The Additional Hetero Ring Contains Ring Nitrogen Patents (Class 514/210.2)
  • Patent number: 11304949
    Abstract: The present application provides methods of treating hidradenitis suppurativa in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a compound which inhibits JAK1 and/or JAK2, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 29, 2019
    Date of Patent: April 19, 2022
    Assignee: Incyte Corporation
    Inventors: Michael D. Howell, Paul Smith
  • Patent number: 11306079
    Abstract: This application relates to compounds of Formula (I) or pharmaceutically acceptable salts 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: December 20, 2018
    Date of Patent: April 19, 2022
    Assignee: Incyte Corporation
    Inventors: Artem Shvartsbart, Andrew P. Combs, Nikoo Falahatpisheh, Padmaja Polam, Lixin Shao, Stacey Shepard
  • Patent number: 11267810
    Abstract: Provided are an aminopyrimidine compound as shown in formula (I), a polymorph, a pharmaceutically acceptable salt, a prodrug, a stereoisomer, an isotopic variant, a hydrate or a solvate thereof, and a pharmaceutical composition containing the same and the use thereof. The aminopyrimidine compound and the composition containing the same have excellent inhibition to protein kinases, and at the same time have better pharmacokinetic parameter characteristics, and can improve the drug concentration of the compound in animals, and thereby improve the efficacy and safety of the drug.
    Type: Grant
    Filed: August 21, 2018
    Date of Patent: March 8, 2022
    Assignee: Shenzhen TargetRx, Inc.
    Inventors: Yihan Wang, Huanyin Li
  • Patent number: 11254676
    Abstract: Provided is a compound represented by Formula 1 having an inhibitory activity on lysine-specific demethylase-1 (LSD1), an optical isomer, a solvate, a tautomer, or a pharmaceutically acceptable salt thereof, which is effective in preventing or treating a disease caused by abnormal activation of LSD1.
    Type: Grant
    Filed: September 13, 2018
    Date of Patent: February 22, 2022
    Assignee: HANMI PHARM. CO., LTD.
    Inventors: In Hwan Bae, Ji Sook Kim, Won Jeoung Kim, Chang Hee Park, Ji Young Song, Young Gil Ahn
  • Patent number: 11225471
    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 Formula (I).
    Type: Grant
    Filed: November 12, 2018
    Date of Patent: January 18, 2022
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Steven L. Colletti, Duane DeMong, Kevin D. Dykstra, Zhiyong Hu, Michael Miller
  • Patent number: 11179371
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, R4, n and m are as defined herein, which have valuable pharmacological properties, in particular bind to the GPR142 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as type 2 diabetes.
    Type: Grant
    Filed: June 28, 2019
    Date of Patent: November 23, 2021
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Armin Heckel, Robert Augustin, Sebastian Bandholtz, Sara Frattini, Bernd Wellenzohn
  • Patent number: 11166940
    Abstract: Methods of inducing bradycardia (slowing a heart rate) in a subject in need thereof, treating a medical condition in which inducing bradycardia (slowing a heart rate) is desirable or beneficial in a subject in need thereof and/or treating a medical condition associated with cardiac arrhythmia, are provided. The methods are effected by blocking SK4 channel in SAN cell of the subject and/or by administering to the subject a therapeutically effective amount of a blocker of an SK4 channel. A method of identifying candidate compounds for treating an arrhythmic cardiac disorder, by identifying compounds that reduce a pacing rate of the SAN cells is also provided.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: November 9, 2021
    Assignee: Ramot at Tel-Aviv University Ltd.
    Inventors: David Weisbrod, Bernard Attali, Asher Peretz
  • Patent number: 11155521
    Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CB1 receptor mediating scaffold and (ii) a second therapeutic scaffold.
    Type: Grant
    Filed: March 4, 2016
    Date of Patent: October 26, 2021
    Assignee: The United States of America as represented by the Secretary, Department of Health and Human Services
    Inventors: Resat Cinar, George Kunos, Malliga R. Iyer, William A. Gahl, Bernadette R. Gochuico, May Christine Vergara Malicdan
  • Patent number: 11091488
    Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylatin-enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 or Ubiquitin Specific Peptidase 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 (I) (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, m, L and X are as defined herein.
    Type: Grant
    Filed: November 29, 2016
    Date of Patent: August 17, 2021
    Assignee: MISSION THERAPEUTICS LIMITED
    Inventors: Mark Ian Kemp, Martin Lee Stockley, Andrew Madin
  • Patent number: 11090289
    Abstract: The disclosure provides methods for treating a subject suffering from a disease associated with sodium channel activity. The method comprises administering to the subject a therapeutically effective amount of a compound according to Formula II or Formula III described in the specification, or a pharmaceutically acceptable salt, prodrug, tautomer, stereoisomer, hydrate, or solvate thereof.
    Type: Grant
    Filed: January 24, 2018
    Date of Patent: August 17, 2021
    Assignee: University of Virginia Patent Foundation
    Inventors: Manoj K. Patel, Mirko Rivara
  • Patent number: 11083709
    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: December 11, 2019
    Date of Patent: August 10, 2021
    Assignee: Proteostasis Therapeutics, Inc.
    Inventors: Benito Munoz, Cecilia M. Bastos, John Miller
  • Patent number: 11077094
    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: August 9, 2019
    Date of Patent: August 3, 2021
    Assignee: Aptinyx Inc.
    Inventors: John A. Lowe, III, M. Amin Khan
  • Patent number: 11077116
    Abstract: The invention refers to the use of isoxazole derivatives to prepare medicament able to induce fetal hemoglobin (HbF) synthesis in ?-thalassemia and sickle cell disease (SCD) patients.
    Type: Grant
    Filed: July 13, 2018
    Date of Patent: August 3, 2021
    Assignee: RARE PARTNERS SRL
    Inventors: Ilaria Lampronti, Roberto Gambari, Daniele Simoni
  • Patent number: 11058686
    Abstract: The invention provides compounds of formula (I) wherein R is —CH3 or —CH2CH3 and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful in the treatment of diseases or disorders mediated by IKKE, TBK1 and/or SIK2 mechanisms in a subject, for example cancer and inflammatory and tissue repair disorders. The invention also provides uses of the compounds of formula (I) and compositions containing them.
    Type: Grant
    Filed: February 23, 2018
    Date of Patent: July 13, 2021
    Assignee: DOMAINEX LIMITED
    Inventors: Gary Karl Newton, Mark Richard Stewart
  • Patent number: 11052094
    Abstract: Provided herein is an ophthalmic composition formulated in deuterated water. Also disclosed herein are methods of treating, ameliorating, or reducing ophthalmic conditions or diseases by administering to an eye of an individual in need thereof an effective amount of an ophthalmic composition as described herein.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: July 6, 2021
    Assignee: SYDNEXIS, INC.
    Inventors: Gregory I. Ostrow, Kenneth J. Widder, David S. Baker
  • Patent number: 11053198
    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 11, 2019
    Date of Patent: July 6, 2021
    Assignee: MISSION THERAPEUTICS LIMITED
    Inventors: Alison Jones, Mark Kemp, Martin Stockley, Karl Gibson, Gavin Whitlock
  • Patent number: 11053225
    Abstract: A pyrimidine derivative compound of Chemical Formula 1, an optical isomer thereof, or a pharmaceutically acceptable salt thereof, and a composition for preventing or treating cancer comprising the same as an active ingredient. The pyrimidine derivative compound of Chemical Formula 1, the optical isomer thereof, or the pharmaceutically acceptable salt thereof has an excellent selective inhibitory effect especially against TYRO 3 among TAM receptor inhibitory effects, and thus can be used as an excellent composition of preventing or treating cancer without adverse effects resulting from the inhibition of Axl and Mer.
    Type: Grant
    Filed: May 2, 2018
    Date of Patent: July 6, 2021
    Assignee: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Sung Yun Cho, Chang Hoon Lee, Yong Ki Min, Jong Yeon Hwang
  • Patent number: 11013728
    Abstract: The present invention aims to provide a novel cyclin-dependent kinase 8 and/or 19 inhibitor useful as an anti-cancer agent. The present invention relates to a cyclin-dependent kinase 8 and/or 19 inhibitor containing a compound represented by the formula (I): [wherein each symbol is as defined in the DESCRIPTION] or a pharmaceutically acceptable salt thereof as an active ingredient, and use thereof as an agent for preventing and/or treating cancer.
    Type: Grant
    Filed: April 2, 2018
    Date of Patent: May 25, 2021
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Tatsuya Kitao, Shigemitsu Takeda, Yoshimichi Shoji, Hiroaki Shirahase
  • Patent number: 10981894
    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: July 16, 2020
    Date of Patent: April 20, 2021
    Assignee: CRINETICS PHARMACEUTICALS, INC.
    Inventors: Sangdon Han, Yunfei Zhu, Sun Hee Kim, Jian Zhao, Shimiao Wang
  • Patent number: 10961222
    Abstract: Provided are a chemical compound of an isocitrate dehydrogenase inhibitor, and an application thereof, belonging to the field of medicinal chemistry; specifically provided is the chemical compound represented by formula I, or its isomer, pharmaceutically acceptable salt, crystal, solvate, or prodrug, as well as their preparation methods and pharmaceutical compositions containing said chemical compound, and an application of said chemical compound or composition. The chemical compound has very good ability to inhibit mutant IDH2 enzyme activity and to inhibit mutant IDH2 neoplastic cells, and may be used for preventing and/or treating a tumor characterized by the presence of mutant IDH2.
    Type: Grant
    Filed: July 20, 2017
    Date of Patent: March 30, 2021
    Assignee: NANJING SANHOME PHARMACEUTICAL CO., LTD.
    Inventors: Yong Wang, Liwen Zhao, Xiaorong Liu, Yan Zhang, Dandan Huang, Chunhuan Jiang, Xinsheng Shi, Hongfeng Gu, Silin Pang, Wei Hai, Bingyang Ge
  • 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