Abstract: The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.
Type:
Grant
Filed:
December 4, 2020
Date of Patent:
August 22, 2023
Assignee:
Theravance Biopharma R&D IP, LLC
Inventors:
Svitlana Kulyk, Christina Owens, Steven D. E. Sullivan, Jennifer Kozak, Adam D. Hughes
Abstract: The present invention relates to a novel synthetic pathway for alpha-tocopherol. The invention discloses different reactions yielding some new intermediates in a very high yield and stereoselectivity.
Type:
Grant
Filed:
May 3, 2021
Date of Patent:
August 15, 2023
Assignee:
DSM IP ASSETS B.V.
Inventors:
Ulla Letinois, Thomas Netscher, August Ruettimann
Abstract: Disclosed are dendrimers of formula (I): and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising the dendrimer of formula (I) and methods of using the same for treating cancer.
Type:
Grant
Filed:
November 11, 2020
Date of Patent:
August 8, 2023
Assignee:
ASTRAZENECA AB
Inventors:
Marianne Bernice Ashford, Iain Grant, Edward John Hennessy, William Mccoull, Michael Giannis, Brian Kelly, David Owen, John Paul Secrist
Abstract: A novel compound suitable as an epoxy curing catalyst; an epoxy curing catalyst using the compound; and a method for producing the compound. A compound represented by formula (1) in which Xm+ represents an m valent counter cation, R1 represents an aromatic group which may have a substituent; R2 represents an alkylene group which may have a substituent; R3 represents a halogen atom, a hydroxyl group, a mercapto group, a sulfide group, a silyl group, a silanol group, a nitro group, a nitroso group, a sulfonic acid ester group, a phosphino group, a phosphinyl group, a phosphonic acid ester group or an organic group; m represents an integer of 1 or more; n represents an integer of 0-3; and R2 may bond with R1 to form a cyclic structure.
Type:
Grant
Filed:
September 26, 2018
Date of Patent:
August 8, 2023
Assignees:
Tokyo Ohka Kogyo Co., Ltd., Daicel Corporation
Abstract: The present technology provides 3,3-difluoroallylamines or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The 3,3-difluoroallylamines or their pharmaceutically acceptable salts exhibit potent inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).
Type:
Grant
Filed:
July 6, 2021
Date of Patent:
August 1, 2023
Assignee:
YUHAN CORPORATION
Inventors:
Tae Dong Han, Hee Jae Tak, Eun Kyung Kim, Eui Chul Lee, Sol Park, Hyok Jun Cho, Cheol Hee Lim, So Young Kim, Hyun Ho Choi, Da Na Jeong, Na Yeon Yang, Na Ry Ha
Abstract: The present disclosure relates to derivatives of bicyclic compounds and their uses in therapy. In particular, the present disclosure relates to derivatives of bicyclic compounds for use in modulating kinase enzymatic activity and accordingly modulating kinase-dependent diseases and conditions such as cancer and in specific embodiments, hepatocellular carcinoma (HCC). The present disclosure also relates to methods of synthesizing these compounds.
Type:
Grant
Filed:
July 23, 2019
Date of Patent:
July 18, 2023
Assignee:
Agency for Science, Technology and Research
Abstract: The invention relates to pyrazole derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to HbS modulators of formula (I) or tautomers thereof, or pharmaceutically acceptable salts of said modulators or tautomers thereof, wherein X, Y, R2 and R3 are as defined in the description. HbS modulators are potentially useful in the treatment of a wide range of disorders, including sickle cell disease (SCD).
Type:
Grant
Filed:
April 12, 2021
Date of Patent:
July 18, 2023
Assignee:
Pfizer Inc.
Inventors:
Ariamala Gopalsamy, Shawn Cabral, Agustin Casimiro-Garcia, Ming Zhu Chen, Chulho Choi, Robert Lee Dow, Olugbeminiyi Omezia Fadeyi, David Hepworth, Jayasankar Jasti, Lyn Howard Jones, Arjun Venkat Narayanan, Mihir Dineshkumar Parikh, David Walter Piotrowski, Lee Richard Roberts, Ralph Pelton Robinson, Jr., Hatice Gizem Yayla
Abstract: The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, cough, itch, and neurogenic inflammation.
Type:
Grant
Filed:
November 16, 2020
Date of Patent:
July 11, 2023
Assignee:
Nocion Therapeutics, Inc.
Inventors:
Bridget McCarthy Cole, James Lamond Ellis
Abstract: Described herein are complexes comprising a cationic antibacterial agent and a metal salt, personal care compositions comprising same; along with methods of making and using these complexes and compositions.
Type:
Grant
Filed:
December 7, 2018
Date of Patent:
July 4, 2023
Assignee:
Colgate-Palmolive Company
Inventors:
Viktor Dubovoy, Junhong Mao, Ravi Subramanyam, Long Pan, Tatiana Brinzari
Abstract: A method of treating intestinal gastrointestinal, or bowel disorders in a subject in need thereof includes administering to the subject a therapeutically effective amount of 15-PGDH inhibitor alone or in combination with a corticosteroid and/or TNF alpha antagonist.
Type:
Grant
Filed:
November 30, 2017
Date of Patent:
July 4, 2023
Assignee:
CASE WESTERN RESERVE UNIVERSITY
Inventors:
Sanford Markowitz, Won Jin Ho, Stephen P. Fink, Vinay Varadan
Abstract: Disclosed herein are compounds which inhibit RIPK1, pharmaceutical compositions, and methods of treatment of RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer.
Type:
Grant
Filed:
November 19, 2020
Date of Patent:
July 4, 2023
Assignee:
Board of Regents, The University of Texas System
Inventors:
Richard T. Lewis, Matthew Hamilton, William J. Ray, Fernando Alvarez, Naphtali Reyna, Jason Cross, Suyambu Kesava Vijayan Ramaswamy
Abstract: It is intended to provide a novel method for treating a cancer using an FGFR inhibitor that exhibits a remarkably excellent antitumor effect and has fewer side effects. The present invention provides a combination preparation for the treatment of a malignant tumor comprising a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof, and one or more additional compound(s) having an antitumor effect or pharmaceutically acceptable salt(s) thereof, and a pharmaceutical composition comprising both the active ingredients. The present invention also provides an antitumor effect enhancer, an antitumor agent, a kit for malignant tumor treatment, etc. comprising a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof.
Abstract: Binding of the transcriptional co-activator, YAP1, to the transcription factor Oct4, induces Sox2, which is a transcription actor necessary for the self-renewal of stem-like cells from non-small cell lung cancer. The WW domain of YAP1 binds to the PPxY motif of Oct4 to induce Sox2. Delivering a peptide corresponding to the WW domain could prevent the induction of Sox2 and sternness. Similarly, peptides and mimetics of the PPxY motif would be able to inhibit sternness. Disclosed are compounds that affect the Yap1:Oct4 interaction.
Type:
Grant
Filed:
March 14, 2019
Date of Patent:
June 27, 2023
Assignee:
H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.
Inventors:
Srikumar Chellappan, Nicholas J. Lawrence, Sujeewa Ranatunga Mahanthe Mudiyanselage
Abstract: The disclosure is directed to, in part, to CDK inhibitors, pharmaceutical compositions comprising the same, as well as methods of their use and preparation.
Type:
Grant
Filed:
September 11, 2020
Date of Patent:
June 13, 2023
Assignee:
Prelude Therapeutics Incorporated
Inventors:
Liang Lu, Rupa Shetty, Andrew Paul Combs, Chaofeng Dai, Raul Andrew Leal, Klare Lazor Bersch
Abstract: Processes that use novel reagents for the removal of colored impurity during the preparation of Salcaprozic Acid and pharmaceutically acceptable salts thereof. The processes include hydrolysis of 8-(2,4-dioxo-1,3-benzoxazin-3-yl)octanoic acid ethyl ester in the presence of or by contacting it with benzotriazole, hydrazine and/or sodium borohydride.
Type:
Grant
Filed:
April 13, 2022
Date of Patent:
June 6, 2023
Assignee:
Navinta III Inc.
Inventors:
Pankaj Vasudev Parmar, Raja Jeyakumar John Muthiah, Vikas Kantilal Chauhan, Jagdish Kanjibhai Solanki
Abstract: AKR1C3-activated prodrugs of Formula (I), pharmaceutical compositions comprising prodrugs of Formula (I), and their use in the treatment of hyperproliferative diseases such as cancer and for cell ablation. The compounds of the invention are able to penetrate neoplasm tissue and be selectively reduced to an active (cytotoxic) form by contact with an AKR1C3 enzyme found in the neoplasm. This active form is therefore able to ablate AKR1C3-expressing target cells of the neoplasm and therefore has particular utility in the treatment of cancer and other hyperproliferative disorders.
Type:
Grant
Filed:
March 25, 2019
Date of Patent:
May 30, 2023
Assignee:
ACHILLES MEDICAL LIMITED
Inventors:
Amir Ashoorzadeh, Christopher Paul Guise, Adam Vorn Patterson, Jeffrey Bruce Smaill
Abstract: The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.
Type:
Grant
Filed:
December 4, 2020
Date of Patent:
May 30, 2023
Assignee:
OMEROS CORPORATION
Inventors:
Neil S. Cutshall, Jennifer Lynn Gage, Sara Rebecca Goldstein, Santosh Kumar Keshipeddy, Do Yeon Kwon, Robert Huerta Lemus, Thomas L. Little, Markus Metz, Peter Kurt Nollert Von Specht, Loren Michael Price, Jennifer Tsoung
Abstract: Compounds of formula (I): (I) and related aspects.
Type:
Grant
Filed:
November 30, 2018
Date of Patent:
May 23, 2023
Assignee:
STEP PHARMA S.A.S.
Inventors:
Abdul Quddus, Andrew Novak, David Cousin, Elli Chatzopoulou, Emma Blackham, Geraint Jones, Jennifer Thomas, Joseph Wrigglesworth, Lorna Duffy, Louise Birch, Pascal George, Saleh Ahmed