Patents Issued in October 6, 2020
  • Patent number: 10793529
    Abstract: Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.
    Type: Grant
    Filed: October 15, 2018
    Date of Patent: October 6, 2020
    Assignee: ARENA PHARMACEUTICALS, INC.
    Inventors: Thuy-Anh Tran, Rena Hayashi, Jason B. Ibarra, Brett Ullman, Ning Zou
  • Patent number: 10793530
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R, R1, R2, R3, m and n are defined herein, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Grant
    Filed: January 22, 2018
    Date of Patent: October 6, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Holger Wagner
  • Patent number: 10793531
    Abstract: Compounds of Formula (I), which are activators of long form cyclic nucleotide phosphodiesterase-4 (PDE4) enzymes, are provided. Methods and uses of these compounds for the treatment or prevention of disorders requiring a reduction of second messenger responses mediated by cyclic 3?,5?-adenosine monophosphate (cAMP) are also described.
    Type: Grant
    Filed: July 10, 2019
    Date of Patent: October 6, 2020
    Assignee: Mironid Limited
    Inventor: Julia Adam
  • Patent number: 10793532
    Abstract: A method is described for production of a high purity compound of the formula (I) in crystalline form of the modification A. In this, starting from high purity gadobutrol, the gadolinium is removed by decomplexation with oxalic acid, and then with a calcium salt the calcium complex is produced in high purity. During the crystallization, a water equivalent of 9-11 weight % is set. The crystalline form of the modification A of the compound of the formula (I) is used in the production of Gadovist.
    Type: Grant
    Filed: September 11, 2017
    Date of Patent: October 6, 2020
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Johannes Platzek, Wilhelm Trentmann
  • Patent number: 10793533
    Abstract: The present invention relates to new class of dimeric macrocycles capable of chelating paramagnetic metal ions, their chelated complexes with the paramagnetic metal ions and the use thereof as contrast agents, particularly suitable for Magnetic Resonance Imaging (MRI) analysis.
    Type: Grant
    Filed: December 11, 2017
    Date of Patent: October 6, 2020
    Assignee: BRACCO IMAGING S.P.A.
    Inventors: Valeria Boi, Roberta Napolitano, Luciano Lattuada, Giovanni Battista Giovenzana
  • Patent number: 10793534
    Abstract: The invention relates to 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.
    Type: Grant
    Filed: July 10, 2019
    Date of Patent: October 6, 2020
    Assignee: Albireo AB
    Inventors: Per-Göran Gillberg, Jan Mattsson, Ingemar Starke, Santosh S. Kulkarni
  • Patent number: 10793535
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: October 6, 2020
    Assignee: Calithera Biosciences, Inc.
    Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
  • Patent number: 10793536
    Abstract: The present application provides a vortioxetine pamoic acid salt, which includes a crystal form, a solvate or an amorphous substance of the vortioxetine pamoic acid salt. The present application provides a preparation method and use of the vortioxetine pamoic acid salt and the crystal form thereof. The vortioxetine pamoic acid salt prepared in the present application prolongs the residence time of the vortioxetine in vivo, achieving a slow release of the vortioxetine in vivo, and is suitable for preparing a long-acting dosage form.
    Type: Grant
    Filed: March 28, 2017
    Date of Patent: October 6, 2020
    Assignee: SHANGHAI SYNERGY PHARMACEUTICAL SCIENCES CO., LTD
    Inventors: Yunfei Li, Xiaoer Xia, Xin Xu, Zhen Zhang, Lei Liu, Xiaojuan Zhang, Liming Zhang, Dongsheng Li, Yijin Wang, Jian Ge
  • Patent number: 10793537
    Abstract: Disclosed herein are a method of acid saccharification of biomass and a method of polymerization of furan compounds. The method of acid saccharification of biomass comprises recovering pentose-derived furan compounds produced during the acid saccharification process of biomass. The method of acid saccharification of biomass comprises introducing furan compounds into the acid saccharification process of biomass, to produce and recover furan polymers.
    Type: Grant
    Filed: November 14, 2019
    Date of Patent: October 6, 2020
    Assignee: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Jeong-Myeong Ha, Hyemin Yang, Ye Seul Jeong, Jae Wook Choi, Dong Jin Suh, Young Hyun Yoon, Gi Seok Yang, Ung Lee
  • Patent number: 10793538
    Abstract: The present invention provides compounds of formula (I): or a pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein W, X, n, s, t, and Ra are as described herein. The present invention relates generally to selective inhibitors of histone deacetylase and to methods of making and using them.
    Type: Grant
    Filed: January 24, 2018
    Date of Patent: October 6, 2020
    Assignee: The Broad Institute, Inc.
    Inventors: Edward Holson, Fanny Lazzaro, David Olson, Florence Fevrier Wagner, Michel Weiwer
  • Patent number: 10793539
    Abstract: The invention relates to a process for the preparation of tocols [tocopherols (T) and tocotrienols (T3)] and squalene from vegetable oil refining by-products like fatty acid distillates. It particularly relates to the process of preparation of tocopherols, tocotrienols and squalene without any degradation from the fatty acid distillates obtained during processing of oils from the palm.
    Type: Grant
    Filed: November 27, 2017
    Date of Patent: October 6, 2020
    Assignee: PRAJ INDUSTRIES LIMITED
    Inventors: Pallavi Vinitkumar Pathak, Prajakt Subhash Charhate, Mangesh Ganesh Kurkarni
  • Patent number: 10793540
    Abstract: The present invention provides an industrially applicable method for production of a fluorine-containing cyclopropane carboxylic acid compound useful as an intermediate for pharmaceutical and agrichemical products. A fluorine-containing cyclopropane monoester is obtained by: forming a fluorine-containing cyclic sulfate with the use of a fluorine-containing diol compound and sulfuryl fluoride (as a cyclic sulfuric esterification step); reacting the fluorine-containing cyclic sulfate with a malonic diester, thereby forming a fluorine-containing cyclopropane diester (as a cyclopropanation step); and hydrolyzing the fluorine-containing cyclopropane diester (as a hydrolysis step).
    Type: Grant
    Filed: September 5, 2019
    Date of Patent: October 6, 2020
    Assignee: Central Glass Company, Limited
    Inventors: Takashi Kashiwaba, Takako Yamazaki, Shoko Ishii, Shunsuke Mimura, Masanori Fushimi, Ryuichi Okamoto, Haruki Kobayashi, Manabu Yasumoto
  • Patent number: 10793541
    Abstract: Disclosed herein is a process of making a compound of formula I The compound of formula I is an inhibitor of MEK and thus can be used to treat cancer.
    Type: Grant
    Filed: February 8, 2019
    Date of Patent: October 6, 2020
    Assignees: Exelixis, Inc., Genentech, Inc.
    Inventors: Sriram Naganathan, Nathan Guz, Matthew Pfeiffer, C. Gregory Sowell, Tracy Bostick, Jason Yang, Amit Srivastava, Neel Kumar Anand
  • Patent number: 10793542
    Abstract: The present invention provides a compound of formula (1): wherein X, Y, Z1, Z2, R1, R2, A, B, p and q are as disclosed in the specification. A pharmaceutical composition and a method for modulating the Hedgehog pathway are also provided. The present invention rurthe r provides a process for preparing the compound.
    Type: Grant
    Filed: November 22, 2017
    Date of Patent: October 6, 2020
    Assignee: DEVELOPMENT CENTER FOR BIOTECHNOLOGY
    Inventors: Mann-Yan Kuo, Ying-Shuan Lee, Yann-Yu Lu, Chia-Wei Liu, Seline Hsieh, Ju-Ying Yang
  • Patent number: 10793543
    Abstract: The present invention provides a compound represented by formula (I), or a pharmaceutically acceptable salt, a solvate, an ester, an acid, a metabolite or a prodrug thereof. The compound itself in the present invention or in combination with at least one therapeutic agent can be used for preventing or treating diseases, disorders or symptoms caused by the adjustment of the activity of tyrosine kinase C-KIT, or affected by the activity of the tyrosine kinase C-KIT or involving in the activity of the tyrosine kinase C-KIT, especially cancers or other cell proliferation diseases.
    Type: Grant
    Filed: March 28, 2017
    Date of Patent: October 6, 2020
    Assignees: PRECEDO PHARMACEUTICALS CO., LTD, HEFEI GRACEVO BIO-MEDICINE CO., LTD
    Inventors: Qingsong Liu, Jing Liu, Qiang Wang, Beilei Wang, Feiyang Liu, Shuang Qi, Ziping Qi, Fengming Zou, Cheng Chen, Wenchao Wang, Chen Hu, Xiaochuan Liu, Wei Wang, Aoli Wang, Li Wang, Zhenquan Hu, Tao Ren
  • Patent number: 10793544
    Abstract: The present disclosure provides compounds that may be useful for inhibiting Wnt pathway comprising compounds of the formula: (Ia) or (Ib) wherein the variables are as defined herein. In some aspects, the compounds may be used to inhibit the Wnt pathway and used to treat cancer, myocardial infarction, osteopetrosis, or used in the maturation of a precursor cell to a mature cell. Also provided herein in are pharmaceutical compositions of the compounds described herein.
    Type: Grant
    Filed: August 31, 2017
    Date of Patent: October 6, 2020
    Inventors: Nageswari Yarravarapu, Chuo Chen, Lawrence Lum, Lin You, Chengwei Zhang, Xiaolei Wang, Lishu Zhang
  • Patent number: 10793545
    Abstract: The present application relates to novel substituted indazoles, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of endometriosis and endometriosis-associated pain and other endometriosis-associated symptoms such as dysmenorrhoea, dyspareunia, dysuria and dyschezia, of lymphoma, rheumatoid arthritis, spondyloarthritis (especially psoriatic spondyloarthritis and Bekhterev's disease), lupus erythematosus, multiple sclerosis, macular degeneration, COPD, gout, fatty liver disorders, insulin resistance, neoplastic disorders and psoriasis.
    Type: Grant
    Filed: April 5, 2019
    Date of Patent: October 6, 2020
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Ulrich Bothe, Holger Siebeneicher, Nicole Schmidt, Reinhard Nubbemeyer, Ulf Bömer, Judith Günther, Holger Steuber, Martin Lange, Christian Stegmann, Andreas Sutter, Alexandra Rausch, Christian Friedrich, Peter Hauff
  • Patent number: 10793546
    Abstract: Complexes and devices, such as organic light emitting devices and full color displays, including a compound of the formula wherein: M is Pd2+, Ir+, Rh+, or Au3+; each of V1, V2, V3, and V4 is coordinated to M and is independently N, C, P, B, or Si; each of L1, L2, L3, and L4 is independently a substituted or unsubstituted aryl, cycloalkyl, cycloalkenyl, heterocyclyl, heteroaryl, carbene, or N-heterocyclic carbene; and Z is O, S, NR, CR2, SiR2, BR, PR, where each R is independently substituted or unsubstituted C1-C4 alkyl or substituted or unsubstituted aryl.
    Type: Grant
    Filed: August 14, 2015
    Date of Patent: October 6, 2020
    Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY
    Inventors: Jian Li, Liang Huang, Tyler Fleetham
  • Patent number: 10793547
    Abstract: Compounds of Formula (I): pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed. Also disclosed are solid state forms of Compound 1 and salts and solvates thereof.
    Type: Grant
    Filed: December 8, 2017
    Date of Patent: October 6, 2020
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Alexander Russell Abela, Timothy Alcacio, Corey Anderson, Paul Timothy Angell, Minson Baek, Jeremy J. Clemens, Thomas Cleveland, Lori Ann Ferris, Peter Diederik Jan Grootenhuis, Raymond Stanley Gross, Anton V. Gulevich, Sara Sabina Hadida Ruah, Clara Kuang-Ju Hsia, Robert M. Hughes, Pramod Virupax Joshi, Ping Kang, Ali Keshavarz-Shokri, Haripada Khatuya, Paul John Krenitsky, Jason McCartney, Mark Thomas Miller, Prasuna Paraselli, Fabrice Jean Denis Pierre, Yi Shi, Muna Shrestha, David Andrew Siesel, Kathy Stavropoulos, Andreas P. Termin, Fredrick F. Van Goor, Johnny Uy, Timothy John Young, Jinglan Zhou
  • Patent number: 10793548
    Abstract: The present invention relates to a method for preparing a tyrosine kinase inhibitor and a derivative thereof. The present method has a short synthesis route, low costs, easy operation, and is suitable for large-scale production.
    Type: Grant
    Filed: April 27, 2017
    Date of Patent: October 6, 2020
    Assignee: Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Guaili Wu, Quanliang Zhang, Yongxing Cao
  • Patent number: 10793549
    Abstract: The present invention relates to a sulfuryl-substituted benzoheterocyclic derivative, a preparation method and medical use thereof. Particularly, disclosed is a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, and a preparation method and application thereof. The definition of each group in the formula can be found in the specification and the claims.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: October 6, 2020
    Assignees: SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD., YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Yunzhou Jin, Xiang Chen, Pengfei Cheng, Ping Bu, Leitao Zhang, Chong Wen, Yingtao Liu, Fusheng Zhou, Ming Weng, Jiong Lan
  • Patent number: 10793550
    Abstract: The invention provides 4-piperidin-chroman-7-sulfonamide derivatives and salts thereof that are sodium channel modulators, as well as compositions containing such a compound or salt and therapeutic methods for using such a compound, salt, or composition.
    Type: Grant
    Filed: March 22, 2018
    Date of Patent: October 6, 2020
    Assignee: GENENTECH, INC.
    Inventors: Daniel Sutherlin, Steven McKerrall, Kwong Wah Lai
  • Patent number: 10793551
    Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I or Formula II, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds X1, X2, X3, X4, X5, Y1, Y2, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the specification. The inventive Formula I and Formula II compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
    Type: Grant
    Filed: October 17, 2018
    Date of Patent: October 6, 2020
    Assignee: eFFECTOR Therapeutics Inc.
    Inventors: Justin T. Ernst, Siegfried H. Reich, Paul A. Sprengeler, Alan X. Xiang
  • Patent number: 10793552
    Abstract: The present invention provides compounds of the Formula (I), or a pharmaceutically acceptable salt thereof, where n and R1 are defined herein, methods of treating patients for liver disease, and processes for preparing the compounds.
    Type: Grant
    Filed: September 26, 2019
    Date of Patent: October 6, 2020
    Assignee: ELI LILLY AND COMPANY
    Inventors: David Andrew Coates, Luo Heng Qin, Yi Wei, Jingye Zhou
  • Patent number: 10793553
    Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TLR7/8 antagonists.
    Type: Grant
    Filed: July 17, 2018
    Date of Patent: October 6, 2020
    Assignee: Merck Patent GmbH
    Inventors: Brian A. Sherer, Nadia Brugger, Ruoxi Lan, Xiaoling Chen
  • Patent number: 10793554
    Abstract: The present disclosure reports solid forms of (4-(2-fluoro-4-(1-methyl-1H- benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone:
    Type: Grant
    Filed: October 29, 2019
    Date of Patent: October 6, 2020
    Assignee: Forma Therapeutics, Inc.
    Inventors: George P. Luke, Stephen Hubbs, Matthew W. Martin, Robert Wenslow, Yawei Shi, Jun Huang
  • Patent number: 10793555
    Abstract: Compounds of the formulae (I) or (II) wherein X is A is O, S, NR5 or CR16R17; R1 is for example hydrogen or C1-C20alkyl R2 is for example hydrogen, C1-C20alkyl or C6-C20aryl R5 for example is C1-C20alkyl; R7, R8, R9, R10 and R11 for example independently of each other are hydrogen. C1-C20alkyl, halogen, CN or NO2; Ar1 is for example unsubstituted or substituted C6-C20aryl, C3-C20heteroaryl, C6-C20aroyl, C3-C20heteroarylcarbonyl or or Ar1 is Ar2 is for example phenylene, all of which are unsubstituted or substituted M is for example unsubstituted or substituted C1-C20alkylene Y is a direct bond, O, S, NR5 or CO; Z1 is for example O or S; Z2 is a direct bond, O, S or NR5; and Q is CO or a direct bond.
    Type: Grant
    Filed: March 12, 2018
    Date of Patent: October 6, 2020
    Assignee: BASF SE
    Inventors: Kazuhiko Kunimoto, Hisatoshi Kura, Hiroshi Yamamoto, Yumiko Nakagawa, Toshikage Asakura, Kaori Sameshima
  • Patent number: 10793556
    Abstract: The invention relates to 8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
    Type: Grant
    Filed: June 24, 2019
    Date of Patent: October 6, 2020
    Assignee: GRUENENTHAL GMBH
    Inventors: Sven Kuehnert, Rene Michael Koenigs, Achim Kless, Anita Wegert, Paul Ratcliffe, Ruth Jostock, Thomas Koch, Klaus Linz, Wolfgang Schroeder
  • Patent number: 10793557
    Abstract: Compounds of general formula (I), of general formula (II), of general formula (III), of general formula (IV), of general formula (V), of general formula (VI), and their pharmaceutically acceptable salts, wherein all variables are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.
    Type: Grant
    Filed: April 1, 2019
    Date of Patent: October 6, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brandon D. Cash, Matthew Lloyd Childers, Jared N. Cumming, Duane E. DeMong, Andrew Marc Haidle, Timothy J. Henderson, James P. Jewell, Matthew A. Larsen, Jongwon Lim, Min Lu, Ryan D. Otte, Benjamin Wesley Trotter
  • Patent number: 10793558
    Abstract: Provided herein are compounds of Formula I, pharmaceutical compositions thereof, and methods of their use for treating, preventing, or ameliorating one or more symptoms of a neurological disease, neurodegenerative disorder, or diabetes.
    Type: Grant
    Filed: June 10, 2019
    Date of Patent: October 6, 2020
    Inventor: Russell Dahl
  • Patent number: 10793559
    Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.
    Type: Grant
    Filed: September 17, 2019
    Date of Patent: October 6, 2020
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Niall Andrew Anderson, Nicholas Paul Barton, Sebastien Andre Campos, Edward Paul Cannons, Anthony William James Cooper, Kenneth David Down, Kevin James Doyle, Julie Nicole Hamblin, Graham George Adam Inglis, Armelle Le Gall, Vipulkumar Kantibhai Patel, Simon Peace, Andrew Sharpe, Gemma Victoria White
  • Patent number: 10793560
    Abstract: Disclosed are compounds useful as inhibitors of the Wnt signalling pathway. Specifically, inhibitors of Porcupine (Porcn) are contemplated by the invention. In addition, the invention contemplates processes to prepare the compounds and uses of the compounds. The compounds of the invention may therefore be used in treating conditions mediated by the Wnt signalling pathway, for example, in treating cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia; or enhancing the effectiveness of an anti-cancer treatment.
    Type: Grant
    Filed: July 17, 2018
    Date of Patent: October 6, 2020
    Assignee: RedX Pharma PLC
    Inventors: Inder Bhamra, Matilda Bingham, Richard Testar, Louise Sargent, Craig Donoghue
  • Patent number: 10793561
    Abstract: 1,8-naphthyridinone compounds as modulators of an adenosine receptor are provided. The compounds may find use as therapeutic agents for the treatment of diseases mediated through a G-protein-coupled receptor signaling pathway and may find particular use in oncology.
    Type: Grant
    Filed: July 18, 2018
    Date of Patent: October 6, 2020
    Assignee: NUVATION BIO INC.
    Inventors: Son Minh Pham, Jiyun Chen, Amantullah Ansari, Pradeep S. Jadhavar, Varshavekumar S. Patil, Farha Khan, Sreekanth A. Ramachandran, Anil Kumar Agarwal, Sarvajit Chakravarty
  • Patent number: 10793562
    Abstract: Disclosed are compounds useful as inhibitors of the Wnt signalling pathway. Specifically, inhibitors of Porcupine (Porcn) are contemplated by the invention. In addition, the invention contemplates processes to prepare the compounds and uses of the compounds. The compounds of the invention may therefore be used in treating conditions mediated by the Wnt signalling pathway, for example, in treating cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia; or enhancing the effectiveness of an anti-cancer treatment.
    Type: Grant
    Filed: January 10, 2019
    Date of Patent: October 6, 2020
    Assignee: Redx Pharma PLC
    Inventors: Inder Bhamra, Michael Mathieson, Craig Donoghue, Richard Testar
  • Patent number: 10793563
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: January 28, 2019
    Date of Patent: October 6, 2020
    Assignees: MERCK PATENT GMBH, VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Matthew Bleich, Jean-Damien Charrier, Huijun Dong, Steven Durrant, Meredith Suzanne Eno, Gorka Etxebarria I Jardi, Simon Everitt, Damien Fraysse, Ronald Knegtel, Igor Mochalkin, Kiri North, Filippos Porichis, Hui Qiu, Robert Pullin, Pierre-Henri Storck, Heather Clare Twin, Yufang Xiao
  • Patent number: 10793564
    Abstract: The invention relates to compounds of formula (A) and formula (I): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are ?v?6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
    Type: Grant
    Filed: March 7, 2019
    Date of Patent: October 6, 2020
    Assignee: PLIANT THERAPEUTICS, INC.
    Inventors: Jacob Cha, Chengguo Dong, Timothy Hom, Lan Jiang, Katerina Leftheris, Hui Li, David J. Morgans, Jr., Manuel Munoz, Maureen Reilly, Yajun Zheng
  • Patent number: 10793565
    Abstract: Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
    Type: Grant
    Filed: March 8, 2019
    Date of Patent: October 6, 2020
    Assignee: Incyte Corporation
    Inventors: Liangxing Wu, Bo Shen, Meizhong Xu, Wenqing Yao
  • Patent number: 10793566
    Abstract: Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I):
    Type: Grant
    Filed: May 22, 2019
    Date of Patent: October 6, 2020
    Assignees: ZIBO BIOPOLAR CHANGSHENG PHARMACEUTICAL CO. LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Xibin Liao, Jia Li, Zhijian Lu, Yubo Zhou, Anhui Gao
  • Patent number: 10793567
    Abstract: Provided are compounds of the formula and pharmaceutically acceptable salts and composition thereof, which are useful in the treatment of conditions associated with inhibition of HDAC (e.g. HDAC2).
    Type: Grant
    Filed: January 11, 2018
    Date of Patent: October 6, 2020
    Assignee: Rodin Therapeutics, Inc.
    Inventors: Nathan Oliver Fuller, John A. Lowe, III
  • Patent number: 10793568
    Abstract: The invention relates to activators of FXR useful in the treatment of autoimmune disorders, liver disease, intestinal disease, kidney disease, cancer, and other diseases in which FXR plays a role, having the Formula (I): (I), wherein L1, A, X1, X2, R1, R2, and R3 are described herein.
    Type: Grant
    Filed: August 23, 2017
    Date of Patent: October 6, 2020
    Assignee: ARDELYX, INC.
    Inventors: Jianhua Chao, Rakesh Jain, Lily Hu, Jason Gustaf Lewis, Helene Baribault, Jeremy Caldwell
  • Patent number: 10793569
    Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, R3, R4, Ar and X1 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
    Type: Grant
    Filed: May 1, 2020
    Date of Patent: October 6, 2020
    Assignee: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Liqi He, Sanjeev Gangwar, Yam B. Poudel, Prasanna Sivaprakasam
  • Patent number: 10793570
    Abstract: The present invention provides methods for radiolabeling compounds useful as Hsp90 inhibitors. The present invention also provides intermediates useful in such methods, and compositions of radiolabeled compounds. The present invention provides, among other things novel methods for the synthesis of radiolabeled compounds. In certain embodiments, the present invention provides compounds of formula I.
    Type: Grant
    Filed: April 26, 2019
    Date of Patent: October 6, 2020
    Assignee: Memorial Sloan-Kettering Cancer Center
    Inventors: Stefan O. Ochiana, NagaVaraKishore Pillarsetty, Tony Taldone, Gabriela Chiosis
  • Patent number: 10793571
    Abstract: The present invention provides compounds of Formula (II) (e.g., compounds of Formula (I)), and pharmaceutically compositions thereof. Compounds of Formula (II) are believed to be binders of bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits using the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain-containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception.
    Type: Grant
    Filed: February 2, 2015
    Date of Patent: October 6, 2020
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: James E. Bradner, Nathanael S. Gray, Jun Qi, Michael R. McKeown, Dennis Buckley
  • Patent number: 10793572
    Abstract: Disclosed are novel compounds useful in the treatment of multiple sclerosis and other autoimmune diseases. The present invention describes compounds of formula (I) wherein: R1 is selected from H and CH3 R2 is selected from H, C4H9 alkyl, C6H13 alkyl and C3H6-phenyl, said phenyl optionally substituted by OH or OCH3, (1R,2S,5S)-5-methylcyclopent-3-ene-1,2-diol X is O or S Y is C, N or S.
    Type: Grant
    Filed: September 29, 2015
    Date of Patent: October 6, 2020
    Assignee: THE PROVOST FELLOWS FOUNDATION SCHOLARS AND THE OTHER MEMBERS OF BOARD OF THE COLLEGE OF THE HOLY AND UNDIVIDED TRINITY OF QUEEN ELIZABETH
    Inventors: John Michael Southern, Stephen J. Connon
  • Patent number: 10793573
    Abstract: A compound of the Formula I and optionally a pharmaceutically acceptable salt thereof is provided: Formula I, wherein, R is one selected from the group consisting of H and CH3; n is an integer ranging from 1 to 4; X is one selected from the group consisting of —CH2—, O, S, —NH—, —NHCHO—, —NHCOCH3—, and —NHCOCF3—; and Ar is one selected from the group consisting of (a) 1,4-phenyl, (b) 2?-fluoro-1,4-phenyl, and (c) 2,5-thienyl. Methods of treating a patient having cancer, targeting mitochondrial metabolism, and targeting SHMT2 and MTHFD2 using the compounds of this invention are disclosed.
    Type: Grant
    Filed: August 30, 2018
    Date of Patent: October 6, 2020
    Assignees: Duquesne University of The Holy Spirit, Wayne State University
    Inventors: Aleem Gangjee, Larry H. Matherly
  • Patent number: 10793574
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
    Type: Grant
    Filed: April 30, 2019
    Date of Patent: October 6, 2020
    Assignee: Nimbus Lakshmi, Inc.
    Inventors: Jeremy Robert Greenwood, Geraldine C. Harriman, Silvana Marcel Leit de Moradei, Craig E. Masse, Thomas H. McLean, Sayan Mondal
  • Patent number: 10793575
    Abstract: An oxoisoquinoline compound of the following formula: or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising the oxoisoquinoline compound or salt; and a method for treating B-cell lymphoma comprising administering the oxoisoquinoline compound or salt to a patient.
    Type: Grant
    Filed: November 24, 2017
    Date of Patent: October 6, 2020
    Assignee: CARNA BIOSCIENCES, INC.
    Inventors: Wataru Kawahata, Takao Kiyoi, Takayuki Irie, Tokiko Asami, Masaaki Sawa, Shigeki Kashimoto
  • Patent number: 10793576
    Abstract: The present invention provides a compound having a structure shown in formula (I) or an isomer, pharmaceutically acceptable solvate, or salt thereof. The compound is used as a Bruton's tyrosine kinase inhibitor, and has a higher inhibitory activity against BTK and less adverse effects.
    Type: Grant
    Filed: February 20, 2017
    Date of Patent: October 6, 2020
    Assignees: CHENGDU BRILLIANT PHARMACEUTICAL CO., LTD., CHENGDU HIGHBRED PHARMACEUTICAL CO., LTD.
    Inventors: Yingfu Li, Haoxi Huang, Guanfeng Liu, Tonghui Chen, Junfeng Ren, Zhonghai Su
  • Patent number: 10793577
    Abstract: Described herein are fused bicyclic compounds, compositions, and methods for their use for the treatment of disease.
    Type: Grant
    Filed: December 31, 2018
    Date of Patent: October 6, 2020
    Assignee: Akarna Therapeutics, Ltd.
    Inventors: Raju Mohan, Benjamin Anthony Pratt
  • Patent number: 10793578
    Abstract: A series of fused pentacyclic imidazole derivatives, being potent modulators of f benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders. In particular, the present invention is concerned with 5,7,8,15-tetrahydro-6H-8,15-methanobenzimidazo[1,2-b][2,5]benzodiazocin-6-one derivatives and analogs thereof.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: October 6, 2020
    Assignees: UCB Biopharma SRL, Sanofi
    Inventors: Jag Paul Heer, Jean Keyaerts