Abstract: The present application relates to securinine or norsecurinine analogues that, when administered to immature myeloid cells, promote differentiation of these cells to mature cells that do not readily proliferate. Therefore, the agents are useful in the treatment of myeloid disorders including myeloproliferative disorders, acute myeloid leukemia, and autoimmune diseases. The agents may also be used as a myeloablative agent in conjunction with a bone marrow transplant or stem cell therapy.
Abstract: Provided is a heterocyclic amide compound that may have a PRS inhibitory action and is expected to be useful as a prophylactic or therapeutic agent for PRS associated diseases and the like including cancer. A compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof.
Abstract: The present invention relates to crystalline forms of Afatinib and its dimaleate salt. The present invention also relates to processes for the preparation of crystalline forms of Afatinib and its dimaleate salt. The present invention further relates to pharmaceutical compositions of such crystalline forms of Afatinib dimaleate and use thereof in the treatment of a patient in need thereof.
Type:
Grant
Filed:
June 10, 2016
Date of Patent:
October 13, 2020
Assignee:
Fresenius Kabi Oncology Ltd.
Inventors:
Walter Cabri, Saswata Lahiri, Bhuwan Bhaskar Mishra, Abul Azim, Nilendu Panda, Poli Reddy Bhavanam, Krishanu Ray, Nikunj Kachhadia, Kumber Singh
Abstract: The present disclosure relates to crystalline forms of venetoclax and process for their preparation. The present disclosure also relates to process for preparation of amorphous venetoclax.
Abstract: Provided are certain compounds or pharmaceutically acceptable salts thereof which can inhibit kinase activity of Bruton's tyrosine kinase (BTK) and may be useful for the treatment of diseases like cancer, immunological disease and inflammation.
Abstract: An oxoisoquinoline compound of the following formula: or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising the oxoisoquinoline compound or salt; and a method for treating B-cell lymphoma comprising administering the oxoisoquinoline compound or salt to a patient.
Abstract: Disclosed is a pH-responsive fluorescent compound, represented by the general formula, which is a novel pH-responsive fluorescent compound capable of being specifically localized in mitochondria within cells, which exhibits strong fluorescence under weakly acidic pH environments in lysosomes, and which is not readily subject to interference from autofluorescence and background fluorescence due to other fluorescent substances within cells. Also disclosed are a composition for detecting mitophagy using the pH-responsive fluorescent compound, and a method for detecting mitophagy within cells. In the general formula, L represents a linker, X represents a pharmaceutically acceptable anion, and Y represents a reactive group that may react with a functional group on a mitochondrial protein to form a covalent bond.
Abstract: The present invention relates to: an organic compound represented by Chemical Formula 1; a composition for an organic optoelectronic diode containing the organic compound; and an organic optoelectronic diode to which the organic compound or the composition is applied. In Chemical Formula 1, Z, R1 to R11, and n1 to n4 are the same as those defined in the specification.
Type:
Grant
Filed:
November 18, 2015
Date of Patent:
September 22, 2020
Assignee:
SAMSUNG SDI CO., LTD.
Inventors:
Sujin Han, Dong Min Kang, Soohyun Min, Eun Sun Yu, Byoungkwan Lee, Hanill Lee, Sung-Hyun Jung, Ho Kuk Jung
Abstract: The present application provides a compound of Formula (I) as an inhibitor against wild-type EGFR and/or mutant EGFR, which may be used for treating human non-small cell lung cancer individually or in combination with other therapeutic agent(s). The compound of Formula (I) of the present application may be used for treating patients of drug-resistant human non-small cell lung cancer harboring wild-type EGFR and/or EGFR T790M mutation and/or EGFR L858R mutation and/or EGFR delE746_A750 mutation.
Type:
Grant
Filed:
December 27, 2016
Date of Patent:
September 22, 2020
Assignee:
PRECEDO PHARMACEUTICALS CO., LTD.
Inventors:
Qingsong Liu, Jing Liu, Xixiang Li, Aoli Wang, Hong Wu, Kailin Yu, Chen Hu, Wenchao Wang, Cheng Chen, Fengming Zou, Ziping Qi, Li Wang, Beilei Wang
Abstract: The present invention relates to sulphate salts of N-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1H-benzo[d]imidazol-2-amine and pharmaceutically acceptable solvates thereof, preparation thereof, pharmaceutical compositions containing them and use of the same in the treatment and/or prevention of neurodegenerative diseases.
Type:
Grant
Filed:
August 27, 2019
Date of Patent:
September 15, 2020
Assignees:
Alzprotect, Universite De Lille 2 Droit Et Sante, INSERM (Institut National De La Sante Et De La Recherche)
Inventors:
Stéphane Burlet, Cécilia Estrella, Mathieu Barrier, Patricia Melnyk, Nicolas Sergeant, Luc Buee, Philippe Verwaerde
Abstract: The invention relates to triazole compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as modulators of demyelinating diseases: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention, methods of using the compositions and kits thereof in the treatment of various demyelinating and neurodegenerative diseases, including multiple sclerosis.
Type:
Grant
Filed:
October 17, 2018
Date of Patent:
September 8, 2020
Assignee:
VERTEX PHARMACEUTCALS INCORPORATED
Inventors:
Robert J. Davies, Jingrong Cao, Meghan Elise Cockerill, Philip Noel Collier, Elisabeth Doyle, James Daniel Frantz, Huai Gao, Brian Anthony Goldman, Ronald Lee Grey, Jr., Anne-Laure Grillot, Wenxin Gu, James A. Henderson, Raul Eduardo Krauss, Adrianne Lynn Kolpak, Yusheng Liao, Sanjay Shivayogi Magavi, David Messersmith, Albert Charles Pierce, Emanuele Perola, Elizabeth Jin-Sun Ryu, Joshua Syken, Jian Wang, Michael Paul DeNinno, Francois Maltais
Abstract: The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1, R2 and n have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use as anti-proliferative and/or cell-killing agents.
Type:
Grant
Filed:
August 1, 2019
Date of Patent:
September 8, 2020
Assignee:
AstraZeneca AB
Inventors:
Robert Hugh Bradbury, Alfred Arthur Rabow, Michael James Waring, James Francis McCabe, Steven Christopher Glossop, Arshed Mahmood, Zoe Ann Cotter
Abstract: Disclosed are substituted fused hexacyclic benzimidazole derivatives of Formula (I) wherein the variables A, B, D, X, M, Q, n, p, q, Z, E, R5, and R12 are defined herein. These compounds are potent modulators of human TNF? activity and of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
Type:
Grant
Filed:
March 31, 2017
Date of Patent:
September 8, 2020
Assignee:
UCB Biopharma SRL
Inventors:
Teresa De Haro Garcia, Michael Louis Robert Deligny, Jag Paul Heer, Helen Tracey Horsley, Sophie Jadot, Jean Keyaerts
Abstract: The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease.
Type:
Grant
Filed:
October 2, 2018
Date of Patent:
September 1, 2020
Assignee:
MyoKardia, Inc.
Inventors:
Johan Oslob, Danielle Aubele, Jae Kim, Robert McDowell, Yonghong Song, Arvinder Sran, Min Zhong
Abstract: The present invention provides a compound of general formula (I) (wherein, R1, X, p and q are as described in the present description and claims), or a pharmacologically acceptable salt thereof, and a pharmaceutical composition containing that compound.
Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Type:
Grant
Filed:
January 2, 2019
Date of Patent:
September 1, 2020
Assignee:
NOVARTIS AG
Inventors:
Atwood Kim Cheung, Donovan Noel Chin, Natalie Dales, Aleem Fazal, Timothy Brian Hurley, John Kerrigan, Gary O'Brien, Lei Shu, Robert Sun, Moo Je Sung
Abstract: Disclosed are an EGFR inhibitor free base or acid salt polycrystalline form, a preparation method therefor, and an application thereof. The present invention specifically relates to an N-(5-((4-(1-cyclopropyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide free base or acid salt polycrystalline form, a preparation method therefor, and an application of the polycrystalline form in preparing a drug for treating an EGFR mutant activity-mediated disease. The present invention is used for inhibiting the activity of an L858R EGFR mutant, a T790M EGFR mutant and an exon 19 deletion activating mutant etc., may be widely applied in preventing and treating cancer, especially non-small cell lung cancer and other related diseases, and is expected to develop into a new generation of EGFR inhibitors.
Abstract: The invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS symptoms in a mammal using compounds of Formula I.
Type:
Grant
Filed:
March 26, 2019
Date of Patent:
August 25, 2020
Assignee:
Gilead Sciences, Inc.
Inventors:
Elizabeth M. Bacon, Elbert Chin, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, John O. Link, Nathan Shapiro, Teresa Alejandra Trejo Martin, Zheng-Yu Yang
Abstract: Embodiments of calcium channel agonists, as well as methods of making and using the calcium channel agonists, are disclosed. The disclosed calcium channel agonists and corresponding salt forms have a structure according to general formula I: wherein each bond depicted as “” is a single bond or a double bond as needed to satisfy valence requirements; Z1, Z2, Z3, Z4, and Z5 independently are nitrogen or carbon; R1 and R3 are alkyl; R2 is alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; and R4 is alkyl or hydroxyalkyl.
Type:
Grant
Filed:
November 16, 2018
Date of Patent:
August 25, 2020
Assignee:
University of Pittsburgh—Of the Commonwealth System of Higher Education
Inventors:
Peter Wipf, Stephen D. Meriney, Mary Liang