Abstract: The present application discloses a synthesis method of chiral nicotine from nicotinate and ?-butyrolactone, including the following steps: Step S1: performing condensation under an alkaline condition, and performing ring opening reaction with hydrochloric acid; Step S2: reacting with (+)—B-diisopinocampheyl chloroborane to produce a chiral hydroxyl group; Step S3: performing a chlorination reaction; and Step S4: performing cyclization under an alkaline condition to obtain the chiral nicotine. In the present application, nicotinate and ?-butyrolactone, both cheap and readily available, are used as raw materials, so as to reduce the production cost of (S)-nicotine. (+)—B-diisopinocampheyl chloroborane is used to reduce a carbonyl group of an intermediate to obtain a target chiral center.
Type:
Grant
Filed:
April 11, 2022
Date of Patent:
May 14, 2024
Assignee:
SHENZHEN ZINWI BIO-TECH CO., LTD
Inventors:
Jun Zou, Yang Zou, Meisen Liu, Weixian Luo
Abstract: Epoxidation methods and catalyst are described herein. The epoxidation catalysts generally include a metal component including silver and a support material including kaolinite, wherein the epoxidation catalyst includes less than 55 wt. % metal component.
Abstract: Disclosed are a phenyl amino sodium propionate derivative, a preparation method therefor and an application thereof. Specifically, disclosed are sodium 3-(4-(2-(9H-carbazole-9-yl)ethoxy)phenyl)-2-((2-(4-(4-(2-sodium forrnate-2-((2-(4-fluorobenzoyl)phenyl)amino)ethyl)phenoxy)benzoyl)phenyl)amino)propionate, a preparation method therefor and the use thereof for quality control of a bulk drug or formulation of Chiglitazar or a derivative thereof. Particularly, the compound can be used as a control substance or standard substance for the detection of impurities/related substances in Chiglitazar or a sodium salt drug thereof.
Abstract: The invention relates to compounds, methods and compositions for improving on nucleic acid polymerization, including DNA replication by in vitro primer extension to generate, for example, polymers for nanopore-based single molecule sequencing of a DNA template. A nucleic acid polymerase reaction composition is provided with polymerization enhancement moieties, which allows enhanced DNA polymerase activity with nucleotide analogs, resulting in improved length of primer extension products for sequencing applications.
Abstract: Methods of treating a disease caused by a positive strand RNA virus. The methods include administering to a subject in need thereof an effective amount of a compound of Formula I or Formula II.
Abstract: The disclosure relates to compounds and pharmaceutical compositions capable of modulating the hydroxysteroid 17-beta dehydrogenase (HSD17B) family member proteins including inhibiting the HSD17B member proteins, e.g. HSD17B13. The disclosure further relates to methods of treating liver diseases, disorders, or conditions with the compounds and pharmaceutical compositions disclosed herein, in which the HSD17B family member protein plays a role.
Abstract: Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
Inventors:
Koen Vandyck, Pierre Jean-Marie Bernard Raboisson, Leonid Beigelman, Vladimir Serebryany, Antitsa Dimitrova Stoycheva, Dorothée Alice Marie-Eve Bardiot, Sandro Boland, Arnaud Didier Marie Marchand
Abstract: Azaindole compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the azaindole compounds.
Type:
Grant
Filed:
February 17, 2021
Date of Patent:
April 2, 2024
Assignee:
Genentech, Inc.
Inventors:
Timothy Heffron, Sushant Malhotra, BinQing Wei, Bryan Chan, Lewis Gazzard, Emanuela Gancia, Michael Lainchbury, Andrew Madin, Eileen Seward, Yonghan Hu
Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunctions; thus, there is also utility for small organic compound ligands and can raise LDL levels.
Type:
Grant
Filed:
November 13, 2020
Date of Patent:
April 2, 2024
Assignee:
SRX Cardio, LLC
Inventors:
Thomas E. Barta, Jonathan William Bourne, Kyle D. Monroe, Michael M. Muehlemann, Anjali Pandey, Simeon Bowers
Abstract: Compounds and compositions useful in methods of treating, ameliorating, or inhibiting the development of an autoimmune disease by modulating the T cell response to antigenic peptide or fragments of antigenic peptides presented by the major histocompatibility (MHC) class II molecule, DQ2.
Type:
Grant
Filed:
December 21, 2021
Date of Patent:
April 2, 2024
Assignee:
ImmunoMolecular Therapeutics, Inc.
Inventors:
Robert B. Perni, Ryan Schutte, James M. Siedlecki
Abstract: Disclosed are a benzyl piperazine compound, a preparation method there for and an application thereof in an antivirus. The benzyl piperazine compound has a structure represented by the following general formula(I). It is proven by experiments that the benzyl piperazine compound not only has significant antiviral activity, but also has the advantages of low cytotoxicity, a high selectivity index and soon.
Type:
Grant
Filed:
November 29, 2019
Date of Patent:
March 26, 2024
Assignee:
INSTITUTE OF MEDICINAL BIOTECHNOLOGY, CHINESE ACADEMY OF MEDICAL SCIENCES
Abstract: The present invention provides an antibacterial chemical compound, its manufacturing method and its use thereof which acts as antibacterial agents being useful for treating a disease or condition characterized by infectious disease, such as gastroenteritis and invasive non-typhoidal Salmonellosis, and also providing a new therapeutic option for patients infected by the bacteria with the resistance to antibiotics.
Type:
Grant
Filed:
March 4, 2022
Date of Patent:
March 12, 2024
Assignees:
NATIONAL TAIWAN UNIVERSITY, NATIONAL YANG MING CHIAO TUNG UNIVERSITY
Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels.
Type:
Grant
Filed:
March 30, 2021
Date of Patent:
March 12, 2024
Assignee:
SRX Cardio, LLC
Inventors:
Thomas E. Barta, Jonathan William Bourne, Kyle D. Monroe, Michael M. Muehlemann, Anjali Pandey, Simeon Bowers
Abstract: Disclosed are compounds of Formula IIIb, their stereoisomers, tautomers, deuterates, pharmacologically acceptable salts, or hydrates thereof, methods of their preparation and pharmaceutical compositions and uses comprising such compounds. The Formula IIIb compounds are useful and highly effective as multi-targeted tyrosine kinase inhibitors in treating several kinds of cancers such as pancreatic cancer, lung cancer, renal cancer, liver cancer, gastric cancer, cervical cancer, leukemia, prostatic cancer, and other antitumor uses.
Abstract: Provided herein are rigid macrocycles comprising a poly(peri-naphthalene) diimide (PPNDI) submit and a second diimide subunit having both high photoluminescent and electron accumulation activities. Also provided herein are methods of preparation of the rigid macrocycles and methods of using the same.
Type:
Grant
Filed:
January 21, 2019
Date of Patent:
February 27, 2024
Assignees:
Northwestern University, King Abdulaziz City for Science and Technology (KACST)
Inventors:
Siva Krishna Mohan Nalluri, James Fraser Stoddart
Abstract: The disclosure is in part directed to crystalline forms of (R)-1?-(3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl)-3H-spiro[benzofuran-2,4?-piperidin]-3-amine, its salt, and variants thereof.
Type:
Grant
Filed:
September 23, 2020
Date of Patent:
February 6, 2024
Assignee:
Relay Therapeutics, Inc.
Inventors:
Alexander M. Taylor, André Lescarbeau, Jing Wang, Yanyan Zhang, Gaodeng Lian
Abstract: Provided herein are compositions, methods and kits for treating inflammatory bowel disease (IBD) such as Crohn's disease and ulcerative colitis in a mammal in need thereof. The method include administering to a subject with IBD a combination therapy containing a therapeutically effective amount of a chemokine receptor 9 (CCR9) inhibitor compound and a therapeutically effective amount of an anti-IL-23 antibody. Also provided herein is a kit containing the CCR9 inhibitor compound and anti-IL-23 antibody.
Type:
Grant
Filed:
March 31, 2021
Date of Patent:
January 30, 2024
Assignee:
CHEMOCENTRYX, INC.
Inventors:
James Campbell, Israel Charo, Thomas Schall, Rajinder Singh, Yibin Zeng, Penglie Zhang
Abstract: The present invention relates to substituted heterocyclic derivative 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 cancer and neoplastic disease.
Abstract: The present invention provides compounds that are dual inhibitors of soluble epoxide hydrolase and fatty acid amide hydrolase. The present invention also provides methods of using the compounds to inhibit soluble epoxide hydrolase and fatty acid amide hydrolase, and to treat cancer.
Type:
Grant
Filed:
December 4, 2020
Date of Patent:
January 16, 2024
Assignee:
The Regents of the University of California
Abstract: This invention relates to the new use of neurokinin-1 receptor antagonists as a treatment of pulmonary fibrosis conditions promoted by mechanical injury to the lungs. Specifically, when the mechanical injury to the lungs is induced by mechanical ventilation or by the act of coughing in a subset of patients with pulmonary fibrosis conditions who cough. The invention further relates to pharmaceutical compositions comprising neurokinin-1 receptor antagonist drugs and to combinations for such uses.