Abstract: A compound that is an inhibitor of at least one of the A2A and A2B adenosine receptors having Formula (I) and compositions containing the compound and methods for synthesizing the compound, are described herein. The use of such compound and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by the adenosine A2A receptor and/or the adenosine A2B receptor.
Type:
Grant
Filed:
May 16, 2018
Date of Patent:
January 11, 2022
Assignee:
ARCUS BIOSCIENCES, INC.
Inventors:
Manmohan Reddy Leleti, Dillon Harding Miles, Jay Patrick Powers, Brandon Reid Rosen, Ehesan Ul Sharif
Abstract: The present invention provides a compound of formula I, a cis-trans isomer, an enantiomer, a diastereoisomer, a racemate, a solvate, a hydrate, or a pharmaceutical acceptable salt and ester thereof, a preparation method for preparing the same, a pharmaceutical composition comprising the same and a use of the compound as an ?5-GABAA receptor regulator, wherein T, Z, A and Y are as defined in the description.
Abstract: Disclosed are compounds of general formulas I-III that may be used to inhibit the action of fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL) or dual FAAH/MAGL.
Type:
Grant
Filed:
January 16, 2020
Date of Patent:
January 4, 2022
Assignee:
Northeastern University
Inventors:
Alexandros Makriyannis, Vidyanand G. Shukla, Shakiru O. Alapafuja
Abstract: The disclosure generally relates to compounds, compositions, and methods for the treatment of cancer by restoring the P53 pathway signaling to repress cancer cell growth. In particular, the compounds comprise Formula I: or a pharmaceutically acceptable salt thereof, wherein: R1 is hydrogen or a haloalkyl group; and each R2, R3, R4, R5, R6, and R7 is, independently, hydrogen, halogen, hydroxyl, cyano, alkyl, alkenyl, alkoxy, substituted or unsubstituted aryl, heteroaryl, phosphate, phosphoramidate, amine, alkylamino, acylamino, aminoalkoxy, or alkylthio.
Type:
Grant
Filed:
January 23, 2019
Date of Patent:
December 21, 2021
Assignee:
Institute For Cancer Research
Inventors:
Wafik S. El-Deiry, Shengliang Zhang, Liz J. Hernandez Borrero
Abstract: There is a crystalline compound of (S)-ethyl 8-(2-amino-6-((R)-1-(5-chloro-[1,1?-biphenyl]-2-yl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)-2,8-diazaspiro[4.5]decane-3-carboxylate that exhibits an XRPD pattern having a characteristic peak at 19.05±0.20 (° 2?). There is also a pharmaceutical composition containing the compound. There is also a dosage form containing the crystalline compound and one or more pharmaceutically acceptable excipients. There is also a method for crystallizing/recrystallizing the compound. There is also a method for treating or preventing a disease with the compound.
Abstract: Methods of treating Primary Biliary Cholangitis and/or Primary Sclerosing Cholangitis with baricitinib, including formulations and dose regimens. The amount of baricitinib may be administered as a 4 mg tablet or pill that includes one or more excipients. The amount of baricitinib may be administered daily or at some other frequency.
Type:
Grant
Filed:
October 10, 2019
Date of Patent:
December 14, 2021
Assignee:
Eli Lilly and Company
Inventors:
Patrick L McCollam, James Michael McGill, Ana Luisa de Macedo Pinto Correia
Abstract: Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.
Type:
Grant
Filed:
December 12, 2019
Date of Patent:
December 7, 2021
Assignee:
Temple University-Of The Commonwealth System of Higher Education
Inventors:
Daniel J. Canney, Benjamin E. Blass, Rong Gao, Magid Abou-Gharbia
Abstract: Disclosed herein, inter alia, are compounds and methods of use thereof for the modulation of certain chemokine receptor activity.
Type:
Grant
Filed:
April 27, 2020
Date of Patent:
December 7, 2021
Assignee:
RAPT THERAPEUTICS, INC.
Inventors:
Jeffrey J. Jackson, John Michael Ketcham, Akinori Okano, Maureen Kay Reilly, Omar Robles-Resendiz, Jacob Bradley Schwarz, Parcharee Tivitmahaisoon, David Juergen Wustrow, Ashkaan Younai, Mikhail Zibinsky
Abstract: The present invention provides a selection of compounds of formula (I): (I) compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R5, R6, R7, A, B, W, X, Y and Z are as defined herein.
Type:
Grant
Filed:
May 31, 2017
Date of Patent:
November 23, 2021
Assignee:
KalVista Pharmaceuticals Limited
Inventors:
Rebecca Louise Davie, Hanna Joy Edwards, David Michael Evans, Simon Teanby Hodgson, Stephen John Pethen, David Philip Rooker
Abstract: The disclosure relates to compounds of formula (I), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, and related diseases.
Type:
Grant
Filed:
June 8, 2018
Date of Patent:
November 23, 2021
Assignee:
Bristol-Myers Squibb Company
Inventors:
Joanne M. Smallheer, Nicholas R. Wurtz, Meriah Neissel Valente, Karen A. Rossi, Ellen K. Kick
Abstract: The present invention provides a compound as shown in general formulas (I) or (II) and a pharmaceutically acceptable salt, an isomer or a mixture form thereof, a solvate, a polymorph, a stable isotope derivative, or a prodrug of the same. The compound of the present invention has CDK kinase inhibitory activity and can be used in treating a disease related to CDK kinase, such as a cancer.
Abstract: The present invention relates to a novel quinolinone derivative compound that regulates intracellular signal transduction mediated by TSLP and IL-33 to exhibit efficacy in preventing or treating allergic diseases such as asthma or atopic dermatitis. The quinolinone derivative compound of the present invention can effectively suppress inflammatory responses of allergic diseases such as asthma or atopic dermatitis. The present invention also relates to a pharmaceutical composition including the quinolinone derivative compound. The pharmaceutical composition of the present invention can be used to fundamentally prevent or treat various allergic and asthmatic diseases.
Type:
Grant
Filed:
January 4, 2018
Date of Patent:
November 9, 2021
Assignee:
Azcuris Co., Ltd.
Inventors:
Youngjoo Byun, Young Ho Jeon, Kiho Lee, Ki Yong Lee, Yong Woo Jung, Sang-Hyun Son
Abstract: Disclosed are 4-pyrazin-2-ylmethyl-morpholines of formula A and pharmaceutically acceptable salts thereof, wherein R1 and R2 are defined herein. Also disclosed are processes for their preparation, pharmaceutical compositions containing the compounds, and their use in therapy, particularly in the treatment or prevention of conditions having an association with NR2B negative allosteric modulating properties.
Abstract: The present disclosure is directed to modulators of SOS1 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same. Modulators of SOS1 have the following general structure of the Formula (II), or a pharmaceutically acceptable salt or a stereoisomer thereof, wherein the variables are as defined herein.
Type:
Grant
Filed:
December 23, 2020
Date of Patent:
November 9, 2021
Assignee:
Revolution Medicines, Inc.
Inventors:
Adrian L. Gill, Andreas Buckl, Elena S. Koltun, Naing Aay, Arlyn A. Tambo-ong, Severin Thompson, Micah James Gliedt, John E. Knox, James Cregg, Anne V. Edwards, Yang Liu, G. Leslie Burnett
Abstract: The present invention relates to the general field of treatment of infectious diseases of mammals (humans and animals) caused by bacteria, in particular to the treatment of diseases like tuberculosis (TB), Buruli ulcer and leprosy caused by mycobacteria. The invention aims at the generation of a new series of benzothiazinone compounds having the potential to overcome the above mentioned problems. In a preferred embodiment the invention is concerned with compounds of the general formula (I) wherein R1 represents NO2, R2 represents CF3, at least one of the substituents R3 and R4 is OH, SR14, NHR15, CN, N3, a saturated or unsaturated, optionally halogenated, linear or branched aliphatic radical having 1-4 carbon atoms, linear or branched C1-C4 alkoxy, C1-C4 acyl, and the other of R3 and R4 may in addition be hydrogen, R6 represents a 2-methyl-1,4-dioxa-8-azaspiro[4.
Type:
Grant
Filed:
September 21, 2017
Date of Patent:
October 26, 2021
Assignees:
University of Notre Dame Du Lac
Inventors:
Florian Kloss, Sebastian Schieferdecker, Axel Brakhage, Julia Dreisbach, Marvin J. Miller, Ute Mollmann, Kamil Philip Wojtas
Abstract: Disclosed are an EGFR inhibitor free base or acid salt polycrystalline form, a preparation method therefor, and an application thereof. The present invention specifically relates to an N-(5-((4-(1-cyclopropyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide free base or acid salt polycrystalline form, a preparation method therefor, and an application of the polycrystalline form in preparing a drug for treating an EGFR mutant activity-mediated disease. The present invention is used for inhibiting the activity of an L858R EGFR mutant, a T790M EGFR mutant and an exon 19 deletion activating mutant etc., may be widely applied in preventing and treating cancer, especially non-small cell lung cancer and other related diseases, and is expected to develop into a new generation of EGFR inhibitors.
Abstract: The present invention relates to inhibitors of PPP1 R15A and PPP1 R15B and their use in therapy, particularly in the treatment of a disease state alleviated by the inhibition of PPP1 R15A and PPP1 R15B, for example a disorder associated with accumulation of misfolded proteins or proteostatsis disorder. Compounds of the invention include compounds having the formula IA or a pharmaceutically acceptable salt thereof, wherein R1a, R3a, R5a, Xa and Ya are as defined herein.
Type:
Grant
Filed:
April 8, 2016
Date of Patent:
October 26, 2021
Assignee:
United Kingdom Research and Innovation
Inventors:
Anne Bertolotti, Indrajit Das, Agnieszka Krzyzosiak, Adrien Rousseau, Kim Schneider, Anna Gudny Sigurdardottir
Abstract: The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease.
Type:
Grant
Filed:
July 21, 2020
Date of Patent:
September 21, 2021
Assignee:
MyoKardia, Inc.
Inventors:
Johan Oslob, Danielle Aubele, Jae Kim, Robert McDowell, Yonghong Song, Arvinder Sran, Min Zhong
Abstract: The invention provides substituted pyrrolo[1,2-a]pyrimidinyl carboxamide and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrrolo[1,2-a]pyrimidinyl carboxamide compounds described herein include substituted 2-heterocyclyl-4-alkyl-pyrrolo[1,2-a]pyrimidine-8-carboxarnide compounds and variants thereof.
Type:
Grant
Filed:
April 6, 2017
Date of Patent:
September 21, 2021
Assignee:
BIAL-BIOTECH INVESTMENTS, INC.
Inventors:
Renato T. Skerlj, Elyse Marie Josee Bourque, Peter T. Lansbury, William J. Greenlee, Andrew C. Good
Abstract: The present disclosure relates to crystalline form CS1 and CS9 of a hypoxia-inducible factor prolyl hydroxylase inhibitor compound (I) GSK1278863, processes for preparation, and uses for preparing drugs treating and/or preventing anemia thereof.