Patents Issued in December 15, 2020
  • Patent number: 10865168
    Abstract: Processes for producing liquid transportation fuels by converting a hydrocarbon feed stream comprising both isopentane and n-pentane. The hydrocarbon feed stream is separated into a first fraction that predominantly comprises isopentane and a second fraction that predominantly comprises n-pentane and some C6 paraffins. The first fraction is catalytically activated to produce an activation effluent comprising olefins and aromatics, while the second fraction is isomerized to convert at least a portion of the n-pentane to isopentane, then combined with the hydrocarbon feed stream to allow the newly-produced isopentane to be separated into the first fraction. Finally, the activation effluent is oligomerized. The process produced increased yields of products that meet specifications for a blend component of liquid transportation fuels.
    Type: Grant
    Filed: April 22, 2020
    Date of Patent: December 15, 2020
    Assignee: Phillips 66 Company
    Inventors: Anthony O. Baldridge, Neal D. McDaniel, James A. Suttil, Jianhua Yao, Edward C. Weintrob, Matthew J. Wülfers, Bruce B. Randolph, Maziar Sardashti
  • Patent number: 10865169
    Abstract: Processes and apparatuses for producing a C8 aromatic isomer product are provided. The process comprises introducing a reformate stream comprising aromatic hydrocarbons to a reformate splitter column to provide a plurality of streams. One or more streams comprising at least one stream from the plurality of streams is passed to a reformate upgrading unit to obtain an upgraded reformate stream. The upgraded reformate stream is passed to an aromatics stripper column to provide an aromatics stripper sidedraw stream comprising C8 aromatic hydrocarbons. The aromatics stripper sidedraw stream is passed to a xylene separation unit to provide the C8 aromatic isomer product and a raffinate product stream. At least a portion of the raffinate product stream is processed in a liquid phase isomerization unit to obtain an isomerized stream.
    Type: Grant
    Filed: May 17, 2017
    Date of Patent: December 15, 2020
    Assignee: UOP LLC
    Inventors: Joseph A. Montalbano, Patrick C. Whitchurch, Gregory R. Werba, Ian G. Horn
  • Patent number: 10865170
    Abstract: A process is disclosed for selectively producing 2-butanol from GVL by using at least one transition metal catalyst selected from the group consisting of iron, ruthenium, cobalt, rhodium and iridium.
    Type: Grant
    Filed: July 11, 2019
    Date of Patent: December 15, 2020
    Assignee: NESTE OYJ
    Inventors: Marina Lindblad, Mats Käldström, Susanna Wallenius, Kaisa Lamminpää
  • Patent number: 10865171
    Abstract: Disclosed is a method for making aromatic enol ethers that have utility as film-hardening additives for coating formulations. The aromatic enol ethers have particular utility as film-hardening additives for water-based coating formulations. The aromatic enol ethers provide improvements in hardness and hardness related properties such as block resistance without contributing to the volatile organic content of the composition.
    Type: Grant
    Filed: September 4, 2019
    Date of Patent: December 15, 2020
    Assignee: Eastman Chemical Company
    Inventor: Matthew Allen Boone
  • Patent number: 10865172
    Abstract: Disclosed are aromatic enol ethers that have utility as film-hardening additives for coating formulations. The aromatic enol ethers have particular utility as film-hardening additives for water-based coating formulations. The aromatic enol ethers provide improvements in hardness and hardness related properties such as block resistance without contributing to the volatile organic content of the composition.
    Type: Grant
    Filed: September 4, 2019
    Date of Patent: December 15, 2020
    Assignee: Eastman Chemical Company
    Inventor: Matthew Allen Boone
  • Patent number: 10865173
    Abstract: An allylic oxidation process includes forming a mixture containing ?-Guaiene and an iron (III)-X porphyrin complex catalyst in a sustainable solvent, introducing molecular oxygen into the mixture, and effecting allylic oxidation to produce an ?,ß-unsaturated ketone, Rotundone.
    Type: Grant
    Filed: December 3, 2018
    Date of Patent: December 15, 2020
    Assignee: GIVAUDAN S.A.
    Inventors: Fridtjof Schröder, Nicole Pfeiffer
  • Patent number: 10865174
    Abstract: A one-step process for hydroformylation of olefins can include iron-catalyzed hydroformylation of olefins. The process can result in the conversion of olefin in the range of 40 to 99%. A reaction mixture includes iron precursor, ligand, substrate and solvent. The reaction mixture can be pressurized with syngas (CO/H2) under constant stirring to obtain a desired aldehyde compound. The ligand can be a monodentate ligand of a phosphines or a phosphite, and the iron precursor can be [HFe(CO)4]?.
    Type: Grant
    Filed: April 27, 2018
    Date of Patent: December 15, 2020
    Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIALRESEARCH
    Inventors: Samir Hujur Chikkali, Swechchha Pandey
  • Patent number: 10865175
    Abstract: A method of synthesizing cyclohexanone can include oxidation of cyclohexane to produce a mixture including cyclohexanone, cyclohexanol, and cyclohexane, and separating cyclohexanone from the mixture using a pervaporation method. The pervaporation method includes contacting the mixture with a first side of a poly(styrene-maleic anhydride-dihydropyrane) membrane and receiving the cyclohexanone from a second side of the poly(styrene-maleic anhydride-dihydropyrane) membrane as a low-pressure vapor. The method can be performed in a pervaporation unit including a reactant portion for receiving the cyclohexane, a permeate portion for receiving the cyclohexanone, and a poly(styrene-maleic anhydride-dihydropyrane) membrane separating the reactant portion from the permeate portion.
    Type: Grant
    Filed: June 7, 2020
    Date of Patent: December 15, 2020
    Assignee: KING SAUD UNIVERSITY
    Inventors: Ahmed Mohammed Aouissi, Zeid Abdullah ALOthman, Abdullah Ali Sultan Al-Kahtani
  • Patent number: 10865176
    Abstract: The present invention provides methods for identifying compounds that act as miR-34a modulators. The present invention also provides miR-34a modulators and compositions containing the modulators. The present invention further provides methods for treating diseases by administration of miR-34a modulators.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: December 15, 2020
    Assignee: The Chinese University of Hong Kong
    Inventor: Yangchao Chen
  • Patent number: 10865177
    Abstract: A process for making a high purity salt comprises the steps of providing an organic compound, providing a metal salt, adding the metal salt and organic compound to an aqueous medium, heating the reaction mixture to react the organic compound and the metal salt to form an organic salt, collecting the organic salt, exposing the collected organic salt to microwave radiation, and exposing the collected organic salt to infrared radiation.
    Type: Grant
    Filed: June 11, 2019
    Date of Patent: December 15, 2020
    Assignee: Milliken & Company
    Inventors: Darin L. Dotson, Xiaoying Wang, Rui Liu
  • Patent number: 10865178
    Abstract: A carboxylic acid or sulfonic acid salt containing a plurality of carbonyl groups, and a surfactant represented by the following formula: R1—C(?O)—R2—C(?O)—R3-A wherein R1, R2 and R3 are as defined herein, and A is —COOX or —SO3X, wherein X is H, a metal atom, NR44, imidazolium optionally containing a substituent, pyridinium optionally containing a substituent, or phosphonium optionally containing a substituent, where R4s are each H or an organic group and are the same as or different from each other; and any two of R1, R2, and R3 optionally bind to each other to form a ring.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: December 15, 2020
    Assignee: DAIKIN INDUSTRIES, LTD.
    Inventors: Masahiro Higashi, Satoru Yoneda, Akiyoshi Yamauchi, Sumi Ishihara, Yosuke Kishikawa, Hirokazu Aoyama
  • Patent number: 10865179
    Abstract: A method for preparing methyl methacrylate from methacrolein and methanol. The method comprises contacting a mixture comprising methacrolein, methanol and oxygen with a heterogeneous catalyst comprising a support and a noble metal, wherein oxygen concentration at a reactor outlet is from 1 to 7.5 mol % and wherein pH at a reactor outlet is no greater than 7.5.
    Type: Grant
    Filed: September 12, 2018
    Date of Patent: December 15, 2020
    Assignees: Dow Global Technologies, LLC, Rohm and Haas Company
    Inventors: Jeffrey Herron, Daniel J. Arriola, D. Wayne Blaylock, Wen-Sheng Lee, Victor Sussman, Daniel A. Hickman, Kirk W. Limbach
  • Patent number: 10865180
    Abstract: The present invention, discloses optically pure compounds of l-Norepinephrine and its acid addition salts and hydrates and process for the preparation thereof. Specifically, the present invention discloses optically pure compounds of l-Norepinephrine bitartrate, its process of preparation and pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: August 9, 2019
    Date of Patent: December 15, 2020
    Assignee: HARMAN FINOCHEM LIMITED
    Inventors: Vijay Trimbak Kadam, Nareesh Saranapu, Amin Rashid Shaikh, Harpreet Singh Minhas, Gurpreet Singh Minhas
  • Patent number: 10865181
    Abstract: The present technology relates to compounds of any one of Formula I, II, IIa, III, IV, and/or V as described herein and their tautomers and/or pharmaceutically acceptable salts, compositions, and methods of uses thereof.
    Type: Grant
    Filed: November 4, 2015
    Date of Patent: December 15, 2020
    Assignees: UNIVERSITY OF KANSAS, Oregon Health & Science University
    Inventors: Sudeshna Roy, Paolo Bernardi, Michael Forte, Frank Schoenen, Justina Sileikyte
  • Patent number: 10865182
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R3, R8, R9, R10 and R11 are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: January 17, 2019
    Date of Patent: December 15, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans P. Maerki, Benoit Hornsperger, Peter Mohr, Michael Reutlinger, Markus Rudolph
  • Patent number: 10865183
    Abstract: The present invention provides a compound of formula (I) or a salt thereof and their use as a biomarker in assessing or monitoring kidney function in a subject, determining predisposition to developing reduced kidney function, classifying a subject according to level of kidney function, diagnosing or monitoring chronic kidney disease. Compositions and method of making of the compound of formula (I) are also described.
    Type: Grant
    Filed: July 27, 2017
    Date of Patent: December 15, 2020
    Assignee: Metabolon, Inc.
    Inventors: Qibo Zhang, Anne M. Evans
  • Patent number: 10865184
    Abstract: This invention provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
    Type: Grant
    Filed: September 5, 2018
    Date of Patent: December 15, 2020
    Assignee: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
    Inventors: Ramesh Narayanan, Duane D. Miller, Thamarai Ponnusamy, Dong-Jin Hwang, Yali He
  • Patent number: 10865185
    Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels.
    Type: Grant
    Filed: August 19, 2016
    Date of Patent: December 15, 2020
    Assignee: SRX Cardio, LLC
    Inventors: Thomas E. Barta, Jonathan William Bourne, Kyle D. Monroe, Michael M. Muehlemann, Anjali Pandey, Simeon Bowers
  • Patent number: 10865186
    Abstract: Provided are compounds, including those of Formula I; and pharmaceutically acceptable salts and solvates thereof. The compounds described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.
    Type: Grant
    Filed: August 22, 2018
    Date of Patent: December 15, 2020
    Assignee: Nektar Therapeutics
    Inventors: Franco J. Duarte, Neel K. Anand, Pankaj Sharma, Devendrapratap Singh
  • Patent number: 10865187
    Abstract: The application describes methods for making a deuterated dextromethorphan of Formula (I), deuterated dextromethorphan produced by these methods, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 24, 2020
    Date of Patent: December 15, 2020
    Assignee: Avanir Pharmaceuticals, Inc.
    Inventors: Matt Johnson, Cunxiang Zhao, Weihua Meng, Zhijun Lu, Yan Li
  • Patent number: 10865188
    Abstract: The present disclosure provides crystalline Compound I and crystalline Compound II, pharmaceutical compositions comprising one of said crystalline compounds suitable for intratympanic administration, and methods for treating otic disorders using the crystalline compounds and the pharmaceutical compositions.
    Type: Grant
    Filed: March 4, 2019
    Date of Patent: December 15, 2020
    Assignee: Pipeline Therapeutics, Inc.
    Inventors: Thomas Jon Seiders, Catherine Yuling Lee, Yiwei Li
  • Patent number: 10865189
    Abstract: A method for the oxidation of ethylene to form ethylene oxide which comprises: providing an aqueous stream containing ethylene glycol and impurities; introducing the aqueous stream in a first ion exchange treatment bed to reduce the content of these impurities; determining whether an outlet of the first ion exchange treatment bed has a conductivity greater than about 5 ?S/cm; upon determining that the outlet of the first ion exchange treatment bed has a conductivity greater than about 5 ?S/cm, introducing the outlet of the first ion exchange treatment bed into a second ion exchange treatment bed; and upon determining that the outlet of the first ion exchange treatment bed has a conductivity greater than about 60 ?S/cm, redirecting the introduction of the aqueous stream to the second ion exchange treatment bed and regenerating the first ion exchange bed.
    Type: Grant
    Filed: July 15, 2019
    Date of Patent: December 15, 2020
    Assignee: Scientific Design Company, Inc.
    Inventors: Shaun McGovern, Mansoor Husain, John Sullivan
  • Patent number: 10865190
    Abstract: A process for producing furan dicarboxylic acid or an ester thereof from a feedstock comprising hydroxymethyl furfural (HMF) and humins is disclosed. Humins are a byproduct from reactions forming HMF from sugars and are typically removed from the HMF prior to any further processing. A humins-containing HMF feedstock is utilized to produce furan dicarboxylic acids and ester substantially free from humins.
    Type: Grant
    Filed: June 20, 2019
    Date of Patent: December 15, 2020
    Assignee: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Pranit S Metkar, Ronnie Ozer, Bhuma Rajagopalan
  • Patent number: 10865191
    Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: A is CR1 or N; B is CR3 or N; D is CR4 or N; L1 is —(CR7R7)m—; L2 is —(CR7R7)n—; and X, Z, R1, R2, R3, R4, R5, and R6 are define herein. Also disclosed are methods of using such compounds as modulators of TNF?, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Grant
    Filed: August 2, 2016
    Date of Patent: December 15, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Hai-Yun Xiao, T. G. Murali Dhar, Ning Li, Jingwu Duan, Bin Jiang, Zhonghui Lu, Khehyong Ngu, William J. Pitts, Joseph A. Tino
  • Patent number: 10865192
    Abstract: The invention provides certain nicotine salts, co-crystals, and salt co-crystals and provides novel polymorphic forms of certain nicotine salts. In particular, nicotine salts with orotic acid are described. The invention further provides methods of preparation and characterization of such nicotine salts. In addition, tobacco products, including smoking articles, smokeless tobacco products, and electronic smoking articles comprising nicotine salts, co-crystals, and/or salt co-crystals are also provided.
    Type: Grant
    Filed: October 10, 2019
    Date of Patent: December 15, 2020
    Assignee: R.J. Reynolds Tobacco Company
    Inventors: Gary M. Dull, Andrew Carr, Emma Sharp
  • Patent number: 10865193
    Abstract: This invention relates to pyridone derivatives, processes for their preparation, pharmaceutical compositions, and their use in therapy.
    Type: Grant
    Filed: June 5, 2019
    Date of Patent: December 15, 2020
    Assignee: JANSSEN SCIENCES IRELAND UNLIMITED COMPANY
    Inventors: David Craig McGowan, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 10865194
    Abstract: Pharmaceutical compounds are disclosed having a bicyclic-sulphonamide structure of Formula 1: wherein R1 represents an unsubstituted or a substituted heteroaryl ring; R2, R3, R4, and R5 are independently selected from hydrogen, alkyl, hydroxyalkyl, and alkyl-O-alkyl, provided that either R2 and R3, or R4 and R5 are linked or taken together to form a bridge between the carbon atoms to which R2 and R3, or R4 and R5 respectively are directly linked, whereby the N-containing ring in Formula 1 is an azabicyclo moiety. The compounds and compositions including the compounds may be used in therapy as brain-cell-death protectants, for example, in the treatment of chronic neurodegenerative diseases. The compounds are active as inhibitors of N-acylethanolamine-hydrolysing acid amidase (NAAA) and may be used for the therapeutic treatment and prevention of pain and inflammatory disorders and other disorders which benefit from the modulation of fatty acid ethanolamides, particularly palmitoylethanolamide (PEA).
    Type: Grant
    Filed: November 3, 2017
    Date of Patent: December 15, 2020
    Assignee: FONDAZIONE ISTITUTO ITALIANO DI TECNOLOGIA
    Inventors: Fabio Bertozzi, Tiziano Bandiera, Silvia Pontis, Angelo Reggiani, Francesca Giacomina, Paolo Di Fruscia
  • Patent number: 10865195
    Abstract: Preparation of novel 2-benzyl-5-methyl-2H-tetrazole derivatives of the formula (I) for use as PET imaging agents. The present invention relates to novel compounds of formula (I) their preparation and use as PET imaging agents for imaging techniques and diagnostics in the field of diseases and disorders mediated by or related to the enzyme autotaxin.
    Type: Grant
    Filed: September 24, 2019
    Date of Patent: December 15, 2020
    Assignee: Novartis AG
    Inventors: Yves Auberson, Emmanuelle Briard, Darren Le Grand, Berndt Oberhauser
  • Patent number: 10865196
    Abstract: The present invention relates to a compound of formula XXII and a compound of formula 17ya, which are defined as anywhere in the specification, to a composition comprising the same, and to a method of using thereof in the treatment of various forms of cancer.
    Type: Grant
    Filed: January 16, 2018
    Date of Patent: December 15, 2020
    Assignees: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION, ONCTERNAL THERAPEUTICS, INC.
    Inventors: Duane D. Miller, Jianjun Chen, James T. Dalton, Chien-Ming Li, Sunjoo Ahn, Wei Li
  • Patent number: 10865197
    Abstract: The present invention relates an enantioselective process for the manufacture of a compound of formula (E) wherein ring A, RB2 and RB3 are as defined in claim 1.
    Type: Grant
    Filed: May 15, 2020
    Date of Patent: December 15, 2020
    Assignee: SYNGENTA CROP PROTECTION AG
    Inventors: James Alan Morris, Sally Elizabeth Russell, Sean Ng
  • Patent number: 10865198
    Abstract: Forms of cerdulatinib and salts or co-crystals thereof were prepared and characterized in the solid state. Also provided are processes of manufacture and methods of using the forms cerdulatinib and salts or co-crystals thereof.
    Type: Grant
    Filed: May 3, 2019
    Date of Patent: December 15, 2020
    Assignee: Alexion Pharmaceuticals, Inc.
    Inventors: Anjali Pandey, Julian Scott Northen, Philippe Fernandes, Ying Chen, Yuelie Lu, Sami Karaborni, Gus Kodersha
  • Patent number: 10865199
    Abstract: The present invention provides novel heterocyclic compounds as anticancer agents, especially as estrogen receptor (ER) antagonists/degraders and process for their preparation.
    Type: Grant
    Filed: October 26, 2016
    Date of Patent: December 15, 2020
    Assignee: Sun Pharma Advanced Research Company Limited
    Inventors: Ranjan Kumar Pal, Amit Pravinbhai Sedani, Kaushikkumar Dhanjibhai Prajapati, Dijixa Pinakin Rana, Sandeep Pankajbhai Pathak, Japan Nitinkumar Desai, Jayraj Dilipbhai Aradhye, Bhavesh Mohanbhai Panchal, Indraneel Ghosh, Trinadha Rao Chitturi
  • Patent number: 10865200
    Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies, and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof. wherein each symbol is as described in the specification, or a salt thereof.
    Type: Grant
    Filed: December 4, 2018
    Date of Patent: December 15, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masami Yamada, Shinkichi Suzuki, Takahiro Sugimoto, Minoru Nakamura, Hiroki Sakamoto, Makoto Kamata
  • Patent number: 10865201
    Abstract: Provided herein are compounds, compositions including them, and methods of modulating GPR120 activity and treating diseases mediated by GPR120 by administering such compounds and compositions.
    Type: Grant
    Filed: September 11, 2017
    Date of Patent: December 15, 2020
    Assignee: Valo Health, Inc.
    Inventors: Brian Raimundo, Elena S. Koltun, John Griffin, Eric Stangeland
  • Patent number: 10865202
    Abstract: The present disclosure relates to compounds and a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing the compounds, and processes for their preparation. The disclosure also relates to the use of the compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.
    Type: Grant
    Filed: April 5, 2019
    Date of Patent: December 15, 2020
    Assignee: ARVINAS OPERATIONS, INC.
    Inventors: Andrew P. Crew, Yimin Qian, Hanqing Dong, Jing Wang
  • Patent number: 10865203
    Abstract: Provided herein are novel pyrazolo-quinolinone compounds and method of using such compounds to treat disorders such as neuropsychiatric disorders with sensorimotor gating deficits, such as schizophrenia, tic disorders, attention deficit hyperactivity disorder, obsessive compulsive disorder, panic disorder, Huntington's disease and nocturnal enuresis; depression; temporomandibular myofascial pain; disorders of trigeminal nerve, such as trigeminal neuralgia and trigeminal neuropathy; migraine; and tinnitus.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: December 15, 2020
    Assignees: UWM Research Foundation, Inc., Medical University of Vienna
    Inventors: James Cook, Daniel Knutson, Marko Mihovilovic, Laurin Wimmer
  • Patent number: 10865204
    Abstract: The present application provides bifunctional compounds of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 4 (CDK4) and/or cyclin-dependent kinase 6 (CDK6). The present application also relates to methods for the targeted degradation of CDK4 and/or CDK6 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK4 and/or CDK6 which can be utilized in the treatment of disorders modulated by CDK4 and/or CDK6.
    Type: Grant
    Filed: April 21, 2017
    Date of Patent: December 15, 2020
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Tinghu Zhang, Calla M. Olson, Yanke Liang, Nicholas Kwiatkowski, Baishan Jiang, Eric Wang
  • Patent number: 10865205
    Abstract: The present application provides bifunctional compounds of Formula (Ia) or (Ib): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 8 (CDK8). The present application also relates to methods for the targeted degradation of CDK8 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK8 which can be utilized in the treatment of disorders modulated by CDK8.
    Type: Grant
    Filed: April 21, 2017
    Date of Patent: December 15, 2020
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Tinghu Zhang, Calla M. Olson, Yanke Liang, Nicholas Kwiatkowski
  • Patent number: 10865206
    Abstract: The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase (e.g., CDK7), and therefore induce cellular apoptosis and/or inhibit transcription in the subject.
    Type: Grant
    Filed: May 15, 2019
    Date of Patent: December 15, 2020
    Assignee: Syros Pharmaceuticals, Inc.
    Inventors: Stephane Ciblat, Anzhelika Kabro, Melissa Leblanc, Serge Leger, Jason J. Marineau, Tom Miller, Stephanie Roy, Darby Schmidt, M. Arshad Siddiqui, Kevin Sprott, Dana K. Winter, Amy Ripka, Dansu Li, Guoli Zhang
  • Patent number: 10865207
    Abstract: The present invention relates to novel compounds of the formula (I) that can be employed in the selective Tau detection of disorders and abnormalities associated with Tau aggregates such as Alzheimer's disease and other tauopathies using Positron Emission Tomography (PET) Imaging.
    Type: Grant
    Filed: July 21, 2017
    Date of Patent: December 15, 2020
    Assignees: AC IMMUNE S.A., LIFE MOLECULAR IMAGING SA
    Inventors: Heiko Kroth, Jérôme Molette, Hanno Schieferstein, Andre Müller, Heribert Schmitt-Willich, Mathias Berndt, Felix Oden
  • Patent number: 10865208
    Abstract: Disclosed are chemical entities which are compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, and Ra have the values described herein. Chemical entities according to the disclosure can be useful as inhibitors of ATG7. Further provided are pharmaceutical compositions comprising a chemical entity of the disclosure and methods of using the compositions in the treatment of cancer.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: December 15, 2020
    Assignee: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Sharmila Adhikari, Emily Frances Calderwood, Dylan Bradley England, Alexandra E. Gould, Sean J. Harrison, Shih-Chung Huang, Liting Ma
  • Patent number: 10865209
    Abstract: The present invention relates to an efficient and industrially advantageous process for preparing temozolomide and the carbamoyl-AICA intermediate through the use of N-methyl carbamoylimidazole in a good overall yield and high purity.
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: December 15, 2020
    Assignee: CRISTÁLIA PRODUTOS QUÍMICOS FARMACÊUTICOS LTDA
    Inventors: Ogari Pacheco, Vincenzo De Sio, Murilo Massoni, Leandro Camargo
  • Patent number: 10865210
    Abstract: This invention is in the area of synthesizing pyrimidine-based compounds useful in the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
    Type: Grant
    Filed: December 21, 2018
    Date of Patent: December 15, 2020
    Assignee: G1 Therapeutics, Inc.
    Inventors: Alexander Smith, Hannah S. White, Francis Xavier Tavares, Sergiy Krasutsky, Jian-Xie Chen, Roberta L. Dorrow, Hua Zhong
  • Patent number: 10865211
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: September 20, 2019
    Date of Patent: December 15, 2020
    Assignee: ENANTA PHARMACEUTICALS, INC.
    Inventors: Joseph Panarese, Samuel Bartlett, Dexter Davis, Katherine Chong, Yat Sun Or
  • Patent number: 10865212
    Abstract: The present invention relates to a process for preparing an intermediate for the preparation of eribulin mesylate with high yields, and an intermediate therefor.
    Type: Grant
    Filed: January 2, 2018
    Date of Patent: December 15, 2020
    Assignee: YONSUNG FINE CHEMICAL CO.. LTD.
    Inventors: Hyoseon Lee, Hyunik Shin, Keeyoung Lee, Changyoung Oh
  • Patent number: 10865213
    Abstract: The present disclosure provides compounds of Formula (I?), Formula (I), Formula (II), Formula (II-A), Formula (III), and Formula (IV). The compounds described herein are MAX binders and/or modulators of Myc, Mad, or Mxi1 (e.g., inhibitors of Myc, Mad, or Mxi1), and may be useful in treating a subject with a disease associated with Myc, such as proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions and kits including the compounds described herein, as well as methods of using and uses of the compounds, compositions, and kits.
    Type: Grant
    Filed: October 22, 2018
    Date of Patent: December 15, 2020
    Assignee: Massachusetts Institute of Technology
    Inventors: Angela N. Koehler, Eric Stefan, Francisco Caballero, Dylan Vijith Neel, Nicholas B. Struntz, Helen L. Evans, Andrew Chen
  • Patent number: 10865214
    Abstract: The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.
    Type: Grant
    Filed: July 5, 2018
    Date of Patent: December 15, 2020
    Assignees: The Trustees of Columbia University in they City of New York, NY State Psychiatric Institute
    Inventors: Kirsten Alison Rinderspacher, Wai Yu, Karen Duff, Donald Landry, Shi-Xian Deng
  • Patent number: 10865215
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: January 10, 2020
    Date of Patent: December 15, 2020
    Assignee: ENANTA PHARMACEUTICALS, INC.
    Inventors: Brian C. Shook, In Jong Kim, Thomas P. Blaisdell, Jianming Yu, Joseph Panarese, Yat Sun Or
  • Patent number: 10865216
    Abstract: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. In addition, species of tricyclic gyrase inhibitors compounds are also disclosed herein. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
    Type: Grant
    Filed: September 11, 2013
    Date of Patent: December 15, 2020
    Assignees: MERCK SHARP & DOHME CORP., LAWRENCE LIVERMORE NATIONAL SECURITY, LLC
    Inventors: Daniel Bensen, Allen Borchardt, Zhiyong Chen, John M. Finn, Thanh To Lam, Suk Joong Lee, Xiaoming Li, Leslie William Tari, Min Teng, Michael Trzoss, Junhu Zhang, Michael E. Jung, Felice C. Lightstone, Sergio E. Wong, Toan B. Nguyen
  • Patent number: 10865217
    Abstract: The present invention relates to process for the preparation of 5-(4-cyano phenoxy)-1,3-dihydro-1-hydroxy-[2,1]-benzoxaborole represented by the following structural formula-1 and polymorphs thereof. The present invention also relates to salts of 5-(4-cyano phenoxy)-1,3-dihydro-1-hydroxy-[2,1]-benzoxaborole and process for their preparation and their use in the preparation of pure compound of the formula-1.
    Type: Grant
    Filed: May 23, 2018
    Date of Patent: December 15, 2020
    Assignee: MSN LABORATORIES PRIVATE LIMITED, R & D CENTER
    Inventors: Thirumalai Rajan Srinivasan, Eswaraiah Sajja, Venkat Reddy Ghojala, Markandeya Bekkam