Purine (including Hydrogenated) Patents (Class 514/263.1)
  • Patent number: 11180472
    Abstract: The present invention relates to the following compounds wherein the integers are as defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of tuberculosis.
    Type: Grant
    Filed: April 14, 2020
    Date of Patent: November 23, 2021
    Assignee: Janssen Sciences Ireland UC
    Inventors: Jérôme Émile Georges Guillemont, Magali Madeleine Simone Motte, Pierre Jean-Marie Bernard Rabiosson, Abdellah Tahri
  • Patent number: 10730872
    Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: November 3, 2016
    Date of Patent: August 4, 2020
    Assignee: Syngenta Participations AG
    Inventors: Pierre Joseph Marcel Jung, Andrew Edmunds, Michel Muehlebach, André Jeanguenat, Daniel Emery, Roger Graham Hall, Vikas Sikervar, Jagadish Pabba
  • Patent number: 10711003
    Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, and Ar are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
    Type: Grant
    Filed: October 22, 2019
    Date of Patent: July 14, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Liqi He, Sanjeev Gangwar, Shoshana L. Posy, Yam B. Poudel, Prasanna Sivaprakasam
  • Patent number: 10398695
    Abstract: 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 are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.
    Type: Grant
    Filed: May 30, 2018
    Date of Patent: September 3, 2019
    Assignee: ICOS CORPORATION
    Inventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • Patent number: 10159668
    Abstract: A composition for inhibiting ?-glucosidase has lower side effects to a user, other than the inhibition of ?-glucosidase. The composition comprises adenine, (3-hydroxy-dl-proline, nicotinic acid, (3,6-dioxo-piperazin-2-yl)-acetic acid amide, 2-ethylhexyl heptanoate, and a pharmaceutically compatible salt.
    Type: Grant
    Filed: February 12, 2018
    Date of Patent: December 25, 2018
    Assignee: TAMKANG UNIVERSITY
    Inventors: San-Lang Wang, Van-Bon Nguyen
  • Patent number: 10010550
    Abstract: 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 are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.
    Type: Grant
    Filed: May 8, 2017
    Date of Patent: July 3, 2018
    Assignee: ICOS Corporation
    Inventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • Patent number: 9487772
    Abstract: 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 are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: November 8, 2016
    Assignee: ICOS CORPORATION
    Inventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • Patent number: 9290517
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Grant
    Filed: August 19, 2013
    Date of Patent: March 22, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James M. Apgar, Ashok Arasappan, Tesfaye Biftu, Ping Chen, Danqing Feng, Erin Guidry, Jacqueline D. Hicks, Ahmet Kekec, Kenneth J. Leavitt, Bing Li, Troy McCracken, Iyassu Sebhat, Xiaoxia Qian, Lan Wei, Robert R. Wilkening, Zhicai Wu
  • Patent number: 9180097
    Abstract: The present invention provides improved formulations of 6-mercaptopurine that exhibit better bioavailability and faster dissolution than previous formulations.
    Type: Grant
    Filed: February 10, 2014
    Date of Patent: November 10, 2015
    Assignee: TEVA PHARMACEUTICAL INDUSTRIES LTD.
    Inventors: E. Itzhak Lerner, Moshe Flashner-Barak, Erwin v. Achthoven, Hans Keegstra, Ruud Smit
  • Patent number: 9034883
    Abstract: The present invention relates to certain DPP-4 inhibitors for treating and/or preventing oxidative stress, vascular stress and/or endothelial dysfunction as well as to the use of such DPP-4 inhibitors in treatment and/or prevention of diabetic or non-diabetic patients, including patient groups at risk of cardiovascular and/or renal disease.
    Type: Grant
    Filed: November 14, 2011
    Date of Patent: May 19, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thomas Klein, Andreas Daiber, Odd-Eric Johansen, Michael Mark, Sanjaykumar Patel, Hans-Juergen Woerle
  • Publication number: 20150119351
    Abstract: Methods for treating diseases in humans and vertebrate animals are provided using competitive antagonists of cellular metabolites combined with a protective agent for protecting host cells from toxic effects of the drugs. Also provided are kits comprising competitive antagonists and suitable protective agents. In addition, screening methods for identifying competitive antagonists, protective agents and potentiating agents, for use according to the methods of the invention, are provided.
    Type: Application
    Filed: August 4, 2014
    Publication date: April 30, 2015
    Inventors: Adam Lubin, Martin Lubin
  • 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
  • Patent number: 8946242
    Abstract: Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an effective amount of a spiro[2.4]heptane as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier, are provided. The spiro[2.4]heptane compounds either possess antiviral activity, or are metabolized to a compound that exhibits such activity.
    Type: Grant
    Filed: January 23, 2014
    Date of Patent: February 3, 2015
    Assignee: University of Georgia Research Foundation, Inc.
    Inventor: Chung K. Chu
  • Patent number: 8940751
    Abstract: The present disclosure relates to purine compounds of formula (I) or formula (II) or its tautomers, polymorphs, stereoisomers, solvates or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2B adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2B receptor. The present disclosure also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: January 27, 2015
    Assignee: Advinus Therapeutics Private Limited
    Inventors: Dinesh Barawkar, Sujay Basu, Vidya Ramdas, Venkata Poornapragnacharyulu Palle, Yogesh Waman, Meena Patel, Anil Panmand
  • Publication number: 20150018337
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: July 29, 2014
    Publication date: January 15, 2015
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Patent number: 8921384
    Abstract: Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an effective amount of a spiro[2.4]heptane as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier, are provided. The spiro[2.4]heptane compounds either possess antiviral activity, or are metabolized to a compound that exhibits such activity.
    Type: Grant
    Filed: January 23, 2014
    Date of Patent: December 30, 2014
    Assignee: Unversity of Georgia Research Foundation, Inc.
    Inventor: Chung K. Chu
  • Patent number: 8865731
    Abstract: Provided are: an agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), which comprises a compound having adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof as an active ingredient; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance or constipation; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance; and the like.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: October 21, 2014
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Jun Ouchi, Shunji Kunori, Yozo Kojima, Katsumi Shinoda, Katsutoshi Sasaki, Shiro Shirakura
  • Patent number: 8859566
    Abstract: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: October 14, 2014
    Assignee: Advinus Therapeutics Private Limited
    Inventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
  • Patent number: 8859490
    Abstract: Disclosed is a peptide nucleic acid monomer as well as a corresponding peptide nucleic acid molecule. The monomer comprises a terminal amino group and a terminal group A. The terminal amino group and the terminal group A are connected by an aliphatic moiety. The main chain of this aliphatic moiety is free of groups that are charged under physiological conditions. The terminal group A is one of —COOH, —COOR3, —COX, —COSR3, —CN, —CONH2, —CONHR3, —CONR3, R4, with R3 and R4 being H or an aliphatic, alicyclic, aromatic, arylaliphatic or arylalicyclic group, and X being a halogen atom. The terminal amino group is substituted by an aliphatic group with a main chain of at least two carbon atoms and optionally 0 to about 2 heteroatoms selected from the group N, O, S, Se and Si. The main chain has a polar head group Z.
    Type: Grant
    Filed: September 3, 2008
    Date of Patent: October 14, 2014
    Assignee: Nanyang Technological University
    Inventors: Chuan Fa Liu, Yun Zeng, Xiao Wei Lu
  • 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: 8853222
    Abstract: Anti-herpetic material such as 2-aminopurine derivatives, e.g., the aminocyclopropylcarboxylate derivatives of acyclovir, penciclovir, and ganciclovir, are described to prevent or treat autoimmune disease or a disease originating from an abnormal functioning of the sympathetic chain in a human subject. Prolonged use of the anti-herpetic compounds reduces prodrome, vesicle formation and viral shedding. The anti-herpetic compounds may be administered alone or in combination with a compound that reduces the rate of renal excretion of the anti-herpetic compound. The anti-herpetic compounds are particularly useful when administered at a level equivalent in activity to at—least about 150 mg/kg famciclovir per day.
    Type: Grant
    Filed: March 6, 2009
    Date of Patent: October 7, 2014
    Inventor: Ray W. Exley
  • Publication number: 20140296261
    Abstract: The invention provides a compound represented by formula (I) which may modulate a kinase, and a pharmaceutical composition thereof, as well as the method for preventing or treating a protein kinase mediated disease or condition.
    Type: Application
    Filed: November 14, 2012
    Publication date: October 2, 2014
    Applicants: CENTAURUS BIOPHARMA CO., LTD., CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD,
    Inventors: Dengming Xiao, Jijun Li, Yan Zhu, Yuandong Hu, Huting Wang, Zhe Wang, Zanping Wang, Yongheng Wei, Yinghui Sun, Qiong Wu, Hui Zhang, Yong Peng, Fansheng Kong, Ying Sun, Hong Luo, Yongxin Han
  • Patent number: 8835444
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF) receptor antagonists Formula (I).
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: September 16, 2014
    Assignee: Novartis AG
    Inventors: David Beattie, Ian Bruce, Anny-Odile Colson, Andrew James Culshaw, Thomas Sharp
  • Publication number: 20140256668
    Abstract: The present disclosure relates to compounds of formula (I-A) using the compounds wherein Ring A and the variables X, Y, R3a, R3b, R3c, R3d, R4, R5, R5?, and m are defined herein, to pharmaceutical compositions comprising the compounds, and methods of using the compounds.
    Type: Application
    Filed: May 23, 2013
    Publication date: September 11, 2014
    Applicant: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Stephen CRITCHLEY, Thomas G. Gant, Steven P. Langston, Edward J. Olhava, Stephane Peluso
  • Publication number: 20140128390
    Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and mutant c-kit protein kinases.
    Type: Application
    Filed: September 5, 2013
    Publication date: May 8, 2014
    Inventors: JACK LIN, JOHN BUELL, KATRINA CHAN, TODD EWING, PRABHA IBRAHIM, MARIKA NESPI, PHUONGLY PHAM, SONGYUAN SHI, WAYNE SPEVAK, GUOXIAN WU, JIAZHONG ZHANG, YING ZHANG
  • Publication number: 20140128408
    Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
    Type: Application
    Filed: January 31, 2012
    Publication date: May 8, 2014
    Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Alan Kozikowski, Jay H. Kalin, Kyle V. Butier, Joel Bergman, Wayne W. Hancock
  • Patent number: 8680108
    Abstract: The present invention provides fused aryl and heteroaryl derivatives of Formula I: wherein X, V, Y, U, W, Z, R1, R2, Cy, and Ar are defined herein, 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: December 17, 2010
    Date of Patent: March 25, 2014
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, Andrew P. Combs, Eddy W. Yue, Hui-Yin Li
  • Patent number: 8673926
    Abstract: Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an effective amount of a spiro[2.4]heptane as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier, are provided. The spiro[2.4]heptane compounds either possess antiviral activity, or are metabolized to a compound that exhibits such activity.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: March 18, 2014
    Assignee: University of Georgia Research Foundation, Inc.
    Inventor: Chung K. Chu
  • Patent number: 8653088
    Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable salt or mixtures thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK mammalian protein kinase, and more particularly inhibitors of GSK-3 mammalian protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.
    Type: Grant
    Filed: September 1, 2009
    Date of Patent: February 18, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jeremy Green, Ronald Grey, Jr., Albert Pierce
  • Patent number: 8653060
    Abstract: The present invention provides improved formulations of 6-mercaptopurine that exhibit better bioavailability and faster dissolution than previous formulations.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: February 18, 2014
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: E. Itzhak Lerner, Moshe Flashner-Barak, Erwin v Achthoven, Hans Keegstra, Ruud Smit
  • Patent number: 8648086
    Abstract: The present invention provides 5,6-bicyclic heteroaryl-containing urea compounds of Formula I or II and use of the same for treating conditions mediated by protein kinase such as VEGFR2, c-Met, PDGFR? c-Kit, CSF1R, or EphA2.
    Type: Grant
    Filed: August 20, 2010
    Date of Patent: February 11, 2014
    Assignee: Ascepion Pharmaceuticals, Inc.
    Inventors: Shan Jiang, Xinglong Xing, Qishan Wang, Ren Kong
  • Patent number: 8637496
    Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.
    Type: Grant
    Filed: June 2, 2008
    Date of Patent: January 28, 2014
    Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche Scientifique
    Inventors: Anne-Laure Bonneau, Cyrille Botte, Michael Deligny, Nadia Saidani, Hélène Hardre, Bernard Rousseau, Roman Lopez, Eric Marechal
  • Patent number: 8629151
    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: May 26, 2010
    Date of Patent: January 14, 2014
    Assignee: Selecta Biosciences, Inc.
    Inventors: Charles Zepp, Grayson B. Lipford, Yun Gao, Lloyd Johnston, Fen-ni Fu, Mark J. Keegan, Sam Baldwin
  • Patent number: 8623881
    Abstract: 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 are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.
    Type: Grant
    Filed: October 7, 2009
    Date of Patent: January 7, 2014
    Assignee: ICOS Corporation
    Inventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • Publication number: 20130338094
    Abstract: The present disclosure relates to compounds of formula (I-A) using the compounds wherein Ring A and the variables X, Y, R3a, R3b, R3c, R3d, R4, R5, R5?, and m are defined herein, to pharmaceutical compositions comprising the compounds, and methods of using the compounds.
    Type: Application
    Filed: May 23, 2013
    Publication date: December 19, 2013
    Applicant: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Stephen CRITCHLEY, Thomas G. Gant, Steven P. Langston, Edward J. Olhava, Stephane Peluso
  • Publication number: 20130310403
    Abstract: The present invention relates to a fluoro-homoneplanocin A, its nucleoside derivative, and synthetic methods. The novel fluoro-homoneplanocin A and its nucleoside derivative in the present invention have an effect on cancer prevention or treatment, and therefore can be used as anticancer drugs.
    Type: Application
    Filed: April 11, 2013
    Publication date: November 21, 2013
    Applicant: EWHA UNIVERSITY - INDUSTRY COLABORATION FOUNDATION
    Inventor: EWHA UNIVERSITY - INDUSTRY COLLABORATION FOUNDATION
  • Patent number: 8546406
    Abstract: Compounds of the formula I, in which D, X, Y, Z, R and R1 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumors.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: October 1, 2013
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Frank Zenke, Mireille Krier, Kai Schiemann
  • Patent number: 8501724
    Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: August 6, 2013
    Assignee: Pharmacyclics, Inc.
    Inventors: Wei Chen, David J. Loury
  • Patent number: 8501749
    Abstract: Disclosed are small molecule inhibitors of the formula (I), which are useful in treating various diseases and conditions involving chymase.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: August 6, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Xin Guo, Chuk Chui Man, Hidenori Takahashi
  • Patent number: 8492389
    Abstract: 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 are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.
    Type: Grant
    Filed: October 7, 2009
    Date of Patent: July 23, 2013
    Assignee: ICOS Corporation
    Inventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • Publication number: 20130183278
    Abstract: The present invention relates to method of identifying whether or not an individual has Parkinson's disease (PD). In particular, the invention relates to a method for identifying whether or not an individual has PD as opposed to another neurodegenerative disease. The method of the invention comprises measuring the concentration of ?-synuclein (?-syn) and the concentration of unphosphorylated tau (tau) and/or phosphorylated tau (p-tau) in a cerebrospinal fluid sample taken from an individual. The method also comprises calculating the ratio of the concentration of tau and/or p-tau to the concentration of ?-syn, and thereby determining whether or not the individual has PD.
    Type: Application
    Filed: July 6, 2011
    Publication date: July 18, 2013
    Applicant: United Arab Emirates University
    Inventors: Omar El-Agnaf, Lucilla Parnetti, Paolo Calabresi
  • Patent number: 8450330
    Abstract: A pharmaceutical acceptable composition is provided. The composition comprises an effective amount of a non-steroidal anti-inflammatory drug (NSAID), a local anesthetic, and an antiviral drug.
    Type: Grant
    Filed: August 28, 2008
    Date of Patent: May 28, 2013
    Assignee: Yung Shin Pharmaceutical Industrial Co., Ltd.
    Inventors: Fangchen Lee, Hui-Ling Shieh, Chiung-Ju Tsai, Shin-Hong Jang
  • Patent number: 8426396
    Abstract: The present application provides, inter alia, methods of treating disorders mediated by FGFRs and methods of screening for Hsp90 inhibitor compounds.
    Type: Grant
    Filed: January 8, 2009
    Date of Patent: April 23, 2013
    Assignee: Shriners Hospitals for Children
    Inventors: William A. Horton, Melanie B. Laederich
  • Publication number: 20130096104
    Abstract: The invention provides compounds of Formulas Ia-Ib, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4, R5 and R16 are defined herein, a pharmaceutical composition that includes a compound of Formulas Ia-Ib and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy, as an inhibitor of TYK2 kinase and conditions related, such as inflammatory illnesses, inflammatory bowel disease or psoriasis.
    Type: Application
    Filed: March 15, 2011
    Publication date: April 18, 2013
    Applicant: GENENTECH, INC.
    Inventors: Yingjie Lai, Jun Liang, Steven R. Magnuson, Kirk D. Robarge, Vickie H. Tsui, Birong Zhang, Aihe Zhou
  • Patent number: 8404805
    Abstract: The presently disclosed subject matter discloses characterization of interactions between ligands and Hsp90 proteins, including GRP94, wherein ligand binding to the N-terminal nucleotide binding domain of GRP94 elicits a conformational change that converts the GRP94 from an inactive to an active conformation, and wherein the chaperone and peptide-binding activities of the GRP94 are markedly stimulated. Also disclosed are purification, screening, and therapeutic methods pertaining to the biological activity of GRP94, and in some instances HSP90, based upon the characterization of ligand interactions of Hsp90 peptide-binding proteins, including GRP94.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: March 26, 2013
    Assignee: Duke University
    Inventors: Christopher V. Nicchitta, James J. Wassenberg, Meredith F. N. Rosser, Robyn C. Reed
  • Publication number: 20130035325
    Abstract: Methods of inhibiting kinases using kinase inhibitors having olefin moieties are disclosed.
    Type: Application
    Filed: November 16, 2010
    Publication date: February 7, 2013
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: John William Taunton, JR., Rebecca Maglathlin, Iana Serafimova, Michael S. Cohen, Rand Miller, Ville Paavilainen, Jesse McFarland, Shyam Krishnan
  • Patent number: 8357691
    Abstract: This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated. In particular, the disclosure provides for substituted purine compounds having the general formula their salts, pharmaceutical compositions, and methods of treatment using the subject compounds and compositions.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: January 22, 2013
    Assignee: Spelman College
    Inventor: Leyte L. Winfield
  • Publication number: 20120316185
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF) receptor antagonists Formula (I).
    Type: Application
    Filed: January 31, 2011
    Publication date: December 13, 2012
    Applicant: NOVARTIS AG
    Inventors: David Beattie, Ian Bruce, Anny-Odile Colson, Andrew James Culshaw, Thomas Sharp
  • Patent number: 8329070
    Abstract: The present invention provides apparatus and processes for producing liposomes. By providing a buffer solution in a first reservoir, and a lipid solution in a second reservoir, continuously diluting the lipid solution with the buffer solution in a mixing chamber produces a liposome. The lipid solution preferably comprises an organic solvent, such as a lower alkanol.
    Type: Grant
    Filed: December 10, 2010
    Date of Patent: December 11, 2012
    Assignee: Protiva Biotherapeutics, Inc.
    Inventors: Ian MacLachlan, Lloyd Jeffs, Lorne R. Palmer, Cory Giesbrecht, Noelle Giesbrecht, legal representative
  • Patent number: 8304419
    Abstract: The present invention relates to compounds that are a non-nucleoside reverse transcriptase inhibitors, and to processes for the preparation and use of the same. Specifically, the present invention includes methods of using such compounds in the treatment of human immunodeficiency virus infection.
    Type: Grant
    Filed: June 5, 2008
    Date of Patent: November 6, 2012
    Assignee: GlaxoSmithKline LLC
    Inventors: Pek Yoke Chong, Andrew James Peat, Paul Richard Sebahar, Michael Youngman, Huichang Zhang