Abstract: The invention relates to a novel process for preparing Spiro derivatives, in particular 7-methyl-2-[4-methyl-6-[4-(trifluoromethyl)-phenyl]pyrimidin-2-yl]-1,7-diazaspiro[4.4]nonan-6-one, and to novel intermediates for use in said process along with processes for preparing said intermediates.
Type:
Grant
Filed:
October 10, 2018
Date of Patent:
October 19, 2021
Assignee:
Biogen Inc.
Inventors:
Gerard M. Giblin, David T. MacPherson, Osama Suleiman, Michael Williams, David R. Witty, Thierry Bonnaud, Richard Edwards
Abstract: The present disclosure relates to salts of compounds of Formula (I) prepared as a xinafoate (1-hydroxy-2-naphthoate) salt (Formula (Ia)), pharmaceutically acceptable compositions comprising same and methods of using the same.
Type:
Grant
Filed:
July 17, 2019
Date of Patent:
October 19, 2021
Assignee:
AstraZeneca AB
Inventors:
Anna Matilda Angelica Pettersen, James McCabe, Carl-Johan Aurell
Abstract: Disclosed is a compound of Formula (I), or a stereoisomer thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions comprising thereof. Also disclosed is a method of treating PI3K? related disorders or diseases by using the compound disclosed herein.
Abstract: The present invention relates to heterocyclic compounds of Formula I useful as anti-infective agents. The present invention further relates to a method of treating an infection by administering such compounds, and to pharmaceutical compositions comprising such compounds.
Type:
Grant
Filed:
June 22, 2017
Date of Patent:
September 28, 2021
Assignee:
Bioimics AB
Inventors:
Leif Kirsebom, Ram Shankar Upadhayaya, Raghava Reddy Kethiri, Anders Virtanen
Abstract: The disclosure relates to compounds of formula (I), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, and related diseases.
Type:
Grant
Filed:
June 8, 2018
Date of Patent:
September 21, 2021
Assignee:
Bristol-Myers Squibb Company
Inventors:
Pravin Sudhakar Shirude, Amit Kumar Chattopadhyay, Nicholas R. Wurtz
Abstract: The present invention discloses a compound of the formula: and optionally comprising a pharmaceutically acceptable salt or hydrate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt or hydrate thereof.
Abstract: Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, Y and Z are as described herein. In certain embodiments, a compound disclosed herein inhibits a cellular TAM receptor, and can be used to treat disease mediated by or involving the TAM receptor family.
Abstract: Provided herein are compounds of the formulas: wherein: n, X2, R3, R3?, R4, R4?, R5, R5?, R6, and R6? are as defined herein. Pharmaceutical compositions of the compounds are also provided. In some aspects, these compounds may be used for the treatment of diseases, including diabetic peripheral neuropathy or cancer.
Type:
Grant
Filed:
January 29, 2020
Date of Patent:
August 24, 2021
Assignee:
UNIVERSITY OF KANSAS
Inventors:
Brian S. J. Blagg, Rick T. Dobrowsky, Mercy Anyika
Abstract: Methods of inhibiting MMP-9 are provided. The methods of inhibiting MMP-9 include methods of inhibiting IL-6/TNF-? crosstalk mediated expression and/or secretion of MMP-9. The inhibition of the IL-6/TNF-? crosstalk pathway may be accomplished using an IL-6 signaling inhibitor, such as AG490 or SC-144. The methods may also include the treatment of dieses through the inhibition of IL-6/TNF-? crosstalk mediated production of MMP-9. In an embodiment the methods may include preventing the progression of cancer or cardiovascular disease through the inhibition of the IL-6/TNF-? crosstalk pathway.
Abstract: The invention relates to novel N-(?-peroxy)carbazole compounds of Formula I and methods for use. The N-(?-peroxy)carbazole compounds described herein are useful for treating or preventing parasitic infections, bacterial infections, and cancer in subjects. The methods include administering an N-(?-peroxy)carbazole compound as described herein to a subject. Also described herein are methods for synthesizing N-(?-peroxy)carbazole compounds.
Type:
Grant
Filed:
January 20, 2020
Date of Patent:
August 24, 2021
Assignee:
KING ABDULLAH UNIVERSITY OF SCIENCE AND TECHNOLOGY
Abstract: The embodiments disclosed herein provide compounds as shown in formula I or a tautomer, a mesomer, a racemate, an enantiomer, a diastereomer, a deuterated compound, a prodrug or a mixture thereof, or a pharmaceutically acceptable salt or solvate of the compounds as shown in formula I or a tautomer, a mesomer, a racemate, an enantiomer, a diastereomer, a deuterated compound, a prodrug or a mixture thereof, wherein R1 to R7 are as defined in the description. This application also provides a preparation method and a medical use of the compounds. The compounds of this disclosure have an activity superior or equivalent to the candidate drug LY2835219 currently under phase III clinical trial, and some of the compounds exhibit better selectivity. Moreover, the preferred compounds exhibit good absorption and good blood-brain distribution when administered orally.
Type:
Grant
Filed:
November 28, 2016
Date of Patent:
August 17, 2021
Assignee:
Gan & Lee Pharmaceuticals
Inventors:
Lei Yin, Wenjian Liu, Heng Li, Dianxi Zhu
Abstract: The present invention relates to a new crystalline form of N-[5-(3,5-difluoro-benzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide, process for its preparation, its utility in treating diseases caused by deregulated protein kinase activity and pharmaceutical compositions containing it.
Type:
Grant
Filed:
June 26, 2020
Date of Patent:
August 17, 2021
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Ilaria Candiani, Giovanni Ottaiano, Attilio Tomasi
Abstract: The present invention relates to crystalline brexpiprazole having a particle size distribution (PSD) characterized by a d(90) of 30 ?m to 100 ?m, by a d(10) of at least 1.0 ?m, and by a d(4,3) of at least 15.0 ?m. The present invention also relates to a pharmaceutical composition comprising a crystalline brexpiprazole having a PSD characterized by a d(90) of 30 ?m to 100 ?m, by a d(10) of at least 1.0 ?m, and by a d(4,3) of at least 15.0 ?m, and to an aqueous suspension comprising said crystalline brexpiprazole. The present invention also relates to a composition comprising a crystalline brexpiprazole having a PSD characterized by a d(90) of 30 ?m to 100 ?m, by a d(10) of at least 1.0 ?m, and by a d(4,3) of at least 15.0 ?m, wherein said composition is essentially free from secondary particles of brexpiprazole.
Abstract: Crystalline 2-hydroxy-N,N-dimethylethanaminium 1-(2-(5-(tert-butyl)-thiophene-2-carboxamido)-3-(4-(5-(4?-ethyl-[1,1?-bi(cyclohexan)]-3-en-4-yl)pyrimidin-2-yl)phenyl)propanoyl)azetidine-3-carboxylate salt, and methods related to synthesis and therapeutic use of the same.
Type:
Grant
Filed:
September 29, 2017
Date of Patent:
July 20, 2021
Assignee:
RECEPTOS LLC
Inventors:
Ephraim Vidal, Roger Bakale, Philip Turnbull, David Moser, Andrew Robbins, Craig Grant
Abstract: The present invention is directed to substituted 5-trifluoromethyl oxadiazole compounds of generic formula (I) or a pharmaceutically acceptable salt thereof. In particular, the invention is directed to a class of aryl and heteroaryl substituted 5-trifluoromethyl oxadiazole compounds of formula I which may be useful as HDAC6 inhibitors for treating cellular proliferative diseases, including cancer, neurodegenerative diseases, such as schizophrenia and stroke, as well as other diseases.
Type:
Grant
Filed:
June 19, 2017
Date of Patent:
July 20, 2021
Assignee:
MERCK SHARP & DOHME CORP.
Inventors:
Abbas Walji, Richard Berger, Craig A. Stump, Kelly-Ann S. Schlegel, James J. Mulhearn, Thomas J. Greshock, Deping Wang, Mark E. Fraley, Kristen G. Jones
Abstract: This invention relates to pharmaceutical compositions containing (?)-?-dihydrotetrabenazine, processes for making them and their therapeutic uses.
Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
Type:
Grant
Filed:
May 4, 2017
Date of Patent:
July 20, 2021
Assignee:
Bristol-Myers Squibb Company
Inventors:
David K. Williams, Weifang Shan, Liping Zhang, Emily Charlotte Cherney, James Aaron Balog
Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g., cancer).
Type:
Grant
Filed:
April 23, 2019
Date of Patent:
July 13, 2021
Assignee:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
David J. Lauffer, Guy Bemis, Michael Boyd, David Deininger, Hongbo Deng, Warren Dorsch, Wenxin Gu, Russell R. Hoover, Mac Arthur Johnson, Jr., Mark Willem Ledeboer, Brian Ledford, Francois Maltais, Marina Penney, Darin Takemoto, Nathan D. Waal, Tiansheng Wang, Pan Li
Abstract: PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
Type:
Grant
Filed:
October 28, 2019
Date of Patent:
July 13, 2021
Assignee:
Novartis AG
Inventors:
Michael Joseph Luzzio, Julien Papillon, Michael Scott Visser
Abstract: A compound of Formula (I): pharmaceutically acceptable salts thereof, deuterated analogs thereof, compositions thereof, and methods of treating disease using a compound thereof are disclosed.
Type:
Grant
Filed:
August 9, 2019
Date of Patent:
July 6, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Stephen Ammann, Elizabeth M. Bacon, Gediminas Brizgys, Elbert Chin, Chienhung Chou, Jeromy J. Cottell, Marilyn Ndukwe, James G. Taylor, Nathan E. Wright, Zheng-Yu Yang, Sheila M. Zipfel