Abstract: Disclosed are compounds of Formula AA and Formula AB: wherein “Heteroaryl-1”, RA1, RA2, RB1, and RC are defined herein, which novel compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formulae AA and AB or their salts, and methods of treating neuropathic pain disorders using the same.

Abstract: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: The present invention relates to processes for preparing enantiopure Lupanine and Sparteine.

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 PI3 kinase activity, are described herein.

Abstract: Intermediates of Ertapenem of formula 2a wherein Np represents (I) or (II), and P1 and P2 represent carboxyl protecting groups, and their preparation methods. Compound 2a prepared by the present methods in solid form is amorphous. The present invention also relates to a composition comprising at least 95% of the intermediate of Ertapenem of formula 2a.

Abstract: The present invention relates to pyrazine derivatives of Formula I, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

Abstract: The instant invention relates to crystalline forms of MK-1775, an inhibitor of Weel kinase. Specifically, the instant invention relates to hemihydrates of MK-1775.

Abstract: A compound with the formula I: wherein: R2 is of formula II: where A is a C5-7 aryl group, X is selected from the group comprising: NHNH2, CONHNH2, formula III, formula IV, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and —Z—(CH2)n—, where Z is selected from a single bond, O, S and NH and n is from 1 to 3; or (ii) Q1 is —CH?CH—, and Q2 is a single bond; R12 is a C5-10 aryl group, optionally substituted by one or more substituents selected from the group comprising: halo, nitro, cyano, ether, C1-7 alkyl, C3-7 heterocyclyl and bis-oxy-C1-3 alkylene; R6 and R9 are independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo; where R and R? are independently selected from optionally substituted C1-12 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NHRR?, nitro, Me3Sn and halo; either: (a) R10 is H, and R11 is OH, ORA, where RA is C1-4 alkyl; (b) R10 and R11 form a nitrogen-carbon double bond between the n

Abstract: The present invention relates to a process for preparing ?-aminobutyryl substituted 5,6,7,8-tetrahydro[1,4]diazolo[4,3-?]pyrazin-7-yl compounds.

Abstract: New pyrrolotriazinone derivatives having the chemical structure of Formula (I) are disclosed; as well as process for theft preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).

Abstract: Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.

Abstract: Presently provided are IDO inhibitors and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosuppression associated with an infectious disease.

Abstract: The present invention relates to derivatives of benzimidazoles of formula (I) as disclosed herein as well as pharmaceutical compositions comprising said derivatives. The derivates according to the present invention are serine/threonine and tyrosine kinase-inhibitors, particularly of PIM1-3- and DYRK1A-kinases and may particularly be used in the treatment of diseases linked to these kinases, such as e.g. leukemias, lymphomas, solid tumors and autoimmune disorders.

Abstract: Dipicolylamine compounds of Formula (I) set forth herein. Also disclosed are pharmaceutical compositions containing metal ions and these compounds. Further disclosed is a method for treating a condition associated with cells containing inside-out phosphatidylserine, with these compounds.

Abstract: Disclosed is a process for obtaining an acrylic compound having a tertaoxaspiro backbone and at least one acrylic unsaturation. Said compound is in embodiments an acrylate, a methacrylate or a crotonate of an alkoxylated, such as an ethoxylated, a propoxylated and/or a butoxylated 2,4,8,10-tetraoxaspiro[5.5]undecane3,9-dialkanol.

Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.

Abstract: Disclosed is a compound of formula (I) wherein Y, Ring D, m and R1-R4 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as pharmaceutically acceptable salts, polymorphs, solvates, and isomers thereofs, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.

Abstract: The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, R4, R5, n, m, p and X are as defined in the description, their preparation and their use as pharmaceutically active compounds.

Abstract: The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, R4, n and X are as defined in the description, their preparation and their use as pharmaceutically active compounds.

Abstract: The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention and its therapeutic uses as complement pathway modulators for the treatment of ocular diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The invention relates to urea-containing mercaptosilanes of the formula I which are prepared by reacting a halosilane of the formula II with compounds of the formula III in an alcohol.

Abstract: The invention relates to urea-containing silanes of the formula I which are prepared by, in a first step, reacting an aminosilane of the formula II with an isocyanate of the formula III and, in a second step, reacting the product from the first process step with sodium sulphide of the formula IV Na2S??(IV) or in a first step, reacting an isocyanatosilane of the formula VI with an amine of the formula VII and, in a second step, reacting the product from the first process step with sodium sulphide of the formula IV Na2S??(IV).

Abstract: The present invention relates to organic compounds that are usable as ligands for preparing complexes of lanthanides or of certain transition metals which are water-soluble, to a method for preparing same, and also to the use thereof as a fluorescent probe.

Abstract: The present disclosure provides for processes and intermediates in the large-scale manufacture of the compound of formula (I) or hydrates thereof.

Abstract: Disclosed herein are methods for recovering diphosphite-containing compounds from mixtures comprising organic mononitriles and organic dinitriles, using liquid-liquid extraction. Also disclosed are treatments to enhance extractability of the diphosphite-containing compounds.

Abstract: The present invention relates to a novel nickel complex and its derivatives, which mimic the active site of Ni-containing superoxide dismutase (NiSOD). The five-coordinate Ni(II) and Ni(III) complexes or their derivatives, and six-coordinate derivatives have the following structures of formula (I) and (II): The nickel complexes and their derivatives of the invention act as anti-oxidants or free radical scavengers. The invented nickel complexes can be used in the preparation of medicines, health foods or cosmetics for human, animals and plants, or can be used in environmental or soil protection.

Abstract: The present invention relates to specific metal complexes of dithiolenes with perfluoroalkyl substituted imidazolidine-2-chalcogenone-4,5-dithione ligands, a process for their preparation and their use as colourless IR absorbers, for optical filters application; especially for plasma display panels, or for laser welding of plastics. The compounds may be used in compositions for inks, paints and plastics, especially in a wide variety of printing systems and are particularly well-suited for security applications.

Abstract: A process for the separation of lignins and sugars from an extracted liquor, including, in the form of dry matter (DM), lignins and sugars, includes: a) concentrating the extracted liquor, in order to obtain a liquor having dry matter in a proportion of between 60 and 70%; b) mixing the concentrated liquor with water in equal parts by weight; c) stirring the mixture in order to disperse the lignins and to obtain a stable suspending of the lignins; d) filtering the solution, wherein the mixing is carried out by introducing the concentrated liquor into the water; and the temperature of the solution, during the suspending, is between 50° C. and 60° C.

Abstract: Provided herein are formulations, methods and substituted tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds.

Abstract: 2?,3?-dideoxy-5-fluorouridine derivatives have general formula 1: wherein: R1 denotes cinchona alkaloid fragment with defined absolute configuration at C-8 and C-9 atoms. A process for the manufacture of 2?,3?-dideoxy-5-fluorouridine derivatives of general formula 1 and application of 2?,3?-dideoxy-5-fluorouridine derivatives of general formula 1 in the anticancer treatment of breast cancer, cervical cancer and hepatic cancer are also indicated.

Abstract: The present disclosure is generally directed to neuroactive 17(20)-Z-vinylcyano-substituted compound of Formula (I) and (II), as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Abstract: N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof.

Abstract: The present application discloses peptides and peptaibols of high purity may be obtained by solid phase peptide synthesis using as the starting resin hydroxy amino acids, hydroxy amino acid amides, hydroxy amino alcohols or small peptides containing hydroxy amino acids attached to polymers through their side chain.

Abstract: The present invention relates to Polycomb Repressive Complex 2 (PRC2) peptide inhibitors and their use for the treatment of cancer and other conditions associated with aberrant PRC2 methyltransferase activity.

Abstract: Compounds of formula (I), salts thereof, and compositions and uses thereof are described. The compounds are useful as V1a vasopressin agonists, for the treatment of, e.g., complications of cirrhosis, including bacterial peritonitis, HRS2 and refractory ascites.

Abstract: The invention provides peptides and analogs of INGAP and HIP peptides. The peptides and analogs can be used in methods for treating various diseases and conditions. Such diseases and conditions can include impaired pancreatic function, treating a metabolic disease, for example, diabetes, both type 1 and type 2 diabetes, islets induction, expansion and proliferation for transplantation, promoting neuroprotection or nerve regeneration, promoting liver regeneration or inhibiting inflammation.

Abstract: The present invention relates to agents, compositions and methods for use in medicine. In particular, the invention relates to agents related to GnRH peptides.

Abstract: Polypeptides that recognize and are strong binders to Influenza A hemagglutinin and can be used, for example, to treat and/or limit development of an influenza infection are disclosed. Isolated nucleic acids encoding the polypeptides of the invention, recombinant expression vectors comprising the nucleic acids encoding the polypeptides of the invention operatively linked to a suitable control sequence, and recombinant host cells comprising the recombinant expression vectors of the invention are disclosed. Antibodies that selectively bind to the polypeptides of the invention, and pharmaceutical compositions comprising one or more polypeptides according to the invention and a pharmaceutically acceptable carrier are disclosed.

Abstract: This invention provides kits, devices, and methods for the detection of antibodies that recognize one or more proteins and/or antigens from porcine reproductive and respiratory syndrome virus (PRRSV). The antibodies may be in a biological fluid of a PRRSV infected or at risk subject. The invention may be advantageously applied to both the diagnosis and prevention of PRRSV infection.

Abstract: The present invention relates to a fusion protein comprising a protein transduction domain capable of introducing the fusion protein into a mammalian cell and an anti-apoptotic protein comprising the amino acid of the sequence of SEQ ID NO:1 or an anti-apoptotically active variant or fragment thereof. The invention also relates to a pharmaceutical composition comprising such a fusion protein, in particular for blocking apoptosis in a patient in need thereof. The invention also provides a polynucleotide encoding such a fusion protein, an expression vector comprising the polynucleotide and a host cell comprising the expression vector. In a further aspect, the invention relates to the use of any of theses materials for the preparation of a medicament for blocking apoptosis in a patient in need thereof.

Abstract: The invention is directed to immunogenic compositions and methods for their use in the formulation and administration of therapeutic and prophylactic pharmaceutical agents. In particular, the invention provides immunogenic compositions and methods for preventing, treating, and/or ameliorating the symptoms of one or more microbial infections, including, for example, influenza.

Abstract: The invention comprises a method for inducing broadly cross-neutralizing antibodies against cutaneous and mucosal papillomavirus types or against heterologous papillomavirus types in humans comprising administering to a human in need thereof an immunogenic peptide or protein (or polynucleotide encoding therefor), where the immunogenic peptide or protein is: (a) a peptide or protein of at least 10 amino acid residues in length having a sequence corresponding to either a sequence from the N terminal amino acids 1-200 of papillomavirus L2 protein (for cross-neutralizing antibodies against cutaneous and mucosal papillomavirus types) or a sequence from the N terminal amino acids 1-88 of papillomavirus L2 protein (for cross-neutralizing antibodies against heterologous papillomavirus types), (b) a peptide or protein of at least 10 amino acid residues in length with at least 55% identity with the sequence from (a), or (c) a peptide or protein as defined in either (a) or (b) which is conjugated or fused to a protein o

Abstract: The invention provides a Pseudomonas exotoxin A (PE) comprising an amino acid sequence having a substitution of one or more B-cell and/or T-cell epitopes. The invention further provides related chimeric molecules, as well as related nucleic acids, recombinant expression vectors, host cells, populations of cells, and pharmaceutical compositions. Methods of treating or preventing cancer in a mammal, methods of inhibiting the growth of a target cell, methods of producing the PE, and methods of producing the chimeric molecule are further provided by the invention.

Abstract: The present invention relates to a myostatin inhibitor comprising extracellular water-soluble domains of delta-like 1 homolog (DLK1) as active ingredients. More particularly, the present invention relates to a composition for inhibiting myostatin activity, comprising, as active ingredients, extracellular water-soluble domains of DLK1 or a deletion mutant of extracellular water-soluble domains of DLK1. The myostatin inhibitor of the present invention is bonded to the myostatin or activin receptor type IIB so as to inhibit the action mechanism of the myostatin, to thereby promote myogenesis and prevent differentiation into fat cells. Therefore, the myostatin inhibitor of the present invention may be used in preventing and treating diseases such as muscular dysplasia that requires differentiation to muscular cells, or metabolic diseases.

Abstract: Nuclear Transport Modifiers such as cSN50 and cSN50.1, afford in vivo islet protection following a 2-day course of intense treatment in autoimmune diabetes-prone, non-obese diabetic (NOD) mice, a widely used model of Type 1 diabetes (T1D), which resulted in a diabetes-free state for one year without apparent toxicity and the need to use insulin. cSN50 precipitously reduces the accumulation of islet-destructive autoreactive lymphocytes while enhancing activation-induced cell death of T and B lymphocytes derived from NOD mice. cSN50 attenuated pro-inflammatory cytokine and chemokine production in immune cells in this model of human T1D. cSN50 also provides cytoprotection of beta cells, therefore preserving residual insulin-producing capacity. Because intracellular delivery of a Nuclear Transport Modifier peptide such as cSN50 and cSN50.1 can result in lowering of fasting blood glucose levels and may ameliorate (e.g.

Abstract: The present application is related to a modified protein comprising a protein having a coiled coil domain and a peptide having the sequence such as shown in SEQ ID NO 1: ZXBBBBZ that is linked to the coiled coil domain wherein: Z is any amino acid or is absent; X is any amino acid; B is an arginine (R) or a lysine (K). Said modified protein is in particular an antigen or a carrier protein, associated to an antigen. This modified protein has an increased affinity for negatively charged polymers such as nucleic acids or heparin, and shows an increased immunogenicity.

Abstract: The invention relates to citrulline peptides with anti-inflammatory properties. The invention also relates to an in vitro model for activation of macrophages, induced by immune complexes between specified IgG of rheumatoid arthritis and their citrulline targets.

Abstract: The disclosure relates to a process of obtaining a fully folded two chain insulin glargine that require no further processing to make it functionally active. The present disclosure discloses a surprising effect of over expression of Kex2p intracellularly under the control of inducible FLD1 promoter in the host Pichia pastoris to produce two chain functional glargine secreted directly in the medium. The schematic diagram of how the two chains are made inside the host Pichia pastoris and secretes into the medium.

Abstract: An insulin analogue comprises a B-chain polypeptide incorporating a halogenated phenylalanine at position B24, B25 or B26. The halogenated phenylalanine may be ortho-monofluoro-phenylalanine, ortho-monobromo-phenylalanine, ortho-monochloro-phenylalanine, or para-monochloro-phenylalanine. The analogue may be of a mammalian insulin, such as human insulin. A nucleic acid encodes such an insulin analogue. The halogenated insulin analogues retain significant activity. A method of treating a patient comprises administering a physiologically effective amount of the insulin analogue or a physiologically acceptable salt thereof to a patient. Halogen substitution-based stabilization of insulin may enhance the treatment of diabetes mellitus in regions of the developing world lacking refrigeration.