Abstract: Platinum(IV) complexes especially suitable for antitumor therapy and methods for their preparation. Further provided is a method for treating a subject, in particular a human, suffering from a disease including administering a platinum(IV) complex of the present invention, which disease is especially preferably but not exclusively a cancer. Further provided is a method of inhibiting the growth of tumor cells by contacting the cells with a platinum(IV) complex of the present invention and a pharmaceutical composition including a platinum(IV) complex of the present invention. The platinum(IV) complexes of the present invention represent a novel class of platinum anticancer prodrugs for the treatment of diseases especially of cancer. The platinum(IV) complexes of the present invention exhibit advantageously high cytotoxic activity in various cancer types superior to commonly used platinum-based complexes. In addition, the complexes proved to be highly effective even against cisplatin-resistant cancers.
Abstract: Therapeutic compounds containing a phenyl core and amide link(s). Also described are pharmaceutical compositions incorporating the therapeutic compounds and a method for treating cancer with the compounds. These compounds are cytotoxic to stomach, colon, breast, and leukemia cancer cell lines via dual inhibition of Src kinases and tubulin.
Type:
Grant
Filed:
July 16, 2021
Date of Patent:
January 4, 2022
Assignee:
King Abdulaziz University
Inventors:
Moustafa E. El-Araby, Abdelsattar M. Omar, Maan T. Khayat, Dhaval Shah, Martin K. Safo, Azizah M. Malebari, Farid Ahmed
Abstract: The invention relates to a novel process for preparing a-carboxamide pyrrolidine derivatives, in particular (2S, 5R)-5-(4-((2-fluorobenzyl)oxy)phenyl)pyrrolidine-2-carboxamide, and to novel intermediates for use in said process along with processes for preparing said intermediates.
Type:
Grant
Filed:
October 5, 2018
Date of Patent:
December 7, 2021
Assignee:
Biogen Inc.
Inventors:
Weirong Chen, Vinny Couming, Erwin Irdam, William F. Kiesman, Daw-Long A. Kwok, Tamera L. Mack, Suzanne M. Opalka, Daniel B. Patience, Donald G. Walker, Wenli Liang
Abstract: In some aspects, the present disclosure provides compositions comprising an N4-based MMC ligand, a cell targeting group, and a fluorophore or a therapeutic compound comprising a formula: wherein the variables are as defined herein. In some embodiments, these compositions may be used in the imaging techniques or in the treatment of a disease or disorder such as cancer.
Type:
Grant
Filed:
July 26, 2019
Date of Patent:
December 7, 2021
Assignee:
THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
Inventors:
Ali Azhdarinia, Sukhen C. Ghosh, Nathaniel L. Wilganowski, Eva M. Sevick-Muraca
Abstract: The invention relates to a process for preparing propylene oxide, comprising (i) providing a stream comprising propene, propane, hydrogen peroxide or a source of hydrogen peroxide, water, and an organic solvent; (ii) passing the liquid feed stream provided in (i) into an epoxidation zone comprising an epoxidation catalyst comprising a titanium zeolite, and subjecting the liquid feed stream to epoxidation reaction conditions in the epoxidation zone, obtaining a reaction mixture comprising propene, propane, propylene oxide, water, and the organic solvent; (iii) removing an effluent stream from the epoxidation zone, the effluent stream comprising propene, propane, propylene oxide, water, and the organic solvent; (iv) separating propene and propane from the effluent stream by distillation, comprising subjecting the effluent stream to distillation conditions in a distillation unit, obtaining a gaseous stream (S1) which is enriched in propene and propane compared to the effluent stream subjected to distillation con
Type:
Grant
Filed:
April 13, 2018
Date of Patent:
November 23, 2021
Assignee:
BASF SE
Inventors:
Nicolai Tonio Woerz, Ulrich Mueller, Andrei-Nicolae Parvulescu, Dominic Riedel, Marvin Kramp, Daniel Urbanczyk, Ulrike Wegerle, Christian Mueller, Bernd Metzen, Markus Weber, Joaquim Henrique Teles
Abstract: Provided are compounds of Formulas (I?), (I), (II?) and (II), or pharmaceutically acceptable salts thereof, and methods for their use and production.
Type:
Grant
Filed:
February 6, 2018
Date of Patent:
November 9, 2021
Assignee:
BIOGEN MA INC.
Inventors:
Felix Gonzalez Lopez de Turiso, Martin Himmelbauer, Michael J. Luzzio
Abstract: This application relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, which modulate the activity of adenosine receptors, such as subtypes A2A and A2B receptors, and are useful in the treatment of diseases related to the activity of adenosine receptors including, for example, cancer, inflammatory diseases, cardiovascular diseases, and neurodegenerative diseases.
Abstract: The present disclosure belongs to the field of chemical synthesis, and in particular relates to an ammonium carboxylate compound, a crystalline form and an amorphous form, and a preparation method thereof. The present disclosure prepares the compound and the crystalline form I and its single crystal, amorphous form and crystalline form II thereof. The compound, the crystalline forms, the single crystal and the amorphous form can stably exist and exhibit good solid forms, suitable for medicine-making. Furthermore, these products possess high purity and less single impurity. Moreover, the preparation methods of the present disclosure are easy to implement due to the simple processes with mild reaction conditions, and could produce products of high yield and high purity without complex purification steps. Furthermore, the preparation methods may facilitate safety, environmental protection, and industrial production.
Type:
Grant
Filed:
April 27, 2018
Date of Patent:
November 2, 2021
Assignee:
WUHAN LL SCIENCE AND TECHNOLOGY DEVELOPMENT CO., LTD.
Inventors:
Bo Zhang, Xiaohua Ding, Dongcheng Dai, Sijun Lei, Xueming Liu, Panpan Duan, Yongkai Chen, Chaodong Wang
Abstract: The present invention relates to a new crystal form of bis(diphenylimidazolidinetrithione-?S4, ?S5)-, (SP-4-1)-nickel(II), a printing ink formulation for security printing and security documents, comprising the new crystal form of bis(diphenylimidazolidinetrithione-?S4, ?S5)-, (SP-4-1)-nickel(II) as well as its use as IR absorber.
Type:
Grant
Filed:
September 18, 2018
Date of Patent:
November 2, 2021
Assignee:
BASF SE
Inventors:
Helmut Reichelt, Hans Reichert, Oliver Seeger, Korinna Dormann, Rene Fischer, Christian Doerr
Abstract: The present disclosure relates to STING (Stimulator of Interferon Genes) agonist compounds, methods of making the compounds and their methods of use.
Type:
Grant
Filed:
July 31, 2020
Date of Patent:
October 26, 2021
Assignee:
Mersana Therapeutics, Inc.
Inventors:
Jeremy R. Duvall, Keith W. Bentley, Brian D. Jones, Eugene W. Kelleher, Soumya S. Ray, Joshua D. Thomas, Dorin Toader
Abstract: The present disclosure relates to novel substituted N-(3-fluoropropyl)-pyrrolidine compounds of formula (I-A), wherein R1 and R2 represent independently a hydrogen atom or a deuterium atom; A represents an oxygen or nitrogen atom; and SERM-F represents a selective estrogen receptor modulator fragment comprising an aryl or heteroaryl group linked to the adjacent “A” group. The disclosure also relates to the preparation and to the therapeutic uses of the compounds of formula (I-A) as inhibitors and degraders of estrogen receptors.
Type:
Grant
Filed:
May 16, 2019
Date of Patent:
October 19, 2021
Assignee:
Sanofi
Inventors:
Monsif Bouaboula, Maurice Brollo, Victor Certal, Youssef El-Ahmad, Bruno Filoche-Romme, Frank Halley, Gary McCort, Laurent Schio, Michel Tabart, Corinne Terrier, Fabienne Thompson
Abstract: Therapeutic compounds containing a phenyl core and amide link(s). Also described are pharmaceutical compositions incorporating the therapeutic compounds and a method for treating cancer with the compounds. These compounds are cytotoxic to stomach, colon, breast, and leukemia cancer cell lines via dual inhibition of Src kinases and tubulin.
Type:
Grant
Filed:
March 4, 2021
Date of Patent:
October 5, 2021
Assignee:
King Abdulaziz University
Inventors:
Moustafa E. El-Araby, Abdelsattar M. Omar, Maan T. Khayat, Dhaval Shah, Martin K. Safo, Azizah M. Malebari, Farid Ahmed
Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 or Ubiquitin Specific Peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (I): (I) or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c, R1d, R1e, R1f, R1g, R2, X, L and A are as defined herein.
Type:
Grant
Filed:
December 16, 2016
Date of Patent:
September 28, 2021
Assignee:
MISSION THERAPEUTICS LIMITED
Inventors:
Mark Ian Kemp, Martin Lee Stockley, Andrew Madin
Abstract: The present invention relates to novel crystal forms of ozanimod. Compared with the prior art, the crystal forms of the present invention have one or more improved properties. The present invention also relates to preparation methods of the crystal forms, pharmaceutical compositions thereof and uses thereof for the manufacture of medicament for treating and/or preventing diseases or adverse conditions associated with modulation, activation, stimulation, inhibition or antagonization of selective sphingosine-1-phosphate (S1P) receptor.
Abstract: Compositions including an odd chain fatty acid, and salts and derivatives thereof, and methods for metabolic syndrome treatment and prophylaxis are provided, including compositions and methods for treating diabetes, obesity, hyperferritinemia, elevated insulin, glucose intolerance, dyslipidemia and related conditions. Methods for the diagnosis and monitoring of metabolic syndrome are also provided.
Type:
Grant
Filed:
August 7, 2019
Date of Patent:
September 14, 2021
Assignee:
United States of America as represented by the Secretary of the Navy
Abstract: In some embodiments, the invention relates to a BTK inhibitor or a pharmaceutically acceptable salt, cocrystal, ester, prodrug, solvate, hydrate or derivative thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, in some embodiments, the present invention relates to imidazopyrazine compounds, pharmaceutical compositions thereof, and the use of the compounds and pharmaceutical compositions in the treatment of a hyperproliferative disorder, an inflammatory disorder, an immune disorder, or an autoimmune disorder.
Type:
Grant
Filed:
June 30, 2020
Date of Patent:
September 7, 2021
Assignee:
Acerta Pharma B.V.
Inventors:
Tjeerd Barf, Edwin de Zwart, Saskia Verkaik, Niels Hoogenboom, Dennis Demont
Abstract: The invention provides (+)-?-dihydrotetrabenazine succinate salt. Also provided are (+)-?-dihydrotetrabenazine succinate salt for use in medicine, pharmaceutical compositions comprising (+)-?-dihydrotetrabenazine succinate salt and a pharmaceutically acceptable excipient and the uses of (+)-?-dihydrotetrabenazine succinate salt as a VMAT2 receptor antagonist and in the treatment of a movement disorder such as Tourette's syndrome. The invention further provides a method for preparing the (+)-?-dihydrotetrabenazine succinate salt.
Abstract: The present application relates to amidine substituted analogues as shown in formula I and uses thereof as an anti-inflammatory agent and/or for the treatment of an immunological disorder or of an inflammatory bowel disease including ulcerative colitis, Crohn's diseases, collagenous colitis and lymphocytic colitis.
Type:
Grant
Filed:
December 21, 2017
Date of Patent:
August 24, 2021
Assignee:
Verlyx Pharma Inc.
Inventors:
François Ravenelle, Michel Therien, Helmi Zaghdane
Abstract: The present invention relates to pharmaceutical products comprising a combination of (i) a MET inhibitor and (ii) an EGFR inhibitor, or a pharmaceutically acceptable salt thereof, respectively, or a prodrug thereof, which are jointly active in the treatment of proliferative diseases, corresponding pharmaceutical formulations, uses, methods, processes, commercial packages and related invention embodiments.
Type:
Grant
Filed:
June 18, 2020
Date of Patent:
August 24, 2021
Assignee:
Novartis AG
Inventors:
Ralph Tiedt, Christian Chatenay-Rivauday, Moriko Ito, Mikhail Akimov, Bin Peng, Ying Gong