Nitrogen Bonded Directly To Ring Carbon Of The Purine Ring System (e.g., Adenine, Etc.) Patents (Class 514/263.4)
  • Patent number: 10385006
    Abstract: The present invention relates to a process for the preparation of amino alcohol derivatives or salts thereof which may be used as intermediates in the preparation of HIV reverse transcriptase inhibitors, more preferably Carbovir and Abacavir. The present invention more specifically relates to a process for the preparation of (1S, 4R)-4-amino-2-cyclopentene-1-methanol of Formula IIIa.
    Type: Grant
    Filed: October 26, 2015
    Date of Patent: August 20, 2019
    Assignee: GRANULES INDIA LIMITED
    Inventors: Krishna Prasad Chigurupati, Prasad Raju Vnkv Vetukuri, Goverdhan Gilla, Rajasekhar Bhupathi
  • Patent number: 10183037
    Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.
    Type: Grant
    Filed: January 20, 2017
    Date of Patent: January 22, 2019
    Assignee: Gilead Pharmasset LLC
    Inventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
  • Patent number: 10111870
    Abstract: A method for inducing a sustained immune response in humans or animal patient suffering from human immunodeficiency virus (HIV) acquired immune deficiency syndrome (AIDS, autoimmune disease, cancer, inflammation, and neurodegenerative diseases comprises daily administration to such patients a single oral tablet, rapidly dissolving film, capsule, liquid or cream dose of an Immediate release naltrexone composition comprising between about 0.01 to about 10 mg of naltrexone. In order to provide a benefit the naltrexone must be an Immediate release composition comprising between about 0.01 and about 10 mg of naltrexone.
    Type: Grant
    Filed: February 20, 2017
    Date of Patent: October 30, 2018
    Inventors: Noreen Griffin, Fengping Shan, Nicholas Plotnikoff
  • Patent number: 10047052
    Abstract: The present invention relates to novel bisaminoquinoline compounds, pharmaceutical compositions comprising these novel compounds and methods for inhibiting autophagy in biological systems. Methods of treating cancer in patients in need using compounds and/or compositions according to the present invention alone or in combination with at least one additional anticancer agent represent additional aspects of the invention. Methods of treating disease states and/or conditions in which inhibition of autophagy plays a favorable treatment role including rheumatoid arthritis, malaria, antiphospholipid antibody syndrome, lupus, chronic urticaria and Sjogren's disease, with compounds according to the present invention represent additional aspects of the invention.
    Type: Grant
    Filed: December 20, 2016
    Date of Patent: August 14, 2018
    Assignee: The Trustees of The University of Pennsylvania
    Inventors: Ravi K. Amaravadi, Jeffrey Winkler
  • Patent number: 9725450
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
    Type: Grant
    Filed: October 21, 2015
    Date of Patent: August 8, 2017
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Steven Clareen, Veronique Plantevin-Krenitsky, Moorthy Palanki, Yoshitaka Satoh
  • Patent number: 9493501
    Abstract: Compounds having methyltransferase inhibitory activity are disclosed. The compounds have the structure and are useful in the treatment of cancer and similar diseases associated with inappropriate methyltransferase activity.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: November 15, 2016
    Assignee: Memorial Sloan-Kettering Cancer Center
    Inventors: Weihong Zheng, Minkui Luo, Glorymar del Valle Ibanez Sanchez
  • Patent number: 9457028
    Abstract: Abacavir, a nucleoside analog reverse transcriptase inhibitor, has been found to exhibit an anti-cancer activity on ATL cells in vitro without inhibiting DNA replication of normal cells. Abacavir or a pharmaceutically acceptable derivative thereof is useful as an active ingredient of a pharmaceutical composition for use in the prevention or the treatment of cancer, in particular a cancer whose DNA repair system is impaired such as breast cancer or adult T-cell leukemia.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: October 4, 2016
    Assignee: KYOTO UNIVERSITY
    Inventors: Akifumi Takaori, Shunichi Takeda, Masayuki Kobayashi, Kohei Tada
  • Patent number: 9187479
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
    Type: Grant
    Filed: March 26, 2014
    Date of Patent: November 17, 2015
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Steven Clareen, Veronique Plantevin-Krenitsky, Moorthy Palanki, Yoshitaka Satoh
  • Patent number: 9119855
    Abstract: A composition and method for the treatment of the side-effects associated with the administration of cancer chemotherapeutic agents involves the oral ingestion of a slow release capsule containing adenine. In some embodiments, the slow release capsule also contains orotate. The systemic administration of a proton pump inhibitor decreases systemic absorption of orotate, and the systemic administration of allopurinol decreases the formation of 2,8-dihydroxy adenine from adenine. In an alternative embodiment, cationic liposomes contain purine/pyrimidine precursors. The cationic liposomes bind to the cells lining the mucosa of the intestinal tract and then the contents of the cationic liposome are then taken up in the interior of the cells to prevent the metabolism of the cancer treatment drug 5-FU into a toxic species. A method for prevention of oral stomatitis and a method for treatment of dysplastic tissue are also disclosed.
    Type: Grant
    Filed: January 23, 2014
    Date of Patent: September 1, 2015
    Assignee: Asymmetric Therapeutics, LLC
    Inventor: John P. Ford
  • Patent number: 9040546
    Abstract: The present invention relates to methods of treating fibromyalgia by administering a therapeutically-effective combination-dosage of famciclovir and celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination-dosage of famciclovir and celecoxib.
    Type: Grant
    Filed: April 11, 2014
    Date of Patent: May 26, 2015
    Assignee: INNOVATIVE MED CONCEPTS, LLC
    Inventor: William L. Pridgen
  • Publication number: 20150132258
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 14, 2015
    Inventor: George D. Hartman
  • Patent number: 9029413
    Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, and in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. Antiviral activity of enzyme inhibitors is demonstrated.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: May 12, 2015
    Assignee: The Trustees of Princeton University
    Inventors: Josh Munger, Bryson Bennett, Thomas Shenk, Joshua Rabinowitz
  • Patent number: 9023857
    Abstract: The invention relates to new substituted 6-(2-aminobenzylamino)purines, represented by the general formula I, which can be used in CDK inhibition, in particular, in the treatment of viral infections and diseases involving cell proliferation. The invention further includes pharmaceutical preparations containing substituted 6-(2-aminobenzylamino)purines.
    Type: Grant
    Filed: January 22, 2010
    Date of Patent: May 5, 2015
    Assignee: Univerzita Palackeho V Olomouci
    Inventors: Libor Havlicek, Vladimir Krystof, Marek Zatloukal, Karel Dolezal, Miroslav Strnad, Borivoj Vojtesek
  • Publication number: 20150111902
    Abstract: This invention relates to methods for altering the splicing of mRNA in cells. In particular, this invention also relates to methods for increasing the ratio of wild type to misspliced forms of mRNA and corresponding encoded proteins in cells possessing a mutant gene encoding either the i) misspliced mRNA corresponding to the mutant protein or ii) a component in the splicing machinery responsible for processing the misspliced mRNA. In addition, this invention relates to treating individuals having a disorder associated with a misspliced mRNA, such as Familial Dysautonomia or Neurofibromatosis 1, by administering to such an individual a cytokinin such as kinetin.
    Type: Application
    Filed: May 19, 2014
    Publication date: April 23, 2015
    Applicant: The General Hospital Corporation
    Inventors: Susan A. Slaugenhaupt, James F. Gusella
  • Publication number: 20150111732
    Abstract: A pesticidal composition comprises a 3-(1H-pyrazol)pyridine compound of formula I or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R9, R10, R12, x, n, and Q are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Martin J. Walsh, Ann M. Buysse, Asako Kubota, Noormohamed M. Niyaz, Yu Zhang, Ricky Hunter, Tony K. Trullinger
  • Publication number: 20150111733
    Abstract: A pesticidal composition comprises at least one compound selected from a 1-(3-pyridyl-N-oxide)pyrazole compound of formula I, II, or III, or any agriculturally acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R12, R13, Y, and Q, are as described herein. A method of controlling pests comprises applying the pesticidal composition near a population of pests.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Martin J. Walsh, Daniel Knueppel, Noormohamed M. Niyaz, Ann M. Buysse, Negar Garizi, Asako Kubota, Yu Zhang, Ricky Hunter, Tony K. Trullinger
  • Patent number: 9006254
    Abstract: This invention relates to compositions, and related compounds and methods, of conjugates of immunomodulatory agents and polymers or unit(s) thereof. The conjugates may be contained within synthetic nanocarriers, and the immunomodulatory agents may be released from the synthetic nanocarriers in a pH sensitive manner.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: April 14, 2015
    Assignee: Selecta Biosciences, Inc.
    Inventors: Charles Zepp, Grayson B. Lipford, Yun Gao, Lloyd Johnston, Fen-ni Fu, Mark J. Keegan, Sam Baldwin
  • Publication number: 20150094275
    Abstract: The present invention provides novel heteroaryl compounds having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.
    Type: Application
    Filed: November 13, 2014
    Publication date: April 2, 2015
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. GRAY, Jianming ZHANG, Barun OKRAM, Xianming DENG, Jae Won CHANG, Amy WOJCIECHOWSKI
  • Patent number: 8993583
    Abstract: 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.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: March 31, 2015
    Assignee: ICOS Corporation
    Inventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg, Kamal Deep Puri
  • Patent number: 8980901
    Abstract: 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.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: March 17, 2015
    Assignee: Icos Corporation
    Inventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg, Kamal Deep Puri
  • Publication number: 20150065471
    Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 5, 2015
    Inventors: Carlos Puig Duran, Francesc Carrera Carrera, Juan Bautista Pérez Garcia, Enrique Moyes Valles, Iolanda Marchueta Hereu
  • Publication number: 20150050241
    Abstract: The present invention is directed to methods and compositions employing 9-(4-hydroxy-2-(hydroxymethyl)butyl)guanine (“H2G”) or derivatives or analogs thereof for the treatment of viral diseases, as well as for the treatment of other conditions, including, but not limited to, cancer, chronic fatigue syndrome, Alzheimer's disease, multiple sclerosis and Graves' disease. The H2G or derivative or analog thereof can be administered in a pharmaceutical composition and can be administered with an additional antiviral therapeutic agent or another agent for the treatment of other conditions.
    Type: Application
    Filed: October 30, 2014
    Publication date: February 19, 2015
    Inventors: Fred VOLINSKY, Steven Daniel DONG
  • Patent number: 8957081
    Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: February 17, 2015
    Assignee: IRM LLC
    Inventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, III, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
  • Publication number: 20150038446
    Abstract: The present disclosure relates to compositions and methods for treating retinal damage and/or retinal degradation. More specifically, this disclosure relates to methods for treating degradation of the retinal pigment epithelium by administering compositions comprising a nucleoside and/or a nucleoside or nucleotide reverse transcriptase inhibitor.
    Type: Application
    Filed: August 1, 2014
    Publication date: February 5, 2015
    Inventors: Jayakrishna Ambati, Benjamin Fowler
  • Patent number: 8946244
    Abstract: The present invention relates to 2?-Fluoro-6?-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Hepatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses.
    Type: Grant
    Filed: November 16, 2010
    Date of Patent: February 3, 2015
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: Chung K. Chu, Jianing Wang
  • Publication number: 20150031689
    Abstract: The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation.
    Type: Application
    Filed: February 15, 2013
    Publication date: January 29, 2015
    Inventors: Rangan Maitra, Alan Bradley Fulp, Yanan Zhang, Herbert H. Seltzman
  • Publication number: 20150011568
    Abstract: A method for the treatment of recurrent herpes labialis in mammals, including humans, which method comprises administering to the mammal in need of such treatment, and effective amount of penciclovir or famciclovir, or a pharmaceutically acceptable salt thereof for a period of one day.
    Type: Application
    Filed: May 6, 2014
    Publication date: January 8, 2015
    Inventors: Stephen Anthony Billstein, Robert Charnas, Spotswood Spruance
  • Publication number: 20150011488
    Abstract: Epicatechins, Epicatechin Oligomers, or Thiolated Epicatechins are applied (A) directly to a genital wart in the form of a cream, ointment, paste or solution, (B) directly to the genital wart wherein such cream, ointment, paste or solution contains as an additional active ingredient a skin permeabilizing agent, (C) following electrosurgical resection or removal of the genital wart in such form of a cream, ointment, paste or solution, (D) following chemical resection or extirpation of the genital wart in such form, (E) following surgical resection or removal of the genital wart in such form, wherein said Epicatechins, Epicatechin Oligomers, or Thiolated Epicatechins both provide antiviral activity against multiple strains of human pappilomavirus (HPV) and promote healing following resection polymers contained in a vehicle. Disclosed are the compositions, therapeutical kits containing such composition, methods of treatment using such composition, and methods of enhancing the stability of such composition.
    Type: Application
    Filed: March 10, 2014
    Publication date: January 8, 2015
    Applicant: CACAO BIO-TECHNOLOGIES, LLC
    Inventors: Daniel PRESTON, Randall B. MURPHY
  • Publication number: 20150005324
    Abstract: A method for the treatment of recurrent herpes labialis in mammals, including humans, which method comprises administering to the mammal in need of such treatment, an effective amount of penciclovir or famciclovir, or a pharmaceutically acceptable salt thereof for a period of one day.
    Type: Application
    Filed: April 14, 2014
    Publication date: January 1, 2015
    Inventors: Stephen Anthony Billstein, Robert Charnas, Spotswood Spruance
  • Publication number: 20140378480
    Abstract: The disclosure relates to methods of treating fibromyalgia, by administering a therapeutically-effective combination of an antiviral component and a COX-2 inhibitor component. The invention is further related to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and celecoxib.
    Type: Application
    Filed: February 6, 2013
    Publication date: December 25, 2014
    Applicant: INNOVATIVE MED CONCEPTS, LLC
    Inventor: William L. Pridgen
  • Patent number: 8916570
    Abstract: Disclosed are (N)-methanocarba adenine nucleosides of formulas (I)-(V), for example, of formula (V): as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides exhibit similar selectivities as agonists of the A3 versus the A1 receptor for both human and mouse adenosine receptors, and are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias.
    Type: Grant
    Filed: February 10, 2012
    Date of Patent: December 23, 2014
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Kenneth A. Jacobson, Dilip K. Tosh
  • Patent number: 8912202
    Abstract: The invention provides novel substituted cyclopropane carboxamide compounds according to Formula (I), their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.
    Type: Grant
    Filed: July 7, 2012
    Date of Patent: December 16, 2014
    Assignee: Merck Patent GmbH
    Inventors: Wolfgang Staehle, Melanie Schultz, Kai Schiemann
  • Patent number: 8901136
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: December 2, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Stephen Critchley, Courtney A. Cullis, Steven P. Langston, Hirotake Mitzutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
  • Publication number: 20140349971
    Abstract: The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection.
    Type: Application
    Filed: August 7, 2014
    Publication date: November 27, 2014
    Inventor: Paul STOFFELS
  • Publication number: 20140343006
    Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl,
    Type: Application
    Filed: August 5, 2014
    Publication date: November 20, 2014
    Inventors: Jerome Emile Georges Guillemont, Patrice Palandijian, Marc Rene DeJonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desire Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Frank Xavier Jozef Herwig Arts
  • Publication number: 20140309242
    Abstract: The present invention relates to adenine which is useful to activate AMP-activated protein kinase (AMPK) and the use of adenine in the prevention or treatment of conditions or disease and thereby prevent or treat conditions or diseases which can be ameliorated by AMPK in a mammal.
    Type: Application
    Filed: April 10, 2013
    Publication date: October 16, 2014
    Inventors: Han-Min CHEN, Cheng-Yi KUO, Chun-Fang HUANG, Jiun-Tsai LIN
  • Publication number: 20140303112
    Abstract: The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity.
    Type: Application
    Filed: April 9, 2013
    Publication date: October 9, 2014
    Inventors: Han-Min CHEN, Cheng-Yi KUO, Chun-Fang HUANG, Jiun-Tsai LIN
  • Patent number: 8841310
    Abstract: The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and/or nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection.
    Type: Grant
    Filed: October 7, 2009
    Date of Patent: September 23, 2014
    Assignee: Janssen R & D Ireland
    Inventor: Paul Stoffels
  • Publication number: 20140271826
    Abstract: The solubility of kinetin and/or of zeatin is increased when either or both are combined in a formulation that includes a polyoxyalkylene-n-glycerol dicarboxylate component and a fatty acid component. These two components provide a synergistic increase in the solubility of kinetin and/or zeatin that is greater than that which would be expected based on the solubility of kinetin and zeatin in the individual components.
    Type: Application
    Filed: March 17, 2014
    Publication date: September 18, 2014
    Applicant: Dow Pharmaceutical Sciences, Inc.
    Inventors: Pramod Sarpotdar, Sarmistha Basu, Varsha D. Bhatt, Yunik Chang, Gordon J. Dow
  • Publication number: 20140249165
    Abstract: Provided herein are methods of treatment of a cystic disease by administering a compound of Formula I. In certain embodiments, the compound for use in the methods provided herein is roscovitine or an analog thereof.
    Type: Application
    Filed: March 10, 2014
    Publication date: September 4, 2014
    Applicant: Genzyme Corporation
    Inventors: Nikolay O. BUKANOV, Oxana BESKROVNAYA
  • Publication number: 20140243359
    Abstract: The compound 2-[1-(6-aminopurin-9-yl)-2-oxoethoxy]prop-2-enal of formula (I), its monohydrate of formula (II), or its corresponding cyclic monohydrate of formula (III), in which the stereochemical chiral center indicated with an asterisk can be R (Rectus), S (Sinister) or racemic, including the tautomers of the adenine ring and the pharmaceutically acceptable salts, are used in the treatment of inflammatory disorders or of pain disorders.
    Type: Application
    Filed: July 20, 2012
    Publication date: August 28, 2014
    Applicant: MEDESTEA RESEARCH & PRODUCTION S.P.A.
    Inventors: Giulia Federica Merizzi, Fabio Grassi, Antonio Soleti
  • Publication number: 20140235562
    Abstract: A method of treating an ocular disorder in a subject includes administering to the subject a therapeutically effective amount of an agent that modulates at least one target in a signaling cascade associated with light induced retinal degeneration, aberrant all-trans-retinal accumulation, and/or generation of reactive oxygen species (ROS).
    Type: Application
    Filed: April 25, 2014
    Publication date: August 21, 2014
    Inventors: Krzysztof Palczewski, Yu Chen
  • Patent number: 8809350
    Abstract: The present invention relates to the use of an inhibitor of CDK2 and/or CDK7 and/or CDK9, or a pharmaceutically acceptable salt thereof, in the preparation of a medicament for treating a disease associated with antinuclear antibodies, wherein the inhibitor of CDK2 and/or CDK7 and/or CDK9 or pharmaceutically acceptable salt thereof is administered in an amount sufficient to down-regulate the levels of antinuclear antibodies. A further aspect of the invention relates to a combination comprising an inhibitor of CDK2 and/or CDK7 and/or CDK9, or a pharmaceutically acceptable salt thereof, and methylprednisolone, and its use in the treatment of diseases associated with antinuclear antibodies, such as SLE.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: August 19, 2014
    Assignee: Cyclacel Limited
    Inventors: Ariela Benigni, Carla Zoja, Giuseppe Remuzzi, Athos Gianella-Borradori
  • Patent number: 8809349
    Abstract: Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: August 19, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp
  • Patent number: 8809351
    Abstract: The present invention relates to methods of treating fibromyalgia, by administering a therapeutically-effective combination of an antiviral component and a COX-2 inhibitor component. The invention is further related to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and celecoxib.
    Type: Grant
    Filed: February 6, 2013
    Date of Patent: August 19, 2014
    Assignee: Innovative Med Concepts, LLC.
    Inventor: William L. Pridgen
  • Publication number: 20140228378
    Abstract: The invention provides novel substituted cyclopropane carboxamide compounds according to Formula (I), their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.
    Type: Application
    Filed: July 7, 2012
    Publication date: August 14, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Wolfgang Staehle, Melanie Schultz, Kai Schiemann
  • Publication number: 20140221399
    Abstract: The present invention relates to methods of treating fibromyalgia by administering a therapeutically-effective combination-dosage of famciclovir and celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination-dosage of famciclovir and celecoxib.
    Type: Application
    Filed: April 11, 2014
    Publication date: August 7, 2014
    Applicant: INNOVATIVE MED CONCEPTS, LLC
    Inventor: William L. Pridgen
  • Publication number: 20140221366
    Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: June 11, 2012
    Publication date: August 7, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Timo Heinrich, Nadia Brugger, Kristopher Josephson
  • Publication number: 20140213559
    Abstract: The present invention provides an inhibitor of intracellular protein degradation for use in the treatment and prevention of muscular dystrophy in a mammal. In particular, the invention provides an autophagy inhibitor and/or an inhibitor of the ubiquitin-proteasome system (such as a proteasome inhibitor) for use in the treatment and prevention of muscular dystrophy (such as congenital muscular dystrophy [e.g. MDC1A) and Duchenne muscular dystrophy [DMD]). The invention further provides corresponding methods of treatment and prevention of muscular dystrophy.
    Type: Application
    Filed: May 27, 2011
    Publication date: July 31, 2014
    Applicant: MD PHARMA AB
    Inventors: Madeleine Durbeej-Hjalt, Virginie Carmingnac
  • Publication number: 20140206697
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
    Type: Application
    Filed: March 26, 2014
    Publication date: July 24, 2014
    Applicant: Signal Pharmaceuticals, LLC
    Inventors: STEVEN CLAREEN, VERONIQUE PLANTEVIN-KRENITSKY, MOORTHY PALANKI, YOSHITAKA SATOH