Abstract: A compound and a pharmaceutical composition for disease associated with an abnormal splice variant, use of the compound and the pharmaceutical composition, or a screening method of the compound and the pharmaceutical composition are provided. One or more embodiments disclose a compound expressed by the following formula (I) or (I?) or prodrugs or pharmaceutically acceptable salts thereof.

Abstract: The invention refers to compounds of general formula (I) wherein the variables take the various meanings, pharmaceutical compositions containing them and their use in medicine, particularly in pain therapy.

Abstract: The disclosure provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the disclosure are useful for treating immunological and oncological conditions.

Abstract: There is provided a process for the preparation of AZD5363, or a salt of AZD5363, comprising: (a) the reaction of 8-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-3-oxa-1,8-diazaspiro[4.5]decane-2,4-dione: or a salt thereof, with (S)-3-amino-3-(4-chlorophenyl)propan-1-ol, or a salt thereof, in the presence of base; and (b) either isolating AZD5363 or isolating AZD5363 as a salt. 8-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-3-oxa-1,8-diazaspiro[4.5]decane-2,4-dione is provided and is prepared by reacting 4-(alkyloxycarbonylamino)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxylic acid, or a salt thereof, with a cyclizing agent.

Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.

Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.

Abstract: Novel methods of treating inflammation and airway constriction using GABAergic compounds with reduced benzo-diazepine-like CNS activity are provided. Novel compounds which selectively target alpha-4 and alpha-5 GABAA receptors and methods of using those compounds to treat bronchoconstriction and inflammation are provided herein.

Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c

Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula I.

Abstract: The present invention provides a new forms of (R)-N-methylnaltrexone, and compositions thereof, useful as a peripheral mu opioid receptor antagonist.

Abstract: Provided herein is a process for the transfer-hydrogenation of ketone analogs of members of the jervine type of Veratrum alkaloids, such as cyclopamine. Also provided herein are novel ruthenium transfer-hydrogenation catalysts.

Abstract: This invention relates to a compound of formula I wherein A and Cy have one of the meanings as indicated in the specification and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.

Abstract: The invention discloses a method for extracting high-purity asarinin and use thereof. The method comprises: putting crude asarum powder in an SFE-CO2 device; under the conditions that an extraction kettle has a pressure of 30-40 Mpa and a temperature of 45-70° C., separating kettles I and II have a pressure of 5-10 Mpa, a temperature of 30-50° C. and the flow rate of CO2 is 35-60 L/h, extracting for 60-240 min to obtain total volatile oil of asarum; standing the total volatile oil of asarum for 24-72 h at a low temperature, and carrying out suction filtration under reduced pressure to obtain crude asarinin; and re-crystallizing the crude asarinin in absolute ethanol twice to obtain pure asarinin. It is found for the first time that asarinin has a good cough-relieving activity and thus can be used in preparing medicines for treating various types of coughs.

Abstract: Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.

Abstract: The present invention provides thieno[2,3-c]pyrrol-4-one compounds that inhibit activity of extracellular-signal-regulated kinase (ERK) and may be useful in the treatment of cancer.

Abstract: Chemical compounds are provided which act on GPR17 receptors and are useful in the treatment or amelioration of chronic and/or acute neurodegenerative diseases, such as multiple sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, and renal diseases.

Abstract: This invention relates to important intermediates in the preparation of a compound which is an inhibitor of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1).

Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I): wherein R1 represents a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R2 and R3 are the same or different and each represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R4 and R5 are the same or different and each represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R6 represents a hydrogen atom or the like, each R7 may be the same or different and may each represent an optionally substituted C1-6 alkoxy group or the like, X represents —CH?, —C(—R7)?, or —N?, and m represents 1 to 4, or a pharmacologically acceptable salt thereof.

Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Abstract: To provide a near-infrared absorption composition which contains a squarylium compound having excellent solvent solubility, a cured film which uses the near-infrared absorption composition, a near-infrared cut filter, a solid-state imaging device, an infrared sensor, and a compound. A near-infrared absorption composition includes a compound represented by the following Formula (1) and a resin. R1 and R2 each independently represent “—S1-L1-T1” or the like, R3 and R4 each independently represent a hydrogen atom or an alkyl group, X1 and X2 each independently represent an oxygen atom or —N(R5)—, R5 represents a hydrogen atom or the like, Y1 to Y4 each independently represent a substituent, p and s each independently represent an integer of 0 to 3, and q and r each independently represent an integer of 0 to 2; and S1 represents an arylene group or the like, L1 represents an alkylene group or the like, and T1 represents an alkyl group or the like.

Abstract: A composition for fabricating an organic film, an organic light-emitting display apparatus manufactured using the same, and a method of manufacturing the organic light-emitting display apparatus, the composition comprising a first compound that includes n substituents Y, and m polymerizable groups P1, wherein n is selected from 1, 2, 3, and 4; m is selected from 1, 2, 3, and 4; OP1 of the first compound is equal to or greater than 2.8 and equal to or less than 4.8; OP1 being (total number of atoms of the first compound)/{(number of carbon atoms of the first compound)?(number of oxygen atoms of the first compound)}; and RP1 of the first compound is equal to or greater than 0.01 and equal to or less than 0.46; RP1 being {(number of carbon atoms of the substituent Y)X n}/(number of carbon atoms of the first compound).

Abstract: The present invention provides compounds that bind to mitochondrial aldehyde dehydrogenase-2 (ALDH2), methods of using said compounds to treat patients with Fanconi Anemia, and methods of preparing said compounds.

Abstract: [Problem] To provide a fluorine-containing phosphate ester-amide which has high flame retardancy such as exhibiting flame retardant effects at a small quantity of addition, and sufficient hydrolysis resistance. [Solution] A fluorine-containing phosphate ester-amide represented by general formula (1). (In the formula, R1 and R2 are the same or different and represent a branched or linear alkyl group having 1 to 20 carbon atoms in which at least one carbon bonded to a nitrogen atom is a secondary or tertiary carbon, wherein R1 and R2 may have a substituent group selected from the group consisting of an alkoxy group, a hydroxy group, an amino group, a methyl amino group, an ethyl amino group, a dimethyl amino group, diethyl amino group and a fluorine atom. In addition, R1 and R2 may be bonded together to form a five- to eight-membered cyclic structure. X and Y are the same or different and represent a hydrogen atom or a fluorine atom, and n and m represent an integer of 1 to 6.

Abstract: Disclosed is a novel tenofovir disoproxil edisylate salt having the structure of Chemical Formula 1.

Abstract: Tetradentate and octahedral metal complexes suitable for use as phosphorescent or delayed fluorescent and phosphorescent emitters in display and lighting applications.

Abstract: The current invention describes new metathesis catalysts, a method for their preparation and their use in metathesis reactions.

Abstract: The invention relates to dendritic compounds, the use of these compounds as pharmaceuticals, pharmaceutical compositions containing the compounds, processes for preparing the compounds, and methods of treating diseases or conditions in which it is desirable to inhibit ?-secretase.

Abstract: Glycosphingolipids (GSLs) compositions and methods for iNKT-independent induction of chemokines are disclosed.

Abstract: The present disclosure relates to the synthesis of non-natural analogs of S-adenosyl-L-methionine (SAM) and/or of Se-adenosyl-L-methionine (SeAM) by reacting a methionine analog and adenosine triphosphate (ATP) in the presence of at least one methionine adenosyltransferase (MAT), and to use thereof with downstream SAM and/or SeAM utilizing enzymes. The non-natural analogs of SAM and/or SeAM have the general formula: where X is S or Se, and R1 is an alkyl group.

Abstract: Described herein are methods, compositions and kits utilizing heterogeneous metal catalysts for the preparation of cycloaddition compounds, such as triazoles and biomolecules.

Abstract: The present application relates to a regioselective and stereoselective processes for the preparation of dehydroepi-androsterone (DHEA) and processes for its intermediates.

Abstract: The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.

Abstract: The template-fixed ?-hairpin peptidomimetics Cyclo(-Tyr-His-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-D-Pro-Pro), disulfide bond between Cys4 and Gysl1, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for where cancer is mediated or resulting from CXCR4 receptor activity.

Abstract: In one aspect, the invention relates to isolated compounds useful as antifungal agents, for example, compounds having a structure represented by a formula: wherein R1 is hydrogen or hydroxyl; wherein R2 is hydrogen, a-xylose or ?-xylose; and wherein R3 and R4 are each hydrogen or together oxygen, or a pharmaceutically acceptable salt thereof; methods of isolating and purifying same; pharmaceutical compositions comprising same; agricultural compositions comprising same; and methods of treating and/or preventing fungal infections using same. In one aspect, R2 is not hydrogen or ?-xylose when R1 is hydroxyl and R3 and R4 are together oxygen. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: The invention is directed to glycopeptide antibiotics and their aglycones that are engineered to overcome bacterial resistance by replacement of a single, specific peptide carboxamide group in the core peptide of the glycopeptide antibiotic with an amidine group. The amidine pseudopeptide analog of the glycopeptide is effective in killing vancomycin-resistant bacteria at therapeutically achievable concentrations in a patient. For example, a [?[C(?NH)NH]Tpg4]-vancomycin aglycon designed to exhibit the dual binding to D-Ala-D-Ala and D-Ala-D-Lac needed to reinstate activity against vancomycin-resistant bacteria has been shown to overcome a common mode of bacterial resistance to the “last resort” antibiotics of the glycopeptide class. The pseudopeptide amidine analogs can be prepared from corresponding pseudopeptide thioamide analogs, which can be prepared synthetically, semi-synthetically, or biosynthetically.

Abstract: In one aspect, the invention relates to substituted urea depsipeptide analogs, derivatives thereof, and related compounds, which are useful as activators the ClpP endopeptidease; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating infectious disease using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: A synthetic peptide includes an amino acid sequence that: has 70-75%, 75-80%, 80-85%, 85-90%, 90-95% or 95-100% homology with an RpoN box of Region III of an RpoN protein; and binds specifically to a ?24, ?12, or ?24/?12 site(s) of an RpoN promoter. The synthetic peptide is effective for repressing transcription and/or gene expression from a binding site of interest, and the binding site of interest is an RpoN binding site or a cryptic promoter upstream of an RpoN binding site.

Abstract: A series of integrin blockers that present strong angiogenesis inhibiting performance, high integrin affinity and integrin-bonding capacity is provided. This series of integrin blockers can be adopted in treatment of solid tumors and rheumatoid arthritis. Specifically, said series of integrin blockers include polypeptide I, polypeptide II and polypeptide III (see SEQ ID NO: 1, SEQ ID NO: 2 and SEQ ID NO: 3) that can be adopted in treatment of solid tumors and rheumatoid arthritis. This invention also relates to application of these three integrin-blocking polypeptides in preparation of anti-tumor drugs, wherein the tumors that can be treated include those primary or secondary cancers originated from head and neck region or other organs such as brain, thyroid, esophagus, pancreas, lung, liver, stomach, breast, kidney, gallbladder, colon, rectum, ovary, cervix, uterus, prostate, bladder and testicle, as well as melanoma and sarcomas.

Abstract: This in invention relates to methods for the nucleic acid amplification of multiple variants (strains) of any pathogen present in a sample, and preferably in a sample from a pathogen infected individual. In preferred embodiments, the pathogen is a retrovirus, such as HIV. The amplified pathogen nucleic acid can be used to identify the pathogen variants present in a sample, to quantitate the pathogen present in a sample, and as a nucleic acid vaccine, or in the preparation of antigen presenting cell vaccines. Nucleic acids produced by the methods of the invention or the proteins encoded thereby can be used to transfect/load antigen presenting cells. The loaded antigen presenting cells can then be used as a vaccine for the treatment of pathogen infection. In another embodiment, nucleic acids produced by the methods of the invention can be used directly as nucleic acid vaccines without prior loading into antigen presenting cells.

Abstract: The present invention provides novel sequences encoding Staphylococcus pseudintermedius proteins/nucleic acids potentially useful in the treatment and/or prevention of canine disorders. In particular, the various protein and/or nucleic acid sequences described herein may find application as vaccines for use in treating and/or preventing a variety of canine diseases and/or conditions caused or contributed to by Staphylococcus pseudintermedius.

Abstract: DIG-657 vegetative insecticidal toxins, polynucleotides encoding such toxins, use of such toxins to control pests, and transgenic plants that produce such toxins are disclosed. The invention includes DIG-657 variants, fragments and analogs.

Abstract: Provided are an artificially designed and modified insecticidal protein or a segment thereof. The insecticidal protein belongs to a Vip3A-type insecticidal protein. The protein or the segment thereof has an insecticidal activity against a pest, especially a lepidoptera pest. Also provided are a nucleic acid for coding the protein or the segment thereof, an insecticidal composition, a DNA constructor, and a transformed microorganism or a plant comprising the nucleic acid, and a method for controlling a pest, especially a plant pest.

Abstract: Described are methods and products useful for identifying subjects with Mycobacterium avium subspecies paratuberculosis (MAP). A number of protein antigens secreted into culture filtrate by MAP are identified and binding proteins selective for these antigens are demonstrated to be useful for detecting subjects with MAP infections including subjects with Johne's disease.

Abstract: The present invention is related to the use of compounds or pharmaceutically acceptable salts thereof that modulate astrocytic release of substances through connexin and pannexin hemichannels, for the treatment of psychiatric disorders. Compounds or pharmaceutically acceptable salts thereof used in the present invention comprise any compound that differentially modulates, blocks, opens, inhibits, and/or activates connexin and/or pannexin hemichannels from astrocytes while not affecting gap junctions. The invention is also related to a method for treating psychiatric disorders, comprising administering to a mammal or human a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof, that modulates astrocytic release of substances through connexin and pannexin hemichannels. Pharmaceutical compositions and a screening method are also considered in the present invention.

Abstract: A glycopeptide, comprising a polyproline backbone and one or more carbohydrate molecules.

Abstract: A spider venom (SV) 82 polypeptide has an amino acid sequence of SEQ ID NO: 2. An SV82 polypeptide-encoding gene having a nucleotide sequence of SEQ ID NO: 1 which is optimized for E. coli codon. A recombinant vector includes the SV82 polypeptide-encoding gene, An E. coli is transformed with the recombinant vector. A method of producing SV82 polypeptide includes transforming a host cell with the recombinant vector. A cosmetic composition for reducing skin wrinkles and maintaining skin elasticity includes SV82 polypeptide as an active ingredient.

Abstract: Compositions and methods are provided for alleviating endometriosis, kidney disease, inflammatory disease and/or transplant rejection in a mammal by administering a therapeutic dose of a pharmaceutical composition that inhibits AXL, MER or Tyro3 protein activity, for example by competitive or non-competitive inhibition of the binding interaction between AXL, MER or Tyro3 and its ligand GAS6.

Abstract: Embodiments of the invention are described, including materials and methods for making molecules and materials that have a specific binding domain of a PlGF2. Embodiments include, for instance, medicaments, biomaterials, biomolecules, molecular fusions, and vaccines.

Abstract: Compounds are provided having inter alia good duration of action, high potency and/or convenient dosing regimens including once weekly administration. The compounds are engineered polypeptides which incorporate an albumin binding domain in combination with one or more biologically active polypeptides. Also provided are pharmaceutical compositions and methods of treatment for diseases and disorders including lipodystrophy, dyslipidemia, hyperlipidemia, overweight, obesity, hypothalamic amenorrhea, Alzheimer's disease, leptin deficiency, fatty liver disease or diabetes (including type I and type II). Additional diseases and disorders which can be treated by the compounds and methods described herein include nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD), metabolic syndrome X and Huntington's Disease.