Abstract: The present invention provides compounds useful for the treatment of narcolepsy or cataplexy in a subject in need thereof. Related pharmaceutical compositions and methods are also provided herein.

Abstract: A macrocyclic TLR7 agonist, a preparation method therefor, a pharmaceutical composition and use thereof. The macrocyclic TLR7 agonist disclosed is as represented by formula I, has good TLR7 agonistic activity, and can be used for treating or preventing tumors or infections caused by viruses.

Abstract: The present invention relates to pharmaceutical agents of formula (I) useful for therapy and/or prophylaxis in a subject, pharmaceutical composition comprising such compounds, and their use as MCL-1 inhibitors, useful for treating diseases such as cancer.

Abstract: The present invention concerns aza-cryptophanes, processes for preparation thereof, and their uses, in particular as in vivo diagnostic tools when complexing a hyperpolarized noble element, or in nanoemulsions.

Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein X, Y, A, G, R1, and R5 are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Abstract: Disclosed herein are compounds that are Hematopoietic Progenitor Kinase 1 (HPK1) inhibitors having a structure according to Formula I, and compositions containing those compounds. Methods of preparing the compounds, and methods of using the compounds for the treatment of diseases, disorders, or conditions are also described.

Abstract: The present disclosure relates to compounds and methods for modulating the expression of fxn, and treating diseases and conditions in which fxn plays an active role. The compound can be a transcription modulator molecule having a first terminus, a second terminus, and oligomeric backbone, wherein: a) the first terminus comprises a DNA-binding moiety capable of noncovalently binding to a trinucleotide repeat sequence GAA; b) the second terminus comprises a protein-binding moiety binding to a regulatory molecule that modulates an expression of a gene comprising the nucleotide repeat sequence GAA; and c) the oligomeric backbone comprising a linker between the first terminus and the second terminus.

Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where R1 and R2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.

Abstract: The present invention relates to novel novel monocyclic and bicyclic ring system substituted carbanucleoside analogues of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as PRMT5 inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Abstract: Described are multi-resonance-thermally-activated delay-fluorescence compounds containing (i) a polycyclic aromatic/heteroaromatic ligand in which a plurality aromatic/heteroaromatic rings are linked by boron and nitrogen atoms and (ii) an N-heterocyclic carbene ligand, with both ligands coordinated to a metal atom/ion that has a high spin-orbit coupling. The use of the high spin-orbit coupling of metals and/or metal ions facilitates the intersystem crossing and/or reversed intersystem crossing processes of MR-TADF emitters, thereby largely accelerating the rate of TADF and substantially shortening the lifetime of deleterious triplet excitons. The MR-TADF emitters can be used to fabricate blue to green emitting OLEDs.

Abstract: The present disclosure provides a novel compound represented by the following Chemical Formula 1, and an organic light emitting device including the same: wherein R1, R2, and n1 are described herein.

Abstract: The invention provides a method for producing radiolabeled tyrosine derivatives with good purity and stability, by a safe method suitable for industrial production of pharmaceuticals. The invention relates to a method for producing Compound (5) and Radiolabeled Compound (6) as follows: wherein each symbol is as defined in the description.

Abstract: Embodiments provide a fused polycyclic compound and a light emitting device including the fused polycyclic compound.

Abstract: Disclosed is a transition metal compound that exhibits high activity and high comonomer incorporation in olefin polymerization and can be used for preparing a polyolefin having a BOCD structure, a method for preparing the same, and a catalyst composition including the same.

Abstract: A method for preparing a siloxane-(meth)acrylate macromonomer is provided. The method includes hydrosilylation, hydrolysis, and condensation. By-products of the method may be recycled to produce additional siloxane-(meth) acrylate macromonomer. An exemplary siloxane-(meth)acrylate macromonomer prepared by the method is 3-(1,1,1,3,5,5,5-heptamethyltrisiloxan-3-yl)propyl methacrylate.

Abstract: Cyclic azastannanes and cyclic oxostannanes having formulas (I) and (II) where X is an alkoxy or dialkylamino group are a new class of cyclic compounds. These compounds have desirably high vapor pressure and high purity (containing low levels of polyalkyl contaminants after purification), and have particular interest for EUV photoresist applications. Methods for preparing these compounds are described.

Abstract: Disclosed are vanadium (V) compounds and pharmaceutical compositions comprising these vanadium compounds. Also disclosed are methods of making and using these vanadium compounds, for example, to treat cancer (e.g., including brain cancer).

Abstract: Organometallic complexes are described which are useful as pre-polymerization catalysts which may form part of olefin polymerization catalyst systems. The catalyst systems find use in the polymerization of ethylene, optionally with one or more C3-12 alpha-olefin comonomers. The organometallic complexes are broadly represented by formula I: wherein L is a bridging group containing a contiguous chain of atoms connecting P with Cy, wherein the contiguous chain contains 2 or 3 atoms and wherein Cy is a cyclopentadienyl-type ligand. The olefin polymerization catalyst system is effective at polymerizing ethylene with alpha-olefins in a solution phase polymerization process at high temperatures and produces ethylene copolymers with high molecular weight and high degrees of alpha-olefin incorporation. Pre-metallation compounds, metallation processes and synthetic methods to make the organometallic complexes as well as polymerization processes are also described.

Abstract: The present invention relates to chromen-4-one derivatives comprising a phosphonium quaternary group, and to associated multi-salts, solvates, prodrugs and pharmaceutical compositions. The present invention also relates to the use of such compounds and compositions in the treatment and prevention of cancer.

Abstract: An aromatic heterocyclic compound, and a pharmaceutical composition and an application thereof. Specifically disclosed are a compound as represented by formula I-A, a stereoisomer thereof, a diastereoisomer thereof, or a pharmaceutically acceptable salt of any one of the described substances, or a crystalline form or a solvate of any one of the described substances. The aromatic heterocyclic compound is novel in structure, and has good CDK7 inhibitory activity and good selectivity.

Abstract: An organometallic compound represented by Formula 1: M1(L1)n1(L2)n2??Formula 1 wherein, M1 is a transition metal, L1 is a ligand represented by Formula 1A, L2 is a ligand represented by Formula 1B, and n1 and n2 are each independently 1 or 2, wherein X1 is C or N, X2 is C or N, at least one R2 is a C1-C10 alkyl group that is substituted with a fluorine, b1 is an integer from 1 to 6, b2 is an integer from 1 to 10, * and *? each indicate a binding site to M1, and the other substituent groups of Formulae 1A and 1B are as described herein.

Abstract: A compound, Ir(LA)(LB)(LC), having a structure of Formula I, is provided. In Formula I, LA includes moieties E and F, LB includes moieties A and B, and LC includes moieties C and D. In addition, moieties A, B, C, D, E, and F are independently monocyclic rings or polycyclic fused ring systems; each of Z1 to Z6 is C or N; three of Z1 to Z6 form covalent bonds to Ir, while the remaining three form dative bonds to Ir; one of Z2 and Z3 forms a covalent bond to Ir, and the other forms a dative bond to Ir; each of L1, L2, L3, and L4 is a direct bond or an organic linker; and each RA, RB, RC, RD, RE, and RF is hydrogen or a General Substituent.

Abstract: An organometallic compound represented by Formula 1: M1(L1)n1(L2)n2??Formula 1 wherein, in Formula 1, M1 is a transition metal, L1 is a ligand represented by Formula 1A, L2 is a ligand represented by Formula 1B, and n1 and n2 are each independently 1 or 2: wherein, X1 is C or N, X2 is C or N, Y1 is O, S, Se, C(R41)(R42), or N(R43), at least one R2 is a C1-C10 alkyl group that is substituted with a fluorine, b2 is an integer from 1 to 6, b11 is 1 or 2, b12 is an integer from 1 to 4, * and *? each indicate a binding site to M1, and the other substituent groups in Formulae 1A and 1B are as described herein.

Abstract: A compound having the following formula is disclosed. The compound is useful as an emitter in OLED applications.

Abstract: The present invention concerns a method for separating different oligosaccharides having at least one carboxylic acid group by contacting them with basic anion exchange resins.

Abstract: The present invention relates to compounds of the following formula (I): as well as their preparation process; their use in cosmetic or dermatological applications, in particular for the treatment and/or prevention of skin aging, skin protection or skin regeneration; for skin plumping and/or skin volumizing and/or skin densifying, and/or wrinkle filling and/or skin or hair moisturising and/or skin or hair relipiding and/or stimulation of hair growth; for the treatment of dry skin and/or atopic dermatitis and/or eczema and/or psoriasis; for the treatment and/or prevention of a fibrosis disease (e.g. an excessive scar such as a keloid or hypertrophic scar) or for healing; or for the treatment of inflammation (e.g. chronic, low-grade inflammation); and their use as adjuvant for preservation and/or protection and/or regeneration of a biological material or a microorganism.

Abstract: The disclosure provides compositions and methods related to activating alpha-kinase 1 (ALPK1) for modulating an immune response and treating or preventing cancer, infection, inflammation and related diseases and disorders as well as potentiating an immune response to a target antigen. The disclosure also provides heterocyclic compounds of formula (I) as agonists of alpha protein kinase 1 (ALPK1) and their use in activating ALPK1, modulating an immune response and treating diseases such as cancer, wherein A1, A2, L1, L2, L3, Z1, Z2, W1, W2, R1, R2, R3, R4, R5, R6 and R7 are defined herein.

Abstract: Described herein are CD73 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of cancer, infections, and neurodegenerative diseases.

Abstract: Provided are oligomeric compounds, methods, and pharmaceutical compositions for reducing the amount or activity of methyl CpG binding protein 2 (MECP2) RNA in a cell or animal, and in certain instances reducing the amount of MECP2 protein in a cell or animal Such oligomeric agents, oligomeric compounds, methods, and pharmaceutical compositions are useful to ameliorate at least one symptom or hallmark of a neurodevelopmental disease or disorder. Such neurodevelopmental diseases or disorders include MECP2 duplication syndrome. Such symptoms or hallmarks include autism, intellectual disability, motor dysfunction, hypotonia, global developmental delays, gastrointestinal symptoms, anxiety, epilepsy, recurrent respiratory tract infections, epileptic encephalopathy, and early death.

Abstract: Provided are a deoxynucleoside modified ruthenium complex, and a preparation method and use thereof, The deoxynucleoside modified ruthenium complex has a structure represented by Formula I, wherein R represents one selected from the group consisting of trifluoromethyl, C1-6 alkyl, alkoxy, halogen, styryl, and nitro-substituted styryl.

Abstract: Described herein are novel LIF/LIFR inhibitors that exhibit improved cytotoxicity and bioavailability. These LIF/LIFR inhibitors are particularly useful for the treatment of tumors associated with overexpression of LIF.

Abstract: A method of producing a polypeptide compound, wherein a peptide compound represented by formula (P) is obtained by inducing an amide formation reaction between an amino-protected lactam compound represented by formula (R1) and an amino acid ester or peptide ester compound represented by formula (R2). The definitions for the reference signs in formulae (R1), (R2), and (P) are as set forth in the claims.

Abstract: An object of the present invention is to provide a method for efficiently producing a high-purity peptide compound with a high yield. It has been found that the object can be achieved by supporting a peptide on a solid phase synthesis resin prior to a first elongation reaction in a solid phase process.

Abstract: The present invention relates to purified peptidomimetic macrocycles. The invention additionally provides methods of preparing and using such macrocycles, for example in therapeutic applications.

Abstract: Herein is reported the use of an immobilized non-covalent complex of a neonatal Fc receptor (FcRn) and beta-2-microglobulin (b2m) as affinity chromotography ligand in general and, for example, for the determination of the in vivo half-live of an antibody by determining the ratio of the retention times of the antibody and a reference antibody.

Abstract: N-Acylated histidine dipeptides of formula are disclosed. The compounds are useful for treating breast cancer.

Abstract: Provided is a peptide compound comprising the amino acid sequence: G-W-Lys-X1-Ser-U-X2-Y-Z-Q wherein: G represents an optional N-terminal a 3,4-dihydrocinnamic acid group; W represents Ala or Ser, or is absent; U represents Tyr, DOPA or a single bond; X1 and X2 independently represent Pro, Hyp or diHyp; Y represents a single bond or represents a 1 to 5 amino acid sequence, in which the amino acids are selected from one or more of the group Pro, Hyp, diHyp, Thr, DOPA and Tyr; Z represents Pro, Hyp, diHyp, Thr, DOPA or Tyr; and Q represents Lys or is absent, as well as regioisomers, stereoisomers, and pharmaceutically- or cosmetically-acceptable salts of said peptide compound, provided that when G is not present, W represents Ala or is absent and Q represents Lys, then Z represents Pro, Hyp, diHyp or Thr.

Abstract: The present invention relates to novel Mannose-binding lectin (MBL)-associated serine protease (MASP) inhibitory compounds, as well as analogues and derivatives thereof, to processes 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 renal and cardiovascular disorders and of ischemia reperfusion injuries.

Abstract: The present invention provides methods for guiding preservation of human neurons or human nerves during surgery by administering a fluorescently-labeled peptide that specifically binds to the human neurons or human nerves. The invention further provides human neuron or nerve targeting molecules comprising fluorescently-labeled peptides that specifically bind to human neurons or human nerves and compositions thereof.

Abstract: The present disclosure relates to agonists of Tacr2, such as peptides agonist of Tacr2 and methods of using the same for treatment of insulin resistance, obesity and/or diabetes. The disclosure also relates to use of said agonists of Tacr2 for enhancement of energy consumption in an individual.

Abstract: The present invention provides a new type of alpha-helix nucleating cross-link (“staple”) formed by olefin metathesis of a proline derivative with an alkenyl side chain and another amino acid derivative with an alkenyl side chain. The proline derivatives as described herein have been found to be strong nucleators of alpha-helix formation. The invention also provides moieties for shielding the free amide N—H's at the N-terminus of an alpha-helix, thereby further stabilizing the helix. The proline derivatives, precursors prior to cross-linking, and the cross-linked peptides are provided as well as methods of using and preparing these compounds and peptides.

Abstract: Described herein are isolated peptides, compositions comprising the same, and methods of using such peptides or compositions in the treatment of depression, central nervous system disorders, and neurodevelopmental disorders.

Abstract: Disclosed herein, are decoy peptides or polypeptides capable of neutralizing and/or inhibiting the binding of anti-Ro antibodies to a hERG potassium channel extracellular pore region, and pharmaceutical compositions containing the decoy peptides or polypeptides and methods of use.

Abstract: The present invention relates to an antagonist of interleukin-17B receptor (IL-17RB) which features interruption of the interaction of IL-17RB and MLK4. The present invention also relates to use of such antagonist for treatment of diseases or disorders associated with IL-17RB activation. Further disclosed is a phosphorylated IL-17RB as a biomarker for predicting prognosis and/or monitoring progression of cancer.

Abstract: Disclosed herein are cross-linked peptides useful for interfering with and inhibiting coronavirus infection (e.g., infection by SARS-CoV-2). Also disclosed are methods of treating and/or preventing a coronavirus infection (e.g., COVID-19).

Abstract: The present invention relates to RNA constructs, and particularly, although not exclusively, to mRNA constructs and saRNA replicons and to nucleic acids and expression vectors encoding such RNA constructs. The invention extends to the use of such RNA constructs in therapy, for example in treating diseases and/or in vaccine delivery. The invention extends to pharmaceutical compositions comprising such RNA constructs, and methods and uses thereof.

Abstract: The invention relates to variants of OB-fold proteins, in particular of the Sac7d family that bind to human and mouse serum albumin and that can be used to increase serum half-life of elements associated therewith.

Abstract: Chlamydiae are intracellular bacterial pathogens responsible for a variety of infections. The inventors have set up candidate vaccines against Chlamydia trachomatis. In particular, the inventors have identified specific epitopes to be included in vaccine candidates thanks to in silico analysis of the amino-acid sequence of these proteins to map predicted MHC-I and -II epitopes by online software (NetMHC-4.0 and NetMHCII-2.3) and peptide binding prediction software. B cell epitopes were also mapped using online software (BepiPred-2.0 and Discotope). Finally, the inventors have generated some specific CD40 or Langerin antibodies comprising one or more identified epitope(s) of the present invention and that are suitable for vaccine purposes. Therefore, the present invention relates to Chlamydia trachomatis (Ct) antigenic polypeptides and uses thereof for vaccine purposes.

Abstract: A HER2-binding polypeptide is provided, comprising the amino acid sequence SEQ ID NO: 1. Also provided is a radiolabeled polypeptide consisting of a radiochelate of the HER2-binding polypeptide and a radionuclide. Also provided are methods and uses employing the polypeptide in therapeutic, diagnostic and prognostic applications, e.g. relating to cancers characterized by overexpression of HER2.

Abstract: Disclosed is a fusion protein including an Ixodes ricinus salivary gland polypeptide. In particular, it relates to a fusion protein including at least one Ixodes ricinus salivary gland polypeptide, at least one serum albumin polypeptide and at least one linker peptide. Also disclosed is the use of such a fusion protein for preventing or treating thrombus formation and/or thrombus growth, as well as pharmaceutical compositions, medicaments and methods including such a fusion protein.