Abstract: The present invention provides a compound having a superior serotonin 5-HT2C receptor activating action. The present invention relates to a compound represented by the formula (1) wherein ring A is an aromatic carbocycle optionally having substituent(s) or an aromatic heterocycle optionally having substituent(s), X is —N(R1)—, —O— or the like, when ring A is an aromatic carbocycle optionally having substituent(s), then R1 is a hydrogen atom, an alkyl group optionally having substituent(s), or the like, and when ring A is an aromatic heterocycle optionally having substituent(s), then R1 is a hydrogen atom, an alkyl group optionally having substituent(s), a cycloalkyl group optionally having substituent(s), or the like, is a single bond or a double bond, and n is an integer of 0, 1 or 2, or a salt thereof.

Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

Abstract: The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.

Abstract: The invention relates to novel phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor compounds of formula (I) and (II), which are conformationally restricted, and for which the meaning of the substituents are listed in the description. Preferred compounds are those wherein X isoxygen, R1 is morpholino and R2 is substituted phenyl or heteroaryl. These compounds are useful, either alone or in combination with further therapeutic agents, for treating disorders mediated by lipid kinases.

Abstract: The present invention provides methods and intermediates for the preparation of (1aR,12bS)-8-cyclohexyl-11-fluoro-N-((1-methylcyclopropyl)sulfonyl)-1a-((3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl)carbonyl)-1,1a,2,12b-tetrahydrocyclopropa[d]indolo[2,1-a][2]benzazepine-5-carboxamide (formula I), including pharmaceutically acceptable salts. The compound has activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract: The present invention relates to fungicidal N-[(trisubstitutedsilyl)methyl]carboxamide or its thiocarboxamide derivative, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.

Abstract: The present invention is directed to a mild, efficient, and general direct C(sp)-H bond silylation. Various embodiments includes methods, each method comprising or consisting essentially of contacting at least one organic substrate comprising a terminal alkynyl C—H bond, with a mixture of at least one organosilane and an alkali metal hydroxide, under conditions sufficient to form a silylated terminal alkynyl moiety. The methods are operable in the substantially absence of transition-metal compounds. The systems associated with these methods are also disclosed.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.

Abstract: This invention is directed to a process for producing a haloorganoalkoxysilane product comprising reacting an olefinic halide, an alkoxysilane, a catalytically effective amount of ruthenium-containing catalyst; and a reaction-promoting effective amount of a peroxy compound, optionally in the presence of an electron-deficient aromatic compound.

Abstract: The present invention refers to a process for the ruthenium-catalyzed trans-selective hydrostannation of alkynes and the so-obtained products. The inventive process makes use of a tin hydride which is reacted with an alkyne in the presence of a cyclopentadienyl-coordinated ruthenium catalyst.

Abstract: The present invention relates to a novel delivery system for delivering therapeutic agents into living cells, and more particularly, to novel chemical moieties that are designed capable of targeting and/or penetrating cells or other targets of interest and further capable of binding therapeutic agents to be delivered to these cells, and to delivery systems containing same.

Abstract: Provided is a catalyst for producing hydrogen, which catalyst has higher performance than conventional catalysts since, for example, it exhibits a certain high level of activity in an aqueous formic acid solution at high concentration even without addition of a solvent, amine and/or the like. The metal phosphine complex is a metal phosphine complex represented by General Formula (1): MHm(CO)Ln, wherein M represents an iridium, iron, rhodium or ruthenium atom; in cases where M is an iridium or rhodium atom, m=3 and n=2, and in cases where M is an iron or ruthenium atom, m=2 and n=3; and the number n of Ls each independently represent a tri-substituted phosphine represented by General Formula (2): PR1R2R3. The catalyst for producing hydrogen comprises the metal phosphine complex as a constituent component.

Abstract: The present invention provides a raw material, formed of a ruthenium complex, for producing a ruthenium thin film or a ruthenium compound thin film by a chemical deposition method, wherein the ruthenium complex is a ruthenium complex represented by the following formula, in which carbonyl groups and a fluoroalkyl derivative of a polyene are coordinated to ruthenium.

Abstract: Oxygen levels in biological tissue or systems can be measured by the phosphorescence quenching method using phosphorescent porphyrin probes, also referred to as a dendritic oxygen probes, with controllable quenching parameters and defined biodistributions. Provided are a “next generation” of oxygen sensors with substantially improved phosphorescence emission for better imaging capabilities, ease of use, increasing the quantum efficiency (phosphorescence intensity) and extending their range of applicability including constructing a class of oxygen sensors for making measurements in organic media. In addition, provided are methods for synthesizing new porphyrin constructs in which the porphyrin is made less flexible and more planar, changing with decrease internal quenching, and thereby increasing the phosphorescence emission used for oxygen sensing.

Abstract: The present teachings relate to compounds and compositions for treatment of cancers. In some embodiments, the composition comprises a platinum (IV) complex having at least one carboxylate or carbamate ligand.

Abstract: The invention concerns a pentasaccharide compound of formula (I) and the salts thereof. The invention also concerns a pharmaceutical composition comprising the synthetic pentasaccharide compound of formula (I) and its salts. The invention further concerns these compounds for use as a medicament, and in particular intended to treat blood clotting disorders, to prevent ischaemia reperfusion injury associated with solid organ transplantation, or to reduce the risk of blood clotting in an extracorporeal blood circuit during cardiac surgery, extracorporeal membrane oxygenation, or during circulatory assistance such as artificial heart.

Abstract: The present invention provides a compound of formula A: or a pharmaceutically acceptable salt thereof, wherein B, Q, R1, R5, R6, R7, R8 and Z are as defined herein, which is a 2?-branched nucleoside useful for the treatment or prevention of viral infections, particularly dengue fever, yellow fever, West Nile virus, Japanese encephalitis virus, tick-borne encephalitis virus, Kunjin virus, Murray Valley encephalitis, St Louis encephalitis, Omsk hemorrhagic fever virus, bovine viral diarrhea virus, Zika virus and Hepatitis C virus.

Abstract: Bringing membrane proteins into aqueous solution generally requires the use of detergents or other amphiphilic agents. The invention provides a new class of amphiphiles, each of which includes a multi-fused ring system as a lipophilic group. These new amphiphiles confer enhanced stability to a range of membrane proteins in solution relative to conventional detergents, leading to improved structural and functional stability of membrane proteins, including integral membrane proteins. Accordingly, the invention provides new amphiphiles for biochemical manipulations and characterization of membrane proteins. These amphiphiles display favorable behavior with membrane proteins and can be used to aid the solubilization, isolation, purification, stabilization, crystallization, and/or structural determination of membrane proteins.

Abstract: The present invention provides intermediates for preparing abiraterone, and processes for preparing abiraterone and intermediates thereof. The intermediates include a compound of formula (IV): wherein R represents a hydroxy-protecting group.

Abstract: Disclosed is a process for the preparation of abiraterone and abiraterone acetate with high yields and purity. A key element of the method is the isolation of a crystalline intermediate that makes the process particularly suitable for implementation on an industrial scale. There is also provided a process for the production of abiraterone acetate by acetylation of abiraterone in the absence of bases or acetylation catalysts.

Abstract: A process is disclosed wherein, using either 17a-(3-hydroxypropyl)-6p,7p;15p,16p-dimethylene-5p-androstane-3p,5,17p-triol (II) or 3?,5^ïI^?^-6?,7?;15?,16?-dimethylene-5?,17?-pregnane-21,17-carbolactone (III) as starting material, through a single-step reaction it is obtained drospirenone (I), a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action.

Abstract: The present invention disclosed N-acetyl amino acid ester derivatives of betulin and the preparation method thereof, the method comprising the steps that in the presence of an alkaline substance, a catalyst and a racemization-inhibitor, the carboxyl group of N-acetyl amino acid is activated by a coupling agent; and then the activated N-acetyl amino acid is reacted with betulin via esterification reaction to obtain the N-acetyl amino acid ester derivative of betulin. The present invention provided a simple synthesis method to synthesize the N-acetyl amino acid ester derivatives of betulin by using betulin as a precursor compound and modifying the molecular structure of betulin. Such structural modification of betulin significantly enhances the anti-tumor activity of the betulin derivatives and therefore has important values.

Abstract: Disclosed herein are novel A-ring epoxidized triterpenoid compounds and derivatives thereof, including those of the formula (I), wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example as antioxidant inflammation modulators, and compositions thereof are also provided.

Abstract: The present invention relates to a compound of formula (I) AA-AA-AA-R1—R2 (I) wherein, in any order, 2 of said AA (amino acid) moieties are cationic amino acids and 1 of said AA is an amino acid with a lipophilic R group, the R group having 14-27 non-hydrogen atoms; R1 is a N atom, which may be substituted by a branched or unbranched C1-C10 alkyl or aryl group, which group may incorporate up to 2 heteroatoms selected from N, O and S; and R2 is an aliphatic moiety having 2-20 non-hydrogen atoms, said moiety being linear, branched or cyclic. The invention further relates to formulations containing these compounds, solid supports having these compounds attached thereto, the use of these compounds in therapy, particularly as antimicrobial, anti-tumor or anti-biofilm agents and non-therapeutic uses of these compounds, particularly their use in inhibiting biofilm formation or removing a biofilm.

Abstract: The present application discloses a method for treating microbial infection using an antimicrobial composition comprises antimicrobial peptide which contains at least one VGFPV motif.

Abstract: The invention provides a novel peptide, and derivatives thereof, which is stable in aqueous solution and which stimulates proliferation and survival of endothelial cells and/or fibroblasts. The present peptide can be used at least to promote the S phase of the cell cycle, to stimulate production of extracellular matrix proteins, to reduce apoptosis, to inhibit production of reactive oxygen species and/or to reduce or prevent damage to cell integrity or morphology under stress conditions of serum deprivation.

Abstract: Compositions with antifungal activity and methods of using such compositions are provided herein. In particular the compositions are peptides of SEQ ID NO: 1 and variations thereof. The peptides may contain L or D amino acids and may be circularized, dimerized or otherwise modified to make the compositions resistant to proteolysis. The compositions may be used to inhibit microbial growth and in particular fungal growth.

Abstract: The present invention provides inventive stitched polypeptides, pharmaceutical compositions thereof, and methods of making and using inventive stitched polypeptides.

Abstract: This invention relates to modified antibiotic peptides, particularly for use in medicine. The invention further relates to compositions and methods for destroying microorganisms, such as bacteria, viruses or fungi, and to methods for treating microbial infections. The object of the invention is to develop novel antibiotic peptides, particularly having enhanced antibiotic activity and an expanded spectrum of activity against other strains of bacteria, particularly gram-positive bacteria such as Staphylococcus aureus. According to the invention, the object is attained in a first aspect by a peptide according to claim 1.

Abstract: This invention provides novel methods of stabilizing peptides and peptides so stabilized. In certain embodiments the methods involve providing a peptide containing at least two S bearing residues within the peptide; and reacting the peptide with a di-halogen-aryl-compounds to form a bis(thioether)-aryl-bridge between said two residues.

Abstract: The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, treat a blood coagulation disorder in a subject, purify TFPI, and identify a TFPI-binding compound.

Abstract: ?-Hairpin peptidomimetics of the general formula cyclo(-Tyr1-His2-Xaa3-Cys4-Ser5-Ala6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Aaa14-DPro15-Pro16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa3, Xaa7, Xaa8, Xaa13 and Xaa14 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

Abstract: The disclosure is generally directed toward the design and synthesis of peptide amphiphile (PA) molecules that comprises a peptide configured to inhibit angiogenesis. The peptide amphiphile comprises a hydrophobic tail, peptide sequence capable of beta-sheet formation; and a peptide, wherein the peptide is configured to inhibit angiogenesis. Optionally the PA further comprises a flexible linker between the peptide sequence capable of beta-sheet formation and the peptides. Further this disclosure is directed to nanostructures comprising peptide amphiphiles configured to inhibit angiogenesis.

Abstract: The present invention relates to a novel cyclohexapeptide, to a method for the preparation of said cyclohexapeptide and to the use of said cyclohexapeptide.

Abstract: The template-fixed B-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-D-Pro-Pro), disulfide bond between Cys4 and Gys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for where cancer is mediated or resulting from CXCR4 receptor activity.

Abstract: The present invention provides a compound including a peptidomimetic which interacts sterically with the binding site of a F11R molecule, the peptidomimetic including a peptidomimetic having the SEQ ID NO: 4D. The present invention also provides a method for treating a disorder comprising administering peptide 4D to a mammal.

Abstract: Briefly described, embodiments of the present disclosure relate to isolated polypeptides useful for treatment of respiratory syncytial virus, and to methods and compositions for treating respiratory syncytial virus.

Abstract: The invention entails synthetic short peptides based on Rift Valley Fever Virus (RVFV) fusion protein. The peptides are broad-spectrum antivirals, and are useful for prophylactic treatment against or therapeutic treatment of infection by hemorrhagic fever viruses, such as RVFV, Ebola Virus, and Andes Virus, as well as vesicular stomatitis virus.

Abstract: The invention is the production of magnetosome-like structures in cells. The invention provides in vitro and in vivo diagnostic and therapeutic methods using eukaryotic cells expressing magnetosome-like structures that act as contrast agents.

Abstract: A chimeric polyvalent recombinant protein for use as a vaccine and diagnostic for Lyme disease is provided. The chimeric protein comprises epitopes of the loop 5 region and/or the alpha helix 5 region of outer surface protein C (OspC) types. The OspC types may be associated with mammaliran Borrelia infections.

Abstract: The present invention relates to stable formulations of Neisseria meningitis rLP2086 Subfamily B Antigens in immunogenic compositions. The present invention also relates to methods of preserving the conformation of Neisseria meningitis rLP2086 Antigens and methods for determining the potency of Neisseria meningitis rLP2086 antigens.

Abstract: The present invention relates to the preparation and use of recombinant variants of group 6 allergens of the Poaceae (true grasses), which are characterized by reduced IgE reactivity compared with known wild-type allergens and at the same time substantially retained reactivity with T-lymphocytes.

Abstract: The present invention relates to a composition for regulating circadian rhythms, a composition for diagnosing circadian rhythm disorders and a diagnostic kit, wherein the composition for regulating circadian rhythms comprises NQ peptides, C12orf39 genes, NQ peptides cDNA and the like, which relate to circadian regulation in vertebrates as main components.

Abstract: Apparatus and methods for generating a solution rich in interleukin-1 receptor antagonist from a tissue comprising cytokine-producing cells. The apparatus can include a filter used with a separation system. The separation system can include a float.

Abstract: Two antigenic and immunogenic proteins of the cattle tick, Rhipicephalus microplus, and the genes encoding these proteins, are effective for eliciting a protective immune response that controls and prevents infestations of bovines and other livestock by the tick. The proteins isolated from the cattle tick include an aquaporin protein and a TC5777 gut membrane protein. Each of the proteins elicit an immunoprotective response in livestock to the cattle tick, and can be formulated and administered as vaccines. Alternatively, the isolated DNA sequences which encode these proteins can be incorporated into nucleic acid constructs which could be utilized as DNA vaccines. The nucleic acid constructs can also be used for the transformation of cells and the production of recombinant proteins. Induction of the protective immune response controls and prevents infestations of the treated animals with the tick, thereby protecting them against tick-borne pathogen transmission.

Abstract: The CA125 gene has been cloned and multiple repeat sequences as well as the carboxy terminus have been identified. The CA125 molecule comprises three major domains: an extracellular amino terminal domain (Domain 1); a large multiple repeat domain (Domain 2); and a carboxy terminal domain (Domain 3) which includes a transmembrane anchor with a short cytoplasmic domain. The amino terminal domain is dominated by its capacity for O-glycosylation and its resultant richness in serine and threonine residues. An amino terminal extension is presented, which comprises four genomic exons. The molecular structure is dominated by a repeat domain comprising 156 amino acid repeat units, which encompass the epitope binding sites. More than 60 repeat units have been identified, sequenced, and contiguously placed in the CA125 domain structure. More specifically, this invention is directed to a CA125 cDNA sequence which can be introduced into animal or human cells to achieve transcription or expression of the cDNA.

Abstract: Polypeptides are susceptible to denaturation or enzymatic degradation in the blood, liver or kidney. Due to the low stability of some polypeptides, it has been required to administer polypeptide drugs in a sustained frequency to a subject in order to maintain an effective plasma concentration of the active substance. Furthermore, pharmaceutical compositions of therapeutic peptides preferably have a shelf-life of several years in order to be suitable for common use. However, peptide compositions are inherently unstable due to sensitivity towards chemical and physical degradation. In part, the invention provides SAP variant proteins, compositions, pharmaceutical preparations and formulations having a prolonged in vivo half-life, prolonged shelf-life, or rather increased in vitro stability, or increased manufacturing efficiency compared to human SAP. Advantages of increased plasma half-life include, but are not limited to, reducing the amount and/or frequency of dosing.

Abstract: The present invention pertains to stabilized A? oligomer compositions. Methods for generating stabilized A? oligomer compounds are also provided herein. Additionally, screening assays employing the A? oligomer compounds and methods for generating therapeutics with the A? oligomers are also provided. In a particular embodiment, the A? oligomer described herein is comprised of A?42 peptide.

Abstract: The NK1 fragment of hepatocyte growth factor (HGF) binds to and activates the Met receptor, a transmembrane receptor tyrosine kinase that plays a critical role in embryonic development and organ formation. The instant application discloses NK1 variant polypeptides which act as agonists or antagonists of HGF. Further disclosed are covalently linked NK1 variant polypeptides. Many of the disclosed variant polypeptides possess improved stability characteristics.

Abstract: The invention provides neuregulin antagonists and methods of using the neuregulin antagonists in delaying the time to tumor recurrence or preventing resistance of cancer cells to treatment with a therapeutic agent.