydrate is reacted with a primary amino group of an affinity ligand. In especially preferred aspects, the Quasi-Amadori product is formed from 2-fluorodeoxyglucose and an affinity moiety that preferentially or selectively binds to a neural cell or neural structure. Where contemplated compounds include 18F, PET imaging using compounds presented herein is especially preferred.

Abstract: This application is directed to the use of aminosteroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.

Abstract: A hydrophobic cationic steroidal anti-microbial (ceragenin) compound forms an amphiphilic compound having a hydrophobic sterol face and a hydrophilic cationic face. The hydrophobic CSA also includes a hydrophobic substituent that gives the ceragenin compound a C Log P value of at least 6.0, 6.25, 6.5, 7.5, 8.5, or 10.

Abstract: Described herein are compositions and methods useful to treat cancers. In addition, the present invention provides screening assays, diagnostic assays, methods to prognose, methods to treat, and kits.

Abstract: Provided is a method for preparing a compound represented by Formula I or a salt thereof, wherein Coleophoma empetri F-11899 (FERM BP2635) and/or a mutant strain thereof is cultured in a medium containing amino acid or a salt thereof, an insoluble organic source, and a sugar alcohol, to produce the compound of Formula I or a salt thereof.

Abstract: The invention relates to a method for inhibiting an ADAM protease, comprising inhibiting binding to an integrin-binding loop of a disintegrin domain in the ADAM protease. Also provided are cyclic peptides which inhibit binding to an integrin-binding loop of an ADAM protease, as well as associated pharmaceutical compositions, uses and methods of treatment.

Abstract: This disclosure relates to immunogenic compositions comprising mutant Streptococcus pneumonia pneumolysin (PLY) proteins. Nucleic acids, polypeptides encoded thereby, compositions containing the same, methods for using such nucleic acids, polypeptides and compositions are also provided.

Abstract: A peptide (Peptide-1) based on the C-terminal of Equine CC10 has been discovered that can be used as a vaccine to protect horses from respiratory airway obstruction (RAO). Antibodies to Peptide-1 may also be administered for short-term passive immunotherapy to RAO-affected horses, and can be used to measure the level of CC10 protein in serum to identify potential RAO horses (horses with reduced CC10). Due to similarities between equine RAO and human asthma, this peptide or its antibodies may also be useful in treatment or prevention of human asthma.

Abstract: Peptides from the Mucin 1 (MUC1) cytoplasmic domain and methods of use therefor are described. These peptides can inhibit MUC1 oligomerization, thereby preventing tumor cell growth, inducing tumor cell apoptosis and necrosis of tumor tissue in vivo.

Abstract: The present invention provides methods of improving the levels and stability of expression of interleukin-12 family cytokine polypeptides by expressing the alpha and beta subunits of the polypeptides at their determined relative molar ratios that increase the levels and stability of expression of the heterodimer, e.g., in comparison to heterodimer expressed at an equimolar ratio.

Abstract: Provided herein are IL-2 muteins and IL-2 mutein Fc-fusion molecules that preferentially expand and activate T regulatory cells and are amenable to large scale production. Also provided herein are variant human IgG1 Fc molecules lacking or with highly reduced effector function and high stability despite lacking glycosylation at N297. Also, provided herein are linker peptides that are glycosylated when expressed in mammalian cells.

Abstract: Preparations including recombinant FSH (rFSH).

Abstract: Peptide analogs of glucagon and peptide analogs of GLP1 are provided herein. Also provided herein are pharmaceutical compositions comprising the analogs, and methods of using the analogs for the treatment and/or prevention of conditions such as obesity and diabetes.

Abstract: High affinity PD-1 mimic polypeptides are provided, which (i) comprise at least one amino acid change relative to a wild-type PD-1 protein; and (ii) have an increased affinity for PD-L1 relative to the wild-type protein. Compositions and methods are provided for modulating the activity of immune cells in a mammal by administering a therapeutic dose of a pharmaceutical composition comprising a high affinity PD-1 mimic polypeptide, which blocks the physiological binding interaction between PD-1 and its ligand PD-L1 and/or PD-L2.

Abstract: Disclosed are methods and compositions for the inhibition of modulation of T cell costimulatory pathway by a pathogenic agent, particularly, the inhibition of activation of a T cell costimulatory pathway by a pyrogenic exotoxin. The direct interaction of a superantigen with a specific site within the dimer interface of a CD28 family member is inhibited using immunomodulatory peptides. Specific antagonist immunomodulatory peptides comprise amino acid sequences derived from a dimer interface of a T cell co-stimulatory pathway member, or peptides which comprise an amino acid sequence which specifically binds to an amino acid sequence within the dimer interface of a T cell co-stimulatory pathway member. Compositions comprising said peptides and methods for the treatment of immune-related disorders are also disclosed. Such molecules may be used in screening for a test substance which specifically binds to the CD28 molecule and is capable of antagonizing pyrogenic exotoxin-mediated activation of Th1 lymphocytes.

Abstract: Modified Protein A, Protein G, Protein L, or Protein A/G that lacks antibody binding activity, and methods of the modified protein's use for purifying antibodies is provided.

Abstract: The invention relates to compositions comprising immunoglobulin for use in the treatment of mucositis by topical application. In particular, the invention relates to compositions comprising J chain-containing IgA and secretory component for the treatment of mucositis.

Abstract: Cripto, a developmental oncoprotein, antagonizes activin and TGF-b signaling by forming a complex with activin and TGF-b and their type II receptors. This complex precludes the formation of a functional activin/TGF-b•type II•type I complex, thereby blocking the signaling of activin and TGF-b. Cripto may be generally capable of blocking antiproliferative Smad2/3 signals and provides a novel mechanism of oncogenic action with multiple therapeutic implications. Inhibiting the formation of Cripto and activin/TGF-b complex may enhance antiproliferative effects of activin and TGF-b.