Abstract: The present application relates to novel (2-phenylimidazo[1,2-a]pyridin-3-yl)methyl-substituted perhydropyrrolo[3,4-c]pyrrole derivatives, to methods for the preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of respiratory disorders including sleep-related respiratory disorders such as obstructive sleep apneas and central sleep apneas and snoring.

Abstract: The present invention relates to novel polymorph of riociguat and process for preparing the polymorph. The present invention also relates to the improved process for the preparation of riociguat.

Abstract: Deuterated quinazolinone compounds and pharmaceutical compositions containing such compounds are provided. In particular, deuterated quinazolinone compounds of formula (I) are provided, as well as pharmaceutical compositions containing such compounds or crystal form, pharmaceutically acceptable salts, hydrates or solvates thereof. The deuterated quinazolinone compounds of formula (I) can be used for treating and/or preventing PI3K kinase-associated diseases, such as cancer, cell proliferative diseases and the like.

Abstract: The present invention relates to compounds of Formula (I) or pharmaceutically acceptable enantiomers, salts, solvates or prodrugs thereof. The invention further relates to the use of the compounds of Formula (I) for the treatment of cystic fibrosis. The invention also relates to a process for manufacturing compounds of Formula (I).

Abstract: The present invention encompasses compounds of formula (I) wherein the groups A, R and q are defined in claim 1, their use as inhibitors of IGF-1R, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.

Abstract: This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.

Abstract: The present invention includes compositions that are useful in preventing or treating metastasis in a subject diagnosed with cancer. The present invention also includes methods of preventing or treating metastasis in a subject diagnosed with cancer, wherein the method comprises administering to the subject in need thereof an effective amount of a pharmaceutical formulation comprising at least one pharmaceutically acceptable carrier and at least one CX3CR1 or fractalkine antagonist.

Abstract: Certain pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds that inhibit cycline dependent kinase (CDK) (e.g., CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8, CDK9, CDK10, CDK11, CDK12, CDK13, etc.) are disclosed. Pharmaceutical compositions comprising these compounds, and the use of these compounds and compositions to inhibit CDK; to treat disorders associated with CDK such as those arising from an inappropriate activity, mutation, overexpression, or upstream pathway activation of CDK; or disorders that are ameliorated by the inhibition of CDK; proliferative disorders; cancer; viral infections; neurodegenerative disorders; ischaemia; renal diseases; and cardiovascular disorders are also disclosed. Optionally, the treatment further comprises simultaneous or sequential treatment with a further active agent, e.g., an aromatase inhibitor, an anti-estrogen, a Her2 blocker, a cytotoxic chemotherapeutic agent, etc.

Abstract: The present invention relates to solid state forms of a p-toluenesulfonic acid salt (PTSA) of the selective PI3K delta inhibitor (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one (TGR-1202). The present invention also relates to methods of preparing the same, pharmaceutical compositions containing them, and methods of treating a PI3K kinase mediated disease or disorder, such as cancer, by administering the same.

Abstract: Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as Cyp8b1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for diabetes and cardiovascular disease.

Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as Cyp8b1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for diabetes and cardiovascular disease.

Abstract: The present invention relates to a method of producing and purifying a high-purity anhydrosugar alcohol in high yield by a simple process and apparatus, the method includes the steps of: allowing a sugar alcohol to react in the presence of an acid catalyst in a reactor, and, at the same time, evaporating a product of the reaction; cooling the evaporated product to remove water and obtain a crude anhydrosugar alcohol; and introducing the crude anhydrosugar alcohol into a melt crystallization process to obtain a high-purity anhydrosugar alcohol.

Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.

Abstract: The present disclosure describes a method to treat conditions, including cancer, using compounds that can target resistant cancer cells. The compounds of the invention can decrease the rate of proliferation of drug-resistant cancer cells, such as glioma, lung cancer, and uterine sarcoma.

Abstract: Fused [1,2]Imidazo[4,5-c] ring compounds (e.g., imidzao[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) substituted on the fused ring with a group that contains a guanidine or substituted guanidine moiety, pharmaceutical compositions containing the compounds, and methods of making the compounds are disclosed. Methods of use of the compounds as immune response modifiers, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are also disclosed.

Abstract: The present invention provides a compound of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

Abstract: A method for preparing a metal-organic framework (MOF) comprising contacting one or more of a rare earth metal ion component with one or more of a tetratopic ligand component, sufficient to form a rare earth-based MOF for controlling moisture in an environment. A method of moisture control in an environment comprising adsorbing and/or desorbing water vapor in an environment using a MOF, the MOF including one or more of a rare earth metal ion component and one or more of a tetratopic ligand component. A method of controlling moisture in an environment comprising sensing the relative humidity in the environment comprising a MOF; and adsorbing water vapor on the MOF if the relative humidity is above a first level, sufficient to control moisture in an environment. The examples relate to a MOF created from 1,2,4,5-Tetrakis(4-carboxyphenyl)benzene (BTEB) as tetratopic ligand, 2-fluorobenzoic acid and Y(NO3)3, Tb(NO3)3 and Yb(NO3)3 as rare earth metals.

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.

Abstract: A novel compound chlorosilylarylgermane, a method for preparing the compound, and the use of the compound are described. A method for preparing trichlorosilyltrichlorogermane and the use of trichlorosilyltrichlorogermane are also described.

Abstract: The present invention relates to novel aminobisphosphonate compounds useful as antiwear and/or friction modifier additive components, lubricant additive compositions and lubricant compositions each comprising such compounds, and methods for making and using the same.

Abstract: Iridium (III) complexes are described together with methods to prepare and use such complexes. Also described are devices that utilize the iridium (III) complexes.

Abstract: A construct of the structure F—S1-S2 where: F—S1 is an aminoalkylglycoside where F is ?-D-galactopyranosyl-(1?4)-?-D-galactopyranosyl-(1?4)-?-D-glucopyranoside and S1 is 2-aminoethyl, 3-aminopropyl, 4-aminobutyl or 5-aminopentyl; S2 is —CO(CH2)2CO—, —CO(CH2)3CO—, —CO(CH2)4CO— or —CO(CH2)5CO—; and L is phosphatidylethanolamine.

Abstract: A flavor composition containing at least one HMG glucoside compound that can be used to enhance the taste of edible compositions including sweet goods, such as confectionery goods, and savory goods, such as pet foods.

Abstract: A group of substituted thienopyrrolopyrimidine ribonucleosides of general formula I, in which R shows strong cytostatic and cytotoxic activities preferably against cancer cell lines of broad spectrum of diseases including tumors of various histogenetic origin.

Abstract: It is an object of the present invention to provide novel and highly active cyclic-di-nucleotide (CDN) immune stimulators that activates DCs via a recently discovered cytoplasmic receptor known as STING (Stimulator of Interferon Genes). In particular, the CDNs of the present invention are provided in the form of a composition comprising one or more cyclic purine dinucleotides that induce STING-dependent TBK1 activation, wherein the cyclic purine dinuclotides present in the composition are substantially pure Rp,Rp or Rp,Sp stereoisomers, and particularly substantially pure Rp,Rp, or RpSp CDN thiophosphate diastereomers.

Abstract: The present invention provides nucleosides an exocyclic amine-protected nucleoside of the formula: A-B where A is a 5?-protected ribose, 5?-protected-2-deoxyribose, 5?-protected-3?-phosphoramidite ribose, or 5?-protected-3?-phosphoramidite-2-deoxyribose moiety; and B is a nucleobase having an exocyclic amine group that is protected with di-tert-butylisobutylsilyl (“BIBS”) protecting group. Use of BIBS protecting group provides an exocyclic amine-protected nucleoside that is stable to a wide variety of reaction conditions associated with oligonucleotide synthesis. The present invention also provides, oligonucleotides comprising the same, and methods for producing the same.

Abstract: The present application relates to a method of preparing compounds of Formula (I) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, R1 is H, ?-OH, ?-OH, or an oxo group.

Abstract: Systems and methods for surgical robotic guidance include a robotic system (124) having a robot (122) configured to pass to a target through a port (134). The robotic system includes a visual component (102) employed in guiding the robot along a path to a location. The location is defined in accordance with a position and orientation of the robot. An ultrasonic probe (125) is guided by the robot to the location to permit engagement of the probe to collect ultrasonic images at the location.

Abstract: The invention relates to materials and methods of conjugating a water soluble polymer to an oxidized carbohydrate moiety of a therapeutic protein comprising contacting the oxidized carbohydrate moiety with an activated water soluble polymer under conditions that allow conjugation. More specifically, the present invention relates to the aforementioned materials and methods wherein the water soluble polymer contains an active aminooxy group and wherein an oxime or hydrazone linkage is formed between the oxidized carbohydrate moiety and the active aminooxy group on the water soluble polymer, and wherein the conjugation is carried out in the presence of a nucleophilic catalyst.

Abstract: Provided herein is a novel method of purifying an IgG antibody from a preparation by use of an electropositive membrane having a defined porosity.

Abstract: A method of preparing collagen active peptides with antiproliferative activity against cancer cells. The collagen active peptides are obtained by hydrolysis of papain and trypsin and a specific purifying process. The collagen active peptides have antiproliferative activity against cancer cells, such as ovarian carcinoma cells including SKOV3, OVCAR3, 436 and SRO82 and the prostate cancer cells including PC3, LnCAPC1, and LnCAPC2.

Abstract: The present invention describes a new peptide aldehyde produced naturally by Streptomyces lividans 66, which we have called livipeptin. Using genome mining of natural products, we predicted that SLI0883-5 genes encode an unprecedented biosynthetic system, unusually small (4.6 Kbp), which produces an acylated peptide aldehyde. Because of the chemical characteristics of the predicted compound, we postulated its anti-proteolytic activity, which we confirmed by identifying and purifying this compound through metabolic profiles of HPLC and MS of the mutated strain lacking these three genes and the wild strain. To this objective, we identified the conditions wherein these genes are strongly expressed. The livipeptin was purified and its inhibitory activity on the proteolytic activity of selected proteases was demonstrated in vitro. The design of an expression cassette for its heterologous expression is also described plus its use for heterologous protein production.

Abstract: New gelatinase inhibitors, processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy and/or prophylaxis of conditions wherein inhibition of gelatinases is useful such as epilepsy, schizophrenia, Alzheimer disease, autism (in particular associated to fragile X syndrome), mental retardation, mood disorders such as bipolar disorders, depression, vascular diseases such as ischemic stroke and atherosclerosis, inflammatory diseases such as multiple sclerosis, rheumatoid arthritis and inflammatory bowel disease, drug addiction, neuropathic pain, lung diseases such as asthma and chronic obstructive pulmonary disease, cancer and sepsis.

Abstract: A synthetic peptide that targets cancer stem cells is provided. The peptide consists of the amino acid sequence of anyone of SEQ ID NO: 1 to SEQ ID NO: 15. Also provided is a composition comprising said synthetic peptide with a therapeutic agent fused thereto, and a pharmaceutically acceptable carrier or diluent. Further provided is a method of screening a peptide specifically targeting to a cancer stem cell. The method comprises the steps of establishing an oligopeptide library by using a phage expression system, contacting the library with a culture of bulk tumor cells of a cancer cell line, contacting the phages which do not bind to the bulk tumor cells with a culture of cancer stem cells of said cancer cell line, and screening a peptide specifically targeting to a cancer stem cell from the phages which bind to the cancer stem cells.

Abstract: The present invention provides peptide compounds that regulate the complement system and methods of using these compounds. The invention is an isolated, purified peptide of 30 amino acids derived from human astrovirus protein, called CP1. The invention is directed to peptide compounds that are peptide mimetics, peptide analogs and/or synthetic derivatives of CP1 having, for example, internal peptide deletions and substitutions, deletions and substitutions at the N-terminus and C-terminus, and that are able to regulate complement activation. The invention further provides pharmaceutical compositions of therapeutically effective amounts of the peptide compounds and a pharmaceutically acceptable carrier, diluent, or excipient for treating a disease or condition associated with complement-mediated tissue damage.

Abstract: The present invention relates generally to novel depsipeptides, to methods for the preparation of these novel depsipeptides, to pharmaceutical compositions comprising the novel depsipeptides; and to methods of using the novel depsipeptides to treat or inhibit various disorders.

Abstract: Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.

Abstract: This invention relates to cytomegalovirus (CMV) proteins suitable for vaccine uses. Provided herein are mammalian host cells, in particular CHO cells, in which the sequence(s) encoding CMV proteins gH, gL, pUL128, pUL130, pUL131 (or a complex-forming fragment thereof) are stably integrated into the genome.

Abstract: There is described an AAV capsid protein having an amino acid sequence which has at least 98% identity to the sequence of SEQ ID NO: 3 or at least 94% identity to the sequence of SEQ ID NO: 4. Also described is a pharmaceutical composition, an AAV capsid and a viral particle comprising the capsid protein, a recombinant AAV vector comprising a nucleotide sequence which encodes for the capsid protein, and a host cell and a transgenic animal comprising the capsid protein or the vector. In addition, there is described a method of transferring a nucleic acid of interest into a mammal comprising introducing a recombinant AAV vector into the mammal, wherein the recombinant AAV vector comprises a gene of interest which is encapsidated into a capsid comprising the capsid protein.

Abstract: The present application relates to methods of producing exosomes. The application also provides a method for preparing a protein composition comprising culturing an exosome-producing cell expressing a Nef-fusion protein comprising a Nef-derived peptide fused to a protein of interest; isolating exosomes from the exosome-producing cell culture; and purifying the protein of interest from the isolated exosomes. The application further discloses compositions that comprise exosomes containing the Nef-fusion protein, as well as methods of using the Nef-fusion protein and exosomes containing the Nef-fusion protein.

Abstract: The invention is directed to MtrE peptides and their use in gonorrhea vaccines.

Abstract: A method for increasing the presentation of ETEC CS6 antigen on cell surface, comprising the step of contacting cells expressing said antigen with an aqueous solution comprising 0.6-2.2 percent phenol by weight, such that the presentation of said antigen is increased by at least 100%. A method for the manufacture of a killed whole cell vaccine for immunization against CS6-expressing ETC. Cells and vaccines obtainable by the above methods.

Abstract: A polynucleotide having at least 80% sequence identity with the full-length nucleotide sequence of SEQ ID NO: 1 and substantially identical polynucleotides; an isolated polypeptide having at least 80% sequence identity with the full-length amino acid sequence of SEQ ID NO: 2 and substantially identical polypeptides; and polynucleotides encoding the Ha WRKY76 polypeptide and substantially identical polypeptides are described. Also described are vectors and recombinant expression cassettes containing the c DNA polynucleotide, a polynucleotide encoding the Ha WRKY76 polypeptide, or substantially identical polynucleotides. Transgenic plants containing such expression cassettes, related methods and uses are also provided.

Abstract: The present invention relates to Huwentoxin-IV variants, polynucleotides encoding them, methods of making and using the foregoing, and methods of alleviating pain with peptide inhibitors of Nav1.7.

Abstract: The present invention includes a genetically-modified non-human animal model of longevity and increased health span, which is associated with reduced tumorigenesis and tumor metastasis, as well as related methods for increasing longevity and health span, reducing tumorigenesis and tumor metastasis, and identifying active agents that confer increased longevity or health span, or reduced tumorigenesis or tumor metastasis.

Abstract: The invention concerns a variant (double mutant form) of the survivin polypeptide; nucleic acid molecules encoding the survivin variant; antigen presenting cells (APCs) such as dendritic cells, or APC precursors, comprising the variant survivin polypeptide or encoding nucleic acid sequence; and methods for treating a malignancy, such as myeloma, or for inducing an immune response, utilizing a variant survivin polypeptide, nucleic acid molecule, or APC.

Abstract: The present invention provides protease-resistant peptides, methods of making such peptides, as well as compositions comprising protease-resistant peptides and method of treatment utilizing such peptides. A combination of lipidation of certain amino acid residues and substitution of alpha-methyl functionalized amino acids for natural amino acids has been determined to produce protease-resistant peptides.

Abstract: The present invention relates to compositions and methods for treating HER2/Neu (ERBB2) expressing cancer cells. In some embodiments, the invention includes an isolated T cell receptor (TCR) having high affinity for and that specifically binds ERBB2369-377 epitope on a target cell. Other embodiments include a T cell or a population of T cells modified to express ERBB2-specific TCR. Further embodiments include methods of using ERBB2-specific TCR gene transfer for treating ERBB2 expressing cancer cells. Also included are methods and pharmaceutical compositions comprising the modified T cells for adoptive therapy.

Abstract: Novel minor histocompatibility antigens (MiHAs) are described. These novel MiHAs were selected based on two features: (i) they are encoded by loci with a minor allele frequency (MAF) of at least 0.05; and (ii) they have adequate tissue distribution. Compositions, nucleic acids and cells related to these novel MiHAs are also described. The present application also discloses the use of these novel MiHAs, and related compositions, nucleic acids and cells, in applications related to cancer immunotherapy, for example for the treatment of hematologic cancers such as leukemia.

Abstract: Provided herein are recombinant masking proteins and recombinant ligand proteins useful in treating cancer, neurodegenerative disease, and cardiovascular disease. The recombinant masking proteins provided herein may, inter alia, be used as non-covalent masks of antagonists of, for example, cellular growth factors (e.g., TNF) or cell surface proteins (e.g., CTLA-4).