Patents Examined by Douglas M Willis
  • Substituted tetrahydropyrazolo[3,4-d]pyrimidines and tetrahydropyrazolo[4,3-d]pyrimidines as C5A receptor modulators
    Patent number: 11608341
    Abstract: The present invention relates to derivatives of formula (I) wherein Ring A, X, Y, Z, RA, R1, R2, R3 and R4 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as C5a receptor modulators.
    Type: Grant
    Filed: January 9, 2019
    Date of Patent: March 21, 2023
    Assignee: Idorsia Pharmaceuticals Ltd.
    Inventors: Sylvie Froidevaux, Francis Hubler, Mark Murphy, Dorte Renneberg, Simon Stamm
  • Substituted heteroaryls as thermally assisted delayed fluorescent materials
    Patent number: 11603370
    Abstract: Thermally assisted delayed fluorescent materials with triad-type materials for use in full color displays and lighting applications with the following generic structures are provided:
    Type: Grant
    Filed: October 9, 2020
    Date of Patent: March 14, 2023
    Assignee: Arizona Board of Regents on Behalf of Arizona State University
    Inventor: Jian Li
  • Process for preparing highly pure temozolomide
    Patent number: 11597731
    Abstract: The present invention provides a new process for preparation of imidazo-tetrazine class of chemical entity useful as anticancer agent. The present invention provides a commercially and economically viable process for preparation of Temozolomide of formula (VI). Present invention also relates to an intermediate compound of formula (III) and its preparation useful in the process for preparing Temozolomide.
    Type: Grant
    Filed: July 17, 2021
    Date of Patent: March 7, 2023
    Assignee: SHIVALIK RASAYAN LIMITED
    Inventors: Akshay Kant Chaturvedi, Bijan Kumar Panda, Amit Kumar, Deepali Chaturvedi
  • Substituted imidazoles as PLXDC2 ligands
    Patent number: 11597717
    Abstract: Provided are compounds of Formula Y-Z: The compounds target plexin domain containing 2 (PLXDC2). The compounds can be used to treat conditions such as inflammatory or immune-mediated diseases, diabetes, infectious diseases, and cancers. The compounds can be used to treat such specific conditions as systemic lupus erythematosus, rheumatoid arthritis, multiple sclerosis, autoimmune encephalitis, diabetic nephropathy, diabetic retinopathy, psoriasis, and inflammatory bowel disease, among other conditions.
    Type: Grant
    Filed: September 29, 2021
    Date of Patent: March 7, 2023
    Assignee: Landos Biopharma, Inc.
    Inventors: Josep Bassaganya-Riera, Andrew Leber, Raquel Hontecillas, Nuria Tubau-Juni
  • Substituted pyrrolizines for the treatment of hepatitis B
    Patent number: 11591334
    Abstract: The present invention relates to a bicyclic nucleocapsid inhibitor and the use of the same as a drug in the treatment of hepatitis B. In particular, disclosed is a compound having a structure shown by the following formula (A1): or a stereoisomer or a tautomer thereof, or a pharmaceutically acceptable salt, a hydrate, or a solvate thereof, that can be used as an HBV inhibitor, wherein the definition of each group is as described in detail in the description. The present invention also relates to a pharmaceutical composition comprising the compound and the use of the same in the treatment of hepatitis B.
    Type: Grant
    Filed: May 4, 2018
    Date of Patent: February 28, 2023
    Assignee: SHANGHAI LONGWOOD BIOPHARMACEUTICALS CO., LTD.
    Inventors: Zhe Wang, Guoqin Fan, Cenbin Lu, Sai Yang, Xiaoguang Wang
  • Solid forms of (R)-N-(2-(5-fluoropyridin-3-yl)-8-isopropylpyrazolo[ 1,5-a][1,3,5]triazin-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-amine maleate as aryl hydrocarbon receptor (AHR) inhibitors
    Patent number: 11591339
    Abstract: The present invention provides solid forms of (R)—N-(2-(5-fluoropyridin-3-yl)-8-isopropylpyrazolo[1,5-a][1,3,5]triazin-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-amine maleate (Compound 2) represented by the formula:
    Type: Grant
    Filed: November 25, 2020
    Date of Patent: February 28, 2023
    Assignee: IKENA ONCOLOGY, INC.
    Inventors: Alfredo C. Castro, James Martin Nolan, III, Sarah Jean Bethune, Corinne Marie Folberth
  • Substituted [1,2,4]triazolo[4,3-a]pyrazines as modulators of mGlu5 receptors
    Patent number: 11591337
    Abstract: Disclosed are triazole, imidazole and pyrrole condensed piperazine derivatives and their use as allosteric modulators of mGlus receptor activity, pharmaceutical compositions comprising such compounds, and methods of treatment therewith. Compounds of the invention can be used for the treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline, dementia or cognitive impairment, or other pathologies that can be related either directly or indirectly to glutamate dysfunction, i.e., disorders treatable by positive allosteric modulation (PAM) or by negative allosteric modulation (NAM) of mGluR5.
    Type: Grant
    Filed: January 17, 2019
    Date of Patent: February 28, 2023
    Assignee: Recordati Industria Chimica e Farmaceutica S.p.A.
    Inventors: Davide Graziani, Carlo Riva, Sergio Menegon, Valerio Tazzari
  • Substituted pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
    Patent number: 11591333
    Abstract: The present invention provides a method for preparing a pyrrolopyrimidine compound and application thereof. Specifically, the present invention provides a compound represented by formula I or pharmaceutically-acceptable salts thereof, a pharmaceutical composition containing the compound or its salts, and a method for preparing the pharmaceutical composition and an application of the pharmaceutical composition as an immunosuppressive drug.
    Type: Grant
    Filed: February 22, 2017
    Date of Patent: February 28, 2023
    Assignees: CINAKATE PHARM TECH (SHANGHAI) CO., LTD., CINKATE PHARMACEUTICAL INTERMEDIATES CO., LTD.
    Inventors: Na Liu, Lixia Bao, Zhepeng Wei, Yufeng Zhou, Bin Rong, Lihui Zhao, Fei Xiao
  • Substituted pyrazolo[3,4-b]pyrazines as SHP2 phosphatase inhibitors
    Patent number: 11591336
    Abstract: The present disclosure relates to compounds of formula (I) and pharmaceutical compositions thereof and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.
    Type: Grant
    Filed: May 25, 2018
    Date of Patent: February 28, 2023
    Assignees: D. E. Shaw Research, LLC, Relay Therapeutics, Inc.
    Inventors: Alexander M. Taylor, André Lescarbeau, Elizabeth H. Kelley, Kelley C. Shortsleeves, Lucian V. DiPietro, W. Patrick Walters, Mark Andrew Murcko, Levi Charles Thomas Pierce, Yong Tang, Fabrizio Giordanetto, Jack Benjamin Greisman, Paul Maragakis, Sathesh Bhat, Markus Kristofer Dahlgren, Eric Therrien
  • Substituted imidazoles as GLP-1 receptor agonists
    Patent number: 11584751
    Abstract: The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of GLP-1 receptor, a pharmaceutical composition comprising a compound of Formula (I), and a method of treating or preventing a disease in which GLP-1 receptor plays a role.
    Type: Grant
    Filed: November 2, 2021
    Date of Patent: February 21, 2023
    Assignee: Eccogene (Shanghai) Co., Ltd.
    Inventors: Zaifang Ren, Xuefeng Sun, Jingye Zhou, Qing Xu
  • Crystalline forms of (S)-4-amino-6-((1-(3-chloro-6-phenylimidazo[1,2-b]pyridazine-7-yl)ethyl)amino)pyrimidine-5-carbonitrile as inhibitors of phosphatidylinositol-3-kinase
    Patent number: 11584750
    Abstract: The present invention belongs to the pharmaceutical field, and provides crystalline forms, solvates and the crystalline forms thereof of the compound (S)-4-amino-6-((1-(3-chloro-6-phenylimidazo[1,2-b]pyridazin-7-yl)ethyl)amino)pyrimidine-5-carbonitrile of the formula shown below, and the pharmaceutical compositions comprising the same as well as the methods of preparing the same and the use thereof.
    Type: Grant
    Filed: April 18, 2019
    Date of Patent: February 21, 2023
    Assignee: HUTCHISON MEDIPHARMA LIMITED
    Inventors: Zhenping Wu, Wenji Li, Ling Feng
  • Triazolopyrimidine derivatives for use as ghrelin o-acyl transferase (GOAT) inhibitors
    Patent number: 11583532
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1 and R2 are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.
    Type: Grant
    Filed: January 28, 2019
    Date of Patent: February 21, 2023
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thomas Trieselmann, Cedrickx Godbout, Christoph Hoenke, Viktor Vintonyak
  • Substituted pyrrolo[1,2-a]pyrazines and pyrrolo[1,2-a][1,4]diazepines as TREX1 inhibitors
    Patent number: 11583538
    Abstract: The present invention provides compounds of Formula I: wherein X, R1, R2, R3 and R4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the TREX1 protein and thus can be used as medicaments for treating or preventing disorders affected by the inhibition of TREX1.
    Type: Grant
    Filed: October 6, 2020
    Date of Patent: February 21, 2023
    Assignee: VENENUM BIODESIGN, LLC
    Inventors: Jeffrey J. Letourneau, Kiruthika Selvarangan Elamparuthi, Chia-Yu Huang, Venugopalareddy Bommireddy Venkata
  • Radio-protective and chemo-protective substituted thiols
    Patent number: 11566032
    Abstract: The present disclosure relates to prodrugs, double prodrugs, derivatives and analogues of 3-(methylamino)-2-((methylamino)methyl)propane-1-thiol. The compounds of this disclosure also relate to The use of these compounds as radio— and chemo—protectors is also described.
    Type: Grant
    Filed: May 7, 2021
    Date of Patent: January 31, 2023
    Assignees: TONIX PHARMACEUTICALS, INC., TONIX PHARMACEUTICALS HOLDING CORP.
    Inventors: Philip S. Schein, Darryl C. Rideout
  • Substituted 2,6-dihydropyrrolo[3,4-c]pyrazoles as pyruvate kinase activators
    Patent number: 11566030
    Abstract: The subject matter described herein is directed to pyruvate kinase activating compounds of Formula I: and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds and methods of administering the compounds for the treatment of diseases associated with PKR and/or PKM2, such as pyruvate kinase deficiency, sickle cell disease, and beta-thalassemia.
    Type: Grant
    Filed: February 7, 2022
    Date of Patent: January 31, 2023
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Lina Q. Setti, Shahul Nilar, Zhe Li, Ming Yu, Manuel Zancanella
  • Substituted 1,2-oxaborolan-2-ols as PDE4 inhibitors
    Patent number: 11559538
    Abstract: The present invention relates to boron containing compounds of Formula (IA): that inhibit phosphodiesterase 4 (PDE4). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating diseases, conditions, or disorders ameliorated by inhibition of PDE4.
    Type: Grant
    Filed: October 28, 2020
    Date of Patent: January 24, 2023
    Assignee: Pfizer Inc.
    Inventors: Joseph Walter Strohbach, Tsutomu Akama, David Clive Blakemore, Robert Toms Jacobs, Peter Jones, David Christopher Limburg, Martins Sunday Oderinde, Matthew Alexander Perry, Jacob John Plattner, Rubben Federico Torella, Yasheen Zhou, Thean Yeow Yeoh
  • Crystalline forms of (S)-7-(1-(but-2-ynoyl)piperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof
    Patent number: 11555038
    Abstract: The present invention relates to a crystalline form of (S)-7-(1-(but-2-ynoyl)piperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide (Compound 1) for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease, such as an allergic disease, an autoimmune disease, an inflammatory disease, and a cancer.
    Type: Grant
    Filed: January 25, 2018
    Date of Patent: January 17, 2023
    Assignee: BEIGENE, LTD.
    Inventors: Yunhang Guo, Desheng Yu, Zhiwei Wang
  • Quaternary ammonium salts of phenanthroindolizidine and phenanthroquinolizidine alkaloids as hypoxia-targeted anticancer agents
    Patent number: 11548891
    Abstract: A compound having a structure of formula (I): Wherein each of R1A, R1B, R1C, R1D, R1E and R1F is independently selected from the group consisting of a hydrogen atom, a hydroxide group, and a substituted or unsubstituted C1-C8 alkoxy group, R2 is selected from the group consisting of a hydrogen atom and a hydroxide group, R3 is hydrogen atom, R4 is selected from the group consisting of a hydrogen atom, a C1-C3 alkyl group, and a C1-C3 fluoroalkyl group, R5 is selected from the group consisting of a hydrogen atom, a C1-C6 alkyl, and a C1-C6 fluoroalkyl, n is 1 or 2, and X is a negatively charged anion. Removal of the substituted nitroimidazole affords a phenanthroindolizidine or phenanthroquinolizidine alkaloid derivative. The compound is used in a pharmaceutical composition and a method of treating a proliferative disease.
    Type: Grant
    Filed: April 22, 2022
    Date of Patent: January 10, 2023
    Assignee: BATTERJEE MEDICAL COLLEGE
    Inventors: Ziad Omran, Omeima Abdullah, Ikhlas A. Sindi, Ahmed Altyar, Afnan S. Batubara
  • Substituted 1,4-methanopyrido[1?,2?:4,5]pyrazino[1,2-a]pyrimidines for treating viral infections
    Patent number: 11548901
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 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: Grant
    Filed: May 6, 2020
    Date of Patent: January 10, 2023
    Assignee: Gilead Sciences, Inc.
    Inventors: Elizabeth M. Bacon, Zhenhong R. Cai, Xiaowu Chen, Jeromy J. Cottell, Manoj C. Desai, Mingzhe Ji, Haolun Jin, Scott E. Lazerwith, Michael R. Mish, Philip Anthony Morganelli, Hyung-Jung Pyun, James G. Taylor, Teresa Alejandra Trejo Martin
  • Process for making crystalline 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(cyclopropylsulfonyl)azetidin-3-yl)acetonitrile
    Patent number: 11548895
    Abstract: The present disclosure provides crystalline forms of 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(cyclopropylsulfonyl)azetidin-3-yl)acetonitrile, pharmaceutical compositions comprising the crystalline forms, methods of using the crystalline forms, and processes for making the crystalline forms.
    Type: Grant
    Filed: April 22, 2020
    Date of Patent: January 10, 2023
    Assignee: Elanco US Inc.
    Inventors: Jingdan Hu, Timothy Andrew Woods