Patents Issued in September 12, 2017
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Patent number: 9758522Abstract: Provided are bifunctional small molecules of Formula (I): or pharmaceutically acceptable salts thereof, wherein M represents a small organic molecule which binds, covalently or non-covalently, a kinase, such as Her3 protein kinase; L1 represents a linker; and RH represents a hydrophobic group. An example of a compound of Formula (I) is a compound of Formula (II): Also provided are pharmaceutical compositions comprising a compound of Formula (I) or (II) and methods of using such compounds for treating proliferative diseases.Type: GrantFiled: October 18, 2013Date of Patent: September 12, 2017Assignees: Dana-Farber Cancer Institute, Inc., Yale UniversityInventors: Nathanael Gray, Ting Xie, Sang Min Lim, Pasi A. Janne, Craig M. Crews
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Patent number: 9758523Abstract: The present invention is directed to [1,2,4]triazolo[4,3-a]pyridine and [1,2,4]triazolo[4,3-a]pyrazine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.Type: GrantFiled: July 9, 2015Date of Patent: September 12, 2017Assignee: Incyte CorporationInventors: Liangxing Wu, Xiaozhao Wang, Wenqing Yao, Colin Zhang
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Patent number: 9758524Abstract: The present invention relates to 6-5 membered fused pyridine ring compounds according to Formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to Formula (I) in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.Type: GrantFiled: February 9, 2016Date of Patent: September 12, 2017Assignee: Merck Sharp & Dohme B.V.Inventors: Tjeerd A. Barf, Christiaan Gerardus Johannes Maria Jans, Adrianus Petrus Antonius de Man, Arthur A. Oubrie, Hans C. A. Raaijmakers, Johannes Bernardus Maria Rewinkel, Jan Gerard Sterrenburg, Jacobus C. H. M. Wijkmans
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Patent number: 9758525Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.Type: GrantFiled: January 29, 2014Date of Patent: September 12, 2017Assignee: Aptinyx Inc.Inventors: John A. Lowe, III, M. Amin Khan
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Patent number: 9758526Abstract: An object to be achieved by the present invention is to provide a novel compound having EGFR inhibitory effects and cell growth inhibitory effects, as well as a medication useful for the prevention and/or treatment of cancer based on the EGFR inhibitory effects. The present invention provides a compound represented by Formula (I) below, or a salt thereof.Type: GrantFiled: December 19, 2016Date of Patent: September 12, 2017Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Takao Uno, Katsumasa Nonoshita, Tadashi Shimamura
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Patent number: 9758527Abstract: The present invention relates to: a cyclohexene derivative; a preparation method therefor; and a pharmaceutical composition for preventing or treating metabolic diseases, containing the same as an active ingredient. The cyclohexene derivative according to the present invention increases the intracellular activity of cyclic adenosine monophosphate (cAMP) by activating G protein-coupled receptor 119 (GPR-119) and simultaneously exhibits weight loss and hypoglycemic effects by inducing the release of glucagon-like peptide-1 (GLP-1), which is a neuroendocrine protein, and thus can be useful as a pharmaceutical composition for preventing or treating metabolic diseases such as obesity, type 1 diabetes, type 2 diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia and syndrome X.Type: GrantFiled: May 1, 2015Date of Patent: September 12, 2017Assignee: HYUNDAI PHARM CO., LTD.Inventors: Jin Yang, Jinwoong Kim, Han Kyu Lee, Jae Hyun Kim, Chang Mo Son, Kyu Hwan Lee, Jeongun Hwang, Hyung-Ho Choi, Daehoon Kim, Jaekeol Rhee
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Patent number: 9758528Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethyl aminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1?-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.Type: GrantFiled: September 27, 2013Date of Patent: September 12, 2017Assignee: Takeda Pharmaceutical Company LimitedInventors: Koichiro Fukuoka, Kazuhiro Miwa, Tsuyoshi Sasaki, Fumiya Komura
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Patent number: 9758529Abstract: Disclosed are compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein Ring B, A1, A2, R6, w and n1 are defined and described herein; compositions thereof; and methods of use thereof. These compounds are useful for treating a variety of neurological and psychiatric disorders, such as those described herein.Type: GrantFiled: February 11, 2016Date of Patent: September 12, 2017Assignees: Sunovion Pharmaceuticals Inc., PGI Drug Discovery LLCInventors: Milan Chytil, Sharon Engel, Taleen G. Hanania, Vadim Alexandrov, Emer Leahy
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Patent number: 9758530Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as or pharmaceutically acceptable salts, or tautomerism isomers, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.Type: GrantFiled: January 8, 2016Date of Patent: September 12, 2017Assignee: Hoffmann-La Roche Inc.Inventors: Lei Guo, Taishan Hu, Yimin Hu, Buelent Kocer, Buyu Kou, Gangqin Li, Xianfeng Lin, Haixia Liu, Hong Shen, Houguang Shi, Guolong Wu, Zhisen Zhang, Mingwei Zhou, Wei Zhu
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Patent number: 9758531Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: GrantFiled: September 8, 2015Date of Patent: September 12, 2017Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
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Patent number: 9758532Abstract: Compositions and methods comprising metal organic frameworks (MOFs) and related uses are generally provided. In some embodiments, an MOF comprises a plurality of metal ions, each coordinated with at least one ligand comprising at least two unsaturated N-heterocyclic aromatic groups arranged about an organic core. In some embodiments, an MOF may be used in applications related to water adsorption.Type: GrantFiled: May 6, 2014Date of Patent: September 12, 2017Assignee: Massacusetts Institute of TechnologyInventors: Mircea Dinca, Casey R. Wade
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Patent number: 9758533Abstract: A reaction method comprising combining a carbonyl-substituted arylboronic acid or ester and an ?-effect amine in aqueous solution at a temperature between about ?5 C to 55 C, and a pH between 2 and 8 to produce an adduct. A process is also provided comprising: contacting a composition having a boron atom bonded to a sp2 hybridized carbon, the boron having at least one labile substituent, conjugated with a cis-carbonyl, with an ?-effect amine, in an aqueous medium for a time sufficient to form an adduct, which may proceed to further products.Type: GrantFiled: April 23, 2015Date of Patent: September 12, 2017Assignee: The Research Foundation for The State University of New YorkInventors: Susan Bane Tuttle, Ozlem Dilek, Kamalika Mukherjee
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Patent number: 9758534Abstract: Organoaminosilanes, such as without limitation di-iso-propylaminosilane (DIPAS), are precursors for the deposition of silicon containing films such as silicon-oxide and silicon-nitride films. Described herein are methods to make organoaminosilane compounds, or other compounds such as organoaminodisilanes and organoaminocarbosilanes, via the catalytic hydrosilylation of an imine by a silicon source comprising a hydridosilane.Type: GrantFiled: December 2, 2015Date of Patent: September 12, 2017Assignee: VERSUM MATERIALS US, LLCInventors: Manchao Xiao, Matthew R. MacDonald, Richard Ho, Xinjian Lei
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Patent number: 9758535Abstract: System, including methods and compositions, for making and using emulsions that include a silicone oil and a silicone surfactant. The emulsions may include aqueous droplets disposed in a continuous phase that includes a silicone oil and a silicone surfactant. The aqueous droplets may contain an analyte, optionally at partial occupancy, and/or a luminescent (e.g., photoluminescent) reporter. An assay of the analyte may be performed with the droplets. In some cases, signals may be detected from the droplets, and a characteristic of the analyte, such as an analyte level or activity, may be determined based on the signals.Type: GrantFiled: March 17, 2014Date of Patent: September 12, 2017Assignee: Bio-Rad Laboratories, Inc.Inventors: Erin R. Chia, Amy L. Hiddessen, Benjamin J. Hindson, Adam Lowe, Chunxiao Han
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Patent number: 9758536Abstract: The present invention concerns phospholipid compositions having a relatively high concentration of compounds of the following structure (I): wherein at least one of R1 and R2 is palmitoleoyl, myristoleoyl or lauroleoyl and methods for their preparation. The present invention also concerns the use of these phospholipid compositions to treat a variety of disorders by administering the composition to a patient in need thereof.Type: GrantFiled: December 6, 2012Date of Patent: September 12, 2017Assignee: Omega Protein CorporationInventors: Ernesto Hernandez, Marina Rusli, Mark Griffin
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Patent number: 9758537Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.Type: GrantFiled: February 25, 2015Date of Patent: September 12, 2017Assignee: Achillion PharmaceuticalsInventors: Jason Allan Wiles, Avinash S. Phadke, Xiangzhu Wang, Dawei Chen, Akihiro Hashimoto, Venkat Rao Gadhachanda, Godwin Pais, Qiuping Wang, Atul Agarwal, Milind Deshpande
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Patent number: 9758538Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1-R11, m, n, and p are defined herein. The novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.Type: GrantFiled: July 13, 2016Date of Patent: September 12, 2017Assignee: PFIZER INC.Inventors: Ping Chen, Hengmiao Cheng, Gary Michael Gallego, Mehran Jalaie, John Charles Kath, Suvi Tuula Marjukka Orr, Mason Alan Pairish
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Patent number: 9758539Abstract: Compounds having the following structure (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein one of R1, R2 or R3 is —P(?O)(OH)2, and the other two of R1, R2 and R3 are each H, are provided. Pharmaceutical compositions comprising the compounds, and methods for use of the compounds for treating diseases associated with overexpression of a cyclin-dependent kinase (CDK) are also provided.Type: GrantFiled: May 18, 2016Date of Patent: September 12, 2017Assignee: Tolero Pharmaceuticals, Inc.Inventors: Adam Siddiqui-Jain, David J. Bearss
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Patent number: 9758540Abstract: Disclosed herein are catalyst compositions containing bicyclic bridged metallocene compounds. These catalyst compositions can be used for the polymerization of olefins. For example, ethylene polymers produced using these catalyst compositions can be characterized by low molecular weights and high melt flow rates, and can be produced without the addition of hydrogen.Type: GrantFiled: May 25, 2016Date of Patent: September 12, 2017Assignee: Chevron Phillips Chemical Company LPInventors: Jeremy M. Praetorius, Qing Yang, Connor D. Boxell, Tony R. Crain
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Patent number: 9758541Abstract: The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt or solvate thereof, a stereoisomer or a mixture of stereoisomers in any ratio, or a water-soluble derivative, as well as to methods for preparing same and to the use thereof, in particular in the treatment of cancer.Type: GrantFiled: October 30, 2014Date of Patent: September 12, 2017Assignee: PARIS SCIENCES ET LETTRES—QUARTIER LATINInventors: Gerard Jaouen, Pascal Pigeon, Siden Top
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Patent number: 9758542Abstract: A coating of a random copolymer of acrylamide and a second monomer, e.g. glycidoxylmethacrylate, for a silica surface is described. The coating is applied to chromatographic support structures having silica based surfaces. The coating is functionalized to produce protein chromatography matrices that are particularly useful for extracting trace amounts of biomarker molecules from biological samples.Type: GrantFiled: November 1, 2012Date of Patent: September 12, 2017Assignee: Purdue Research FoundationInventors: Mary J. Wirth, Yimin Hua, Zhaorui Zhang
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Patent number: 9758543Abstract: An alkenyl glycoside is prepared by reacting a metathesis-derived unsaturated fatty alcohol containing 10 to 30 carbon atoms with either (1) a reducible monosaccharide or composition hydrolyzable to a reducible monosaccharide, or (2) a hydrocarbyl glycoside produced by reacting an alcohol containing up to 6 carbon atoms with a reducible monosaccharide or composition hydrolyzable to a reducible monosaccharide. Each of these reactions is performed in the presence of an acid catalyst and under conditions sufficient to form the alkenyl glycoside or hydrocarbyl glycoside. The preferred alkenyl glycosides are 9-decen-1-yl glycoside; 9-dodecen-1-yl glycoside; 9-tridecen-1-yl glycoside; 9-pentadecen-1-yl glycoside; 9-octadecen-yl glycoside; or 9-octadecen-1,18-diyl glycoside.Type: GrantFiled: January 13, 2016Date of Patent: September 12, 2017Assignee: Elevance Renewable Sciences, Inc.Inventors: Ryan A. Littich, Jonathan Brekan, Timothy Montavon
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Patent number: 9758544Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.Type: GrantFiled: December 16, 2015Date of Patent: September 12, 2017Assignee: Alios BioPharma, Inc.Inventors: Leonid Beigelman, David Bernard Smith, Guangyi Wang, Natalia Dyatkina
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Patent number: 9758545Abstract: The present invention relates to a scaffolded sensor with a container comprising a drug for triggering drug release, wherein the scaffold is intrinsically conformationally metastable and a method to its manufacture.Type: GrantFiled: October 24, 2011Date of Patent: September 12, 2017Assignee: UNIVERSITÉ DE FRIBOURGInventors: Katharina Fromm, Christian Bochet
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Patent number: 9758546Abstract: Provided herein are methods for the synthesis of oligomeric compounds wherein removal of the 5?-terminal trityl group is performed at reduced temperature and lower pH relative to standard methods. In certain embodiments, the present methods provide detritylated oligomeric compounds having a reduced percentage of depurination relative to the same detritylated oligomeric compounds prepared using standard methods. In certain embodiments, the present methods provide detritylated oligomeric compounds with increased purity relative to the same detritylated oligomeric compounds prepared using standard methods. In certain embodiments, the present method provide an increased rate of detritylation compared to standard methods.Type: GrantFiled: October 21, 2014Date of Patent: September 12, 2017Assignee: Ionis Pharmaceuticals, Inc.Inventor: Dana Chreng
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Patent number: 9758547Abstract: Ligand functionalized substrates, methods of making ligand functionalized substrates, and methods of using functionalized substrates are disclosed.Type: GrantFiled: March 21, 2013Date of Patent: September 12, 2017Assignee: 3M Innovative Properties CompanyInventors: Jerald K. Rasmussen, Kannan Seshadri, Robert T. Fitzsimons, Jr., James I. Hembre, Catherine A. Bothof, Erin A. Satterwhite, George W. Griesgraber, Yi He, Louis C. Haddad
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Patent number: 9758548Abstract: A method of treating a bacterial infection in a subject is disclosed. The method comprises administering to the subject a therapeutically effective amount of a peptide being between 3 and 5 amino acids, wherein at least one amino acid of the 3 and 5 amino acids is selected from the group consisting of tryptophan, cysteine, proline and methionine.Type: GrantFiled: May 10, 2012Date of Patent: September 12, 2017Assignee: Technion Research & Development Foundation LimitedInventors: Noam Adir, Sharon Navon, Tali Swartzmann
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Patent number: 9758549Abstract: The present invention relates to peptide ligands of the melanocortin receptors, in particular the melancortin-4 receptor, and as such, are useful in the treatment of disorders responsive to the activation of this receptor, such as obesity, diabetes mellitus and sexual dysfunction.Type: GrantFiled: February 29, 2016Date of Patent: September 12, 2017Assignee: Ipsen Pharma S.A.S.Inventors: Zheng Xin Dong, Daniel B. Deoliveira, Jeanne Mary Comstock
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Patent number: 9758550Abstract: The present invention relates to a cobalamin acquisition protein, compositions containing the cobalamin acquisition protein, and the use of such compositions.Type: GrantFiled: December 3, 2015Date of Patent: September 12, 2017Assignee: Woods Hole Oceanographic InstitutionInventors: Makoto Saito, Erin M. Bertrand
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Patent number: 9758551Abstract: Nucleic acids encoding a chimeric or fusion polypeptide which polypeptide comprises a first domain comprising a translocation polypeptide; and a second domain comprising at least one antigenic peptide are disclosed. The preferred translocation polypeptide is a bacterial toxin translocation polypeptide, such as domain II of Pseudomonas aeruginosa exotoxin A (ETA(dII)). Such nucleic acids, expression vectors thereof, and cells expressing these vectors are used as vaccine compositions in a method for enhancing an antigen specific immune response, a method of increasing the numbers of CD8+ CTLs specific for a selected desired antigen in a subject, or a method of inhibiting the growth of a tumor in a subject.Type: GrantFiled: March 5, 2012Date of Patent: September 12, 2017Assignee: The Johns Hopkins UniversityInventors: Tzyy-Choou Wu, Chien-Fu Hung
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Patent number: 9758552Abstract: A ligand recombinant protein inhibiting HB-EGF (Heparin-Binding Epidermal Growth Factor like), from the R domain of diphtheria toxin, which can be used for the treatment and diagnosis of diseases involving the activation of the HB-EGF/EGFR pathway.Type: GrantFiled: March 19, 2013Date of Patent: September 12, 2017Assignee: COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVESInventors: Daniel Gillet, Benoit Villiers, Sylvain Pichard, Bernard Maillere, Alain Sanson
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Patent number: 9758553Abstract: Lower eukaryotic host cells have been engineered to produce glycoprotein having at least one terminal ?-galactosyl epitope. The glycoproteins are useful for the production of highly antigenic glycoprotein compositions with advantages for the production of vaccines.Type: GrantFiled: July 2, 2014Date of Patent: September 12, 2017Assignee: MERCK SHARP & DOHME CORP.Inventors: Natarajan Sethuraman, Robert C. Davidson, Terrance A. Stadheim, Stefan Wildt
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Patent number: 9758554Abstract: The present disclosure relates to a collection of novel muteins derived from human ?1m (or a1m) polypeptide or a functional homolog thereof. The disclosure further refers to a ?1m mutein capable of specifically binding to one or more targets other than a target to which wild-type ?1m binds. The disclosure also relates to a method for producing such collection of muteins and a method for isolating a mutein capable of binding one or more such non-natural targets of wild-type ?1m polypeptide. These aspects are made possible due to, e.g, the structural elucidation of ?1m disclosed herein by the present inventors, an appreciation of ligand-binding sights thereof and, hence, an understanding of which amino acid positions are most suitable for mutagenesis for re-engineering specificity and affinity for any given target while maintaining the secondary and/or tertiary structure of a1m.Type: GrantFiled: January 31, 2013Date of Patent: September 12, 2017Assignee: TECHNISCHE UNIVERSITAET MUENCHENInventors: Arne Skerra, Winfried Meining, Evelyn Eggenstein
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Patent number: 9758555Abstract: The present invention relates to methods for treating and/or preventing tumors and/or promoting apoptosis in a neoplastic cell comprising contacting the neoplastic cell with an cell-penetrating dominant-negative ATF5 (“CP-d/n-ATF5”), wherein the CP-d/n-ATF5 is capable of inhibiting ATF5 function and/or activity.Type: GrantFiled: January 27, 2017Date of Patent: September 12, 2017Assignees: The Trustees of Columbia University in the City of New York, The Regents of the University of CaliforniaInventors: Lloyd A. Greene, James Angelastro
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Patent number: 9758556Abstract: The present invention relates to methods for treating and/or preventing tumors and/or promoting apoptosis in a neoplastic cell comprising contacting the neoplastic cell with an cell-penetrating dominant-negative ATF5 (“CP-d/n-ATF5”), wherein the CP-d/n-ATF5 is capable of inhibiting ATF5 function and/or activity.Type: GrantFiled: January 27, 2017Date of Patent: September 12, 2017Assignees: The Trustees of Columbia University in the City of New York, The Regents of the University of CaliforniaInventors: Lloyd A. Greene, James Angelastro
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Patent number: 9758557Abstract: Isolated C1q peptides, fusion proteins and compositions comprising such and fusion proteins comprising are provided. Isolated fusion proteins comprising X4WX5YX6 as defined herein and compositions comprising such are also provided. Methods of treating autoimmune disorders are provided.Type: GrantFiled: July 15, 2014Date of Patent: September 12, 2017Assignee: The Feinstein Institute for Medical ResearchInventor: Betty A. Diamond
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Patent number: 9758558Abstract: A biodegradable hydrogel has been made based on high concentrations of whey protein isolate (WPI). WPI gels of different compositions were fabricated by thermally inducing gelation of high-concentration suspensions of protein, and characterized for compressive strength and modulus, hydration swelling and drying properties, mechanical behavior change due to polysaccharide additives, and intrinsic pore network structure. The gels were shown to be compatible with bone cells and could be used as bone tissue scaffolds. In addition, WPI fibers were produced by electrospinning. Several additives could be incorporated into the WPI gels, including structural additives, growth factors, amino acids, etc. The WPI hydrogels can be made with glycerol to increase flexibility and stability.Type: GrantFiled: April 1, 2011Date of Patent: September 12, 2017Assignee: Board of Supervisors of Louisiana State University And Agriculture and Mechanical CollegeInventors: James E. Henry, Mia Dvora
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Patent number: 9758559Abstract: The present invention relates to short peptides based on the amino acids sequence of the N-terminal domain of the human mitochondrial protein voltage-dependent anion channel 1 (VDAC) and to peptide conjugates having a cell permeability enhancing moiety. The peptides, peptide conjugates and pharmaceutical compositions containing them are useful for treating diseases characterized by cell hyperproliferation or resistance to cell death and in particular, cancer.Type: GrantFiled: July 24, 2014Date of Patent: September 12, 2017Assignees: B.G. Negev Technologies and Applications Ltd., at Ben-Gurion University, The National Institute for Biotechnology in the Negev Ltd.Inventor: Varda Shoshan-Barmatz
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Patent number: 9758560Abstract: The invention relates to a derivative of a GLP-1 peptide, which peptide has two Lys residues, namely a first and a second Lys residue, and a maximum of eight amino acid changes as compared to GLP-1(7-37) (SEQ ID NO: 3), which derivative comprises two protracting moieties attached to the epsilon amino group of said first and second Lys residue, respectively, via a linker, wherein the protracting moiety is selected from Chem. 15: HOOC—(CH2)x-CO—*, and Chem. 16: HOOC—C6H4-O—(CH2)y-CO—*, in which x is an integer in the range of 10-16, and y is an integer in the range of 8-12; and the linker comprises a first linker element *—NH—CH(CH2OH)—CO—*. A preferred linker is g Glu-Ser-Ser-Gly-Ser-Ser-Gly (SEQ ID NO: 2). The derivative of the invention has a very good potency, and a very good binding to the GLP-1 receptor. The invention also relates to the pharmaceutical use of the derivative, for example in the treatment and/or prevention of all forms of diabetes and related diseases.Type: GrantFiled: September 6, 2012Date of Patent: September 12, 2017Assignee: Novo Nordisk A/SInventors: Jesper Lau, Paw Bloch, Patrick William Garibay
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Patent number: 9758561Abstract: The present invention relates to dual GLP-1/glucagon receptor agonists and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as for reduction of excess food intake.Type: GrantFiled: April 6, 2015Date of Patent: September 12, 2017Assignee: SANOFIInventors: Martin Bossart, Ralf Elvert, Andreas Evers, Torsten Haack, Siegfried Stengelin, Michael Wagner, Dieter Kadereit
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Patent number: 9758562Abstract: Provided herein are peptides and variant peptides that exhibit enhanced activity at the GLP-1 receptor, as compared to native glucagon.Type: GrantFiled: September 8, 2015Date of Patent: September 12, 2017Assignee: Indiana University and Technology CorporationInventors: Richard D. DiMarchi, David L. Smiley
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Patent number: 9758563Abstract: An insulin analog comprises a B-chain polypeptide incorporating a chlorinated phenylalanine. The chlorinated phenylalanine may be located at position B24. The chlorinated phenylalanine may be para-monochloro-phenylalanine. The analog may be of a mammalian insulin, such as human insulin. A nucleic acid encodes such an insulin analog. The chlorinated insulin analogs retain significant activity. A method of treating a patient comprises administering a physiologically effective amount of the insulin analog or a physiologically acceptable salt thereof to a patient. Chlorine substitution-based stabilization of insulin may reduce fibrillation and thereby enhance the treatment of diabetes mellitus in regions of the developing world lacking refrigeration.Type: GrantFiled: June 22, 2015Date of Patent: September 12, 2017Assignee: Case Western Reserve UniversityInventor: Michael Weiss
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Patent number: 9758564Abstract: Provided are an acid-resistant yeast cell with genetic modification and reduced Fps1 activity compared to that of a parent cell without the genetic modification; and a method of producing lactate by using the yeast cell.Type: GrantFiled: June 23, 2015Date of Patent: September 12, 2017Assignee: SAMSUNG ELECTRONICS CO., LTD.Inventors: Juyoung Lee, Hyunyoung Shin, Changduk Kang, Seunghyun Lee, Kwangmyung Cho
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Patent number: 9758565Abstract: The present invention provides soluble CTLA4 mutant molecules which bind with greater avidity to the CD80 and/or CD86 antigen than wild type CTLA4 or non-mutated CTLA4Ig. The soluble CTLA4 molecules have a first amino acid sequence comprising the extracellular domain of CTLA4, where certain amino acid residues within the S25-R33 region and M97-G107 region are mutated. The mutant molecules of the invention may also include a second amino acid sequence which increases the solubility of the mutant molecule.Type: GrantFiled: May 29, 2014Date of Patent: September 12, 2017Assignee: Bristol-Myers Squibb CompanyInventors: Robert James Peach, Joseph Naemura, Peter S. Linsley, Jurgen Bajorath
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Patent number: 9758566Abstract: This invention relates to recombinant CTLA-4 proteins, e.g., soluble CTLA-4 or CTLA-4 fusion toxins, and methods for making and using them.Type: GrantFiled: February 28, 2013Date of Patent: September 12, 2017Assignee: The General Hospital CorporationInventors: Zhirui Wang, David H. Sachs, Christene A. Huang
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Patent number: 9758567Abstract: The present invention provides a hemojuvelin (HJV) fusion protein (e.g., a human HJV.Fc) protein, polynucleotides and vectors encoding such proteins, and methods for making such proteins. Also provided are methods for treating iron-related disorders which include administration of a HJV fusion protein to a patient in need thereof.Type: GrantFiled: October 20, 2014Date of Patent: September 12, 2017Assignee: THE GENERAL HOSPITAL CORPORATIONInventors: Herbert Y. Lin, Jodie Babitt, Clifford J. Woolf, Tarek A. Samad
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Patent number: 9758568Abstract: The present invention relates to oligopeptide-free cell culture media comprising at least 0.5 mg/L of a polyamine and to methods for cultivating cells in said oligopeptide-free cell culture media comprising at least 0.5 mg/L of a polyamine. The invention also relates to methods for expressing at least one protein in a medium comprising at least 0.5 mg/L of a polyamine and to methods for producing at least one virus in a medium comprising at least 0.5 mg/L of a polyamine.Type: GrantFiled: November 16, 2015Date of Patent: September 12, 2017Assignees: Baxalta GmbH, Baxalta IncorporatedInventors: Leopold Grillberger, Manfred Reiter, Wolfgang Mundt, Artur Mitterer
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Patent number: 9758569Abstract: Novel collagen mimics are disclosed with a tripeptide unit having the formula (Xaa-Yaa-Gly)n, where one of the positions Xaa or Yaa is a bulky, non-electron withdrawing proline derivative. By substituting a proline derivative at either the Xaa or Yaa position in the native collagen helix, the stability of the helix is increased due solely to steric effects relative to prior known collagen-related triple helices. Methods are also disclosed for making the novel collagen mimics.Type: GrantFiled: May 25, 2007Date of Patent: September 12, 2017Assignee: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Ronald T. Raines, Matthew D. Shoulders, Jonathan A. Hodges
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Patent number: 9758570Abstract: The present invention generally provides processes for purification of Inter-alpha inhibitor proteins (I?Ip) and compositions thereof from blood.Type: GrantFiled: September 21, 2015Date of Patent: September 12, 2017Assignee: ProThera Biologics, Inc.Inventors: Yow-Pin Lim, Edward S. Sirya, Peter Brne
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Patent number: 9758571Abstract: There are provided peptide tags derived from bacteriophytochrome (BphP) that is photoreceptor protein of Deinococcus radiodurans, an antibody capable of specifically recognizing the peptide tags, hybridoma cell lines capable of producing the antibody, and uses thereof. The novel peptide tag has advantages in that it has a short length and can remove a non-specific reaction of the conventional c-myc tag and FLAG tag. Therefore, in the case of using the novel peptide tag and antibody thereto, the fusion protein expressed in a recombinant cell can be very effectively detected or purified. In addition, an epitope tagging system including the novel peptide tag and antibody thereto can be applied in various fields such as a determination of an intracellular site, a confirmation of functionality, detection and purification of specific protein, and researches on interaction between proteins.Type: GrantFiled: June 20, 2013Date of Patent: September 12, 2017Assignees: University—Industry Cooperation Group Of Kyung Hee University, Myongji University Industry and Academia Cooperation FoundationInventors: Seong Hee Bhoo, Tae Ryong Hahn, Tae Lim Kim, Joo Won Suh, Seung Hwan Yang