Patents Issued in August 27, 2024
  • Patent number: 12071383
    Abstract: A method for forming a high temperature coating includes forming a pre-sintered ceramic coating on a ceramic composite substrate. The pre-sintered ceramic coating includes a plurality of ceramic particles. The method further includes sintering at least a portion of the pre-sintered ceramic coating by heating the portion of the pre-sintered ceramic coating to a sintering temperature of the plurality of ceramic particles using joule heating. The sintering temperature is greater than about 1000 degrees Celsius (° C.).
    Type: Grant
    Filed: April 21, 2021
    Date of Patent: August 27, 2024
    Assignee: Honeywell International Inc.
    Inventors: Mehrad Mehr, Bahram Jadidian
  • Patent number: 12071384
    Abstract: The present invention relates to a fertilizer composition comprising nitrogen and phosphorus, wherein nitrogen is provided by basic L-amino acid(s) complexed to polyphosphate(s). The complex may be precipitated with multivalent metal ion(s) to provide a solid phase fertilizer composition. The basic L-amino acid is advantageously L-arginine and/or L-lysine. The fertilizer composition is capable of providing controlled release of nitrogen during prolonged periods of time.
    Type: Grant
    Filed: May 16, 2017
    Date of Patent: August 27, 2024
    Assignee: AREVO AB
    Inventors: Jonas Öhlund, Torgny Näsholm, Mattias Holmlund
  • Patent number: 12071385
    Abstract: The present disclosure is concerned with fertilizer compositions that provide controlled, delayed, and/or prolonged release of micronutrients in soil. In one embodiment, the inventive composition comprises a dry, powdered blend of a first target micronutrient source in chelated form and a second source of the same target micronutrient but provided in non-chelated form. In another embodiment, the inventive composition provides at least two sources of boron, with one source being a water-soluble form and the other source being a water-insoluble form. Regardless of the embodiment, the methods of using the fertilizer composition results in increased uptake of the particular micronutrient, nitrogen, and/or potassium compared to the prior art.
    Type: Grant
    Filed: January 18, 2019
    Date of Patent: August 27, 2024
    Assignee: Koch Agronomic Services, LLC
    Inventors: Tapasya Babu, Elliott Martin, Robert A. Geiger, Andres Reyes Gaige
  • Patent number: 12071386
    Abstract: The present disclosure relates to a process for preparing long-chain alkanes and alkenes from alcohols, aldehydes, or both. The process proceeds via acceptorless dehydrogenation and decarbonylative coupling using a supported catalyst.
    Type: Grant
    Filed: February 14, 2023
    Date of Patent: August 27, 2024
    Assignee: THE GEORGE WASHINGTON UNIVERSITY
    Inventors: Adelina M. Voutchkova, Diana Ainembabazi, Darren Dolan, Jonathan Horlyck
  • Patent number: 12071387
    Abstract: The present disclosure relates to a thermal coupling method for preparing ethylene by ethanol dehydration and device thereof. The device includes an ethanol dehydration reaction system, a quenching compression system, an alkaline washing system, a molecular sieve drying system and an ethylene purification and propylene refrigeration cycle system; ethanol dehydration reaction products in the ethanol dehydration reaction system serve as a heat source for preheating, vaporization and superheating of a raw material of ethanol; tower bottoms of an evaporation tower in the quenching compression system serve as a heat source for preheating of a feed stream of the evaporation tower and heating of an overhead gas of a quenching tower; products of ethylene in the alkaline washing system serve as a cold source for cooling of crude ethylene.
    Type: Grant
    Filed: June 19, 2023
    Date of Patent: August 27, 2024
    Assignee: TIANJIN UNIVERSITY
    Inventors: Minhua Zhang, Hao Gong, He Dong, Feng Shi, Fang Meng, Yingzhe Yu, Haoxi Jiang
  • Patent number: 12071388
    Abstract: A full continuous flow synthesis process of fluorine-containing aromatic hydrocarbon compounds.
    Type: Grant
    Filed: December 7, 2021
    Date of Patent: August 27, 2024
    Assignees: Fujian Zhongxin Fluoride Material Gaobao Technology Co., Ltd., Zhejiang Zhongxin Fluoride Materials Co., Ltd.
    Inventors: Qiliang Yuan, Yongyi Miao, Yonggen Shi, Yiqiang Zhang, Yinhao Chen, Chao Wang
  • Patent number: 12071389
    Abstract: The present disclosure relates in its first aspect to a process of converting a stream comprising methane into chemicals, said process being remarkable in that it comprises the steps of providing a first stream (1, 5, 11) comprising methane, providing a second stream (79) which is a bromine-rich stream, putting into contact said first stream (15) with said second stream (79) to obtain a third stream (21) comprising at least unreacted methane, methyl bromide, dibromomethane, and hydrogen bromide and removing said dibromomethane from said third stream (21), to produce a dibromomethane stream (103) and a fourth stream (27) comprising unreacted methane, methyl bromide and hydrogen bromide; wherein the fourth stream (27) is converted into chemicals. In its second aspect, the present disclosure concerns an installation for carrying out the process of the first aspect.
    Type: Grant
    Filed: July 11, 2023
    Date of Patent: August 27, 2024
    Assignees: TOTALENERGIES ONETECH, SULZER MANAGEMENT AG
    Inventors: Romuald Coupan, Nikolai Nesterenko, Gleb Veryasov
  • Patent number: 12071390
    Abstract: A process for preparing a fluorinating reagent from a calcium-containing compound is disclosed. The process bypasses the requirement to form hydrofluoric acid. The fluorinating reagent can be used to prepare high-value fluorochemicals.
    Type: Grant
    Filed: May 24, 2023
    Date of Patent: August 27, 2024
    Assignee: Oxford University Innovation Limited
    Inventors: Veronique Gouverneur, Gabriele Pupo, Duncan Browne, Jamie Leitch
  • Patent number: 12071391
    Abstract: The present disclosure provides industrially scalable methods of making (Z)-endoxifen or a salt thereof, crystalline forms of endoxifin, and compositions comprising them. The present disclosure also provides methods for treating hormone-dependent breast and hormone-dependent reproductive tract disorders.
    Type: Grant
    Filed: March 30, 2023
    Date of Patent: August 27, 2024
    Assignee: ATOSSA THERAPEUTICS, INC.
    Inventors: Steven C. Quay, Yao-Lin Sun, LungHu Wang, ChangJung Wu, ChuanDer Huang
  • Patent number: 12071392
    Abstract: The present disclosure provides adamantyl compounds having one or more amine groups and one or more nitrate groups. The aminoadamantyl nitrate compounds can be used to treat disorders of the central nervous system, including neurodegenerative and non-neurodegenerative diseases.
    Type: Grant
    Filed: September 19, 2022
    Date of Patent: August 27, 2024
    Assignee: Panorama Research, Inc.
    Inventors: Cyrus K. Becker, Meenakshi S. Venkatraman, Xiaoming Zhang, James W. Larrick, Stuart Arthur Lipton
  • Patent number: 12071393
    Abstract: The present invention generally relates to a process for selective and direct activation and subsequent amidation of aliphatic and aromatic carboxylic acids to afford an amide R3CONR1R2. That the process is capable of delivering gaseous or low-boiling point amines provides a major advantage over existing methodologies, which involves an intermediate of triacyloxyborane-amine complex [(R3CO2)3—B—NHR1R2]. This procedure readily produces primary, secondary, and tertiary amides, and is compatible with the chirality of the acid and amine involved. The preparation of known pharmaceutical molecules and intermediates has also been demonstrated.
    Type: Grant
    Filed: August 20, 2021
    Date of Patent: August 27, 2024
    Assignee: Purdue Research Foundation
    Inventors: Padinjaremadhom V. Ramachandran, Henry J. Hamann
  • Patent number: 12071394
    Abstract: Monoisocyanate impurities are removed from a process stream obtained when solvent is separated from a polyisocyanate product. The monoisocyanates are reacted with amine compounds at specific molar ratios to produce ureas. The ureas can be discarded by burning, landfilling or otherwise. Alternatively the ureas can be recycled back into the polyisocyanate manufacturing process, where they are formed into biuret compounds that can remain with the polyisocyanate product.
    Type: Grant
    Filed: July 31, 2019
    Date of Patent: August 27, 2024
    Assignees: Dow Global Technologies LLC, Dow, Portugal Produtos Quimicos, Sociedade Unipessoal
    Inventors: Robert E. Hefner, Jr., Helge Braun, Armenio Costa, Brian Cramm
  • Patent number: 12071395
    Abstract: A method for producing a carbodiimide compound, comprising a carbodiimide production step of reacting an aliphatic tertiary isocyanate compound (A) in the presence of an inorganic alkali metal compound (B) and at least one of a phase transfer catalyst (C), a compound (D-1) represented by general formula (2-1), and a compound (D-2) represented by general formula (2-2).
    Type: Grant
    Filed: March 12, 2019
    Date of Patent: August 27, 2024
    Assignee: NISSHINBO CHEMICAL INC.
    Inventors: Nobuyuki Matsumoto, Kenichi Yanagisawa
  • Patent number: 12071396
    Abstract: The present invention provides methods of efficiently producing various optically active aromatic amino acid derivatives by reacting, using an additive, a specific ester compound with an aromatic halide and zinc in the presence of a catalyst. The present invention also provides amino acid derivatives that can be produced by the methods.
    Type: Grant
    Filed: March 13, 2020
    Date of Patent: August 27, 2024
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventor: Manabu Wadamoto
  • Patent number: 12071397
    Abstract: The present invention relates to pharmaceutical compositions and methods useful for the treatment of dermatological disorders, and in particular acne vulgaris and skin pigmentation disorders. Pharmaceutical compositions comprising one or more arginine, salicylic acid and/or azelaic acid that are useful for the treatment of dermatological diseases and the symptoms and underlying causes of such dermatological diseases are also disclosed.
    Type: Grant
    Filed: April 16, 2021
    Date of Patent: August 27, 2024
    Assignee: Evologie LLC
    Inventors: Gary I. Weinberger, H. Robert Nagel, Richard A. Brown
  • Patent number: 12071398
    Abstract: A process for catalyzed reaction of CO and H2 into methanol includes the step of reacting the CO and H2 with a catalyst comprising a transition metal and at least one Lewis basic ligand together with at least one nucleophilic promoter so as to produce the methanol as a product.
    Type: Grant
    Filed: December 10, 2019
    Date of Patent: August 27, 2024
    Assignee: CREATIVEQUANTUM GMBH
    Inventors: Marek Pawel Checinski, Matthias Beller, Pavel Ryabchuk, Kathrin Junge
  • Patent number: 12071399
    Abstract: The present invention relates to a process for the preparation of arylsulfonylpro-penenitriles. The reaction starting from arylsulfonyl halides is catalyzed by a cat-alyst compound comprising a transition metal. The process is scalable, environ-mentally benign and provides the product in good yield.
    Type: Grant
    Filed: November 4, 2019
    Date of Patent: August 27, 2024
    Assignee: Kemira Oyj
    Inventors: Jaakko Hiltunen, Petteri Suominen, Ivan Ogibalov, Ain Uustare
  • Patent number: 12071400
    Abstract: The present invention describes a selective glycerol oxidation process comprising a set of steps. In the first step, a glycerol-containing raw material and an oxidizing agent are fed into a reaction vessel containing an iron oxide-containing catalyst. Subsequently, the glycerol-containing raw material, the oxidizing agent, and said iron oxide-containing catalyst are brought into contact at a temperature in the range of 100 to 350° C., wherein the glycerol-oxidation reaction occurs.
    Type: Grant
    Filed: November 12, 2019
    Date of Patent: August 27, 2024
    Assignees: PETRÓLEO BRASILEIRO S.A.—PETROBRAS, UNIVERSIDADE FEDERAL DE MINAS GERAIS—UFMG
    Inventors: Marcio De Figueiredo Portilho, Victor Augusto Araujo De Freitas, Luiz Carlos Alves De Oliveira
  • Patent number: 12071401
    Abstract: A calcium carboxylate is prepared by reacting water, calcium oxide, and a compound of formula (I): wherein R is a C1-C3 alkyl and R1 is a C1 or C2 alkyl. The reaction solution is heated to remove an amount of a co-product from the reaction solution. The calcium carboxylate may be recovered in a solid form from the reaction solution.
    Type: Grant
    Filed: September 1, 2023
    Date of Patent: August 27, 2024
    Assignee: NIACET CORPORATION
    Inventors: Kelly Brannen, David J. Harrigan, Donal S. Tunks, Stanley A. Sojka
  • Patent number: 12071402
    Abstract: The present invention relates to a solid phase pharmaceutical composition comprising one or more pharmaceutically acceptable excipients and an active pharmaceutical ingredient (“API”) which is a compound of formula A1 or A2 or a pharmacologically acceptable salt, solvate or hydrate thereof, wherein the API is not exposed to a basic compound.
    Type: Grant
    Filed: April 14, 2021
    Date of Patent: August 27, 2024
    Assignee: NOVARTIS AG
    Inventors: Philippe Michel Rene Bouillot, Emeric Reynaud
  • Patent number: 12071403
    Abstract: The present invention describes compounds modulating the function of mitochondrial complex I (NADH-quinone oxidoreductase) having formula (I)
    Type: Grant
    Filed: September 7, 2023
    Date of Patent: August 27, 2024
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Kai Gerlach, Christian Eickmeier, Jan Magnus Kriegl, Lothar Kussmaul, Klaus Rudolf, Bernhard Schmid
  • Patent number: 12071404
    Abstract: Disclosed are sulfonamide compounds with GPR17 modulating properties, which are useful for treating or preventing a variety of CNS and other diseases, in particular for preventing and treating myelinating diseases or disorders.
    Type: Grant
    Filed: October 20, 2021
    Date of Patent: August 27, 2024
    Assignee: UCB Pharma GmbH
    Inventors: Christa E. Mueller, Cécile Pegurier, Michael Louis Robert Deligny, Ali El-Tayeb, Joerg Hockemeyer, Marie Ledecq, Joël Mercier, Laurent Provins, Nader M. Boshta, Sanjay Bhattarai, Vigneshwaran Namasivayam, Mario Funke, Lukas Schwach, Sabrina Gollos, Daniel Von Laufenberg, Anaïs Barré
  • Patent number: 12071405
    Abstract: The present application relates to compounds of formula (I) containing a group selected from amino groups, bridged amino groups and carbazole groups, to processes for preparation thereof, and to the use thereof in electronic devices, and in particular OLEDs.
    Type: Grant
    Filed: September 5, 2018
    Date of Patent: August 27, 2024
    Assignee: Merck Patent GmbH
    Inventors: Elvira Montenegro, Teresa Mujica-Fernaud, Florian Maier-Flaig, Frank Voges
  • Patent number: 12071406
    Abstract: The present invention is related to crystalline forms of 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1-yl)-4-(o-tolyl)pyridin-3-yl)propanamide which is an NK-1 antagonist useful in the treatment of induced vomiting and other disorders.
    Type: Grant
    Filed: February 25, 2021
    Date of Patent: August 27, 2024
    Assignee: Helsinn Healthcare SA
    Inventors: Christian Bacilieri, Gionata Frasca
  • Patent number: 12071407
    Abstract: An 6-(4-hydroxyphenyl)-2-(2-cthoxycthoxy)-4-(4-methoxyphenyl)nicotinonitrile compound, its synthesis, and its use as an antimicrobial agent.
    Type: Grant
    Filed: December 5, 2023
    Date of Patent: August 27, 2024
    Assignee: KING FAISAL UNIVERSITY
    Inventors: Mai Mostafa Khalaf Ali, Hany Mohamed Abd El-Lateef Ahmed, Mohamed Gouda, Antar Ahmed Abdelhamid Ahmed
  • Patent number: 12071408
    Abstract: Disclosed are compounds of Formula III, their stereoisomers, tautomers, deuterates, pharmacologically acceptable salts, or hydrates thereof, methods of their preparation and pharmaceutical compositions comprising such compounds. The Formula III compounds are useful and highly effective as multi-targeted tyrosine kinase inhibitors in treating several kinds of cancers such as liver cancer, bladder cancer, thyroid cancer, cervical cancer, leukemia.
    Type: Grant
    Filed: August 11, 2022
    Date of Patent: August 27, 2024
    Assignee: Shanghai AB PharmaTech Ltd.
    Inventor: Zheng-Yun James Zhan
  • Patent number: 12071409
    Abstract: The present invention relates to quinoline derived small molecule inhibitors of nicotinamide N-methyltransferase (NNMT), the preparation thereof and uses thereof.
    Type: Grant
    Filed: June 7, 2022
    Date of Patent: August 27, 2024
    Assignee: The Board of Regents of the University of Texas
    Inventors: Stanley Watowich, Harshini Neelakantan, Hua-Yu Wang, Stanton Mchardy
  • Patent number: 12071410
    Abstract: Cost effective, semi-continuous flow methods and systems for synthesizing the antimalarial drug hydroxychloroquine (HCQ) in high yield are provided. The synthesis method that uses simple, inexpensive reagents to obtain the crucial intermediate 5-(ethyl(2-hydroxyethyl)-amino)pentan-2-one, vertical-integration of the starting material 5-iodopentan-2-one and the integration of continuous stirred tank reactors.
    Type: Grant
    Filed: February 25, 2019
    Date of Patent: August 27, 2024
    Assignee: Virginia Commonwealth University
    Inventors: Frank B. Gupton, Saeed Ahmad, Hari P. R. Gunuru, Nakul S. Telang
  • Patent number: 12071411
    Abstract: The present disclosure is directed to compounds that are inhibitors of HIF-2? having a structure according to Formula I, and compositions containing those compounds. Methods of using the compounds for the treatment of diseases, disorders, or conditions are also described.
    Type: Grant
    Filed: October 28, 2022
    Date of Patent: August 27, 2024
    Assignee: Arcus Biosciences, Inc.
    Inventors: Joel Worley Beatty, Samuel Lawrie Drew, Matthew Epplin, Jeremy Fournier, Balint Gal, Clayton Hardman, Artur Karenovich Mailyan, Kenneth Victor Lawson, Manmohan Reddy Leleti, Dongdong Liu, Guillaume Mata, Ma{hacek over (s)}a Podunavac, Jay Patrick Powers, Brandon Reid Rosen, Kai Yu
  • Patent number: 12071412
    Abstract: Provided herein are compounds of formula I, compositions comprising the compounds and method of treating various diseases with the compounds and compositions.
    Type: Grant
    Filed: February 1, 2023
    Date of Patent: August 27, 2024
    Assignee: NOBO Medicine Inc.
    Inventors: Alfred P. Spada, Robert J. Temansky, Michael Mueller
  • Patent number: 12071413
    Abstract: The present invention relates to a novel azole derivative as an apelin receptor agonist and a method for treating cardiovascular disease, diabetic disease, renal disease, hypertension, and arteriosclerosis, etc., using the same. The present invention provides a compound represented by formula (I) or a pharmacologically acceptable salt thereof wherein X1 represents —N? or —CH?, X2 represents —CH? or —N?, R1 and R2 each represent a C1 to C6 alkoxy group or the like, R3 represents a heteroaryl group (the heteroaryl group is optionally substituted by a methyl group or the like) or the like, and R4 represents a C1 to C6 alkylthio group or a C2 to C6 alkenyl group (the C1 to C6 alkylthio group and the C2 to C6 alkenyl group are each optionally substituted by one carboxy group or the like) or the like.
    Type: Grant
    Filed: October 20, 2021
    Date of Patent: August 27, 2024
    Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
    Inventors: Takuya Ikeda, Yoshiyuki Kobayashi, Naoki Miyoshi, Osamu Suzuki, Takahiro Nagayama, Takashi Tsuji, Layton H. Smith, Anthony B. Pinkerton
  • Patent number: 12071414
    Abstract: Provided herein are agonists of the apelin receptor for the treatment of disease. The compounds disclosed herein are useful for the treatment of a range of cardiovascular, renal and metabolic conditions.
    Type: Grant
    Filed: April 28, 2023
    Date of Patent: August 27, 2024
    Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
    Inventors: Layton H. Smith, Anthony B. Pinkerton, Paul Hershberger, Patrick Maloney, Danielle McAnally
  • Patent number: 12071415
    Abstract: The present invention provides new compounds and compositions thereof that release carbon monoxide for the treatment of medical disorders that are responsive to carbon monoxide, for example, inflammatory, pain, and dermatological disorders.
    Type: Grant
    Filed: April 16, 2021
    Date of Patent: August 27, 2024
    Assignee: GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.
    Inventors: Binghe Wang, Xingyue Ji, Ladie Kimberly de la Cruz, Xiaoxiao Yang
  • Patent number: 12071416
    Abstract: The present invention relates to prodrugs of 4-((1R,3S)-6-cloro-3-phenyl-2,3-dihydro-1H-inden-1-yl)-1,2,2-trimethylpiperazine in the form of 1a and 1b; and 4-((1R,3S)-6-chloro-3-(phenyl-d5)-2,3-dihydro-1H-inden-1-yl)-2,2?-dimethyl-1-(methyl-d3)piperazine in the form of 2a and 2b, wherein X? is a counter ion, or pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical composition comprising prodrugs, or pharmaceutically acceptable salts thereof, of the invention.
    Type: Grant
    Filed: November 23, 2022
    Date of Patent: August 27, 2024
    Assignee: H. Lundbeck A/S
    Inventors: Mikkel Fog Jacobsen, Morten Jørgensen
  • Patent number: 12071417
    Abstract: A method for catalytically synthesizing furaneol, which uses a specific peptide to function as a catalyst, uses rhamnose to function as a raw material, and uses an organic solvent and a phosphate buffer to function as a reaction solvent to be co-heated to prepare furaneol.
    Type: Grant
    Filed: September 20, 2021
    Date of Patent: August 27, 2024
    Assignee: Xiamen Oamic Biotech Co., Ltd.
    Inventors: Chupei Xu, Zhou Zhu, Shunchuan Ke, Yibin Zhang, Gang Liu
  • Patent number: 12071418
    Abstract: The present invention generally relates to an improved process for the preparation of dapagliflozin of Formula I or its solvates or co-crystals thereof. Dapagliflozin is an inhibitor of sodium dependent glucose transporters and used for treating diabetes. The present invention also encompasses novel intermediates and their use in the preparation of dapagliflozin. An exemplary process according to the present is shown below, wherein X1, R1, R2, P1, P2, P3 and P4 are as described herein.
    Type: Grant
    Filed: July 5, 2022
    Date of Patent: August 27, 2024
    Assignee: LAURUS LABS LIMITED
    Inventors: Uma Maheswar Rao Vasireddi, Sanjay Kumar Dehury, Madana Venkata Sudhakar Gutti, Krishna Murthy Thopudurthi
  • Patent number: 12071419
    Abstract: This invention is for improving the manufacturing pharmaceutical grade CBD and other cannabinoids following current Good Manufacturing Practices (cGMP) of the US FDA for use in clinical trials for CNS and other indications by the NIH and other researchers. The major cannabinoids in marijuana (Cannabis) and hemp originate from Cannabigerolic Acid (CBGA) present in the biomass of the plant. Plant enzymes that are specific to different strains of biomass converts CBGA to different carboxylic acids of cannabinoids including Cannabidiolic Acid (CBDA) and ?9-Tetrahydrocannabinolic Acid (?9-THCA). These are relatively stable in the growing and fresh-cut plants. These are converted by thermal decarboxylation to Cannabidiol (CBD) and ?9-Tetrahydrocannabinol (?9-THC), carbon dioxide and water. Cannabinoids can be manufactured by first heating the Cannabis biomass to convert carboxylic acids prior to extraction and purification.
    Type: Grant
    Filed: April 24, 2022
    Date of Patent: August 27, 2024
    Inventor: Trevor Percival Castor
  • Patent number: 12071420
    Abstract: The invention relates to a compound of formula (I) wherein A1, A2, X and R1-R3 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: December 17, 2020
    Date of Patent: August 27, 2024
    Assignees: HOFFMANN-LA ROCHE INC., ETH ZUERICH
    Inventors: Luca Gobbi, Uwe Grether, Julian Kretz, Simon M. Ametamey
  • Patent number: 12071421
    Abstract: Disclosed are compounds including phosphate and N-oxide prodrugs of the NK1 antagonist netupitant, useful in the prevention and/or treatment of diseases including emesis induced by chemotherapy. Also disclosed are methods of making a di-tert-butyl (chloromethyl) phosphate useful in the manufacture of such prodrugs by reacting a dialkylphosphate salt with an acid to obtain the corresponding ester of phosphoric acid, reacting the ester with a quaternary ammonium hydroxide base to form a monobasic salt, and reacting the monobasic salt with chloroiodomethane to form the corresponding chloromethyl dialkyl phosphate.
    Type: Grant
    Filed: March 21, 2022
    Date of Patent: August 27, 2024
    Assignee: Helsinn Healthcare SA
    Inventors: Luca Fadini, Peter Manini, Claudio Pietra, Claudio Giuliano, Emanuela Lovati, Roberta Cannella, Alessio Venturini, Valentino J. Stella
  • Patent number: 12071422
    Abstract: Provided herein are methods to synthesize compounds useful in the treatment of cancer where such compounds comprise a quinazolinyl core moiety and at least one stereoisomeric or atropisomeric moiety.
    Type: Grant
    Filed: February 3, 2023
    Date of Patent: August 27, 2024
    Assignees: Genentech, Inc., Hoffmann-La Roche Inc.
    Inventors: Rene Lebl, Ngiap Kie Lim, Roland Christoph Meier, Ugo Jonathan Orcel, Joerg Sedelmeier, Jeff Shen, Lauren Elizabeth Sirois, Jacob C. Timmerman, Etienne Trachsel, Nicholas Andrew White, Jie Xu, Haiming Zhang, Stephan Bachmann, Thomas Michael Bass, Raphael Bigler, Johannes Adrian Burkhard, Kyle Bradley Pascual Clagg, Francis Gosselin, Chong Han, Dainis Kaldre, Sean M. Kelly, Sebastian Herold, Christian Leitner
  • Patent number: 12071423
    Abstract: The embodiments of present invention provide processes for the large-scale preparation of 2,4,6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl]benzamide hemisuccinate, and formulations and product forms, such as tablets, made by these processes. Additionally, embodiments of the present invention provide tablets including 25 mg, 50 mg, 100 mg, or 200 mg free base equivalent of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide hemisuccinate.
    Type: Grant
    Filed: April 14, 2023
    Date of Patent: August 27, 2024
    Assignee: Eli Lilly and Company
    Inventors: Aktham Aburub, David Andrew Coates, Scott Alan Frank, Mark Steven Kerr, Roger Ryan Rothhaar, Radhe Krishan Vaid
  • Patent number: 12071424
    Abstract: Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.
    Type: Grant
    Filed: February 28, 2023
    Date of Patent: August 27, 2024
    Assignee: Cornell University
    Inventors: Joseph P. Vacca, Dansu Li, Sarah Elizabeth Bettigole
  • Patent number: 12071425
    Abstract: Described herein are phenoxy-pyridyl-pyrimidine compounds with inositol requiring enzyme 1 (IRE1) modulation activity or function having the Formula I structure or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such IRE1 modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Grant
    Filed: September 12, 2019
    Date of Patent: August 27, 2024
    Assignee: Genentech, Inc.
    Inventors: Marie-Gabrielle Braun, Cuong Q. Ly, Georgette Castanedo, Paul Gibbons, Wendy Lee, Joachim Rudolph, Nicole Alice Blaquiere, Jacob Bradley Schwarz, Ramsay Beveridge, Jean-Philippe Leclerc, Alexandre Lemire, Leo Fu
  • Patent number: 12071426
    Abstract: Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.
    Type: Grant
    Filed: December 2, 2019
    Date of Patent: August 27, 2024
    Assignee: Cornell University
    Inventors: Joseph P. Vacca, Sarah Elizabeth Bettigole
  • Patent number: 12071428
    Abstract: Disclosed herein are compounds and methods of treating diseases and/or conditions associated with FGFR inhibition.
    Type: Grant
    Filed: February 22, 2024
    Date of Patent: August 27, 2024
    Assignee: TYRA BIOSCIENCES, INC.
    Inventors: Robert L. Hudkins, Daniel C. Bensen
  • Patent number: 12071429
    Abstract: The invention provides a compound of formula (I): or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.
    Type: Grant
    Filed: February 1, 2021
    Date of Patent: August 27, 2024
    Assignees: ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Gianni Chessari, Steven Howard, Ildiko Maria Buck, Benjamin David Cons, Christopher Norbert Johnson, Rhian Sara Holvey, David Charles Rees, Jeffrey David St. Denis, Emiliano Tamanini, Bernard Thomas Golding, Ian Robert Hardcastle, Celine Florence Cano, Duncan Charles Miller, Martin Edward Mäntylä Noble, Roger John Griffin, James Daniel Osborne, Joanne Peach, Arwel Lewis, Kim Louise Hirst, Benjamin Paul Whittaker, David Wyn Watson, Dale Robert Mitchell
  • Patent number: 12071430
    Abstract: Itraconazole, a widely used antifungal drug, has been found to possess potent anti-angiogenic and anti-hedgehog activities, exhibiting promising antitumor activity in several human clinical studies. The wider use of itraconazole in the treatment of cancer, however, has been limited by its potent inhibition of the drug metabolic enzyme CYP3A4 which causes drug-drug interactions. In an effort to eliminate the CYP3A4 inhibition of itraconazole while retaining its anti-angiogenic activity, we synthesized a series of itraconazole derivatives. The newly synthesized analogs of itraconazole were evaluated for their cytotoxicity against human umbilical vein endothelial cells (HUVEC) and their inhibitory activity against CYP3A4 enzyme.
    Type: Grant
    Filed: October 3, 2019
    Date of Patent: August 27, 2024
    Assignee: The Johns Hopkins University
    Inventors: Jun Liu, Yingjun Li, Kalyan Kumar Pasunooti, Wukun Liu, Wei Shi, Ruojing Li, Sarah Head
  • Patent number: 12071431
    Abstract: The present invention relates to a novel class of pyridine-sulfonamide compounds and to compositions comprising the same. The compounds and compositions are useful as medicaments in the treatment of diseases responsive to inhibition of IL-1?, such as non-alcoholic steatohepatitis (NASH) and idiopathic pulmonary fibrosis (IPF).
    Type: Grant
    Filed: November 14, 2019
    Date of Patent: August 27, 2024
    Assignee: ALLINKY BIOPHARMA
    Inventors: Miguel Vega, Esther Carrasco, Patricia Gómez, Pedro Campos, Juan Gómez-Reino, Juan Jesús Pérez, Ángel Messeguer
  • Patent number: 12071432
    Abstract: Described herein are compounds that are inhibitors of autophagy and their use in the treatment of disorders such as cancers.
    Type: Grant
    Filed: June 6, 2022
    Date of Patent: August 27, 2024
    Assignee: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Yu Mi Ahn, Timothy Caldwell, Lakshminarayana Vogeti
  • Patent number: 12071433
    Abstract: The present invention is related to compounds of structure (I) as heme oxygenase 1 (HMOX 1) inducers. (Formula I) The present invention is also related a method of controlling the activity or the amount, or both the activity and the amount, of heme-oxygenase 1 in a mammalian subject. The definitions of the variables are provided herein.
    Type: Grant
    Filed: October 6, 2023
    Date of Patent: August 27, 2024
    Assignee: Astellas Engineered Small Molecules US, Incorporated
    Inventors: Margaret Biddle, Arthur Kluge, Sanjita Sasmal, Bharat Lagu, Xinyuan Wu, Takashi Ogiyama, Eric Bell