Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4, R5, R6, W1, W2, W3, A and X are as described herein, compositions including the compounds and methods of using the compounds for the treatment and prophylaxis of respiratory syncytial virus infection.

Abstract: The present invention relates to compounds of the formula (I) wherein R1a, R1b, R2, R3, and X are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), to methods for the preparation of such compounds of formula (I), and especially to their use as TPH modulators.

Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is N; W is: (i) —(CR3R3)1-4—; (ii) —(CR3R3)x—Y—(CR3R3)y—; Or (iii) —Y—(CR3R3)2—Y—; and Y, R1, R2, R3, R5, R6, R8, x, and y are defined herein. Also disclosed are methods of using such compounds as modulators of TNF?, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Abstract: The application relates to inhibitors of USP1 useful in the treatment of cancers, and other USP1 associated diseases and disorders, having the Formula: where R1, R2, R3, R3?, R4, R5, X1, X2, X3, X4, and n are described herein.

Abstract: The present invention relates to dihydropyrazolo[1,5-a]pyrimidine compounds of formula I, defined herein, as WNT pathways modulators, processes for making them, and pharmaceutical compositions comprising them. Methods of treatment of conditions mediated by WNT pathway signalling including cancer, fibrosis, stem cell and diabetic retinopathy, rheumatoid arthritis, psoriasis and myocardial infarction, comprising the compounds of formula I are also provided.

Abstract: The present invention provides a compound of formula (1), wherein R1, R2, R3, R4a, R4b, R5a and R5b are as defined in the description, which has an autotaxin inhibitory activity, a pharmaceutical composition comprising the compound as an active ingredient, and a method of prevention or treatment of a disease involving autotaxin, which is characterized by administering the compound.

Abstract: Compounds of formula (I) defined herein are phosphoinositide 3-kinases (PI3K) inhibitors and are useful for the treatment of disorders associated with PI3K enzymes.

Abstract: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3 and R4 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of JAK kinase-associated diseases and disorders, such as autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: 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: An oxime ester compound represented by general formula (I), wherein R1to R8 are as defined in the description, and n is 0 or 1; a photopolymerization initiator containing the compound; a photosensitive composition, alkali-developable photosensitive resin composition, and colored alkali-developable photosensitive resin composition containing the photopolymerization initiator; and a cured product of these compositions are provided. The compound is useful as a high-sensitivity photopolymerization initiator that has good stability and low sublimability and that efficiently absorbs, and is activated by, near-ultraviolet light, e.g., at 365 nm.

Abstract: The present invention relates to positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4) that may be used for the treatment of conditions such as Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.

Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.

Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.

Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.

Abstract: Processes for preparing oxymorphone are provided. Said processes encompass a step which is a hydrogenation of an 14-hydroxymorphinone salt in the presence of trifluoroacetic acid and/or a glycol.

Abstract: The present invention provides conformationally restricted 4-substituted 2,6-dimethylfuro[2,3-d]pyrimidine compounds and pharmaceutical compositions comprising these compounds. Preferably, the compounds exhibit dual inhibition of microtubule assembly and receptor tyrosine kinases. Methods of treating cancer comprising administering a therapeutically effective amount of at least one conformationally restricted 4-substituted 2,6-dimethylfuro[2,3-d]pyrimidine compound to a patient is disclosed.

Abstract: The invention relates to novel substituted pyrimidine compounds of general formula (I) in which the chemical groupings, substituents, variables and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.

Abstract: The present invention provides compounds of formula (I), wherein: R1 is unsubstituted C1-C6 alkyl; La is substituted or unsubstituted C1-C6 alkyl linker, substituted or unsubstituted C3-C10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R2 and R3 are each, independently, H, substituted or unsubstituted C1-C6 alkyl, or substituted or unsubstituted C6-C10 aryl; or alternatively, R2 and R3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S.

Abstract: The use of sGC stimulators, sGC activators alone, or in combination with PDE5 inhibitors for the prevention and treatment of fibrotic diseases, such as systemic sclerosis, scleroderma, and the concomitant fibrosis of internal organs.

Abstract: Disclosed herein are substituted 8-aminothieno[3,2-e][1,2,4]triazolo[4,3-b]pyridazine-7-carboxamide compounds, which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

Abstract: The invention provides deuterium-enriched isoindolinonyl-piperidinonyl conjugates, deuterium-enriched oxoquinazolin-3(4H)-yl-piperidinonyl conjugates, pharmaceutical compositions, and methods of using such conjugates and pharmaceutical compositions to treat cancer, angiogenesis disorders, immune disorders, and other medical disorders.

Abstract: The instant disclosure relates to (among other things) compounds that are derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine. The compounds provided possess unique effects and differences over other phenyltriazines known in the art.

Abstract: The invention relates to novel hydrates of dolutegravir sodium and to processes for their preparation. Furthermore, the invention relates to a novel crystalline form of dolutegravir sodium, which is a useful intermediate for the preparation of one of the novel hydrates. In addition, the invention relates to the use of the novel hydrates for the production of pharmaceutical compositions. Finally, the invention relates to pharmaceutical compositions comprising an effective amount of the novel hydrates, to oral dosage forms comprising said pharmaceutical compositions, to a process for preparing said oral dosage forms, and to the use of said pharmaceutical compositions or dosage forms in the treatment of retroviral infections such as HIV-1 infections.

Abstract: The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), LRKK2, EphA2, polo kinase 1, 2, 3, or 4, Ack1, Ack2, Abl, DCAMKL1, ABL1, Abl mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.

Abstract: The present invention provides a novel phenothiazine-pyridine compound that is an effective photosensitizer useful for photodynamic therapy. Also provided is a method for inhibiting cell proliferation or for treating a disease involving inappropriate cell proliferation.

Abstract: There are provided 5,6-dihydro-4H-benzo[b]thieno-[2,3-d]azepine derivatives which are useful in the treatment of respiratory syncytial virus (RSV) infection and for the prevention of disease associated with RSV infection.

Abstract: A catalyst includes a bis(2-pyridylmethyl)amine-based ligand. A method of forming a catalyst, may include: reacting bis(2-pyridylmethyl)amine-based compound with a terminal azide and/or a terminal alkyne in the presence of Cu(I) to form a bis(2-pyridylmethyl)amine-based ligand. A method of using such catalysts may include neutralizing toxicity of at least one organophosphorus-based compound by reacting the organophosphorus-based compound with a bis(2-pyridylmethyl)amine-based ligand-metal complex.

Abstract: Gold(I) complexes as antiproliferative or antitumor agents. The gold(I) ion is connected to a N-heterocyclic carbene and further coordinated to a selone ligand. Also described are a pharmaceutical composition incorporating the gold(I) complex, a method of synthesizing the gold(I) complex, and a method for treating a proliferative disorder (e.g.

Abstract: Provided are a lithium secondary battery having improved initial capacity and excellent cycle property, an electrolyte solution for the lithium secondary battery, and an additive for the electrolyte solution for the lithium secondary battery. The lithium secondary battery includes positive and negative electrodes both having a lithium-ion intercalation/de-intercalation ability, and a non-aqueous electrolyte solution contacted with the positive and negative electrodes. The non-aqueous electrolyte solution contains lithium hexafluorophosphate and a boroxine compound represented by (RO)3(BO)3 liquefying at 25° C. R(s) each independently represent an organic group of a linear chain alkyl group having 3 or more carbon atoms. Herein, the chain alkyl group may have a branch, and when the branch is included, the number of carbon atoms of the chain alkyl group constructing a linear portion thereof is 3 or more.

Abstract: The present document discloses an organosilicon modified photoinitiator represented by the general formula (I): wherein, R1 and R2 are each independently selected from the group consisting of C1-C20 alkyl, C2-C8 alkenyl, C5-C8 cycloalkyl, aryl C1-C3 alkyl; one of R3, R4, R5, R6, and R7 is SIL1-X, and the others are each independently selected from the group consisting of hydrogen, C1-C20 alkyl, C2-C8 alkenyl, C5-C8 cycloalkyl, aryl C1-C3 alkyl, and halogen; X is a direct bond or C1-C12 alkylene; and SIL1 and SIL2 are each independently represented by the formula —SiR8R9R10 or (R?SiO3/2)a(R?2SiO2/2)b(R??3SiO1/2)c, wherein R8, R9 and R10 are each independently selected from the group consisting of C1-C20 alkyl, C2-C8 alkenyl, C5-C8 cycloalkyl, aryl, and aryl C1-C3 alkyl, R?, R? and R?? each independently selected from the group consisting of C1-C20 alkyl, C2-C8 alkenyl, C5-C8 cycloalkyl, and phenyl C1-C3 alkyl, and a, b, and c are numbers that satisfy a?0, b?0, c>0, the ratio of a to c is from 0 to 10

Abstract: The present invention concerns a method for depolymerizing oxygenated polymer materials and the use of said method in the recycling of plastic materials and the preparation of aromatic compounds that can be used as fuel, synthesis intermediates and raw materials in the construction sectors and in the petrochemical, electrical, electronic, textile, aeronautical, pharmaceutical, cosmetics and agrochemical industries. The present invention also concerns the use of aromatic compounds obtained by the method for depolymerizing oxygenated polymer materials according to the invention, in the production of fuels, electronic components, plastic polymers, rubber, drugs, vitamins, cosmetic products, perfumes, food products, synthetic threads and fibers, synthetic leathers, glues, pesticides and fertilizers.

Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R12 or R13 on the A group is an amino substituent (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

Abstract: The present invention relates to a novel crystalline form of oxazolidinone antibiotics, which has advantages in the aspects of solubility, hygroscopicity, crystallinity and stability; the present invention also relates to a method for preparing the novel crystalline form, a pharmaceutical composition containing thereof and the use thereof in the preparation of drugs for treating and/or preventing diseases caused by microbial infection.

Abstract: In some embodiments, the present disclosure pertains to a compound, comprising a transition metal complex having the formula ?-[M (x,y)-L1 (w,v)-L2 (t,u)-L3]p+An?mZ?p?m. In an embodiment of the present disclosure ? may be ?. In another embodiment ? may be ?. In some embodiments of the present disclosure, M is a transition metal. In a related embodiment, p is an integer corresponding to the oxidation state of M. In some embodiments of the present disclosure, each of x, y, w, v, t, and u independently comprise R. In other embodiments, each of x, y, w, v, t, and u independently comprise S. In an embodiment of the present disclosure, each of L1, L2, and L3 independently is a ligand comprising a substituted diamine. In some embodiments, An? comprises a lipophilic anion, where m is from 1 to 3, and where Z? comprises an optional second anion.

Abstract: Provided are crystalline forms of nicotinamide riboside, including a Form II of nicotinamide riboside chloride: nicotinamide riboside chloride. Also disclosed are pharmaceutical compositions comprising the crystalline Form II of nicotinamide riboside chloride, and methods of producing such pharmaceutical compositions. In other aspects, the present disclosure pertains to methods comprising administering to a subject the crystalline Form II of nicotinamide riboside chloride. The present disclosure also provides methods of preparing the crystalline Form II of nicotinamide riboside chloride. Also provided are a crystalline Form II of nicotinamide riboside chloride that is prepared according to any of the disclosed methods for preparing the crystalline Form II.

Abstract: The invention provides compounds of the purine cyclic dinucleotide (CDN) class, useful as inhibitors of the STING (Stimulator of Interferon Genes) pathway, and methods of their administration to individuals in need thereof.

Abstract: Novel compositions and methods for engineering wireframe architectures and scaffolds of increasing complexity by creating gridiron-like DNA structures (FIG. 1). A series of four-arm junctions are used as vertices within a network of double-helical DNA fragments. Deliberate distortion of the junctions from their most relaxed conformations ensures that a scaffold strand can traverse through individual vertices in multiple directions. DNA gridirons, ranging from two-dimensional arrays with reconfigurability to multilayer and three-dimensional structures and curved objects, can be assembled according the methods presented herein.

Abstract: Provided are a peptide consisting of the amino acid sequence of SEQ ID NO:1 or a pharmaceutically acceptable salt thereof, and the use thereof. Cancer can be effectively prevented or treated by application of the peptide.

Abstract: A cell-penetrating peptide characterized in that it comprises an amino acid sequence consisting of XWXRLXXXXXX (SEQ ID No: 5), wherein X in position 1 is beta-A or S; X in positions 3, 9 and 10 are, independently from each other, W or F; X in position 6 is R if X in position 8 is S, and X in position 6 is S if X in position 8 is R; X in position 7 is L or none; X in position 11 is R or none, and wherein X in position 7 is L if X in position 11 is none.

Abstract: The invention provides a recombinant polypeptide comprising the EDIII domain of each of Dengue virus serotype DENV-1, DENV-2, DENV-3, and DENV-4 linked to the N-terminal of HBsAg.

Abstract: Ebolavirus is a highly lethal filovirus that causes hemorrhagic fever in humans and non-human primates. With no approved treatments or preventatives, the development of an anti-ebolavirus therapy to protect against natural infections and potential weaponization is an urgent unmet global health need. The design, biophysical characterization, and validation of peptide mimics of the ebolavirus N-trimer (“N-trimer mimics”) are described herein.

Abstract: The object of the present invention is to, by analyzing PPR proteins that act to bind to DNA with a prediction that RNA recognition rules of PPR motifs can also be used for recognition of DNA, find a PPR protein showing such a characteristic. According to the present invention, it was revealed that, with a protein that can bind in a DNA base-selective manner or a DNA base sequence-specific manner, which contains one or more, preferably 2 to 30, more preferably 5 to 25, most preferably 9 to 15, of PPR motifs having a structure of the following formula 1 (wherein, in the formula 1, Helix A is a part that can form an ?-helix structure; X does not exist, or is a part consisting of 1 to 9 amino acids; Helix B is a part that can form an ?-helix structure; and L is a part consisting of 2 to 7 amino acids), and having a specific combination of amino acids corresponding to a DNA base or DNA base sequence as amino acids of three positions of No. 1 A.A., No. 4 A.A., in Helix A of the formula 1 and No. “ii” (?2) A. A.

Abstract: The technology relates in part to compositions and methods for inducing an immune response against a Bob1 antigen. Provided are methods for treating hyperproliferative diseases by inducing an immune response against a Bob1 antigen; the immune response may be induced using a Bob1 polypeptide fragment, or by specifically targeting Bob1-expressing cells using T cell receptors directed against Bob1.

Abstract: This disclosure provides an isolated polypeptide comprising no more than 35 amino acids, wherein the amino acid sequence comprises, or alternatively consists essentially of, or alternatively consisting of XXXRYSYXXSYX (SEQ ID NO: 1) and equivalents thereof, wherein X is a basic amino acid and Y is a hydrophobic amino acid. Polynucleotides encoding the polypeptides and antibodies that bind to the polypeptides are also provided. Therapeutic and diagnostic uses are further provided.

Abstract: In certain aspects, the present disclosure provides compositions and methods for increasing red blood cell and/or hemoglobin levels in vertebrates, including rodents and primates, and particularly in humans. In some embodiments, the compositions of the disclosure may be used to treat or prevent sideroblastic anemias and myelodysplastic syndromes or one or more complications associated sideroblastic anemias and myelodysplastic syndromes.

Abstract: Modified FGF-21 polypeptides and uses thereof are provided, for example, for the treatment of diseases associated with fibrosis. Modified FGF-21 polypeptides are disclosed that contain an internal deletion and optionally replacement peptide, optionally modified with at least one non-naturally-encoded amino acid, and/or optionally fused to a fusion partner.

Abstract: The invention includes a thioamide-modified peptide, wherein the thioamide modification increases the in vivo half-life of the peptide. The invention further includes methods of treating or preventing a disease or disorder in a subject in need thereof, the method comprising administering to the subject a thioamide-modified peptide of the invention.

Abstract: The present invention provides recombinant proteins or peptides comprising a mutated listeriolysin O (LLO) protein or fragment thereof, comprising a substitution or internal deletion of the cholesterol-binding domain or a portion thereof, fusion proteins or peptides comprising same, nucleotide molecules encoding same, and vaccine vectors comprising or encoding same. The present invention also provides methods of utilizing recombinant proteins, peptides, nucleotide molecules, and vaccine vectors of the present invention to induce an immune response to a peptide of interest.

Abstract: The present invention relates to peptides, proteins, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer. The present invention furthermore relates to tumor-associated T-cell peptide epitopes, alone or in combination with other tumor-associated peptides that can for example serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses, or to stimulate T cells ex vivo and transfer into patients. Peptides bound to molecules of the major histocompatibility complex (MHC), or peptides as such, can also be targets of antibodies, soluble T-cell receptors, and other binding molecules.

Abstract: The present invention relates to polypeptides and uses thereof for reducing CD95-meditated cell motility. In particular, the present invention relates to a polypeptide having an amino acid sequence having at least 70% of identity with the amino acid sequence ranging from the amino-acid residue at position 175 to the amino-acid residue at position 191 in SEQ ID NO:1.