Patents Issued in November 17, 2020
  • Flavor modulator having pyridine derivative or salt thereof as active ingredient
    Patent number: 10836724
    Abstract: 2-(phenylalkyloxyalkyl)pyridine derivative or a 2-(phenylalkylthioalkyl)pyridine derivative imparts, when added to food and drink or cosmetics as an active ingredient, a flavor of natural impression thereto; and in particular, when added to food and drink, the compound imparts an umami imparting or enhancing, a saltiness enhancing a sweetness enhancing, and in particular, when added to a milk or dairy product, a food or drink product containing a milk or dairy product, or a dairy replacement product, the compound provides a milk richness enhancing.
    Type: Grant
    Filed: September 5, 2019
    Date of Patent: November 17, 2020
    Assignee: T. HASEGAWA CO., LTD.
    Inventors: Yamato Miyazawa, Yasutaka Ohkubo, Kenji Haraguchi, Michinaga Takahashi, Shogo Yoshida
  • Modulators of the integrated stress pathway
    Patent number: 10836725
    Abstract: Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.
    Type: Grant
    Filed: May 5, 2017
    Date of Patent: November 17, 2020
    Assignee: AbbVie Inc.
    Inventors: Marina Pliushchev, Jennifer M. Frost, Lawrence A. Black, Xiangdong Xu, Ramzi Farah Sweis, Lei Shi, Qingwei I. Zhang, Yunsong Tong, Charles W. Hutchins, Seungwon Chung, Michael J. Dart
  • AZO-quaternary pyridinium salts with acid-enhanced antibacterial efficacy, methods of use, methods of synthesis, and uses thereof
    Patent number: 10836726
    Abstract: A new azo-type quaternary pyridinium salt (Azo-QPS) shows enhanced activity at acidic conditions (e.g., pH=5); in neutral or basic conditions, this new Azo-QPS shows a much lower level (2-50 times less) anti-bacterial activity. The use of such a “stimulus-enhance” antibiotic can response to the proliferation of bacteria directly. It helps reduce or prevent the build-up of potent antibacterial agents in the oral environment. The antibacterial properties of Azo-QPS are “activated” when the environmental pH becomes acidic; this acidic pH may be indicative of the accumulation of Streptococcus mutans, or the initiation of tooth decay.
    Type: Grant
    Filed: October 3, 2017
    Date of Patent: November 17, 2020
    Inventor: Jirun Sun
  • Crystal forms of lenvatinib
    Patent number: 10836727
    Abstract: The present invention provides novel crystalline forms of 4-[3-Chloro-4-(N?-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide methanesulfonate, as well as methods for their preparation.
    Type: Grant
    Filed: September 15, 2017
    Date of Patent: November 17, 2020
    Assignee: Indena S.P.A.
    Inventors: Nicola Sardone, Stefano Luca Giaffreda, Andrea Gambini, Alex Petrolati, Pietro Allegrini, Enrico Modena
  • Substituted 3-dialkylaminomethyl-piperidin-4-yl-benzamides and methods of making and using same
    Patent number: 10836728
    Abstract: The invention relates to certain substituted 3-dialkylaminomethyl-piperidin-4-yl-benzamides, and compositions comprising the same, which in certain embodiments are useful for treating and/or preventing pain in a subject in need thereof.
    Type: Grant
    Filed: January 17, 2018
    Date of Patent: November 17, 2020
    Assignee: Mebias Discovery, Inc.
    Inventors: Brett A. Tounge, Shariff Bayoumy, Lawrence C. Kuo, Scott L. Dax
  • Metabolically stable 5-HMF derivatives for the treatment of hypoxia
    Patent number: 10836729
    Abstract: 5-HMF derivative compounds that bind covalently with hemoglobin are provided. Methods of treating sickle cell disease and other hypoxia-related disorders by administering such compounds are also provided.
    Type: Grant
    Filed: May 4, 2020
    Date of Patent: November 17, 2020
    Assignee: King Abdulaziz University
    Inventors: Abdelsattar Mansour Ebeid Omar, Moustafa El-Sayed El-Araby, Martin K. Safo
  • Process for preparation and purification of vortioxetine hydrobromide
    Patent number: 10836730
    Abstract: The present invention is related to an improved process for the preparation and purification of crystalline Vortioxetine hydrobromide of Formula-I. The process according to present invention is operationally simple and suitable for industrial application which will avoid hazardous chemicals and eliminate column chromatography to get ICH quality of pharmaceutically acceptable active pharmaceutical ingredient having snow white appearance.
    Type: Grant
    Filed: February 21, 2018
    Date of Patent: November 17, 2020
    Assignee: UNICHEM LABORATORIES LTD.
    Inventors: Dhananjay G. Sathe, Arijit Das, Vishal Kulkarni, Tushar Patil, Yogesh Patil, Prafulla Nagawade
  • Precipitation method and synthesis method of 2,6-diamino-3,5-dinitropyrazine-1-oxide
    Patent number: 10836731
    Abstract: A method for precipitating as particles 2,6-diamino-3,5-dinitropyrazine-1-oxide (or ANPZO) present in an acid medium, which comprises adding the acid medium to an aqueous solution and which is characterized in that the aqueous solution comprises a nitrate salt. Further disclosed is a method for synthesizing ANPZO implementing this precipitation method. The synthesis method comprises converting 2,6-diaminopyrazine-1-oxide (or DAPO) into ANPZO by nitration in an acid medium, and then precipitating as particles the ANPZO by adding the acid medium to an aqueous solution, and is characterized in that the aqueous solution comprises a nitrate salt.
    Type: Grant
    Filed: February 26, 2018
    Date of Patent: November 17, 2020
    Assignee: COMMISSARIAT A L'ÉNERGIE ATOMIQUE ET AUX ÉNERGIES ALTERNATIVES
    Inventors: Eric Pasquinet, Anne Wuillaume, Nicolas Pin, Arnaud Beaucamp, Christelle Barthet
  • Compounds for combating arthropods
    Patent number: 10836732
    Abstract: The invention relates inter alia to novel compounds of the general formula (I) in which the A1-A4, T, W, Q, R1 and B1-B4 radicals are each as defined in the description. Also described are processes for preparing the compounds of the formula (I). The inventive compounds are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.
    Type: Grant
    Filed: November 5, 2014
    Date of Patent: November 17, 2020
    Assignee: BAYER ANIMAL HEALTH GMBH
    Inventors: Werner Hallenbach, Ulrich Goergens, Andreas Turberg, Kerstin Ilg, Sebastian Horstmann, Johannes Kobberling
  • HDAC inhibitors and therapeutic methods using the same
    Patent number: 10836733
    Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
    Type: Grant
    Filed: August 31, 2016
    Date of Patent: November 17, 2020
    Assignee: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Alan Kozikowski, Irina Gaisina
  • Spiroquinone derivative compound, production method thereof, and pharamaceutical composition for preventing or treating neurological disorders which contains same as active ingredient
    Patent number: 10836734
    Abstract: The present invention relates to a novel spiroquinone derivative compound, a production method thereof, and a pharmaceutical composition for preventing or treating neurological disorders which contains the compound as an active ingredient.
    Type: Grant
    Filed: July 24, 2018
    Date of Patent: November 17, 2020
    Assignees: GACHON UNIVERSITY OF INDUSTRY—ACADEMIC COOPERATION FOUNDATION, GIL MEDICAL CENTER
    Inventors: Mi-Hyun Kim, Sun Yeou Kim, Sang-Yoon Lee, Venkanna Arramshetti, Kang Kim, Kyohee Cho, Prema Dhorma Lama
  • Compositions and methods for treating cancers
    Patent number: 10836735
    Abstract: The invention describes compounds that inhibit both HDAC and GSK3? (i.e., HDAC/GSK3? dual inhibitors). The invention further describes compositions containing these HDAC/GSK3? dual inhibitors, as well as methods and kits using these HDAC/GSK3? dual inhibitors to treat various medical conditions. The invention also provides methods and kits using a HDAC inhibitor and a GSK3? to treat various medical conditions, and compositions containing a HDAC inhibitor and a GSK3?. Medical conditions treatable with various embodiments of the invention include but are not limited to cancers and tumors.
    Type: Grant
    Filed: March 4, 2019
    Date of Patent: November 17, 2020
    Assignee: CEDARS-SINAI MEDICAL CENTER
    Inventors: Mouad Edderkaoui, Ramachandran Murali, Stephen Pandol
  • Pharmaceutical composition with cytotoxic activity on colorectal cancer cells
    Patent number: 10836736
    Abstract: A compound of formula (I), wherein R1 is an optionally substituted aryl or an optionally substituted heteroaryl, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, and R3 is an optionally substituted alkylamino, an optionally substituted cycloalkylamino, an optionally substituted arylamino, an optionally substituted heterocyclylamino, an optionally substituted heterocyclyl, and an optionally substituted dialkylamino. A pharmaceutical composition which includes the compound of formula (I) and a pharmaceutically acceptable carrier and/or excipient. A method of treating colorectal cancer in a subject, whereby a therapeutically effective amount of the compound of formula (I) is administered to the subject.
    Type: Grant
    Filed: August 5, 2020
    Date of Patent: November 17, 2020
    Assignee: King Abdulaziz University
    Inventors: Moustafa E. El-Araby, Abdelsattar M. Omar, Martin K. Safo, Radwan S. Elhaggar, Tamer M. Abdelghany, Mostafa H. Ahmed
  • Cystine diamide analogs for the prevention of cystine stone formation in cystinuria
    Patent number: 10836737
    Abstract: Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R? pair are independently selected from (i) or (ii); (i) R and R? are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R? together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.
    Type: Grant
    Filed: August 26, 2016
    Date of Patent: November 17, 2020
    Assignee: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
    Inventors: Longqin Hu, Amrik Sahota
  • Epoxidation process with concentrated ethylene oxide solutions
    Patent number: 10836738
    Abstract: An improved process for the recovery of ethylene oxide from the aqueous scrubbing solution in which the ethylene oxide is recovered into a vaporous stream highly enriched in ethylene oxide.
    Type: Grant
    Filed: April 30, 2019
    Date of Patent: November 17, 2020
    Assignee: Scientific Design Company, Inc.
    Inventors: Chun Chau Chan, Eunice Yamada, Barry Jay Billig
  • Epoxycyclohexane dicarboxylic acid diester, plasticizer, stabilizer and resin composition
    Patent number: 10836739
    Abstract: The purpose of the present invention is to provide a novel compound which is useful as a plasticizer that has improved heat resistance and cold resistance, while having good inherent plasticization performance as a plasticizer, or which is useful as a stabilizer for chlorine-containing resins. The inventors have found that a novel epoxycyclohexane dicarboxylic acid diester having a specific structure, which has an epoxy group in the molecular structure and has improved cold resistance and heat resistance, enables the achievement of the above-described purpose, and have been able to achieve a novel compound that is useful as a plasticizer and as a stabilizer.
    Type: Grant
    Filed: May 25, 2016
    Date of Patent: November 17, 2020
    Assignee: NEW JAPAN CHEMICAL CO., LTD
    Inventors: Takahiro Inoue, Taiki Tsuji, Masahiro Morikawa, Minako Tsujimoto, Shoki Yoshichika, Ken-ichi Miyazaki, Yuka Sato
  • Antifungal compound process
    Patent number: 10836740
    Abstract: The present invention relates to a process for preparing a compound of 5 or 5*, or a mixture thereof, that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compounds 7 or 7* and 11 or 11* and substituted derivatives thereof.
    Type: Grant
    Filed: July 1, 2019
    Date of Patent: November 17, 2020
    Assignee: MYCOVIA PHARMACEUTICALS, INC.
    Inventors: David Dale Wirth, Christopher M. Yates, William J. Hoekstra, Martin F. Bindl, Eduard Hartmann
  • Quinazolinones and azaquinazolinones as ubiquitin-specific protease 7 inhibitors
    Patent number: 10836741
    Abstract: The present disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R4, R4?, X1, Y1, Y2, Y3, Y4, n, and m are described herein.
    Type: Grant
    Filed: November 25, 2019
    Date of Patent: November 17, 2020
    Assignee: Valo Early Discovery, Inc.
    Inventors: Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell, David R. Lancia, Jr.
  • N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
    Patent number: 10836742
    Abstract: This application relates to N-substituted bicyclic lactams of formula (I), compositions comprising them and their uses in the treatment of diseases and conditions in which inhibition of a bromodomain is indicated. For example, the application relates to the N-substituted bicyclic lactams of formula (I) and to their use as bromodomain inhibitors. The present application is also related to the treatment or prevention of proliferative disorders, auto-immune disorders, inflammatory disorders, dermal disorders, and neoplasms, including tumors and/or cancers.
    Type: Grant
    Filed: August 11, 2016
    Date of Patent: November 17, 2020
    Assignee: Neomed Institute
    Inventors: Guillaume Jacquemot, Stephen Claridge, Malken Bayrakdarian, Shawn Johnstone, Jeffrey S. Albert, Andrew Griffin
  • Fluorinated cyclopropylamine compound, preparation method therefor, pharmaceutical composition thereof, and uses thereof
    Patent number: 10836743
    Abstract: Provided is a fluorinated cyclopropylamine compound represented by formula I, a racemate thereof, an R-isomer thereof, an S-isomer thereof, a pharmaceutical salt thereof, and a mixture thereof. Also provided are pharmaceutical compositions containing the compound, a preparation method for the compound, and uses thereof as a lysine specific demethylase 1 (LSD1) inhibitor, and in the treatment of cancers.
    Type: Grant
    Filed: March 16, 2017
    Date of Patent: November 17, 2020
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Hong Liu, Jia Li, Jiang Wang, Mingbo Su, Shuni Wang, Yubo Zhou, Wei Zhu, Wei Xu, Chunpu Li, Hualiang Jiang, Kaixian Chen
  • Diamide compounds having muscarinic receptor antagonist and ?2 adrenergic receptor agonist activity
    Patent number: 10836744
    Abstract: The invention relates to a pharmaceutical composition comprising an isotonic aqueous solution comprising a compound of formula I: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 28, 2020
    Date of Patent: November 17, 2020
    Assignee: Theravance Respiratory Company, LLC
    Inventors: Adam D. Hughes, Daniel Byun, Yan Chen, Melissa Fleury, John R. Jacobsen, Eric Stangeland, Richard D. Wilson, Rose Yen
  • Cocrystal, production method thereof, and medicament containing cocrystal
    Patent number: 10836745
    Abstract: The present invention provides a cocrystal of (S)-3-(1-((1-acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-1H-1,2,4-triazol-5(4H)-one and an organic acid capable of forming a cocrystal with the compound.
    Type: Grant
    Filed: December 22, 2016
    Date of Patent: November 17, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Koya Kimoto, Mitsuo Yamamoto, Masato Kitayama, Yasuhiro Sawai, Miyuki Hohokabe, Kentaro Iwata
  • Therapeutic compounds
    Patent number: 10836746
    Abstract: The invention provides compounds having Formula (I): or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising the same, processes for their preparation, and methods of treating and preventing HIV infection by their administration.
    Type: Grant
    Filed: February 14, 2019
    Date of Patent: November 17, 2020
    Assignee: Gilead Sciences, Inc.
    Inventors: Gediminas Brizgys, Eda Canales, Chienhung Chou, Michael Graupe, Jiayao Li, Roland D. Saito, Scott D. Schroeder, Winston C. Tse, Qiaoyin Wu, Jennifer R. Zhang
  • Ethane-sulfonate salt of quinoline derivative
    Patent number: 10836747
    Abstract: The present invention relates to an ethane-sulfonate salt of N-{5-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-pyridinyl}-2,5-dioxo-1-phenyl-1,2,5,6,7,8-hexahydro-3-quinolinecarboxamide, which has an Axl-inhibiting activity and is useful as a prophylactic and/or therapeutic agent for immune diseases, cancer and the like, a crystal thereof, and a pharmaceutical composition thereof.
    Type: Grant
    Filed: January 25, 2018
    Date of Patent: November 17, 2020
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Takahiro Nekado, Hideomi Kijima, Shizuka Ono, Toshihiko Nishiyama
  • Bradykinin B2 receptor antagonists
    Patent number: 10836748
    Abstract: The invention relates to a compound according to general formula (I), which acts as a bradykinin (BK) B2 receptor antagonist; to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to uses of said compound(s), including the use as a medicament.
    Type: Grant
    Filed: April 28, 2020
    Date of Patent: November 17, 2020
    Assignee: Pharvaris Netherlands B.V.
    Inventors: Christoph Gibson, Joern Saupe, Horst-Dieter Ambrosi, Lars Ole Haustedt
  • Substituted quinoline-8-carbonitrile derivatives having androgen receptor degradation activity and uses thereof
    Patent number: 10836749
    Abstract: The present disclosure relates to novel compounds, pharmaceutical compositions containing such compounds, and their use in prevention and treatment of cancer and related diseases and conditions. In some embodiments, the compounds disclosed herein exhibit androgen receptor degradation activity.
    Type: Grant
    Filed: June 1, 2020
    Date of Patent: November 17, 2020
    Assignee: ACCUTAR BIOTECHNOLOGY INC.
    Inventors: Jie Fan, Yimin Qian, Wei He, Ke Liu
  • TLR7/8 antagonists and uses thereof
    Patent number: 10836750
    Abstract: Compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TLR7/8 antagonists, are described herein.
    Type: Grant
    Filed: August 13, 2020
    Date of Patent: November 17, 2020
    Assignee: Merck Patent GmbH
    Inventors: Brian A. Sherer, Nadia Brugger, Ruoxi Lan, Xiaoling Chen
  • Methods for preparing Nintedanib and intermediates thereof
    Patent number: 10836751
    Abstract: The present application provides a method for preparing nintedanib. The method of the present application is carried out by using 4-halo-3-nitro-benzoic acid methyl ester (compound II) and 3-oxo-3-phenylpropionate (compound III) as raw materials, and preparing nintedanib via intermediates of methyl 4-(1-alkoxy-1,3-dioxo-3-phenyl propan-2-yl)-3-nitrobenzoate (compound IV) and methyl 3-benzoyl-2-oxoindoline-6-formate (compound V). The method for preparing nintedanib (I) provided by the present application has the advantages of using easily obtained raw materials, having a simple process, being cost effective and environmentally friendly, and is suitable for industrial-scale production.
    Type: Grant
    Filed: October 11, 2017
    Date of Patent: November 17, 2020
    Assignees: Zhejiang Huahai Pharmaceutical Co., Ltd., Shanghai Syncores Technologies, Inc.
    Inventors: Zeng Li, Xiaosong Cheng, Xianliang He, Jicheng Zhang, Luning Huang, Anping Tao, Hong Gu
  • Method for synthesizing 1-(naphthalen-2-ylsulfonyl)-3-(thiophen-2-yl) diaziridine
    Patent number: 10836752
    Abstract: A microwave assisted method for synthesizing a diarziridine in the absence of aminating agents, by reacting a sulphonylhydrazine and an aldehyde to form a mixture and exposing the mixture to microwave radiation for a duration of time sufficient to produce a diarziridine.
    Type: Grant
    Filed: April 2, 2020
    Date of Patent: November 17, 2020
    Assignee: QATAR UNIVERSITY
    Inventors: Ismail Warad, Abd Daraghmeh, Mohammed Al-Nuri, Abdelkader Zarrouk, Mohammad Mousa, Anas Al-Ali, Amjad M. Shraim
  • Co-crystals of SGLT2 inhibitors, process for their preparation and pharmaceutical compositions thereof
    Patent number: 10836753
    Abstract: The present invention provides solid forms of SGLT2 inhibitors, to processes for their preparation and their use in the purification of SGLT2 inhibitors and also provided pharmaceutical compositions comprising them and their use in therapy.
    Type: Grant
    Filed: August 2, 2019
    Date of Patent: November 17, 2020
    Assignee: Laurus Labs Limited
    Inventors: Kameswar Rao Chivukula, Ram Thaimattam, Veeranarayana Bandlamudi, Durga Visweswar Rao Padala, Narapa Reddy Gade, Nageswar Rao Regandla, Sivarami Reddy Yasam, Venkata Rama Krishna Murthy Moturu, Venkata Sunil Kumar Indukuri, Uma Maheswar Rao Vasireddi, Srihari Raju Kalidindi, Satyanarayana Chava
  • Crystalline form of the compound (S)-3-{4-[5-(2-cyclopentyl-6-methoxy-pyridin-4-yl)-[1,2,4]oxadiazol-3-yl]-2-ethyl-6-methyl-phenoxy}-propane-1,2-diol
    Patent number: 10836754
    Abstract: The present invention relates to a crystalline form of the compound (S)-3-{4-[5-(2-cyclopentyl-6-methoxy-pyridin-4-yl)-[1,2,4]oxadiazol-3-yl]-2-ethyl-6-methyl-phenoxy}-propane-1,2-diol.
    Type: Grant
    Filed: July 3, 2019
    Date of Patent: November 17, 2020
    Assignee: IDORSIA PHARMACEUTICALS LTD
    Inventors: Cyrille Lescop, Jasper Dingemanse, Andreas Krause
  • Cardiac sarcomere inhibitors
    Patent number: 10836755
    Abstract: Provided are compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein A, Z, B, R1, R2, R3, G1, G2, and G3 are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 18, 2019
    Date of Patent: November 17, 2020
    Assignee: CYTOKINETICS, INC.
    Inventors: Chihyuan Chuang, Bradley P. Morgan, Mark Vanderwal, Wenyue Wang, Luke W. Ashcraft
  • Crystalline salts of peptide epoxyketone immunoproteasome inhibitor
    Patent number: 10836756
    Abstract: Provided herein is a peptide epoxyketone immunoproteasome inhibitor having a structure: Formula (I) wherein X— is a counterion, crystal forms, salts, and processes for making the same, and formulations thereof.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: November 17, 2020
    Assignee: KEZAR LIFE SCIENCES
    Inventors: Henry Johnson, Evan Lewis, Sean Dalziel, Dustin McMinn
  • Polymorphic forms of metopimazine
    Patent number: 10836757
    Abstract: Provided herein are novel polymorphic forms of metopimazine mesylate. These polymorphic forms are useful in methods, compositions, and kits for the treatment of an enteric nervous system disorder.
    Type: Grant
    Filed: April 2, 2020
    Date of Patent: November 17, 2020
    Assignee: NEUROGASTRX, INC.
    Inventor: Shu Yu
  • Acyl sulfonamide NaV1.7 inhibitors
    Patent number: 10836758
    Abstract: The present disclosure relates to compounds of formula I which inhibit NaV1.7, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions.
    Type: Grant
    Filed: October 26, 2017
    Date of Patent: November 17, 2020
    Assignee: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Yong-Jin Wu, Jason M. Guernon
  • Thiazole derivatives useful as mutant IDH1 inhibitors for treating cancer
    Patent number: 10836759
    Abstract: A compound of Formula II or a pharmaceutically acceptable salt thereof, wherein CyN is a cyclic amine group bound via a nitrogen atom; X is C or N; R1 and R2 are each independently a halogen, CN, CF3, CHF2, CH2F, a C1-C10alkyl group, a C1-C10alkoxy group, a di(C1-C5alkyl)amino; m and n are each independently 1, 2, or 3, and represents either a single bond or a double bond, wherein the racemic mixture of 3-(4-(4-chlorophenyl)thiazol-2-yl)-1-(2-ethyl-5-methoxyphenyl)-6-(2-methylprop-1-en-1-yl)-5-(piperazine-1-carbonyl)pyridin-2(1H)-one atropisomers is excluded.
    Type: Grant
    Filed: June 21, 2017
    Date of Patent: November 17, 2020
    Assignees: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
    Inventors: Matthew Brian Boxer, Xiaodong Wang, Kyle Ryan Brimacombe, Mindy Irene Emily Davis, Yuhong Fang, Matthew Hall, Ajit Jadhav, Surendra Karavadhi, Li Liu, Natalia Martinez, Andrew Louis McIver, Rajan Pragani, Jason Matthew Rohde, Anton Simeonov, Wei Zhao, Min Shen
  • Compositions and methods for the treatment of presbyopia
    Patent number: 10836760
    Abstract: The invention provides compositions and methods for the treatment of presbyopia. The methods preferably comprise storing an aceclidine composition in a container having a headspace at a temperature from about 2 to about 8 degrees Celsius. The methods further comprise filling the container under an inert gas overlay and/or enclosing the container an anti-leaching material or disposing the container in a second container containing an anti-leaching material.
    Type: Grant
    Filed: October 8, 2019
    Date of Patent: November 17, 2020
    Assignee: Presbyopia Therapies LLC
    Inventor: Gerald Horn
  • Cinchonine-derived catalysts and methods of using same
    Patent number: 10836761
    Abstract: The present invention includes certain conchinine-derived phase-transfer catalysts of formula (I), compositions comprising the same, and methods of promoting asymmetric addition reactions using the same.
    Type: Grant
    Filed: December 16, 2015
    Date of Patent: November 17, 2020
    Assignee: Brandeis University
    Inventors: Yongwei Wu, Li Deng
  • Network-centric sensor coverage management
    Patent number: 10836762
    Abstract: Embodiments described herein are directed to employing an aggregation of participant sensor coverage areas to determine if there are missing coverage areas or unwanted overlapping coverage areas. If there are missing coverage areas, then at least one participant is instructed to modify its sensor coverage area to at least partially cover the missing coverage area. Conversely, if at least one participant has a sensor that is providing unwanted overlap of other sensor coverage areas, then that participant may be instructed to stop using that sensor, utilize that sensor for other data transmission purposes, or modify the coverage area to be non- or less-overlapping.
    Type: Grant
    Filed: June 20, 2019
    Date of Patent: November 17, 2020
    Assignee: Quixotic Holdings LLC
    Inventors: Matthew David Perdew, Ryan Scott Luther
  • 5 to 7 membered heterocyclic amides as JAK inhibitors
    Patent number: 10836763
    Abstract: The invention provides compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds and methods of using such compounds to treat respiratory diseases.
    Type: Grant
    Filed: September 3, 2019
    Date of Patent: November 17, 2020
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Daniel D. Long, Cameron Smith, Corbin Thompson
  • 5-HT2C receptor agonists and compositions and methods of use
    Patent number: 10836764
    Abstract: The present invention relates to compounds of Formula A and pharmaceutical compositions thereof that modulate the activity of the 5-HT2C receptor.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: November 17, 2020
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Graeme Semple, Albert S. Ren, Thomas O. Schrader, Michelle Kasem, Xiuwen Zhu
  • Process for the preparation of valacyclovir
    Patent number: 10836765
    Abstract: The present invention relates to an improved process for the preparation of Valacyclovir or pharmaceutically acceptable salts thereof, which comprises reaction of amine-protected Valacyclovir or its salt with deprotecting agent in a continuous flow reactor.
    Type: Grant
    Filed: February 24, 2017
    Date of Patent: November 17, 2020
    Assignee: Aurobindo Pharma Ltd
    Inventors: Sandeep Jain, Komel Ansari, Subramanyam Maddala, Sivakumaran Meenakshisundaram
  • Aurora kinase inhibitors for inhibiting mitotic progression
    Patent number: 10836766
    Abstract: The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.
    Type: Grant
    Filed: June 1, 2018
    Date of Patent: November 17, 2020
    Assignee: MILLENIUM PHARMACEUTICALS, INC.
    Inventors: Christopher F. Claiborne, Todd B. Sells, Stephen G. Stroud
  • Serum stable pro-coelenterazine analogues
    Patent number: 10836767
    Abstract: Described are pro-coelenterazine analogues, methods for making the analogues, kits comprising the analogues, and methods of using the compounds for the detection of luminescence in luciferase-based assays or fragment complementary luciferase. The disclosed pro-coelenterazine analogues provide increased serum stability for live cell assays, and are capable of tuning the brightness and assay windows as needed for the applications.
    Type: Grant
    Filed: June 29, 2018
    Date of Patent: November 17, 2020
    Assignee: PROMEGA CORPORATION
    Inventors: Wenhui Zhou, Brock Binkowski, Poncho Meisenheimer, Andrew L. Niles, Kevin Kupcho, James Unch
  • N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists
    Patent number: 10836768
    Abstract: A method for treating and/or preventing polycystic ovary syndrome (PCOS) including the administration, to a patient in need thereof, of a pharmaceutically effective amount of a compound of Formula I or a pharmaceutically acceptable solvate thereof.
    Type: Grant
    Filed: November 29, 2018
    Date of Patent: November 17, 2020
    Assignee: Ogeda SA
    Inventors: Hamid Hoveyda, Guillaume Dutheuil, Graeme Fraser
  • Substituted pyrrolizine compounds and uses thereof
    Patent number: 10836769
    Abstract: This application relates generally to certain substituted pyrrolizine compounds, and pharmaceutical compositions which inhibit HBV replication, and methods of making and using them.
    Type: Grant
    Filed: February 25, 2019
    Date of Patent: November 17, 2020
    Assignee: GILEAD SCIENCES, INC.
    Inventors: David Alan Gutierrez, Tetsuya Kobayashi, Scott E. Lazerwith, Rick Andrew Lee, Philip Anthony Morganelli, Hyung-Jung Pyun
  • Imidazopyridazine compounds useful as modulators of IL-12, IL-23 and/or INF alpha responses
    Patent number: 10836770
    Abstract: Compounds of formula I or a stereoisomer or pharmaceutically-acceptable salt thereof, are useful in the modulation of IL-12, IL-23 and/or IFNa, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of formula I are useful for the treatment of inflammatory or autoimmune diseases.
    Type: Grant
    Filed: October 2, 2017
    Date of Patent: November 17, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Steven H. Spergel, Michael E. Mertzman
  • Compositions for activating pyruvate kinase
    Patent number: 10836771
    Abstract: Compositions for the activation of PKR are provided, as well as therapeutic administration of the compositions for the treatment of pyruvate kinase-related medical conditions, such as pyruvate kinase deficiency (PKD).
    Type: Grant
    Filed: October 4, 2019
    Date of Patent: November 17, 2020
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Neal Green, Gary Gustafson, David R. Lancia, Jr., Lorna Mitchell, Tatiana Shelekhin
  • DNA polymerase IIIC inhibitors and use thereof
    Patent number: 10836772
    Abstract: The present invention relates to compounds and methods useful for inhibiting the DNA polymerase IIIC enzyme. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of Gram-positive bacterial infections.
    Type: Grant
    Filed: June 15, 2020
    Date of Patent: November 17, 2020
    Assignee: Acurx Pharmaceuticals, LLC
    Inventors: Xiang Y. Yu, Li H. Xing, Minghua Wang, Casey McComas, Michael Silverman, Richard Soll
  • 6-fluoro-2-methylbenzo[d]thiazol-5-yl compounds
    Patent number: 10836773
    Abstract: The present invention provides a compound of Formula I: wherein R is hydrogen or methyl; and Z is: or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula I for treating neurodegenerative diseases, such as Alzheimer's disease.
    Type: Grant
    Filed: July 28, 2020
    Date of Patent: November 17, 2020
    Assignee: Eli Lilly and Company
    Inventors: Nicolas Jacques Francois Dreyfus, Jose Eduardo Lopez, Leonard Larry Winneroski, Jr., Eric Michael Woerly