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.
Type:
Application
Filed:
October 17, 2016
Publication date:
May 11, 2017
Inventors:
Aymen Allian, Jayanthy Jayanth, Mohamed-Eslam Mohamed, Mathew Mulhern, Lars Fredrick Nordstroem, Ahmed Othman, Michael Rozema, Lakshmi Bhagavatula, Patrick J. Marroum, Peter T. Mayer
Abstract: A spirooxoindole compound represented by the formula selected from the group consisting of formula (IA) and (IB), wherein all symbols are as defined in the description. The compound can find use in a method of prevention and/or treatment of diseases selected from the group consisting of cancer, immune diseases, inflammatory conditions, allergic skin diseases associated with excessive proliferation, and viral infections.
Type:
Application
Filed:
June 11, 2015
Publication date:
May 11, 2017
Inventors:
Marcin FEDER, Iwona KALINOWSKA, Joanna Adriana JASZCZEWSKA, Ewa BURCHARD, Wojciech LEWANDOWSKI, Urszula BULKOWSKA, Maria MAZUR, Katarzyna WOS-LATOSI
Abstract: Disclosed is a new compound that inhibits binding between a DX2 protein and a p14/ARF protein, a pharmaceutical composition including the new compound as an effective component for treating or preventing a cancer disease, an anticancer adjuvant for improving an anticancer effect of a drug-resistant anticancer drug, and a composition including an AIMP2-DX2 protein or a fragment thereof for diagnosing lung cancer.
Type:
Application
Filed:
June 30, 2015
Publication date:
May 11, 2017
Applicants:
PUSAN NATIONAL UNIVERSITY INDUSTRY-UNIVERSITY COOPERATION FOUNDATION, THE INDUSTRY & ACADEMIC COOPERATION IN CHUNGNAM NATIONAL UNIVERSITY (IAC)
Inventors:
Bum Joon PARK, Gyu Yong SONG, Ah-Young OH, Jee-Hyun LEE, Jin-Hyuk HER
Abstract: A series of fused bicyclic heteroaromatic derivatives of formula (IA) or (IB), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase III? (PI4KIII?) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
Type:
Application
Filed:
June 11, 2015
Publication date:
May 11, 2017
Inventors:
Daniel James Ford, Qiuya Huang, Judi Charlotte Neuss, James Thomas Reuberson, Bart Vanderhoydonck
Abstract: This disclosure relates to an improved synthesis of cephalosporin antibiotic compounds such as ceftolozane, and compositions and methods of use thereof. Thiadiazolyl-oximinoacetic acid compounds such as TATD can be reacted to yield the activated thiadiazolyl-oximinoacetic acid methanesulfonate ester compounds useful in the manufacture of cephalosporin antibiotic compounds.
Type:
Application
Filed:
June 19, 2015
Publication date:
May 11, 2017
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Kristos Adrian Moshos, Valdas Jukauskas, Manuel Scanu, Michele Benotti
Abstract: The present application provides a composition comprising a core formed by gold nanoparticle, a compound of Formula (I): wherein dashed lines in Formula (I) represent (i) with or without an attachment of benzol group, (ii) a delocalized bond where shown within a ring; R1 is hydrogen or a halogen; R2 is a linker selected from C6-20 alkyl or polyethylene glycol; R3 is C1-20 alkyl, C1-20 substituted alkyl, hexadecanyl amido, pyridinyl, benzyl or pyrimidinyl; and a compound of Formula (II): wherein dashed lines, R1, R2 and R3 are defined as in Formula (II), and M is a metal. The composition has an inhibition ability against a cancer.
Type:
Application
Filed:
November 4, 2016
Publication date:
May 11, 2017
Applicant:
National Dong Hwa University
Inventors:
Ivan Jyh Biau LIN, Tina H. T. HSU, Shiu-Huey CHOU
Abstract: Disclosed is a compound of formula (I): (R1 R2N)SinH2n(NR3R4) (I) wherein subscript n, R1, R2, R3 and R4 are as defined herein. Also disclosed are a method of making, intermediates useful therein, method of using, and composition comprising the compound of formula (I).
Abstract: Disclosed is a spirocyclic aryl phosphorus oxide or sulfide as an ALK inhibitor, particularly, a compound represented by formula (I) as an ALK inhibitor or pharmaceutically acceptable salt thereof.
Abstract: The present invention relates generally to olefin metathesis. In some embodiments, the present invention provides methods for Z-selective ring-closing metathesis.
Type:
Application
Filed:
August 5, 2016
Publication date:
May 11, 2017
Inventors:
Amir H. Hoveyda, Miao Yu, Chenbo Wang, Richard R. Schrock
Abstract: Complexes comprising a platinum compound and an immune checkpoint inhibitor, and related methods, are generally provided. In some embodiments, the immune checkpoint inhibitor is an inhibitor for indoleamine-2,3-dioxygenase.
Type:
Application
Filed:
November 10, 2016
Publication date:
May 11, 2017
Applicant:
Massachusetts Institute of Technology
Inventors:
Stephen J. Lippard, Samuel Gorman Awuah, Mohammed Abdulfattah AlDajani
Abstract: A process for the preparation of C4 oxygenate compounds such as threose, erythrose or erythrulose starting from a composition comprising C1-3 oxygenate compounds such as formaldehyde, glycolaldehyde, glyoxal, pyruvaldehyde or acetol, wherein the process is carried out in the presence of a crystalline microporous material having a ring pore structure selected from an eight-membered ring pore structure or a ten-membered ring pore structure.
Abstract: This application is directed to the use of aminosteroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.
Type:
Application
Filed:
October 6, 2016
Publication date:
May 11, 2017
Applicant:
Ohr Pharmaceutical, Inc.
Inventors:
Michael McLane, Inez Ruiz-White, W. Lee Maloy, Henry R. Wolfe
Abstract: Provided are a clinically applicable drug for radical cure of Alzheimer's disease (AD), and a drug for treating neurological diseases associated with axonal dysfunction other than AD, wherein the drug utilizes the mechanism of action of the AD radical cure therapy. The drugs are oral drugs, each comprising one or more compounds selected from diosgenin, a diosgenin derivative and a pharmaceutically acceptable salt thereof, the one or more compounds being suspended in an edible oil.
Abstract: The invention relates to novel betulinic proline substituted derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.
Type:
Application
Filed:
June 25, 2015
Publication date:
May 11, 2017
Applicant:
HETERO RESEARCH FOUNDATION
Inventors:
Bandi PARTHASARADHI REDDY, Kura RATHNAKAR REDDY, Gazula Levi DAVID KRUPADANAM, Adulla PANDURANGA REDDY, Bammidi ESWARA RAO, Ranga REDDY
Abstract: The present invention relates to novel betulinic proline imidazole derivatives and related compounds, compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.
Abstract: Disclosed herein are formulations, substrates, and arrays for amino acid and peptide synthesis on microarrays. In certain embodiments, methods for manufacturing and using the formulations, substrates, and arrays including one-step coupling, e.g., for synthesis of peptides in a C?N orientation are disclosed. In some embodiments, disclosed herein are formulations and methods for high efficiency coupling of biomolecules to a substrate.
Abstract: A cyclic dipeptide-containing composition containing each of tyrosine-containing cyclic dipeptides selected from the group consisting of cyclotryptophanyltyrosine, cycloseryltyrosine, cycloprolyltyrosine, cyclotyrosylglycine, cyclotyrosyltyrosine, cyclophenylalanyltyrosine, cycloleucyltyrosine, cyclolysyltyrosine, cyclohistidyltyrosine, cycloalanyltyrosine, cycloglutamyltyrosine, cyclovalyltyrosine, cycloisoleucyltyrosine, cyclothreonyltyrosine, cycloaspartyltyrosine, cycloasparaginyltyrosine, cycloglutaminyltyrosine, cycloarginyltyrosine, and cyclomethionyltyrosine, or a salt thereof in a specified amount. The cyclic dipeptide-containing composition of the present invention has an excellent action of lowering a uric acid level, and the cyclic dipeptide-containing composition is useful in, for example, prevention or treatment of hyperuricemia, gout or the like.
Abstract: The invention relates to a process for solution-phase synthesis of D-Arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide, an active ingredient used for both common and rare diseases including a mitochondrial targeted therapy for ischemia reperfusion injury.
Abstract: A method of selectively modulating the activity of C5a receptor 2 (C5aR2). The method includes exposing the receptor to a compound that selectively modulates C5aR2 compared to C5a receptor 1 (C5aR1). In some cases, the compound is peptide P32 or P59. Methods of recruiting ?-arrestin 2 in a cell, modulating C5a-induced ERK1/2 activation in a macrophage, selectively inhibiting the release of IL-6 from a macrophage, are also provided.
Type:
Application
Filed:
October 17, 2016
Publication date:
May 11, 2017
Inventors:
Dimitrios Morikis, Christodoulos A. Floudas, Trent M. Woodruff, Matthew A. Cooper, Daniel E. Croker, Peter N. Monk
Abstract: Affinity peptide ligands of mouse polyomavirus capsomers and a designed screening method thereof. The affinity peptide ligands can be used for separation and purification of the capsomers.
Type:
Application
Filed:
November 10, 2014
Publication date:
May 11, 2017
Applicant:
TIANJIN UNIVERSITY
Inventors:
Lin ZHANG, Xiaoyan DONG, Yanying LI, Xiaodan LIU, Yan SUN
Abstract: Fusion peptides and methods of inhibiting GrB-EHITSN or a fragment thereof are provided. The fusion peptides include an NPF peptide and a cell-permeable peptide operably connected thereto. Fusion peptides and methods of inhibiting activity of GrB-EHITSN or fragment thereof are provided. An aspect includes a fusion peptide comprising an isolated NPF peptide comprising an amino acid sequence having at least 90% identity to SEQ ID NO: 2 and a cell-permeable peptide operably connected to the isolated NPF peptide, wherein the fusion peptide inhibits activity of GrB-EHITSN or a fragment thereof.
Abstract: A peptide with antimicrobial, anticancer and/or wound-healing promoting activities is provided. The peptide with antimicrobial, anticancer and/or wound-healing promoting activities, includes: an ?-helix peptide; and a short peptide consisting of about 4-10 positively charged amino acids, connected to an N-terminus of the ?-helix peptide to form the peptide with antimicrobial, anticancer and/or wound-healing promoting activities, wherein the total length of the peptide with antimicrobial, anticancer and/or wound-healing promoting activities is about 10-20 amino acids.
Abstract: The invention provides processes of preparing a peptide including a GCC agonist sequence selected from the group consisting of SEQ ID NOs: 1-249 described herein.
Type:
Application
Filed:
January 13, 2017
Publication date:
May 11, 2017
Applicant:
Synergy Pharmaceuticals Inc.
Inventors:
Juncai Bai, Ruoping Zhang, Jun Jian, Junfeng Zhou, Qiao Zhao, Guoquing Zhang, Kunwar Shailubhai, Stephen Comiskey, Rong Feng
Abstract: The present disclosure relates to complex comprising an engineered polypeptide having affinity for interleukin-6 (in the following referred to as IL-6) and an antibody or an antigen binding fragment thereof, wherein said engineered polypeptide having affinity for IL-6 belongs to a class of engineered polypeptides comprising the sequence EEX3X4AWX7EIHX11 LPNLX16X17X18QX20X21AFIX25X26LX28X29. The present disclosure also relates to the use of said complex as a therapeutic agent.
Abstract: Provided are non-naturally occurring cystine knot peptides (CKPs) that bind to VEGF-A. Additionally, provided are methods of using non-naturally occurring CKPs that bind to VEGF-A, including diagnostic and therapeutic compositions and methods. Non-naturally CKPs that bind low density lipoprotein receptor-related protein 6 (LRP6) are also provided.
Abstract: The present invention relates to the provision of a biologically safe hemolymph sera, preferably hemocyanin, more preferably KLH (keyhole limpet hemocyanin). A method for producing virus free hemocyanin is provided.
Type:
Application
Filed:
June 12, 2014
Publication date:
May 11, 2017
Applicant:
Biosyn Arzneimittel GmbH
Inventors:
Ortwin Kottwitz, Thomas Stiefel, Shammana N. Muddukrishna
Abstract: LEDGF peptides with anti-protein aggregation activity and methods of use are provided. The LEDGF peptides disclosed herein demonstrate an ability to treat degenerative diseases and diseases with various cellular stresses including oxidative stress and protein-aggregation stress. In addition, extended release formulations, including formulations suitable for ophthalmic administration are provided.
Type:
Application
Filed:
November 10, 2016
Publication date:
May 11, 2017
Inventors:
Uday B. KOMPELLA, Rinku BAID, Arun K. UPADHYAY, Sarath YANDRAPU
Abstract: The present disclosure provides genetically modified animals and cells comprising a polynucleotide encoding human profilin1. Also provided are methods of assessing the effects of agents in genetically modified animals and cells comprising a polynucleotide encoding human profilin1.
Type:
Application
Filed:
June 19, 2015
Publication date:
May 11, 2017
Applicant:
Board of Trustees of the University of Arkansas
Abstract: The present invention provides a fusion protein comprising a latency associated peptide (LAP), a pharmaceutically active agent and an amino acid sequence comprising a dimerisation domain, wherein the LAP and the pharmaceutically active agent are connected by an amino acid sequence comprising a proteolytic cleavage site. Also provided are nucleic acids enclosing such fusion proteins, process for their preparation, pharmaceutical compositions, kits and uses thereof in medicine.
Type:
Application
Filed:
June 26, 2015
Publication date:
May 11, 2017
Inventors:
Yuti Chernajovsky, Lisa Mullen, Gillian Adams, David James Gould, Hawzheen Muhammad
Abstract: The present invention relates to a method for preparing a recombinant cell line producing recombinant glycoproteins having a high sialic acid content by inhibiting glycosphingolipid (GSL) biosynthesis pathway in a cell line producing recombinant glycoproteins. Particularly, the present invention produces erythropoietin (EPO), containing a high content of sialic acid in a cell, from a cell line, which induces CGT inhibition by using siRNA and miRNA specifically binding to ceramide glucosyltransferase (CGT), thereby increasing the in vivo half-life of a recombinant therapeutic protein, and thus can be useful in the treatment of disease using the same.
Type:
Application
Filed:
September 24, 2014
Publication date:
May 11, 2017
Inventors:
Jung-Hoe KIM, Chan-Yeong KWAK, Seung-Yeol PARK, Woo-Yong SHIM
Abstract: This document provides methods and materials related to natriuretic polypeptides and the use of natriuretic polypeptides to treat cardiovascular and/or renal conditions. For example, chimeric polypeptides having at least one amino acid segment (e.g., N-terminus tail, ring structure, C-terminus tail, or a combination thereof) of a natriuretic peptide (e.g., ANP, BNP, CNP, URO, or DNP) and an amino acid segment of an angiotensin polypeptide (e.g., Ang-(1-7)) are provided.
Abstract: The present invention relates to a novel method for purifying teriparatide, a therapeutically active polypeptide fragment of full-length human parathyroid hormone. The method is based on ion exchange chromatography and is effective in separating the therapeutically active polypeptide from undesirable variants, such as truncated polypeptides. The method of the invention can be used at a preparative scale which allows it to be implemented into the production process for teriparatide. Accordingly, the invention also provides a method for the production of teriparatide which includes a step in which teriparatide is purified by the novel ion exchange chromatography method of the invention.
Abstract: The present invention describes methods and processes for the production of proteins, particularly glycoproteins, by animal cell or mammalian cell culture, preferably, but not limited to, fed-batch cell cultures. In one aspect, the methods comprise the addition of glucocorticoid compound during the culturing period. The addition of glucocorticoid compound sustain a high viability of the cultured cells, and can yield an increased end titer of protein product, and a high quality of protein product, as determined, e.g., by sialic acid content of the produced protein.
Abstract: The present invention describes methods and processes for the production of proteins, particularly glycoproteins, by animal cell or mammalian cell culture, preferably, but not limited to, fed-batch cell cultures. In one aspect, the methods comprise the addition of glucocorticoid compound during the culturing period. The addition of glucocorticoid compound sustain a high viability of the cultured cells, and can yield an increased end titer of protein product, and a high quality of protein product, as determined, e.g., by sialic acid content of the produced protein.
Abstract: The present invention relates to improved methods for the recombinant production of von Willebrand factor (vWF) in a bioreactor by separating different multimeric forms of vWF with different molecular weight during fermentation.
Abstract: The invention relates to neutralizing antibodies, and antibody fragments thereof, having high potency in neutralizing hCMV, wherein said antibodies and antibody fragments are specific for one, or a combination of two or more, hCMV gene UL products. The invention also relates to immortalized B cells that produce, and to epitopes that bind to, such antibodies and antibody fragments. In addition, the invention relates to the use of the antibodies, antibody fragments, and epitopes in screening methods as well as in the diagnosis, prevention, and therapy of disease.
Abstract: The invention relates to neutralizing antibodies, and antibody fragments thereof, having high potency in neutralizing hCMV, wherein said antibodies and antibody fragments are specific for one, or a combination of two or more, hCMV gene UL products. The invention also relates to immortalized B cells that produce, and to epitopes that bind to, such antibodies and antibody fragments. In addition, the invention relates to the use of the antibodies, antibody fragments, and epitopes in screening methods as well as in the diagnosis, prevention, and therapy of disease.
Abstract: Helicobacter pylori, one of the most common human pathogens, is associated with the development of human chronic gastritis, peptic ulcers and gastric cancer. The invention relates to a ?1,6-glucan-containing Helicobacter pylori compound comprising the structure of Formula I: wherein R is a ?-DDHep-3-?-L-Fuc-3-?-GlcNAc trisaccharide substituted with an ?1,6-glucan linked to an ?1,3-DD-heptan, and wherein the last DD-Hep residue of ?1,3-DD-heptan is capped with ?-GlcNAc residue. Compositions comprising the compound, uses of the compound, and antibodies raised against the compound are also described.
Type:
Application
Filed:
October 24, 2016
Publication date:
May 11, 2017
Inventors:
Eleonora Altman, Blair A. Harrison, Vandana Chandan
Abstract: Antibody molecule-drug conjugates (ADCs) that specifically bind to lipopolysaccharides (LPS) are disclosed. The antibody molecule-drug conjugates can be used to treat, prevent, and/or diagnose bacterial infections and related disorders.
Type:
Application
Filed:
November 10, 2016
Publication date:
May 11, 2017
Inventors:
Obadiah Joseph Plante, James C. Delaney, Karthik Viswanathan, Boopathy Ramakrishnan, Zachary Holmes Shriver, Andrew M. Wollacott
Abstract: Provided herein are methods of preventing and treating polybacterial infections comprising administering an effective amount of an antibody or antigen-binding fragment thereof that specifically binds to an epitope produced by at least one of the bacterium in the polybacterial infection. For example, an antibody that specifically binds to Staphylococcus aureus alpha toxin can be administered to a patient with a polybacterial infection comprising Staphylococcus aureus and Pseudomonas aeruginosa to inhibit the growth of Pseudomonas aeruginosa.
Type:
Application
Filed:
June 19, 2015
Publication date:
May 11, 2017
Inventors:
Bret SELLMAN, Jamese Johnson HILLIARD, Omari JONES, Charles Ken STOVER
Abstract: A new use of a molecule comprising at least one moiety which is a biologically active protein and at least one moiety capable of binding to a serum albumin of a mammal is provided, for preparation of a medicament which elicits no or a reduced immune response upon administration to the mammal, as compared to the immune response elicited upon administration to the mammal of the biologically active protein per se. Also provided is a method of reducing or eliminating the immune response elicited upon administration of a biologically active protein to a human or non-human mammal, which comprises coupling the polypeptide to at least one moiety capable of binding to a serum albumin of the mammal.
Abstract: The invention relates to polypeptides that comprise a portion of filamentous bacteriophage gene 3 protein (g3p) sufficient to bind to and/or disaggregate amyloid, e.g., the N1-N2 portion of g3p and mutants and fragments thereof wherein that g3p amino acid sequence has been modified through amino acid substitution to be substantially less immunogenic than the corresponding wild-type g3p amino acid sequence when used in vivo. The polypeptides of the invention retain their ability bind to and/or disaggregate amyloid. The invention relates furthermore to the use of these variant g3p-polypeptides in the treatment and/or prevention of diseases associated with misfolding or aggregation of amyloid.
Type:
Application
Filed:
May 28, 2014
Publication date:
May 11, 2017
Inventors:
Richard A. FISHER, Robert George Edward HOLGATE, Francis Joseph CARR, Timothy David JONES
Abstract: There is disclosed a pharmaceutical composition and method for treating sepsis, including septic shock and ARDS (acute respiratory distress syndrome), comprising administering an effective amount of a HMG1 antagonist. There is further disclosed a diagnostic method for monitoring the severity or potential lethality of sepsis or septic shock, comprising measuring the serum concentration of HMG1 in a patient exhibiting or at risk of exhibiting sepsis or septic shock symptoms. Lastly, there is disclosed a pharmaceutical composition and method for effecting weight loss or treating obesity, comprising administering an effective amount of HMG1 or a therapeutically active HMG1 fragment.
Abstract: The present disclosure provides methods for modulating the interaction between a TAM ligand and a lipid membrane containing phosphatidyl serine (PtdSer). In one example, such methods use a TAM receptor agonist having a PtdSer-containing lipid bilayer membrane with Gas6 and/or Protein S bound to the membrane to activate signaling from one or more TAM receptors and treat an autoimmune disease. In another example, methods are provided for treating a subject with a pathological condition characterized by overactivation of TAM signaling and/or reduction in Type I IFN response, such as infection by an enveloped virus, by use of agents that decrease the interaction between a TAM ligand and PtdSer. Also provided are methods for classifying a virus as susceptible to anti-TAM therapy. Methods of identifying an agent that blocks virus infectivity are also provided.
Type:
Application
Filed:
September 20, 2016
Publication date:
May 11, 2017
Applicants:
Salk Institute for Biological Studies, Kolltan Pharmaceuticals, Inc.
Inventors:
Greg E. Lemke, Lawrence C. Fritz, Benedikt Vollrath, Carla V. Rothlin
Abstract: The present invention provides an antibody which comprises a variable heavy (VH) chain comprising CDR1, CDR2 and CDR3, and/or a variable light (VL) chain comprising CDR1, CDR2 and CDR3, wherein the CDRs have the same amino acid sequence as those from a complete antibody isolated from a synovial tissue sample of rheumatoid arthritis patients, as listed in Tables 1 and 2 or Tables 1 A and 2 A.
Abstract: The inventors successfully produced anti-Epiregulin antibodies showing cross-species reactivity between cynomolgus monkey (non-human animals) and human, anti-Epiregulin antibodies with suppressed chemical degradation, anti-Epiregulin antibodies with lowered isoelectric point, anti-Epiregulin antibodies with increased thermal denaturation midpoint temperature, and anti-Epiregulin antibodies with reduced amount of aggregate by performing appropriate amino acid residue substitutions in the variable-region sequences of the humanized EP27 antibody which inhibits growth of cancer cells by exhibiting cytotoxic activity and neutralizing activity against human Epiregulin-expressing cells.
Abstract: The present invention provides novel, rationally designed human control antibodies for use in various in vivo and in vitro applications. The antibodies of the present invention have well characterized variable domains that have been designed to minimize or eliminate antigen binding without altering gross antibody structure. Using the antibodies of the present invention in various assays allows researchers to distinguish effects that result from specific antigen-antibody interactions from other, non-specific antibody effects.
Type:
Application
Filed:
October 26, 2016
Publication date:
May 11, 2017
Inventors:
HSIU-CHING CHANG, YEN-MING HSU, JENG-SHIN LEE