Abstract: Provided are new bifunctional chelators for use in the manufacture of radiolabeled targeting agents for therapeutic or diagnostic use. Also provided are conjugates of the new bifunctional chelators with various cancer antigen targeting agents.
Abstract: Methods are provided for modulating MRGPRX2 or a MRGPRX2 ortholog generally, or for treating a MRGPRX2 or a MRGPRX2 ortholog dependent condition more specifically, by contacting the MRGPRX2 or the MRGPRX2 ortholog by administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I): or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein W, Z, R1, R2, R3, R4, R5, R6 and Rx are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.
Type:
Grant
Filed:
October 20, 2021
Date of Patent:
April 30, 2024
Assignee:
Escient Pharmaceuticals, Inc.
Inventors:
Marion Lanier, Marcus Boehm, Liming Huang, Esther Martinborough, Marcos Sainz, Brandon Selfridge, Adam Yeager
Abstract: Disclosed herein are acetal and cyclic acetal compounds, compositions, their preparation, and their uses. Some embodiments relate to their use as liver-targeting compounds.
Abstract: Compounds for treating preventing malaria and, particularly, to larvicidal agents that are 4-[(substituted 1H-benzimidazol-2-ylsulfanyl)methyl]-6-substituted-2H-chromen-2-ones derivatives and their use as larvicidal agents.
Type:
Grant
Filed:
October 23, 2023
Date of Patent:
April 30, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Katharigatta N. Venugopala, Osama I. Alwassil, Pran Kishore Deb, Rashmi Venugopala, Priya R. Kadam, Yadav D. Bodke, Vijaykumar Uppar
Abstract: The present invention relates to crystalline compounds comprising vadadustat and L-proline and processes for their preparation. Furthermore, the invention relates to a pharmaceutical composition comprising one or more of the crystalline compounds of the present invention and at least one pharmaceutically acceptable excipient. The pharmaceutical composition of the present invention can be used as a medicament, in particular for the treatment and/or prevention of anemia for example in patients with end-stage renal disease (ESRD) and/or chronic kidney disease (CKD).
Type:
Grant
Filed:
November 7, 2019
Date of Patent:
April 30, 2024
Assignee:
Sandoz AG
Inventors:
Verena Adamer, Andrea Thaler, Erwin Schreiner
Abstract: Provided are new bifunctional chelators for use in the manufacture of radiolabeled targeting agents for therapeutic or diagnostic use. Also provided are conjugates of the new bifunctional chelators with various cancer antigen targeting agents.
Abstract: Provided is a method for synthesizing bipyridine that includes performing a dimerization reaction of a reactant including a piperidine-based compound, a pyridine-based compound, or a mixture thereof in the presence of a catalyst in which an active metal is supported on a composite metal oxide support including silica (SiO2) and alumina (Al2O3).
Type:
Grant
Filed:
August 22, 2022
Date of Patent:
April 9, 2024
Assignees:
HYUNDAI MOTOR COMPANY, KIA CORPORATION, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
Inventors:
Jihui Seo, Jaeyong Lee, Pyung Soon Kim, Jin Woo Choung, Yongwoo Kim, Ji Hoon Park, Soo Min Kim, Jeong Jae Lee, Kwanyong Jeong
Abstract: The present subject matter relates to a new liquid and solid-state laser system comprising a laser structure and novel 7H-pyrano[2,3-b:4,5-b?]diquinoline derivative compounds as the laser active media; the novel 7H-pyrano[2,3-b:4,5-b?]diquinoline derivative compounds comprising 10-chloro-7H-pyrano[2,3-b:4,5-b?]diquinoline [(Cl-PD)] and 10-methoxy-7H-pyrano[2,3-b:4,5-b?]diquinoline [(MeO-PD)]; and a method of synthesizing the organic 7H-pyrano[2,3-b:4,5-b?]diquinoline derivative compounds used in the laser system.
Abstract: The present disclosure provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that modulate the activity of phosphoinositide 3-kinases-gamma (PI3K?) and are useful in the treatment of diseases related to the activity of PI3K? including, for example, autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
Type:
Grant
Filed:
March 25, 2022
Date of Patent:
April 9, 2024
Assignee:
Incyte Corporation
Inventors:
Richard B. Sparks, Stacey Shepard, Andrew P. Combs, Andrew W. Buesking, Lixin Shao, Haisheng Wang, Nikoo Falahatpisheh
Abstract: Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.
Type:
Grant
Filed:
December 2, 2019
Date of Patent:
April 2, 2024
Assignee:
Cornell University
Inventors:
Joseph P. Vacca, Sarah Elizabeth Bettigole
Abstract: Quinolines, polyquinolines, polybenzoquinolines, molecular segments of fullerenes and graphene nanoribbons, and graphene nanoribbons and processes for producing such materials are provided. The processes utilize a form of an aza-Diels-Alder (Povarov) reaction to first form quinolines and/or polyquinolines. In some such embodiments polyquinolines thus produced are used to form graphene nanoribbon precursors, and molecular segments and graphene nanoribbons. In many such embodiments the graphene nanoribbone precursors are formed from polybenzoquinolines.
Type:
Grant
Filed:
January 22, 2021
Date of Patent:
April 2, 2024
Assignee:
The Regents of the University of California
Inventors:
Alon Gorodetsky, David Joshua Dibble, Mehran Umerani, Amir Mazaheripour, Young Suk Park, Anthony Burke
Abstract: Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.
Type:
Grant
Filed:
November 2, 2018
Date of Patent:
March 26, 2024
Assignee:
AbbVie Inc.
Inventors:
Jennifer M. Frost, Lei Shi, Yunsong Tong, Michael J. Dart, Kathleen J. Murauski
Abstract: A 5-(4,5-bis(4-bromophenyl)-2-(4-chlorophenyl)-1H-imidazol-1-yl)pentanoic acid compound, its synthesis, and its use as an antimicrobial agent.
Type:
Grant
Filed:
October 25, 2023
Date of Patent:
March 26, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Hany Mohamed Abd El-Lateef Ahmed, Mai Mostafa Khalaf Ali, Antar Ahmed Abdelhamid Ahmed, Amer A. Amer
Abstract: The present disclosure relates generally to compounds that bind to Lysophosphatidic Acid Receptor 1 (LPAR1) and act as antagonists of LPAR1. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of LPAR1, including fibrosis and liver diseases such as non-alcoholic steatohepatitis (NASH), interstitial lung disease (ILD), or chronic kidney disease (CKD).
Type:
Grant
Filed:
December 6, 2022
Date of Patent:
March 26, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Brian P. Bestvater, Joshua A. Kaplan, Barton W. Phillips, Kin S. Yang, Anna Zagorska
Abstract: Compounds for treating tuberculosis and, particularly, to anti-tubercular compounds that are substituted 1,4-dihydropyrmidines and their use as anti-tubercular agents.
Type:
Grant
Filed:
August 16, 2023
Date of Patent:
March 19, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Katharigatta N. Venugopala, Mohamed A. Morsy, Pran Kishore Deb, Melandran Pillay, Ramasamy Durai, Madhusudana Reddy Muthukurpalya Bhojegowd, Dhakshanamurthy Thirumalai, Viresh Mohanlall
Abstract: A 9-(4-nitrobenzylidene)-4-(4-nitrophenyl)-3-cyano-2-methoxy-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridine compound, its synthesis, and its use as an antimicrobial agent.
Type:
Grant
Filed:
December 12, 2023
Date of Patent:
March 19, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Mai Mostafa Khalaf Ali, Hany Mohamed Abd El-Lateef Ahmed, Mohamed Gouda, Antar Ahmed Abdelhamid Ahmed
Abstract: Embodiments and methods for a new class of potent non-peptidic covalent inhibitors of nsP2 cysteine protease that inhibit Venezuelan equine encephalitis virus's (VEEV) replication in neuroblasts are disclosed. More particularly, an acrylate and vinyl sulfone-based chemical series were investigated as promising starting scaffolds against VEEV and as inhibitors of the cysteine protease domain of VEEV's non-structural protein 2 (nsP2). The invention discloses compounds of Formula I and analogues for treatment of VEEV.
Type:
Grant
Filed:
January 25, 2021
Date of Patent:
February 20, 2024
Assignee:
Jackson State University
Inventors:
Ifedayo Victor Ogungbe, Huaisheng Zhang
Abstract: A compound 1-cyclopropyl-6-fluoro-7-(4-(2-hydroxy-3-(naphthalen-2-yloxy)propylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid, its synthesis, and its use as an insecticidal agent.
Type:
Grant
Filed:
August 29, 2023
Date of Patent:
February 20, 2024
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Hany Mohamed Abd El-Lateef Ahmed, Mai Mostafa Khalaf Ali, Antar Ahmed Abdelhamid Ahmed, Mohamed A. Gad