Abstract: The present invention provides compounds as represented by structural formula (I). In formula (I), R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, and R14 are separately H or deuterium (D) independently. Moreover, at least one of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, and R14 must be D. Also provided is use of any of the compounds or its pharmaceutical composition in the preparation of a drug for treating an anxiety.
Type:
Grant
Filed:
November 18, 2019
Date of Patent:
June 14, 2022
Assignee:
BEIJING JUNKE HUAYUAN MED TECH CO., LTD.
Abstract: The present invention discloses a method for preparing a cyclopenta[c]chromene compound. A cationic rare earth compound [Ln(CH)3CN)9]3+[(AlCl4)3]3?.CH3CN is used as a catalyst, and p-methyl thiophenol is used as an accelerator for a catalytic reaction of a chalcone compound so as to prepare a product; and Ln, contained in the catalyst, represents a positive trivalent rare earth metal ion and is selected from one of La, Nd, Sm, Gd and Yb. According to the method, the starting materials are easy to obtain, the reaction process is simple, the catalyst usage is low, the catalyst is universally applicable to various substituted 2-hydroxy chalcones, and the obtained cyclopenta[c]chromene compound has not been reported. The catalyst synthesis method is simple and easy to obtain, and the yield of the target product is high.
Type:
Grant
Filed:
January 31, 2021
Date of Patent:
June 14, 2022
Assignee:
SOOCHOW UNIVERSITY
Inventors:
Fan Xu, Dandan Li, Xiaoyou Ding, Yanan Zhu, Zhigang Yao
Abstract: The present invention is directed to a compound having Formula (I) and its enantiomer: wherein the definitions of n, R, X, Y and Y3, and Z are provided in the disclosure. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use as opioid-like agonists in the treatment of pain.
Type:
Grant
Filed:
March 18, 2019
Date of Patent:
June 7, 2022
Assignee:
THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
Inventors:
Kenner Cralle Rice, Arthur E. Jacobson, Fuying Li, Eugene S. Gutman, Eric W. Bow
Abstract: PI3K signalling is the most increased pathway in human cancers. The four isoforms of PI3K are thought to be activated by different redundant mechanisms leading to a common downstream signalling. The inventors questioned this concept, by mapping differential isoform-specific downstream signalling in response to their constant selective inhibition in pancreatic cancer, a disease currently without therapy. They identified common and specific signals activated by each PI3K isoform. These data make the rational for the development of highly selective PI3K isoform drugs used in combination, instead of compounds inhibiting all PI3Ks. In particular, the inventors showed that combined p110a and 110? inhibition is the most efficient strategy for pancreatic cancer patients.
Type:
Grant
Filed:
October 12, 2018
Date of Patent:
June 7, 2022
Assignees:
INSERM, Université Paul Sabatier Toulouse III, CNRS, Klinikum Rechts der Isar der Technischen Universität München
Abstract: Disclosed are imidazo[1,2-b]pyrimido[4,5-d]pyridazin-5(6H)-one compounds, specifically represented by the Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A and R1-R5 are defined herein. Compounds having Formula I are Wee1 kinase inhibitors. Therefore, compounds of the disclosure may be used to treat diseases caused by abnormal Wee1 activity.
Type:
Grant
Filed:
July 10, 2018
Date of Patent:
May 31, 2022
Assignee:
IMPACT THERAPEUTICS (SHANGHAI), INC
Inventors:
Suixiong Cai, Ye Edward Tian, Zhiqiang Dong, Xiaozhu Wang
Abstract: Provided are solid forms of a compound useful for treating cancer, pharmaceutical compositions thereof, and methods of treating cancer comprising administering the solid forms described herein to a patient in need thereof.
Abstract: The invention relates to a serotonin receptor (5-HTR) inhibitor selected from the group consisting of a type 1 5-HTR inhibitor and a type 2 5-HTR inhibitor for use in the prevention and/or treatment of a haematological malignancy. Additionally, the invention relates to in vitro methods for the identification or isolation of a malignant cell from a haematological malignancy or for diagnosing a haematological malignancy based on detecting the expression of type 1 5-HTR and/or type 2 5-HTR. Furthermore, the invention relates to in vitro methods for determining the prognosis, for monitoring the effect of a therapy or for designing a customized therapy in a subject suffering from a haematological malignancy based on determining the levels of type 1 5-HTR and or type 2 5-HTR.
Type:
Grant
Filed:
December 11, 2018
Date of Patent:
May 24, 2022
Assignee:
Institut de Recerca Contra la Leucémia Josep Carreras
Abstract: The present disclosure is drawn to methods of treating diseases or disorders, and uses of preparing medicaments. The methods of administering and/or preparation of medicaments can include the use of a compound of Formula (I) disclosed herein, or a geometric isomer, stereoisomer, and/or pharmaceutically acceptable salt or solvate thereof.
Type:
Grant
Filed:
December 16, 2020
Date of Patent:
May 17, 2022
Assignee:
Kynan Duke IP, LLC
Inventors:
Colin Charles Duke, Rujee Kyokajee Duke, Van Hoan Tran
Abstract: The present invention relates to a process for preparing compounds of the formula (I) by halogenating compounds of the formula (II), where in R1, R2, R3 and X are defined according to the invention.
Abstract: Disclosed are methods and compositions related to STK1 inhibitors, such as Inh2-B1 (methyl 5-oxo-3-(phenyl carbamoyl)-1-thioxo-4,5dihydro[1,3]thiazolo[3,4-a]quinazoline-8-carboxylate). The STK1 inhibitors can act as an antibiotic resistance breakers against multidrug-resistant Staphylococcus aureus.
Abstract: The present invention covers substituted. Pyrazolo-pyrrolo-pyrimidine-dione (PPPD) compounds of general formula (I): in which R1, R2 and R3 are as defined herein, methods of preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of neurogenic diseases, as a sole agent or in combination with other active ingredients.
Inventors:
Marcus Koppitz, Holger Siebeneicher, Nico Bräuer, Elisabeth Pook, Andrea Rotgeri, Roland Neuhaus, Oliver Martin Fischer, Jens Nagel, Adam James Davenport, James Lindsay Carr, Robert James Townsend, Nina Connelly Ursinyova, Shelley Anne Parrott
Abstract: This application relates to compounds of formulae (I) and (II) and compositions thereof useful as inhibitors of PIM kinases. Also provided are methods of synthesis and methods of use of PIM inhibitors in treating individuals suffering from cancerous malignancies.
Type:
Grant
Filed:
November 5, 2018
Date of Patent:
May 3, 2022
Assignee:
SNAP BIO, INC.
Inventors:
Mark J. Burk, Brandon Chen, Jingyi Li, Shawn Bachan
Abstract: Provided are a (hetero)arylamide compound as shown in formula (I) having an inhibitory effect on protein kinase activity, a pharmaceutically acceptable salt, a stereoisomer, a solvate or hydrate thereof, a pharmaceutical composition including the compound or a derivative thereof, and a method for preparing the compound. The compound can be used as an irreversible inhibitor for protein kinase, for preparing a plurality of drugs including an anti-tumour drug.
Abstract: A composition for the treatment of cellulitis is provided that includes an antibiotic. The composition may also include an analgesic, an anaesthetic, or a combination thereof. A method use is also provided by which the composition is applied topically or to affected skin. A method of use is also provided prior to a medical procedure involving an incision through the skin of a patient in a predetermined area, the method including the application, to the predetermined area and prior to the procedure of the composition.
Abstract: The present invention relates to a composition of a CD47-SIRP? blocking agent and one or more anti-cancer agent(s), where the CD47-SIRP? blocking agents are represented by a compound of formula (I). The present invention also relates to a method of treating a cancer in a subject by administering a therapeutically effective amount of a CD47-SIRP? blocking agent represented by formula (I) in combination with one or more anti-cancer agent(s).
Abstract: The invention relates to a method for directly producing morin derivatives and high-purity morin of formula (I). The invention also relates to morin derivatives and high-purity morin that can be obtained using the claimed method.
Abstract: Glycine is an organic compound that can be used in the making of a synthetic base that obviates all the drawbacks of strong bases such as sodium hydroxide. The new compound is made by dissolving glycine in water and adding calcium hydroxide at a molar ration of about 1:1. Next, sodium percarbonate is dissolved in the solution to produce the new compound, which can be referred to as glycine hydroxide.
Abstract: Methods and uses for diagnosing and treating Tourette syndrome are encompassed, wherein diagnosis and treatment may be based upon an assessment of genetic alterations in metabotropic glutamate receptor (mGluR) network genes and wherein treatment is with nonspecific activators of mGluRs such as fasoracetam.