Patents by Inventor Rajinder Singh

Rajinder Singh has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • DIRECT AMPK ACTIVATORS
    Publication number: 20180051006
    Abstract: Disclosed are benzimidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R1, R2, R3, R4, Y and X are as described herein. In certain embodiments, a compound disclosed herein activates AMPK, and can be used to treat disease by activating the AMPK pathway.
    Type: Application
    Filed: August 15, 2017
    Publication date: February 22, 2018
    Inventors: Simon Shaw, Xiang Xu, Sarkiz Issakani, Rajinder Singh, Yasumichi Hitoshi, Matthew Duncton, Nan Lin
  • Compounds and method for treating autoimmune diseases
    Patent number: 9890144
    Abstract: Compounds and embodiments of a method for treating and/or preventing autoimmune diseases are disclosed. The method includes administering to a subject having an autoimmune disease, such as an inflammatory bowel disease, a therapeutically effective amount of a compound according to formula I wherein X and Y independently are O or NR1; each R1 is independently H or C1-C6 alkyl; ring A is aryl; each R2 independently is H, alkyl, alkoxy, amide, cyano, halo, haloalkyl, hydroxyalkyl, heteroalkyl, heterocyclyl, sulfonyl, sulfonamide, or two R2 groups, taken together with the atom or atoms to which they are attached, combine to form a 4-10 membered ring system; p is 0, 1, 2, 3, or 4; R3 and R4 independently are H or C1-C6 alkyl; and R5 is halo, cyano, or C1-C6 alkyl.
    Type: Grant
    Filed: June 25, 2015
    Date of Patent: February 13, 2018
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Esteban Masuda, Rajinder Singh, Vanessa Taylor, Donald G. Payan
  • TGF-beta inhibitors
    Patent number: 9884868
    Abstract: Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R? are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-?, and can be used to treat disease by blocking TGF-? signaling.
    Type: Grant
    Filed: February 26, 2016
    Date of Patent: February 6, 2018
    Assignees: Rigel Pharmaceuticals, Inc., Bristol-Myers Squibb Company
    Inventors: Todd Kinsella, Marina Gelman, Hui Hong, Ihab S. Darwish, Rajinder Singh, Jiaxin Yu, Robert M. Borzilleri, Upender Velaparthi, Peiying Liu, Chetan Darne, Hasibur Rahaman, Jayakumar Sankara Warrier
  • Protein Kinase C Inhibitors and Uses Thereof
    Publication number: 20180030050
    Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: May 5, 2017
    Publication date: February 1, 2018
    Inventors: Rajinder Singh, Matthew Duncton, Jing Zhang, Salvador Alvarez, Kin Tso, Sacha Holland, Rose Yen, Rao Kolluri, Thilo Heckrodt, Yan Chen, Esteban Masuda, Hui Li, Donald G. Payan, Ryan Kelley
  • GDF-8 inhibitors
    Patent number: 9878992
    Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.
    Type: Grant
    Filed: July 13, 2017
    Date of Patent: January 30, 2018
    Assignee: RIGEL PHARMACEUTICALS, INC.
    Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
  • TYROSINE KINASE INHIBITORS
    Publication number: 20180008589
    Abstract: Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, Y and Z are as described herein. In certain embodiments, a compound disclosed herein inhibits a cellular TAM receptor, and can be used to treat disease mediated by or involving the TAM receptor family.
    Type: Application
    Filed: July 10, 2017
    Publication date: January 11, 2018
    Inventors: Sacha Holland, Rajinder Singh, Somasekhar Bhamidipati, Pingyu Ding, Rao Kolluri, Ihab Darwish, Esteban Masuda, Jiaxin Yu
  • IMMUNOMODULATOR COMPOUNDS
    Publication number: 20180008554
    Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (II): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: June 26, 2017
    Publication date: January 11, 2018
    Inventors: Christopher LANGE, Viengkham MALATHONG, Darren J. McMURTRIE, Sreenivas PUNNA, Rajinder SINGH, Ju YANG, Penglie ZHANG
  • Tetrazolones as a Carboxylic Acid Bioisosteres
    Publication number: 20180002297
    Abstract: The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Application
    Filed: June 8, 2017
    Publication date: January 4, 2018
    Inventors: Matthew Duncton, Rajinder Singh
  • 2,4-DIAMINO-PYRIMIDINE COMPOUNDS AND METHOD FOR MAKING AND USING THE COMPOUNDS
    Publication number: 20170369476
    Abstract: Compounds within the scope of the present invention have a Formula 1 or a salt or prodrug thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 ?M to 3.7 ?M; a TAK1 IC50 of from 0.008 ?M to 132 ?M; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.
    Type: Application
    Filed: June 26, 2017
    Publication date: December 28, 2017
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Rose Yen, Jiaxin Yu, Vanessa Taylor, Rajinder Singh
  • Protein Kinase C Inhibitors and Uses Thereof
    Publication number: 20170360786
    Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: December 30, 2016
    Publication date: December 21, 2017
    Inventors: Rajinder Singh, Matthew Duncton, Jing Zhang, Salvador Alvarez, Kin Tso, Sacha Holland, Rose Yen, Rao Kolluri, Thilo Heckrodt, Yan Chen, Esteban Masuda, Hui Li, Donald G. Payan
  • Nrf2 activating compounds and uses thereof
    Patent number: 9845307
    Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: February 2, 2017
    Date of Patent: December 19, 2017
    Inventors: Matthew Duncton, Rajinder Singh
  • Nrf2 activating compounds and uses thereof
    Patent number: 9845311
    Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds may find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: February 1, 2017
    Date of Patent: December 19, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Matthew Duncton, Rajinder Singh
  • Kinase inhibitors and their uses
    Patent number: 9834568
    Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.
    Type: Grant
    Filed: June 30, 2015
    Date of Patent: December 5, 2017
    Assignee: RIGEL PHARMACEUTICALS, INC.
    Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland
  • Modulators of chemokine receptors
    Patent number: 9834545
    Abstract: Compounds are provided as chemokine inhibitors having the structure:
    Type: Grant
    Filed: November 17, 2016
    Date of Patent: December 5, 2017
    Assignee: CHEMOCENTRYX, INC.
    Inventors: Xi Chen, Dean R. Dragoli, Junfa Fan, Jaroslaw Kalisiak, Antoni Krasinski, Manmohan Reddy Leleti, Venkat Mali, Jeffrey McMahon, Rajinder Singh, Hiroko Tanaka, Ju Yang, Chao Yu, Penglie Zhang
  • GDF-8 Inhibitors
    Publication number: 20170342048
    Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.
    Type: Application
    Filed: July 13, 2017
    Publication date: November 30, 2017
    Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
  • Fumarate analogs and uses thereof
    Patent number: 9801866
    Abstract: Aspects of the present disclosure include compounds that find use for the treatment of a variety of autoimmune and inflammatory diseases and disorders. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: October 31, 2017
    Assignee: Rigl Pharmaceutical, Inc.
    Inventors: Matthew Duncton, Somasekhar Bhamidipati, Jiaxin Yu, Ihab Darwish, Rajinder Singh
  • COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
    Publication number: 20170298054
    Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.
    Type: Application
    Filed: June 29, 2017
    Publication date: October 19, 2017
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
  • Alpha-7 nicotinic acetylcholine receptor modulators and uses thereof-I
    Patent number: 9790173
    Abstract: The present invention relates to chemical compounds of formula (I), with the substituents as described in the specification, useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7 nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of ?7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: October 17, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Andrew Harvey, Thomas Avery, Dharam Paul, Justin Ripper, Belinda Huff, Rajinder Singh, Laurent Schaeffer, Christophe Joseph, Christophe Morice, Bruno Giethlen
  • Prodrugs of 2,4-Pyrimidinediamine Compounds and Their Uses
    Publication number: 20170291909
    Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.
    Type: Application
    Filed: November 23, 2016
    Publication date: October 12, 2017
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Somasekhar Bhamidipati, Esteban Masuda, Thomas Sun, Valentino J. Stella
  • Method of treating melanoma by administration of pharmaceutical formulations of (S)-methyl (1-((4-(3-(5-chloro-2-fluoro-3-(methylsulfonamido)phenyl)-1-isopropyl-1H-pyrazol-4-yl)pyrimidin-2-yl)amino)propan-2-yl)carbamate
    Patent number: 9763941
    Abstract: This invention relates to solid oral pharmaceutical formulations of (S)-methyl (1-((4-(3-(5-chloro-2-fluoro-3-(methyl -sulfonamido)phenyl)-1-isopropyl-1H-pyrazol-4-yl)pyrimidin-2-yl)amino)propan-2-yl)carbamate (COMPOUND A) and the use of these formulations for treating proliferative diseases, such as solid tumor diseases.
    Type: Grant
    Filed: June 10, 2016
    Date of Patent: September 19, 2017
    Assignee: Array BioPharma, Inc.
    Inventors: Daya Verma, Yogita Krishnamachari, Xiaohong Shen, Hanchen Lee, Ping Li, Rajinder Singh, LayChoo Tan