Abstract: The present invention relates to a compound of formula (I) wherein Ar is (II) or (II); R is CH3 or OCH3; or a pharmaceutically acceptable acid addition salt or a corresponding enantiomer thereof. The compounds are modulators of ?-secretase (A ?42) and may be useful for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis-Dutch type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
Abstract: The present invention provides a compound represented by formula [I] shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme.
Abstract: Compounds that inhibit p38? MAPK protein, and methods of using the same, are provided for treating or preventing diseases such as cancer or inflammatory diseases.
Type:
Grant
Filed:
April 15, 2021
Date of Patent:
June 14, 2022
Assignees:
University of Maryland, Baltimore, The United States of America as represented by The Department of Veterans Affairs
Inventors:
Paul S. Shapiro, Alexander D. MacKerell, Jr., Jeffrey D. Hasday
Abstract: The present disclosure relates generally to thienopyrimidine compounds that bind to Acetyl-CoA Carboxylase (ACC) and act as inhibitors of ACC. The disclosure further relates to the use of the thienopyrimidine compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of ACC, including liver diseases such as non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH).
Type:
Grant
Filed:
August 6, 2020
Date of Patent:
June 7, 2022
Assignee:
Gilead Sciences, Inc.
Inventors:
Jamie G. Bates, Ana Z. Gonzalez Buenrostro, Hongyan Guo, Xiaochun Han, Brian J. Kirby, Yurong Lai, Michael L. Mitchell, Gregg M. Schwarzwalder, James G. Taylor, Ting Wang
Abstract: A method of preparing Compound (1) or a pharmaceutically acceptable salt thereof: comprises: (a) reacting Compound (X): or a pharmaceutically acceptable salt thereof with Compound (Y): in the presence of a palladium catalyst and a carbonate or phosphate base to form compound (Z): or a pharmaceutically acceptable salt thereof; and (b) deprotecting the Ts group of Compound (Z) to form Compound (1) or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
March 9, 2020
Date of Patent:
May 31, 2022
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Gerald J. Tanoury, William Aloysius Nugent, Vadims Dvornikovs, Peter Jamison Rose
Abstract: A quaternary lactam compound of formula (I). The compound is used in the manufacture of a medicament for the treatment and/or prevention of thrombotic or thromboembolic disorders.
Type:
Grant
Filed:
March 29, 2019
Date of Patent:
May 31, 2022
Assignee:
SHANGHAI MEIYUE BIOTECH DEVELOPMENT CO., LTD.
Inventors:
Shanghai Yu, Yan Feng, Shiqiang Li, Xiaolin Wang, Zhilong Hu, Yawen Ding, Feihong Dai, Qian He, Chaodong Wang
Abstract: The present disclosure relates to a novel compound as a JAK inhibitor, a composition, and an application thereof. Specifically, the present disclosure provides a compound having high JAK inhibitory activity (as represented by formula (I)) or its isomer, solvate, hydrate, pharmaceutically-acceptable salt, and prodrug, and a pharmaceutical composition containing the compound. Also disclosed is a use of the present compound or pharmaceutical composition in preparation of a medicament for treating autoimmune diseases or cancers.
Abstract: Described herein are ASK1 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with ASK1 activity.
Abstract: The present invention relates to a compound represented by formula (1): the compound having antagonist activity against serotonin 5-HT2A receptors and serotonin 5-HT7 receptors; or a pharmaceutically acceptable salt of the compound. (In the formula, Z is a nitrogen atom and the like; Y is carbonyl and the like; m and n are 1 and the like; R1a through R1d, R2a through R2d, and R4a through R4d are a hydrogen atom and the like; R3 is alkyl and the like; and Q is a specific bicyclic group.
Type:
Grant
Filed:
November 17, 2021
Date of Patent:
May 24, 2022
Assignee:
SUMITOMO DAINIPPON PHARMA CO., LTD.
Inventors:
Yuki Fujii, Masayuki Sakuma, Yoshinori Aihara, Jeremy Besnard, Andrew Simon Bell
Abstract: A novel class of inhibitors of protein kinases useful in the treatment of proliferative cell diseases and conditions including cancers, and especially those characterised by over-expression of CDK8 and/or one or more aberrant CDK8 activity, including certain cancers of lung, breast, brain, ovary, prostate, colorectal cancer and leukaemias. The inhibitors have the general structure I.
Type:
Grant
Filed:
January 14, 2019
Date of Patent:
May 10, 2022
Assignee:
AUCENTRA HOLDINGS PTY LTD
Inventors:
Shudong Wang, Stephen Philip, Mingfeng Yu
Abstract: The present disclosure includes novel compounds useful as antimicrobial agents. The present disclosure further includes methods useful. The present disclosure further includes compositions and methods for treating or preventing a bacterial infection. The present disclosure further includes compositions and methods useful for preventing or reducing the growth or proliferation of microorganisms.
Abstract: The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
Type:
Grant
Filed:
June 11, 2020
Date of Patent:
May 10, 2022
Assignee:
CORTEXYME, INC.
Inventors:
Andrei W. Konradi, Robert A. Galemmo, Jr., Stephen S. Dominy, Casey C. Lynch, Leslie J. Holsinger
Abstract: Some embodiments of the invention include inventive compounds (e.g., compounds of Formula (I)). Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions (e.g., pharmaceutical compositions) for treating, for example, certain diseases using the inventive compounds. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating (e.g., diseases such as cancer). Further embodiments include methods for making the inventive compounds. Additional embodiments of the invention are also discussed herein.
Type:
Grant
Filed:
July 22, 2016
Date of Patent:
April 26, 2022
Assignee:
University of Lousville Research
Foundation, Inc.
Inventors:
Geoffrey J. Clark, John O. Trent, Joseph A. Burlison, Nagaraju Miriyala
Abstract: The present disclosure relates generally to eukaryotic initiation factor 2B modulators, or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers, or prodrug thereof, and methods of making and using thereof.
Type:
Grant
Filed:
May 28, 2021
Date of Patent:
April 19, 2022
Assignee:
Denali Therapeutics Inc.
Inventors:
Robert A. Craig, II, Javier de Vicente Fidalgo, Anthony A. Estrada, Jianwen A. Feng, Brian M. Fox, Maksim Osipov, Arun Thottumkara
Abstract: The present invention provides compounds of Formula (I): Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
Abstract: The present invention provides a novel crystalline form of verubecestat (Crystalline Form II of Verubecestat) and pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an A? pathology and/or a symptom or symptoms thereof. Non-limiting examples of such A? pathologies, including Alzheimer's disease and mild cognitive impairment, are disclosed herein.
Type:
Grant
Filed:
June 8, 2018
Date of Patent:
April 19, 2022
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Laura M. Artino, William Morris, Eric Sirota, Richard J. Varsolona
Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the structure of Formula A.
Type:
Grant
Filed:
December 12, 2019
Date of Patent:
April 12, 2022
Assignee:
CORTEVA AGRISCIENCE LLC
Inventors:
Natalie C. Giampietro, David Demeter, Lindsey G. Horty, Gary D. Crouse, Thomas C. Sparks
Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.
Type:
Grant
Filed:
April 12, 2019
Date of Patent:
April 12, 2022
Assignee:
Incyte Corporation
Inventors:
Joshua Hummel, Minh Nguyen, Alexander Sokolsky, Oleg Vechorkin, Qinda Ye, Wenqing Yao
Abstract: Thiazole compounds of Formula (I) shown below and pharmaceutical compositions containing one of such compounds: wherein R1 and R2 are defined in the specification. Also disclosed are methods of inhibiting a tyrosine kinase and treating cancer associated with a tyrosine kinase with one of the thiazole compounds.
Type:
Grant
Filed:
November 19, 2020
Date of Patent:
April 12, 2022
Assignees:
National Health Research Institutes, Taivex Therapeutics Corporation
Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
Type:
Grant
Filed:
July 11, 2018
Date of Patent:
April 12, 2022
Assignee:
Bristol-Myers Squibb Company
Inventors:
Donald J. P. Pinto, Tarun Kumar Maishal