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: Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.
Type:
Grant
Filed:
February 10, 2020
Date of Patent:
July 20, 2021
Assignee:
Akebia Therapeutics, Inc.
Inventors:
James Densmore Copp, Ann W. Newman, Anne Luong
Abstract: Methods of synthesizing fluoroquinolones such as ciprofloxacin are provided. The methods utilize affordable materials, reduce the number of synthesis steps and provide high yields.
Abstract: Described herein are compounds that are LOXL2 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 LOXL2 activity.
Type:
Grant
Filed:
August 27, 2019
Date of Patent:
July 13, 2021
Assignee:
PHARMAKEA, INC.
Inventors:
Martin W. Rowbottom, John Howard Hutchinson
Abstract: Provided herein are spirocyclic and fused bicyclic carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.
Type:
Grant
Filed:
November 15, 2017
Date of Patent:
July 13, 2021
Assignee:
H. LUNDBECK A/S
Inventors:
Cheryl A. Grice, Daniel J. Buzard, Michael B. Shaghafi
Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R1, R5, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
Type:
Grant
Filed:
June 24, 2020
Date of Patent:
July 6, 2021
Assignee:
Bristol-Myers Squibb Company
Inventors:
Alaric J. Dyckman, Dharmpal S. Dodd, Christopher P. Mussari, Trevor C. Sherwood, Brian K. Whiteley, John L. Gilmore, Sreekantha Ratna Kumar, Laxman Pasunoori, Pitani Veera Venkata Srinivas, Srinivasan Kunchithapatham Duraisamy, Subramanya Hegde, Rushith Kumar Anumula
Abstract: Disclosed are small molecule inhibitors of ?v?6 integrin, and methods of using them to treat a number of diseases and conditions.
Type:
Grant
Filed:
June 26, 2019
Date of Patent:
June 29, 2021
Assignee:
Morphic Therapeutic, Inc.
Inventors:
Bryce A. Harrison, Matthew G. Bursavich, Mark Brewer, Aleksey I. Gerasyuto, Kristopher N. Hahn, Kyle D. Konze, Fu-Yang Lin, Blaise S. Lippa, Alexey A. Lugovskoy, Bruce N. Rogers, Mats A. Svensson, Dawn M. Troast
Abstract: Methods for treating a subject for a food allergy condition are provided. Aspects of the methods include administering to a subject in need thereof a psychedelic agent in a manner effective to treat the subject for a food allergy condition. Effective administration of a psychedelic agent may include administering the psychedelic agent in an amount effective to treat the subject for the food allergy condition. In some instances, the subject is known to have a food allergy condition.
Type:
Grant
Filed:
November 27, 2019
Date of Patent:
June 29, 2021
Assignee:
Palo Alto Investors LP
Inventors:
Anthony Joonkyoo Yun, Conrad Minkyoo Yun
Abstract: Disclosed are small molecule inhibitors of ?v?6 integrin, and methods of using them to treat a number of diseases and conditions.
Type:
Grant
Filed:
February 27, 2018
Date of Patent:
June 29, 2021
Assignee:
Morphic Therapeutic, Inc.
Inventors:
Bryce A. Harrison, Matthew G. Bursavich, Aleksey I. Gerasyuto, Kristopher N. Hahn, Kyle D. Konze, Fu-Yang Lin, Blaise S. Lippa, Alexey A. Lugovskoy, Bruce N. Rogers, Mats A. Svensson, Dawn M. Troast
Abstract: Disclosed are small molecule inhibitors of ?v?6 integrin, and methods of using them to treat a number of diseases and conditions.
Type:
Grant
Filed:
February 27, 2018
Date of Patent:
June 22, 2021
Assignee:
Morphic Therapeutic, Inc.
Inventors:
Mark Brewer, Matthew G. Bursavich, Aleksey I. Gerasyuto, Kristopher N. Hahn, Bryce A. Harrison, Kyle D. Konze, Fu-Yang Lin, Blaise S. Lippa, Alexey A. Lugovskoy, Bruce N. Rogers, Mats A. Svensson, Dawn M. Troast
Abstract: The present invention generally relates to compounds as a dual kinase-demethylase inhibitor useful for the treatment of diseases mediated by a kinase and/or a histone demethylase, such as inflammation, cancer, viral and bacterial infections, neurological and immunological disorders. Pharmaceutical compositions and methods for treating those diseases are within the scope of this invention.
Type:
Grant
Filed:
March 29, 2018
Date of Patent:
June 22, 2021
Inventors:
Herman O. Sintim, Neetu Dayal, Clement Opoku-Temeng
Abstract: Compounds are provided having the structure of the following Formula I: where R, R1, R2, R3a and R3b are as defined herein. Pharmaceutical compositions comprising such compounds, as well as methods related to their manufacture and use, are also provided.
Type:
Grant
Filed:
May 11, 2020
Date of Patent:
June 22, 2021
Assignee:
RECEPTOS LLC
Inventors:
Adam Yeager, Philip Turnbull, Lin Zhang, Junhua Fan, Junko Tamiya, Marcos Steinberg, Tom Fowler, Hanae Benelkebir, Raffaele Pasceri, Maria Ieva, Kevan Grant, Yang Tran
Abstract: The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.
Type:
Grant
Filed:
November 27, 2019
Date of Patent:
June 15, 2021
Assignee:
Nuvation Bio Inc.
Inventors:
Sarvajit Chakravarty, Son Minh Pham, Jiyun Chen, Jayakanth Kankanala, Jeremy D. Pettigrew, Anjan Kumar Nayak, Anup Barde, Brahmam Pujala
Abstract: Described herein are compounds that are somatostatin modulators, 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 that would benefit from modulation of somatostatin activity.
Type:
Grant
Filed:
July 24, 2018
Date of Patent:
June 8, 2021
Assignee:
CRINETICS PHARMACEUTICALS, INC.
Inventors:
Jian Zhao, Yunfei Zhu, Shimiao Wang, Sangdon Han, Sun Hee Kim
Abstract: The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
Type:
Grant
Filed:
September 11, 2017
Date of Patent:
June 8, 2021
Assignee:
Padlock Therapeutics, Inc.
Inventors:
Rajesh Devraj, Gnanasambandam Kumaravel, Cristina Lecci, Pui Leng Loke, Mirco Meniconi, Nathaniel Julius Thomas Monck, Carl Leslie North, Mark Peter Ridgill, Heather Tye
Abstract: There is provided compounds of formula I (I) or pharmaceutically-acceptable salts thereof, wherein L, R1, R2, R3 and X have meanings provided in the description, which compounds are useful in the treatment of cancers.
Type:
Grant
Filed:
February 7, 2018
Date of Patent:
June 8, 2021
Assignee:
Oblique Therapeutics AB
Inventors:
Benjamin Pelcman, Edgars Suna, William Stafford, Martins Priede
Abstract: The present embodiments relate to substituted heterocyclic derivative therapeutic compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of diseases mediated by aberrant cell signalling, such as inflammatory disorders, cancer and neoplastic disease. Particular compounds described herein exhibit selective inhibitory activity against CBP compared with BRD4.
Type:
Grant
Filed:
January 27, 2020
Date of Patent:
June 1, 2021
Assignee:
CELGENE QUANTICEL RESEARCH, INC.
Inventors:
Lynnie Trzoss, Juan Manuel Betancort, Toufike Kanouni, Michael Brennan Wallace, Amogh Boloor
Abstract: Disclosed are small molecule inhibitors of ?v?6 integrin, and methods of using them to treat a number of diseases and conditions.
Type:
Grant
Filed:
August 24, 2020
Date of Patent:
June 1, 2021
Assignee:
Morphic Therapeutic, Inc.
Inventors:
Bryce A. Harrison, James E. Dowling, Matthew G. Bursavich, Dawn M. Troast, Blaise S. Lippa, Bruce N. Rogers, Cheng Zhong, Qi Qiao, Fu-Yang Lin, Brian Sosa, Aleksey I. Gerasyuto, Andrea Bortolato
Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to ?v-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of av-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
Type:
Grant
Filed:
November 7, 2017
Date of Patent:
May 25, 2021
Assignee:
Bristol-Myers Squibb Company
Inventors:
Pratik Devasthale, Fang Moore, Guohua Zhao, Susan Nicole Pieniazek, Kumaravel Selvakumar, Suresh Dhanusu, Manoranjan Panda, Lawrence R. Marcin
Abstract: The present invention relates to a pyridine derivative of formula (1) wherein R1 is optionally-substituted C1-6 alkyl, optionally-substituted C3-10 cycloalkyl, or optionally-substituted 5- to 10-membered saturated or partially-unsaturated heterocyclyl; R2 is halogen atom, cyano, C1-6 alkyl which may be optionally substituted with 1 to 3 the same or different halogen atoms, C1-6 alkoxy which may be optionally substituted with 1 to 3 the same or different halogen atoms, or amino which may be optionally substituted with 1 to 2 the same or different C1-6 alkyl; and the bind with broken line is single or double bond, or a pharmaceutically acceptable salt thereof, which is useful as a medicament for treating symptoms in anxiety-related disorder.
Type:
Grant
Filed:
March 12, 2018
Date of Patent:
May 25, 2021
Assignee:
SUMITOMO DAINIPPON PHARMA CO., LTD.
Inventors:
Hidefumi Yoshinaga, Hiro Uemachi, Tomomi Ohno, Jeremy Besnard