Adenosine Or Derivative Patents (Class 514/46)
  • Patent number: 10639326
    Abstract: Provided herein are formulations for topical and/or transdermal administration, and methods of using these formulations for the treatment of proliferative diseases related to cancer such as cancers and related conditions, and solid tumors. Also provided are formulations for topical and/or transdermal administration, and methods of using these formulations for melasma, gout, skin disorders, and other diseases and disorders described herein as well as methods for modulating the pH (e.g. raising) of a tissue or microenvironment proximal to a tumor, modulating pH, or improving the effectiveness of know chemotherapeutic agents, immunotherapy and the like for the prevention, treatment of cancers and related conditions described herein.
    Type: Grant
    Filed: August 20, 2019
    Date of Patent: May 5, 2020
    Assignee: AMPERSAND BIOPHARMACEUTICALS, INC.
    Inventor: Ryan Beal
  • Patent number: 10584104
    Abstract: The present invention relates to the pharmaceutical field for the treatment of hyperuricemia and gout. In particular, the present invention relates to a carboxylic acid urate transporter 1 (URAT1) inhibitor of a general formula (I) containing a diarylmethane structure and a preparation method thereof, and a pharmaceutical composition containing the same and a use thereof in the preparation of medicaments for treating hyperuricemia and gout, wherein R1 is selected from H, C1-C10 alkyl, C3-C10 cycloalkyl, F, Cl, Br, I, CN, NO2, SR4 or OR4; R2 is selected from H, F, Cl, Br or I; R3 is selected from H or C1-C4 alkyl; X is selected from S or CH2; wherein R4 is selected from C1-C10 alkyl.
    Type: Grant
    Filed: April 28, 2016
    Date of Patent: March 10, 2020
    Assignee: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCH CO., LTD.
    Inventors: Guilong Zhao, Wei Liu, Qian Shang, Zhixing Zhou, Yuli Wang, Yuquan Li, Haizhi Zhang, Chuan Li, Changying Liu, Yuqiang Liu, Yafei Xie, Jingwei Wu, Huihui Chen, Weiren Xu, Lida Tang
  • Patent number: 10525074
    Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase DOT1L and one or more therapeutic agents, particularly anticancer agents, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.
    Type: Grant
    Filed: August 26, 2016
    Date of Patent: January 7, 2020
    Assignee: Epizyme, Inc.
    Inventors: Christine Klaus, Maria Alejandra Raimondi, Scott R. Daigle, Roy MacFarlane Pollock
  • Patent number: 10508308
    Abstract: Described herein are compositions and methods for diagnosing or monitoring type 1 diabetes.
    Type: Grant
    Filed: October 16, 2017
    Date of Patent: December 17, 2019
    Assignee: L2 Disgnostics, LLC
    Inventor: Sahar Usmani-Brown
  • Patent number: 10441541
    Abstract: The invention provides methods and compositions for treating or inhibiting the development of osteoarthritis in a subject having osteoarthritis or at risk for developing osteoarthritis and for stimulating or increasing cartilage production or formation in a subject. The methods feature administering to the subject a therapeutically effective amount of a composition comprising one or more agent from among adenosine, an adenosine receptor agonist, and an agent that upregulates or increases the amount of or the biological activity of adenosine, or an analog or derivative thereof. The adenosine receptor may be an A1, A2A, A2B and A3 adenosine receptor. The agent that upregulates or increases the amount of or the biological activity of adenosine may be dipyridamole or ticagrelor. The composition may be administered via intraarticular injection such as injection into the synovial fluid of a joint.
    Type: Grant
    Filed: September 12, 2016
    Date of Patent: October 15, 2019
    Assignee: New York University
    Inventors: Bruce N. Cronstein, Carmen Corciulo
  • Patent number: 10400005
    Abstract: The present invention relates to substituted purine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: June 23, 2017
    Date of Patent: September 3, 2019
    Assignee: Epizyme, Inc.
    Inventor: Nigel J. Waters
  • Patent number: 10369166
    Abstract: The present invention provides compounds and pharmaceutical compositions adapted to reduce a load of an RNA virus by at least 50%, the virus causing a pathogenic disease in a mammalian subject, the compound adapted to inhibit the formation of S-adenosyl methionine (SAM) in the virus, the compound being a DOTIL inhibitor, wherein the compound has a molecular weight of less than 1000, and a therapeutic index (TI=LD.sub.50:ED.sub.50) greater than 30 in the mammalian subject.
    Type: Grant
    Filed: September 20, 2015
    Date of Patent: August 6, 2019
    Inventor: Susan Eve Vecht-Lifshitz
  • Patent number: 10358458
    Abstract: The application discloses compounds of Formula I wherein the variable substituents are as defined herein. The compounds of Formula I and pharmaceutical compositions comprising compounds of Formula I are useful for the treatment of diseases mediated by RSV.
    Type: Grant
    Filed: September 25, 2015
    Date of Patent: July 23, 2019
    Assignee: RIBOSCIENCE LLC
    Inventors: Mark Smith, Klaus G. Klumpp
  • Patent number: 10351536
    Abstract: Novel crystalline forms of lesinurad and its sodium salt, processes for their preparation, pharmaceutical compositions comprising these new forms, and use of them for treating or delaying progression or onset of diseases or disorders related to activity of uric acid transporter 1 (URAT1) proteins are disclosed. These novel forms were characterized by X-ray powder diffraction, differential scanning calorimetry, and other techniques. They can be readily prepared and are suitable for preparation of solid dosage forms owing to their ease of handling and superior pharmacological properties.
    Type: Grant
    Filed: November 20, 2014
    Date of Patent: July 16, 2019
    Assignees: Crystal Pharmatech Co., Ltd., Suzhou Pengxu Pharmatech Co., Ltd.
    Inventors: Minhua Chen, Yanfeng Zhang, Chaohui Yang, Xiaoyu Zhang, Peng Wang, Pixu Li
  • Patent number: 10350231
    Abstract: 2-Chloro-2?-deoxyadenosine, hereinafter referred to as cladribine, or a pharmaceutically acceptable salt thereof may be used in the treatment or amelioration of neuromyelitis optica, hereinafter referred to as NMO e.g. in patients known to have NMO-IgG seropositivity or in patients optic neuritis, myelitis and at least two of MRI evidence of contiguous spinal cord lesion 3 or more segments in length, onset brain MRI nondiagnostic for multiple sclerosis or NMO-IgG seropositivity.
    Type: Grant
    Filed: January 27, 2015
    Date of Patent: July 16, 2019
    Assignee: Chord Therapeutics S.a.r.l.
    Inventors: Arthur Henry Roach, Konrad Rejdak
  • Patent number: 10287268
    Abstract: The present disclosure provides imidazolyl compounds of Formula (I) and methods of preparing the compounds. The provided compounds are able to bind protein kinases and may be useful in modulating (e.g., inhibiting) the activity of a protein kinase in a subject or cell and/or in treating or preventing a disease (e.g., proliferative disease, genetic disease, hematological disease, neurological disease, painful condition, psychiatric disorder, or metabolic disorder) in a subject in need thereof. Also provided are pharmaceutical compositions, kits, methods, and uses that include or involve a compound described herein.
    Type: Grant
    Filed: July 21, 2015
    Date of Patent: May 14, 2019
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Hwan Geun Choi, Yanke Liang
  • Patent number: 10262107
    Abstract: A system includes a substance to be consumed by a subject and one or more indicia labeling the substance with: genomic biomarkers; drug exposure and clinical response variability; risk for adverse events; genotype-specific dosing; polymorphic drug target and disposition genes; and treatment based on the biomarker.
    Type: Grant
    Filed: April 4, 2016
    Date of Patent: April 16, 2019
    Inventor: Bao Tran
  • Patent number: 10143704
    Abstract: The present invention relates to DOT1L inhibitors. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: November 13, 2014
    Date of Patent: December 4, 2018
    Assignee: Epizyme, Inc.
    Inventors: Roy M. Pollock, Scott R. Daigle, Eric Hedrick, Nigel Waters, Blythe Thomson
  • Patent number: 10117890
    Abstract: Methods for treating pain such as fibromyalgia, comprising administering to a subject in need thereof an effective amount of an adenosine analog, wherein the adenosine analog may be a compound of Formula (I): (I), or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions comprising the adenosine analog for use in treating pain (e.g., fibromyalgia), optionally further comprising Substance P (SP), are also provided.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: November 6, 2018
    Assignee: Academia Sinica
    Inventors: Chih-Cheng Chen, Yun-Lian Lin, Jim-Min Fang, Yijuang Chern, Chia-Ching John Lin, Wei-Nan Chen, Chun-Jung Lin
  • Patent number: 10100077
    Abstract: 6-aryl-9-glycosidpurines of general formula I and pharmaceutically acceptable salts thereof with alkali metals, ammonia, amines, or addition salts with acids, wherein Gly represents ?-D-arabinofuranosyl or ?-D-2?-deoxyribofuranosyl, Ar represents benzyl or furfuryl, each of which can be unsubstituted or substituted by one or more, preferably one to three, substituents selected from the group comprising hydroxyl, alkyl, halogen, alkoxy, amino, mercapto, carboxyl, cyano, amido, sulfo, sulfamido, acyl, acylamino, acyloxy, alkylamino, dialkylamino, alkylmercapto, trifluoromethyl, trifluoromethoxy, for use as antisenescent and UV protective compounds in animals.
    Type: Grant
    Filed: September 14, 2015
    Date of Patent: October 16, 2018
    Assignee: UNIVERZITA PALACKEHO V OLOMOUCI
    Inventors: Karel Dolezal, Lucie Plihalova, Hana Vylicilova, Marek Zatloukal, Ondrej Plihal, Jiri Voller, Miroslav Strnad, Magdalena Bryksova, Jitka Vostalova, Alena Rajnochova Svobodova, Jitka Ulrichova, Lukas Spichal
  • Patent number: 10081633
    Abstract: The present invention relates to novel adenine based inhibitors of adenylyl cyclase of the formula: wherein X, L, R1, R2, R5 are those defined herein. Compounds of the present invention are useful to treat cardiovascular diseases. The present invention also relates to a method of preventing heart failure by administering an effective amount of compound according to the invention following vascular injury and reperfusion therapy.
    Type: Grant
    Filed: June 19, 2017
    Date of Patent: September 25, 2018
    Inventors: Daniel E. Levy, Patricio Abarzúa
  • Patent number: 9932302
    Abstract: The present disclosure provides compounds, compositions, and methods for use of the compounds. The compounds are N-phenyl or N-benzyl enaminones. The compositions can be pharmaceutical compositions. For example, the compounds/compositions are used in treating seizure disorders. The methods entail administering a composition comprising one or more of the compounds to a subject in need thereof. Articles of manufacture comprising one or more of the compounds/compositions are also provided.
    Type: Grant
    Filed: October 21, 2014
    Date of Patent: April 3, 2018
    Assignee: University of Maryland Eastern Shore
    Inventors: Patrice L. Jackson-Ayotunde, Tawes Harper
  • Patent number: 9925151
    Abstract: The present invention relates to the use of multiple doses of Cladribine combined with beta interferon for the treatment of multiple sclerosis in patients who are refractory to at least one conventional therapy.
    Type: Grant
    Filed: May 23, 2007
    Date of Patent: March 27, 2018
    Assignee: MERCK SERONO SA
    Inventors: H. James Brentzel, Jr., Maria Lopez-Bresnahan, Nazih Ammoury
  • Patent number: 9862743
    Abstract: Disclosed herein are nucleosides, nucleotides and nucleotide analogs, methods of synthesizing the same and methods of treating diseases and/or conditions such as a Picornavirus and/or Flaviviridae infection with one or more nucleosides, nucleotides and nucleotide analogs.
    Type: Grant
    Filed: October 9, 2014
    Date of Patent: January 9, 2018
    Assignee: Alios BioPharma, Inc.
    Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith, Marija Prhavc, Christian Andreas Jekle, Jerome Deval
  • Patent number: 9771360
    Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for preparation thereof, to the use thereof, alone or in combinations, for the treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: March 18, 2015
    Date of Patent: September 26, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Alexandros Vakalopoulos, Philipp Buchgraber, Niels Lindner, Markus Follmann, Frank Wunder, Johannes-Peter Stasch, Tobias Marquardt, Gorden Redlich, Lisa Dietz, Volkhart Min-Jian Li
  • Patent number: 9738679
    Abstract: The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning calorimetry profile, as well as a unique crystalline structure.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: August 22, 2017
    Assignee: Epizyme, Inc.
    Inventor: Edward James Olhava
  • Patent number: 9738630
    Abstract: There are disclosed compounds that are inhibitors of EZH2, pharmaceutical compositions containing said compounds and methods of treating hyperproliferative, inflammatory, infectious, and immunoregulatory disorders and diseases, utilizing the compounds of the invention.
    Type: Grant
    Filed: November 18, 2014
    Date of Patent: August 22, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kyoung S. Kim, Liping Zhang, Ashok Vinayak Purandare, Steven P. Seitz
  • Patent number: 9597348
    Abstract: The present invention relates to methods of treating disorders in which DOT1L-mediated protein methylation plays a part, such as cancer, by administering DOT1L inhibitor compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: September 6, 2013
    Date of Patent: March 21, 2017
    Assignee: Epizyme, Inc.
    Inventors: Edward J. Olhava, Richard Chesworth, Kevin W. Kuntz, Victoria M. Richon, Roy M. Pollock, Scott Richard Daigle
  • Patent number: 9580457
    Abstract: The present invention relates to a novel process for the preparation of (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl)-6-aminopurin-2-yl}pyrazole-4-yl)-N-methylcarboxamide.
    Type: Grant
    Filed: October 28, 2013
    Date of Patent: February 28, 2017
    Assignee: Biophore India Pharmaceuticals PVT. Ltd.
    Inventors: Manik Reddy Pullagurla, Jagadeesh Babu Rangisetty, Mecheril Valsan Nandakumar
  • Patent number: 9562041
    Abstract: This invention relates to novel substituted benzamides according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
    Type: Grant
    Filed: May 15, 2013
    Date of Patent: February 7, 2017
    Assignee: GlaxoSmithKline LLC
    Inventors: Joelle Lorraine Burgess, Steven David Knight
  • Patent number: 9556237
    Abstract: The invention entails synthetic short peptides based on Rift Valley Fever Virus (RVFV) fusion protein. The peptides are broad-spectrum antivirals, and are useful for prophylactic treatment against or therapeutic treatment of infection by hemorrhagic fever viruses, such as RVFV, Ebola Virus, and Andes Virus, as well as vesicular stomatitis virus.
    Type: Grant
    Filed: June 4, 2015
    Date of Patent: January 31, 2017
    Assignee: The United States of America, as represented by the Secretary of the Army, on behalf of the U.S. Army Medical Research Institute of Infectious Diseases
    Inventors: Connie Schmaljohn, Robert F. Garry, Jeffrey W. Koehler, Mary Guttieri
  • Patent number: 9534202
    Abstract: The described invention provides methods and regimens for treating adverse consequences of a persistent and progressive myocardial injury-due to a vascular insufficiency that occurs early or late in a subject in need thereof, and progressive myocardial injury-preventing compositions that contain a chemotactic hematopoietic stem cell product, and, optionally, an additional active agent.
    Type: Grant
    Filed: October 31, 2011
    Date of Patent: January 3, 2017
    Assignee: Amorcyte, Inc.
    Inventors: Andrew L. Pecora, Robert A. Preti
  • Patent number: 9526707
    Abstract: Disclosed herein are ribonucleotide reductase inhibitors, compositions comprising ribonucleotide reductase inhibitors, and methods for treating and/or preventing autoimmune diseases and neuroinflammatory diseases with the ribonucleotide reductase inhibitors.
    Type: Grant
    Filed: August 13, 2008
    Date of Patent: December 27, 2016
    Inventor: Howard L. Elford
  • Patent number: 9492468
    Abstract: The present disclosure provides methods and compositions for treating acute heart failure, by administering to a subject in need thereof a therapeutically effective amount of an AICA riboside analog or a pharmaceutically acceptable salt or prodrug thereof.
    Type: Grant
    Filed: October 2, 2009
    Date of Patent: November 15, 2016
    Assignee: PERICOR THERAPEUTICS, INC.
    Inventor: Richard R. Stover
  • Patent number: 9446064
    Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase DOT1L and one or more therapeutic agents, particularly anticancer agents, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: September 20, 2016
    Assignee: Epizyme, Inc.
    Inventors: Christine Klaus, Maria Alejandra Raimondi, Scott R. Daigle, Roy MacFarlane Pollock
  • Patent number: 9441006
    Abstract: The invention relates to a compound which is, 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine, which is a selective A2A adenosine receptor agonist in myocardial imaging. The new polymorph of 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine (designated as polymorph E) is characterized by an X-ray diffraction pattern of X-RPD showing the following reflections at 2 Theta=5.8°, 12.3°, 15.9°, 17.3°, 20.5°, 22.6°, 23.6°, 27.7°, and 29.2°; and further characterized by a DSC scan showing marked endotherm in the range of 258 to 264° C.; and further characterized by a specific IR spectra.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: September 13, 2016
    Assignee: Farmak, a.s.
    Inventors: Lubomir Kvapil, Pavel Hradil, Martin Grepl, Petr Slezar, Barbora Dvorakova
  • Patent number: 9414901
    Abstract: Drug eluting stents (DES) useful for the treatment of restenosis are described. The stents comprise biocompatible polymers and adenosine receptor modulators.
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: August 16, 2016
    Assignee: Indiana University Research and Technology Corporation
    Inventors: Michael Sturek, Kinam Park
  • Patent number: 9403847
    Abstract: The present invention provides fused derivatives of Formula I: that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Grant
    Filed: May 29, 2014
    Date of Patent: August 2, 2016
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Andrew P. Combs, Yun-Long Li, Eddy W. Yue, Richard B. Sparks
  • Patent number: 9303057
    Abstract: The present invention is provides isolated riboswitches with FRET pairs for distinguishing changes in regulatory interactions controlled by the expression platform domain found in riboswitches. The invention further provides methods of using those riboswitches to detect structural changes in the expression platform domain and to identify potential antibiotics.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: April 5, 2016
    Assignees: CORNELL UNIVERSITY, LEOPOLD-FRANZENS UNIVERSITAT INNSBRUCK
    Inventors: Scott C. Blanchard, Ronald Micura, Andrea Haller
  • Patent number: 9295627
    Abstract: The present invention has an object to provide a mouthwash composition for preventing and/or treating periodontal diseases safely and effectively. The present invention solves the above object by providing a mouthwash composition for preventing and/or treating periodontal diseases, characterized in that it comprises, as an effective ingredient(s), one or more members selected from the group consisting of adenosine N1-oxide, 3?-glucosyladenosine N1-oxide, 5?-glucosyladenosine N1-oxide, 5?-adenosine diphosphate N1-oxide, and 5?-adenosine triphosphate N1-oxide but does not contain any saccharide assimilable by periodontal disease bacteria.
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: March 29, 2016
    Assignee: HAYASHIBARA CO., LTD.
    Inventors: Keizo Kohno, Emiko Ohashi, Tsunetaka Ohta
  • Patent number: 9295423
    Abstract: A system and method for assisting in a determination of one or more maladies associated with a human voice anatomy utilizes voice information acquired over at least two temporally displaced acquisitions. Acquired voice samples, including plural vowel sounds, are digitized and passed through one or more bandpass filters to isolate one or more frequency ranges. Curve fitting of acquired data is completed in accordance with a plurality of parameter weights applied in either a time domain or frequency domain model of the voice. This process is repeated a second, later time, for the same human, and the same process is completed for the subsequently-acquired voice information. A difference between the curve information in the respective data sets is analyzed relative to the weights, and corresponding changes are correlated to maladies of various areas of the human voice anatomy.
    Type: Grant
    Filed: April 3, 2013
    Date of Patent: March 29, 2016
    Assignee: Toshiba America Electronic Components, Inc.
    Inventor: Rakesh Sethi
  • Patent number: 9289383
    Abstract: Provided herein is a method of reducing intraocular pressure (IOP) in humans using N6-cyclopentyladenosine (CPA), CPA derivatives or prodrugs or enhanced cornea permeability formulations of CPA. In one embodiment, the invention is directed to CPA derivatives or prodrugs that are permeable to the cornea. In another embodiment, the invention is directed to uses of certain compounds in human subjects for reducing and/or controlling elevated or abnormally fluctuating IOPs in the treatment of glaucoma or ocular hypertension (OHT).
    Type: Grant
    Filed: November 24, 2014
    Date of Patent: March 22, 2016
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Norman N. Kim, William K. McVicar, Thomas G. McCauley, Prakash Jagtap
  • Patent number: 9289445
    Abstract: The invention provides methods, compositions, and kits featuring a ribonucleoside chain terminator for use in preventing or inhibiting a retrovirus infection.
    Type: Grant
    Filed: October 4, 2011
    Date of Patent: March 22, 2016
    Assignee: University of Rochester
    Inventor: Baek Kim
  • Patent number: 9289446
    Abstract: A myocardial imaging method that is accomplished by administering one or more adenosine A2A adenosine receptor agonist to a human undergoing myocardial imaging as well as pharmaceutical compositions comprising at least one A2a receptor agonist, at least one liquid carrier, and at least one co-solvent.
    Type: Grant
    Filed: November 4, 2014
    Date of Patent: March 22, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Luiz Belardinelli, Mitchell Rosner
  • Patent number: 9254289
    Abstract: The present invention discloses methods for treating eye disorders. The methods include the step of administering an effective amount of a topically-administered dipyridamole. Preferably, the topically-administered dipyridamole is formulated as a solution. Preferably, the topically-administered dipyridamole is at least one agent selected from the group consisting of: dipyridamole, and a pharmaceutically-acceptable salt thereof. Preferably, the effective amount corresponds to a concentration of at least about 10?5 molarity. Preferably, the effective amount is based on a treatment administration of at least once every other day.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: February 9, 2016
    Assignee: REMEDEYE INC.
    Inventor: Moshe Rogosnitzky
  • Patent number: 9199102
    Abstract: The present invention relates to compositions and methods for modulating melanin production, secretion and/or accumulation in human skin cells. In particular, the present invention relates to the use of A3 adenosine receptor antagonists in compositions and methods for the treatment and amelioration of hyper-pigmentation conditions and for the lightening of skin, and to the use of A3 adenosine receptor agonists in compositions and methods for the treatment and amelioration of hypo-pigmentation conditions and for the tanning of skin.
    Type: Grant
    Filed: July 20, 2010
    Date of Patent: December 1, 2015
    Assignee: ORADIN PHARMACEUTICAL LTD.
    Inventors: Lea Levana Madi, Rafi Korenstein
  • Patent number: 9175032
    Abstract: The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: November 3, 2015
    Assignee: Epizyme, Inc.
    Inventor: Edward James Olhava
  • Patent number: 9163057
    Abstract: The present invention provides a method of myocardial perfusion imaging using reduced doses of (1-{9-[(4S,2R,3R,5R)3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: October 20, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Luiz Belardinelli, Brent K. Blackburn, Zhenhai Gao
  • Patent number: 9096634
    Abstract: The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: October 16, 2013
    Date of Patent: August 4, 2015
    Assignee: Epizyme, Inc.
    Inventors: Edward J. Olhava, Richard Chesworth, Kevin W. Kuntz, Victoria M. Richon, Roy M. Pollock, Scott R. Daigle
  • Patent number: 9085601
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
    Type: Grant
    Filed: August 19, 2013
    Date of Patent: July 21, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Jeff Zablocki, Elfatih Elzein, Robert Seemayer, Travis Lemons
  • Patent number: 9045519
    Abstract: The present disclosure provides a process for the preparation of 2-adenosine N-pyrazole compounds exemplified by the structure shown below that are potent and selective agonists for A2A adenosine receptor, compositions comprising these compounds, and methods for using these compound to stimulate mammalian coronary vasodilatation for imaging the heart.
    Type: Grant
    Filed: September 6, 2013
    Date of Patent: June 2, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle, Luiz Belardinelli
  • Patent number: 9040073
    Abstract: The invention provides formulations comprising adenosine in a silk fibroin-based, sustained-release delivery system. The formulations provide sustained, focal release of adenosine at therapeutic levels for the treatment of epilepsy and/or the prevention of epileptogenesis.
    Type: Grant
    Filed: May 15, 2009
    Date of Patent: May 26, 2015
    Assignee: Trustees of Tufts College
    Inventors: Detlev Boison, David L. Kaplan
  • Patent number: 9040498
    Abstract: The present invention relates to novel 1,2,3-triazolyl purine derivatives. The invention also relates to using the derivatives to treat cancer and various viral infections.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: May 26, 2015
    Assignee: Research Foundation of the City University of New York
    Inventor: Mahesh K. Lakshman
  • Patent number: RE47301
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
    Type: Grant
    Filed: July 19, 2017
    Date of Patent: March 19, 2019
    Assignee: Gilead Sciences, Inc.
    Inventors: Jeff Zablocki, Elfatih Elzein, Robert Seemayer, Travis Lemons
  • Patent number: RE47351
    Abstract: N-pyrazole substituted 2-adenosine compounds and methods for using the compounds as A2A-adenosine receptor agonists useful to stimulate mammalian coronary vasodilation for therapeutic purposes and as adjuncts in cardiological imaging.
    Type: Grant
    Filed: June 27, 2017
    Date of Patent: April 16, 2019
    Assignee: Gilead Sciences, Inc.
    Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle, Luiz Belardinelli