Abstract: The invention relates to compounds having the structure of formula (I) which can be used for the treatment of or against influenza infections.
Type:
Grant
Filed:
April 3, 2020
Date of Patent:
September 14, 2021
Assignee:
JANSSEN SCIENCES IRELAND UNLIMITED COMPANY
Inventors:
Tim Hugo Maria Jonckers, David Craig McGowan, Jérôme Émile Georges Guillemont, Werner Constant J Embrechts, Guillaume Jean Maurice Mercey, Christophe Francis Robert Nestor Buyck, Wendy Mia Albert Balemans, Pierre Jean-Marie Bernard Raboisson
Abstract: Small molecule carbazole compounds for use as androgen receptor inhibitors are provided herein. Also provided herein are methods for using the carbazole compounds in treating prostate cancer, including castration-resistant prostate cancer and enzalutamide-resistant prostate cancer. The methods include administering to a subject an effective amount of a compound or composition as described herein.
Type:
Grant
Filed:
October 23, 2019
Date of Patent:
August 31, 2021
Assignee:
GEORGETOWN UNIVERSITY
Inventors:
Milton L. Brown, Shujie Hou, Partha Banerjee, Karishma Amin
Abstract: The present invention provides a process for the manufacture of a compound of formula VIIIa and salts forms of VIIIa where Rc is an aryl sulfonic acid
Type:
Grant
Filed:
August 8, 2019
Date of Patent:
August 24, 2021
Assignee:
Genentech, Inc.
Inventors:
Jinguang Lin, Alexandra Chestakova, Wei Gu, Hans Iding, Jing Li, Xin Linghu, Patrik Meier, Chunbo Sha, Jeffrey Stults, Youchu Wang, Haiming Zhang, Jianqian Zhang, Tao Zhang
Abstract: Provided are a Syk inhibitor and a use method therefor, and in particular, disclosed are quinolinone represented by formula (I) or quinazoline derivatives or pharmaceutically acceptable salts thereof, a preparation method, a pharmaceutical composition, and uses in preparing a medicament for treatment of Syk receptor related diseases.
Type:
Grant
Filed:
June 14, 2018
Date of Patent:
August 17, 2021
Assignee:
Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
Abstract: Provided are a fosaprepitant phosphate intermediate (IV) preparation method, a fosaprepitant phosphate intermediate (IV-A) and a method of (AA) for preparing fosaprepitant dimeglumine by using the intermediate (IV-A). IV: R1 and R2 are independently selected from C1-C7 alkyl groups or benzyl groups; IV-A: R1 and R2 are independently selected from C1-C7 alkyl groups, and R1 and R2 are not both benzyl groups.
Abstract: The present invention relates to an oxopicolinamide derivative, a preparation method therefor and the pharmaceutical use thereof. In particular, the present invention relates to an oxopicolinamide derivative as shown in the general formula (AI), a preparation method therefor and a pharmaceutical composition comprising the derivative, and to the use thereof as a therapeutic agent, in particular as an inhibitor of blood coagulation factor XIa (Factor XIa, FXIa for short) and the use thereof in the preparation of a drug for treating diseases such as thromboembolism, wherein the definition of each substituent in the general formula (AI) is the same as defined in the description.
Abstract: The disclosure is directed to compounds of Formula I Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.
Type:
Grant
Filed:
January 16, 2020
Date of Patent:
August 3, 2021
Assignee:
Prelude Therapeutics, Incorporated
Inventors:
Hong Lin, Juan Luengo, Rupa Shetty, Michael Hawkins
Abstract: In one aspect, methods of treating bacterial infections are described herein employing compounds having more than one target for antibacterial activity. Additionally pharmaceutical compositions comprising such compounds are also described.
Type:
Grant
Filed:
August 1, 2018
Date of Patent:
August 3, 2021
Assignee:
THE TRUSTEES OF PRINCETON UNIVERSITY
Inventors:
Zemer Gitai, James Martin, Hsin-Jung Li, Max Wilson, Hahn Kim
Abstract: The present invention relates to bioactive cyclic compounds and their use as antimicrobial agents. In particular, the present invention relates to barbiturate mimics of Eusynstyelamides or small antimicrobial peptides. The compounds of the invention are represented by Formula (I).
Type:
Grant
Filed:
March 28, 2018
Date of Patent:
July 27, 2021
Assignee:
Universitetet i Tromsø—Norges Arktiske Universitet
Inventors:
Morten Bøhmer Strøm, Annette Bayer, Stig Olov Magnus Engqvist, Marianne Hagensen Paulsen, Dominik Ausbacher
Abstract: The present invention provides a process for the manufacture of a compound of formula VIIIa and salts forms of VIIIa where Rc is an aryl sulfonic acid
Type:
Grant
Filed:
December 18, 2019
Date of Patent:
July 20, 2021
Assignee:
Genentech, Inc.
Inventors:
Jinguang Lin, Alexandra Chestakova, Wei Gu, Hans Iding, Jing Li, Xin Linghu, Patrik Meier, Chunbo Sha, Jeffrey Stults, Youchu Wang, Haiming Zhang, Jianqian Zhang, Tao Zhang
Abstract: A process for the purification of a melamine melt (5) containing melamine and by-products, comprising the steps of: (a1) quenching of said melamine melt; (a2) decomposition of by-products with alkali, providing an alkaline aqueous solution of melamine (26); (b) stripping of said alkaline aqueous solution of melamine (26); (c) crystallization of melamine with a first alkali-containing solution (6b) and separation of solid melamine (7) from a mother liquor (8); (d) treatment of said mother liquor, providing a waste water stream (11) containing carbonates; (e) decomposition of at least part of the carbonates contained in said waste water stream (11) into carbon dioxide and alkali, providing a second alkali-containing aqueous solution (30); (f) recycle of at least part of said alkali-containing aqueous solution (30) to at least one of said steps (a1), (a2) and (c).
Abstract: Bcl-2 inhibitors, pharmaceutical compositions thereof, and methods of use thereof are provided. In particular, Bcl-2 inhibitors of formula (I) are provided, wherein the variable groups are as defined in the specification. The Bcl-2 inhibitors can be used to treat cell proliferative disorders.
Abstract: The present invention relates to compounds of Formula (I) that are useful as inhibitors of the activity of the ubiquitin specific protease USP19. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in therapy.
Type:
Grant
Filed:
July 26, 2017
Date of Patent:
July 6, 2021
Assignee:
ALMAC DISCOVERY LIMITED
Inventors:
Peter Hewitt, Mary Melissa McFarland, James Samuel Shane Rountree, Frank Burkamp, Christina Bell, Lauren Proctor, Matthew Duncan Helm, Colin O'Dowd, Timothy Harrison
Abstract: A subject of the present invention is a compound having the general formula (I): a pharmaceutically acceptable salt thereof or a tautomeric form thereof, wherein A, B3, B4, B5, Y, X, B1 and B2 are as defined in any one of claims 1 to 10. Another subject of the invention is the compound as defined above for use as a medicament, in particular for preventing and/or treating inflammation and inflammatory diseases, immune and auto-immune diseases, pain related diseases, genetic diseases and/or cancer.
Type:
Grant
Filed:
July 13, 2017
Date of Patent:
June 29, 2021
Assignees:
Centre National de la Recherche Scientifique, Institut National de la Sante et de la Recherche Medicale, Universite de Strasbourg, Universite Paris-Sud, Centre International de Recherche aux Frontieres de la Chimie
Abstract: The invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.
Type:
Grant
Filed:
March 4, 2019
Date of Patent:
June 22, 2021
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Benno Rothenhaeusler, Rene Trussardi, Fabienne Hoffmann-Emery, Urs Schwitter, Jean-Michel Adam, Olaf Grassmann, Thomas Hartung, Frederic Ran, Ralph Diodone, Christophe Pfleger, Bjorn Bartels