Patents Issued in July 15, 2014
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Patent number: 8779090Abstract: Peptides that act as GC-C receptor agonists and contain at least one D-cys and are useful for the treatment of diuresis and heart disease as well as other disorders are described.Type: GrantFiled: February 26, 2008Date of Patent: July 15, 2014Assignee: Ironwood Pharmaceuticals, Inc.Inventors: Daniel Zimmer, Angelika Fretzen, Mark Currie, G. Todd Milne
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Patent number: 8779091Abstract: A selective targeting method is disclosed comprising contacting a library of ligands, particularly a peptide library, with an anti-target to allow the ligands to bind to the anti-target; separating the non-binding ligands from the anti-target bound ligands, contacting the non-binding anti-target ligands with a target allowing the unbound ligands to bind with the target to form a target-bound ligand complex; separating the target-bound ligand complex from ligands which do not bind to the target, and identifying the target-bound ligands on the target-bound ligand complex wherein the target-bound ligands have a KD in the range of about 10?7 to 10?10 M. Additionally claimed are the ligands identified according to the method.Type: GrantFiled: October 23, 2012Date of Patent: July 15, 2014Assignee: Danisco US Inc.Inventors: Christopher J. Murray, Pilar Tijerina, David A. Estell, Yiyou Chen
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Patent number: 8779092Abstract: The present invention concerns peptide sequences that specifically recognize cells of human hepatic metastases. The invention comprises also the use of nucleic acids coding for such peptides, as well as conjugates and formulations of such peptides for diagnostic and therapeutic purposes.Type: GrantFiled: November 30, 2007Date of Patent: July 15, 2014Assignee: Universita Degli Studi di TorinoInventors: Federico Bussolino, Serena Marchio
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Patent number: 8779093Abstract: This invention relates to methods and compositions for detection and treatment of neurodegenerative diseases. In particular, the invention relates to polypeptides that can protect against neuron degeneration, nucleic acid molecules that encode such polypeptides, and antibodies that recognize said polypeptides.Type: GrantFiled: September 10, 2009Date of Patent: July 15, 2014Assignee: INSERM (Institut National de la Sante et de la Recherche Medicale)Inventors: Thierry Leveillard, Celine Jaillard, Jose-Alain Sahel
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Patent number: 8779094Abstract: The present invention also provides a high concentration low viscosity suspension of an pharmaceutically acceptable solvent with one or more sub-micron or micron-sized non-crystalline particles comprising one or more proteins or peptides. Optionally one or more additives in the pharmaceutically acceptable solvent to form a high concentration low viscosity suspension with a concentration of at least 20 mg/ml and a solution viscosity of between 2 and 100 centipoise that is suspendable upon shaking or agitation, wherein upon delivery the one or more sub-micron or micron-sized peptides dissolves and do not form peptide aggregates syringeable through a 21 to 27-gauge needle.Type: GrantFiled: November 10, 2009Date of Patent: July 15, 2014Assignee: Board of Regents, The University of Texas SystemInventors: Keith P. Johnston, Maria Andrea Mazuski, Joshua Engstrom, Miguel Angelo Rodrigues
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Patent number: 8779095Abstract: LAT (Linker for Activation of T-cells) is a protein involved in signaling through the T-cell receptor (TCR). The invention provides a LAT protein including mutations at ubiquitylation sites that result in an increase in stability of LAT in stimulated and unstimulated cells, and enhanced signaling through the TCR. The invention further provides use for a LAT protein including mutations at ubiquitylation sites for therapeutic and laboratory methods.Type: GrantFiled: April 30, 2010Date of Patent: July 15, 2014Assignee: The United States of America, as represented by the Secretary, Department of Health & Human ServicesInventors: Lawrence E. Samelson, Lakshmi Balagopalan
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Patent number: 8779096Abstract: The invention relates to novel neurogenin proteins, nucleic acids and antibodies.Type: GrantFiled: June 26, 2012Date of Patent: July 15, 2014Assignee: California Institute of TechnologyInventors: David J. Anderson, Quifa Ma, Lukas Sommer
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Patent number: 8779097Abstract: The invention discloses a process for the acceleration of gelling time of regenerated silk fibroin using gelling agent, preferably silica to create a porous structure, devoid of microbial growth.Type: GrantFiled: July 30, 2010Date of Patent: July 15, 2014Assignee: Council of Scientific & Industrial ResearchInventors: Shailesh Prakash Nagarkar, Ashish Kishore Lele
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Patent number: 8779098Abstract: The invention provides the identification and characterization of disease and cancer-associated antigen, RAAG10. The invention also provides a family of monoclonal antibodies that bind to antigen RAAG10, methods of diagnosing and treating various human cancers and diseases that express RAAG10.Type: GrantFiled: March 27, 2009Date of Patent: July 15, 2014Assignee: MacroGenics West, Inc.Inventors: Jennie P. Mather, Ronghao Li, Zhuangyu Pan, Penelope E. Roberts
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Patent number: 8779099Abstract: Methods and compositions for using the MHC class II invariant chain polypeptide, Ii (also known as CD74), as a receptor for macrophage migration inhibitory factor (MIF), are disclosed. These include methods and compositions for using this receptor, as well as agonists and antagonists of MIF which bind to this receptor, or which otherwise modulate the interaction of MIF with CD74 or the consequences of such interaction, in treatment of conditions characterized by locally or systemically altered MIF levels, particularly inflammatory conditions and cancer.Type: GrantFiled: June 14, 2011Date of Patent: July 15, 2014Assignees: Baxter International Inc., Baxter Healthcare S.A.Inventors: Richard J. Bucala, Lin Leng, Christine N. Metz
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Patent number: 8779100Abstract: The invention provides therapeutic anti-beta7 antibodies, compositions comprising, and methods of using these antibodies.Type: GrantFiled: January 12, 2012Date of Patent: July 15, 2014Assignee: Genentech, Inc.Inventors: Sherman Fong, Mark S. Dennis
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Patent number: 8779101Abstract: Proteins that bind IL-17 and/or IL-17F are described along with there use in composition and methods for treating, preventing, and diagnosing IL-17 related diseases and for detecting IL-17 in cells, tissues, samples, and compositions.Type: GrantFiled: August 5, 2013Date of Patent: July 15, 2014Assignee: AbbVie, Inc.Inventors: Chung-Ming Hsieh, Margaret Hugunin, Anwar Murtaza, Bradford L. McRae, Yuliya Kutskova, John E. Memmott, Jennifer M. Perez, Suju Zhong, Edit Tarcsa, Anca Clabbers, Craig Wallace, Shaughn H. Bryant, Mary R. Leddy
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Patent number: 8779102Abstract: The invention relates to recognition molecules directed towards tumors, and it also relates to pharmaceutical compositions comprising such recognition molecules, methods for the production of such recognition molecules, and to the use of such recognition molecules in the diagnosis and therapy of tumor diseases.Type: GrantFiled: January 23, 2004Date of Patent: July 15, 2014Assignee: Glycotope GmbHInventors: Steffen Goletz, Antje Danielczyk, Renate Stahn, Uwe Karsten
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Patent number: 8779103Abstract: The present invention relates to drug fusions that have improved serum half lives. These fusions and conjugates comprise polypeptides, immunoglobulin (antibody) single variable domains and GLP and/or exendin molecules. The invention further relates to uses, formulations, compositions and devices comprising such drug fusions and conjugates.Type: GrantFiled: March 24, 2010Date of Patent: July 15, 2014Assignee: Glaxo Group LimitedInventors: Christopher Herring, Lucy J. Holt, Laurent S. Jespers, Sebastian Mayer, Malgorzata Pupecka-Swider
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Patent number: 8779104Abstract: The present invention provides methods and compositions useful in the treatment or prevention of Chlamydia infections and cancer. The methods and compositions inhibit the entry of Chlamydia into a host cell expressing EMP2 by interfering with the interaction between the Chlamydia and EMP2. The methods and compositions target cancers which express or overexpress EMP2 nucleic acids and polypeptides by targeting EMP2.Type: GrantFiled: August 21, 2013Date of Patent: July 15, 2014Assignee: The Regents of the University of CaliforniaInventors: Jonathan Braun, Lynn K. Gordon, Kaori Shimazaki Dadgostar, Madhuri Wadehra, Kathleen A. Kelly, Anna M. Wu
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Patent number: 8779105Abstract: The present invention provides isolated monoclonal antibodies, particularly human monoclonal antibodies, that specifically bind to PD-1 with high affinity. Nucleic acid molecules encoding the antibodies of the invention, expression vectors, host cells and methods for expressing the antibodies of the invention are also provided. Immunoconjugates, bispecific molecules and pharmaceutical compositions comprising the antibodies of the invention are also provided. The invention also provides methods for detecting PD-1, as well as methods for treating various diseases, including cancer and infectious diseases, using anti-PD-1 antibodies. The present invention further provides methods for using a combination immunotherapy, such as the combination of anti-CTLA-4 and anti-PD-1 antibodies, to treat hyperproliferative disease, such as cancer. The invention also provides methods for altering adverse events related to treatment with such antibodies individually.Type: GrantFiled: August 15, 2011Date of Patent: July 15, 2014Assignee: Medarex, L.L.C.Inventors: Alan J. Korman, Mohan Srinivasan, Changyu Wang, Mark J. Selby, Bing Chen, Josephine M. Cardarelli, Haichun Huang
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Patent number: 8779106Abstract: Various embodiments of the invention provide human kinases and phosphatases (KPP) polypeptides and polynucleotides which identify and encode KPP. Embodiments of the invention also provide expression vectors, host cells, antibodies, agonists, and antagonists. Other embodiments provide methods for diagnosing, treating, or preventing disorders associated with aberrant expression of KPP.Type: GrantFiled: July 30, 2012Date of Patent: July 15, 2014Assignee: Incyte CorporationInventors: Vicki S. Elliott, Reena Khare, Thomas W. Richardson, Joseph P. Marquis, Anita Swarnakar, April J. A. Hafalia, Shanya D. Becha, Narinder K. Chawla-Walia, Mariah R. Baughn, Soo Yeun Lee, Uyen K. Tran, Henry Yue, Danniel B. Nguyen, Michael B. Thornton, Rajagopal Gururajan, Ameena R. Gandhi, Yan Lu, Monique G. Yao, Joana X. Li, Wen Luo, Ernestine A. Lee, Ian J. Forsythe, Craig H. Ison, Amy D. Wilson, Pei Jin
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Patent number: 8779107Abstract: The present disclosure relates to a composition for targeting dendritic cells. In particular, the present disclosure relates to a composition comprising: a) one or more antigens; b) an anti-DC-SIGN immunoglobulin single variable domain; and c) a carrier which carries a) and b). The disclosure further relates to formulations, compositions and devices comprising such anti-DC-SIGN molecules and their use as a medicament and in the treatment of cancer, suitably melanoma.Type: GrantFiled: October 19, 2009Date of Patent: July 15, 2014Assignees: Lipotek Pty Ltd, Domantis LimitedInventors: Joseph Altin, Ines Atmosukarto, Rudolf Maria De Wildt, Christopher Parish, Jason Price
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Patent number: 8779108Abstract: Human monoclonal antibodies directed against B7-H1 and uses of these antibodies in diagnostics and for the treatment of diseases associated with the activity and/or expression of B7-H1 are disclosed. Additionally, hybridomas or other cell lines expressing such antibodies are disclosed.Type: GrantFiled: November 24, 2010Date of Patent: July 15, 2014Assignee: MedImmune, LimitedInventors: Christophe Queva, Michelle Morrow, Scott Hammond, Marat Alimzhanov, John Babcook, Ian Nevin Foltz, Jaspal Singh Kang, Laura Sekirov, Melanie Boyle, Matthieu Chodorge, Ross A. Stewart, Kathleen Ann Mulgrew
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Patent number: 8779109Abstract: The invention relates to growth hormone compounds with a protracted profile. The effect is obtained by linking an albumin binding residue via a hydrophilic spacer to growth hormone variants. Further described are methods of preparing and using such compounds. These growth hormone compounds are based on there althered profile considered particular useful in therapy.Type: GrantFiled: December 18, 2013Date of Patent: July 15, 2014Assignee: Novo Nordisk Health Care AGInventors: Carsten Behrens, Nils Langeland Johansen, Henrik Sune Andersen, Leif Noerskov-Lauritsen
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Patent number: 8779110Abstract: The invention provides an efficient method of purification of a modified cytokine. The process includes the use of a chromatographic technique for the purification of the desired cytokine. The purified cytokine can be used as a therapeutic composition.Type: GrantFiled: June 23, 2009Date of Patent: July 15, 2014Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.Inventors: Chaiti Roy, Darshan Koticha, Vivek Arthanari
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Patent number: 8779111Abstract: A novel gene 024P4C12 (also designated 24P4C12) and its encoded protein, and variants thereof, are described wherein 24P4C12 exhibits tissue specific expression in normal adult tissue, and is aberrantly expressed in the cancers listed in Table I. Consequently, 24P4C12 provides a diagnostic, prognostic, prophylactic and/or therapeutic target for cancer. The 24P4C12 gene or fragment thereof, or its encoded protein, or variants thereof, or a fragment thereof, can be used to elicit a humoral or cellular immune response; antibodies or T cells reactive with 24P4C12 can be used in active or passive immunization.Type: GrantFiled: September 14, 2012Date of Patent: July 15, 2014Assignee: Agensys, Inc.Inventors: Arthur B. Raitano, Karen Jane Meyrick Morrison, Wangmao Ge, Pia M. Challita-Eid, Aya Jakobovits
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Patent number: 8779112Abstract: This invention relates to modified polynucleotides encoding modified proteases, and methods for altering the production of proteases in microorganisms. In particular, the present invention relates to methods for altering the expression of proteases in microorganisms, such as Bacillus species. The invention discloses modified polynucleotides, vectors, modified polypeptides, and processes for enhancing the production of proteases.Type: GrantFiled: March 12, 2008Date of Patent: July 15, 2014Assignee: Danisco US Inc.Inventors: Eugenio Ferrari, David A. Estell
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Patent number: 8779113Abstract: The invention provides a group of nucleic acid fragments, shown in the sequence listing, for prevention of HIV infection or AIDS and the usage thereof. In the invention, a series of RNA fragments, which are highly homogenous to all the published HIV gene sequences, were obtained by homology compare. The double-stranded RNA (dsRNA) derived from these fragments can effectively inhibit the expression of the HIV genes. The RNA transcribed by plasmid, also can suppress the expression of the HIV in the cell. After the adenovirus or associated virus which carry DNA corresponding above RNA infect the cell, the transcription dsRNA can inhibit the expression of the HIV genes.Type: GrantFiled: January 10, 2011Date of Patent: July 15, 2014Assignee: Beijing Solobio Genetechnology Company Ltd.Inventors: Zhiwen Zhou, Yuxia Feng, Conglin Zuo, Yuejuan Li
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Patent number: 8779114Abstract: Provided are an siRNA-polymer conjugate, and a method for preparing the same, and more specifically, to a hybrid conjugate formed by covalently bonding siRNA and a polymeric compound for improving the in vivo stability of siRNA, and to a preparation method of the hybrid conjugate. The conjugate of the present invention can improve the in vivo stability of siRNA, thereby achieving an efficient delivery of therapeutic siRNA into cells and exhibiting the activity of siRNA even with a small dose of a relative low concentration. Therefore, the conjugate can advantageously be used as not only an siRNA treatment tool for cancers and other infectious disease, but also a novel type siRNA delivery system.Type: GrantFiled: May 13, 2010Date of Patent: July 15, 2014Assignee: Bioneer CorporationInventors: Bo Ram Han, Han Oh Park, Mi Sik Shin, Sam Young Lee
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Patent number: 8779115Abstract: Methods, compositions, and kits that include small hairpin RNA (shRNA) useful for inhibition of gene expression, such as viral-mediated gene expression, are described.Type: GrantFiled: August 22, 2012Date of Patent: July 15, 2014Assignee: Somagenics Inc.Inventors: Qing Ge, Brian H. Johnston, Sergei A Kazakov, Heini Ilves, Anne Dallas
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Patent number: 8779116Abstract: The present invention is directed to small interfering RNA molecules (siRNA) targeted against an allele of interest, and methods of using these siRNA molecules.Type: GrantFiled: November 5, 2012Date of Patent: July 15, 2014Assignee: University of Iowa Research FoundationInventors: Beverly L. Davidson, Henry Paulson, Victor Miller, Cynthia Gouvion
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Patent number: 8779117Abstract: Provided herein are pharmaceutical compositions or dosage forms comprising crystalline 5-azacytidine monohydrate. The pharmaceutical compositions or dosage forms provided herein may be used for oral administration in the treatment of diseases, including the treatment of myelodysplastic syndromes (MDS).Type: GrantFiled: May 25, 2010Date of Patent: July 15, 2014Assignee: Pharmion LLCInventors: Dumitru Ionescu, Peter Blumbergs, Gary L. Silvey
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Patent number: 8779118Abstract: Provided herein are novel base modified bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, novel pyrimidine bicyclic nucleosides are provided wherein each pyrimidine base is substituted at the 5 position with an optionally substituted, aromatic or heteroaromatic ring system comprising from 5 to 7 ring atoms selected from C, N, O and S. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.Type: GrantFiled: January 6, 2011Date of Patent: July 15, 2014Assignee: Isis Pharmaceuticals, Inc.Inventors: Charles Allerson, Balkrishen Bhat, Eric E. Swayze
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Patent number: 8779119Abstract: The invention provides a metal salt of a crosslinked cellulose derivative represented by the following formula (I), wherein the degree of substitution of the hydroxyl group of glucose unit of the crosslinked cellulose derivative by a functional group a is 1 or more. R—O—A??(I) {In the formula (I), R represents a crosslinked cellulose residue and A represents a functional group a having cation-exchange ability.Type: GrantFiled: December 26, 2007Date of Patent: July 15, 2014Assignee: JNC CorporationInventors: Naoyuki Yoshida, Kazushi Ishida, Shuji Sasaki, Ippei Yamaoka
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Patent number: 8779120Abstract: The present invention relates to novel macrocyclic derivatives of glycolurils of general formula I, and methods of their preparation. These novel derivatives can be used for the selective removing of various compounds from solutions in polar and nonpolar solvents, and from water, e.g. for water purification and desalination, also for separation of liquid mixtures and mixtures of gases and organic solvent vapors, preparation of ion-exchange materials and materials which are used as stationary phase in chromatography, construction of sensors, transport and targeting of drugs in organisms, and also preparation of materials bearing aromatic or curative compounds.Type: GrantFiled: October 26, 2010Date of Patent: July 15, 2014Assignee: Masarykova UniverzitaInventors: Vladimir Sindelar, Jan Svec, Vaclav Havel
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Patent number: 8779121Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.Type: GrantFiled: October 11, 2013Date of Patent: July 15, 2014Assignee: Les Laboratoires ServierInventors: Maria Del Pilar Carranza, Maria Isabel Garcia Aranda, José Lorenzo Gonzalez, Frédéric Sanchez
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Patent number: 8779122Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.Type: GrantFiled: November 6, 2013Date of Patent: July 15, 2014Assignee: Les Laboratoires ServierInventors: Maria Del Pilar Carranza, Maria Isabel Garcia Aranda, José Lorenzo Gonzalez, Frédéric Sanchez
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Patent number: 8779123Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.Type: GrantFiled: December 3, 2013Date of Patent: July 15, 2014Assignee: Les Laboratoires ServierInventors: Maria Del Pilar Carranza, Maria Isabel Garcia Aranda, José Lorenzo Gonzalez, Frédéric Sanchez
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Patent number: 8779124Abstract: A redox ammoximation process in which a ketone or aldehyde is reacted with ammonia and oxygen in the presence of a catalyst, wherein: the catalyst is an aluminophosphate based redox catalyst having the qualitative general formula (I) M1M2AlPO-5 (I) in which M1 is at least one transition metal atom having redox catalytic capability; M2 is at least one metal atom in the (IV) oxidation state; M1 and M2 are different from each other; and a proportion of the phosphorous atoms in the M1M2AlPO-5 type structure are replaced by M2 atoms.Type: GrantFiled: May 8, 2013Date of Patent: July 15, 2014Assignee: University of SouthamptonInventors: Robert Raja, Alexander James Patterson
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Patent number: 8779125Abstract: A redox ammoximation process in which a ketone or aldehyde is reacted with ammonia and oxygen in the presence of a catalyst; wherein the catalyst is an aluminophosphate based redox catalyst having at least two different redox catalytic sites comprising different transition metal atoms.Type: GrantFiled: May 8, 2013Date of Patent: July 15, 2014Assignee: University of SouthamptonInventors: Robert Raja, John Meurig Thomas
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Patent number: 8779126Abstract: A dye, having a structure represented by formula (1A): wherein A represents a group of atoms necessary for forming a ring together with the carbon-nitrogen bond; at least one of Y1A and Y2A represents an acidic group, in which when they each represent an acidic group, they may be the same as or different from each other, or when only one of them represents an acidic group, the other represents an electron-withdrawing group; D represents a group to give a dye; n represents an integer of 1 or greater; L represents a single bond or a divalent linking group; and Y3A represents an acidic group.Type: GrantFiled: October 29, 2009Date of Patent: July 15, 2014Assignee: Fujifilm CorporationInventors: Katsumi Kobayashi, Keizo Kimura, Tatsuya Susuki, Hirotaka Satou, Yukio Tani
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Patent number: 8779127Abstract: The present invention provides a facile process for the preparation of tri- and tetra—substituted pyrimidines. The process is useful for preparing inhibitors of protein kinases, especially Aurora kinase. These inhibitors are useful for treating or lessening the severity of Aurora—mediated diseases or conditions.Type: GrantFiled: August 15, 2012Date of Patent: July 15, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Francesca Mazzei, David Kay, Andrew Miller
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Patent number: 8779128Abstract: Oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3? and/or 5?-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.Type: GrantFiled: May 27, 2011Date of Patent: July 15, 2014Assignee: Sarepta Therapeutics, Inc.Inventors: Gunnar J. Hanson, Charles Rudolph, Bao Zhong Cai, Ming Zhou, Dwight D. Weller
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Patent number: 8779129Abstract: The present invention provides novel compounds of formula I wherein W1, W2, W3, W4, W5, B, X1, X2, X3, X4, X5, E and L are as defined herein; invention compounds are gamma amino butyrique acid receptor-subtype B (“GABAB”) positive allosteric modulators (enhancers), which are useful to provide methods of treating or preventing diseases or disorders, including treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, panic disorder, posttraumatic stress disorders, urge urinary incontinence, gastroesophageal reflux disease, transient lower oesophageal sphincter relaxations, functional gastrointestinal disorders and irritable bowel syndrome.Type: GrantFiled: December 14, 2012Date of Patent: July 15, 2014Assignee: Addex Pharma S.A.Inventors: Eric Riguet, Brice Campo, Antoine Gibelin, Karim Mhalla
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Patent number: 8779130Abstract: A process for high-pressure, liquid phase conversion of urea into melamine is disclosed, where molten urea is fed to a first reaction zone (S1) where the melamine melt is under mechanical agitation, and a heat input (Q1) is provided to maintain the endothermic reaction, and the liquid is then passed to a second reaction zone (S2) kept at a lower temperature and where further agitation is provided. Embodiments of plants adapted to carry out the process are also disclosed, including multiple stirred reactors in cascade and a single reactor with multiple internal compartments defining said first and second reaction zones.Type: GrantFiled: May 14, 2009Date of Patent: July 15, 2014Assignee: Urea Casale SAInventor: Giancarlo Sioli
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Patent number: 8779131Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed. An exemplary compound disclosed in this application is shown below.Type: GrantFiled: February 12, 2013Date of Patent: July 15, 2014Assignee: Icos CorporationInventors: Edward A. Kesicki, Kerry W. Fowler, Danwen Huang, Hua Chee Ooi, Amy Oliver, Kamal Deep Puri, Fuqiang Ruan, Jennifer Treiberg
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Patent number: 8779132Abstract: The invention provides a compound for use in medicine, the compound being a compound of the formula (VI0) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R1 is hydrogen, hydroxy, or O—Rz; R2a is hydroxy, methoxy or O—Rz; provided that at least one of R1 and R2a is O—Rz; Rz is Lp-Rp1; SO3H; a glucuronide residue; a mono-, di- or tripeptide residue; or Lp is a bond, C?O, (C?O)O, (C?O)NRp1 or S(O)xNRp1; x is 1 or 2; Rp1 is hydrogen or a an optionally substituted C1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that Rp1 is not hydrogen when Lp is a bond, C?O or (C?O)O; and provided also that O—Rz does not contain an O—O moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group Rp1; and R3, R4a, R8 and R10 are defined in the claims.Type: GrantFiled: October 12, 2007Date of Patent: July 15, 2014Assignee: Astex Therapeutics LimitedInventors: Miles Stuart Congreve, Lynsey Helen Fazal, Martyn Frederickson, Christopher William Murray, Michael Alistair O'Brien, Andrew James Woodhead, John Francis Lyons, Neil Thomas Thompson
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Patent number: 8779133Abstract: Provided are novel ligands for transition metal complexes which exhibit high coordination power with respect to metals by being free of substituents at the positions ortho to phosphorus or arsenic and which have electron-withdrawing power comparable to the highest level known in conventional ligands. One ligand includes a compound represented by General Formula (1): R1R2R3A or General Formula (2): R1R2A-Y-AR3R4 and having a total of 15 to 110 carbon atoms. In the formulae, A is phosphorus or arsenic; R1, R2, R3 and R4 are each independently a substituted pyridyl group having optionally different electron-withdrawing groups bonded to the positions meta to the atom A as well as hydrogen atoms bonded to the positions ortho to the atom A; and Y is a divalent group derived from a C2-20, optionally substituted and optionally heteroatom-containing, aliphatic, alicyclic or aromatic compound or from ferrocene.Type: GrantFiled: February 16, 2012Date of Patent: July 15, 2014Assignee: National University Corporation Okayama UniversityInventors: Toshinobu Korenaga, Takashi Sakai, Aram Ko
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Patent number: 8779134Abstract: A six-coordinated ruthenium complex is represented by the following formula (I): RuL1L2L3??(I) wherein L1 represents a 2,2?-bipyridine-based bidentate ligand having at least two functional groups selected from COOH, a carboxylate group and the combination thereof; and L2 and L3 independently represent a 1-(haloalkylpyrazole)-isoquinoline-based bidentate ligand of formula (II) or formula (III).Type: GrantFiled: October 18, 2013Date of Patent: July 15, 2014Assignee: National Tsing Hua UniversityInventors: Yun Chi, Fa-Chun Hu, Sheng-Wei Wang, Wan-Ping Ku, Pei-Hua Chen, Ya-Wan Yang
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Patent number: 8779135Abstract: The technology of this invention concerns a method for the manufacture of hydroxy diphosphonic acids containing an amino moiety. The method specifically involves reacting a liquid P4O6 with an aminocarboxylic acid in the presence of a sulfonic acid. The aminocarboxylic acid is selected from 3 structurally different compounds. The amino hydroxy diphosphonic acids can be synthesized with high selectivity and purity and the unreacted starting raw materials can easily and conveniently be recirculated.Type: GrantFiled: October 4, 2010Date of Patent: July 15, 2014Assignee: Straitmark Holding AGInventors: Samuel Corentin Cogels, David Lemin, Patrick Notté
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Patent number: 8779136Abstract: The present invention provides novel ruthenium based catalysts, and a process for preparing amines, by reacting a primary alcohol and ammonia in the presence of such catalysts, to generate the amine and water. According to the process of the invention, primary alcohols react directly with ammonia to produce primary amines and water in high yields and high turnover numbers. This reaction is catalyzed by novel ruthenium complexes, which are preferably composed of quinolinyl or acridinyl based pincer ligands.Type: GrantFiled: October 18, 2013Date of Patent: July 15, 2014Assignee: Yeda Research and Development Co. Ltd.Inventors: David Milstein, Chidambaram Gunanathan
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Patent number: 8779137Abstract: The present invention provides a novel compound having an excellent property to inject a hole into a device such as an organic EL device.Type: GrantFiled: December 22, 2010Date of Patent: July 15, 2014Assignee: Sumitomo Chemical Company, LimitedInventor: Satoshi Kobayashi
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Patent number: 8779138Abstract: Camptothecin-based compounds are useful for treating a neoplasm in mammalian subjects by administering such compound to the subjects in combination with radiotherapy, i.e., the treatment of tumors with radioactive substances or radiation from a source external to the subject. Camptothecin-based compounds are modified by positioning at least one electron-affinic group around the camptothecin structure to enhance their value in combination with radiotherapy. New Camptothecin-based compounds are disclosed that are useful for treating cancer by administering the novel compounds alone or in combination with radiotherapy.Type: GrantFiled: January 24, 2011Date of Patent: July 15, 2014Assignees: Sutter West Bay Hospital, Catholic Healthcare WestInventor: Li-Xi Yang
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Patent number: 8779139Abstract: The present invention provides methods for the preparation of substituted 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole derivative useful as intermediates and methods for producing and using such intermediates.Type: GrantFiled: August 23, 2012Date of Patent: July 15, 2014Assignee: Intra-Cellular Therapies, Inc.Inventors: John Charles Tomesch, Peng Li, Wei Yao, Qiang Zhang, James David Beard, Andrew S. Thompson, Hua Cheng, Lawrence P. Wennogle