October 2023 US Patents by Issue Date (2024)

Aromatic substituted alkane-core monomers and polymers thereof for volume Bragg gratings

Patent number: 11780819

Abstract: The disclosure provides recording materials including aromatic substituted alkane-core derivatized monomers and polymers for use in volume Bragg gratings, including, but not limited to, volume Bragg gratings for holography applications. Several structures are disclosed, including Formula I. When used in Bragg gratings applications, the monomers and polymers disclosed lead to materials with higher refractive index, low birefringence, and high transparency. The disclosed derivatized monomers and polymers can be used in any volume Bragg gratings materials, including two-stage polymer materials where a matrix is cured in a first step, and then the volume Bragg grating is written by way of a second curing step of a monomer.

Type: Grant

Filed: November 13, 2020

Date of Patent: October 10, 2023

Assignee: META PLATFORMS TECHNOLOGIES, LLC

Inventors: Lafe Purvis, Austin Lane, Matthew E. Colburn

2,6-disubstituted pyridine derivative

Patent number: 11780820

Abstract: The present invention relates to a pyridine derivative of formula (1) wherein R1 is optionally-substituted C1-6 alkyl, optionally-substituted C3-10 cycloalkyl, or optionally-substituted 5- to 10-membered saturated or partially-unsaturated heterocyclyl; R2 is halogen atom, cyano, C1-6 alkyl which may be optionally substituted with 1 to 3 the same or different halogen atoms, C1-6 alkoxy which may be optionally substituted with 1 to 3 the same or different halogen atoms, or amino which may be optionally substituted with 1 to 2 the same or different C1-6 alkyl; and the bind with broken line is single or double bond, or a pharmaceutically acceptable salt thereof, which is useful as a medicament for treating symptoms in anxiety-related disorder.

Type: Grant

Filed: April 23, 2021

Date of Patent: October 10, 2023

Assignee: SUMITOMO PHARMA CO., LTD.

Inventors: Hidefumi Yoshinaga, Hiro Uemachi, Tomomi Ohno, Jeremy Besnard

Inhibitors of fibroblast activation protein

Patent number: 11780821

Abstract: Compounds and compositions for modulating fibroblast activation protein (FAP) are described. The compounds and compositions may find use as therapeutic agents for the treatment of diseases, including hyperproliferative diseases.

Type: Grant

Filed: December 14, 2018

Date of Patent: October 10, 2023

Assignee: PRAXIS BIOTECH LLC

Inventors: Jennifer Alfaro, Sebastian Belmar, Sebastian Bernales, Brahmam Pujala, Dayanand Panpatil, Bhawana Bhatt

HDAC inhibitor solid state forms

Patent number: 11780822

Abstract: The present disclosure relates to various solid-state forms of N-hydroxy 2-{6-[(6-fluoro-quinolin-2-ylmethyl)-amino]-3-aza-bicyclo[3.1.0]hex-3-yl}pyrimidine-5-carboxamide and methods of making the same. Such forms of N-hydroxy 2-{6-[(6-fluoro-quinolin-2-ylmethyl)-amino]-3-aza-bicyclo[3.1.0]hex-3-yl}pyrimidine-5-carboxamide are useful in preparation of pharmaceutical compositions and dosage forms for the treatment of cancer, immune disorders and inflammation.

Type: Grant

Filed: December 13, 2022

Date of Patent: October 10, 2023

Assignee: VIRACTA SUBSIDIARY, INC.

Inventors: Xiaohu Deng, Stewart Jones, David Slack

Indazole-3-carboxamides and their use as Wnt/?-catenin signaling pathway inhibitors

Patent number: 11780823

Abstract: Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

Type: Grant

Filed: June 14, 2021

Date of Patent: October 10, 2023

Assignee: BioSplice Therapeutics, Inc.

Inventors: John Hood, Sunil Kumar KC

Process for preparing osimertinib or a salt thereof

Patent number: 11780824

Abstract: Provided herein are improved processes and methods for preparing osimertinib or a salt thereof, in particular osimertinib mesylate. The improved process removes the necessity of isolating the unstable aniline intermediate of formula (III) and enables the direct coupling to form the amide product of formula (II): The present invention is suitable for a large-scale production, avoiding the isolation of unstable intermediate, thereby providing osimertinib or a mesylate salt thereof in both high yields and high purity.

Type: Grant

Filed: December 16, 2020

Date of Patent: October 10, 2023

Assignee: ScinoPharm Taiwan, Ltd.

Inventors: Kuan-Hsun Huang, Chung-Yang Huang, Tsung-Cheng Hu

Thyroid hormone receptor agonists and use thereof

Patent number: 11780825

Abstract: The application relates to a compound of Formula (I?) or (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of thyroid hormone receptors, a pharmaceutical composition comprising a compound of Formula (I?) or (I), and a method of treating or preventing a disease or disorder regulated by thyroid hormone.

Type: Grant

Filed: January 13, 2021

Date of Patent: October 10, 2023

Assignee: Eccogene (Shanghai) Co., Ltd.

Inventors: Jingye Zhou, Jiuxiang Zhu, Mingwei Zheng

Bisamide sarcomere activating compounds and uses thereof

Patent number: 11780826

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.

Type: Grant

Filed: February 15, 2022

Date of Patent: October 10, 2023

Assignees: AMGEN INC., CYTOKINETICS, INC.

Inventors: Luke Ashcraft, Alessandro Boezio, John Butler, Aroop Chandra, Chihyuan Chuang, Scott E. Collibee, Mikkel Debenedetto, Vincent Dimassa, Russell Graceffa, Justin Malinowski, David Moebius, Bradley P. Morgan, Joshua Payette, Antonio Romero, David St. Jean, Jr., Richard Vargas, John Yeoman, Hanmo Zhang, Alan Cheng, Felix Gonzalez Lopez De Turiso, Michael Garrett Johnson

Substituted 3-phenoxyazetidin-1-yl-pyrazines

Patent number: 11780827

Abstract: The invention relates to substituted 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) for use as a medicament, pharmaceutical compositions comprising the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.

Type: Grant

Filed: March 29, 2021

Date of Patent: October 10, 2023

Assignees: Boehringer Ingelheim International GmbH, Arena Pharmaceuticals, Inc.

Inventors: Kai Gerlach, Graeme Semple, Yifeng Xiong, Barbara Bertani, Marco Ferrara, Giacomo Fossati, Scott Hobson, Uta Friederike Lessel, Frank Runge, Ursula Mueller-Vieira, Julian Wippich

Contraceptive compounds and methods

Patent number: 11780828

Abstract: The invention provides a compound of formula (I): or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, wherein R1-R6 have any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as contraceptive agents.

Type: Grant

Filed: May 3, 2022

Date of Patent: October 10, 2023

Assignee: REGENTS OF THE UNIVERSITY OF MINNESOTA

Inventors: Ingrid Gunda Georg, Narsihmulu Cheryala

Organic electroluminescent materials and devices

Patent number: 11780829

Abstract: A compound of Formula X wherein ring A is absent, or present and selected from a 5-membered or 6-membered, carbocyclic or heterocyclic ring, which is optionally substituted; ring B is absent, or present and selected from a 5-membered or 6-membered, carbocyclic or heterocyclic ring, which is optionally substituted; and at least one of ring A or ring B is present, and the hash line represents ring A fused to ring N—W1—W3 and ring B fused to ring N—W4—W6; W1, W2, W3, W4, W5, and W6 are independently selected from CR1 or N; Z is selected from CRZ or N; and Y is selected from a group consisting of C(R2)2, B(R2)2, Al(R2)2, Si(R2)2, and Ge(R2)2. An optoelectronic device selected from the group consisting of a photovoltaic device, a photodetector device, a photosensitive device, and an OLED, the optoelectronic device including an organic layer that comprises a compound of Formula X. A consumer product that includes the optoelectronic device.

Type: Grant

Filed: January 16, 2020

Date of Patent: October 10, 2023

Assignee: The University of Southern California

Inventors: Mark E. Thompson, Abegail Tadle, Karim El Roz, Peter Ivan Djurovich, Daniel Sylvinson Muthiah Ravinson, Jessica H. Golden, Stuart W. Sawyer

Triazolone derivatives or salts thereof and pharmaceutical compositions comprising the same

Patent number: 11780830

Abstract: The present technology provides triazolone derivatives or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and the use thereof. The triazolone derivatives or their pharmaceutically acceptable salts exhibit selective inhibitory activity on VAP-1 and therefore can be usefully applied, e.g. for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).

Type: Grant

Filed: March 22, 2021

Date of Patent: October 10, 2023

Assignee: Yuhan Corporation

Inventors: Tae Dong Han, Hee Jae Tak, Eun Kyung Kim, Su Bin Choi, Sol Park, Dong Hoon Kim, So Young Kim, Hyun Ho Choi, Tae Wang Kim, Mi Kyeong Ju, Na Ry Ha, Eui Chui Lee

Compound, display panel and display apparatus

Patent number: 11780831

Abstract: Provided is a compound represented by formula 1, and a display panel and a display apparatus including the compound. In formula 1, L1 and L2 are each independently selected from the group consisting of a single bond, C6-C30 aryl, and C4-C30 heteroaryl; a and b are each independently selected from 0, 1, 2, 3, or 4; D1 and D2 are each independently a nitrogen-containing electron donor unit selected from the group consisting of carbazolyl and derivative groups thereof, acridinyl and derivative groups thereof, diarylamino and derivative groups thereof, and triarylamino and derivative groups thereof; and c and d are each independently selected from 0, 1, 2, 3, or 4, and c+d?1.

Type: Grant

Filed: September 29, 2020

Date of Patent: October 10, 2023

Assignees: SHANGHAI TIANMA AM-OLED CO., LTD., WUHAN TIANMA MICRO-ELECTRONICS CO., LTD

Inventors: Wei Gao, Lei Zhang, Wenpeng Dai, Quan Ran, Lu Zhai, Wenjing Xiao, Jinghua Niu

Lactivicin compounds, their preparation and use as antibacterial agents

Patent number: 11780832

Abstract: Lactivicin compounds of formula (I) and pharmaceutically acceptable salts of the compounds of formula (I) are provided, wherein the compounds comprise antibiotics suitable for use either alone or in combination with ?-lactamase inhibitors and/or other antibiotics (including ?-lactam and non-?-lactam antibiotics) in the treatment or prevention of bacterial infections.

Type: Grant

Filed: March 29, 2022

Date of Patent: October 10, 2023

Assignee: FEDORA PHARMACEUTICALS INC.

Inventors: Renata Jankowska, Sameeh M. Salama, Samarendra N. Maiti

Emetine derivatives, prodrugs containing same, and methods of treating conditions using same

Patent number: 11780833

Abstract: Compounds are provided herein which are emetine derivatives that can be used as prodrugs which selectively undergo activation to release emetine in specific cellular conditions. In one aspect, a blocking group is incorporated onto the emetine molecule by the derivization of the N2?-position with moieties that can be selectively removed by hydrolysis in the cancer/tumor microenvironment. Such compounds are less cytotoxic than emetine and are substantially inactive in non-cancerous cells. In one aspect, the compounds described herein can be used for the treatment of metastatic and non-metastatic cancers, including, for example, breast cancer, prostate cancer, lung cancer, and leukemia.

Type: Grant

Filed: July 25, 2018

Date of Patent: October 10, 2023

Assignee: HOWARD UNIVERSITY

Inventors: Oladapo Bakare, Samuel Ray Denmeade, Emmanuel S. Akinboye

Solid forms of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3- yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol and processes for preparing fused tricyclic compounds comprising a substituted phenyl or pyridinyl moiety, including methods of their use

Patent number: 11780834

Abstract: Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.

Type: Grant

Filed: December 3, 2020

Date of Patent: October 10, 2023

Assignees: Genentech, Inc., Hoffmann-La Roche Inc.

Inventors: Cheol Keun Chung, Jie Xu, Hans Iding, Kyle Clagg, Michael Dalziel, Alec Fettes, Francis Gosselin, Ngiap-Kie Lim, Andrew McClory, Haiming Zhang, Paroma Chakravarty, Karthik Nagapudi, Sarah Robinson

Pyrazolo[3,4-b]pyridine compounds as inhibitors of TAM and MET kinases

Patent number: 11780835

Abstract: Provided herein are compounds of the Formula (I): and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein R1, R2, R9, X1 and G are as defined herein, which are inhibitors of one or more TAM kinases and/or c-Met kinase, and are useful in the treatment and prevention of diseases which can be treated with a TAM kinase inhibitor and/or a c-Met kinase inhibitor.

Type: Grant

Filed: July 15, 2021

Date of Patent: October 10, 2023

Assignee: Array BioPharma Inc.

Inventors: Ronald Jay Hinklin, Shelley Allen, Patrick Barbour, Adam Cook, Joshua Dahlke, John Gaudino, Ellen Laird, Oren T. McNulty, Qian Zhao

Process of preparing a PD-1/PD-L1 inhibitor

Patent number: 11780836

Abstract: The present invention relates to processes of preparing PD-1/PD-L1 inhibitor (R)-1-((7-cyano-2-(3?-(3-(((R)-3-hydroxypyrrolidin-1-yl)methyl)-1,7-naphthyridin-8-ylamino)-2,2?-dimethylbiphenyl-3-yl)benzo[d]oxazol-5-yl)methyl)pyrrolidine-3-carboxylic acid, or salts thereof, related synthetic intermediates, and salts of the intermediates, where the PD-1/PD-L1 inhibitor is useful in the treatment of various diseases including infectious diseases and cancer.

Type: Grant

Filed: November 5, 2021

Date of Patent: October 10, 2023

Assignee: Incyte Corporation

Inventors: Jiacheng Zhou, Shili Chen, Zhongjiang Jia, Yi Li, Qiyan Lin, Pingli Liu, Yongchun Pan, Timothy Martin, Bo Shen, Chongsheng Eric Shi, Naijing Su, Yongzhong Wu, Michael Xia

CXCR4 inhibitors and uses thereof

Patent number: 11780837

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.

Type: Grant

Filed: March 14, 2022

Date of Patent: October 10, 2023

Assignee: X4 Pharmaceuticals, Inc.

Inventors: Elyse Marie Josee Bourque, Renato Skerlj

Pyrrolo[3,2-b]quinoline compounds as antibacterial agents

Patent number: 11780838

Abstract: The pyrrolo[3,2-b]quinoline compounds are antibacterial agents. The emergence of drug-resistant bacteria calls for constant development of new antibacterial agents with the aim of generating medicaments that are potent against drug sensitive and resistant bacteria and are well tolerated. The present compounds are not only new, but have very valuable antimicrobial properties. These compounds showed a broad spectrum of activity against gram-positive and gram-negative bacteria, as well tuberculosis mycobacteria. They also showed potent activity against drug-resistant bacteria, such as MRSA and VRSA. The molecular target of these compounds was identified as DNA Gyrase B. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.

Type: Grant

Filed: March 23, 2023

Date of Patent: October 10, 2023

Assignee: KING FAISAL UNIVERSITY

Inventors: Michelyne Haroun, Christophe Tratrat

Compounds for treating Huntington's disease

Patent number: 11780839

Abstract: The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease. In particular, the present description relates to substituted monocyclic heteroaryl compounds of Formula (I) or Formula (II), forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease.

Type: Grant

Filed: March 27, 2019

Date of Patent: October 10, 2023

Assignee: PTC THERAPEUTICS, INC.

Inventors: Nadiya Sydorenko, Md Rauful Alam, Lukiana Amedzo, Suresh Babu, Ramil Y. Baiazitov, Scott J. Barraza, Anuradha Bhattacharyya, Gary Mitchell Karp, Nathaniel T. Kenton, Anthony R. Mazzotti, Young-Choon Moon, Nicholas W. Mszar, Jana Narasimhan, Sudipta Pal, Jigar S. Patel, Anthony Turpoff, Matthew G. Woll, Zhenrong Xu, Nanjing Zhang

Tricyclic urea compounds as JAK2 V617F inhibitors

Patent number: 11780840

Abstract: The present application provides tricyclic urea compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.

Type: Grant

Filed: July 1, 2021

Date of Patent: October 10, 2023

Assignee: Incyte Corporation

Inventors: Yanran Ai, Onur Atasoylu, Yu Bai, Joseph Barbosa, David M. Burns, Daniel Levy, Brent Douty, Hao Feng, Leah C. Konkol, Cheng-Tsung Lai, Xun Liu, Song Mei, Jun Pan, Haisheng Wang, Liangxing Wu, Wenqing Yao, Eddy W. Yue

3,6-methano-1H-pyrrolo[3,2-b]pyridine and 3,6-methano-1H-pyrrolo[3,2-c]pyridine compounds and medicaments using same

Patent number: 11780841

Abstract: The present disclosure provides a compound that is useful for the treatment and prophylaxis of rabies. The present disclosure provides a compound represented by formula XXIIF or formula XXIIB: wherein R1, R2A, R2B, R3, and R4 are defined in the specification, a solvent, or a pharmaceutically acceptable salt thereof, use of such a compound, solvate, or pharmaceutically acceptable salt thereof for the treatment or prophylaxis of rabies and cancer, a pharmaceutical composition comprising such a compound, solvate, or pharmaceutically acceptable salt thereof, and a method for the treatment or prophylaxis of rabies and cancer using the same.

Type: Grant

Filed: February 23, 2022

Date of Patent: October 10, 2023

Assignee: Irimajiri Therapeutics Inc.

Inventors: Hiroyuki Kouji, Kentaro Yamada, Akira Katoh, Toshimasa Ishizaki, Shigeru Matsuoka, Akira Nishizono, Tadashi Mishina, Atsushi Yoshimori

TYK2 pseudokinase ligands

Patent number: 11780842

Abstract: Described herein are TYK2 pseudokinase ligands and methods of utilizing TYK2 pseudokinase ligands in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

Type: Grant

Filed: March 25, 2020

Date of Patent: October 10, 2023

Assignee: VENTYX BIOSCIENCES, INC.

Inventors: Raju Mohan, John Nuss, Jason Harris, Shendong Yuan

Compounds active towards nuclear receptors

Patent number: 11780843

Abstract: Disclosed are compounds active towards nuclear receptors, pharmaceutical compositions containing the compounds and use of the compounds in therapy.

Type: Grant

Filed: March 31, 2021

Date of Patent: October 10, 2023

Assignee: NUEVOLUTION A/S

Inventors: Sanne Schrøder Glad, Ian Sarvary, Alex Haahr Gouliaev, Thomas Franch, Luigi Piero Stasi, Montserrat Erra Solà, Joan Taltavull Moll, Paul Robert Eastwood

Compounds and methods for treatment of viral infections

Patent number: 11780844

Abstract: Compounds and methods of using said compounds, singly or in combination with additional agents, and salts or pharmaceutical compositions of said compounds for the treatment of viral infections are disclosed.

Type: Grant

Filed: March 6, 2023

Date of Patent: October 10, 2023

Assignee: Gilead Sciences, Inc.

Inventors: Mark J. Bartlett, Daniel H. Byun, Yifan Deng, Jennifer L. Cosman Ellis, Rao V. Kalla, Richard L. Mackman, Dustin S. Siegel, Xianhuang Zeng

FGFR inhibitors and methods of use thereof

Patent number: 11780845

Abstract: The present disclosure relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of FGFR enzymes with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with FGFR signaling with the compounds and compositions of the disclosure.

Type: Grant

Filed: January 31, 2023

Date of Patent: October 10, 2023

Assignees: Relay Therapeutics, Inc., D.E. Shaw Research, LLC

Inventors: Bakary-Barry Touré, Heike Schoenherr, Fabrizio Giordanetto, Demetri T. Moustakas, Brandi M. Hudson

Compound, organic electroluminescent device including the same and electronic apparatus

Patent number: 11780846

Abstract: A compound having a structure represented by Formula I, and an organic electroluminescent device and an electronic apparatus including the same. The compound may be used as a hole transport material of an organic electroluminescent device. The compound provided by the present disclosure has a shallow LUMO, an appropriate hom*o energy level and a high triplet energy level ET, and can effectively improve hole transport ability, and block electron transition and exciton transport; meanwhile, the compound has high electron mobility, and excellent thermal stability and thin film stability. The compound provided by the present disclosure is used as the hole transport material of an organic electroluminescent device, so that the material has good solubility and appropriate mobility and the inter-pixel cross-talk is effectively avoided, which is conducive to improving light emitting efficiency and lifetime of the device.

Type: Grant

Filed: May 27, 2020

Date of Patent: October 10, 2023

Assignees: WUHAN TIANMA MICRO-ELECTRONICS CO., LTD., WUHAN TIANMA MICROELECTRONICS CO., LTD. SHANGHAI BRANCH

Inventors: Wenpeng Dai, Wei Gao, Jinghua Niu, Lei Zhang, Wenjing Xiao

Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1- carboxamide and solid state forms thereof

Patent number: 11780847

Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.

Type: Grant

Filed: February 27, 2023

Date of Patent: October 10, 2023

Assignee: AbbVie Inc.

Inventors: Jayanthy Jayanth, Mohamed-Eslam F. Mohamed, Ahmed A. Othman, Patrick J. Marroum, Peter T. Mayer, Ben Klünder

Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1- carboxamide and solid state forms thereof

Patent number: 11780848

Abstract: The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).

Type: Grant

Filed: March 1, 2023

Date of Patent: October 10, 2023

Assignee: AbbVie Inc.

Inventors: Mohamed-Eslam F. Mohamed, Ahmed A. Othman, Aileen L. Pangan, In-Ho Song, Ben Klünder, Jeffrey W. Voss, Robert J. Padley, Heidi S. Camp

Imino sulfanone inhibitors of ENPP1

Patent number: 11780849

Abstract: The present disclosure relates generally to inhibitors of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), compositions thereof, and methods of using said compounds and compositions thereof. More specifically, the present disclosure relates to sulfoximine-based inhibitors of ENPP1 and methods of their use for treating disease mediated by ENPP1.

Type: Grant

Filed: May 3, 2021

Date of Patent: October 10, 2023

Assignee: Volastra Therapeutics, Inc.

Inventors: Derek A. Cogan, Sarah Bettigole, Leon Van Berkom, Piotr Nieczypor, Michael Su, Rutger Folmer

Purification of rapamycin derivatives using temperature induced phase separation

Patent number: 11780850

Abstract: The present invention provides methods for obtaining purified rapamycin derivatives, including purified Biolimus A9. A crystalline form of Biolimus A9 is also described.

Type: Grant

Filed: June 28, 2021

Date of Patent: October 10, 2023

Assignee: Biosensors International Group, Ltd.

Inventors: Margaret W. Kayo, Richard S. Fornicola, Ivan Kovacik, Leelakrishna Kondaveti, Aniruddh Singh

LRRK2 inhibitors

Patent number: 11780851

Abstract: The present invention is directed to compounds of formula I The compounds are considered useful for the treatment of diseases associated with LRRK2 such as Parkinson's disease.

Type: Grant

Filed: October 26, 2022

Date of Patent: October 10, 2023

Assignee: H. Lundbeck A/S

Inventors: Thomas Jensen, Mikkel Jessing, Wanwan Yu, David Rodriguez Diaz, Jacob Nielsen, Christopher Richard Jones, Thomas Andersen, Mikkel Fog Jacobsen

Methods for treating Crohn's disease using 3-((1R,3s,5S)-3-((7-((5-methyl-1H-pyrazol-3-yl)amino)-1,6-naphthyridin-5-yl)amino)-8-azabicyclo[3.2.1]octan-8-yl)propanenitrile

Patent number: 11780852

Abstract: Disclosed are methods for treating Crohn's disease using a compound of the formula: or a pharmaceutically-acceptable salt thereof.

Type: Grant

Filed: February 10, 2021

Date of Patent: October 10, 2023

Assignee: Theravance Biopharma R&D IP, LLC

Inventors: Ryan Hudson, Jennifer Kozak, Dante D. Podesto, Xiaojun Huang, Venkat R. Thalladi

Substituted N-pyrimidin-4-yl-3-aminopyrrolo[3,4-C]pyrazoles as protein kinase C inhibitors

Patent number: 11780853

Abstract: The present invention relates to protein kinase C beta II inhibiting compounds of Formula (A): wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. The invention further relates to pharmaceutical compositions comprising the compounds of Formula (A), or pharmaceutically acceptable salts thereof, and methods for treating a disease or disorder selected from the group consisting of Alzheimer's disease, cancer, a cardiovascular disease, a central nervous system disorder, depression, a dermatological disease, diabetes mellitus, a complication arising from diabetes mellitus, a disease in which the liver is a target organ inflammation, an inflammatory disorder, ischemia, and a viral disease.

Type: Grant

Filed: December 1, 2021

Date of Patent: October 10, 2023

Assignee: PFIZER INC.

Inventors: Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin

Prolyl hydroxylase domain-containing protein (PHD) inhibitors and uses thereof

Patent number: 11780854

Abstract: Described herein are PHD inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of anemia.

Type: Grant

Filed: February 15, 2023

Date of Patent: October 10, 2023

Assignee: Insilico Medicine IP Limited

Inventors: Xiao Ding, Liena Qin, Feng Ren, Jianyu Xu

2-(2?-diarylaminophenyl) borabenzene derivative and organic electronic device including the derivative

Patent number: 11780855

Abstract: A compound useful as a hole transport material for an organic electronic device, in particular, an organic electroluminescent (EL) device. The compound of the present specification is represented by the following General Formula (1).

Type: Grant

Filed: September 14, 2018

Date of Patent: October 10, 2023

Assignee: LG Chem, Ltd.

Inventor: Hisayuki Kawamura

Compound and organic light-emitting device comprising same

Patent number: 11780856

Abstract: A compound of Chemical Formula 1 and an organic light emitting device including the same, the compound used as a material of an organic material layer of the organic light emitting device and providing high color purity and enhanced lifetime properties of the organic light emitting device.

Type: Grant

Filed: November 27, 2020

Date of Patent: October 10, 2023

Assignee: LG CHEM, LTD.

Inventors: Hye Min Cho, Sujeong Geum, Seonwoo Kim, Wanpyo Hong

Probe compounds for amino alcohols, and simultaneous fluorescence and circular dichroism analysis method

Patent number: 11780857

Abstract: The present disclosure relates to a novel probe compound, i.e., 1-(ortho-benzophenylaminoalkyl)-phenylboronic acid, or its derivative for a fluorescence and/or circular dichroism (CD) sensor for amine compounds containing aminoalcohols. Also, the present disclosure relates to a simultaneous fluorescence and CD analysis method of of amine compounds containing aminoalcohols using the novel probe compound to obtain concentration and optical purity of the amine compounds.

Type: Grant

Filed: April 17, 2020

Date of Patent: October 10, 2023

Assignee: EWHA UNIVERSITY—INDUSTRY COLLABORATION FOUNDATION

Inventors: Kwan Mook Kim, Juyoung Yoon, Eknath Shirbhate Mukesh, Ah-Young Song

Pyridinamine-pyridone and pyrimidinamine-pyridone compounds

Patent number: 11780858

Abstract: The invention provides novel pyridinamine-pyridone and pyrimidinamine-pyridone compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer, type II diabetes, inflammatory disease, neurodegenerative disorders, cardiovascular disorders, autoimmune diseases and viral infections; wherein R1, R2, R3 and Z are as defined in the specification.

Type: Grant

Filed: November 18, 2021

Date of Patent: October 10, 2023

Assignee: Sprint Bioscience AB

Inventors: Johan Lindström, Rickard Forsblom, Tobias Ginman, Fredrik Rahm, Jenny Viklund

Halogen free syntheses of aminosilanes by catalytic dehydrogenative coupling

Patent number: 11780859

Abstract: Compounds and method of preparation of Si—X and Ge—X compounds (X?N, P, As and Sb) via dehydrogenative coupling between the corresponding unsubstituted silanes and amines (including ammonia) or phosphines catalyzed by metallic catalysts is described. This new approach is based on the catalytic dehydrogenative coupling of a Si—H and a X—H moiety to form a Si—X containing compound and hydrogen gas (X?N, P, As and Sb). The process can be catalyzed by transition metal heterogenous catalysts such as Ru(0) on carbon, Pd(0) on MgO) as well as transition metal organometallic complexes that act as hom*ogeneous catalysts. The —Si—X products produced by dehydrogenative coupling are inherently halogen free. Said compounds can be useful for the deposition of thin films by chemical vapor deposition or atomic layer deposition of Si-containing films.

Type: Grant

Filed: February 4, 2022

Date of Patent: October 10, 2023

Assignee: L'Air Liquide, Société Anonyme pour l'Etude et l'Exploitation des Procédés Georges Claude

Inventors: Antonio Sanchez, Gennadiy Itov, Peng Zhang, Matthew Stephens, Manish Khandelwal

Substituted cyanophosphine additives for lithium conducting carbon phosphonitrides

Patent number: 11780860

Abstract: Cyanophosphines other than P(CN)3 react with lithium dicyanamide to produce lithiated carbon phosphonitrides with mobile Li+ ions.

Type: Grant

Filed: November 9, 2022

Date of Patent: October 10, 2023

Assignee: The Government of the United States of America, as represented by the Secretary of the Navy

Inventors: Brian L. Chaloux, Andrew P. Purdy, Albert Epshteyn

Phosphine reagents for azine fluoroalkylation

Patent number: 11780861

Abstract: A new set of bench-stable fluoroalkylphosphines that directly convert C—H bonds in pyridine building blocks, drug-like fragments, and pharmaceuticals, into fluoroalkyl derivatives. No pre-installed functional groups or directing motifs are required. The reaction tolerates a variety of sterically and electronically distinct pyridines and is exclusively selective for the 4-position in most cases. The reaction proceeds via initial phosphonium salt formation followed by sp2-sp3 phosphorus ligand-coupling, an underdeveloped manifold for C—C bond formation.

Type: Grant

Filed: October 20, 2021

Date of Patent: October 10, 2023

Assignee: Colorado State University Research Foundation

Inventors: Andrew McNally, Kyle Nottingham, Chirag Patel, Jeffrey Levy, Xuan Zhang

Inhibitors of MEK kinase

Patent number: 11780862

Abstract: Provided herein are inhibitors of MEK kinase, pharmaceutical compositions comprising said inhibitory compounds, and methods for using said MEK kinase inhibitory compounds for the treatment of disease.

Type: Grant

Filed: February 27, 2023

Date of Patent: October 10, 2023

Assignee: KINNATE BIOPHARMA INC.

Inventors: Toufike Kanouni, Robert S. Kania, Jason M. Cox

Quinone methide analog signal amplification

Patent number: 11780863

Abstract: Disclosed herein are novel quinone methide analog precursors and embodiments of a method and a kit of using the same for detecting one or more targets in a biological sample. The method of detection comprises contacting the sample with a detection probe, then contacting the sample with a labeling conjugate that comprises an enzyme. The enzyme interacts with a quinone methide analog precursor comprising a detectable label, forming a reactive quinone methide analog, which binds to the biological sample proximally to or directly on the target. The detectable label is then detected. In some embodiments, multiple targets can be detected by multiple quinone methide analog precursors interacting with different enzymes without the need for an enzyme deactivation step.

Type: Grant

Filed: November 7, 2018

Date of Patent: October 10, 2023

Assignee: Ventana Medical Systems, Inc.

Inventors: Christopher Bieniarz, Julia Ashworth-Sharpe, Brian D. Kelly, Nathan Polaske

Rhenium(V) alkylidyne complexes and methods of use and preparation thereof

Patent number: 11780864

Abstract: Non-d0 rhenium(V) alkylidyne catalysts useful for catalyzing alkyne metathesis reactions, such as hom*o- and cross-metathesis of alkynes or diynes, ring closing metathesis and ring-opening metathesis, methods or use, and preparation thereof. The catalysts are stable to air and moisture and tolerate a variety of functional groups in substrates.

Type: Grant

Filed: July 5, 2022

Date of Patent: October 10, 2023

Assignee: The Hong Kong University of Science and Technology

Inventors: Guochen Jia, Mingxu Cui

Organic electroluminescent materials and devices

Patent number: 11780865

Abstract: Novel ligands for metal complexes that are useful as phosphorescent emitters in OLEDs are disclosed. The ligands contain an aryl covalently bonded to the coordinating metal where the aryl group has at least two different alkyl side chains that are linked ortho and para compared to the linkage of the coordinating metal on that aryl group.

Type: Grant

Filed: December 15, 2017

Date of Patent: October 10, 2023

Assignee: UNIVERSAL DISPLAY CORPORATION

Inventors: Pierre-Luc T. Boudreault, Bert Alleyne, Scott Joseph, Harvey Wendt

Organometallic compound, organic light-emitting device including organometallic compound, and diagnostic composition including organometallic compound

Patent number: 11780866

Abstract: Provided are an organometallic compound represented by Formula 1, an organic light-emitting device including the organometallic compound, and a diagnostic composition including the organometallic compound: M(L1)n1(L2)n2??Formula 1 wherein, in Formula 1, M, L1, L2, n1 and n2 may each be understood by referring to the descriptions thereof provided herein.

Type: Grant

Filed: September 25, 2020

Date of Patent: October 10, 2023

Assignee: SAMSUNG ELECTRONICS CO., LTD.

Inventors: Sunyoung Lee, Yoonhyun Kwak, Juhyun Kim, Sangho Park, Sunghun Lee, Jeoungin Yi

Organometallic compound, organic light-emitting device including the organometallic compound, and diagnostic composition including the organometallic compound

Patent number: 11780867

Abstract: An organometallic compound represented by Formula 1: M(L1)n1(L2)n2??Formula 1 wherein M, L1, L2, n1, and n2 are the same as described in the specification.

Type: Grant

Filed: December 21, 2020

Date of Patent: October 10, 2023

Assignee: SAMSUNG ELECTRONICS CO., LTD.

Inventors: Whail Choi, Seungyeon Kwak, Jiwhan Kim, Hwayoung Cho, Hyeonho Choi, Kyuyoung Hwang, Yoonhyun Kwak, Ohyun Kwon

hom*oleptic metal coordination complexes as antifungal agents

Patent number: 11780868

Abstract: Provided herein are hom*oleptic metal coordination complexes that induce cellular apoptosis and cell cycle arrest in G0/G1 phase in fungus, such as Candida spp. Also disclosed are methods of inhibiting fungal growth and methods of treating fungal infections using the disclosed compounds. The disclosed compounds exhibit anti-Candida activity against fluconazole resistant and sensitive strains of C. albicans at low concentrations.

Type: Grant

Filed: April 28, 2023

Date of Patent: October 10, 2023

Assignee: KING ABDULAZIZ UNIVERSITY

Inventors: Irfan Ahmad Rather, Majid Rasool Kamli, Khalid Rehman Hakeem, Ahmad Firoz, Jamal S. M. Sabir, Mohmmad Younus Wani, Yong Ha Park, Yan Yan Hor