Polycyclo Ring System Which Contains The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/211.09)
  • Patent number: 11583538
    Abstract: The present invention provides compounds of Formula I: wherein X, R1, R2, R3 and R4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the TREX1 protein and thus can be used as medicaments for treating or preventing disorders affected by the inhibition of TREX1.
    Type: Grant
    Filed: October 6, 2020
    Date of Patent: February 21, 2023
    Assignee: VENENUM BIODESIGN, LLC
    Inventors: Jeffrey J. Letourneau, Kiruthika Selvarangan Elamparuthi, Chia-Yu Huang, Venugopalareddy Bommireddy Venkata
  • Patent number: 11306098
    Abstract: The present invention provides compounds of Formula I wherein X, R1, R2, R3 and R4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the TREX1 protein and thus can be used as medicaments for treating or preventing disorders affected by the inhibition of TREX1.
    Type: Grant
    Filed: March 25, 2020
    Date of Patent: April 19, 2022
    Assignee: Venenum Biodesign, LLC
    Inventors: Jeffrey J. Letourneau, Kiruthika Selvarangan Elamparuthi, Chia-Yu Huang, Venugopalareddy Bommireddy Venkata
  • Patent number: 11224601
    Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
    Type: Grant
    Filed: September 23, 2020
    Date of Patent: January 18, 2022
    Assignee: AMGEN INC.
    Inventors: Paul E. Harrington, Kate Ashton, Sean P. Brown, Matthew R. Kaller, Todd J. Kohn, Brian Alan Lanman, Kexue Li, Yunxiao Li, Jonathan D. Low, Ana Elena Minatti, Alexander J. Pickrell, Markian M. Stec, Joshua Taygerly
  • Patent number: 11103489
    Abstract: There is provided a drug for preventing or treating inflammatory bowel disease, comprising as an active ingredient an RXR agonist which is a compound represented by Formula (1). In Formula (1), it is preferred that: R1 is an alkyl group; R2 is an alkyl group; W is NR3, and R3 is an alkyl group; X1 is CH; Y1 is N; X2 and Y2 are CH; and Z is a carboxyl group. Thus, a drug capable of strongly preventing or treating inflammatory bowel disease while suppressing the onset of side effects is provided.
    Type: Grant
    Filed: June 29, 2016
    Date of Patent: August 31, 2021
    Assignee: NATIONAL UNIVERSITY CORPORATION OKAYAMA UNIVERSITY
    Inventor: Hiroki Kakuta
  • Patent number: 11098048
    Abstract: Compounds of formula (I) wherein R1, R2, A, W, m, n, p and q are as described herein, compositions including the compounds and methods of using the compounds as autotaxin inhibitors.
    Type: Grant
    Filed: March 23, 2020
    Date of Patent: August 24, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Patrick Di Giorgio, Jerome Hert, Daniel Hunziker, Holger Kuehne, Patrizio Mattei, Markus Rudolph
  • Patent number: 11067580
    Abstract: Low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations for modifying biomolecules is provided. Compositions, methods, and kits relating to low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations are also provided.
    Type: Grant
    Filed: April 1, 2020
    Date of Patent: July 20, 2021
    Assignee: Life Technologies Corporation
    Inventors: Kyle Gee, Upinder Singh, Scott Grecian, Scott Clarke
  • Patent number: 11013747
    Abstract: Dosage forms containing nefopam, nefopam metabolite, nefopam prodrug, isomers thereof or combinations of the foregoing, optionally an acid, and optionally an opioid analgesic and/or NSAID, and associated methods for treating various types of pain in patients.
    Type: Grant
    Filed: June 25, 2020
    Date of Patent: May 25, 2021
    Inventor: Shahin Fatholahi
  • Patent number: 10821115
    Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
    Type: Grant
    Filed: February 6, 2020
    Date of Patent: November 3, 2020
    Assignee: AMGEN INC.
    Inventors: Paul E. Harrington, Kate Ashton, Sean P. Brown, Matthew R. Kaller, Todd J. Kohn, Brian Alan Lanman, Kexue Li, Yunxiao Li, Jonathan D. Low, Ana Elena Minatti, Alexander J. Pickrell, Markian M. Stec, Joshua Taygerly
  • Patent number: 10654857
    Abstract: Compounds of formula (I) wherein R1, R2, A, W, m, n, p and q are as described herein, compositions including the compounds and methods of using the compounds as autotaxin inhibitors.
    Type: Grant
    Filed: December 19, 2018
    Date of Patent: May 19, 2020
    Assignee: Hoffman-La Roche Inc.
    Inventors: Patrick Di Giorgio, Jerome Hert, Daniel Hunziker, Holger Kuehne, Patrizio Mattei, Markus Rudolph
  • Patent number: 10632128
    Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
    Type: Grant
    Filed: August 22, 2019
    Date of Patent: April 28, 2020
    Assignee: AMGEN INC.
    Inventors: Paul E. Harrington, Kate Ashton, Sean P. Brown, Matthew R. Kaller, Todd J. Kohn, Brian Alan Lanman, Kexue Li, Yunxiao Li, Jonathan D. Low, Ana Elena Minatti, Alexander J. Pickrell, Markian M. Stec, Joshua Taygerly
  • Patent number: 10556896
    Abstract: The present invention relates to novel crystalline forms of compound (I), (3-Amino-oxetan-3-ylmethyl)-[2-(5,5-dioxo-5,6,7,9-tetrahydro-5lambda*6*-thia-8-aza-benzocyclohepten-8-yl)-6-methyl-quinazolin-4-yl]-amine and pharmaceutical compositions comprising the crystalline forms thereof disclosed herein, which may be used for the treatment or prophylaxis of a viral disease in a patient relating to respiratory syncytial virus (RSV) infection or a disease caused by RSV infection.
    Type: Grant
    Filed: August 8, 2018
    Date of Patent: February 11, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Wei Zhang, Lin Wang, Wei Li
  • Patent number: 10500213
    Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
    Type: Grant
    Filed: March 11, 2019
    Date of Patent: December 10, 2019
    Assignee: AMGEN INC.
    Inventors: Sean P. Brown, Kexue Li, Yunxiao Li, Markian M. Stec
  • Patent number: 10494352
    Abstract: The present invention relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: September 18, 2018
    Date of Patent: December 3, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin
  • Patent number: 10450284
    Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: December 14, 2018
    Date of Patent: October 22, 2019
    Assignee: Forma Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin
  • Patent number: 10442776
    Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: December 13, 2018
    Date of Patent: October 15, 2019
    Assignee: Forma Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Heather Davis, Aleksandra Rudnitskaya, David R. Lancia, Jr., Kenneth W. Bair, David S. Millan, Matthew W. Martin
  • Patent number: 10428109
    Abstract: The present invention relates to a process for the preparation of certain 1,5-benzothiazepine compounds, and in particular to a process for the preparation of elobixibat. The process can be carried out under mild and safe conditions and may be used to prepare elobixibat on an industrial scale. The invention also relates to a process for the preparation of a crystalline monohydrate of elobixibat.
    Type: Grant
    Filed: March 29, 2019
    Date of Patent: October 1, 2019
    Assignee: Elobix AB
    Inventors: Ganapati G. Bhat, Johnson M. Coutinho, Mikael Dahlström, Michael Lofthagen, Akinori Tatara
  • Patent number: 10428031
    Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: December 12, 2018
    Date of Patent: October 1, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin, Kenneth W. Bair
  • Patent number: 10392368
    Abstract: The invention provides compounds of formula (I): or a pharmaceutically-acceptable salt thereof, wherein the variables are defined in the specification, that are inhibitors of JAK kinases, particularly JAK3. The invention also provides crystalline forms, pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: July 31, 2018
    Date of Patent: August 27, 2019
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Erik Fenster, Tom M. Lam, Mandy Loo, Robert Murray McKinnell, Anthony Francesco Palermo, Diana Jin Wang, Breena Fraga, Jerry Nzerem, Marta Dabros, Venkat R. Thalladi, Miroslav Rapta
  • Patent number: 10377726
    Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: October 29, 2018
    Date of Patent: August 13, 2019
    Assignee: Forma Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin
  • Patent number: 10300075
    Abstract: Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
    Type: Grant
    Filed: March 28, 2018
    Date of Patent: May 28, 2019
    Assignee: AMGEN INC.
    Inventors: Sean P. Brown, Kexue Li, Yunxiao Li, Markian M. Stec
  • Patent number: 10239845
    Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: February 2, 2016
    Date of Patent: March 26, 2019
    Assignee: Forma Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin
  • Patent number: 10221143
    Abstract: The invention provides alkyl benzene compounds. The compounds are useful for treating conditions including Alzheimer's disease, Parkinson's disease, diabetes, cancer, inflammation, hyperresponsiveness, allergic conditions, asthma, and psychotic disorders such as schizophrenia. The compounds are also useful to lower IL-4, IL-5, or IL-15 levels in an animal.
    Type: Grant
    Filed: March 1, 2016
    Date of Patent: March 5, 2019
    Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY
    Inventors: Carl Wagner, Peter Jurutka, Pamela Marshall
  • Patent number: 10214500
    Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: February 2, 2016
    Date of Patent: February 26, 2019
    Assignee: Forma Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Heather Davis, Aleksandra Rudnitskaya, David R. Lancia, Jr., Kenneth W. Bair, David S. Millan, Matthew W. Martin
  • Patent number: 10214501
    Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: February 2, 2016
    Date of Patent: February 26, 2019
    Assignee: Forma Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin, Kenneth W. Bair
  • Patent number: 10112915
    Abstract: The present invention relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: February 2, 2016
    Date of Patent: October 30, 2018
    Assignee: Forma Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin
  • Patent number: 10071999
    Abstract: The present invention relates to novel crystalline forms of compound (I), (3-Amino-oxetan-3-ylmethyl)-[2-(5,5-dioxo-5,6,7,9-tetrahydro-5lambda*6*-thia-8-aza-benzocyclohepten-8-yl)-6-methyl-quinazolin-4-yl]-amine and pharmaceutical compositions comprising the crystalline forms thereof disclosed herein, which may be used for the treatment or prophylaxis of a viral disease in a patient relating to respiratory syncytial virus (RSV) infection or a disease caused by RSV infection.
    Type: Grant
    Filed: January 12, 2018
    Date of Patent: September 11, 2018
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Wei Zhang, Lin Wang, Wei Li
  • Patent number: 9725443
    Abstract: Described are ROR? modulators of the formula (I), or pharmaceutically acceptable salts thereof, wherein all substituents are defined herein. The invention includes stereoisomeric forms of the compounds of formula I, including stereoisomerically-pure, scalemic and racemic form, as well as tautomers thereof. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR? activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR? activity, for example, autoimmune and/or inflammatory disorders.
    Type: Grant
    Filed: September 18, 2014
    Date of Patent: August 8, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: T. G. Murali Dhar, Jingwu Duan, Hua Gong, Bin Jiang, Zhonghui Lu, David S. Weinstein
  • Patent number: 9402828
    Abstract: Provided herein are methods and compositions for treating a patient with cancer wherein the cancer is characterized by a PTEN gene mutation and/or a PI3K gene mutation. In particular embodiments, the methods comprise administering to the patient a composition comprising a therapeutically effective amount of a PLK4 antagonist.
    Type: Grant
    Filed: January 9, 2015
    Date of Patent: August 2, 2016
    Assignee: University Health Network
    Inventors: Guohua Pan, Jacqueline M. Mason, Xin Wei, Miklos Feher
  • Patent number: 9403800
    Abstract: Methods and small molecule compounds for inhibition of cancer cell proliferation are provided. One example of a class of compounds that may be used is represented by the compound of Formula I or a pharmaceutically acceptable salt, N-oxide or solvate thereof, wherein A, B, D, E, F, G, I, J, R, R1, R2, R2?, R3, R4, R5, R6, R7, R8, R9 are as described herein.
    Type: Grant
    Filed: January 24, 2013
    Date of Patent: August 2, 2016
    Assignee: ChemRegen, Inc.
    Inventors: John Cashman, Mark Mercola, Dennis Schade, Masanao Tsuda
  • Patent number: 9340533
    Abstract: Provided are novel compound that is useful as a treatment agent or a prophylactic agent for cardiac failure, cardiac failure due to dystelectasis, left ventricular diastolic impairment, angina or cardiac infarct, hypertension, ischemic cardiac disease, and myocardial relaxation impairment recognized in cardiac failure, atrial fibrillation or ventricular arrhythmia, and a pharmaceutical composition containing the same. The invention pertains to a 1,4-benzothiazepine-1-oxide derivative represented by general formula [I] (In the formula, R represents a hydrogen atom or a hydroxyl group.) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same [I].
    Type: Grant
    Filed: December 24, 2013
    Date of Patent: May 17, 2016
    Inventor: Noburo Kaneko
  • Patent number: 9339480
    Abstract: Provided herein are methods of utilizing bile acid transport inhibitors for the treatment of obesity and diabetes.
    Type: Grant
    Filed: November 23, 2009
    Date of Patent: May 17, 2016
    Assignee: SATIOGEN PHARMACEUTICALS, INC.
    Inventors: Andrew A. Young, Bronislava Gedulin, Howard E. Greene
  • Patent number: 9254292
    Abstract: The present invention relates to novel Fused Tetracycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A?, B, G, R1, U, V, W, W?, X, X?, Y and Y? are as defined herein. The present invention also relates to compositions comprising at least one Fused Tetracycle Derivative, and methods of using the Fused Tetracycle Derivatives for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: September 28, 2011
    Date of Patent: February 9, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Brian J. Lavey, Michael P. Dwyer, Joseph A. Kozlowski, Stuart B. Rosenblum
  • Patent number: 9139546
    Abstract: Cannabinoid derivatives according to formula (I) are disclosed wherein, X, Y, R1, R2, and W can have the definitions provided herein. Without limitation, use of such compounds, their salts or pro-drug, or compositions containing the compounds, salts, or pro-drug, to modify the activity of CB1 and CB2 receptors and treat conditions mediated by these receptors.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: September 22, 2015
    Assignee: The University of Tennessee Research Foundation
    Inventors: Bob M. Moore, II, Himanshu Bhattacharjee, Suni Mustafa
  • Patent number: 9115139
    Abstract: Provided is a compound having a serotonin 5-HT2c receptor activating action, useful for lower urinary tract conditions, obesity and cancer. A compound represented by the formula (I0): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: June 14, 2010
    Date of Patent: August 25, 2015
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Shigekazu Sasaki, Tomokazu Kusumoto
  • Patent number: 9040518
    Abstract: Compounds of Formula I and methods for treating metabolic disorders are disclosed.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: May 26, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: Christopher Joseph Aquino, Jon Loren Collins, David John Cowan, Yulin Wu
  • Publication number: 20150141396
    Abstract: The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases.
    Type: Application
    Filed: July 3, 2013
    Publication date: May 21, 2015
    Applicant: Ares Trading S.A.
    Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Patrick Gerber, Mathilde Muzerelle
  • Publication number: 20150111857
    Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Douglas Wilson, Yulian Zhang
  • Patent number: 8999968
    Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: April 7, 2015
    Assignee: University Health Network
    Inventors: Peter Brent Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Guohua Pan
  • Patent number: 8962574
    Abstract: A method for preventing stroke in a patient suffering from atrial fibrillation, wherein the patient has at least one risk factor for major bleeding events, the method comprising administering to the patient 110 mg b.i.d. of dabigatran etexilate, optionally in the form of a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: February 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Paul Anthony Reilly
  • Patent number: 8962610
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: February 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • Patent number: 8946205
    Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: February 3, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma, S.A.
    Inventors: Jose Maria Cid-Nunez, Ana Isabel De Lucas Olivares, Andres Avelino Trabanco-Suarez, Gregor James MacDonald
  • Publication number: 20150025061
    Abstract: The present invention is directed to a method of enhancing visual acuity in a subject, comprising intravitreally administering to the subject in need of such enhancement, a therapeutically effective amount of an extrasynaptic GABAA receptor antagonist. The present invention is also directed to an ocular implant comprising a therapeutically effective amount of the extrasynaptic GABAA receptor antagonist.
    Type: Application
    Filed: July 10, 2014
    Publication date: January 22, 2015
    Inventor: Movses H. Karakossian
  • Patent number: 8933070
    Abstract: Provided herein are methods, uses and compositions for treating a patient with cancer wherein the cancer is characterized by a PTEN gene mutation. In particular embodiments, the methods comprise administering to the patient a composition comprising a therapeutically effective amount of a PLK4 antagonist, and identifying a patient that is likely to be responsive to PLK4 antagonist therapy, if PTEN gene mutation is present.
    Type: Grant
    Filed: July 4, 2011
    Date of Patent: January 13, 2015
    Assignee: University Health Network
    Inventors: Guohua Pan, Jacqueline M. Mason, Xin Wei, Miklos Feher
  • Patent number: 8927535
    Abstract: The present invention provides cyclopropyl-fused-1,3-thiazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: January 6, 2015
    Assignee: Hoffman-La Roche Inc.
    Inventor: Thomas Woltering
  • Publication number: 20140378436
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Application
    Filed: November 23, 2011
    Publication date: December 25, 2014
    Applicant: Exelixis, Inc.
    Inventor: Kenneth D. Rice
  • Publication number: 20140378437
    Abstract: The present invention relates to 1,4-benzothiazepine derivatives and their use to treat conditions, disorders and diseases associated with ryanodine receptors (RyRs) that regulate calcium channel functioning in cells. The invention also discloses pharmaceutical compositions comprising the compounds and uses thereof to treat diseases and conditions associated with RyRs, in particular cardiac, musculoskeletal and central nervous system (CNS) disorders.
    Type: Application
    Filed: September 3, 2014
    Publication date: December 25, 2014
    Inventors: JIAMING YAN, SANDRO BELVEDERE, YAEL WEBB, MARC BERTRAND, NICOLE VILLENEUVE
  • Publication number: 20140377332
    Abstract: Nano-constructs comprising nanoshells and methods of using the nano-constructs for treating or ameliorating a medical condition are provided.
    Type: Application
    Filed: November 21, 2013
    Publication date: December 25, 2014
    Inventors: Florian N. Ludwig, Stephen D. Pacetti, Syed F.A. Hossainy, Dariush Davalian
  • Publication number: 20140371202
    Abstract: The present teaching provide indazole compounds represented by Structural Formulae (I) or (I?) or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as TTK protein kinase, polo-like kinase 4 (PLK4) and Aurora kinases having anticancer activity against breast cancer cells, colon cancer cells, and ovarian cancer cells.
    Type: Application
    Filed: October 12, 2012
    Publication date: December 18, 2014
    Applicant: University Health Network
    Inventors: Heinz W. Pauls, Radoslaw Laufer, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Yunhui Lang, Narendra Kumar B. Patel, Louise G. Edwards, Grace Ng, Peter Brent Sampson, Miklos Feher, Donald E. Awrey
  • Patent number: 8906904
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: December 9, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Jehrod Burnett Brenneman, John Ginn, Michael D. Lowe, Christopher Ronald Sarko, Edward S. Tasber, Zhonghua Zhang
  • Patent number: RE47731
    Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.
    Type: Grant
    Filed: March 6, 2018
    Date of Patent: November 19, 2019
    Inventors: Peter Brent Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel