Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/350)
  • Patent number: 11999741
    Abstract: The present disclosure relates to processes for preparing 64(3s,4s)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-3-(tetrahydropyran-4-yl-7h-imidazo[1,5-a]pyrazin-8-one.
    Type: Grant
    Filed: April 19, 2022
    Date of Patent: June 4, 2024
    Assignee: Cardurion Pharmaceuticals, Inc.
    Inventors: Niels Svenstrup, Jun Zhang, Jikui Sun, Yuyin Chen, Jianshe Kong, Rujian Ma, Junhua Zhang, Liang Qin, Huanming Xiao, Jinxu Sun, Xiao Meng, Fenglai Sun, Jingyang Zhu
  • Patent number: 11976074
    Abstract: The present invention provides salts and crystalline forms of Linsitinib (OSI-906; cis-3-[8-amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methyl-cyclobutanol). These forms of Linsitinib provide increased solubility and improved pharmacokinetic profiles for orally administered pharmaceutical formulations. Accordingly, the invention enables improved methods for treating human insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR) mediated conditions.
    Type: Grant
    Filed: June 26, 2023
    Date of Patent: May 7, 2024
    Assignee: SLING THERAPEUTICS, INC.
    Inventors: Ronald Dadino, Ryan Zeidan
  • Patent number: 11896592
    Abstract: Provided are certain triazolopyridines and triazolopyrazines of Formula 1, wherein X, Y, R1, R2, R3, R4 and R5 have any of the meanings described herein; processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of cell proliferative disorders.
    Type: Grant
    Filed: February 3, 2021
    Date of Patent: February 13, 2024
    Assignee: Hutchison Medipharma Limited
    Inventors: Wei-Guo Su, Hong Jia, Guangxiu Dai
  • Patent number: 11781168
    Abstract: Described are processes for preparing substituted imidazo[1,2-a]pyrazine compounds of formula (I): by reacting a compound of formula (xi): with carbonyldiimidazole to form the compound of formula (I).
    Type: Grant
    Filed: April 26, 2021
    Date of Patent: October 10, 2023
    Assignee: PROMEGA CORPORATION
    Inventors: Anton Shakhmin, Thomas Kirkland, Joel Walker, Thomas Machleidt, Mary Hall, Keith V. Wood
  • Patent number: 11739094
    Abstract: Compounds of general formula (I) wherein R1, R2, R3, R4, R5 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions, skin conditions and ocular conditions.
    Type: Grant
    Filed: November 24, 2020
    Date of Patent: August 29, 2023
    Assignee: ENTERPRISE THERAPEUTICS LIMITED
    Inventors: Clive McCarthy, Jonathan David Hargrave, Duncan Alexander Hay, Thomas Beauregard Schofield, Naomi Went
  • Patent number: 11731974
    Abstract: A method for treating and/or preventing polycystic ovary syndrome (PCOS) including the administration, to a patient in need thereof, of a pharmaceutically effective amount of a compound of Formula I or a pharmaceutically acceptable solvate thereof.
    Type: Grant
    Filed: October 8, 2020
    Date of Patent: August 22, 2023
    Assignee: Ogeda SA
    Inventors: Hamid R. Hoveyda, Guillaume Dutheuil, Graeme Fraser
  • Patent number: 11384082
    Abstract: Polymorphs of a bis-mesylate salt of a compound of Formula IA: are provided. Also provided are process for making the polymorphs and methods of use thereof.
    Type: Grant
    Filed: August 10, 2018
    Date of Patent: July 12, 2022
    Assignee: Kronos Bio, Inc.
    Inventors: Tim G. Elford, Peter Chee-Chu Fung, Paul Robert Hartmeier, Jesper Alexis Jernelius, Henry Morrison
  • Patent number: 11370795
    Abstract: The present invention relates a process for the synthesis of 6-((3S,4S)-4-methyl-1-(pyrimidin-2 ylmethyl)pyrrolidin-3-yl)-3-tetrahydropyran-4-yl-7H-imidazo[1,5-a]pyrazin-8-one, comprising use of the chiral acid (+)-O,O-Dibenzoyl-D-tartaic acid.
    Type: Grant
    Filed: May 25, 2018
    Date of Patent: June 28, 2022
    Assignee: Imara Inc.
    Inventors: Niels Svenstrup, Jun Zhang, Jikui Sun, Yuyin Chen, Jianshe Kong, Rujian Ma, Junhua Zhang, Liang Qin, Huanming Xiao, Jinxu Sun, Xiao Meng, Fenglai Sun, Jingyang Zhu
  • Patent number: 11358964
    Abstract: The present disclosure is directed to methods of treating or ameliorating various conditions by the administration of a BCN057, BCN512 or analogs of these compounds. The compounds can be used to reduce tumor burden in cancers, including pancreatic cancer and gastrointestinal (GI) cancer. The compounds can also be used to protect against chemotherapy induced toxicity to the GI tract. Further, they can be used to treat fibrosis and various inflammatory conditions. Analogs of BCN057 and BCN512 are also described.
    Type: Grant
    Filed: August 24, 2020
    Date of Patent: June 14, 2022
    Assignee: BCN Biosciences L.L.C.
    Inventors: Andrew J. Norris, Sudip Chakrabortty
  • Patent number: 11345709
    Abstract: A preparation method for a compound represented by formula I or a pharmaceutically acceptable salt thereof, The method includes a step of reacting a compound represented by formula II with an inorganic or organic acid selected from the group consisting of hydrochloric acid, phosphoric acid and maleic acid to provide a compound represented by formula II? In the above formulas II and II?, R1 may be trifluoromethyl; and X may be hydrochloric acid, phosphoric acid, or maleic acid. The method also includes a step of reacting the compound represented by formula II? with a compound represented by formula IV: to provide the compound represented by formula I, wherein Ra is selected from hydroxyl, halogen or alkoxy.
    Type: Grant
    Filed: January 8, 2019
    Date of Patent: May 31, 2022
    Assignee: JIANGSU HENGRUI MEDICINE CO., LTD.
    Inventors: Wenhai Li, Yingjie Zhang
  • Patent number: 11306099
    Abstract: Provided herein, inter alia, are compounds and methods for modulating Bruton's Tyrosine Kinase.
    Type: Grant
    Filed: August 27, 2020
    Date of Patent: April 19, 2022
    Assignee: Angel Pharmaceutical Co., Ltd.
    Inventors: Ryan Hudson, Anne-Marie Beausoleil, Richard A. Miller, Erik Verner
  • Patent number: 11292796
    Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof. Further provided herein are methods for preparing a compound of formula (I), the method comprising contacting a compound of formula (III) with a compound of the following formula: R1-Y, in a solvent, in the presence of a palladium catalyst, wherein said contacting occurs in the presence of a base, wherein R1-R4, Y, the palladium catalyst and the base are as defined herein.
    Type: Grant
    Filed: May 4, 2020
    Date of Patent: April 5, 2022
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Jan Elsner, Roy L. Harris, Branden Gingsee Lee, Deborah Mortensen, Garrick K. Packard, Patrick Papa, Jason Parnes, Sophie Perrin-Ninkovic, Jennifer Riggs, John Sapienza, Graziella I. Shevlin, Lida Tehrani, Jingjing Zhao
  • Patent number: 11174266
    Abstract: Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine.
    Type: Grant
    Filed: January 11, 2019
    Date of Patent: November 16, 2021
    Assignee: F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Terry Shi, Sam Lou, Ottorino De Lucchi, Pierluigi Padovan
  • Patent number: 11117894
    Abstract: Disclosed herein, inter alia, are pyridopyrazines and methods of using the same.
    Type: Grant
    Filed: June 21, 2018
    Date of Patent: September 14, 2021
    Assignees: City of Hope, National and Kapodistrian University of Athens
    Inventors: Sangkil Nam, David Horne, Ravi Salgia, Alexios-Leandros Skaltsounis, Nikolaos Lougiakis, Nicole Pouli, Panagiotis Marakos
  • Patent number: 11077107
    Abstract: Disclosed are compounds of the formula (I) wherein the groups R1 to R3 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Grant
    Filed: April 19, 2019
    Date of Patent: August 3, 2021
    Inventors: Harald Engelhardt, Davide Gianni, Christian Smethurst
  • Patent number: 11015216
    Abstract: Described are substituted imidazo[1,2-a]pyrazine compounds, which are coelenterazine analogues, kits comprising the compounds, and methods of using the compounds for the detection of luminescence in luciferase-based assays. Also described are methods of making the compounds, such as a method using aminopyrazine acetophosphonates as synthesis intermediates.
    Type: Grant
    Filed: May 4, 2020
    Date of Patent: May 25, 2021
    Assignee: PROMEGA CORPORATION
    Inventors: Anton Shakhmin, Thomas Kirkland, Joel Walker, Thomas Machleidt, Mary Hall, Keith V. Wood
  • Patent number: 10899767
    Abstract: Crystalline forms of ACP-196, preparation methods, pharmaceutical compositions and uses thereof in the preparation of drugs for treatment and/or prevention of Bruton's tyrosine kinase (BTK)-mediated disorders such as autoimmune diseases or disorders, heteroimmune diseases or disorders, cancers including lymphoma and inflammatory diseases or disorders. As compared with the known solid form of ACP-196, the crystalline forms of the present invention have advantages in crystallinity.
    Type: Grant
    Filed: October 5, 2016
    Date of Patent: January 26, 2021
    Assignee: Hangzhou SoliPharma Co., Ltd.
    Inventors: Xiaohong Sheng, Xiaoxia Sheng, Tao Zhu
  • Patent number: 10836768
    Abstract: A method for treating and/or preventing polycystic ovary syndrome (PCOS) including the administration, to a patient in need thereof, of a pharmaceutically effective amount of a compound of Formula I or a pharmaceutically acceptable solvate thereof.
    Type: Grant
    Filed: November 29, 2018
    Date of Patent: November 17, 2020
    Assignee: Ogeda SA
    Inventors: Hamid Hoveyda, Guillaume Dutheuil, Graeme Fraser
  • Patent number: 10800787
    Abstract: The present invention provides processes for the preparation of Acalabrutinib (1), as well as intermediates useful in the preparation thereof. In particular, processes are provided for coupling of a compound of Formula (5) and 2-butynoic acid in the presence of Carbodiimide (8) to afford Acalabrutinib (1).
    Type: Grant
    Filed: April 17, 2018
    Date of Patent: October 13, 2020
    Assignee: Apotex Inc.
    Inventors: Prabhudas Bodhuri, Boris Gorin, Melanie R. A. Green, Gamini Weeratunga
  • Patent number: 10766899
    Abstract: Provided are methods of preparing compounds of Formula 201:
    Type: Grant
    Filed: April 7, 2014
    Date of Patent: September 8, 2020
    Assignee: CYTOKINETICS, INCORPORATED
    Inventors: Bradley P. Morgan, David J. Morgans, Jr., Alex Muci
  • Patent number: 10738046
    Abstract: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.
    Type: Grant
    Filed: August 7, 2018
    Date of Patent: August 11, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Jason W. Brown, Stephen Hitchcock, Maria Hopkins, Shota Kikuchi, Holger Monenschein, Holly Reichard, Kristin Schleicher, Huikai Sun, Todd Macklin
  • Patent number: 10683298
    Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
    Type: Grant
    Filed: November 12, 2018
    Date of Patent: June 16, 2020
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Jan Elsner, Roy L. Harris, Branden Gingsee Lee, Deborah Mortensen, Garrick K. Packard, Patrick Papa, Jason Parnes, Sophie Perrin-Ninkovic, Jennifer Riggs, John Sapienza, Graziella I. Shevlin, Lida Tehrani, Jingjing Zhao
  • Patent number: 10669568
    Abstract: Described are substituted imidazo[1,2-a]pyrazine compounds, which are coelenterazine analogues, kits comprising the compounds, and methods of using the compounds for the detection of luminescence in luciferase-based assays. Also described are methods from making the compounds, such as a method using aminopyrazine acetophosphonates as synthesis intermediates.
    Type: Grant
    Filed: April 22, 2019
    Date of Patent: June 2, 2020
    Assignee: PROMEGA CORPORATION
    Inventors: Anton Shakhmin, Thomas Kirkland, Joel Walker, Thomas Machleidt, Mary Hall, Keith V. Wood
  • Patent number: 10584129
    Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.
    Type: Grant
    Filed: September 6, 2018
    Date of Patent: March 10, 2020
    Assignee: Janssen Pharmaceuticals NV
    Inventors: Sergio-Alvar Alonso-de Diego, José Maria Cid-Núñez, Óscar Delgado-González, Annelies Marie Antonius Decorte, Michiel Luc Maria Van Gool, Gregor James MacDonald, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez, Aránzazu García-Molina, José Ignacio Andrés-Gil
  • Patent number: 10577370
    Abstract: Described are coelenterazine analogues, methods for making the analogues, kits comprising the analogues, and methods of using the compounds for the detection of luminescence in luciferase-based assays.
    Type: Grant
    Filed: December 1, 2017
    Date of Patent: March 3, 2020
    Assignee: PROMEGA CORPORATION
    Inventors: Mary Hall, Thomas Kirkland, Poncho Meisenheimer, Rachel Friedman Ohana, Anton Shakhmin, Joel R. Walker, Wenhui Zhou
  • Patent number: 10556908
    Abstract: The present invention is directed to imidazo[1,2-a]pyrazine derivatives of Formula I, or a pharmaceutically acceptable salt thereof, which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: September 13, 2018
    Date of Patent: February 11, 2020
    Assignee: Incyte Corporation
    Inventors: Liangxing Wu, Joel R. Courter, Chunhong He, Jingwei Li, Liang Lu, Yaping Sun, Xiaozhao Wang, Wenqing Yao, Colin Zhang, Jincong Zhuo
  • Patent number: 10406157
    Abstract: Disclosed is a compound of Formula 1, and a pharmaceutically acceptable salt thereof. This disclosure also relates to materials and methods for preparing the compound of Formula 1, to pharmaceutical compositions which contain it, and to its use for treating diseases, disorders, and conditions associated with GPR6.
    Type: Grant
    Filed: June 15, 2018
    Date of Patent: September 10, 2019
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Jason W. Brown, Stephen Hitchcock, Maria Hopkins, Shota Kikuchi, Holger Monenschein, Holly Reichard, Kristin Schleicher, Huikai Sun, Todd Macklin
  • Patent number: 10328074
    Abstract: Method for treating AML and MM by administration of a compound of the formula (I) wherein the groups R1 to R3 have the meanings given in the specification.
    Type: Grant
    Filed: January 14, 2016
    Date of Patent: June 25, 2019
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Harald Engelhardt, Davide Gianni, Christian Smethurst
  • Patent number: 10280447
    Abstract: Described are substituted imidazo[1,2-a]pyrazine compounds of formula (I), which are coelenterazine analogs, methods for making the compounds, kits comprising the compounds, and methods of using the compounds for the detection of luminescence in luciferase-based assays.
    Type: Grant
    Filed: November 1, 2017
    Date of Patent: May 7, 2019
    Assignee: Promega Corporation
    Inventors: Mary Hall, Thomas Kirkland, Thomas Machleidt, Anton Shakhmin, Joel R. Walker, Keith V. Wood, Wenhui Zhou
  • Patent number: 10280170
    Abstract: The present invention relates to substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrazine derivatives and 5,6,7,8-tetrahydro-4H-pyrazolo[1,5-a][1,4]diazepine derivatives of formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as ROS1 inhibitors. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: March 26, 2015
    Date of Patent: May 7, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Laurence Anne Mevellec, Elisabeth Therese Jeanne Pasquier, Sophie Descamps, Guillaume Jean Maurice Mercey, Berthold Wroblowski, Jorge Eduardo Vialard, Lieven Meerpoel, Matthieu Ludovic Jeanty, Thierry Francois Alain Jean Jousseaume
  • Patent number: 10214533
    Abstract: Novel compounds of Formula I and their use in therapeutic treatments.
    Type: Grant
    Filed: April 18, 2018
    Date of Patent: February 26, 2019
    Assignee: OGEDA SA
    Inventors: Hamid Hoveyda, Guillaume Dutheuil, Graeme Fraser
  • Patent number: 10183948
    Abstract: A method for treating and/or preventing polycystic ovary syndrome (PCOS) including the administration, to a patient in need thereof, of a pharmaceutically effective amount of a compound of Formula I or a pharmaceutically acceptable solvate thereof.
    Type: Grant
    Filed: October 27, 2017
    Date of Patent: January 22, 2019
    Assignee: OGEDA SA
    Inventors: Hamid Hoveyda, Guillaume Dutheuil, Graeme Fraser
  • Patent number: 10167290
    Abstract: Provided herein are methods for the preparation of substituted pyrazino[2,3-b]pyrazines of the formula (II): the method comprising contacting a compound of formula (VI): with R1—Y in a solvent, in the presence of a palladium catalyst, wherein said contacting occurs in the presence of a base, wherein R1-R3, Y, the palladium catalyst and the base are as defined herein.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: January 1, 2019
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Jan Elsner, Roy L. Harris, Branden Gingsee Lee, Deborah Mortensen, Garrick K. Packard, Patrick Papa, Jason Parnes, Sophie Perrin-Ninkovic, Jennifer Riggs, John Sapienza, Graziella I. Shevlin, Lida Tehrani, Jingjing Zhao
  • Patent number: 10167282
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 1-(5-tert-butyl-2-aryl-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea compounds (referred herein as “TBAP compounds”) that, inter alia, inhibit RAF (e.g., BRAF, CRAF, etc.). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF, CRAF, etc.); and to treat disorders including: proliferative disorders; cancer (including, e.g., malignant melanoma, colorectal carcinoma, pancreatic adenocarcinoma); inflammation; immunological disorders; viral infections; fibrotic disorders; disorders associated with a mutated form of RAF (e.g., BRAF, CRAF, etc.); disorders ameliorated by the inhibition of RAF (e.g., BRAF, CRAF, etc.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: January 1, 2019
    Assignees: CANCER RESEARCH TECHNOLOGY LIMITED, INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)
    Inventors: Caroline Joy Springer, Richard Marais, Romina Girotti, Dan Niculescu-Duvaz, Ion Niculescu-Duvaz, Alfonso Zambon
  • Patent number: 10138248
    Abstract: This application relates to compounds of Formula (I): or pharmaceutically acceptable salts or stereoisomers thereof, which are inhibitors of PI3K-? which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
    Type: Grant
    Filed: June 23, 2017
    Date of Patent: November 27, 2018
    Assignee: Incyte Corporation
    Inventors: Andrew W. Buesking, Richard B. Sparks, Andrew P. Combs, Brent Douty, Nikoo Falahatpisheh, Lixin Shao, Stacey Shepard, Eddy W. Yue
  • Patent number: 10125133
    Abstract: The present invention is directed to [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-a]pyrazine derivatives of Formula I, or a pharmaceutically acceptable salt thereof, which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: June 5, 2017
    Date of Patent: November 13, 2018
    Assignee: Incyte Corporation
    Inventors: Liangxing Wu, Xiaozhao Wang, Wenqing Yao, Colin Zhang
  • Patent number: 10112950
    Abstract: The present invention is directed to imidazo[1,2-a]pyrazine derivatives of Formula I, or a pharmaceutically acceptable salt thereof, which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: June 5, 2017
    Date of Patent: October 30, 2018
    Assignee: Incyte Corporation
    Inventors: Liangxing Wu, Joel R. Courter, Chunhong He, Jingwei Li, Liang Lu, Yaping Sun, Xiaozhao Wang, Wenqing Yao, Colin Zhang, Jincong Zhuo
  • Patent number: 10100053
    Abstract: The present invention pertains generally to the field of organic chemical synthesis, and in particular to certain methods for the synthesis of 8-(4-aminophenyoxy)-4H-pyrido[2,3-b]pyrazin-3-one and related compounds (denoted herein as (3)) from 4-(4-aminophenyoxy)pyridine-2,3-diamine and related compounds (denoted herein as (1)), by reaction with glyoxylic acid (denoted herein as (2)). The compounds (3) are useful in the synthesis of known anti-cancer agents, such as 1-(5-tert-butyl-2-(4-methyl-phenyl)-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea.
    Type: Grant
    Filed: June 28, 2017
    Date of Patent: October 16, 2018
    Assignees: Cancer Research Technology Limited, Institute of Cancer Research: Royal Cancer Hosp. (The)
    Inventors: Alfonso Zambon, Dan Niculescu-Duvaz, Richard Chubb, Caroline Joy Springer
  • Patent number: 10047092
    Abstract: The present invention is directed to a compound of Formula (I) and to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Grant
    Filed: April 21, 2015
    Date of Patent: August 14, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael K. Ameriks, Jason C. Rech, Brad M. Savall
  • Patent number: 10045982
    Abstract: The invention relates to new pyridopyrazine derivative compounds of formula (I-A) or formula (I-B): to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: February 9, 2016
    Date of Patent: August 14, 2018
    Assignee: ASTEX THERAPEUTICS LTD
    Inventors: Valerio Berdini, Gordon Saxty, Patrick Rene Angibaud, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet, Bruno Roux, Lieven Meerpoel
  • Patent number: 10039766
    Abstract: The present invention discloses certain new solid state forms of (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide, processes for preparing such forms, pharmaceutical compositions comprising them, and the use of such forms in therapy.
    Type: Grant
    Filed: October 12, 2016
    Date of Patent: August 7, 2018
    Assignee: AstraZeneca AB
    Inventor: Gary Peter Tomkinson
  • Patent number: 10030025
    Abstract: Novel compounds of Formula I and their use in therapeutic treatments.
    Type: Grant
    Filed: July 8, 2016
    Date of Patent: July 24, 2018
    Assignee: OGEDA SA
    Inventors: Hamid Hoveyda, Guillaume Dutheuil, Graeme Fraser
  • Patent number: 10017514
    Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.
    Type: Grant
    Filed: July 30, 2015
    Date of Patent: July 10, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Susana Conde-Ceide, Michiel Luc Maria Van Gool, Maria Luz Martin-Martin
  • Patent number: 10004733
    Abstract: The invention relates to new pyridopyrazine derivative compounds of formula (I-A) or formula (I-B): to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: February 9, 2016
    Date of Patent: June 26, 2018
    Assignee: ASTEX THERAPEUTICS LTD
    Inventors: Valerio Berdini, Gordon Saxty, Patrick Rene Angibaud, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet, Bruno Roux, Lieven Meerpoel
  • Patent number: 10004735
    Abstract: Provided herein are methods for treating or preventing a cancer, comprising administering an effective amount of a TOR kinase inhibitor and an effective amount a second active agent to a patient having a cancer.
    Type: Grant
    Filed: July 20, 2017
    Date of Patent: June 26, 2018
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Kimberly Elizabeth Fultz, Tam Minh Tran, Shuichan Xu, Weiming Xu
  • Patent number: 9987274
    Abstract: A method for treating and/or preventing hot flashes, by administering, to a patient in need thereof, of a pharmaceutically effective amount of a compound of Formula I or a pharmaceutically acceptable solvate thereof.
    Type: Grant
    Filed: December 7, 2016
    Date of Patent: June 5, 2018
    Assignee: OGEDA SA
    Inventors: Hamid Hoveyda, Guillaume Dutheuil, Graeme Fraser
  • Patent number: 9981971
    Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to the Compound for formula 1: having the name 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and tautomers thereof.
    Type: Grant
    Filed: July 8, 2016
    Date of Patent: May 29, 2018
    Assignee: Signal Pharmaceuticals, LLC
    Inventor: Nathan Boersen
  • Patent number: 9975898
    Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to the compound of formula (I): having the name 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and tautomers thereof.
    Type: Grant
    Filed: October 26, 2016
    Date of Patent: May 22, 2018
    Assignee: Signal Pharmaceuticals, LLC
    Inventor: Jeffrey Eckert
  • Patent number: 9968601
    Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: May 15, 2018
    Assignee: Gilead Sciences, Inc.
    Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Jennifer R. Lo, Scott A. Mitchell, Aaron C. Schmitt, Sundaramoorthi Swaminathan, Jin-Ming Xiong, Jianjun Xu, Zhongdong Zhao
  • Patent number: 9956218
    Abstract: Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
    Type: Grant
    Filed: October 14, 2016
    Date of Patent: May 1, 2018
    Assignee: Hutchison Medipharma Limited
    Inventors: Wei-Guo Su, Hong Jia, Guangxiu Dai