Abstract: The present invention relates to compounds of formula (Ib), wherein R1 to R3, M and L are as described herein, and their pharmaceutically acceptable salt, enantiomers and diastereomers thereof, and compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
August 22, 2024
Date of Patent:
March 11, 2025
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jianguo Chen, Lei Guo, Haixia Liu, Hong Shen, Junwei Xi, Weixing Zhang, Dan Zhao, Wei Zhu
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.
Abstract: The present invention relates to methods for treating patients with compensated cirrhosis, comprising administering to a patient in need thereof a therapeutically effective amount of a soluble guanylate cyclase (sGC) activator, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
March 20, 2023
Date of Patent:
February 18, 2025
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Judith Maria Ertle, Jochen Huber, Leo John Seman
Abstract: The present invention addresses the problem of providing a pharmaceutical composition for treatment of a variety of conditions accompanied by renal dysfunction. Renal dysfunction is improved by a pharmaceutical composition that comprises an optical isomer of a 1,4-benzothiazepine-1-oxide derivative represented by general formula [II] wherein, R represents a hydrogen atom or a hydroxyl group, and “*” indicates being an optical isomer. or a pharmacologically acceptable salt thereof.
Abstract: The present invention relates to safmamide or a pharmaceutically acceptable salt thereof for use in the treatment of a condition caused by pathological sarcolemma hyperexcitability, and/or of any other condition in which the restoration of normal sarcolemma excitability may produce a therapeutic benefit or improvement, wherein said condition is preferably a myotonic disorder.
Abstract: The present disclosure provides compounds of Formula (I). The compounds described herein may be useful in treating and/or preventing proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.
Type:
Grant
Filed:
May 4, 2021
Date of Patent:
July 11, 2023
Assignees:
Children's Medical Center Corporation, Beth Israel Deaconess Medical Center, Inc.
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, for use in the treatment of diseases or disorders that can be alleviated by sGC activation or potentiation, selected from chronic liver diseases, Non-Alcoholic Steatohepatitis (NASH), cirrhosis and portal hypertension.
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.
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.
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
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
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
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
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.
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
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
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
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.
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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.
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
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
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
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].
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
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
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.
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
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
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.
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.
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.
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