Abstract: The present invention disclosed a class of pyrimidine or pyridine compounds, pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, preparation method therefor and pharmaceutical compositions and pharmaceutical uses thereof. See e.g., Formula I below. The compounds can inhibit the variants of EGFR (Epidermis Growth Factor Receptor) proteinases, and therefore can inhibit the growth of a variety of tumor cells effectively. The compounds can be used to prepare antitumor drugs, used for the treatment, combined therapy or prevention of various different cancers. The compounds can overcome the drug resistance induced by the existing first-generation EGFR inhibitors such as gefitinib, erlotinib and so on. Particularly, the compounds can be used to prepare drugs for treating or preventing diseases, disturbances, disorders or conditions mediated by epidermis growth factor receptor variants (such as L858R activated mutants, Exon19 deletion activated mutants and T790M resistant mutants).

Abstract: The present invention relates to a novel imidazotriazinone or imidazopyrazinone derivative, a tautomer thereof, a stereoisomer thereof and their mixture, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating a tankyrase-related disease, which contains the same as an active ingredient.

Abstract: The present invention relates to a selective dual delta (?) and gamma (?) PI3K protein kinase modulator (S)-N-(5-(4-amino-1-(1-(5-fluoro-3-(3-fluorophenyl)-4-oxo-4H-chromen-2-yl)ethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl) methane sulfonamide, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of PI3K kinase mediated diseases or disorders with them.

Abstract: Disclosed herein, inter alia, are compounds and methods of use thereof for the modulation of CCR4 activity.

Abstract: The present invention provides a novel RET inhibitor comprising, as an active ingredient, a compound or a salt thereof that have not been known for their RET inhibitory activity, and also provides an agent for preventing or treating diseases (e.g., malignant tumors) that can be prevented or treated by RET inhibitory activity. The RET inhibitor comprises, as an active ingredient, a compound represented by Formula (I) below or a salts thereof: wherein A, R1 to R3, X, and n are as defined in the specification.

Abstract: The invention provides compounds of formula I: wherein A, B, X, and Y have any of the values defined in the specification, as well as pharmaceutical compositions comprising such compounds, processes for preparing such compounds, and therapeutic methods for treating cancer and other topoisomerase mediated conditions.

Abstract: A compound of formula I, (I) or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer.

Abstract: The present invention relates to spiro-cyclic amine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl each optionally substituted with CN or one or more fluoro atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-6C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms, monocyclic heterocycle optionally independently substituted with halogen, (1-6C)a

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y-L-R??(I) which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.

Abstract: Provided herein are formulations, methods and substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds.

Abstract: The present invention relates in general to a method for the synthesis and purification of 1) the polyhedral borane decahydrodecaborate and dodecahydrododecaborate anions and their salts and 2) amines and amine boranes. The organoammonium halide is combined with alkali metal tetrahydroborate to form organoammonium tetrahydroborate, which upon pyrolysis provides organoammonium decahydrodecaborate and organoammonium dodecahydrododecaborate.

Abstract: Therapeutically-effective amounts of novel analogs or derivatives of alkyl fatty acids, such as but not limited to lipoic acid, and pharmaceutical formulations comprising such analogs or derivatives and pharmaceutically-acceptable carriers therefor, are useful for the treatment, prevention, imaging, and/or diagnosis of medical disorders.

Abstract: This invention relates to compounds that are selective inhibitors of Matrix Metalloprotease-12 (MMP-12), to cosmetic and pharmaceutical compositions containing them, and to their use in the prevention and/or treatment of ailments associated with MMP-12. Formula (I).

Abstract: A formic acid decomposition catalyst system includes organometallic complexes having formula 1: wherein: M is a transition metal; E is P, N, or C (as in imidazolium carbene); R1, R2 are independently C1-6 alkyl groups; o is 1, 2, 3, or 4; R3 are independently hydrogen, C1-6 alkyl groups, OR14, NO2, halogen; R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R15, R16 are independently hydrogen or C1-6 alkyl groups; R14 is a C1-6 alkyl group; and X? is a negatively charge counter ion.

Abstract: A method for producing P1,P4-di(uridine 5?-)tetraphosphate (UP4U) that can avoid reduction of the synthetic efficiency without using UTP free is developed. A method for producing UP4U comprising reacting a phosphoric acid-activating compound represented by formula [II] or [III] with a phosphoric acid compound selected from the group consisting of UMP, UDP, UTP and a pyrophosphoric acid or a salt thereof (excluding UTP free) in water or a hydrophilic organic solvent, in the presence of a metal ion selected from the group consisting of an iron (II) ion, an iron (III) ion, a trivalent aluminum ion, a trivalent lanthanum ion, and a trivalent cerium ion. where, in the formula [II], R1 represents a uridyl group binding to the 5?-position, X represents a heterocyclic group, and n represents an integer of 1 or 2, where, in the formula [III], X represents a heterocyclic group selected from the group consisting of an imidazolyl group, a benzimidazolyl group, and a 1,2,4-triazolyl group.

Abstract: The present invention relates to crystalline forms of S-[4-(3-fluoro-3-methylbutyryloxy)but-2-ynyl] 6?,9?-difluoro-17?-(furan-2-yl)carbonyloxy-11?-hydroxy-16?-methyl-3-oxoandrosta-1,4-diene-17?-carbothioate, an anti-inflammatory and anti-allergic glucocorticoid compound.

Abstract: Disclosed are compositions and methods useful for targeting and internalizing molecules into cells of interest and for penetration by molecules of tissues of interest. The compositions and methods are based on peptide sequences, such as truncated LyP-1 peptides, that are selectively internalized by a cell, penetrate tissue, or both. The disclosed internalization and tissue penetration is useful for delivering therapeutic and detectable agents to cells and tissues of interest.

Abstract: Provided are a conotoxin peptide ?-CPTx-btl04 and a derivative polypeptide. The amino acid sequence of the conotoxin peptide is indicated by SEQ ID NO: 1. Also provided are a conotoxin peptide preparation method and uses of the conotoxin peptide in the treatment of diseases related to a calcium ion channel.

Abstract: Polypeptides and other compounds that can bind specifically to the CH2-CH3 cleft of an immunoglobulin molecule, and methods for using such polypeptides and compounds to inhibit Fc-mediated immune complex formation, are described.

Abstract: Melanocortin receptor-specific cyclic peptides of the formula where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and z are as defined in the specification, compositions and formulations including the peptides of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes.

Abstract: Described herein is the generation of optimized H5N1 influenza HA polypeptides for eliciting a broadly reactive immune response to H5N1 influenza virus isolates. The optimized HA polypeptides were developed through a series of HA protein alignments, and subsequent generation of consensus sequences, based on human and avian H5N1 isolates. Provided herein are optimized H5N1 HA polypeptides, and compositions, fusion proteins and VLPs comprising the HA polypeptides. Further provided are codon-optimized nucleic acid sequences encoding the HA polypeptides. Methods of eliciting an immune response against influenza virus in a subject are also provided by the present disclosure.

Abstract: Provided herein are influenza hemagglutinin stem domain polypeptides, compositions comprising the same, vaccines comprising the same and methods of their use.

Abstract: The present invention relates to a method of making a crosslinked thermoset resin. One embodiment of this method comprises: (i) separating a plant-derived flour mixture into a protein fraction comprising proteins and a carbohydrate fraction comprising carbohydrates; (ii) subjecting the carbohydrate fraction to an oxidizing agent to yield oxidized carbohydrates comprising aldehyde functional groups or both aldehyde functional groups and carboxyl functional groups; and (iii) reacting the oxidized carbohydrates with the protein fraction under conditions effective to crosslink the proteins, thereby yielding a crosslinked thermoset resin. The present invention also relates to a crosslinked thermoset resin and composites, nanofiber membranes, and adhesives comprising the crosslinked thermoset resin.

Abstract: The present invention relates to Kv1.3 antagonists, and polynucleotides encoding them, and methods of making and using the foregoing.

Abstract: The present invention is directed to antibodies and fragments thereof having binding specificity for CGRP. Another embodiment of this invention relates to the antibodies described herein, and binding fragments thereof, comprising the sequences of the VH, VL and CDR polypeptides described herein, and the polynucleotides encoding them. The invention also contemplates conjugates of anti-CGRP antibodies and binding fragments thereof conjugated to one or more functional or detectable moieties. The invention also contemplates methods of making said anti-CGRP antibodies and binding fragments thereof. Embodiments of the invention also pertain to the use of anti-CGRP antibodies, and binding fragments thereof, for the diagnosis, assessment and treatment of diseases and disorders associated with CGRP.

Abstract: Antibody molecules, in particular fully human antibodies that bind to human IGF-1 and cross-react with IGF-2 such that binding of IGF-1 and IGF-2 to the IGF-1 receptor is prevented and IGF-1 receptor-mediated signaling is inhibited. The antibodies do not bind to insulin and thus do not affect the mitogenic properties of insulin that are mediated by its binding to the insulin receptors. The antibodies are useful for the treatment of hyperproliferative diseases, in particular cancer.

Abstract: The invention relates to a multiple-variable dose method for treating a disorder in which TNF? activity is detrimental, comprising administering to a subject in need thereof a first induction dose of an anti-TNF? antibody which ranges from 161 to 320 mg such that a threshold level of TNF? inhibitor is achieved within an induction phase; and subsequently administering to the subject at least one treatment dose of the TNF? inhibitor within a treatment phase, such that treatment occurs.

Abstract: Antibodies and compositions capable of neutralizing oncostatin M biological functions are useful in treating diseases and disorders associated with oncostatin M, such as osteoarthritis and idiopathic pulmonary fibrosis.

Abstract: This invention relates to methods of screening for anti-PACAP antibodies, or anti-PACAP receptor antibodies, and antigen binding fragments thereof, for potential use in treating or preventing PACAP-associated photophobia or light aversion, and therapeutic compositions containing and methods of using anti-PACAP antibodies, or anti-PACAP receptor antibodies, and antigen binding fragments thereof.

Abstract: Antibodies that are capable of specifically binding and preventing the activation of TREM-1, a protein expressed on monocytes, macrophages and neutrophils with both good affinity and low viscosity at clinically relevant concentrations are described. Such antibodies find utility in the treatment of individuals with an inflammatory disease, such as rheumatoid arthritis and inflammatory bowel disease.

Abstract: The present invention relates to isolated antibodies, or an antigen portions thereof, which bind to human HER3. The novel antibodies are of great utility since they allow for the sensitive and specific detection of human HER3. Detection of human HER3 is, e.g., possible in a tissue sample, even when such tissue sample is a formalin-fixed paraffin embedded tissue (FFPET) sample.

Abstract: The invention relates to novel pharmaceutical compositions including, as active ingredient, an antibody binding the human anti-Müllerian hormone type II receptor (AMHR-II) and an anticancer agent, as well as the therapeutic applications of these compositions.

Abstract: The invention relates generally to antibodies that bind CD71, activatable antibodies that specifically bind to CD71 and methods of making and using these anti-CD71 antibodies and anti-CD71 activatable antibodies in a variety of therapeutic, diagnostic and prophylactic indications.

Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

Abstract: The present invention provides antibodies that bind to prostate-specific membrane antigen (PSMA), bispecific antibodies that bind to PSMA and CD3, and methods of using the same. According to certain embodiments, the antibodies of the invention bind human PSMA with high affinity and bind CD3 to induce human T cell proliferation. The invention includes antibodies that bind PSMA and CD3 and induce T cell-mediated killing of PSMA-expressing tumor cells. According to certain embodiments, the present invention provides bispecific antigen-binding molecules comprising a first antigen-binding domain that specifically binds human CD3, and a second antigen-binding molecule that specifically binds human PSMA. In certain embodiments, the bispecific antigen-binding molecules of the present invention are capable of inhibiting the growth of prostate tumors expressing PSMA.

Abstract: The invention provides anti-HER2 antibodies and immunoconjugates and methods of using the same.

Abstract: The invention relates to anti-Factor D antibody variants, their production and their use in the preparation of compositions and medicaments for treatment of diseases and disorders associated with excessive or uncontrolled complement activation.

Abstract: The present invention comprises a humanized monoclonal antibody that binds to the human immunoglobulin heavy chain variable region germline gene VH1-69. This antibody is derived from Mab G6 and recognizes the same epitope. Moreover, the antibody is used in combination with vaccines to augment an immune response to the antigen.

Abstract: The invention relates to a method for dissolving the components of gel forming materials suitable for use in wound care comprising the steps of admixing said components with an ionic liquid. The ionic liquid may be selected from the group of tertiary amine N-oxides, N,N-dimethyl formamide/nitrogen tetroxide mixtures, dimethyl sulphoxide/paraformaldehyde mixtures and solutions of limium chloride in N,N-dimethyl acetamide or N-methyl pyrrolidone.

Abstract: The present invention provides crosslinked carboxymethylcellulose having high elastic modulus coupled with high absorbance capacity when swollen in simulated gastric fluid/water (1:8) and simulated intestinal fluids. The invention further provides methods of making the crosslinked carboxymethylcellulose, compositions comprising the crosslinked carboxymethylcellulose and methods of using the crosslinked carboxymethylcellulose, for example, for treating overweight or obesity or for enhancing glycemic control.

Abstract: A portable electric (battery) powered paint system designed to worn in a typical workman's tool belt and thus accompany the painter as he moves from wall to wall and room to room without the restriction of electrical cords plugged into wall outlets. The invention consists of a paint reservoir, an electric paint pump, a power pack of two or more 18 Volt batteries, a paint applicator and associated paint supply tubing for transfer of paint from the reservoir to the paint applicator. The invention provides the painter with a self-contained powered painting system.

Abstract: A process is described for introducing a catalyst into a polymerization zone by detecting one or a combination of (i) a change in a concentration of the catalyst in a catalyst feed stream upstream of the polymerization zone, (ii) a change in a concentration of monomer in the polymerization zone, and (iii) a change in a polymer production rate of the polymerization zone, adjusting a first catalyst flow rate of the catalyst in the catalyst feed stream to a second catalyst flow rate based on the one or a combination of (i), (ii), and (iii), and introducing the catalyst into the polymerization zone downstream of a location in the catalyst feed stream where the step of adjusting is performed. A catalyst injection system for carrying out such a process is also provided.

Abstract: A method for synthesizing a modified polymer comprising epoxide groups along the polymer chain, by a hydrosilylation reaction of the unsaturations with a hydrosilane bearing an epoxide function in the presence of a suitable catalyst is provided. The method is simple, reproducible and able to be used on an industrial scale, and makes it possible to obtain high grafting yields, since they may reach 100%.

Abstract: A curable composition and a permanent resist film made using this curable composition are provided. The composition dissolves well in solvents, gives coatings superior in alkali developability, thermal decomposition resistance, light sensitivity, and resolution, and is particularly suitable for the formation of permanent resist films. Specifically, the composition is a curable composition for permanent resist films and contains a phenolic hydroxyl-containing compound (A) that has a molecular structure represented by structural formula (1): (where R1 is hydrogen, alkyl, or aryl, and n is an integer of 2 to 10; R2 is alkyl, alkoxy, aryl, aralkyl, or halogen, and m is an integer of 0 to 4; if m is 2 or more, the plurality of R2s may be the same or different from one another, and may be bonded to either of the two aromatic rings in the naphthylene structure) and a photosensitizer (B1) or curing agent (B2).

Abstract: This invention relates to products H made by reaction of a cyclic alkyleneurea U, at least one multifunctional aldehyde A2, and at least one of (a) an aminoplast former M that is not the same as the cyclic alkyleneurea U, and (b) a monofunctional aldehyde A1, which product H is optionally etherified by reaction of at least a part of the hydroxyl groups formed by addition reaction of N—H groups and aldehyde groups, with an alcohol having from one to ten carbon atoms, and wherein glyoxal is present in the at least one multifunctional aldehyde A2, to processes for their preparation, and to a method of use thereof in coating compositions.

Abstract: The invention relates to thioallophanates which contain silane groups and are of the general formula (I) in which R1, R2 and R3 are identical or different radicals and are each a saturated or unsaturated, linear or branched, aliphatic or cycloaliphatic radical or an optionally substituted aromatic or araliphatic radical having up to 18 carbon atoms, where said radical may optionally contain up to 3 heteroatoms from the group of oxygen, sulphur and nitrogen, X is a linear or branched organic radical having at least 2 carbon atoms, Y is a linear or branched, aliphatic or cycloaliphatic radical or an araliphatic or aromatic radical having up to 18 carbon atoms, and n is an integer from 1 to 20, to a process for preparation thereof, and to the use thereof as starting components in the production of polyurethane plastics.

Abstract: A composition containing an epoxide compound with two or more epoxide groups, a thiol ester with two or more ester groups and two or more thiol groups and/or a thiol ether with two or more thiol groups, and 0.005-2 wt. %, based on the total weight of the composition, of a tertiary amine which has a 5- or 6-membered aliphatic nitrogen heterocycle, said composition containing less than 1 wt. % of a primary amine. The composition can be used as, an embedding medium for microscopy and as an adhesive and to an optical element which comprises the composition.

Abstract: The present invention relates to a catalyst composition for curing epoxy group containing compounds comprising a base and a quaternary ammonium salt, of Formula (I): with R1, R2, R3, R4, R5, Y, A and X being as defined herein. Also encompassed are adhesive compositions containing said catalyst composition and the use of the catalyst composition.

Abstract: An oligomer, composition, and composite material employing the same are provided. The oligomer can be a reaction product of a reactant (a) and a reactant (b). The reactant (a) is a reaction product of a reactant (c) and a reactant (d). The reactant (b) can be or a combination thereof, wherein a is 0 or 1, and R1 is independently hydrogen or and wherein b is 0-6; c is 0 or 1; and, d is 0-6. The reactant (c) is wherein R2 is C5-10 alkyl group. The reactant (d) is wherein e is 0-10.