Abstract: Provided are novel heteroaromatic compound as an Autotaxin inhibitor, a pharmaceutical composition comprising the compound, and a use thereof in a treatment of a disease with a pathological feature of Autotaxin overexpression in a mammal, wherein the compound is according to formula (I), or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, tautomer, nitrogen oxide, metabolite, prodrug, or mixture thereof; wherein each of R1, Ar1, Ar2, Ar3, W, Y, Z, and Cy is defined in the present disclosure.
Type:
Grant
Filed:
May 22, 2019
Date of Patent:
June 20, 2023
Assignee:
GUANGZHOU HENOVCOM BIOSCIENCE CO., LTD.
Inventors:
Jiancun Zhang, Qingan Zou, Yanwei Chen, Ning Kang, Lijun Zhang, Yang Hu, Jufu Zhang
Abstract: The present invention describes new amino pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel amino pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.
Type:
Grant
Filed:
October 22, 2021
Date of Patent:
June 13, 2023
Assignee:
Novartis AG
Inventors:
Daniela Angst, François Gessier, Anna Vulpetti
Abstract: The present invention aims to provide a novel low-molecular-weight compound showing an orexin receptor agonist activity and expected to be useful as a prophylactic or therapeutic agent for narcolepsy and the like. The present invention provides a compound represented by the formula (I): wherein each symbol is as described in the description, or a pharmaceutically acceptable acid addition salt thereof, which has an orexin receptor agonist activity, and an orexin receptor agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.
Type:
Grant
Filed:
December 11, 2018
Date of Patent:
June 13, 2023
Assignees:
University of Tsukuba, BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
Abstract: Disclosed herein are methods for treating a cancer comprising administering to a subject in need thereof an effective dose of a CYP26-resistant retinoic acid receptor (RAR) alpha (RAR?) selective agonist, whereby as a result of the treatment the tumor burden is reduced in the subject and cancer stem cells resident in the bone marrow are substantially reduced.
Type:
Grant
Filed:
December 29, 2020
Date of Patent:
May 16, 2023
Assignees:
IO Therapeutics, Inc., The Johns Hopkins Univercity
Inventors:
Gabriel Ghiaur, Richard J. Jones, Salvador Alonso, Roshantha A. Chandraratna
Abstract: The present invention concerns a compound having the following formula (I): wherein: —A is in particular —N(R?a)—C(?O)—R, R?a being H or a (C1-C6)alkyl group, and R being preferably a group having the following formula (II): —X is in particular chosen from the group consisting of: —SO2—N(R?b)—, R?b being H or a (C1-C6)alkyl group, —N(R?b)—SO2—, R?b being H or a (C1-C6)alkyl group, —CO—NH—, and —NH—CO—, for use for the treatment of pathologies characterized by bronchoconstriction, such as asthma.
Type:
Grant
Filed:
June 6, 2018
Date of Patent:
March 21, 2023
Assignees:
INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE NANTES, CHU NANTES
Inventors:
Vincent Sauzeau, Gervaise Loirand, Jacques Lebreton, Arnaud Tessier, Agnes Quemenier
Abstract: The present application provides a medicament having an anti-inflammatory bowel disease function, and a preparation method therefor and an application thereof. The medicament has a structure as represented in formula I or formula II. The medicament and a pharmaceutically acceptable salt, a solvate, a prodrug, a tautomer, a stereoisomer, or a pharmaceutical composition thereof provided by the present application have a good effect on inflammatory bowel diseases, can be used for preparing medicaments for treating the inflammatory bowel diseases, and have important clinical significance and wide application prospects.
Type:
Grant
Filed:
July 28, 2018
Date of Patent:
March 14, 2023
Assignee:
SUZHOU PHARMAVAN CO., LTD
Inventors:
Shiping Deng, Yu Cao, Zhi Li, Yunhui Yu, Kui Zhang, Minjie Zhang, Gaogang Yuan, Tao Xu, Gang Yu, Chuanliang Jiang
Abstract: The invention generally relates to compositions for inducing vasoconstriction. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.
Abstract: The present invention provides a prophylactic or therapeutic agent for hypoxic injury, ischemia-reperfusion injury or inflammation, an agent for protecting cells for transplantation, and an agent for preserving organism. A prophylactic or therapeutic agent for hypoxic injury, ischemia-reperfusion injury or inflammation, an agent for protecting cells for transplantation, or an agent for preserving organism, containing, as an active ingredient, at least one kind selected from a heterocyclic compound represented by the formula (I) wherein each symbol is as described in the DESCRIPTION, or a salt thereof; an isothiocyanate compound represented by the formula S?C?N—R5 (II) wherein the symbol is as described in the DESCRIPTION; and a TRPA1 agonist.
Abstract: The present invention relates to crystalline polymorph forms of (S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide (GDC-0077), having the structure, Formula I: or stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, and processes of preparing the polymorph forms.
Type:
Grant
Filed:
May 15, 2020
Date of Patent:
February 28, 2023
Assignee:
Genentech, Inc.
Inventors:
Paroma Chakravarty, Chong Han, Sean M. Kelly, Karthik Nagapudi, Scott Savage
Abstract: The present invention provides compounds of Formula I: pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.
Abstract: The present invention concerns a PTGDR-1 antagonist, a PTGDR-2 antagonist, a dual PTGDR-1/PTGDR-1 antagonist, or a combination of PTGDR-1 antagonist and PTGDR-2 antagonist, and pharmaceutical compositions containing them, for use for preventing and/or treating SLE.
Type:
Grant
Filed:
April 13, 2020
Date of Patent:
January 24, 2023
Assignees:
INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), UNIVERSITE PARIS CITE
Inventors:
Nicolas Charles, Christophe Pellefigues
Abstract: Compounds of Formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
Type:
Grant
Filed:
June 3, 2020
Date of Patent:
January 17, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Evangelos Aktoudianakis, Aesop Cho, Zhimin Du, Michael Graupe, Lateshkumar Thakorlal Lad, Paulo A. Machicao Tello, Jonathan William Medley, Samuel E. Metobo, Prasenjit Kumar Mukherjee, Devan Naduthambi, Eric Q. Parkhill, Barton W. Phillips, Scott Preston Simonovich, Neil H. Squires, Peiyuan Wang, William J. Watkins, Jie Xu, Kin Shing Yang, Christopher Allen Ziebenhaus
Abstract: Provided herein are spirolactone compounds of Formula I that are useful as inhibitors of ACC1 and/or ACC2. The spirolactone compounds described herein can be used for treating a disease or disorder associated with aberrant ACC1 and/or ACC2 activities, for example, non-alcoholic steatohepatitis (NASH), acne, obesity, diabetes, and cancer. Also provided herein are pharmaceutical compositions comprising the spirolactone compound of Formula I, or pharmaceutically acceptable salt thereof.
Abstract: The present invention relates to a composition for injectable formulation, the composition comprising: —An aqueous solution of ibuprofen and arginine with a molar ratio of ibuprofen:arginine comprised between 1:1.1 and 1:2.1; —An aqueous solution of a diuretic compound comprising between 3.9% and 4.35% w/v of the diuretic compound. The present invention also concerns a pharmaceutical composition comprising said composition and the use of said composition and said pharmaceutical composition.
Abstract: It is provided a pharmaceutical composition comprising 3-beta-hydroxy-5-alpha-pregnan-20-one, at least one sterol or an ester thereof and a mixture of acylglycerols with a solid fat content of less than 25% at 25° C. and 0% at 37° C. In addition it is provided a method for preparing the pharmaceutical composition.
Abstract: The present invention provides methods and composition suitable for stabilizing cell-containing samples such as blood samples. The stabilizers used are primary or secondary carboxylic acid amides.
Type:
Grant
Filed:
March 18, 2014
Date of Patent:
December 13, 2022
Assignee:
QIAGEN GmbH
Inventors:
Ralf Wyrich, Thorsten Voss, Kalle Günther, Uwe Oelmüller
Abstract: A drug product and method for treating a parasitic disease in a host is described. The drug product comprises: a carrier matrix; and a drug substance having the formula: wherein: R1 is selected from the group consisting of H, aliphatic of 1 to 100 carbons and arene comprising up to 100 carbons; each R3 is independently selected from the group consisting of H, aliphatic of 1 to 100 carbons and arene comprising up to 100 carbons; Y represents those elements necessary to form a 5 or 6 membered ring; X is selected from the group consisting of B, O, N, S, Se and P; and n is 1-4 as necessary to complete the valence of X.
Type:
Grant
Filed:
March 6, 2020
Date of Patent:
November 29, 2022
Assignee:
Clemson University
Inventors:
Daniel C. Whitehead, James C. Morris, Chandima J. Narangoda
Abstract: Neuropeptide FF receptor modulators based on a proline scaffold are provided which offer NPFF receptor potencies in the nanomolar range and antagonistic selectivity for the NPFF1 receptor. Methods, compounds and compositions for modulating the function of neuropeptide FF receptors are provided for pharmacotherapies capable of influencing conditions or disorders affected by the neuropeptide FF receptors.
Abstract: The present invention discloses a composition comprising 70%-80% w/w tetrahydrocurcuminoids, 10%-20% w/w hexahydrocurcuminoids and 5%-10% w/w octahydrocurcuminoids and its therapeutic application. More specifically, the present invention discloses the use of a composition comprising 70%-80% w/w tetrahydrocurcuminoids, 10%-20% w/w hexahydrocurcuminoids and 5%-10% w/w octahydrocurcuminoids in the therapeutic management of interstitial lung disease or lung fibrosis.
Type:
Grant
Filed:
October 15, 2020
Date of Patent:
November 8, 2022
Assignee:
SAMI-SABINSA GROUP LIMITED
Inventors:
Muhammed Majeed, Kalyanam Nagabhushanam, Lakshmi Mundkur, Rajendran Ramanujam