Abstract: Provided herein are inhibitors of protein arginine deiminases (PADs), pharmaceutical compositions comprising said the compounds, and methods for using the compounds for the treatment of diseases.
Abstract: The present disclosure provides for a compound according to formula (I) or a pharmaceutically acceptable salt thereof as Cav1.2 activators for the treatment of schizophrenia, bipolar disorder, major depressive disorder, substance use disorder, ADHD, Phelan-McDermid Syndrome, autism spectrum disorder, multiple sclerosis, frontotemporal dementia, Alzheimer's disease, Brugada Syndrome, Short QT syndrome, and early repolarization syndrome.
Type:
Grant
Filed:
June 11, 2021
Date of Patent:
September 27, 2022
Assignee:
NOVARTIS AG
Inventors:
Thomas Charles Caya, James Neef, Tejaskumar Pankajbhai Pathak, Amir Masoud Sadaghiani, Xilin Zhou
Abstract: Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, and Formula IV or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.
Type:
Grant
Filed:
August 29, 2019
Date of Patent:
September 20, 2022
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, Joel Charles Barrish, William Greenlee, Kyle J. Eastman
Abstract: This invention relates to the large-scale production of psilocybin for use in medicine. Move particularly, it relates to a method of obtaining high purity crystalline psilocybin, particularly, in the form of Polymorph A. It further relates to a method for the manufacture of psilocybin and intermediates in the production thereof and formulations containing psilocybin.
Type:
Grant
Filed:
November 19, 2021
Date of Patent:
September 20, 2022
Assignee:
COMPASS PATHFINDER LIMITED
Inventors:
Derek John Londesbrough, Christopher Brown, Julian Scott Northen, Gillian Moore, Hemant Kashinath Patil, David E. Nichols
Abstract: The invention provide novel pyrimidine derivatives and analogs having inhibitory activities towards certain tyrosine kinases, e.g., Bruton's tyrosine kinase (Btk) and/or Focal adhesion kinase (FAK), extracellular signal-regulated kinase (ERK), pharmaceutical compositions thereof, and methods of treatment, reduction or prevention of certain diseases or conditions mediated by such by tyrosine kinases, e.g., cancers, tumors, fibrosis, inflammatory diseases, autoimmune diseases, diabetes, or immunologically mediated diseases.
Abstract: The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of ATR kinase for the treatment or prevention of cancer.
Type:
Grant
Filed:
September 1, 2020
Date of Patent:
September 6, 2022
Assignees:
Board of Regents, The University of Texas System, ChemPartner Corporation
Inventors:
Maria Emilia Di Francesco, Philip Jones, Christopher Lawrence Carroll, Jason Bryant Cross, Suyambu Kesava Vijayan Ramaswamy, Michael Garrett Johnson, Sarah Lively, David Lapointe
Abstract: Provided are a novel process for preparing a diaminopyrimidine derivative or acid addition salt thereof having an activity as a 5-HT4 receptor agonist, crystalline forms of a hydrochloride of the diaminopyrimidine derivative, and processes for preparing the same.
Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to (E)-1-(4-(1-(((4-cyclohexyl-3-(trifluoromethyl)benzyl)oxy)imino)ethyl)-2-ethylbenzyl)azetidine-3-carboxylic acid.
Abstract: The present application relates to psilocin derivatives of Formula (I), to processes for their preparation, to compositions comprising them and to their use in activation of a serotonin receptor in a cell, as well as to treating diseases, disorders or conditions by activation of a serotonin receptor in a cell.
Abstract: Provided herein are compounds and pharmaceutical compositions useful for treating meibomian gland dysfunction (MGD), comprising administering to a subject in need thereof a therapeutically effective amount of a compound of Formula (I) or a compound of Formula (I?), or pharmaceutical composition described herein.
Type:
Grant
Filed:
November 23, 2020
Date of Patent:
August 30, 2022
Assignee:
NOVARTIS AG
Inventors:
Kelly D. Boss, Yi Fan, Alec Nathanson Flyer, Declan Hardy, Zhihong Huang, Kathryn Taylor Linkens, Jon Christopher Loren, Fupeng Ma, Valentina Molteni, Duncan Shaw, Jeffrey Smith, Catherine Fooks Solovay
Abstract: N-oxides, or salts thereof, wherein G, L2, R1, R5, R9, R10, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
Type:
Grant
Filed:
December 18, 2018
Date of Patent:
August 23, 2022
Assignee:
Bristol-Myers Squibb Company
Inventors:
Alaric J. Dyckman, Dharmpal S. Dodd, Christopher P. Mussari, Trevor C. Sherwood, Tasir Shamsul Haque, Shoshana L. Posy, Sreekantha Ratna Kumar, Laxman Pasunoori, Subramanya Hegde, Rushith Kumar Anumula
Abstract: Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R? pair are independently selected from (i) or (ii); (i) R and R? are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R? together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.
Type:
Grant
Filed:
October 12, 2020
Date of Patent:
August 23, 2022
Assignee:
RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
Abstract: Adducts are described, obtainable from the reaction product of a secondary amine and a diketone, with carbon allotropes in which the carbon is sp2 hybridized, such as graphene, graphite, fullerene, carbon nanotubes and the like, and an inorganic oxide-hy-droxide. A process for preparing said adducts is also described.
Type:
Grant
Filed:
November 9, 2017
Date of Patent:
August 16, 2022
Assignees:
PIRELLI TYRE S.p.A., POLITECNICO DI MILANO
Abstract: The present disclosure relates to a novel compound and a pharmaceutical composition comprising the same. The compound according to the present disclosure has effects for activating autophagy, and thus can be valuably used for preventing or treating diseases associated with autophagy regulation.
Type:
Grant
Filed:
May 31, 2019
Date of Patent:
August 9, 2022
Assignee:
AUTOPHAGYSCIENCES INC.
Inventors:
Jung Ju Kim, Seong-Won Song, Hye Jeong Shin, Hyeongwan Choi
Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
Type:
Grant
Filed:
July 30, 2018
Date of Patent:
August 9, 2022
Assignee:
AMGEN INC.
Inventors:
Michael D. Bartberger, Hilary Plake Beck, Michael R. Degraffenreid, Brian M. Fox, Felix Gonzalez Lopez De Turiso, Lisa D. Julian, Frank Kayser, Julio C. Medina, Steven H. Olson, Yosup Rew, Philip M. Roveto, Daqing Sun, Xuelei Yan
Abstract: Provided herein are (alpha-substituted aralkylamino or heteroarylalkylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, e.g., a compound of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for treating proliferative diseases.
Abstract: The present invention discloses compounds of Formula (Ia), and pharmaceutically acceptable salts, thereof: which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (Ia) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (Ia) or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
September 20, 2021
Date of Patent:
July 12, 2022
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Guoqiang Wang, Ruichao Shen, Yong He, Xuri Gao, Jun Ma, Xuechao Xing, Hui Cao, Joseph D. Panarese, Yat Sun Or
Abstract: The various aspects present inventions provide various crystalline forms of (S)-(?)-amisulpride, (R)-(+)-amisulpride, and solvates thereof and methods of making same. In various aspects, the inventions also provide methods of resolving racemic amisulpride.
Type:
Grant
Filed:
August 17, 2020
Date of Patent:
June 28, 2022
Assignee:
Sunovion Pharmaceuticals Inc.
Inventors:
John R. Snoonian, Harold Scott Wilkinson, Haitao Zhang
Abstract: Provided is a compound of Chemical Formula 1: wherein: each X is independently N or CH, with the proviso that at least one X is N; Y is O or S; L1 and L2 are each independently a single bond, a substituted or unsubstituted C6-60 arylene, or a substituted or unsubstituted C2-60 heteroarylene containing at least one heteroatom selected from the group consisting of N, O, and S; Ar1 and Ar2 are each independently a substituted or unsubstituted C6-60 aryl, or a substituted or unsubstituted C2-60 heteroaryl containing at least one heteroatom selected from the group consisting of N, O, and S; and Ar3 is a substituted or unsubstituted C6-60 aryl, or a substituted or unsubstituted C2-60 heteroaryl containing at least one heteroatom selected from the group consisting of N, O, and S; and to an organic light emitting device including the same.
Type:
Grant
Filed:
March 6, 2019
Date of Patent:
June 28, 2022
Assignee:
LG CHEM, LTD.
Inventors:
Min Woo Jung, Dong Hoon Lee, Boon Jae Jang, Jungha Lee, Su Jin Han, Seulchan Park