Abstract: Disclosed herein are methods and compounds for inducing DDB1- and CUL4-associated factor 16 (DCAF16)-mediated protein degradation in mammalian cells. In some embodiments, also disclosed herein are methods of modulating the substrate selectivity of a DCAF16-CUL4-RBX1-DDB1 complex (CRL4) for modulating protein degradation.
Type:
Application
Filed:
October 11, 2019
Publication date:
June 18, 2020
Inventors:
Benjamin CRAVATT, Vincent CROWLEY, Xiaoyu ZHANG
Abstract: A chromene compound having at least one indenonaphthopyran moiety which has a group forming a spiro ring together with the 13-position carbon atom and further an oligomer chain group selected from a polyalkylene oxide oligomer chain group having at least three recurring units and a polyester oligomer chain group having at least three recurring units, represented by the following formula and having reduced matrix dependence: wherein R1 and R2 are each a group which may have an oligomer chain group, the ring Z bonded to the 13-position carbon atom of the chromene compound is a Spiro ring group, and R3 and R4 are each an aryl group or heteroaryl group which may have an oligomer chain group. Preferably, the chromene compound has at least one oligomer chain group in the molecule.
Abstract: Disclosed is a novel quinazoline compound. Specifically, disclosed are a compound represented by the formula (I) and a pharmacologically acceptable salt.
Type:
Application
Filed:
December 29, 2017
Publication date:
June 18, 2020
Inventors:
Xile LIU, Charles Z. DING, Shuhui CHEN, Lingyun WU, Lihong HU, Haiwen WAN
Abstract: The present invention relates to a pyridinium oxazole dyad scaffold of formula (I) and a process for the preparation thereof. The present invention further discloses a pyridine compound of formula (II) which is used for the preparation of formula (I) and a process for preparation thereof.
Abstract: The disclosure includes compounds of Formula (A): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12, j, k, m, n, Y, W, W1, W2, W3, V, L, Z1, Q1, Q2, Q3, and Q4, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.
Abstract: The present disclosure relates to certain macrocyclic derivatives, pharmaceutical compositions containing them, and methods of using them to treat disease, such as cancer.
Type:
Application
Filed:
January 30, 2020
Publication date:
June 18, 2020
Applicant:
Turning Point Therapeutics, Inc.
Inventors:
Evan W. Rogers, Jingrong J. Cui, Dayong Zhai, Han Zhang, Jane Ung, Wei Deng, Jeffrey Whitten
Abstract: The present invention covers bicyclic pyrazole compounds of general formula (I): in which G, A, R1, R2, R3, and Q are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.
Type:
Application
Filed:
April 23, 2018
Publication date:
June 18, 2020
Applicant:
Bayer Animal Health GMBH
Inventors:
Nils GRIEBENOW, Wei ZHUANG, Daniel KULKE, Adeline KÖHLER, Thomas ILG, Claudia WELZ, Hans-Georg SCHWARZ, Ulrich GÖRGENS, Walter HÜBSCH, Johannes KÖBBERLING
Abstract: The present invention provides bicyclic heterocyclyl kinase enzyme inhibitor compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors. wherein A, Y, Z, X1, X2, X3, R1, R3, ‘m’, ‘n’ and ‘p’ have the meanings given in the specification and pharmaceutically acceptable salt or stereoisomer thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical composition comprising at least one of the compounds of compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
Abstract: A condensed cyclic compound is represented by Formula 1. An organic light-emitting device includes: a first electrode; a second electrode; and an organic layer between the first electrode and the second electrode and comprising an emission layer, the organic layer including the condensed cyclic compound represented by Formula 1. A display apparatus includes: a thin-film transistor comprising a source electrode, a drain electrode, and an active layer; and the organic light-emitting device.
Type:
Application
Filed:
July 17, 2019
Publication date:
June 18, 2020
Inventors:
Seulong Kim, Sunwoo Kang, Pilgu Kang, Jiyoung Kwon, Taekyung Kim, Soonchul Chang, Dahye Cho
Abstract: A zinc-based metal organic framework and method of making is described. The zinc-based metal organic framework is in the form of an interpenetrating diamondoid framework where each Zn2+ ion center is linked with four other Zn2+ ion centers in a distorted tetrahedral geometry. The linking occurs through diamine and dicarboxylic acid linkers. The zinc-based metal organic framework may be deposited on a transparent conducting film and used as a photoelectrode for photoelectrochemical water splitting.
Type:
Application
Filed:
April 25, 2019
Publication date:
June 18, 2020
Applicant:
King Fahd University of Petroleum and Minerals
Abstract: The present invention provides a novel polycyclic aromatic compound having a plurality of aromatic rings linked by a boron atom, a nitrogen atom, and the like, and thus increases the number of alternatives of a material for an organic electroluminescent (EL) device. Furthermore, the present invention provides an excellent organic EL device by using a novel polycyclic aromatic compound as a material for an organic EL device.
Abstract: The objective of the invention is to provide a polycyclic aromatic compound in which solubility to a solvent, film formability, wet coatability, thermal stability, and in-plane orientation are improved. This objective is achieved by a light emission layer-forming composition comprising: as a first component, at least one type of dopant material selected from the group consisting of polycyclic aromatic compounds represented by general formula (A) and polycyclic aromatic oligomer compounds including a plurality of structures represented by general formula (A); as a second component, a specific low-molecular-weight host material; and, as a third component, at least one type of organic solvent. In formula (A), ring A, ring B, and ring C each independently represent an aryl ring or a hetero aryl ring, Y1 is B, and X1 and X2 each independently represent O or N—R wherein at least one of X1 and X2 is N—R.
Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
Abstract: The present disclosure encompasses solid state forms of Ixazomib Citrate and pharmaceutical compositions thereof. Also disclosed are processes for preparation of Ixazomib Citrate.
Type:
Application
Filed:
February 26, 2020
Publication date:
June 18, 2020
Inventors:
Martin VALIK, Roman GABRIEL, Pavel VRASPIR, David LUKAS
Abstract: The present invention relates to process for the preparation of 5-(4-cyano phenoxy)- 1,3-dihydro-1-hydroxy-[2,1]-benzoxaborole represented by the following structural formula-1 and polymorphs thereof. The present invention also relates to salts of 5-(4-cyano phenoxy)-1,3-dihydro-1-hydroxy-[2,1]-benzoxaborole and process for their preparation and their use in the preparation of pure compound of the formula-1.
Type:
Application
Filed:
May 23, 2018
Publication date:
June 18, 2020
Applicant:
MSN LABORATORIES PRIVATE LIMITED, R&D CENTER
Abstract: The present invention relates to an organic electroluminescent device comprising a light-emitting layer B containing at least one host compound H of Formula (I) wherein each of X?1 and X?2 is independently from another selected from the group consisting of nitrogen and an optionally substituted carbon atom, and wherein at least one of R?1—R?10 is CN and at least one of RA—RE is a substituted silane residue.
Abstract: The present disclosure provides a delayed fluorescent compound of following Formula, and an organic light emitting diode including a first electrode, a second electrode and an organic emitting layer between the first and second electrodes, where the delayed fluorescent compound is included in the organic emitting layer, and an organic light emitting display device including the organic emitting compound.
Type:
Application
Filed:
December 3, 2019
Publication date:
June 18, 2020
Applicant:
LG Display Co., Ltd.
Inventors:
Suk-Young BAE, In-Ae SHIN, Jun-Yun KIM, Ik-Rang CHOE
Abstract: A method of producing a halosiloxane, the method comprising: i) combining water, a halosilane, and a first solvent to form a reaction mixture, ii) partially hydrolyzing and condensing the halosilane to form a reaction product mixture comprising the halosiloxane, the solvent, unreacted halosilane, and hydrogen halide, iii) adding a second solvent, where the second solvent has a boiling point the boiling point of the halosiloxane, to the reaction mixture in i) or to the reaction product mixture in ii), and iv) recovering the halosiloxane from the reaction product mixture.
Type:
Application
Filed:
May 24, 2018
Publication date:
June 18, 2020
Inventors:
Noel Mower Chang, Barry Ketola, Andrew Millward, Xiaobing Zhou
Abstract: Nanoscale metal halide perovskites are provided. The nanoscale metal halide perovskites may have a 2D structure, a quasi-2D structure, or a 3D structure. Methods also are provided for making the nanoscale metal halide perovskites. The color emitted by the nanoscale metal halide perovskites may be tuned.
Abstract: The present disclosure involves a composition enriched in compound 61501b, wherein the compound 61501b has a purity of not less than 90% or more. The composition has a significant advantage in preparing a high-purity compound Sp-1. In addition, the present disclosure also provides a preparation method of the composition enriched in compound 61501b. The method adopts a crystallization technique to perform separation and purification, has a simple and convenient operation and good reproducibility, and therefore the compound 61501b in the prepared composition has high purity and quality. Further, the present disclosure also involves a novel crystal form of compound 61501b.
Abstract: The present invention provides various compositions, including compounds of Formula (I) or (Ia), or a species thereof, and pharmaceutically acceptable salts, solvates (e.g., hydrates), stereoisomer, tautomers, isotopic and other specified forms thereof. Also provided are methods (or uses) and kits involving the compounds or pharmaceutically acceptable compositions containing them for treating or preventing a disease (e.g., a proliferative disease such as cancer) in a subject. Administration of a compound or pharmaceutical composition described herein is expected to inhibit cyclin-dependent kinase 7 (CDK7), and thereby, induce apoptosis in tumor cells in the subject.
Type:
Application
Filed:
February 11, 2020
Publication date:
June 18, 2020
Inventors:
Jason J. Marineau, Michael Bradley, Claudio Edmundo Chuaqui, Stephane Ciblat, Anzhelika Kabro
Abstract: The present invention relates to a new crystal form of bis(diphenylimidazolidinetrithione-?S4, ?S5)-, (SP-4-1)-nickel(II), a printing ink formulation for security printing and security documents, comprising the new crystal form of bis(diphenylimidazolidinetrithione-?S4, ?S5)-, (SP-4-1)-nickel(II) as well as its use as IR absorber.
Type:
Application
Filed:
September 18, 2018
Publication date:
June 18, 2020
Applicant:
BASF SE
Inventors:
Helmut REICHELT, Hans REICHERT, Oliver SEEGER, Korinna DORMANN, Rene FISCHER, Christian DOERR
Abstract: Embodiments of the present disclosure are directed towards metal complexes that can be utilized to form polymers. As an example, the present disclosure provides a metal complex of Formula I: wherein each Me represents methyl.
Abstract: Compounds and methods for purifying oligonucleotides such as RNA and DNA. A target oligonucleotide is reacted with an orthoester linker comprising an affinity tag to form an orthoester oligonucleotide-orthoester linker conjugate which is subjected to a purification technique to separate the target oligonucleotide from impurities such as truncated oligonucleotides. The orthoester linker can be then removed under mild conditions to generate the target oligonucleotide in high purity.
Type:
Application
Filed:
August 17, 2018
Publication date:
June 18, 2020
Inventors:
Douglas J. DELLINGER, Joel MYERSON, Brian SMART
Abstract: New 2-deoxy-2,3-dehydro-sialic acids and 2,7-anhydro-sialic acids, which are useful as sialidase inhibitors, and enzymatic methods for preparing them are disclosed. The methods include forming a reaction mixture comprising a glycoside acceptor, a sialic acid donor, and a sialyltransferase; maintaining the reaction mixture under conditions sufficient to form a sialoside; and contacting the sialoside with a Streptococcus pneumoniae sialidase to form the sialic acid product. Methods for the inhibition and sialidases and the treatment of cancer and infectious diseases are also disclosed.
Type:
Application
Filed:
April 27, 2018
Publication date:
June 18, 2020
Inventors:
Xi CHEN, An XIAO, Wanqing LI, Xixuan LI, Yanhong LI, Teri SLACK
Abstract: The present invention relates to novel Inclusion Complexes of Compound A, compositions comprising an Inclusion Complex of Compound A, and methods of using the Inclusion Complexes of Compound A for preparing compositions useful for treating or preventing HCV infection in a patient, wherein Compound A has the structure:
Type:
Application
Filed:
December 11, 2019
Publication date:
June 18, 2020
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Michael J. McNevin, Alfred Lee, Jason T. Ash, Itzia Arroyo, Binfeng Xia
Abstract: The disclosure relates to nucleic acids that contain modifications at the 5?-end, 3?-end or 5?-end and 3?-ends, and compounds that can be used to make the modified nucleic acids are disclosed. The modified nucleic acids have improved expression, lower immunogenicity and improved stability compared to unmodified nucleic acids.
Type:
Application
Filed:
February 26, 2020
Publication date:
June 18, 2020
Inventors:
David BARNES-SEEMAN, Scott Louis COHEN, John Louis DIENER, Christian GAMPE, James ROACHE, Amy WHITE, Sarah Louise WILLIAMS, Jun YUAN, Frederic ZECRI
Abstract: Described herein are solid state 17?-ethynylandrost-5-ene-3?,7?,17?-triol including amorphous and crystalline forms and specific polymorphic forms thereof, and use of solid state 17?-ethynylandrost-5-ene-3?,7?,17?-triol in treating numerous diseases and disorders, including hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions, and neurodegenerative conditions in subjects or human patients.
Type:
Application
Filed:
October 10, 2019
Publication date:
June 18, 2020
Inventors:
Steven K. White, Igor Ivanisevic, Kyle Stephens, Mark Andres, Brenton Skylar Wolfe
Abstract: Compounds and methods of synthesizing oxysterols are provided. The compounds and methods provided allow the oxysterol to be safely produced at a high yield. The compounds and methods provided can produce the oxysterol in a stereoselective manner.
Type:
Application
Filed:
February 14, 2020
Publication date:
June 18, 2020
Inventors:
Roger E. Harrington, Jerbrena C. Jacobs, Damodaragounder Gopal, Ke-Qing Ling, Marco Burello
Abstract: A method for the synthesis of a molecular lasso structure in which a linear moiety is covalently attached to a cyclic moiety and with its free end is partially threaded through the orifice formed by the cyclic moiety, including the following steps: 1) provision of a cyclic and a first linear structural element and establishing conditions in which the first linear structural element is threaded through the orifice of the cyclic moiety; 2) covalently attaching a stopper element to one terminal end of the linear structural element; 3) separating unthreaded from threaded molecular assemblies by chemical or physical separation; and 4) reacting the threaded molecular assemblies with a second linear structural element so that it is covalently attached to the first linear structural element at its end opposite to the end where the stopper is attached, and so that the second linear structural element is covalently attached to the cyclic moiety.
Abstract: A method for generating a dimerization and/or degradation moiety for a first protein and a second protein, where the method includes (a) generating, in silico a set of poses by docking a first protein, and a second protein, (b) generating a subset of poses by selecting one or more poses from the set of poses based on the scores of the poses, (c) identifying a candidate pose from the subset of poses based on the spatial relationship between the two proteins, (d) designing a linker between the first ligand and the second ligand that accommodates the candidate pose, and (e) synthesizing or having synthesized the dimerization and/or degradation moiety having the first ligand, the second ligand, and the linker.
Abstract: The invention pertains to methods of purifying fusion proteins, in particular TNFR:Fc fusion proteins. Methods disclosed herein can be used to produce highly pure TNFR:Fc fusion proteins (e.g., etanercept) having a biological activity by removing hard to separate product related impurities such as clipped and/or mis-fold/aggregated TNFR:Fc fusion proteins.
Abstract: The invention provides methods of purifying and/or producing a protein. In some embodiments, a method of the present invention comprises the step of eluting a protein from a Protein L matrix by lowering a conductivity. In some embodiments, the protein is an antibody. The invention also provides an antibody.
Abstract: Provided are a novel peptide compound, a method of producing the same, and use of the peptide compound. Since the peptide compound has anticancer activity, the peptide compound may be used for the prevention or treatment of cancer.
Type:
Application
Filed:
February 28, 2020
Publication date:
June 18, 2020
Inventors:
Jong Heon Shin, Ki Bong Oh, Dong Chan Oh, Sang Kook Lee, Lijuan Liao, Min Jung You
Abstract: The present invention relates to a peptide for inhibiting skin inflammation and a pharmaceutical composition and a cosmetic composition for preventing or treating skin inflammation including the same. Since the peptide, pharmaceutical composition and cosmetic composition are effective for improving symptoms of skin inflammation caused by atopic dermatitis and the like, they are useful for preventing, improving or treating skin inflammation.
Type:
Application
Filed:
December 17, 2018
Publication date:
June 18, 2020
Inventors:
Yi Yong BAEK, Jun Sub CHOI, Hye Cheong KOO
Abstract: Disclosed are compositions and methods useful for targeting molecules to activated macrophages, such as tumor associated macrophages. The compositions and methods are based on peptide sequences, such as AMT peptides, that home to activated macrophages. The disclosed homing to activated macrophages is useful for delivering therapeutic and detectable agents to cells and tissues where immune system effects or inflammation are occurring.
Abstract: According to aspects of the present invention, a peptide with any one sequence of SEQ ID NOS:1 to 3 exhibits high selective binding affinity to a target and the microcapsule has superior physicochemical stability. Therefore, the cosmetic composition containing the microcapsule linked to the peptide manifests high delivery efficiency of an active ingredient included in the capsule to target cells, thereby exhibiting superior skin-condition improvement effects.
Type:
Application
Filed:
January 19, 2018
Publication date:
June 18, 2020
Inventors:
Sang Keun HAN, Hyun Sook LEE, Eun Ah KIM, Seung Min HYUN, Hyeong CHOI, So Yoon BAEK, Jae Hwa HONG, Chae Mi LIM, Da Jeong BAK, Hye Jin JO, Hak Sung LEE, Ji Hun PARK, Eun Young LEE
Abstract: Self-assembling peptides comprising non-ionic polar amino acids for anti-adhesion are provided herein. Compositions, peptide solutions and macroscopic scaffolds of self-assembling peptides consisting essentially of non-ionic, polar amino acids are provided to prevent adhesion or to provide anti-adhesion properties. Particular peptides include those consisting essentially of, serine, threonine, tyrosine, cysteine, glutamine, asparagine, methionine, tryptophan, hydroxy-proline, and combinations thereof. Methods and kits are also provided.
Type:
Application
Filed:
December 15, 2016
Publication date:
June 18, 2020
Inventors:
Eun Seok Gil, Marc Rioult, Keiji Nagano, Karl Patrick Gilbert, Toshiro Kiyofuji, Yuya Hasegawa
Abstract: The invention relates to the field of antibiotics, more specifically to peptide antibiotics, such as antimicrobial peptides and their use in the treatment of diseases associated with microbial infections. In particular, the invention provides a peptide with antimicrobial activity comprising an amino acid sequence RRWVQRWIRRWR (SEQ ID NO: 24) or an analogue thereof.
Type:
Application
Filed:
April 24, 2018
Publication date:
June 18, 2020
Inventors:
Marinus Van Eijk, Albert Van Dijk, Hendrik Peter Haagsman, Cornelis Korstiaan Van Der Ent
Abstract: The present disclosure relates to compositions, methods, mixtures, and kits for detecting the presence of, and for removing, a virus from a product produced in an insect cell. The disclosure also relates to proteins, peptides, polypeptides, drug substances, biological products, vaccine antigens, and virus-like particles that are produced in an insect cell and that are free or substantially free of a virus. The disclosure also relates to compositions, methods, assays, and kits for detecting a rhabdovirus in a sample.
Abstract: The present disclosure relates generally to bacterial delivery vehicles for use in efficient transfer of a desired payload into a target bacterial cell. More specifically, the present disclosure relates to bacterial delivery vehicles with desired host ranges based on the presence of a chimeric receptor binding protein (RBP) composed of a fusion between the N-terminal region of a RBP derived from a lambda-like bacteriophage and the C-terminal region of a different RBP.
Abstract: The present invention relates to macromolecular complexes comprising micron-scale networks which include binding motifs thereon which allow the covalent bonding of the micron-scale networks to particles which provide nanoscale display surfaces. In particular the present invention relates to micron-scale networks of TMV coat proteins comprising a peptide tag (e.g. SpyTag) and particles providing a nanoscale display surface comprising GFP and a corresponding binding protein (e.g. SpyCatcher) wherein the peptide tag and binding protein pair are capable of spontaneously forming a covalent bond.
Type:
Application
Filed:
May 31, 2018
Publication date:
June 18, 2020
Inventors:
ANDREW JOHN LOVE, MIKHAIL EMMANUILOVICH TALIANSKI, KARA McGEACHY
Abstract: Fusion proteins containing a targeting sequence, an exosporium protein, or an exosporium protein fragment that targets the fusion protein to the exosporium of a Bacillus cereus family member are provided. Recombinant Bacillus cereus family members expressing such fusion proteins are also provided. Genetically inactivated Bacillus cereus family members and recombinant Bacillus cereus family members that overexpress exosporium proteins are also provided. Seeds coated with the recombinant Bacillus cereus family members and methods for using the recombinant Bacillus cereus family members (e.g., for stimulating plant growth) are also provided. Various modifications of the recombinant Bacillus cereus family members that express the fusion proteins are further provided. Fusion proteins comprising a spore coat protein and a protein or peptide of interest, recombinant bacteria that express such fusion proteins, seeds coated with such recombinant bacteria, and methods for using such recombinant bacteria (e.g.
Abstract: The present invention relates to a novel pyruvate transporter. By using the novel enzyme of the present invention, biomass and metabolite production amounts of a microorganism can be increased. Accordingly, by massively incubating the microorganism having improved growth characteristics, biomass or target protein production efficiency, or biodiesel production efficiency can be improved, and bioenergy production costs can be reduced, which may bring out the effect of industrial development.
Type:
Application
Filed:
April 18, 2018
Publication date:
June 18, 2020
Applicant:
IUCF-HYU (INDUSTRY-UNIVERSITY COOPERATION FOUNDATION HANYANG UNIVERSITY)
Inventors:
EonSeon JIN, Kwang Suk CHANG, Seung Beom SEO
Abstract: The invention provides variant venom peptides and polypeptides that specifically block potassium voltage gated ion channel Kv1.3. The invention also provides methods of inhibiting Kv1.3 channel activity, methods for treating disorders that are associated with undesired or aberrant Kv1.3 channel activity, methods for detecting Kv1.3 expression in target cells such as lymphocytes, and methods for diagnosing diseases or disorders that are associated with aberrant Kv1.3 overexpression.
Abstract: A method for drying moist jellyfish matter is provided. Jellyfish matter undergoes a controlled drying process until the jellyfish matter comprises a dried flake or mass.
Abstract: The present disclosure relates to constitutively active profilin-1 (Pfn1S137A) for use in the therapy and/or treatment of a neurological disorder and/or for promoting neuronal regeneration, kit and related products thereof.
Type:
Application
Filed:
May 7, 2018
Publication date:
June 18, 2020
Inventors:
Monica Luisa RIBEIRO MENDES DE SOUSA, Sérgio Ricardo CARVALHO LEITE, Ana Rita PINTO COSTA, Raquel ALBUQUERQUE SIMÕES BAETA MENDES, Joana Beatriz ANTUNES MOREIRA CARVALHO MARQUES, Sara Patrícia CASTRO SOUSA
Abstract: Provided are a novel polypeptide wherein a portion of DCTN1 protein is fused to a portion of RET protein; a polynucleotide encoding the polypeptide; a method for detecting the polynucleotide or the polypeptide; a method of screening for a compound that inhibits expression of the polynucleotide or expression and/or activity of the polypeptide; and a pharmaceutical composition containing a compound that inhibits RET as an active ingredient.