Quinazoline (including Hydrogenated)(i.e., The Second Cyclo In The Bicyclo Ring System Is An Ortho-fused Six-membered Carbocycle) Patents (Class 514/266.1)
  • Patent number: 10428054
    Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: October 1, 2019
    Assignee: CHDI Foundation, Inc.
    Inventors: Leticia M. Toledo-Sherman, Celia Dominguez, Michael Prime, William Mitchell, Naomi Went
  • Patent number: 10266518
    Abstract: The present invention provides compounds of Formula I, for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.
    Type: Grant
    Filed: August 31, 2017
    Date of Patent: April 23, 2019
    Assignee: Symphony Evolution, Inc.
    Inventors: Kenneth D. Rice, Neel K. Anand, Joerg Bussenius, Simona Costanzo, Abigail R. Kennedy, Csaba J. Peto, Tsze H. Tsang, Charles M. Blazey
  • Patent number: 10251886
    Abstract: a pharmaceutical composition for preventing, treating, or ameliorating one or more symptoms of a malignant tumor associated with EGFR mutation and/or K-RAS mutation is provided. The pharmaceutical composition includes a 4-anilinoquinazoline derivative having a formula (I) where A is iodine when m is 1 and n is zero, or A is albumin when m is an integral ranging from 1 to 7 and n is 1.
    Type: Grant
    Filed: February 23, 2018
    Date of Patent: April 9, 2019
    Assignee: National Chiao Tung University
    Inventors: Jui-I Chao, Chin-Piao Chen, Kuang-Kai Liu
  • Patent number: 10035780
    Abstract: The present invention relates to novel heterocyclic compounds based on a quinazoline scaffold, which bind effectively to the mitochondrial translocator protein (TSPO), and counteract cell death processes. These compounds can also stimulate neuronal differentiation. The present invention further relates to pharmaceutical compositions including such compounds, and methods of using these compounds for the prevention and treatment of brain damage resulting from brain injury, especially secondary brain damage due to traumatic brain injury (TBI). The compounds of the invention are also useful in preventing, treating, and curing brain damage due to neurodegenerative diseases, including underlying and associated pathological and mental disorders. The compounds can also be used to prevent and treat brain damage due to infection, toxic challenges, and excessive drug use, e.g., recreational, over the counter, or prescription drugs.
    Type: Grant
    Filed: April 22, 2015
    Date of Patent: July 31, 2018
    Assignee: TECHNION RESEARCH & DEVELOPMENT FOUNDATION LTD.
    Inventors: Moshe Gavish, Jehuda Arieh Veenman, Alex Shterenberg, Ilan Marek, Alex Vainshtein, Avraham Avital
  • Patent number: 9981965
    Abstract: The present invention relates to an improved process for preparing Idelalisib (1). In this process, acid addition salts of idelalisamine (2) are useful intermediates for purification purposes.
    Type: Grant
    Filed: March 24, 2016
    Date of Patent: May 29, 2018
    Assignee: Synthon B.V.
    Inventors: Libor Vyklicky, Miroslav Zabadal
  • Patent number: 9937174
    Abstract: The invention relates to pharmaceutical combinations comprising an HDAC inhibitor and bendamustine; pharmaceutical compositions comprising the same; and methods of using such combinations and compositions for treating lymphoma in a subject in need thereof.
    Type: Grant
    Filed: December 4, 2015
    Date of Patent: April 10, 2018
    Assignee: UNIVERSITY OF MODENA AND REGGIO EMILIA
    Inventors: Samantha Pozzi, Maria Cosenza
  • Patent number: 9889134
    Abstract: Polymorphs of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine are provided herein. Processes for preparing the polymorphs and pharmaceutical composition comprising the polymorphs are also disclosed.
    Type: Grant
    Filed: October 26, 2015
    Date of Patent: February 13, 2018
    Assignee: Array BioPharma Inc.
    Inventors: Donald T. Corson, Christopher M. Lindemann, Daniel J. Watson
  • Patent number: 9822096
    Abstract: A compound of formula I wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Grant
    Filed: August 29, 2016
    Date of Patent: November 21, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: James A. Johnson, Heather Finlay, James Neels, Naveen Kumar Dhondi, Ashokkumar Adisechan
  • Patent number: 9737521
    Abstract: This present invention relates to a method of treating a autoimmune, respiratory and/or inflammatory disease or condition (e.g., psoriasis, rheumatoid arthritis, asthma, COPD). The method comprises administering a PI3K Delta inhibitor or a dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor. The present invention also relates to pharmaceutical compositions containing a PI3K Delta or dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor.
    Type: Grant
    Filed: November 7, 2013
    Date of Patent: August 22, 2017
    Assignee: Rhizen Pharmaceuticals SA
    Inventors: Swaroop K. Vakkalanka, Srikant Viswanadha
  • Patent number: 9708353
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Grant
    Filed: February 12, 2015
    Date of Patent: July 18, 2017
    Assignee: BIOGEN MA INC.
    Inventors: Richard D. Caldwell, Kevin Guckian, Gnanasambandam Kumaravel, Wen-Cherng Lee, Edward Yin-Shiang Lin, Xiaogao Liu, Bin Ma, Daniel M. Scott, Zhan Shi, Jermaine Thomas, Arthur G. Taveras, Guo Zhu Zheng
  • Patent number: 9693989
    Abstract: This invention provides compounds of Formula I wherein B, G, A, E, R1, R2, R3, m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.
    Type: Grant
    Filed: September 23, 2013
    Date of Patent: July 4, 2017
    Assignee: Array Biopharma, Inc.
    Inventors: Joseph P. Lyssikatos, Julie Marie Hicks, Fredrik P. Marmsater, Qian Zhao
  • Patent number: 9670205
    Abstract: The present disclosure relates generally to toll like receptor modulator compounds, such as diamino pyrido[3,2 D]pyrimidine compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR-8), and methods of making and using them.
    Type: Grant
    Filed: March 2, 2016
    Date of Patent: June 6, 2017
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Evangelos Aktoudianakis, Gregory Chin, Richard L. Mackman, Samuel E. Metobo, Michael R. Mish, Hyung-jung Pyun, Jeff Zablocki
  • Patent number: 9546180
    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 P13 kinase activity, are described herein.
    Type: Grant
    Filed: June 5, 2014
    Date of Patent: January 17, 2017
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
  • Patent number: 9499522
    Abstract: Compounds and compositions useful for treating disorders related to Kit are described herein.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: November 22, 2016
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Lucian V. DiPietro, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Steven Mark Wenglowsky, Douglas Wilson, Yulian Zhang
  • Patent number: 9290480
    Abstract: The present invention relates to a novel quinazoline-2,4-dione derivative of formula (I), a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising a compound of formula (I) as an active ingredient for preventing or treating neurological brain disease.
    Type: Grant
    Filed: December 11, 2012
    Date of Patent: March 22, 2016
    Assignee: Shin Poong Pharmaceuticals Co., Ltd.
    Inventors: Il Hwan Cho, Eun Bang Lee, Sin Cheol Kang, Won Seok Kim, Chul Kyu Lee
  • Patent number: 9199973
    Abstract: A pharmaceutical formulation comprising the compound of formula
    Type: Grant
    Filed: November 10, 2014
    Date of Patent: December 1, 2015
    Assignee: Novartis AG
    Inventors: Malcolm Clive Carter, George Stuart Cockerill, Karen Elizabeth Lackey
  • Patent number: 9199990
    Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
    Type: Grant
    Filed: October 14, 2014
    Date of Patent: December 1, 2015
    Assignee: Resverlogix Corp.
    Inventor: Henrik C. Hansen
  • Patent number: 9174966
    Abstract: The present invention relates to the solid state of 6-(1H-imidazol-1-yl)-2-phenylquinazoline (I) and therefore to novel crystalline forms of the base and of pharmaceutically acceptable salts and solvates thereof, and also to methods for preparing them, to the respective pharmaceutical formulations and to their therapeutic use. Compound (I) may be obtained as the free base in five different crystalline forms, three polymorphic forms and two hydrates. Some pharmaceutically acceptable salts of (I) that have physicochemical characteristics acceptable for pharmaceutical development were obtained, and the respective polymorphic forms and/or hydrates were characterized.
    Type: Grant
    Filed: June 4, 2010
    Date of Patent: November 3, 2015
    Assignee: ROTTAPHARM S.P.A.
    Inventors: Antonio Giordani, Stefano Mandelli, Francesca Porta, Matteo Ghirri, Lucio Claudio Rovati
  • Patent number: 9168254
    Abstract: Polymorphs of N4-(4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine are provided herein. Processes for preparing the polymorphs and pharmaceutical composition comprising the polymorphs are also disclosed.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: October 27, 2015
    Assignee: Array BioPharma Inc.
    Inventors: Donald T. Corson, Christopher M. Lindemann, Daniel J. Watson
  • Patent number: 9168255
    Abstract: The invention relates to aryl substituted quinazolines of Formula I, and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, A, and R1-R4 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: May 19, 2015
    Date of Patent: October 27, 2015
    Assignee: Purdue Pharma L.P.
    Inventors: R. Richard Goehring, Laykea Tafesse, Jiangchao Yao
  • Patent number: 9102629
    Abstract: The present invention relates to polymorphic forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide p-toluenesulfonate with the characteristic X-ray powder diffraction data as stated in the description, preparation methods thereof, pharmaceutical compositions comprising the same and the use thereof.
    Type: Grant
    Filed: November 18, 2014
    Date of Patent: August 11, 2015
    Assignee: SHANGHAI ALLIST PHARMACEUTICALS, INC.
    Inventors: Jianhui Guo, Yong Jiang
  • Patent number: 9066979
    Abstract: The invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof: which possess inhibitory activity against activating mutant forms of EGFR, and are accordingly useful for their anti-cancer activity and in methods of treatment of the human or animal body. The invention also relates pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: June 30, 2015
    Assignee: AstraZeneca AB
    Inventors: David Yunzhi Li, Jiabing Wang, Zhenfan Yang, Qingbei Zeng, Xiaolin Zhang
  • Patent number: 9045435
    Abstract: The invention relates to aryl substituted quinazolines of Formula I, and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, A, and R1-R4 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: June 2, 2015
    Assignee: Purdue Pharma, L.P.
    Inventors: R. Richard Goehring, Laykea Tafesse, Jiangchao Yao
  • Patent number: 9029538
    Abstract: The present application provides compounds of Formula I or salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c, Y, R3, X, E and G are as defined herein, compositions, methods of treatment and uses thereof.
    Type: Grant
    Filed: May 13, 2014
    Date of Patent: May 12, 2015
    Assignee: Ignyta, Inc.
    Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
  • Patent number: 8987285
    Abstract: The present invention relates to a novel crystalline anhydrous form of [(5-chlorothiophene-2-ylsulfonylcarbamoyl)-(4-(6-fluoro-7-(methylamino)-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)phenyl)amide, potassium salt, and its use in the treatment or prevention of a condition or a disorder with platelet ADP receptor inhibition, in particular, P2Y12 inhibition, in animals, particularly humans. It also relates processes for making such a novel crystalline form. The present invention also relates to a solid, oral formulation of this novel crystalline form, its preparation and use thereof.
    Type: Grant
    Filed: December 5, 2011
    Date of Patent: March 24, 2015
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Ulrich Meier, Nicole Bieri, Dieter Becker, Julien Taillemite, Marie-Pierre Filliot, Tanja Meister
  • Patent number: 8987284
    Abstract: Disclosed are novel quinazoline derivatives containing phosphorus substitutions and methods for the treatment of hyperproliferative diseases (e.g. cancer) using the compounds. These compounds are type I receptor protein kinase inhibitors useful in treating disorders related to abnormal protein kinase activities such as cancer and inflammation in mammals. Also disclosed are pharmaceutical compositions containing the compounds, methods for the preparation of the compounds and their pharmaceutically acceptable salts.
    Type: Grant
    Filed: July 2, 2010
    Date of Patent: March 24, 2015
    Assignee: Newgen Therapeutics, Inc.
    Inventors: Wang Shen, Aimin Zhang, Junfa Fan, Xiaoling Zheng
  • Patent number: 8946247
    Abstract: The invention provides novel quinazoline carboxamide azetidine compounds according to Formula (I) and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: November 11, 2011
    Date of Patent: February 3, 2015
    Assignee: Merck Patent GmbH
    Inventors: Bayard R. Huck, Reinaldo Jones, Yufang Xiao, Constantin Neagu, Donald Bankston, Andreas Goutopoulos
  • Patent number: 8927530
    Abstract: The present invention provides a combination comprising (a) a compound of formula (I) and (b) one or more antineoplastic agents selected from the group consisting of an antimetabolite agent, analkylating or alkylating-like agent, an intercalating agent, a topoisomerase I or II inhibitor, an antimitotic agent, a kinase inhibitor, a proteasome inhibitor and an antibody inhibiting a growth factor or its receptor, wherein active ingredients of the combination are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate or solvate thereof, useful in the treatment of tumors.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: January 6, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Barbara Valsasina, Italo Beria, Antonella Ciavolella, Dario Ballinari, Enrico Pesenti, Juergen Moll, Mara Emanuela Casnaghi, Alessandro Luciano Croci
  • Patent number: 8916572
    Abstract: Novel bis-quinazoline derivatives as tyrosine kinase inhibitors, synthesis of these compounds, and novel methods for treating tyrosine kinase mediated diseases or disorders using these compounds are disclosed. In particular, the present invention provides tethered quinazoline derivative dimers as inhibitors to the epidermal growth factor receptor (EGFR) tyrosine kinase, pharmaceutical compositions thereof, and their therapeutic uses for treating EGFR kinase-mediated diseases or disorders, such as various cancers, as well as synthetic methods for preparing these novel compounds.
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: December 23, 2014
    Assignee: Tetranov International Inc.
    Inventors: Yusheng Wu, Chengshan Niu, Dapeng Zou, Jingya Li, Ruiyun Guo
  • Patent number: 8916573
    Abstract: The invention relates to antibacterial compounds of formula (I), wherein R1 is H, halogen, (C1-C3)alkyl or (C1-C3)alkoxy; R2 is H, halogen, (C1-C3)alkyl, (C1-C3)alkoxy or pyrrolidin-1-yl; R3 is H, halogen, (C1-C3)alkyl, (C1-C3)alkoxy, vinyl or 2-methoxycarbonyvinyl or R2 and R3 together with the two carbon atoms which bear them form a phenyl ring; R4 is H, halogen, (C1-C3)alkyl or (C1-C3)alkoxy; and R5 is H, (C1-C3)alkyl or cyclopropyl, or R4 and R5form together a —CH2CH2CH2— group; A is the divalent group —CH2—, —CH2CH2—, #—CH(OH)CH2—*, #—CH2N(R6)—* and —CH2NHCH2—, wherein # indicates the point of attachment to the optionally substituted (quinazoline-2,4-dione-3-yl)methyl residue and * represents the point of attachment to the substituted (oxazolidinon-4-yl)methyl residue; R6 is H or acetyl; Y is CH or N; and Q is O or S; and salts of such compounds.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: December 23, 2014
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
  • Patent number: 8916574
    Abstract: The present invention relates to 4-(substituted anilino)-quinazoline derivatives as tyrosine kinase inhibitors. Specifically, compounds of formula I, or pharmaceutically acceptable salts or solvates thereof are disclosed, in which each substitutent in formula I is defined in the description. Preparation method of the compounds of formula I, pharmaceutical compositions and pharmaceutical uses thereof are also disclosed. The compounds of formula I are effective tyrosine kinase inhibitors.
    Type: Grant
    Filed: September 20, 2010
    Date of Patent: December 23, 2014
    Assignee: Qilu Pharmaceutical Co., Ltd.
    Inventors: Jingyi Wang, Chuanwen Fan, Long Zhang, Zhongru Guo, Ying Li, Shaobo Yang, Shousheng Yan, Jianrong Zhu, Qingmin Yang, Minghui Zhang
  • Patent number: 8916575
    Abstract: This invention relates to quinazoline derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy of disorders in which the modulation of toll-like-receptors is involved.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: December 23, 2014
    Assignee: Janssen R&D Ireland
    Inventors: David McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers, Stefaan Julien Last, Werner Embrechts, Serge Maria Aloysius Pieters
  • Patent number: 8912205
    Abstract: A pharmaceutical formulation comprising the compound of formula
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: December 16, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Malcolm Clive Carter, George Stuart Cockerill, Karen Elizabeth Lackey
  • Patent number: 8912186
    Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: December 16, 2014
    Assignee: Universitaet des Saarlandes
    Inventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
  • Publication number: 20140350024
    Abstract: The invention provides methods of treating a bacterial infection in a mammal comprising administering to the mammal a substituted bicyclic heteroaromatic ring compound of formula I: wherein two of X1 to X8 are N and the remaining of X1 to X8 are CH; or a pharmaceutically acceptable salt thereof, as well as novel compounds of formula I and salts thereof and pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: January 11, 2013
    Publication date: November 27, 2014
    Inventors: Edmond J. LaVoie, Ajit Parhi, Daniel S. Pilch, Malvika Kaul
  • Patent number: 8883808
    Abstract: Patients suffering from serotonin-mediated diseases or conditions, such as depression, may be treated by administering an effective combined amount of a 5-HT7 receptor antagonist and a serotonin reuptake inhibitor.
    Type: Grant
    Filed: October 18, 2006
    Date of Patent: November 11, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Pascal Bonaventure, Christine Dugovic, Curt A. Dvorak, Dale A. Rudolph, Jonathan Edward Shelton
  • Publication number: 20140329821
    Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: July 9, 2014
    Publication date: November 6, 2014
    Inventors: Xicheng Sun, Jian Qiu, Adam Stout
  • Publication number: 20140309190
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Application
    Filed: June 17, 2014
    Publication date: October 16, 2014
    Applicant: BIOGEN IDEC MA INC.
    Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Ma Bin, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
  • Patent number: 8835445
    Abstract: The present disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R5, R6 and Z are as described herein. The disclosure also provides pharmaceutical compositions thereof; and methods for inhibiting DHFR activity; and methods for treating cell proliferative diseases, autoimmune disease, inflammatory disease or bacterial, fungal or parasitic infection by administering a compound of Formula I.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: September 16, 2014
    Assignee: Trius Therapeutics, Inc.
    Inventors: Zhiyong Chen, Christopher J. Creighton, Mark Cunningham, John Finn, Mark Hilgers, Michael Jung, Lucy Aguirre Kohnen, Thanh Lam, Xiaoming Li, Mark Stidham, Les Tari, Michael Trzoss, Junhu Zhang
  • Patent number: 8829014
    Abstract: Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.
    Type: Grant
    Filed: June 15, 2012
    Date of Patent: September 9, 2014
    Assignees: Board of Supervisors of Louisiana State University and Agricultural and Mechanical College, B.V. Patel Pharmaceutical Education & Research Development (PERD) Centre
    Inventors: Anthony Giordano, Kamala K. Vasu, Hardik M. Thakar, Rajan S. Giri, Vasudevan Sudarsanam, Swapnil G. Yerande, Gajanan S. Inamdar
  • Patent number: 8815878
    Abstract: Substituted spiro hemiaminals and methods for their use in the treatment of viral diseases, including hepatitis C viral infections, are described herein.
    Type: Grant
    Filed: July 27, 2011
    Date of Patent: August 26, 2014
    Assignee: NovaDrug, LLC
    Inventor: Eliezer Huberman
  • Patent number: 8809354
    Abstract: Surprising antiviral activity of 3-amino-2-(4-nitrophenyl)-4-(3H)-quinazolinone (Compound 1) was reported in the treatment or prevention of viral infections, particularly in combination with other antiviral agents such as interferon and/or ribavarin.
    Type: Grant
    Filed: December 31, 2011
    Date of Patent: August 19, 2014
    Inventors: Sheikh Riazuddin, Osman Ali, Usman Ashfaq, Shaheen N. Khan, Javed Akram, Atta-ur Rahman, M. Iqbal Choudhary, Khalid M. Khan, Zulfiqar Ali Khan
  • Patent number: 8809353
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: March 18, 2008
    Date of Patent: August 19, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Dean Wilson, Lev T. D. Fanning, Paul Krenitsky, Andreas Termin, Pramod Joshi, Urvi Sheth
  • Patent number: 8802675
    Abstract: Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition.
    Type: Grant
    Filed: January 31, 2010
    Date of Patent: August 12, 2014
    Assignees: Technion Research and Development Foundation Ltd, Yeda Research and Development Company Ltd.
    Inventors: Moussa B. H. Youdim, Mati Fridkin, Hailin Zheng
  • Patent number: 8802659
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: August 12, 2014
    Assignee: Biogen Idec MA Inc.
    Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
  • Patent number: 8796180
    Abstract: The invention relates to aminoquinazoline compounds or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein A1, A2, A3, A4, R1, R2, R3, R4, R5a, R5b, R5c, R5d and p are defined as in the description.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: August 5, 2014
    Assignee: BASF SE
    Inventors: Steffen Gross, Matthias Pohlman, Arun Narine, Claudia Rosenbaum, Prashant Deshmukh, Joachim Dickhaut, Nina Gertrud Bandur, Karsten Koerber, Florian Kaiser, Wolfgang Von Deyn, Juergen Langewald, Deborah L. Culbertson, Cecille Ebuenga
  • Patent number: 8796294
    Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: August 5, 2014
    Assignee: Exelixis Patent Company LLC
    Inventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
  • Patent number: 8791129
    Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R43 and X have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: July 29, 2014
    Assignee: Merck Patent GmbH
    Inventors: Hans-Michael Eggenweiler, Christian Sirrenberg, Hans-Peter Buchstaller
  • Patent number: 8765773
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, Ra, R2a, R2b, R1, and X have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Grant
    Filed: October 14, 2011
    Date of Patent: July 1, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Dylan B. England, Kenneth M. Gigstad, Alexandra E. Gould, Liting Ma, He Xu
  • Patent number: 8754092
    Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: June 17, 2014
    Assignee: Exelixis Patent Company LLC
    Inventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang