Additional Hetero Ring Attached Directly Or Indirectly To The Four-membered Hetero Ring By Nonionic Bonding Patents (Class 514/210.18)
  • Patent number: 10729688
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs 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: March 27, 2019
    Date of Patent: August 4, 2020
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Jorden Kass, Byung-Chul Suh, Hui Cao, Wei Li, Xiaowen Peng, Xuri Gao, Yat Sun Or
  • Patent number: 10724102
    Abstract: Provided herein are methods of treating a subject having a cancer, methods of selecting a treatment for a subject having a cancer, methods of selecting a subject having a cancer for a treatment that does not include a Trk inhibitor, methods of determining the likelihood that a subject having a cancer will have a positive response to a treatment with a Trk inhibitor, methods of predicting the efficacy of a Trk inhibitor in a subject having cancer, methods of determining a subject's risk for developing a Trk inhibitor-resistant cancer, and methods of determining the presence of a Trk inhibitor-resistant cancer in a subject, based on the detection of a cell from a sample from the subject that has at least one of the point mutations in NTRK1 and/or NTRK2 and/or NTRK3.
    Type: Grant
    Filed: October 26, 2016
    Date of Patent: July 28, 2020
    Assignees: Loxo Oncology, Inc., Array BioPharma, Inc.
    Inventors: Nisha Nanda, Joshua H. Bilenker, James F. Blake, Gabrielle R. Kolakowski, Barbara J. Brandhuber, Steven W. Andrews
  • Patent number: 10723700
    Abstract: The present disclosure relates to tosylate salts 1-{[4-(methoxymethyl)-4-({[(1R,2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid, methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of the LSD1-associated or mediated diseases such as cancer.
    Type: Grant
    Filed: June 20, 2019
    Date of Patent: July 28, 2020
    Assignee: Incyte Corporation
    Inventors: Yongchun Pan, Wayne Han, Ganfeng Cao, Zhongjiang Jia, Jiacheng Zhou
  • Patent number: 10696661
    Abstract: Anti-angiogenic treatments, for example treatment of ocular neovascularization or cancer, treatments of hyperpermeability disorders, treatments of neuropathic and neurodegenerative disorders, pain treatments, methods of treating or preventing fibrosis and compounds for use in such methods are described.
    Type: Grant
    Filed: October 14, 2016
    Date of Patent: June 30, 2020
    Assignee: Exonate Limited
    Inventors: David Bates, Jonathan Morris, Hamish Toop, Jennifer Batson, Andrew David Morley
  • Patent number: 10683269
    Abstract: The invention relates to novel compounds of formula I which are inhibitors of deubiquitylating enzymes (DUBs) and/or desumoylating enzymes. In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 7 or ubiquitin specific peptidase 7 (USP7). The invention further relates to methods for the preparation of these compounds and to their use in the treatment of cancer.
    Type: Grant
    Filed: March 17, 2017
    Date of Patent: June 16, 2020
    Assignee: MISSION THERAPEUTICS LIMITED
    Inventors: Karl Richard Gibson, Alison Jones, Mark Ian Kemp, Andrew Madin, Martin Lee Stockley, Gavin Alistair Whitlock, Michael D Woodrow, Keith Allan Menear
  • Patent number: 10676472
    Abstract: The invention relates to crystalline salts of a compound having the structure of formula (I), methods for their preparation, and related pharmaceutical compositions comprising the crystalline salt. The invention further relates to methods of treating or preventing cancer or an immunological or neurological disease comprising administering a crystalline salt of the invention.
    Type: Grant
    Filed: June 7, 2019
    Date of Patent: June 9, 2020
    Assignee: Calithera Biosciences, Inc.
    Inventors: Timothy F. Stanton, James J. Springer, Jacqueline N. Williams
  • Patent number: 10662159
    Abstract: Provided herein are compounds and pharmaceutical compositions for selectively inhibiting serine hydrolase a/b-hydrolase domain 6 (ABHD6) and dually inhibiting ABHD6 and monoacylglycerol lipase (MGL). The compounds and pharmaceutical compositions disclosed herein are useful for treating a number of therapeutic conditions related to cannabinergic receptor function such as pain, inflammation, neuropathy, neurodegenerative diseases, anxiety disorders, motor function disorder, metabolic disorder, glaucoma and chemotherapy-induced nausea and vomiting and cancer.
    Type: Grant
    Filed: November 21, 2018
    Date of Patent: May 26, 2020
    Assignee: MAKSCIENTIFIC, LLC
    Inventors: Alexandros Makriyannis, Michael Malamas, Manjunath Lamani, Shrouq I. Farah
  • Patent number: 10654837
    Abstract: Potent 5-HT2B antagonist of Formula (A), including stereochemically isomeric forms, and salts, hydrates, solvates thereof and their use wherein R1 to R4 and Ar have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them, alone or in combination with other drugs, in fibrosis and/or cirrhosis prevention or therapy.
    Type: Grant
    Filed: February 6, 2018
    Date of Patent: May 19, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: Zhao-Kui Wan, Haibing Guo, Koen Vandyck, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri
  • Patent number: 10647696
    Abstract: Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Grant
    Filed: September 12, 2017
    Date of Patent: May 12, 2020
    Assignee: ChemoCentryx, Inc.
    Inventors: Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jay Powers, Ju Yang
  • Patent number: 10647708
    Abstract: A compound of formula (I) wherein: R1 is optionally one or more halo or methyl groups; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted C5-12 heteroaryl.
    Type: Grant
    Filed: September 3, 2015
    Date of Patent: May 12, 2020
    Assignee: CTXT PTY. LTD
    Inventors: Richard Charles Foitzik, Michelle Ang Camerino, Scott Raymond Walker, H. Rachel Lagiakos
  • Patent number: 10626112
    Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. The compound has a superior TRPA1 antagonist activity, and can provide a medicament useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.
    Type: Grant
    Filed: July 28, 2016
    Date of Patent: April 21, 2020
    Assignee: EA PHARMA CO., LTD.
    Inventors: Kaori Kobayashi, Tamotsu Suzuki, Tomohiro Fujii, Tatsuya Okuzumi
  • Patent number: 10555941
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Grant
    Filed: March 14, 2016
    Date of Patent: February 11, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings
  • Patent number: 10512638
    Abstract: The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine 5 receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
    Type: Grant
    Filed: December 19, 2016
    Date of Patent: December 24, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael T. Rudd, David M. Tellers, Jenny Miu-Chun Wai
  • Patent number: 10493074
    Abstract: N-{(R)-1-[8-Chloro-2-(1-oxypyridin-3-yl)-quinolin-3-yl]-2,2,2-trifluoroethyl}-pyrido[3,2-d]pyrimidin-4-ylamine is effective in the treatment and/or prevention of Sjögren's syndrome.
    Type: Grant
    Filed: April 20, 2016
    Date of Patent: December 3, 2019
    Assignee: UCB BIOPHARMA SPRL
    Inventors: Rodger Anthony Allen, Francesca Barone, William Anthony Fahy, Saba Nayar
  • Patent number: 10487045
    Abstract: The present invention provides a pharmaceutical composition for treating or preventing a cognitive disease or disorder, containing a compound represented by Formula (I), an enantiomer thereof, a diastereomer thereof, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 26, 2017
    Date of Patent: November 26, 2019
    Assignees: Tohoku University, Brain Innovation Co., Inc.
    Inventors: Shigeki Moriguchi, Koji Fukunaga, Yoshiharu Iwabuchi
  • Patent number: 10487068
    Abstract: Compounds of formula I: or pharmaceutical salts thereof, wherein m, n, A, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Grant
    Filed: November 1, 2017
    Date of Patent: November 26, 2019
    Assignee: Genentech, Inc.
    Inventors: Benjamin Fauber, Monique Bodil van Niel, Andrew Cridland, Christopher Hurley, Jonathan Killen, Stuart Ward
  • Patent number: 10463671
    Abstract: The present invention relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and one or more other therapeutic agents, particularly anticancer agents such as prednisone, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: November 5, 2019
    Assignee: Epizyme, Inc.
    Inventors: Heike Keilhack, Sarah K. Knutson, Kevin W. Kuntz
  • Patent number: 10464956
    Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
    Type: Grant
    Filed: February 14, 2019
    Date of Patent: November 5, 2019
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Venkat Rao Gadhachanda, Qiuping Wang, Godwin Pais, Akihiro Hashimoto, Dawei Chen, Xiangzhu Wang, Atul Agarwal, Milind Deshpande, Avinash S. Phadke
  • Patent number: 10457655
    Abstract: The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes.
    Type: Grant
    Filed: October 17, 2017
    Date of Patent: October 29, 2019
    Assignee: FORMA THERAPEUTICS, INC.
    Inventors: Kenneth W. Bair, David R. Lancia, Jr., Hongbin Li, James Loch, Wei Lu, Matthew W. Martin, David S. Millan, Shawn E.R. Schiller, Mark J. Tebbe
  • Patent number: 10407445
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C 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 HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: January 27, 2016
    Date of Patent: September 10, 2019
    Assignees: Enanta Pharmaceuticals, Inc., Novartis AG
    Inventors: Yao-Ling Qiu, Hui Cao, Xiaowen Peng, Xuri Gao, Yat Sun Or, Zachary Kevin Sweeney
  • Patent number: 10392401
    Abstract: The present invention relates to crystal form A of a compound. The present invention also discloses a preparation method and a pharmaceutical composition of the crystal form A. The crystal form A has strong hypoglycemic activity in vivo and is expected to be a novel pharmaceutically active ingredient for treating or preventing type II diabetes and/or complications of type II diabetes.
    Type: Grant
    Filed: February 3, 2016
    Date of Patent: August 27, 2019
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Hong Liu, Jiang Wang, Jian Li, Jia Li, Jingya Li, Shengbin Zhou, Mingbo Su, Hualiang Jiang, Xiaomin Luo, Kaixian Chen
  • Patent number: 10377753
    Abstract: Substituted 4-azaindoles as NR2B receptor ligands. Such compounds may be used in NR2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by NR2B receptor activity.
    Type: Grant
    Filed: March 20, 2018
    Date of Patent: August 13, 2019
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Christa C. Chrovian, Michael A. Letavic, Jason C. Rech, Akinola Soyode-Johnson, Jessica L. Wall
  • Patent number: 10377759
    Abstract: The present invention relates to a compound represented by general formula (I) (wherein, all symbols represent the same meanings as the symbols set forth in the specification), a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug of any of these. Since the compound has a Brk inhibitory activity, the compound is useful as a drug ingredient for the prevention and/or treatment of Brk-related diseases such as cancer, for example.
    Type: Grant
    Filed: June 21, 2016
    Date of Patent: August 13, 2019
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shingo Yamamoto, Hiroshi Tokura, Masakuni Kurono, Yoshinori Nomura, Shingo Hotta
  • Patent number: 10370727
    Abstract: Provided herein are methods of treating a subject having a cancer, methods of selecting a treatment for a subject having a cancer, methods of selecting a subject having a cancer for a treatment that does not include a Trk inhibitor, methods of determining the likelihood that a subject having a cancer will have a positive response to a treatment with a Trk inhibitor, methods of predicting the efficacy of a Trk inhibitor in a subject having cancer, methods of determining a subject's risk for developing a Trk inhibitor-resistant cancer, and methods of determining the presence of a Trk inhibitor-resistant cancer in a subject, based on the detection of a cell from a sample from the subject that has at least one of the the point mutations in NTRK1 and/or NTRK2 and/or NTRK3.
    Type: Grant
    Filed: October 16, 2017
    Date of Patent: August 6, 2019
    Assignees: Loxo Oncology, Inc., Array BioPharma, Inc.
    Inventors: Nisha Nanda, Joshua H. Bilenker, James F. Blake, Gabrielle R. Kolakowski, Barbara J. Brandhuber, Steven W. Andrews
  • Patent number: 10329288
    Abstract: The invention provides processes of preparation thereof useful in the preparation of compounds that can be used as CHK1 inhibitors.
    Type: Grant
    Filed: August 21, 2014
    Date of Patent: June 25, 2019
    Assignees: Genentech, Inc., Array BioPharma Inc.
    Inventors: Chong Han, Keena Green, Francis Gosselin, Michelangelo Scalone, Paul J. Nichols, Weidong Liu, Keith L. Spencer, Zackary D. Crane, Peter J. Stengel, Sagar Shakya
  • Patent number: 10329297
    Abstract: The present invention relates to compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of IDO, and for the treatment of IDO-related disorders.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: June 25, 2019
    Assignee: Merck Patent GmbH
    Inventor: Brian A. Sherer
  • Patent number: 10323019
    Abstract: The present invention provides compounds of the formula below (I?): where R, and R1-R3 are as described herein, methods of treating patients for certain types of autoimmune diseases and cancer, and processes for preparing the compounds.
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: June 18, 2019
    Assignee: Eli Lilly and Company
    Inventors: Jolie Anne Bastian, Joshua Ryan Clayton, David Andrew Coates, Daniel Jon Sall, Timothy Andrew Woods
  • Patent number: 10314844
    Abstract: Inhibitors for Bruton's Tyrosine Kinase (BTK) are disclosed as are compositions thereof, methods for their preparation, and methods for their use.
    Type: Grant
    Filed: February 23, 2018
    Date of Patent: June 11, 2019
    Assignees: GILEAD SCIENCES, INC., ONO PHARMACEUTICAL CO., LTD.
    Inventors: Seung H. Lee, Shingo Yamamoto
  • Patent number: 10316030
    Abstract: The invention relates to crystalline salts of a heterocyclic compound, methods of their preparation, and related pharmaceutical preparations thereof. The invention further relates to methods of treatment using the crystalline salts of the invention.
    Type: Grant
    Filed: August 7, 2015
    Date of Patent: June 11, 2019
    Assignee: Calithera Biosciences, Inc.
    Inventors: Timothy F. Stanton, James J. Springer, Jacqueline N. Williams
  • Patent number: 10301318
    Abstract: The invention described herein relates generally to neuroactive compounds and compositions for the treatment psychotic disorders, methods for treating psychosis using these neuroactive compounds, and methods for screening for novel neuroactive compounds. Certain aspects are directed to a family of compounds called “finazines.” Certain aspects are directed to in vivo screening methods using high-through-put behavioral assays in zebrafish.
    Type: Grant
    Filed: June 25, 2015
    Date of Patent: May 28, 2019
    Assignee: The General Hospital Corporation
    Inventors: Randall T. Peterson, Andrew J. Rennekamp, David Kokel, You Wang
  • Patent number: 10294223
    Abstract: Compounds that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Grant
    Filed: November 8, 2017
    Date of Patent: May 21, 2019
    Assignee: PRINCIPIA BIOPHARMA, INC.
    Inventors: Erik Verner, Kenneth Albert Brameld
  • Patent number: 10294202
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof: wherein R1, R2, R3, R4, R5, R6, Q1, Q2, Y1, and Y2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: December 2, 2014
    Date of Patent: May 21, 2019
    Assignee: FMC CORPORATION
    Inventors: Andrew Duncan Satterfield, Thomas Paul Selby, David Andrew Travis, Kanu Maganbhai Patel, Andrew Edmund Taggi
  • Patent number: 10287295
    Abstract: Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R? are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-?, and can be used to treat disease by blocking TGF-? signaling.
    Type: Grant
    Filed: January 2, 2018
    Date of Patent: May 14, 2019
    Assignees: Rigel Pharmaceuticals, Inc., Bristol-Meyers Squibb Company
    Inventors: Todd Kinsella, Marina Gelman, Hui Hong, Ihab S. Darwish, Rajinder Singh, Jiaxin Yu, Robert M. Borzilleri, Upender Velaparthi, Peiying Liu, Chetan Padmakar Darne, Hasibur Rahaman, Jayakumar Sankara Warrier
  • Patent number: 10280169
    Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.
    Type: Grant
    Filed: December 11, 2014
    Date of Patent: May 7, 2019
    Assignee: BIOGEN MA INC.
    Inventors: Brian T. Hopkins, Bin Ma, Timothy Raymond Chan, Gnanasambandam Kumaravel, Hua Miao, Andrea Bertolotti-Ciarlet, Kevin Otipoby
  • Patent number: 10280159
    Abstract: The invention relates to (hetero)cyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor.
    Type: Grant
    Filed: December 22, 2016
    Date of Patent: May 7, 2019
    Assignee: ABBVIE DEUTSCHLAND GMBH & CO. KG
    Inventors: Wilhelm Amberg, Udo Lange, Herve Geneste, Michael Ochse, Ralf Biesinger, Frank Oellien
  • Patent number: 10238633
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Grant
    Filed: June 6, 2017
    Date of Patent: March 26, 2019
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ralf Anderskewitz, Florian Binder, Matthias Grauert, Marc Grundl, Peter Wilhelm Haebel, Thorsten Oost, Alexander Pautsch, Stefan Peters, Viktor Vintonyak
  • Patent number: 10221146
    Abstract: The invention provides certain bicyclic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2, R3, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.
    Type: Grant
    Filed: October 12, 2017
    Date of Patent: March 5, 2019
    Assignees: Lycera Corporation, Merck Sharp & Dohme Corp.
    Inventors: Thomas D. Aicher, Chad A. VanHuis, William D. Thomas, John K. MacLean, Brian M. Andresen, Kenneth J. Barr, Corey E. Bienstock, Neville J. Anthony, Matthew Daniels, Kun Liu, Yuan Liu, Catherine M. White, Blair T. Lapointe, Nunzio Sciammetta, Vladimir Simov
  • Patent number: 10201546
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: February 12, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings, Kelly McClure, Virginia Tanis
  • Patent number: 10189836
    Abstract: Compounds of Formula (I) and methods of use as Janus kinase inhibitors are described herein.
    Type: Grant
    Filed: June 15, 2018
    Date of Patent: January 29, 2019
    Assignee: Genentech, Inc.
    Inventors: Yun-Xing Cheng, Rongbao Hua, Terry Kellar, Wei Li, Paul Gibbons, Mark Edward Zak
  • Patent number: 10183937
    Abstract: The present invention relates to 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: November 21, 2017
    Date of Patent: January 22, 2019
    Assignee: Bayer Aktiengesellschaft
    Inventors: Adam James Davenport, Nico Bräuer, Oliver Martin Fischer, Andrea Rotgeri, Antje Rottmann, Ioana Neagoe, Jens Nagel, Anne-Marie Godinho-Coelho, Jürgen Klar
  • Patent number: 10160760
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. The compounds of this invention have formula I-A or I-B: wherein the variables are as defined herein.
    Type: Grant
    Filed: December 5, 2014
    Date of Patent: December 25, 2018
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jean-Damien Charrier, Christopher John Davis, Damien Fraysse, Gorka Etxebarria I Jardi, Simon Pegg, Francoise Pierard, Joanne Pinder, John Studley, Carl Zwicker, Tapan Sanghvi, Michael Waldo, Ales Medek, David Matthew Shaw, Maninder Panesar, Yuegang Zhang, Naziha Alem
  • Patent number: 10160763
    Abstract: Described are compounds that disrupt the WDR5-MLL1 protein-protein interaction, pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating disorders and conditions in a subject.
    Type: Grant
    Filed: September 13, 2017
    Date of Patent: December 25, 2018
    Assignee: Vanderbilt University
    Inventors: Stephen W. Fesik, Shaun R. Stauffer, William P. Tansey, Edward T. Olejniczak, Jason Phan, Feng Wang, KyuOk Jeon, Rocco D. Gogliotti
  • Patent number: 10138230
    Abstract: The present invention relates to compounds of formula (I): wherein R1, R2, R3, R4a, R4b, R4C, R4d, L, A, Q, W and HET are each as defined herein. The compounds of the present invention are inhibitors of autotaxin (ATX) enzyme activity. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions (e.g. fibrosis) in which ATX activity is implicated.
    Type: Grant
    Filed: February 4, 2016
    Date of Patent: November 27, 2018
    Assignee: Cancer Research Technology Limited
    Inventors: Francesca Blum, James Lindsay Carr, Pritom Shah, Maria Del Mar Jimenez Quesada, Irene Farre Gutierrez
  • Patent number: 10118913
    Abstract: Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.
    Type: Grant
    Filed: March 30, 2018
    Date of Patent: November 6, 2018
    Assignee: 3-V Biosciences, Inc.
    Inventors: Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu, Allan S. Wagman
  • Patent number: 10087167
    Abstract: Compounds of Formula I, including their salts, as well as compositions and methods of using the compounds are set forth. The compounds have activity against hepatitis C virus (HCV) and areuseful in treating those infected with HCV.
    Type: Grant
    Filed: February 17, 2016
    Date of Patent: October 2, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhiwei Yin, John F. Kadow
  • Patent number: 10085996
    Abstract: A pharmaceutical combination comprising: (a) a phosphatidylinositol-3-kinase inhibitor selected from 5-(2,6-di-morpholin-4-yl-pyrimidin-4-yl)-4-trifluoromethyl-pyridin-2-ylamine, (S)-Pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide) or any pharmaceutically acceptable salt thereof and (b) a gonadorelin agonist and, optionally, (c) an antiestrogen agent, particularly for use in the treatment or prevention of a cancer; uses of such a combination in the preparation of a medicament for the treatment or prevention of a cancer; pharmaceutical compositions of the combination of said therapeutic agents and methods of treating a cancer in a subject comprising administering to said subject a therapeutically effective amount of such a combination.
    Type: Grant
    Filed: July 11, 2017
    Date of Patent: October 2, 2018
    Inventors: Samit Hirawat, Cristian Massacesi
  • Patent number: 10065945
    Abstract: The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
    Type: Grant
    Filed: January 20, 2015
    Date of Patent: September 4, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Timothy A. Blizzard, Brian T. Campbell, Helen Y. Chen, John S. Debenham, Sunita V. Dewnani, Byron Dubois, Candido Gude, Zack Zhiqiang Guo, Bart Harper, Zhiyong Hu, Songnian Lin, Ping Liu, Ming Wang, Feroze Ujjainwalla, Jiayi Xu, Libo Xu, Rui Zhang
  • Patent number: 10030013
    Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.
    Type: Grant
    Filed: September 12, 2017
    Date of Patent: July 24, 2018
    Assignee: Merck Patent GmbH
    Inventors: Catherine Jorand-Lebrun, Reinaldo Jones, Annie Cho Won, Ngan Nguyen, Theresa L. Johnson, Lizbeth Celeste Deselm, Kausik Panda
  • Patent number: 10022376
    Abstract: A compound having the structure: or a pharmaceutically acceptable salt or solvate thereof, wherein A and A? are C or N, where C may be substituted by halo or C1-C6 alkyl; R and R0 are selected from the group consisting of H, C1-C6 alkyl, —(CH2)n—W, etc., where W is 5- or 6-membered heteroaryl or heterocyclic containing N, S and/or O atoms, —NR?SO2—R?, etc., where R? and R? are C1-C6 alkyl, etc.; wherein each alkyl, etc., may be substituted; or, R and Ro and the N atom to which they are bonded together to form a monocyclic or bicyclic heterocyclic ring, etc.; R1 is H, halo or cyano; R2 and R2? are H, C1-C6 alkyl, etc.; X is a bond, etc.; R3 is H, C1-C4 alkyl, etc.; Y is a bond, —(CH2)m—, etc. The invention also relates to compositions and uses in the treatment of various diseases.
    Type: Grant
    Filed: November 3, 2016
    Date of Patent: July 17, 2018
    Assignee: Pfizer Inc.
    Inventors: Jotham Wadsworth Coe, Christoph Martin Dehnhardt, Peter Jones, Yogesh Anil Sabnis, Joseph Walter Strohbach, Florian Michel Wakenhut, Gavin Alistair Whitlock
  • Patent number: 10023589
    Abstract: Compounds of the formula I or II: wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: July 17, 2018
    Assignees: Hoffmann-La Roche Inc., Roche Palo Alto LLC
    Inventors: Nidhi Arora, Shaoqing Chen, Johannes Cornelius Hermann, Andreas Kuglstatter, Sharada Shenvi Labadie, Clara Jeou Jen Lin, Matthew C. Lucas, Amy Geraldine Moore, Eva Papp, Francisco Xavier Talamas, Jutta Wanner, Yansheng Zhai