The Additional Hetero Ring Contains Ring Nitrogen Patents (Class 514/210.2)
  • Patent number: 10889578
    Abstract: The present invention provides an improved process for preparing an aminopyrimidine derivative or pharmaceutically acceptable salt thereof having a selective inhibitory activity against protein kinases, especially against the protein kinases for mutant epidermal growth factor receptors. And also, the present invention provides novel intermediates useful for said process and processes for preparing the same.
    Type: Grant
    Filed: July 25, 2018
    Date of Patent: January 12, 2021
    Assignee: Yuhan Corporation
    Inventors: Sang-Ho Oh, Ja-Heouk Khoo, Jong-Chul Lim, Seong-Ran Lee, Hyun Ju, Woo-Seob Shin, Dae-Gyu Park, Su-Min Park, Yoon-Ah Hwang
  • Patent number: 10844013
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: August 7, 2019
    Date of Patent: November 24, 2020
    Assignee: NAVITOR PHARMACEUTICALS, INC.
    Inventors: David John O'Neill, Eddine Saiah, Seong Woo Anthony Kang, Andrew Brearley, Jonathan Bentley
  • Patent number: 10836743
    Abstract: Provided is a fluorinated cyclopropylamine compound represented by formula I, a racemate thereof, an R-isomer thereof, an S-isomer thereof, a pharmaceutical salt thereof, and a mixture thereof. Also provided are pharmaceutical compositions containing the compound, a preparation method for the compound, and uses thereof as a lysine specific demethylase 1 (LSD1) inhibitor, and in the treatment of cancers.
    Type: Grant
    Filed: March 16, 2017
    Date of Patent: November 17, 2020
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Hong Liu, Jia Li, Jiang Wang, Mingbo Su, Shuni Wang, Yubo Zhou, Wei Zhu, Wei Xu, Chunpu Li, Hualiang Jiang, Kaixian Chen
  • Patent number: 10813929
    Abstract: This invention relates to methods and compositions for treating pancreatic cancer. More specifically, this invention relates to treating pancreatic cancer with certain ATR inhibitors in combination with gemcitabine and/or radiation therapy. This invention also relates to methods and compositions for treating non-small cell lung cancer. More specifically, this invention relates to treating non-small cell lung cancer with an ATR inhibitor in combination with cisplatin or carboplatin, etoposide, and ionizing radiation.
    Type: Grant
    Filed: February 28, 2014
    Date of Patent: October 27, 2020
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: John Robert Pollard, Philip Michael Reaper
  • Patent number: 10792360
    Abstract: Provided herein are compositions, methods and kits for treating inflammatory bowel disease (IBD) such as Crohn's disease and ulcerative colitis in a mammal in need thereof. The method include administering to a subject with IBD a combination therapy containing a therapeutically effective amount of a chemokine receptor 9 (CCR9) inhibitor compound and a therapeutically effective amount of an anti-TNF? antibody. Also provided herein is a kit containing the CCR9 inhibitor compound and anti-TNF? antibody.
    Type: Grant
    Filed: January 13, 2020
    Date of Patent: October 6, 2020
    Assignee: ChemoCentryx, Inc.
    Inventors: Thomas Schall, James J. Campbell
  • Patent number: 10786500
    Abstract: Provided is a stable pharmaceutical composition for oral administration comprising 6-ethyl-3-({3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)-5-(tetrahydro-2H-pyran-4-ylamino)pyrazine-2-carboxamide (hereinafter referred to as compound A) or a pharmaceutically acceptable salt thereof, wherein the generation of related substances during storage is inhibited. In the stable pharmaceutical composition for oral administration, the proportion of crystals of compound A or a pharmaceutically acceptable salt thereof is 60% or more with respect to the total amount of compound A or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 1, 2016
    Date of Patent: September 29, 2020
    Assignee: ASTELLAS PHARMA INC.
    Inventors: Masakazu Miyazaki, Ryohei Ishiba, Yuki Takaishi, Fumiaki Uejo
  • Patent number: 10781202
    Abstract: The invention provides certain azetidinyloxyphenylpyrrolidine compounds, particularly compounds of formula I, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder.
    Type: Grant
    Filed: September 3, 2015
    Date of Patent: September 22, 2020
    Assignee: Eli Lilly and Company
    Inventors: Gary G. Deng, Danwen Huang, Cynthia Darshini Jesudason, Joshua O. Odingo
  • Patent number: 10774050
    Abstract: The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A1, X, A2, W1, W2, W3, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
    Type: Grant
    Filed: June 1, 2018
    Date of Patent: September 15, 2020
    Assignee: Purdue Pharma, L.P.
    Inventors: Chiyou Ni, Laykea Tafesse, Jiangchao Yao, Mark A. Youngman, Minnie Park, Bin Shao
  • Patent number: 10766877
    Abstract: Described herein are compounds that are melanocortin subtype-2 receptor (MC2R) modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of MC2R activity.
    Type: Grant
    Filed: December 13, 2019
    Date of Patent: September 8, 2020
    Assignee: CRINETICS PHARMACEUTICALS, INC.
    Inventors: Sangdon Han, Yunfei Zhu, Sun Hee Kim, Jian Zhao
  • Patent number: 10709706
    Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula (I) or their pharmaceutically acceptable salts, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.
    Type: Grant
    Filed: December 30, 2016
    Date of Patent: July 14, 2020
    Assignee: Karopharm Therapeutics Inc.
    Inventor: Erkan Baloglu
  • Patent number: 10676469
    Abstract: Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: wherein X, Y, R1, R2, R4, R5 R6, R7, R8 and R11 are as defined herein.
    Type: Grant
    Filed: March 16, 2018
    Date of Patent: June 9, 2020
    Assignees: BLACKTHORN THERAPEUTICS, INC., THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Edward Roberts, Miguel A. Guerrero, Mariangela Urbano, Hugh Rosen, Robert M. Jones, Candace Mae Laxamana, Xianrui Zhao, Eric Douglas Turtle
  • Patent number: 10604507
    Abstract: Described herein are compounds that are melanocortin subtype-2 receptor (MC2R) modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of MC2R activity.
    Type: Grant
    Filed: August 27, 2019
    Date of Patent: March 31, 2020
    Assignee: CRINETICS PHARMACEUTICALS, INC.
    Inventors: Sangdon Han, Yunfei Zhu, Sun Hee Kim, Jian Zhao, Shimiao Wang
  • Patent number: 10588891
    Abstract: The present invention relates to pyrrolidine sulfonamide analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
    Type: Grant
    Filed: September 20, 2017
    Date of Patent: March 17, 2020
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Edward J. Brnardic, Carl A. Brooks, Brian Griffin Lawhorn, Guosen Ye, Linda S. Barton, Brian W. Budzik, Jay M. Matthews, John Jeffrey McAtee, Jaclyn R. Patterson, Joseph E. Pero, Robert Sanchez, Matthew Robert Sender, Lamont Roscoe Terrell, David J. Behm, James V. Thomas
  • Patent number: 10570124
    Abstract: There are provided, inter alia, compounds useful for binding to deoxycytidine kinase, and compounds and methods useful to modulate deoxycytidine kinase.
    Type: Grant
    Filed: January 9, 2017
    Date of Patent: February 25, 2020
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Caius G. Radu, Raymond M. Gipson
  • Patent number: 10562884
    Abstract: Described herein are compounds that are melanocortin subtype-2 receptor (MC2R) modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of MC2R activity.
    Type: Grant
    Filed: June 5, 2019
    Date of Patent: February 18, 2020
    Assignee: CRINETICS PHARMACEUTICALS, INC.
    Inventors: Sangdon Han, Yunfei Zhu, Sun Hee Kim, Jian Zhao, Shimiao Wang
  • Patent number: 10548878
    Abstract: The present disclosure features compounds such as those having the Formulae (I) and (II), which can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells. The present disclosure also features methods of treating a condition associated with decreased CFTR activity or a condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a disclosed compound, such as a compound of Formula (I) or (II).
    Type: Grant
    Filed: July 25, 2016
    Date of Patent: February 4, 2020
    Assignee: Proteostasis Therapeutics, Inc.
    Inventors: Benito Munoz, Cecilia M. Bastos, John Miller
  • Patent number: 10544108
    Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Grant
    Filed: November 28, 2018
    Date of Patent: January 28, 2020
    Assignee: Karyopharm Therapeutics Inc.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
  • Patent number: 10500195
    Abstract: Compounds of Formula (I), or a stereoisomer or a pharmaceutically acceptable salt thereof, their preparation, pharmaceutical compositions comprising such compounds and their use in treating and/or preventing bacterial infections are disclosed.
    Type: Grant
    Filed: April 24, 2017
    Date of Patent: December 10, 2019
    Assignee: WOCKHARDT LIMITED
    Inventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Piyush Ambalal Patel, Rajib Bhuniya, Sachin Bhagwat, Swapna Shripad Takalkar, Rajesh Chavan, Anusuya Patel, Vipul Rane, Mahesh Vithalbhai Patel
  • Patent number: 10471051
    Abstract: The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.
    Type: Grant
    Filed: September 1, 2017
    Date of Patent: November 12, 2019
    Assignee: Asana BioSciences, LLC
    Inventors: Aranapakam M. Venkatesan, Scott K. Thompson, Roger A. Smith, Sanjeeva P. Reddy, Raghava Reddy Kethiri, Purushottam M. Dewang, Gurulingappa Hallur, Chandrika Mulakala, Ramesh Mullangi, Mohd Zainuddin
  • Patent number: 10457826
    Abstract: A polymer-bound lead refill for writing, drawing and/or painting devices, in particular for pencils or colored pencils, including at least one binding agent, at least one wax, at least one coloring agent and at least one filling agent. The lead refill including at least one surfactant.
    Type: Grant
    Filed: November 7, 2014
    Date of Patent: October 29, 2019
    Assignee: STAEDTLER MARS GMBH & CO. KG
    Inventor: Johannes Herbolsheimer
  • Patent number: 10441572
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: May 2, 2018
    Date of Patent: October 15, 2019
    Assignee: Aptinyx Inc.
    Inventors: John A. Lowe, III, M. Amin Khan
  • Patent number: 10441571
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: May 2, 2018
    Date of Patent: October 15, 2019
    Assignee: Aptinyx Inc.
    Inventors: John A. Lowe, III, M. Amin Khan
  • Patent number: 10421761
    Abstract: Compounds active on protein kinases and methods for regulating protein kinase pathways are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Grant
    Filed: December 11, 2017
    Date of Patent: September 24, 2019
    Assignee: Plexxikon Inc.
    Inventors: Chao Zhang, Klaus-Peter Hirth, Prabha N. Ibrahim, Marika Nespi, Songyuan Shi, Wayne Spevak, Gaston G. Habets, Elizabeth A. Burton
  • Patent number: 10385070
    Abstract: The invention relates to chroman spirocyclic piperidine amide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: August 20, 2019
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Mark Thomas Miller, Edward Adam Kallel, Brian Richard Bear, Vijayalaksmi Arumugam, Michael Paul Deninno, Jinglan Zhou, Johnny Uy, Bryan A. Frieman
  • Patent number: 10369130
    Abstract: The present invention relates to novel antibacterial compounds, pharmaceutical compositions containing them and their use as antimicrobials.
    Type: Grant
    Filed: December 11, 2015
    Date of Patent: August 6, 2019
    Assignee: AZIEN DE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.
    Inventors: Rosella Ombrato, Barbara Garofalo, Giorgina Mangano, Alessandra Capezzone De Joannon, Gaia Corso, Gabriele Magaro′, Guido Furlotti, Tommaso Iacoangeli
  • Patent number: 10343992
    Abstract: The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (II) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R8, R9, R10, R12, Z, Y and m are as defined herein.
    Type: Grant
    Filed: March 24, 2016
    Date of Patent: July 9, 2019
    Assignee: Missions Therapeutics Limited
    Inventors: Alison Jones, Mark Kemp, Martin Stockley, Karl Gibson, Gavin Whitlock
  • Patent number: 10344020
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Grant
    Filed: October 13, 2016
    Date of Patent: July 9, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Imadul Islam, Srinivasan Thangathirupathy, Jayakumar Sankara Warrier, Srinivas Cheruku, Poornima Shetty, Grandhi Venkat Ram Krishna Mohan Gupta, John E. Macor
  • Patent number: 10301289
    Abstract: The present invention relates to a process for preparing 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-ol (I—enol form) or 2-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1,2-dihydro-3H-pyrazol-3-one (I—keto form) and sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-olate (II) from 1,2,3-triazole (III), methyl bromoacetate (IV-Me-Br) or ethyl bromoacetate (IV-Et-Br), 4,6-dichloropyrimidine (VIII), morpholine (IX) and hydrazine (XII).
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: May 28, 2019
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Hans-Christian Militzer, Johannes Eggert
  • Patent number: 10280160
    Abstract: The invention relates to a compound of Formula I and methods of treating CFTR (cystic fibrosis transmembrane conductance regulator) mediated diseases, in particular cystic fibrosis, comprising the step of administering a therapeutically effective amount of a compound of Formula I to a patient in need thereof:
    Type: Grant
    Filed: June 6, 2017
    Date of Patent: May 7, 2019
    Assignee: FLATLEY DISCOVERY LAB, LLC
    Inventor: Bridget M. Cole
  • Patent number: 10258621
    Abstract: Certain adjunctive therapies comprising a kynurenine-3-monooxygenase inhibitor and an antiviral agent for treating HIV-related disorders are provided herein. These disorders include AIDS dementia complex, AIDS-induced encephalopathy, HIV-associated neurocognitive disorder, asymptomatic neurocognitive impairment, minor neurocognitive disorder, minor cognitive motor disorder, vacuolar myelopathy, peripheral neuropathies, and polymyositis. Also provided are pharmaceutical compositions comprising a kynurenine-3-monooxygenase inhibitor and an antiviral agent.
    Type: Grant
    Filed: July 17, 2015
    Date of Patent: April 16, 2019
    Assignee: CHDI Foundation, Inc.
    Inventors: Celia Dominguez, Ignacio Muñoz-Sanjuán, Leticia Toledo-Sherman
  • Patent number: 10174038
    Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
    Type: Grant
    Filed: June 9, 2017
    Date of Patent: January 8, 2019
    Assignee: Gilead Sciences, Inc.
    Inventors: Hon Chung Hui, Jay P. Parrish, Michael Sangi, Dustin Siegel, David Sperandio, Hai Yang
  • Patent number: 10172952
    Abstract: The invention relates to inhibitory compounds of a p38 MAP kinase having a structure of type (I)-(VII) which can be used for the treatment or prophylaxis of adhesion. Pharmaceutical compositions are disclosed containing an effective amount of the substance SB203580 or one or more of the conjugated compounds of type (I)-(VII) or a combination thereof, and a pharmaceutically acceptable carrier, a diluent or an excipient. Also disclosed is the use of the substance SB203580 as an agent having anti-adhesion activity. Also disclosed is a method for the prophylaxis and/or treatment of a disease or a condition in which there is a possibility of the formation and/or growth of adhesions, which makes it possible to dispense with the additional administration of a preparation in the post-operative period.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: January 8, 2019
    Assignee: Joint Stock Company “Pharmasyntez”
    Inventors: Mikhail Gennadievich Shurygin, Irina Aleksandrovna Shurygina
  • Patent number: 10173995
    Abstract: The present invention is directed to novel pyridines, their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The present invention discloses compounds of Formulas I and II. The compounds and compositions of the present invention have protein kinases inhibitory activities and are expected to be useful for the treatment of protein kinases mediated diseases and conditions.
    Type: Grant
    Filed: January 11, 2014
    Date of Patent: January 8, 2019
    Assignee: Teligene Ltd.
    Inventor: Dawei Zhang
  • Patent number: 10174002
    Abstract: A compound having the structure of Formula II, or a stereoisomer, tautomer, or a pharmaceutically acceptable salt thereof that is useful as CFTR modulator. Further, a method of using the compound and pharmaceutical composition comprising the compound are provided for treating diseases in lungs, pancreas, gastrointestinal system, sinuses, reproductive system, and the sweat glands.
    Type: Grant
    Filed: October 6, 2016
    Date of Patent: January 8, 2019
    Assignee: NuBridge BioSciences
    Inventors: Lin Zhang, Yu Ge
  • Patent number: 10160744
    Abstract: The present invention relates to quinoline compounds of formula I wherein the variables are defined as in the claims and the description. The invention further relates to a pharmaceutical composition containing such compounds, to their use as modulators of the 5-HT6 receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of the 5-HT6 receptor, and to methods for preventing or treating conditions and disorders which respond to the modulation of the 5-HT6 receptor.
    Type: Grant
    Filed: March 14, 2017
    Date of Patent: December 25, 2018
    Assignee: ABBVIE DEUTSCHLAND GMBH & CO. KG
    Inventors: Hervé Geneste, Andreas Haupt, Frauke Pohlki, Ana Lucia Relo, Liliane Unger, Karsten Wicke
  • Patent number: 10155777
    Abstract: A substituted trans-cycloheptene according to formula (I); wherein: a) Z and L are each selected from the group consisting of SiR1R2, CH2, CHOH, and CHR2; R1 is phenyl or CH3; R2 is phenyl, CH3, (CH2)nCN, or (CH2)nOH, wherein n is an integer from 1 to 5; Ra and Rb are each individually selected from the group consisting of H, OH, and CH3; and Z and L are not both SiR1R2; or b) Z is BocN, L is CH2, Ra is H, and Rb is H; or c) Z is C=0, L is CH2, Ra is H, and Rb is H.
    Type: Grant
    Filed: April 7, 2016
    Date of Patent: December 18, 2018
    Assignee: UNIVERSITY OF DELAWARE
    Inventors: Joseph Fox, Han Zhang, Yinzhi Fang
  • Patent number: 10125130
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein A, L, D, R1-R15, w, x, y, and z are defined herein. The novel cycloalkyl-linked diheterocycle derivatives that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. The present invention also relates to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.
    Type: Grant
    Filed: November 29, 2017
    Date of Patent: November 13, 2018
    Assignee: Pfizer Inc.
    Inventors: Aaron Craig Burns, Michael Raymond Collins, Samantha Elizabeth Greasley, Robert Louis Hoffman, Peter Qinhua Huang, Robert Steven Kania, Pei-Pei Kung, Maria Angelica Linton, Lakshmi Sourirajan Narasimhan, Paul Francis Richardson, Daniel Tyler Richter, Graham Smith
  • Patent number: 10071957
    Abstract: The invention provides novel compounds having the general formula (I) and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, ring D, R1, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: July 5, 2013
    Date of Patent: September 11, 2018
    Assignees: GENENTECH, INC., XENON PHARMACEUTICALS INC.
    Inventors: Christoph Martin Dehnhardt, Sultan Chowdhury, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Brian Safina, Daniel P. Sutherlin
  • Patent number: 10059667
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Grant
    Filed: February 3, 2015
    Date of Patent: August 28, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harry Chobanian, Duane DeMong, Yan Guo, Zhiyong Hu, Michael Miller, Barbara Pio, Christopher W. Plummer, Dong Xiao, Cangming Yang
  • Patent number: 10059687
    Abstract: The present disclosure relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyridine derivative compounds, and compositions (including pharmaceutical compositions) that include these compounds. The subject compounds and compositions are useful for inhibition of at least one histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer or neoplastic disease, such as prostate cancer, breast cancer, bladder cancer, lung cancer, melanoma, retinoblastoma, or multiple endocrine neoplasia type 1.
    Type: Grant
    Filed: December 27, 2016
    Date of Patent: August 28, 2018
    Assignee: Celgene Quanticel Research, Inc.
    Inventors: Young K. Chen, Michael Brennan Wallace
  • Patent number: 10052308
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: October 28, 2016
    Date of Patent: August 21, 2018
    Assignee: Aptinyx Inc.
    Inventors: John A. Lowe, III, M. Amin Khan
  • Patent number: 10017477
    Abstract: The present invention provides kinase inhibitors, such as compounds of Formula (I) and Formula (II). The compounds may covalently or non-covalently bind a kinase (e.g., Janus kinase 3 (JAK3)). Also provided are pharmaceutical compositions, kits, methods, and uses that involve the compounds for reducing the activity of a kinase and/or treating and/or preventing a condition associated with aberrant activity of a kinase (e.g., a proliferative disease, inflammatory disorder, autoimmune disorder, painful condition, and/or viral infection).
    Type: Grant
    Filed: April 23, 2015
    Date of Patent: July 10, 2018
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Li Tan
  • Patent number: 9981945
    Abstract: A compound having the structure of Formula II, or a stereoisomer, tautomer, or a pharmaceutically acceptable salt thereof: The compound is useful as CFTR modulator. Further, a method of using the compound and pharmaceutical composition comprising the compound are provided for treating diseases in lungs, pancreas, gastrointestinal system, sinuses, reproductive system, and the sweat glands.
    Type: Grant
    Filed: October 6, 2016
    Date of Patent: May 29, 2018
    Assignee: NuBridge BioSciences
    Inventors: Lin Zhang, Yu Ge
  • Patent number: 9938257
    Abstract: The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
    Type: Grant
    Filed: September 7, 2016
    Date of Patent: April 10, 2018
    Assignees: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Ning Xi, Minxiong Li, Xiaobo Li, Wuhong Chen, Tao Zhang, Haiyang Hu, Weilong Dai, Yanjun Wu
  • Patent number: 9908875
    Abstract: The present application relates to compounds having the inhibitory activity to apoptosis signal-regulating kinase (ASK1), thus are thus useful in treating ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.
    Type: Grant
    Filed: December 15, 2014
    Date of Patent: March 6, 2018
    Assignee: GILEAD SCIENCES, INC.
    Inventor: Gregory Notte
  • Patent number: 9895308
    Abstract: Provided are certain pharmaceutical formulations of omecamtiv mecarbil and methods for their preparation and use.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: February 20, 2018
    Assignee: AMGEN INC.
    Inventor: William Brett Caldwell
  • Patent number: 9896445
    Abstract: The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.
    Type: Grant
    Filed: June 15, 2016
    Date of Patent: February 20, 2018
    Assignee: Ansana BioSciences, LLC
    Inventors: Aranapakam M. Venkatesan, Scott K. Thompson, Roger A. Smith, Sanjeeva P. Reddy, Raghava Reddy Kethiri, Purushottam M. Dewang, Gurulingappa Hallur, Chandrika Mulakala, Ramesh Mullangi, Mohd Zainuddin
  • Patent number: 9879001
    Abstract: Compounds of formula (I) wherein X1, X2, W, R1 to R5, L and m have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: January 30, 2018
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Lesley Liu-Bujalski, Theresa L. Johnson
  • Patent number: 9868700
    Abstract: The present invention relates to carbamoyl hydrazine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the FPR receptor.
    Type: Grant
    Filed: March 13, 2017
    Date of Patent: January 16, 2018
    Assignee: Allergan, Inc.
    Inventors: Vidyasagar Vuligonda, Thong Vu, Veena Viswanath, John E. Donello, Richard L. Beard
  • Patent number: 9868723
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: July 29, 2016
    Date of Patent: January 16, 2018
    Assignee: Celgene CAR LLC
    Inventors: Kwangho Lee, Deqiang Niu, Matthew Frank Baevsky