Bicyclo Ring System Having The 1,3-diazine As One Of The Cyclos Patents (Class 514/258.1)
  • Patent number: 10259805
    Abstract: The present invention relates to a process for preparation of crystalline Form 1 of gefitinib of formula (1) characterized by a XRPD powder diffraction pattern comprising, inter alia, peaks at about 7.14, 11.26, 14.25, 15.86, 24.33 and 26.40 degrees 2 theta (±0.2 degrees 2 theta), the process comprising the steps: 1. Dissolving gefitinib in a solvent mixture comprising water and an alcohol selected form ethanol and butanol, wherein the ratio between water and alcohol is between 1:16 and 1:25 (vol:vol) 2. Isolating gefitinib Form 1.
    Type: Grant
    Filed: December 22, 2016
    Date of Patent: April 16, 2019
    Assignee: Synthon B.V.
    Inventors: Petr Melsa, Radomir Skoumal
  • Patent number: 10172818
    Abstract: In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of reducing or preventing small dense LDL (“sdLDL”) oxidation in a subject, the method comprising administering to the subject a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof.
    Type: Grant
    Filed: June 16, 2015
    Date of Patent: January 8, 2019
    Assignee: Amarin Pharmaceuticals Ireland Limited
    Inventor: Richard Preston Mason
  • Patent number: 10125140
    Abstract: Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, 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: July 16, 2018
    Date of Patent: November 13, 2018
    Assignee: Pharmacyclics LLC
    Inventors: Norbert Purro, Mark S. Smyth, Erick Goldman, David D. Wirth
  • Patent number: 10045979
    Abstract: The present invention relates to novel anthelmintic compounds of formula (I) below: wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X1, X6, X8, Q1, Q2, Q3, Q4, Q5, Q6, Ring A, Ring B, W, W?, R2, R3, R, R?, m, n and q are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.
    Type: Grant
    Filed: May 19, 2015
    Date of Patent: August 14, 2018
    Assignee: MERIAL INC.
    Inventors: Alan Long, Srinivas Reddy Gurrala
  • Patent number: 10029990
    Abstract: The invention relates to medicine and can be used for treating a range of diseases in the treatment of which interferon is used. The agent for inducing endogenous interferon is comprised of the compound 6-(3-methoxycarbonyl phenyl) amino-2,4 (1H, 3H)-pyrimidinedione C12H11N3O4 of general formula: (I). The preparation exhibits greater activity both when injected and when administered orally.
    Type: Grant
    Filed: October 10, 2011
    Date of Patent: July 24, 2018
    Inventors: Viktor Veniaminovich Tets, Georgy Viktorovich Tets, Viktor Iosifovich Krutikov
  • Patent number: 9937177
    Abstract: The invention provides a compound of formula I: wherein X, Y, Z have any of the values defined in the specification or a salt thereof. The compound is useful as anti-cancer agents. The invention also provides processes and intermediates disclosed herein that are useful for preparing a compound of formula I or a salt thereof.
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: April 10, 2018
    Assignee: University of Iowa Research Foundation
    Inventor: Leonard R. MacGillivray
  • Patent number: 9493469
    Abstract: The present invention relates to new piperidine inhibitors of Janus kinase 3 activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: January 14, 2015
    Date of Patent: November 15, 2016
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Tadimeti Rao, Chengzhi Zhang
  • Patent number: 9487540
    Abstract: The compound “2-((4-nitrophenyl)amino)-6,7,8,9-tetrahydro-3H-cyclohepta[4,5]thieno-[2,3-d]pyrimidin-4(5H)-one” and method of synthesizing it, wherein the compound is effective to inhibit the growth and proliferation of human liver cancer cells HepG2. The compound has an inhibitory concentration value (IC50) of 0.7 ?g, compared to reference medication Doxorubicin that has an (IC50) value of 1.2 ?g. It further surpasses that reference medication Doxorubicin at all tested concentraions. The method includes the steps of: preparing a first compound of cycloheptanone, ethylcyanoacetate, sulfur, ethanol and diethyl amine; preparing a second compound by heating of the first compound with excess of hydrazine hydrate in absolute ethanol as solvent; and preparing the effective compound of the invention by reaction of the second chemical compound with 4-nitrophenylisothiocyanate in dry dimethylformamide as solvent.
    Type: Grant
    Filed: March 25, 2015
    Date of Patent: November 8, 2016
    Inventor: Zainab Saeed Alghamdi
  • Patent number: 9422298
    Abstract: The invention provides novel substituted pyridopyrimidines represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of the phosphoinositide 3? OH kinase family (PI3K) for the treatment of inflammatory diseases, cancer, cardiovascular diseases, allergy, asthma and autoimmune disorders.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: August 23, 2016
    Assignees: CMG Pharmaceutical Co., Ltd., Sung Kwang Medical Foundation
    Inventors: Gilnam Lee, Chul Soo Lim, Han Won Cho, Jeongbeob Seo, Albert C. Gyorkos, Suk Young Cho, Eun Kyung Choi, Choung Soo Kim, Jung Jin Hwang, Jin Sung Kim, Hee Jung An, Yong Wha Moon
  • Patent number: 9382241
    Abstract: The invention provides novel compounds having the general formula: wherein A, R1, R2 and R3 are as defined herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: July 5, 2016
    Assignee: Genentech, Inc.
    Inventors: Huifen Chen, Terry Crawford, Seth F. Harris, Steven R. Magnuson, Chudi Ndubaku, Lan Wang
  • Patent number: 9346805
    Abstract: The present invention provides compounds of Formula I including tautomers, resolved enantiomers, resolved diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as Akt protein kinase inhibitors and for the treatment of Akt-mediated diseases, for example, hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: November 14, 2012
    Date of Patent: May 24, 2016
    Assignee: ARRAY BIOPHARMA INC.
    Inventors: Anna Banka, Josef R. Bencsik, James F. Blake, Kin Chiu Fong, Martin F. Hentemann, Ian S. Mitchell, Douglas McCord Sammond, Tony P. Tang, Eli M. Wallace, Rui Xu, James Graham
  • Patent number: 9301528
    Abstract: A synergistic antimicrobial composition containing lenacil and one of 4,5-dichloro-2-n-octyl-4-isothiazolin-3-one or 2-n-octyl-4-isothiazolin-3-one is provided. Also provided is a method of inhibiting the growth of or controlling the growth of microorganisms in a building material by adding such a synergistic antimicrobial composition. Also provided is a coating composition containing such a synergistic antimicrobial composition, and a dry film made from such a coating composition.
    Type: Grant
    Filed: November 29, 2013
    Date of Patent: April 5, 2016
    Assignees: Rohm and Haas Company, Dow Global Technologies LLC
    Inventors: Kenneth M. Donnelly, Pierre Marie Alain Lenoir, Lukas Thomas Johannes Villiger
  • Patent number: 9266841
    Abstract: Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atherosclerosis.
    Type: Grant
    Filed: October 24, 2014
    Date of Patent: February 23, 2016
    Assignee: Glaxo Group Limited
    Inventors: Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith, Steven James Stanway
  • Patent number: 9216960
    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: November 24, 2014
    Date of Patent: December 22, 2015
    Assignee: University of Georgia Research Foundation, Inc.
    Inventor: Chung K. Chu
  • Patent number: 9193741
    Abstract: The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with RNA-viruses belonging to the family of the Retroviridae, the family of the Flaviviridae and the family of the Picornaviridae and more preferably infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: November 24, 2015
    Assignee: Katholieke Universiteit Leuven, K. U. Leuven R&D
    Inventors: Steven De Jonghe, Ling-Jie Gao, Piet Herdewijn, Jean Herman, Miyeon Jang, Pieter Leyssen, Thierry Louat, Johan Neyts, Christophe Pannecouque, Bart Vanderhoydonck
  • Patent number: 9174995
    Abstract: Compounds of the formula I in which X, R1 and Y have the meanings indicated in claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
    Type: Grant
    Filed: April 6, 2013
    Date of Patent: November 3, 2015
    Assignee: MERCK PATENT GMBH
    Inventors: Dieter Dorsch, Hans-Peter Buchstaller
  • Patent number: 9156845
    Abstract: The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and R5 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: October 13, 2015
    Assignee: Pfizer Inc.
    Inventors: Paul Galatsis, Matthew Merrill Hayward, Bethany Lyn Kormos, Travis T. Wager, Lei Zhang, Antonia Friederike Stepan, Jaclyn Louise Henderson, Ravi G. Kurumbail, Patrick Robert Verhoest
  • Patent number: 9155742
    Abstract: There is provided pyrimidinyl compounds of Formula (I), wherein: R2 is or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: February 26, 2015
    Date of Patent: October 13, 2015
    Assignee: AstraZeneca AB
    Inventors: Kevin Michael Foote, Johannes Wilhelmus Maria Nissink, Paul Turner
  • Patent number: 9029383
    Abstract: Methods for treating and/or preventing skin ulcers are provided featuring administration of pharmaceutical compositions comprising inhibitors of activity or expression Of Lp-PLA2 protein to patients subject to or at risk of developing skin ulcers.
    Type: Grant
    Filed: May 9, 2008
    Date of Patent: May 12, 2015
    Assignee: The Trustees Of The University of Pennsylvania
    Inventors: Robert Wilensky, Damir Hamamdzic, Harrilla Profka
  • Publication number: 20150126513
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Christine Hiu-Tung Chen, Donovan Noel Chin, Lucian V. DiPietro, Jianmei Fan, Mark G. Palermo, Michael David Shultz, Bakary-Barry Toure
  • Publication number: 20150119362
    Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.
    Type: Application
    Filed: October 24, 2013
    Publication date: April 30, 2015
    Inventors: Mark E. Gurney, Timothy J. Hagen, Joel R. Walker, Xuesheng Mo, A. Samuel Vellekoop, Robert Campbell, Lei Zhu, Donna L. Romero
  • Patent number: 9018218
    Abstract: The invention relates to substituted pyrimidine ammonia compounds. The structure of the compounds is represented as the general formula (I): The groups are as defined as specification. The compound represented by formula (I) can be used in the prevention of plants diseases caused by a plurality of pathogenic bacteria such as oomycota, basidiomycota, ascomycota, and fungi imperfecti, and due to these compounds have good bioactivity, which make them have very good effects at very low doses, especially more effective to powdery mildew of wheat. Therefore, the present invention relates to the use of the compounds having general formula I as fungicides, both in agriculture and other fields.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: April 28, 2015
    Assignees: Sinochem Corporation, Shenyang Research Institute of Chemical Industry Co., Ltd.
    Inventors: Changling Liu, Baoshan Chai, Zhinian Li, Xufeng Sun, Zhonggang Shan
  • Patent number: 9012462
    Abstract: The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: May 21, 2009
    Date of Patent: April 21, 2015
    Assignee: Ariad Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Wei-Sheng Huang, Shuangying Liu, William C. Shakespeare, R. Mathew Thomas, Jiwei Qi, Feng Li, Xiaotian Zhu, Anna Kohlman, David C. Dalgarno, Jan Antoinette C. Romero, Dong Zou
  • Publication number: 20150105407
    Abstract: The present invention provides substituted pyrrolo-, furano-, and cyclopentylpyrimidine bicyclic compounds of Formula III, and Formula IV, and pharmaceutically acceptable salts, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds and pharmaceutical compositions for treating tumor cells and inhibiting mitosis of cancerous cells.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventor: Aleem Gangjee
  • Patent number: 9006251
    Abstract: Aminoquinazolinyl compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.
    Type: Grant
    Filed: June 24, 2014
    Date of Patent: April 14, 2015
    Assignee: Janssen Pharamceutica NV
    Inventors: Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
  • Patent number: 8999984
    Abstract: Methods of inhibiting one or more biological activities of Macrophage migration inhibitory factor (MIF) polypeptides are provided using an MIF inhibitory compound. The methods include therapeutic methods for treating cancers and inflammatory diseases.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: April 7, 2015
    Assignee: University of Louisville Research Foundation, Inc.
    Inventors: Robert A. Mitchell, John O. Trent, Jason B. Meier
  • Patent number: 8999997
    Abstract: There is provided pyrimidinyl compounds of Formula (I), wherein: R2 is or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: September 18, 2013
    Date of Patent: April 7, 2015
    Assignee: AstraZeneca AB
    Inventors: Kevin Foote, Johannes Wilhelmus Maria Nissink, Paul Turner
  • Patent number: 8993579
    Abstract: There is provided a crystalline form of Lapatinib, termed APO-I, and methods for making APO-I. There is also provided a crystalline solvate form of Lapatinib, termed APO-II, and methods for making APO-II.
    Type: Grant
    Filed: April 21, 2011
    Date of Patent: March 31, 2015
    Assignee: Apotex Pharmachem Inc
    Inventors: Carlos Zetina-Rocha, Eduardo Gustavo Cammisa, Gamini Weeratunga
  • Patent number: 8962633
    Abstract: The present invention provides compostions and methods useful for treating and preventing metabolic bone diseases and disorders by inhibition of Lp-PLA2. The compositions and methods are useful for treating and preventing metabolic bone diseases and disorders such as, for example osteoporosis, osteopenia and osteopenia related diseases and abnormal bone marrow.
    Type: Grant
    Filed: May 12, 2008
    Date of Patent: February 24, 2015
    Assignee: Thomas Jefferson University
    Inventors: Yi Shi, Theresa Freeman
  • Publication number: 20150045375
    Abstract: Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atherosclerosis.
    Type: Application
    Filed: October 24, 2014
    Publication date: February 12, 2015
    Inventors: Deirdre Mary Bernadette HICKEY, Robert John IFE, Colin Andrew LEACH, Ivan Leo PINTO, Stephen Allan SMITH, Steven James STANWAY
  • Publication number: 20150031709
    Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
    Type: Application
    Filed: February 8, 2013
    Publication date: January 29, 2015
    Applicant: SUNOVION PHARMACEUTICALS, INC.
    Inventors: John Emmerson Campbell, Una Campbell, Taleen G. Hanania, Liming Shao
  • Patent number: 8940893
    Abstract: The present invention encompasses compounds of the formula (I) wherein the groups X and Cy are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: January 27, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Todd Bosanac, Darren Disalvo, Joshua Courtney Horan, Shuang Liang, Renee M. Zindell
  • Publication number: 20150025070
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: January 22, 2015
    Applicant: Novartis AG
    Inventors: Atwood Kim Cheung, Donovan Noel Chin, Jianmei Fan, Karen Marie Miller-Moslin, Michael David Shultz, Troy D. Smith, Ronald Charles Tomlinson, Bakary-Barry Toure, Michael Scott Visser
  • Patent number: 8937074
    Abstract: The invention provides a method of enhancing the action of a pharmaceutical agent selected from the group consisting of the anti-infective agents, the group comprising of the antimicrobial agents, the anthelmintic agents and the anti-ectoparasitic agents, but excluding coal tar solution and H1-antagonist antihistamines, and from the group consisting of the CPNS agents selected from the group of compounds acting on the central or peripheral nervous system, but excluding coal tar solution and H1-antagonist antihistamines and also excluding anti-inflammatory, analgesic and antipyretic agents and also provides an enhanced method for the administration of a nucleic acid substance to the cells of an animal, a plant or a micro-organism.
    Type: Grant
    Filed: December 10, 2012
    Date of Patent: January 20, 2015
    Assignee: North West University
    Inventor: Petrus Johannes Meyer
  • Patent number: 8933084
    Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
    Type: Grant
    Filed: May 13, 2011
    Date of Patent: January 13, 2015
    Assignee: Array BioPharma Inc.
    Inventors: Steven Wade Andrews, Kevin Ronald Condroski, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Jeongbeob Seo, HongWoon Yang, Qian Zhao
  • Patent number: 8921369
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Grant
    Filed: December 2, 2009
    Date of Patent: December 30, 2014
    Assignee: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Patent number: 8916161
    Abstract: The present invention provides a method of treating BPH using modified pore-forming proteins (MPPs). These MPPs are derived from naturally occurring cytotoxic proteins (nPPs) that kill cells by forming pores or channels in the cell membrane, resulting in cell death. The MPPs are generated by modification of the nPPs such that they are capable of being selectively activated at normal prostate cells. Such modification may include the addition of a prostate-specific protease cleavage site to the activation sequence, and/or the addition of a prostate-specific targeting domain to allow selective targeting of prostate cells. These MPPs are capable of selectively targeting and killing normal prostate cells in vivo. The MPPs may be used either alone or in combination with other therapies for the treatment of BPH.
    Type: Grant
    Filed: June 14, 2006
    Date of Patent: December 23, 2014
    Assignee: Sophiris Bio Inc.
    Inventor: James Thomas Buckley
  • Patent number: 8907086
    Abstract: The present invention is directed to novel bicyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: March 1, 2012
    Date of Patent: December 9, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Chad E. Bennett, Duane A. Burnett, Hongmei Li, Yonggang Chen, Troy McCracken, Monica Vicarel
  • Patent number: 8901133
    Abstract: Compounds and pharmaceutical compositions 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 PI3 kinase activity, are described herein.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: December 2, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
  • Patent number: 8901132
    Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: December 2, 2014
    Assignee: Katholieke Universiteit Leuven, K.U. Leuven R&D
    Inventors: Piet Herdewijn, Steven De Jonghe, Ling-Jie Gao, Mi-Yeon Jang, Bart Vanderhoydonck, Mark Jozef Albert Waer, Yuan Lin, Jean Ferdinand Herman, Thierry Andre Michel Louat
  • Patent number: 8895566
    Abstract: Compounds of Formula I are useful for inhibiting AKT protein kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Grant
    Filed: November 15, 2012
    Date of Patent: November 25, 2014
    Assignees: Array Biopharma Inc., Genetech, Inc.
    Inventors: Anna Banka, Josef R. Bencsik, James F. Blake, Martin F. Hentemann, Nicholas C. Kallan, Jun Liang, Ian S. Mitchell, Stephen T. Schlachter, Eli M. Wallace, Rui Xu, Tony P. Tang
  • Patent number: 8883800
    Abstract: The present invention relates to substituted quinazolines of formula (I): wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: November 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Markus Frank, Thomas Klein
  • Publication number: 20140323435
    Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, R6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.
    Type: Application
    Filed: May 22, 2014
    Publication date: October 30, 2014
    Applicants: Cancer Research Technology Limited, Cephalon, Inc.
    Inventors: Bruce D. Dorsey, Keith S. Learn, Emma L. Morris, Gregory R. Ott, Jonathan R.A. Roffey, Christelle N. Soudy, Jason C. Wagner
  • 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: 8859567
    Abstract: The present invention relates to 1.5 hydrate of of 1-{(2S)-2-amino-4-[2,4-bis(trifluoromethyl)-5,8-dihydropyrido[3,4-d]pyrimidin-7(6H)-yl]-4-oxobutyl}-5,5-difluoropiperidin-2-one tartrate, a process for preparing the same, and a pharmaceutical composition for inhibiting DPP-IV, which comprises said compound as the active component.
    Type: Grant
    Filed: October 31, 2011
    Date of Patent: October 14, 2014
    Assignee: LG Life Sciences Ltd.
    Inventors: Ki Sook Park, Jung Min Yun, Bong Chan Kim, Kyu Young Kim, Ji Hye Lee
  • Patent number: 8859562
    Abstract: The present invention relates to the use of an agent that inhibits the activity of an enzyme that mediates repair of a DNA strand break in the manufacture of a medicament for the treatment of diseases caused by a defect in a gene that mediates homologous recombination.
    Type: Grant
    Filed: July 23, 2004
    Date of Patent: October 14, 2014
    Assignee: The University of Sheffield
    Inventor: Thomas Helleday
  • Publication number: 20140303188
    Abstract: The present invention provides substituted cyclopenta and cyclopentyl pyrimidine bicyclic compounds of Formula III, and 5,6-saturated and unsaturated and pharmaceutically acceptable salts, prodrugs, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.
    Type: Application
    Filed: April 3, 2014
    Publication date: October 9, 2014
    Applicant: DUQUESNE UNIVERSITY OF THE HOLY SPIRIT
    Inventor: Aleem Gangjee
  • Publication number: 20140275021
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables R1, R2, R3, and R4 are as defined herein.
    Type: Application
    Filed: December 6, 2013
    Publication date: September 18, 2014
    Inventors: Jean-Damien Charrier, Chris Davis, Steven Durrant, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Michael O'Donnell, Francoise Pierard, Joanne Pinder, Pierre-Henri Storck, Heather Twin
  • Patent number: 8829006
    Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2, R3 and R4 are defined as mentioned in the description, the tautomers thereof, the isomers thereof, the diastereomers thereof, the enantiomers thereof, the hydrates thereof, the mixtures thereof and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Grant
    Filed: November 21, 2008
    Date of Patent: September 9, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Schaenzle, Dirk Stenkamp