Abstract: The present invention relates to the fields of medicinal chemistry and pharmacotherapy, and specifically relates to the chemical compound of formula (I), and its racemate, R-isomer, S-isomer, pharmaceutically acceptable salt, and mixtures thereof, as well as its method for preparation, a pharmaceutical composition containing said chemical compound, and use as a lysine-specific demethylase 1 (LSD 1) inhibitor. The cyclopropylamine chemical compound to which the present invention relates may be used in the treatment of cancer.
Type:
Grant
Filed:
June 2, 2017
Date of Patent:
January 16, 2024
Assignee:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Inventors:
Hong Liu, Jia Li, Wei Zhu, Yubo Zhou, Jiang Wang, Mingbo Su, Shuni Wang, Wei Xu, Chunpu Li, Weijuan Kan, Hualiang Jiang, Kaixian Chen
Abstract: The disclosure discloses a linker compound, a polyethylene glycol-linker conjugate and a derivative thereof, and a polyethylene glycol-linker-drug conjugate. The linker compound as well as the conjugate thereof with the polyethylene glycol and the derivative thereof may be used for modifying a drug, and a modification reaction is simple and easy to carry out. Moreover, a reaction yield is high, and an application range of the modified drug is wide. The modified drugs gradually degrade from a chain of the conjugate in vivo, and may stay in a lesion (such as a cancer site) for a longer period of time, achieving purposes of sustained and controlled release, reducing an administration frequency, and greatly improving a bioavailability of the drug and a patient compliance.
Type:
Grant
Filed:
March 30, 2020
Date of Patent:
January 2, 2024
Assignee:
JenKem Technology Co., Ltd. (Tianjin)
Inventors:
Zewang Feng, Qingbin Wang, Jinliang Wang, Yanping Song, Yanli Xiong, Leimin Wang, Jinghui Du, Xuan Zhao
Abstract: Disclosed herein are salts and solid state forms of psilocybin, including psilocybin HCl, and salts and solid forms of O-acetylpsilocin, including O-acetylpsilocin fumarate. Also disclosed are methods for making the salts and solid forms and methods for administering the salts and solid forms. The salts and solid forms disclosed herein are useful for treating neurological disease and/or a psychiatric disorder in a subject.
Abstract: Embodiments provide, among other compounds, a family of compounds that can be used as therapeutic anti-cancer agents, methods for using such compounds to treat cancer, and methods of making such compounds.
Abstract: In alternative embodiments, provided are processes comprising the continuous isolation and purification of cannabinoids and further isomerization of the purified cannabidiol to ?8tetrahydrocannabinol (?8THC) and ?9tetrahydrocannabinol (?9THC). In alternative embodiments, provided are processes for converting ?8-THC into ?9-THC. In alternative embodiments, provided are processes for the industrial scale continuous isolation and purification of cannabinoids and further isomerization of the purified cannabidiol to ?9-THC.
Abstract: In alternative embodiments, provided are processes for obtaining or purifying a substantially pure ?8tetrahydrocannabinol (?8THC) and/or ?9tetrahydrocannabinol (?9THC) and optionally a plurality of cannabinoids or terpenes from a natural or a synthetic source, wherein the natural or the synthetic source comprises a cannabidiol (CBD) and optionally a plurality of cannabinoids or terpenes. Also provided are processes comprising the continuous isolation and purification of cannabinoids or terpenes, and further isomerization of the purified cannabidiol to ?8tetrahydrocannabinol (?8THC) and ?9tetrahydrocannabinol (?9THC). In alternative embodiments, provided are processes for converting ?8-THC into ?9-THC. In alternative embodiments, provided are processes for the industrial scale continuous isolation and purification of cannabinoids and further isomerization of the purified cannabidiol to ?9-THC.
Abstract: The description relates to imide-based compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.
Type:
Grant
Filed:
December 17, 2021
Date of Patent:
December 5, 2023
Assignee:
YALE UNIVERSITY
Inventors:
Craig M. Crews, George Burslem, Philipp M. Cromm, Saul Jaime-Figueroa, Momar Toure
Abstract: A method for preparing dihydromyricetin nanocrystals includes: uniformly dispersing dihydromyricetin in a good solvent to obtain a dihydromyricetin solution; uniformly dispersing a precipitator and a stabilizer in water to obtain a mixed solution, and then adding the dihydromyricetin solution into the mixed solution and mixing uniformly under a stirring condition to obtain a dihydromyricetin nanocrystal solution; and drying the dihydromyricetin nanocrystal solution to obtain the dihydromyricetin nanocrystals. The method for preparing the dihydromyricetin nanocrystals by an anti-solvent method is simple and easy to implement, low in cost, good in nanocrystal stability, small in organic solvent consumption, and safe and environment-friendly in preparation process.
Type:
Grant
Filed:
March 1, 2023
Date of Patent:
December 5, 2023
Assignee:
SHAANXI UNIVERSITY OF SCIENCE AND TECHNOLOGY
Inventors:
Yang Kong, ChangZhao Wang, Bin Tian, Fang Lin, Zihao Li
Abstract: The invention provides novel compounds having the general formula I: wherein R1, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.
Abstract: The present invention provides novel piperidinyl-containing nociceptin receptor ligand compounds and pharmaceutical compositions useful in the treatment of neurological diseases and conditions where such ligands mediate the negative effects of the condition. Such neurological diseases and conditions include acute and chronic pain, substance abuse/dependence, alcohol addiction, anxiety, depression, sleep disorders, gastrointestinal disorders, renal disorders, cardiovascular disorders and Parkinson's disease.
Abstract: Disclosed is a crystal form of a hepatitis B surface antigen inhibitor and a preparation method, and an application of the crystal form in the preparation of the hepatitis B surface antigen inhibitor.
Abstract: The present disclosure relates generally to compounds and compositions thereof for inhibition of ErbB2, including mutant forms of ErbB2, particularly those harboring an Exon 20 mutation, methods of preparing said compounds and compositions, and their use in the treatment or prophylaxis of various cancers, such as lung, glioma, skin, head neck, salivary gland, breast, esophageal, liver, stomach (gastric), uterine, cervical, biliary tract, pancreatic, colorectal, renal, bladder or prostate cancer.
Type:
Grant
Filed:
November 1, 2022
Date of Patent:
November 7, 2023
Assignee:
EnLiven Therapeutics, Inc.
Inventors:
Joseph P. Lyssikatos, Samuel Kintz, Li Ren, Qiang Su
Abstract: The present subject matter involves novel pyrido[3,4-b]indol-1-one compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrido[3,4-b]indol-1-one compounds are useful as anticancer and/or antitumor agents.
Abstract: The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains, and methods of synthesis of these compounds.
Type:
Grant
Filed:
February 10, 2022
Date of Patent:
October 17, 2023
Assignee:
Forma Therapeutics, Inc.
Inventors:
Shawn E. R. Schiller, Torsten Herbertz, Hongbin Li, Bradford Graves, Steven Mischke, Angela V. West, Jennifer R. Downing, Anna Ericsson
Abstract: This invention provides small organic molecules useful as therapeutics of neurodegenerative diseases. Small organic molecules that act as inhibitors of bone morphogenetic proteins (BMPs) are useful in the treatment of neuroinflammatory disorders, in particular multiple sclerosis.
Type:
Grant
Filed:
July 22, 2021
Date of Patent:
October 10, 2023
Assignee:
THE MEDICAL RESEARCH, INFRASTRUCTURE AND HEALTH SERVICES FUND OF THE TEL AVIV MEDICAL CENTER
Abstract: This application relates to methods of diagnosing and treating anorexia nervosa (AN) and binge eating disorder (BED) with a nonselective activator of metabotropic glutamate receptors (mGluRs).
Abstract: Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.
Type:
Grant
Filed:
December 3, 2020
Date of Patent:
October 10, 2023
Assignees:
Genentech, Inc., Hoffmann-La Roche Inc.
Inventors:
Cheol Keun Chung, Jie Xu, Hans Iding, Kyle Clagg, Michael Dalziel, Alec Fettes, Francis Gosselin, Ngiap-Kie Lim, Andrew McClory, Haiming Zhang, Paroma Chakravarty, Karthik Nagapudi, Sarah Robinson
Abstract: The present technology is directed to methods of inhibiting or modulating p97 and compounds and compositions useful in such methods. Diseases and conditions that can be treated with the compounds and compositions of the present technology include, but are not limited to, antibacterial infection, antiviral infection, cancer and neurodegenerative disorders susceptible to treatment by inhibition or modulation of p97.
Type:
Grant
Filed:
December 7, 2021
Date of Patent:
October 3, 2023
Assignee:
University of Pittsburgh—Of the Commonwealth System of Higher Education
Inventors:
Donna M. Huryn, Peter Wipf, Matthew G. LaPorte