Patents Issued in August 3, 2017
  • Publication number: 20170217976
    Abstract: The present invention relates to a composition for use in an orally, or rectally, transdermally or nasally administered medicament, characterized in that it includes: (b) at least one compound of Formula (I) and (b) at least one permeation enhancer, selected from the group consisting of saturated and/or unsaturated organic fatty acids, or pharmaceutically and pharmacologically acceptable salts thereof, and thiomers. It further relates to a pharmaceutical formulation comprising said composition. It furthermore relates to bioreversible esters of compounds of Formula (I).
    Type: Application
    Filed: March 23, 2015
    Publication date: August 3, 2017
    Inventor: Helmut SCHMIDHAMMER
  • Publication number: 20170217977
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.
    Type: Application
    Filed: September 9, 2016
    Publication date: August 3, 2017
    Applicant: Rensselaer Polytechnic Institute
    Inventor: Mark P. WENTLAND
  • Publication number: 20170217978
    Abstract: An improved process for preparing buprenorphine and a method for increasing the yield of buprenorphine or a derivative thereof.
    Type: Application
    Filed: April 17, 2017
    Publication date: August 3, 2017
    Applicant: Johnson Matthey Public Limited Company
    Inventors: Nicolas ARCHER, David AUGUST, Michael BEASE, Barbara JAMIESON, Robert S. MARMOR
  • Publication number: 20170217979
    Abstract: The present invention provides a crystal of 6-arylamino pyridone carboxamide compound and a preparation method thereof. The crystal is obtained by dissolving 6-(2-chloro-4-iodophenylamino)-N-(2-hydroxylethyoxyl)-5-methyl-4-oxo-4,5-dihydrofuro[3,2-c]pyridin-7-carboxamide in an aprotic polar solvent and adding a second solvent thereto. The crystallization method has the advantage of simple and convenient operations, and is beneficial to an industrial production. The resulting crystal has the advantage a high purity and good stability, and is benefit to the manufacture and storage of a medicament containing the same.
    Type: Application
    Filed: August 5, 2015
    Publication date: August 3, 2017
    Applicants: Chia Tai Tianqing Pharmaceutical Group Co., Ltd., Centaurus Biopharma Co., Ltd.
    Inventors: LULU WANG, Xiquan ZHANG, Fei LIU, Yizhong ZHU, Chap GAO, Song TANG, Bo ZHU, Jianqiu TANG
  • Publication number: 20170217980
    Abstract: Provided herein are amlexanox analogs and methods for the treatment and/or prevention of diabetes, impaired insulin signaling, obesity, or other related diseases and conditions therewith.
    Type: Application
    Filed: January 27, 2017
    Publication date: August 3, 2017
    Inventors: Hollis D. Showalter, Alan R. Saltiel, John J. Tesmer, Xinmin Gan
  • Publication number: 20170217981
    Abstract: The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibutors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Application
    Filed: September 25, 2015
    Publication date: August 3, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: MICHAEL D. ALTMAN, JASON D. BRUBAKER, MATTHEW L. CHILDERS, ANTHONY DONOFRIO, THIERRY FISCHMANN, CRAIG R. GIBEAU, SOLOMON D. KATTAR, CHARLES A. LESBURG, JONGWON LIM, JOHN K.F. MACLEAN, UMAR F. MANSOOR, ALAN B. NORTHRUP, JOHN M. SANDERS, GRAHAM F. SMITH
  • Publication number: 20170217982
    Abstract: A compound (3R,5S,5aS,6R,7S,8R,8aS)-8-chloro-8a-hydroxy-5-(2-hydroxy acetoxy) hexahydro-1H-3,6-methanocyclopenta[e][1,3]dioxepin-7-yl 3,4-dihydroxybenzoate (KS534), the isomer thereof, the pharmaceutically acceptable salt or solvates thereof, a composition comprising the same as an active ingredient for treating allergic disease, inflammatory disease, asthma or chronic obstructive pulmonary disease (COPD)
    Type: Application
    Filed: July 22, 2015
    Publication date: August 3, 2017
    Inventors: Yongnam LEE, Ji-seok YOO, Dae-hee SHIN, Byung-hwan RYOO, Sei-ryang OH, Kyung-seop AHN, Hyeongkyu LEE, Su Ui LEE, Hyuk-hwan SONG, In Sik SHIN, Hyung Won RYU
  • Publication number: 20170217983
    Abstract: Disclosed are compounds of formula (I): and pharmaceutically acceptable N-oxides, salts, hydrates, solvates, complexes, bioisosteres, metabolites, and prodrugs thereof, which are of use in the treatment of infection with, and diseases caused by, Clostridium difficile.
    Type: Application
    Filed: January 29, 2016
    Publication date: August 3, 2017
    Applicant: Summit Therapeutics PLC
    Inventors: Peter David Johnson, Richard John Vickers, Francis Xavier Wilson, Colin Richard Dorgan, Lauren Jayne Sudlow, Stephen Paul Wren, Renate Maria van Well
  • Publication number: 20170217984
    Abstract: Compounds are provided which bind to an allosteric site on the mammalian alpha-7 nicotinic acetylcholine receptor (alpha-7 nAChR) and act as positive allosteric modulators with or without allosteric agonist activity. The compounds are useful in diagnosing, preventing, or treating a variety of disorders involving cognition, learning, memory, neurodegeneration, drug addiction, inflammation, chronic pain, and neuropathic pain. The compounds also can be used to enhance memory and learning in normal individuals.
    Type: Application
    Filed: July 23, 2015
    Publication date: August 3, 2017
    Inventors: Ganeshsingh A. THAKUR, Abhijit R. KULKARNI, Roger Lee PAPKE
  • Publication number: 20170217985
    Abstract: The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
    Type: Application
    Filed: November 21, 2016
    Publication date: August 3, 2017
    Inventors: Andrew P. Combs, Eddy W. Yue, Thomas P. Maduskuie, JR.
  • Publication number: 20170217986
    Abstract: The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z1, Z2, V1, V2, V3, R6, R6A, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: March 2, 2015
    Publication date: August 3, 2017
    Applicants: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: John A. McCauley, David Jonathan Bennett, Christopher J. Bungard, Thomas J. Greshock, M. Katharine Holloway, Peter D. Williams, Christian Beaulieu, Sheldon Crane, Stephanie Lessard, Daniel Mckay, Carmela Molinaro, Oscar Miguel Moradei, Vijayasaradhi Sivalenka, Vouy Linh Truong, Satyanarayana Tummanapalli
  • Publication number: 20170217987
    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.
    Type: Application
    Filed: July 29, 2015
    Publication date: August 3, 2017
    Applicant: Lek Pharmaceuticals d.d.
    Inventors: Andreas Hotter, Andrea Thaler, Andrija Lebar, Biljana Jankovic, Klemen Naversnik, Uros Klancar, Zrinka Abramovic
  • Publication number: 20170217988
    Abstract: The present invention relates to a novel process for the synthesis of everolimus of formula (I): and intermediates thereof.
    Type: Application
    Filed: August 4, 2015
    Publication date: August 3, 2017
    Inventors: Dharmaraj Ramachandra RAO, Geena MALHOTRA, Venkata Srinivas PULLELA, Vinod Parameshwaran ACHARYA
  • Publication number: 20170217989
    Abstract: Compounds of formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Application
    Filed: October 1, 2015
    Publication date: August 3, 2017
    Inventors: Tao Wang, Zhongxing Zhang, John F. Kadow
  • Publication number: 20170217990
    Abstract: The present invention relates to compounds of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: April 10, 2017
    Publication date: August 3, 2017
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Song Feng, Haixia Liu, Guolong Wu, Hongying Yun, Dongdong Chen, Chao Li
  • Publication number: 20170217991
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disase pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Application
    Filed: December 12, 2016
    Publication date: August 3, 2017
    Inventors: Hui LI, Seiji NUKUI, Stephanie Anne SCALES, Min TENG, Chunfeng YIN
  • Publication number: 20170217992
    Abstract: The present invention relates to an organic electroluminescent compound and an organic electroluminescent device comprising the same. By using the organic electroluminescent compound of the present invention, it is possible to produce an organic electroluminescent device having low driving voltage and excellent luminous efficiency such as current efficiency and power efficiency, emitting color of high purity, and having improved lifespan.
    Type: Application
    Filed: August 7, 2015
    Publication date: August 3, 2017
    Inventors: Ji-Song Jun, Sang-Hee Cho, Kyoung-Jin Park
  • Publication number: 20170217993
    Abstract: Lubricant additives useful as friction reducing additives are disclosed herein that have a structure according to general formula I, where M is metal such as Ag, Au, Zn or Cu, and R1, R2, and R3, are each a hydrogen, or an alkyl, a substituted alkyl, or an aryl group.
    Type: Application
    Filed: February 2, 2016
    Publication date: August 3, 2017
    Inventors: Massimiliano Delferro, Tobin J. Marks, Q. Jane Wang, Yip-Wah Chung, Hassan S. Bazzi, Afif M. Seyam, Michael Desanker, Blake Johnson, Danni Jin
  • Publication number: 20170217994
    Abstract: A method for treating cancer and gold(III) complexes with diaminocyclohexane ligand as anticancer agents. Also described are a pharmaceutical composition incorporating the gold(III) complexes and a method of synthesizing the gold(III) complexes.
    Type: Application
    Filed: April 20, 2017
    Publication date: August 3, 2017
    Applicant: KING FAHD UNIVERSITY OF PETROLEUM AND MINERALS
    Inventors: Anvarhusein A. ISAB, Muhammad Altaf
  • Publication number: 20170217995
    Abstract: Guanidine-functionalized particles and methods of making and using such particles.
    Type: Application
    Filed: April 17, 2017
    Publication date: August 3, 2017
    Inventors: George W. Griesgraber, Robert T. Fitzsimons, JR., Douglas A. Hanggi, Masayuki Nakamura, Jerald K. Rasmussen
  • Publication number: 20170217996
    Abstract: The invention relates to processes for large-scale diastereoselective syntheses of cycloheptadienylsulfone and stereotetrads, key intermediates for the preparation of Aplyronine A.
    Type: Application
    Filed: April 4, 2017
    Publication date: August 3, 2017
    Applicant: Purdue Research Foundation
    Inventors: Philip L. Fuchs, Mohammad Noshi
  • Publication number: 20170217997
    Abstract: In one embodiment, the present application discloses a photo-cleavable surface binding compound of the Formula I and Formula II: wherein the variables EG, EG1, SP1, SP2, SP3, Ar and BG are as defined herein. In another embodiment, the application discloses a method for forming a coating on a surface of a substrate using the surface binding compound.
    Type: Application
    Filed: January 27, 2017
    Publication date: August 3, 2017
    Inventors: Byung Jun Ahn, Bruce H. Lipshutz, Sam L. Nguyen, Roscoe Linstadt
  • Publication number: 20170217998
    Abstract: Therapeutically-effective amounts of novel analogs or derivatives of alkyl fatty acids, such as but not limited to lipoic acid, and pharmaceutical formulations comprising such analogs or derivatives and pharmaceutically-acceptable carriers therefor, are useful for the treatment, prevention, imaging, and/or diagnosis of medical disorders.
    Type: Application
    Filed: April 14, 2017
    Publication date: August 3, 2017
    Inventors: Robert Shorr, Robert Rodriguez, Paul Bingham, Lakmal Boteju, Thomas Kwok, James Marecek
  • Publication number: 20170217999
    Abstract: In one embodiment, the present application discloses a surface binding compound of the Formula I or Formula II: wherein the variables EG, EG1, SP1, SP2, SP3, Ar and BG are as defined herein. In another embodiment, the application discloses a method for forming a coating on a surface of a substrate using the surface binding compound of the Formula I or Formula II.
    Type: Application
    Filed: January 27, 2017
    Publication date: August 3, 2017
    Inventors: Byung Jun Ahn, Bruce H. Lipshutz, Sam L. Nguyen
  • Publication number: 20170218000
    Abstract: The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: April 17, 2017
    Publication date: August 3, 2017
    Inventors: Yihan Wang, Wei-Sheng Huang, Shuangying Liu, William C. Shakespeare, R. Mathew Thomas, Jiwei Qi, Feng Li, Xiaotian Zhu, Anna Kohlmann, David C. Dalgarno, Jan Antoinette C. Romero, Dong Zou
  • Publication number: 20170218001
    Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or prodrug thereof, and their use in medicine particular as anti-viral agents; wherein: X is selected from O and NR11; Y is selected from O, S and NR12; A is selected from —(CR1R2)n-, —(CR9R10)—, —(CR9R10)—(CR1R2)n-, —(CR1R3)—(CR2R4)—(CR1R2)n-, —CR3?CR4—(CR1R2)n- and —C?C—(CR1R2)n-; R1 and R2 are independently selected from H, alkyl, hydroxyl, hydroxymethyl and halogen; R3 and R4 are independently selected from H and alkyl, or R3 and R4 together with the carbon atoms to which they are attached form a mono or bicyclic ring system selected from cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, aryl and heteroaryl; R5 is selected from H, P(?O)(OH)2 and P(?O)(OH)—O—P(?O)(OH)2; R6 is selected from H and alkyl; R7 and R8 are independently selected from H, alkyl, halogen and hydroxymethyl R9 and R19 together with the carbon atoms to which they are attached form a mono or bicyclic ring system selected
    Type: Application
    Filed: May 22, 2015
    Publication date: August 3, 2017
    Inventors: Anita MAGUIRE, Alan Ford, Jan BALZARINI, Wim DEHAEN
  • Publication number: 20170218002
    Abstract: The present invention relates to a method for producing a Tebbe complex having high purity and high activity and having excellent storage stability in a high yield, the method including allowing bis(cyclopentadienyl)titanium dichloride and trimethylaluminum to react with each other in the presence of a solvent such that a solubility of the Tebbe complex in 1 g of the solvent at 25° C. is 0.5 mmol/g or less.
    Type: Application
    Filed: September 18, 2015
    Publication date: August 3, 2017
    Applicant: KURARAY CO., LTD
    Inventors: Shinji HATAE, Syuichi SUNAGA, Tomoaki TSUJI
  • Publication number: 20170218003
    Abstract: Therapeutically-effective amounts of novel analogs or derivatives of alkyl fatty acids, such as but not limited to lipoic acid, and pharmaceutical formulations comprising such analogs or derivatives and pharmaceutically-acceptable carriers therefor, are useful for the treatment, prevention, imaging, and/or diagnosis of medical disorders.
    Type: Application
    Filed: April 14, 2017
    Publication date: August 3, 2017
    Inventors: Robert Shorr, Robert Rodriguez, Paul Bingham, Lakmal Boteju, Thomas Kwok, James Marecek
  • Publication number: 20170218004
    Abstract: The invention relates to nucleic acids encoding a feruloyl-CoA:monolignol transferase and the feruloyl-CoA:monolignol transferase enzyme that enables incorporation of monolignol ferulates, for example, including p-coumaryl ferulate, coniferyl ferulate, and sinapyl ferulate, into the lignin of plants.
    Type: Application
    Filed: August 15, 2016
    Publication date: August 3, 2017
    Inventors: Curtis Wilkerson, John Ralph, Saunia Withers, Shawn D. Mansfield
  • Publication number: 20170218005
    Abstract: Various aspects of the invention relate to compositions comprising C-2a gentamicin. A composition may be substantially free from one or more of C-1 gentamicin, C-1a gentamicin, C-2 gentamicin, C-2b gentamicin, gentamicin A, gentamicin B, and gentamicin X. In some aspects, the invention relates to a method for treating a condition in a subject, comprising administering a composition comprising C-2a gentamicin to the subject. The condition may be, for example, a bacterial infection, genetic disease or disorder, or cancer.
    Type: Application
    Filed: January 27, 2017
    Publication date: August 3, 2017
    Inventors: George Tidmarsh, James Rolke, Lakhmir Chawla
  • Publication number: 20170218006
    Abstract: A process for the preparation of a compound of formula (I) including all isomers, stereoisomers, enantiomers and diastereomers thereof (I), and salts thereof; the process comprising providing a mixture comprising a compound of formula (II) and a compound of formula (III) subjecting the mixture provided in a) to reaction conditions in the presence of one or more Lewis acids to the mixture provided in a), obtaining a mixture comprising the compound of formula (I).
    Type: Application
    Filed: July 31, 2015
    Publication date: August 3, 2017
    Applicant: Sandoz AG
    Inventors: Thorsten Wilhelm, Hans-Peter Spitzenstätter, Olga Schöne, Frank Richter, Erwin Schreiner
  • Publication number: 20170218007
    Abstract: The present invention pertains to process for preparing nucleoside phosphoramidate and its intermediate. The present invention provides novel intermediate, its process for preparation and its use for the preparation of Sofosbuvir.
    Type: Application
    Filed: July 31, 2015
    Publication date: August 3, 2017
    Inventors: Bhairab Nath ROY, Girij Pal SINGH, Dhananjai SHRIVASTAVA, Kishor Gulabrao MEHARE, Vineet MALIK, Sharad Chandrabhan DEOKAR, Abhijeet Avinash DANGE
  • Publication number: 20170218008
    Abstract: The present invention provides cyclic-di-nucleotide (CDN) compounds that inhibit signaling at a recently discovered cytoplasmic receptor known as STING (Stimulator of Interferon Genes). In particular, the CDNs of the present invention are provided in the form of a composition comprising one or more cyclic purine dinucleotides which inhibit STING-dependent TBK1 activation and the resulting production of type I interferon.
    Type: Application
    Filed: January 20, 2017
    Publication date: August 3, 2017
    Inventors: Thomas W. Dubensky, JR., David B. Kanne
  • Publication number: 20170218009
    Abstract: Described herein are compounds that inhibit or prevent protein aggregation, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with protein aggregation.
    Type: Application
    Filed: February 2, 2017
    Publication date: August 3, 2017
    Inventors: Rui HOU, Kang ZHANG
  • Publication number: 20170218010
    Abstract: The invention relates to a method for peptide synthesis, wherein said method comprises the steps of reacting a first amino acid or a first peptide with an ?-amine protected second amino acid in a solvent selected from the group consisting of water, alcohol, and a mixture of water and alcohol, and removing the ?-amine protecting group with a deprotecting solution. The invention further relates to protective agents, their use and an apparatus for carrying out a method for solid phase synthesis of peptides.
    Type: Application
    Filed: September 29, 2015
    Publication date: August 3, 2017
    Inventors: Sascha KNAUER, Tobias Michael Louis ROESE, Olga AVRUTINA, Harald KOLMAR, Christina UTH
  • Publication number: 20170218011
    Abstract: Materials and methods for use of constrained cohydration agents in the purification of biological materials such as antibodies, viruses, cells, and cellular organelles in connection with convective chromatography, fluidized bed or co-precipitation applications.
    Type: Application
    Filed: March 10, 2017
    Publication date: August 3, 2017
    Inventor: Peter Stanley Gagnon
  • Publication number: 20170218012
    Abstract: Provided herein are integrated continuous biomanufacturing processes for producing a therapeutic protein drug substance. Also provided are systems that are capable of continuously producing a therapeutic protein drug substance.
    Type: Application
    Filed: April 21, 2017
    Publication date: August 3, 2017
    Applicant: Genzyme Corporation
    Inventors: Konstantin Konstantinov, Rahul Godawat, Veena Warikoo, Sujit Jain
  • Publication number: 20170218013
    Abstract: The present invention refers to a method for binding a polycarboxylic acid to a solid phase. Further, the invention refers to a solid phase having a polycarboxylic acid immobilized thereto and methods of using the solid phase, e.g. for purifying His-tagged recombinant polypeptides.
    Type: Application
    Filed: April 19, 2017
    Publication date: August 3, 2017
    Applicant: Max-Planck-Gesellschaft zur Foerderung der Wissenschaften e.V.
    Inventors: Dirk GOERLICH, Steffen FREY
  • Publication number: 20170218014
    Abstract: Azaindoline compounds as granzyme B inhibitors, compositions that include the compounds, and methods for using the compounds. Methods for treating cutaneous scleroderma, epidermolysis bullosa, radiation dermatitis, alopecia areata, and discoid lupus erythematosus are provided.
    Type: Application
    Filed: July 31, 2015
    Publication date: August 3, 2017
    Applicant: viDA Therapeutics Inc.
    Inventor: Dale R. Cameron
  • Publication number: 20170218015
    Abstract: The present invention provides a process for the liquid phase synthesis of the Ghrelin analog H-Inp-(D)Bal-(D)Trp-Phe-Apc-NH2 (SEQ ID NO: 1, Formula (I)), pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: March 4, 2015
    Publication date: August 3, 2017
    Inventors: Karel Decroos, Olivier Titeux
  • Publication number: 20170218016
    Abstract: Disclosed herein are compositions and methods related to aromatic-cationic peptides. In particular, the compositions and methods relate to aromatic-cationic peptides in conjunction with cytochrome c.
    Type: Application
    Filed: October 5, 2016
    Publication date: August 3, 2017
    Inventor: D. Travis Wilson
  • Publication number: 20170218017
    Abstract: The subject invention pertains to a modified MC1R peptide ligand comprising a peptide that is a melanocortin 1 receptor (MC1R) ligand and a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The subject invention also pertains to a MC1R peptide ligand-micelle complex comprising a peptide that is a melanocortin 1 receptor ligand connected via a click reaction product to a micelle. The micelle is stable in vivo and can target melanoma tumor cells by association of the peptide ligand with the MC1R or the tumor and selectively provide a detectable and/or therapeutic agent (such as an imageable contrast agent and/or anti-cancer agent) selectively to the tumor cell.
    Type: Application
    Filed: September 12, 2016
    Publication date: August 3, 2017
    Inventors: ROBERT J. GILLIES, DAVID L. MORSE, NATALIE M. BARKEY, KEVIN N. SILL, JOSEF VAGNER, NARGES K. TAFRESHI, JONATHAN L. SESSLER, CHRISTIAN PREIHS, VICTOR J. HRUBY
  • Publication number: 20170218018
    Abstract: Structural and functional analysis of peptide inhibitor binding to the cyclin D and cyclin A groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.
    Type: Application
    Filed: June 24, 2016
    Publication date: August 3, 2017
    Inventors: Campbell Mcinnes, Shu Liu, Padmavathy Nandha Premnath, Joshua K. Bolger
  • Publication number: 20170218019
    Abstract: Provided are a synthetic peptide having a multinucleation-inducing activity that can cause multinucleation in a target cell, a multinucleation-inducing agent containing this peptide, and a multinucleation induction method that uses this peptide, The synthetic peptide provided by the present invention is an artificially synthesized peptide that contains (A) a membrane-permeable peptide sequence and (B) a multinucleation-inducing peptide sequence, and that can cause multinucleation in at least one type of eukaryotic cell of human origin Or non-human mammal origin. The multinucleation-inducing peptide sequence is constituted of an amino acid sequence given by SEQ ID NO: 1 or SEQ ID NO: 2 or a modified amino acid sequence therefrom.
    Type: Application
    Filed: June 22, 2015
    Publication date: August 3, 2017
    Inventors: Nahoko Baileykobayashi, Tetsuhlko Yoshida, Makoto Sawada
  • Publication number: 20170218020
    Abstract: The invention relates to a peptide compound and its pharmaceutical composition for inhibiting platelet aggregation and preventing/treating thrombogenic diseases. The invention develops pentapeptides and hexapeptides derived from snake venom C-type lectin-like proteins (CLPs) fragments, which can inhibit platelet aggregation and have antithrombotic activity without hemorrhagic tendency. Accordingly, they can be used as potential agents for the prevention and therapy of thrombogenic diseases.
    Type: Application
    Filed: February 27, 2017
    Publication date: August 3, 2017
    Inventors: TUR-FU HUANG, CHIEN-HSIN CHANG, CHING-HU CHUNG
  • Publication number: 20170218021
    Abstract: The present application provides stable peptide-based Botulinum neurotoxin (BoNT) serotype A capture agents and methods of use as detection and diagnosis agents and in the treatment of diseases and disorders. The application further provides methods of manufacturing BoNT serotype A capture agents using iterative on-bead in situ click chemistry.
    Type: Application
    Filed: January 31, 2017
    Publication date: August 3, 2017
    Inventors: Blake Farrow, James R. Heath, Heather Dawn Agnew
  • Publication number: 20170218022
    Abstract: A peptide can have a sequence of one of SEQ ID NOs: 78-91. A conformationally-constrained kinked peptide includes: a conformationally-constraining portion and a kinked portion linked to the conformationally-constraining portion that conformationally constrains the kinked portion having a peptide sequence of one of SEQ NOs: 78-97. A cell-targeting compound can include a conformationally-constrained kinked peptide having a peptide sequence of one of SEQ ID NOs: 78-97. The peptide sequence can be one of SEQ ID NOs: 78-97, or 78-91, or 92-97. A cell-targeting compound can include a conformationally-constrained kinked peptide linked to a branched linker with one branch arm linked to a specific targeting moiety and one branch ann linked to a general targeting moiety. The specific targeting moiety can be an antibody. The general targeting moiety can be a lipid or cholesterol derivative.
    Type: Application
    Filed: April 5, 2017
    Publication date: August 3, 2017
    Inventor: Blake R. Peterson
  • Publication number: 20170218023
    Abstract: Embodiments of this invention include synthetic compounds (NRP analogues) of peptides termed neural regeneration peptides (NRPs). NRP analogues are made by substituting amino acids in the native peptide sequence, modifying amino acids chemically, by replacing amino acids with synthetic moieties, by stabilizing ?-turns, acetylation of terminal glycine residues or by cyclization. NRP analogues can be used to treat a variety of conditions involving degeneration of neural cells, and includes treating disorders of the nervous system, including peripheral neuropathy, multiple sclerosis, diabetic peripheral neuropathy, neurotoxin-induced neurodegeneration, and amyotrophic lateral sclerosis.
    Type: Application
    Filed: April 13, 2017
    Publication date: August 3, 2017
    Inventors: Paul William Richard Harris, Margaret Anne Brimble, Frank Sieg
  • Publication number: 20170218024
    Abstract: The present invention relates to novel low substituted polymyxins and compositions thereof.
    Type: Application
    Filed: June 29, 2015
    Publication date: August 3, 2017
    Inventors: VIDAR BJORNSTAD, SOLVI GUNNES, TORBEN KOCH, CLAES MELANDER
  • Publication number: 20170218025
    Abstract: The present invention is directed at bouvardin analogs arid related compounds for the treatment of disorders including cancer. Provided herein are bouvardin analogs and related compounds, pharmaceutical compositions and kits comprising at least one bouvardin analog or related compound, and methods for treating disorders including cancer. In some aspects the compounds inhibit translation elongation at the ribosome. The compounds are used in combination with radiation therapy or with known chemotherapeutic compositions.
    Type: Application
    Filed: August 10, 2016
    Publication date: August 3, 2017
    Inventors: Tin Tin SU, Mara N. GLADSTONE, Gan ZHANG, Tarek SAMMAKIA