Abstract: The present invention relates to novel tricyclic compounds of formula (I) and (II) More particularly, the present invention relates to novel tricyclic compounds of formula (I) and (II) and process of preparation of these compounds from 4,5-di-methyl-o-phenylinediamine. Further, the present invention relates to a process for preparation of tricyclic compound hunanamycin A.

Abstract: The invention relates to compounds of formula I wherein is a bond or is absent, V is CH, CR6 or N; R0 is H or, if is a bond, may also be alkoxy; R1 is H or halogen; U is CH or N when is a bond, or, if is absent, U is CH2, NH or NR9; R2 is H, alkylcarbonyl or —CH2—R3; R3 is H, alkyl or hydroxyalkyl; R4 is H or, if n is not 0 and R5 is H, may also be OH; R5 is H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; R6 is hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH2)q—NR7R8, q being 1, 2 or 3 and each of R7 and R8 independently being H or alkyl or R7 and R8 forming with the N atom bearing them a ring; R9 is alkyl or hydroxyalkyl; A is —(CH2)p—, —CH2CH2CH(OH)— or —COCH2CH(OH)—; G is substituted phenyl or G1 or G2 wherein Q is O or S and X is CH or N; and Y1, Y2 and Y3 may each be CH or N; and n is 0 when A is —CH2CH2CH(OH)— or —COCH2CH(OH)—, and n is 0, 1 or 2 when A is —(CH2)p—, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to salts there

Abstract: Compounds of Formula (I), their preparation, and use in preventing or treating a bacterial infection are disclosed.

Abstract: This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.

Abstract: The present invention discloses pyridoindolobenz[b,d]azepines compositions of Formula 1, wherein Y is a single bond or a double bond. A and B are independently —(CH2)n—; and ‘n’ varies from 0 to 3. R1 to R10 are various electron donating, electron withdrawing, hydrophilic, or lipophilic groups selected to optimize the physicochemical and biological properties of compounds of Formula I.

Abstract: Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.

Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

Abstract: The present invention relates to a novel family of protein kinase inhibitors of Formula I: as well as to the processes of preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative, inflammatory, autoimmune or infectious diseases, disorders, or conditions in which protein kinase activity is implicated.

Abstract: The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.

Abstract: Indoline derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indoline derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.

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 disclosure describes bicyclic heteroaromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

Abstract: Provided are benzopyran compounds of formula I, for example, pomiferin-3?,4?-dimethyl ether, and the use of such compounds and compositions thereof to modulate (e.g., inhibit) melanogenesis and pigmentation. wherein R3, R4, R5, R6, R7 and R8 are described herein. Also provided are plant extracts containing a compound of formula I, and the use of such a plant extract to modulate (e.g., inhibit) melanogenesis and pigmentation. The compound or plant extract may be prepared as pharmaceutical and cosmetic compositions, and may be used for the prevention and treatment of conditions that are related to aberrant melanogenesis activity.

Abstract: The present invention relates to new generation of triazole functionality containing 6-nitro-2,3-dihydroimidazooxazole agents for general formula I, their method of preparation and their use as drugs for treatment of tuberculosis, MDR-TB and XDR-TB either alone or in combination with other anti-tubercular agents.

Abstract: The present invention relates to the use of a class of novel isothiazolo[4,3-b]pyridine derivatives as well as to pharmaceutical compositions comprising one or more of said isothiazolo[4,3-b]pyridine derivatives and one or more pharmaceutically acceptable excipients as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as viral diseases.

Abstract: The substituted spirooxindoles are MDM2-p53 inhibitors bearing a benzylidine (styryl) arm and have a complex fused ring system ideally suited for binding to the MDM2 protein, thereby interrupting its protein-protein interaction (PPI). Sixteen compounds, designated 4a-4p, were synthesized in a simple smooth method using an asymmetric 1,3-dipolar reaction as the key step. Testing showed that the compounds exhibit anti-cancer activity against various forms of cancer cells affecting humans.

Abstract: Provided are amido spirocyclic amide and sulfonamide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.

Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.

Abstract: Chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with P13 kinase activity are described herein.

Abstract: Disclosed are hexacoordinate silicon-containing precursors, methods of synthesizing the same, and methods of using the same to deposit silicon-containing films using vapor deposition processes for manufacturing semiconductors, photovoltaics, LCD-TFT, flat panel type devices, refractory materials, or aeronautics. The hexacoordinate silicon-containing molecule have the following formula: (I), wherein each L1, L2, L3 and L4 is independently selected from oxygen or nitrogen atoms; L1 and L2 are joined together via a carbon bridge having one to three carbon atoms; L3 and L4 are joined together via a carbon bridge having one to three carbon atoms; L1, L2 and the carbon bridge forming a monoanionic ligand bonded to silicon; and L3, L4 and the carbon bridge form a monoanionic ligand bonded to silicon.

Abstract: Provided is an organic light-emitting device including a first electrode, a second electrode, an emission layer between the first electrode and the second electrode, and a hole transport region between the first electrode and the emission layer, wherein the hole transport region includes an auxiliary layer, the auxiliary layer including at least one amine-based compound represented by Formula 1: where R11, R12, R13, R14, R15, R16, X11, L11, L12, L13, a11, a12, a13, b15, and b16 are as defined in the specification.

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: The subject matter disclosed herein relates to compositions and methods of making and using the compositions. In a further aspect, the subject matter disclosed herein relates to inhibitors of STAT3 dimerization. Methods of making these compositions as well as compositions comprising these compositions are also disclosed. Also disclosed are methods of treating or preventing certain cancers by administering to an individual in need thereof and effective amount of the compounds disclosed herein. Still further, disclosed herein are methods of inhibiting STAT3 by contacting a cell with a compound or composition as disclosed herein.

Abstract: The present discovery pertains to the discovery of certain amphiphilic compounds that may be useful for the management of sebum secretion in subjects with acne, oily skin, or seborrheic dermatitis. These compounds are 1-dialkylphosphorylalkanes with the longest alkyl group being seven or more carbons. Preferably, a compound is dissolved in a dermatologically acceptable vehicle, and delivered to the skin in a solution, gel, lotion, cream, or ointment. The method of application may be with the surface of the finger, or via an applicator. The decrease is sebum secretion in certain subjects may result in skin conditions that enhance cosmetic appearance and ameliorate skin disorders.

Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or prodrug thereof, wherein the groups are as defined in the claims. Further aspects of the invention relate to pharmaceutical compositions comprising compounds of formula (I), and the use of compounds of formula (I) in the preparation of a medicament for treating a viral disorder.

Abstract: Compounds of Formula I: and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.

Abstract: The present disclosure is related to a pharmaceutical composition for treatment of cancer comprising a cyclometalated N-heterocyclic carbene complex. The cyclometalated N-heterocyclic carbene complex contains a gold(III) or a platinum(II) atom. The pharmaceutical composition possesses anti-cancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of topoisomerase and/or poisoning of topoisomerase.

Abstract: The present invention relates to methods for the synthesis of fondaparinux and intermediates thereto.

Abstract: The present invention provides N-alkyl 2-(disubstituted)alkynyladenosine-5?-uronamides and derivatives thereof and pharmaceutical compositions containing the same that are selective agonists of A2A adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.

Abstract: The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).

Abstract: This invention relates to the application of hydroxyapatite chromatography to the purification of at least one antibody from a preparation containing high molecular weight aggregates. Further, this invention relates to an integration of ceramic hydroxyapatite chromatography into a combination chromatographic protocol for the removal of high molecular weight aggregates from an antibody preparation.

Abstract: Benzodiazepine dimers having a structure represented by wherein R1 is wherein the variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).

Abstract: Racemization-free methods are disclosed for the synthesis of carfilzomib. Novel intermediates and methods of making carfilzomib employing fragment condensation using the novel intermediates are disclosed. Amorphous carfilzomib and methods of making same are disclosed.

Abstract: The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degarelix, its protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degarelix itself. Degarelix can be obtained by subjecting a Degarelix precursor according to formula II: (P1)AA1-AA2-AA3-AA4(P4)-AA5-AA6(P6)-AA7-AA8(P8)-AA9-AA10-NH2 (II) or a salt or solvate thereof, to a treatment with a cleaving agent in an organic solvent, wherein P1 is an amino protecting groups; preferably acetyl; P4 is hydrogen or a hydroxyl protecting group, preferably a hydroxyl protecting group; P6 is hydrogen or an amino protecting groups; preferably an amino protecting groups; and P8 is an amino protecting group.

Abstract: Disclosed are novel compounds having NPR-B agonistic activity. Preferred compounds are linear peptides containing 8-13 conventional or non-conventional L- or D-amino acid residues connected to one another via peptide bonds.

Abstract: Provided are a substance capable of binding to EGFR specifically with a high affinity and a pharmaceutical agent containing the substance. A peptide which contains at least an amino acid sequence is represented by the formula (1), (2) or (3), as described in the specification, and is composed of 12 to 50 amino acids: (SEQ?ID?NO:?55) X1-His-X2-X3-Asp-X4-X5-X6-X7-X8-Trp-His(1) (SEQ?ID?NO:?56) Phe-His-Asp-Trp-X11-Pro-X12-X13-X14-X15-X16-X17(2) (SEQ?ID?NO:?57) Leu-His-X21-Ser-X22-Trp-Met-X23-X24-X25-X26-X27(3).

Abstract: The present disclosure relates to a polypeptide having multiple directionality and a self-assembled nanostructure containing the same. Since R1 and R3 domains having ?-sheet structures are arranged to have antiparallel structures, it provides a more stabilized ?-helix structure than the existing polypeptide having single directionality. In addition, since the polypeptide of the present disclosure is prepared as an antiparallel pseudo-cyclic structure without additional structural element such as a linker, the associated synthesis process is simple and the molecular weight is relatively small. Since the polypeptide having multiple directionality having the structural and functional characteristics described above and a self-assembled nanostructure containing the same have excellent stability and transportability, they are applicable in various fields as drugs, for detection of substances in vivo, for targeting for drug delivery, and for inhibiting protein-mediated biomacromolecular interactions.

Abstract: In one aspect, the invention relates to a composition including a first polypeptide having the sequence set forth in SEQ ID NO: 1 and a second polypeptide having the sequence set forth in SEQ ID NO: 2. In one embodiment, the composition includes about 120 ?g/ml of a first polypeptide including the amino acid sequence set forth in SEQ ID NO: 1, 120 ?g/ml of a second polypeptide including the amino acid sequence set forth in SEQ ID NO: 2, about 2.8 molar ratio polysorbate-80 to the first polypeptide, about 2.8 molar ratio polysorbate-80 to the second polypeptide, about 0.5 mg/ml aluminum, about 10 mM histidine, and about 150 mM sodium chloride. In one embodiment, a dose of the composition is about 0.5 ml in total volume. In one embodiment, two-doses of the composition induce a bactericidal titer against diverse heterologous subfamily A and subfamily B strains in a human.

Abstract: This disclosure relates to graphene derivatives, as well as related devices including graphene derivatives and methods of using graphene derivatives.

Abstract: The present invention relates to compositions and fusion proteins containing at least two Mycobacterium sp. antigens, and polynucleotides encoding such compositions and fusion proteins. The invention also relates to methods for their use in the treatment, prevention and/or diagnosis of tuberculosis infections.

Abstract: The invention relates to lentiviral vector particles pseudotyped with a determined heterologous viral envelope protein or viral envelope proteins originating from a RNA virus and which comprise in its genome at least one recombinant polynucleotide encoding at least one polypeptide(s) carrying epitope(s) of an antigen of a Plasmodium parasite capable of infecting a mammalian host. The lentiviral vector particles are used in order to elicit an immunological response against malaria parasites.

Abstract: A recombinant Flagrp170 protein and pharmaceutical compositions comprising a Flagrp170 protein and related molecules encoding same, and cells presenting such a protein are provided. The Flagrp170 protein comprises an NF-KB-activating domain of Flagellin and an ATP-binding domain truncated Grp170. The pharmaceutical compositions of the invention can be used for the treatment or prevention of cancer or infectious disease.

Abstract: A method of preventively treating a subject at the risk of developing infections of a respiratory virus is disclosed. The method includes a step of administering to the subject an effective amount of a peptide synthesized through a chemical route or by a genetic engineering process, characterized in that the peptide has a functional domain capable of binding to a surface glycoprotein of a respiratory virus and has an activity of inhibiting infection of the respiratory virus, wherein the peptide has 5 or more basic amino acids, among which 2 or more basic amino acids are in N-terminal region or C-terminal region of the peptide; and wherein the peptide consists of an amino acid sequence that is at least 90% identical to SEQ ID NO: 10. The invention also discloses the mechanism of the peptides in inhibition of said infections, which provides theory support for developing new prophylactic/therapeutic agents with broad-spectrum antiviral activities.

Abstract: Disclosed are yeast expression constructs encoding a polypeptide containing a signal sequence, a Golgi-directing pro sequence, and a human amyloid beta protein, and mammalian expression constructs encoding a polypeptide containing a selected signal sequence and a human amyloid beta protein. Also disclosed are methods of screening cells to identify compounds that prevent or suppress amyloid beta-induced toxicity and genetic suppressors or enhancers of amyloid beta-induced toxicity. Compounds identified by such screens can be used to treat or prevent neurodegenerative disorders such as Alzheimer's disease.

Abstract: The present invention relates, inter alia, to certain hepcidin peptide analogs, including peptides and dimers thereof, and to the use of the peptides and peptide dimers in the treatment and/or prevention of a variety of diseases, conditions or disorders, including treatment and/or prevention of iron overload diseases, which include hereditary hemochromatosis and iron-loading anemias, and other conditions and disorders described herein.

Abstract: A method for crystallizing insulin or insulin analogs under alkaline conditions and purifying the insulin or insulin analog crystals by filtering through a filter and drying the insulin or insulin analog crystals captured on the filter to produce crystalline insulin or insulin analog crystal compositions is described. In particular aspects, the method may be used to crystalize insulin glargine.

Abstract: An electromagnetic band gap element is provided. In the electromagnetic band gap element, a first planar conductor and a second planar conductor are respectively formed on a first plane and a second plane which are parallel to each other, and a first linear conductor is formed on at least one third plane that is parallel to the first plane and the second plane and is located between the first plane and the second plane. The first planar conductor and the second planar conductor are connected via the first linear conductor.

Abstract: The present invention discloses cryopreserved recombinant cells for screening drug candidates that transiently overexpress one or more drug transporter proteins and/or drug metabolizing enzymes. Advantageously, such cells provide a cost-efficient consumable product that streamlines the process of screening whether drug candidates are substrates or inhibitors of drug transporter proteins and/or drug metabolizing enzymes.

Abstract: This invention provides a method for inhibiting the rejection of transplanted islet cells, comprising administering to the subject a polypeptide comprising all or a portion of the extracellular domain of ILT3, wherein the polypeptide is water soluble. This invention further provides a method of treating diabetes, by inhibiting the rejection of transplanted islet cells through the administration of the polypeptide to the subject.

Abstract: Disclosed is a T cell receptor (TCR) having antigenic specificity for an HLA-A2-restricted epitope of human papillomavirus (HPV) 16 E6, E629-38. Related polypeptides and proteins, as well as related nucleic acids, recombinant expression vectors, host cells, and populations of cells are also provided. Antibodies, or an antigen binding portion thereof, and pharmaceutical compositions relating to the TCRs of the invention are also provided. Also disclosed are methods of detecting the presence of a condition in a mammal and methods of treating or preventing a condition in a mammal, wherein the condition is cancer, HPV 16 infection, or HPV-positive premalignancy.