Additional Hetero Ring Attached Directly Or Indirectly To The Four-membered Hetero Ring By Nonionic Bonding Patents (Class 514/210.18)
  • 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: 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: 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: 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
  • Patent number: 10023519
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.
    Type: Grant
    Filed: September 8, 2015
    Date of Patent: July 17, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yan Shi, Ying Wang, Peter T. W. Cheng, Shung C. Wu
  • Patent number: 10004232
    Abstract: The invention relates to heteroarylpiperidine and -piperazine derivatives of formula (I) to agrochemically active salts thereof, to their use and also to methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants, to methods for producing such compositions and to treated seed, and also to the use thereof for controlling phytopathogenic harmful plants in agriculture, horticulture and forestry, in animal health, in materials protection and also in the household and hygiene sector. The present invention further relates to a method for producing heteroarylpiperidine and -piperazine derivatives.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: June 26, 2018
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Stefan Hillebrand, Tomoki Tsuchiya, Sebastian Hoffmann, Pierre Cristau, Pierre Wasnaire, Thomas Seitz, Juergen Benting, Ulrike Wachendorff-Neumann, Peter Jan Schmidt
  • Patent number: 9994551
    Abstract: Compounds of formula I: or pharmaceutical salts thereof, wherein R1, R2, R3 and R4 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: June 12, 2018
    Assignee: Genentech, Inc.
    Inventors: Benjamin Fauber, Monique Bodil van Niel, Andrew Cridland, Christopher Hurley, Jonathan Killen, Stuart Ward, Paul Winship
  • Patent number: 9988379
    Abstract: The present invention relates to a novel compound having GPR40 receptor agonist activity that promotes insulin secretion and inhibits blood sugar rise after glucose loading, and is thereby useful for the treatment of diabetes and complications thereof, the preparation method thereof and pharmaceutical composition containing them as an active ingredient.
    Type: Grant
    Filed: November 8, 2013
    Date of Patent: June 5, 2018
    Assignee: LG CHEM, LTD.
    Inventors: Sung Bae Lee, Seung Yup Paek, Sook Kyung Yoon, Seung Hyun Yoon, Jeung Soon Choi
  • Patent number: 9987278
    Abstract: Provided are a pharmaceutical composition for treating an FLT3 mutation-positive cancer; a mutant FLT3 inhibitor; and uses thereof.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: June 5, 2018
    Assignee: FUJIFILM Corporation
    Inventors: Tomoki Naoe, Hitoshi Kiyoi, Shinji Hagiwara, Masaru Takasaki, Daisuke Hirano, Toshiyuki Nakatani, Takeshi Yamaura
  • Patent number: 9980964
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: February 2, 2017
    Date of Patent: May 29, 2018
    Assignee: CELGENE CAR LLC
    Inventors: Nadia Haq, Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh, Zhendong Zhu
  • Patent number: 9963447
    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: July 8, 2016
    Date of Patent: May 8, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Christa C. Chrovian, Michael A. Letavic, Jason C. Rech, Akinola Soyode-Johnson, Jessica L. Wall
  • Patent number: 9951064
    Abstract: This invention relates to novel compounds which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.
    Type: Grant
    Filed: May 12, 2016
    Date of Patent: April 24, 2018
    Assignee: GENENTECH, INC.
    Inventors: Marian C. Bryan, Bryan Chan, Francois Diederich, Jennafer Dotson, Emily Hanan, Timothy Heffron, Michael Lainchbury, Robert Heald, Eileen M. Seward
  • Patent number: 9951046
    Abstract: This disclosure relates to polycyclic heteroaromatic compounds useful as TRPA1 modulators, as well as compositions and methods of treating pain that include the compounds.
    Type: Grant
    Filed: July 6, 2016
    Date of Patent: April 24, 2018
    Assignee: Algomedix, Inc.
    Inventors: Jeffrey M. Herz, Edward A Kesicki
  • Patent number: 9951052
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: October 27, 2014
    Date of Patent: April 24, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Haifeng Tang, Jessica Frie, Ronald Dale Ferguson, Zhiqiang Guo, Zhi-Cai Shi, Brian Cato, Qinghong Fu
  • Patent number: 9925188
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: February 29, 2016
    Date of Patent: March 27, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • Patent number: 9926299
    Abstract: The invention provides novel poly-substituted 5-membered heterocyclic compounds represented by Formula (IV), or a pharmaceutically acceptable salt, solvate, metabolite, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as selective irreversible bruton's tyrosine kinase (Btk) inhibitors and are further useful to treat inflammatory, auto immune diseases associated with aberrant B-cell proliferation such as RA (rheumatoid arthritis) and cancers. This invention also provides the preparation of a medicament using of Formula (IV), and methods of preventing or treating diseases associated with excessive Btk activity in mammals, especially humans.
    Type: Grant
    Filed: November 29, 2013
    Date of Patent: March 27, 2018
    Assignee: Centaurus BioPharma Co., Ltd.
    Inventors: Yongxin Han, Rong Yu, Zanping Wang, Zhi Liang, Quan Hu, Li Zhu, Yuandong Hu, Yinghui Sun, Na Zhao, Yong Peng, Xiaofeng Zhai, Hong Luo, Dengming Xiao
  • Patent number: 9920031
    Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR4 or N; R1, R2, R3, R4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Grant
    Filed: May 30, 2017
    Date of Patent: March 20, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Qingjie Liu, Scott Hunter Watterson, Saleem Ahmad
  • Patent number: 9920054
    Abstract: The present invention provides methyl- and trifluoromethyl-substituted pyrrolopyridines, pharmaceutical compositions thereof, methods of modulating ROR? activity and/or reducing the amount of IL-17 in a subject, and methods of treating various medical disorders using such pyrrolopyridines and pharmaceutical compositions thereof.
    Type: Grant
    Filed: April 28, 2017
    Date of Patent: March 20, 2018
    Assignee: Pfizer Inc.
    Inventor: Mark Edward Schnute
  • Patent number: 9908887
    Abstract: Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: March 6, 2018
    Assignee: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
  • Patent number: 9908886
    Abstract: The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, Alzheimer's disease), as well as methods of treating these diseases.
    Type: Grant
    Filed: April 1, 2013
    Date of Patent: March 6, 2018
    Assignee: Agency for Science, Technology and Research
    Inventors: Kassoum Nacro, Athisayamani Jeyaraj Duraiswamy, Lohitha Rao Chennamaneni
  • Patent number: 9880180
    Abstract: Provided are methods of detecting the presence or amount of a vitamin D metabolite in a sample using mass spectrometry. The methods generally are directed to ionizing a vitamin D metabolite in a sample and detecting the amount of the ion to determine the presence or amount of the vitamin D metabolite in the sample. Also provided are methods to detect the presence or amount of two or more vitamin D metabolites in a single assay.
    Type: Grant
    Filed: December 22, 2016
    Date of Patent: January 30, 2018
    Assignee: Quest Diagnostics Investments Incorporated
    Inventors: Nigel J. Clarke, Brett Holmquist, Gloria Kwang-Ja Lee, Richard E. Reitz
  • Patent number: 9828364
    Abstract: The present invention encompasses compounds of the formula (I) wherein the groups R1, Cy, and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
    Type: Grant
    Filed: January 23, 2015
    Date of Patent: November 28, 2017
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Joerg Bentzien, Angela Kay Berry, Todd Bosanac, Michael Jason Burke, Darren Todd Disalvo, Can Mao, Wang Mao, Yue Shen
  • Patent number: 9815819
    Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: November 14, 2017
    Assignee: NOVARTIS AG
    Inventors: Eva Altmann, Ulrich Hommel, Edwige Liliane Jeanne Lorthiois, Jeurgen Klaus Maibaum, Nils Ostermann, Jean Quancard, Stefan Andreas Randl, Olivier Rogel, Anna Vulpetti
  • Patent number: 9815834
    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: February 4, 2015
    Date of Patent: November 14, 2017
    Assignee: PRINCIPIA BIOPHARMA, INC.
    Inventors: Erik Verner, Kenneth Albert Brameld
  • Patent number: 9790178
    Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Ring B, and Ring C are as defined herein, and wherein Ring B moiety and the NH—C(?X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.
    Type: Grant
    Filed: November 13, 2013
    Date of Patent: October 17, 2017
    Assignee: Array BioPharma Inc.
    Inventors: Shelley Allen, Steven Wade Andrews, James F. Blake, Barbara J. Brandhuber, Yutong Jiang, Timothy Kercher, Shannon L. Winski
  • Patent number: 9782412
    Abstract: Provided is a preventive and/or therapeutic agent for immune diseases containing a compound having a BTK inhibitory activity or a salt thereof, as an active ingredient. A preventive and/or therapeutic agent of immune diseases, comprising a compound represented by Formula (I), where R1 to R3, W, X, Y, Z, and n represent those as defined in the specification, or a salt thereof, as an active ingredient.
    Type: Grant
    Filed: October 19, 2016
    Date of Patent: October 10, 2017
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Fumihito Hosoi, Yoshinori Nakachi, Daisuke Kajiwara
  • Patent number: 9771370
    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: September 4, 2015
    Date of Patent: September 26, 2017
    Assignee: Merck Patent GmbH
    Inventor: Brian A. Sherer
  • Patent number: 9745288
    Abstract: Compounds and methods for treating or preventing cancer associated with binding to the urokinase receptor are provided. Biological processes affected by the compounds include cell migration, cell growth, cell adhesion, angiogenesis, cancer cell invasion, apoptosis, tumor formation, tumor progression, metastasis, degradation of the extracellular matrix, pericellular proteolysis, activation of plasminogen, changes in the levels of an extracellular protease, and changes in the levels of a VEGF receptor.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: August 29, 2017
    Assignee: Indiana University Research and Technology Corporation
    Inventor: Samy O. Meroueh