Patents Examined by Brian McDowell
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Patent number: 9812658Abstract: The present invention relates to compounds of formula (I) based on a porphyrin core and a ?-conjugated linker or acceptor introduced between the porphyrin core and an anchoring group having a high absorption coefficient covering the whole UV-Visible and near-infrared spectral response, and their use as sensitizer or dye and an electrochemical or optoelectronic device including a compound of the invention.Type: GrantFiled: December 4, 2014Date of Patent: November 7, 2017Assignee: Ecole Polytechnique Federale de Lausanne (EPFL)Inventors: Chenyi Yi, Fabrizio Giordano, Shaik Mohammad Zakeeruddin, Michael Graetzel
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Patent number: 9802904Abstract: Disclosed are inhibitors of the USP1/UAF1 deubiquitinase complex, for example. of formula (I), wherein R1, R2, and Q are as defined herein, which are useful in treating diseases such as cancer, and improving the efficacy of DNA damaging agents in cancer treatment. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the invention, a method of method of inhibiting a heterodimeric deubiquitinase complex in a cell, and a method of enhancing the chemotherapeutic treatment of cancer in a mammal undergoing treatment with an anti cancer agent. Further disclosed is a method of preparing compounds of the invention.Type: GrantFiled: December 26, 2013Date of Patent: October 31, 2017Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, University of DelawareInventors: David J. Maloney, Andrew S. Rosenthal, Ajit Jadhav, Thomas S. Dexheimer, Anton Simeonov, Zhihao Zhuang, Qin Liang, Diane K. Luci
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Patent number: 9796732Abstract: The present invention belongs to the field of pharmaceutical Chemistry. In particular, the present invention relates to a pyridopyrimidine or pyrimidopyrimidine compound as represented by general formula (I), or an isomer thereof or a pharmaceutically acceptable salt, ester, prodrug or solvate thereof, a preparation method, a pharmaceutical composition and uses thereof in preparing a mTOR inhibitor. As a mTOR inhibitor, the compound or the pharmaceutical composition thereof can be used for treating a disease or condition due to PI3K-AKT-mTOR signalling pathway malfunction.Type: GrantFiled: September 1, 2015Date of Patent: October 24, 2017Assignee: SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.Inventors: Jingkang Shen, Ke Yu, Tao Meng, Lanping Ma, Arie Zask, Lanfang Meng, Xin Wang, Yiyi Chen
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Patent number: 9796717Abstract: Tricyclic chemical modulators of FOXO transcription factor proteins are disclosed. The compounds are useful to treat cancer, age-onset proteotoxicity, stress-induced depression, inflammation, and acne. The compounds are of the following and similar genera: in which Het is an aromatic heterocyclic ring and Y is a point of attachment of various side chains and rings.Type: GrantFiled: February 19, 2014Date of Patent: October 24, 2017Assignee: ICAHN SCHOOL OF MEDICINE AT MOUNT SINAIInventors: Michael Ohlmeyer, David Kastrinsky
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Patent number: 9790231Abstract: The invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine for the treatment of diseases, disorders associated with the modulation of calcium release-activated calcium (CRAC) channel. The invention also relates to pharmaceutical compositions containing such compounds in treating diseases disorders associated with calcium release-activated calcium (CRAC) channel modulators.Type: GrantFiled: June 23, 2014Date of Patent: October 17, 2017Assignee: LUPIN LIMITEDInventors: Nageswara Rao Irlapati, Kiran Chandrashekhar Kulkarni, Vijay Pandurang Karche, Gokul Keruji Deshmukh, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
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Patent number: 9789206Abstract: Compounds, systems, and methods are provided for a non-invasive, analyte sensing dressing. The dressing includes a sensor and a matrix. The sensor is capable of detecting analytes such as molecular oxygen, carbon dioxide, nitric oxides, dissolved analytes in plasma, and hydrogen ions. The device emits a detectable signal when the sensor is excited in the presence of the analyte. The sensor may include a meso-unsubstituted metallated porphyrin that is sensitive towards oxygen. The porphyrin can be excited when illuminated at a first wavelength, followed by emission of phosphorescence at a second wavelength whose intensity is an indicator for oxygen concentration. An example metallated porphyrin has the Formula(I): wherein M is a metal, each R is independently an atom or a group of atoms, and at least one R is —OR1, wherein R1 is an atom or a group of atoms.Type: GrantFiled: June 13, 2014Date of Patent: October 17, 2017Assignee: The General Hospital CorporationInventors: Conor L. Evans, Gabriela Apiou, Alexander J. Nichols, Emmanouil Rousakis, Zongxi Li
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Patent number: 9776975Abstract: A new class of antibiotics effective against methicillin-resistant Staphylococcus aureus (MRSA) is disclosed. Compounds of this class can impair cell-wall biosynthesis by binding to both the allosteric and the catalytic domains of penicillin-binding protein (PBP) 2a. This class of antibiotics holds promise in reversing obsolescence of staphylococcal PBPs as important targets for antibiotics. Embodiments of the invention thus provide novel antibacterial compounds that target penicillin-binding proteins and/or other important cellular targets. Methods for inhibiting the growth and/or replication of bacteria using the compounds described herein are also provided. Various embodiments exhibit activity against gram positive bacteria, including drug-resistant strains of Staphylococcus aureus.Type: GrantFiled: March 5, 2014Date of Patent: October 3, 2017Assignee: University of Notre Dame du LacInventors: Mayland Chang, Shahriar Mobashery, Renee Bouley
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Patent number: 9777006Abstract: The present invention is directed to compounds encompassed by the Formula (I): pharmaceutical compositions thereof, methods for inhibiting LTA-4 hydrolase, and methods for the treatment of a disease and disorder which is ameliorated by the inhibition of LTA4h activity. Non-limiting examples of such diseases and conditions include inflammatory and autoimmune diseases and disorders.Type: GrantFiled: September 10, 2015Date of Patent: October 3, 2017Assignee: Celtaxsys, Inc.Inventor: William Guilford
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Patent number: 9777019Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A3, A4, A5, A6, L, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: February 11, 2016Date of Patent: October 3, 2017Assignee: Amgen Inc.Inventors: Ryan White, Yuan Cheng, Ana Elena Minatti, Bryant Yang, Xiao Mei Zheng, Patricia Lopez, Jason B. Human, Oleg Epstein, Ted Judd, Kelvin Sham, Qiufen Xue
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Patent number: 9775839Abstract: The invention provides certain pyrazine-2-carboxamide compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A, B, and X are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).Type: GrantFiled: March 9, 2015Date of Patent: October 3, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Michael D. Altman, Brandon Cash, John Michael Ellis, Matthew L. Maddess, Alan B. Northrup, Ryan D. Otte, Binyuan Sun
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Patent number: 9765075Abstract: Provided herein are novel substituted bridged urea and related analogs and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: May 13, 2014Date of Patent: September 19, 2017Assignee: GLAXOSMITHKLINE LLCInventors: Charles A. Blum, Richard Dana Caldwell, Rebecca Casaubon, Jeremy S. Disch, Ryan Michael Fox, Karsten Koppetsch, Pui Yee Ng, Christopher Oalmann, Robert B. Perni, Bruce G. Szczepankiewicz, Brian H. White
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Patent number: 9765054Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.Type: GrantFiled: January 23, 2012Date of Patent: September 19, 2017Assignee: CHDI Foundation, Inc.Inventors: Roland W. Bürli, Andrew J. Stott, Perla Breccia, Celia Dominguez, Ignacio Muñoz-Sanjuàn, Christopher A. Luckhurst, Samantha J. Hughes, Alan F. Haughan
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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: 9758515Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.Type: GrantFiled: December 5, 2014Date of Patent: September 12, 2017Assignee: SHIONOGI & CO., LTD.Inventors: Chika Takahashi, Hindenori Mikamiyama, Toshiyuki Akiyama, Kenji Tomita, Yoshiyuki Taoda, Makoto Kawai, Kosuke Anan, Masayoshi Miyagawa, Naoyuki Suzuki
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Patent number: 9751873Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, W, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: GrantFiled: February 18, 2016Date of Patent: September 5, 2017Assignee: Genentech, Inc.Inventors: Benjamin Fauber, Alberto Gobbi, Olivier Rene, Monique Bodil van Niel, Emanuela Gancia, Simon Gaines, Tammy Ladduwahetty, David Vesey, Stuart Ward, Paul Winship
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Patent number: 9738615Abstract: A compound that can function as a Cyclophilin D can include a structure of Formula 1 or Formula 2 or Formula 3 or Formula 4 or Formula 5 or Formula 6 or Formula 7 or Formula 8, derivative thereof, prodrug thereof, salt thereof, or stereoisomer thereof, or having any chirality at any chiral center, or tautomer, polymorph, solvate, or combination thereof, as presented herein. The Cyclophilin D inhibitors can inhibit onset or treat neurodegenerative disease, such as Alzheimer's disease, or can be used for inhibiting progression or treating diabetes.Type: GrantFiled: September 11, 2015Date of Patent: August 22, 2017Assignee: The University of KansasInventors: Shirley ShiDu Yan, Koteswara Rao Valasani
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Patent number: 9732107Abstract: This invention provides a method of preparing a ?-hematin crystal comprising a step of heating, the ?-hematin crystal obtained by such method, and a vaccine adjuvant composition containing the ?-hematin crystal. The ?-hematin crystal has a needle-like morphology, it has an average particle size of 0.6 to 1.2 ?m, and it exhibits main peaks characteristics for angles of diffraction (2?) of 7.4°, 12.2°, 21.6°, and 24.1° in an X-ray diffraction pattern obtained by powder X-ray diffractometry with Cu—K? rays (with each peak including a plus-minus 0.2° diffraction angle).Type: GrantFiled: June 4, 2014Date of Patent: August 15, 2017Assignees: Osaka University, Nippon Zenyaku Kogyo Co., Ltd.Inventors: Shizuo Akira, Ken Ishii, Cevayir Coban, Yoshikatsu Igari, Yasumasa Kano, Akina Otsuki
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Patent number: 9732093Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, L and R2 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.Type: GrantFiled: January 31, 2014Date of Patent: August 15, 2017Assignee: JANSSEN PHARMACEUTICA NVInventors: Wendy Eccles, Anne E. Fitzgerald, Michael D. Hack, Natalie A. Hawryluk, William M. Jones, John M. Keith, Paul Krawczuk, Alec D. Lebsack, Jing Liu, Neelakandha S. Mani, Kelly J. McClure, Steven P. Meduna, Mark D. Rosen
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Patent number: 9723838Abstract: Disclosed is a pyrazole amide compound of a novel structure as represented by general formula I, wherein, each substituent group is as defined in the specification. The compound of general formula I has good insecticidal activity, and can be used for pest control.Type: GrantFiled: November 24, 2014Date of Patent: August 8, 2017Assignee: Shenyang Sinochem Agrochemicals R&D Co., LTDInventors: Huibin Yang, Junwu Ying, Yuquan Song, Lin Chen, Keke Li, Xuegeng Shi, Cong Feng, Qi Huang, Xiaoxi Fan, Bin Li
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Patent number: 9708330Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease.Type: GrantFiled: January 23, 2014Date of Patent: July 18, 2017Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Zehong Wan, Yingxia Sang, Qing Zhang