1,4-diazine As One Of The Cyclos Patents (Class 514/249)
  • Patent number: 11685746
    Abstract: The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease. In particular, the present description relates to substituted bicyclic heteroaryl compounds of Formula (I), Formula (II), Formula (III), or Formula (IV), forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease.
    Type: Grant
    Filed: June 25, 2019
    Date of Patent: June 27, 2023
    Assignee: PTC Therapeutics, Inc.
    Inventors: Guangming Chen, Anuradha Bhattacharyya, Yao Jiang, Gary Mitchell Karp, Jana Narasimhan, Anthony Turpoff, Nanjing Zhang
  • Patent number: 11674185
    Abstract: The present application mainly relates to a method for determining a prognosis for a subject diagnosed with high-grade serous ovarian cancer. The method comprises determining the prognosis based on activities of at least two cellular signaling pathways including a phosphatidylinositide 3-kinase (PI3K) pathway and a nuclear factor-kappa B (NFkB or NF?B) pathway in a sample of the subject. The present application also relates to a method for identifying a subject diagnosed with high-grade serous ovarian cancer that will be suitable for a PI3K pathway targeting therapy or an NFkB pathway targeting therapy. The method comprises identifying the subject based on activities of at least two cellular signaling pathways including a PI3K pathway and an NFkB pathway in a sample of the subject. The present application further relates to corresponding apparatuses, non-transitory storage media, computer programs and kits.
    Type: Grant
    Filed: May 1, 2020
    Date of Patent: June 13, 2023
    Assignee: KONINKLIJKE PHILIPS N.V.
    Inventors: Anja Van de Stolpe, Wilhelmus Franciscus Johannes Verhaegh
  • Patent number: 11674965
    Abstract: Disclosed herein is a method for analyzing the concentration of a fluorescent compound in the plasma of a patient. The method includes collecting a sample of plasma from a patient, diluting the sample with a solvent and analyzing the diluted sample by HPLC. The sample does not need to be dried down during sample preparation nor is an internal standard required.
    Type: Grant
    Filed: November 15, 2018
    Date of Patent: June 13, 2023
    Assignee: MediBeacon Inc.
    Inventor: Jeng J. Shieh
  • Patent number: 11673901
    Abstract: The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: June 11, 2020
    Date of Patent: June 13, 2023
    Assignee: REVOLUTION MEDICINES, INC.
    Inventors: Elena S. Koltun, Naing N. Aay, Andreas Buckl, Kevin T. Mellem, Brian R. Blank, Jennifer Pitzen, Gang Wang, Ashutosh S. Jogalekar, Walter S. Won, Christos Tzitzilonis, Jie Jack Li, Adrian Liam Gill, James Joseph Cregg
  • Patent number: 11649224
    Abstract: Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.
    Type: Grant
    Filed: May 6, 2021
    Date of Patent: May 16, 2023
    Assignee: Cornell University
    Inventors: Joseph P. Vacca, Dansu Li, Sarah Bettigole
  • Patent number: 11649237
    Abstract: Provided herein, inter alia, are substituted imidazo[1,5-?]pyrazine compounds, compositions and methods for treating or preventing an IRE1?-related disease or disorder. In certain embodiments, the disease or disorder is selected from the group consisting of a neurodegenerative disease, a demyelinating disease, cancer, an eye disease, a fibrotic disease, and diabetes.
    Type: Grant
    Filed: August 31, 2018
    Date of Patent: May 16, 2023
    Assignees: Optikira LLC, The Regents of the University of California
    Inventors: Richard M. Keenan, Bradley J. Backes, Dustin J. Maly, Charles Reynolds, Ben Whittaker, Jamie Knight, Jonathan Mark Sutton, George Hynd, Feroz R. Papa, Scott A. Oakes
  • Patent number: 11642351
    Abstract: The present invention relates to orally administered liquid pharmaceutical compositions of eslicarbazepine. The liquid compositions are in the form of ready to use suspension and suspension powder for reconstitution. It also relates to the processes for the preparation of said liquid compositions. The present invention provides liquid compositions of eslicarbazepine with desired technical attributes such as release profile and pH. The prepared compositions are useful in patients having difficulties in swallowing tablets and provide physician with providing a more convenient and less cumbersome posology.
    Type: Grant
    Filed: March 23, 2020
    Date of Patent: May 9, 2023
    Inventors: Dinesh Kumar, Saurabh Srivastava, Indranil Nandi, Rakesh K. Singh, Amit Jha, Kamal S. Mehta
  • Patent number: 11639356
    Abstract: Provided are compounds of formula (I): or cosmeceutically acceptable or pharmaceutically acceptable salts thereof. Additionally provided are cosmeceutical and/or pharmaceutical compositions comprising the compounds of formula (I), or the cosmeceutically acceptable or pharmaceutically acceptable salts thereof. Also provided are therapeutic and/or cosmetic methods using the cosmeceutical and/or pharmaceutical compositions comprising the compounds of formula (I), or the cosmeceutically acceptable or pharmaceutically acceptable salts thereof, for modulating cyclic adenosine monophosphate response element binding (CREB)-binding protein (CBP)/?-catenin mediated signaling in treating skin related diseases, conditions, or disorders mediated by aberrant CBP/?-catenin signaling and cosmetic methods for treating skin conditions mediated by aberrant CBP/?-catenin signaling.
    Type: Grant
    Filed: October 1, 2021
    Date of Patent: May 2, 2023
    Assignee: Genesis Molecular Technologies, Inc.
    Inventor: Fuqiang Ruan
  • Patent number: 11633395
    Abstract: Provided are a compound that is useful for the prevention of and/or as a treatment agent for a disease in which a group II mGlu receptor is involved; and a medical application of said compound. Provided is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 22, 2018
    Date of Patent: April 25, 2023
    Assignee: SUMITOMO PHARMA CO., LTD.
    Inventors: Yohei Ikuma, Kengo Tojo, Ryo Fukazawa, Shuji Masumoto
  • Patent number: 11634435
    Abstract: The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: June 11, 2020
    Date of Patent: April 25, 2023
    Assignee: REVOLUTION MEDICINES, INC.
    Inventors: Elena S. Koltun, Naing N. Aay, Andreas Buckl, Kevin T. Mellem, Brian R. Blank, Jennifer Pitzen, Gang Wang, Ashutosh S. Jogalekar, Walter S. Won, Christos Tzitzilonis, Jie Jack Li, Adrian Liam Gill, James Joseph Cregg
  • Patent number: 11629146
    Abstract: The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.
    Type: Grant
    Filed: November 28, 2017
    Date of Patent: April 18, 2023
    Assignee: PRAXIS PRECISION MEDICINES, INC.
    Inventors: Kiran Reddy, Gabriel Martinez Botella, Andrew Mark Griffin, Brian Edward Marron
  • Patent number: 11617752
    Abstract: The present invention features compositions including sepiapterin, or a pharmaceutically acceptable salt thereof, and methods for the treatment of BH4-related disorders. In some embodiments, these compositions and methods result in an increase in plasma, CSF, and/or brain exposure of sepiapterin.
    Type: Grant
    Filed: May 30, 2019
    Date of Patent: April 4, 2023
    Assignee: PTC Therapeutics MP, Inc.
    Inventors: Neil Smith, Jonathan Reis
  • Patent number: 11613544
    Abstract: Described herein, inter alia, are certain substituted imidazo[1,5-a]pyrazines of formula (I) and methods of using the same for modulating the activity of Ire1.
    Type: Grant
    Filed: September 24, 2020
    Date of Patent: March 28, 2023
    Assignees: The Regents of the University of California, University of Washington Through Its Center For Commercialization
    Inventors: Bradley J. Backes, Dustin J. Maly, Scott A. Oakes, Feroz R. Papa, Gayani Perera, Likun Wang
  • Patent number: 11602537
    Abstract: The present disclosure relates to the field of synthesizing substantially pure varenicline and its intermediates. It also relates to the pharmaceutical compositions comprising varenicline and the method of use of these pharmaceutical compositions for smoking cessation.
    Type: Grant
    Filed: April 15, 2022
    Date of Patent: March 14, 2023
    Assignee: Par Pharmaceutical, Inc.
    Inventors: Joseph Prabahar Koilpillai, Sayuj Nath, Satish Patil, Somasundaram Muthuramalingam, Selvakumar Viruthagiri, Mohankumar Lakshmanan
  • 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
  • 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
  • Patent number: 11590129
    Abstract: The present invention relates to the combination of PM01183 with several anticancer drugs, in particular other anticancer drugs selected from antitumor platinum coordination complexes, antimetabolites, mitotic inhibitors, anticancer antibiotics, topoisomerase I and/or II inhibitors, proteasome inhibitors, histone deacetylase inhibitors, nitrogen mustard alkylating agents, nitrosourea alkylating agents, nonclassical alkylating agents, estrogen antagonists, androgen antagonists, mTOR inhibitors, tyrosine kinase inhibitors, and other agents selected from aplidine, ET-743, PM02734 and PM00104, and the use of these combinations in the treatment of cancer.
    Type: Grant
    Filed: November 28, 2017
    Date of Patent: February 28, 2023
    Assignee: PHARMA MAR, S.A.
    Inventors: Victoria Moneo Ocaña, Gema Santamaría Núñez, Luis Francisco García Fernández, Carlos María Galmarini, María José Guillén Navarro, Pablo Manuel Avilés Marín
  • Patent number: 11578068
    Abstract: The invention relates to compounds of formula (I) inhibiting Rho Kinase that are oxidazole derivatives, processes for preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
    Type: Grant
    Filed: December 12, 2018
    Date of Patent: February 14, 2023
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Alessandro Accetta, Fabio Rancati, Christine Edwards, Elizabeth Anne Skidmore
  • Patent number: 11576913
    Abstract: The disclosure relates to methods for treating or preventing an Insomnia Disorder by administering to a human in need thereof a compound of formula (I), or a compound of formula (IA), (IB), or (IC), or a solvate thereof, in a daily dose of from about 0.5 mg to about 6.0 mg. In certain embodiments, such compounds effectively treat or prevent an Insomnia Disorder in the animal, while producing reduced side effects compared to previously available compounds.
    Type: Grant
    Filed: January 22, 2019
    Date of Patent: February 14, 2023
    Assignee: Purdue Pharma L.P.
    Inventors: Stephen C. Harris, Ram P. Kapil, Donald J. Kyle, Garth Whiteside
  • Patent number: 11576906
    Abstract: Methods of treating patients diagnosed with cancer harboring an IDH-1 mutation are provided, including the therapeutic administration of a certain inhibitor of a mutant IDH-1 as a single agent, or in combination with azacitidine (AZA).
    Type: Grant
    Filed: May 16, 2019
    Date of Patent: February 14, 2023
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Patrick F. Kelly, Alan Collis, Jeff Davis, Duncan Walker, Susan Ashwell, Blythe Thomson, Wei Lu
  • Patent number: 11571423
    Abstract: The present invention relates to compounds of formula (I). The compounds maybe used to modulate the Stimulator of Interferon Genes (STING) protein and thereby treat diseases such as cancer and microbial infections.
    Type: Grant
    Filed: June 21, 2018
    Date of Patent: February 7, 2023
    Assignee: Curadev Pharma Limited
    Inventors: Monali Banerjee, Sandip Middya, Sourav Basu, Rajib Ghosh, David Pryde, Dharmendra Yadav, Ritesh Shrivastava, Arjun Surya
  • Patent number: 11530220
    Abstract: Provided herein are compounds, compositions and methods of using the compounds and compositions for the treatment of diseases modulated, as least in part, by AhR. The compounds are represented by formula: wherein the letters and symbols a, b, c, d, e, f, A, R1, X1, Ar1 and Ar2 have the meanings provided in the specification.
    Type: Grant
    Filed: February 5, 2019
    Date of Patent: December 20, 2022
    Assignee: IDEAYA BIOSCIENCES, INC.
    Inventors: Hilary Plake Beck, Marcos Gonzalez-Lopez, James Clifford Sutton, Jr.
  • Patent number: 11529348
    Abstract: Cellular biological activities are tightly controlled by intracellular signaling processes initiated by extracellular signals. Protein tyrosine phosphatases, which remove phosphate groups from tyrosine phosphorylated signaling molecules, play equally important tyrosine roles as protein kinases in signal transduction. SHP-2, a cytoplasmic SH2 domain containing protein tyrosine phosphatase, is involved in the signaling pathways of a variety of growth factors and cytokines. Recent studies have clearly demonstrated that this phosphatase plays an important role in transducing signal relay from the cell surface to the nucleus, and is a critical intracellular regulator in mediating cell proliferation and differentiation.
    Type: Grant
    Filed: September 28, 2018
    Date of Patent: December 20, 2022
    Assignees: D. E. Shaw Research, LLC, Relay Therapeutics, Inc.
    Inventors: Alexander M. Taylor, W. Patrick Walters, Mark Andrew Murcko, Fabrizio Giordanetto, Eric Therrien, Sathesh Bhat, Markus Kristofer Dahlgren
  • Patent number: 11523986
    Abstract: Disclosed herein are compositions including diphenhydramine, or a pharmaceutically acceptable salt thereof, and a liquid vehicle. The compositions may be administered intranasally to patients in need of diphenhydramine. The compositions provide increase plasma and brain concentrations relative to orally administered compositions, but without the limitations associated with intravenously administered compositions.
    Type: Grant
    Filed: March 19, 2020
    Date of Patent: December 13, 2022
    Assignee: DBBH, LLC
    Inventors: John Sramek, Anthony R. DiSanto
  • Patent number: 11517570
    Abstract: The present disclosure relates to compounds that are Syk inhibitors or pharmaceutically acceptable salts or co-crystals thereof, and pharmaceutical compositions thereof, and to their use in the treatment of various disease states, including cancer and inflammatory conditions.
    Type: Grant
    Filed: October 28, 2020
    Date of Patent: December 6, 2022
    Assignee: Kronos Bio, Inc.
    Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Jennifer R. Lo, Scott A. Mitchell, Aaron C. Schmitt, Sundaramoorthi Swaminathan, Jin-Ming Xiong, Jianjun Xu, Zhongdong Zhao
  • Patent number: 11517537
    Abstract: The present invention relates generally to abuse-deterrent formulations containing dextroamphetamine sulfate.
    Type: Grant
    Filed: November 11, 2019
    Date of Patent: December 6, 2022
    Assignee: Vallon Pharmaceuticals, Inc.
    Inventors: Yaron Daniely, David Baker, Hanna Ron, David Siner
  • Patent number: 11497793
    Abstract: Compositions and methods for treating malignant gliomas such as glioblastoma are provided, comprising a combination of a peptide conjugate comprising an amino acid sequence derived from the N-terminus of the receptor PAR-1, and the chemotherapeutic agent temozolomide.
    Type: Grant
    Filed: April 16, 2019
    Date of Patent: November 15, 2022
    Assignee: TEL HASHOMER MEDICAL RESEARCH INFRASTRUCTURE AND SERVICES LTD.
    Inventors: Joab Chapman, Efrat Shavit-Stein
  • Patent number: 11484527
    Abstract: Abuse deterrent solid dosage formulations containing 5-({[2-Amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid, and processes for the preparation and administration of these formulations.
    Type: Grant
    Filed: December 8, 2021
    Date of Patent: November 1, 2022
    Assignee: Allergan Holdings Unlimited Company
    Inventors: Tim Costello, Jens Jozef Ceulemans, Eugeen Maria Jozef Jans, Philip Erna H. Heyns
  • Patent number: 11478491
    Abstract: Disclosed herein are compositions comprising tobramycin or a tobramycin derivative that exhibit improvements in permeation of corneal cells, retention in corneal cells, or both. Such compositions can comprise tobramycin or tobramycin derivative(s) complexed to an agent which facilitates improved permeation of corneal cells, retention in corneal cells, or both. The invention also relates to a process of preparing such compositions.
    Type: Grant
    Filed: November 1, 2021
    Date of Patent: October 25, 2022
    Assignee: Somerset Therapeutics, LLC
    Inventors: Mandar V. Shah, Veerappan Subramanian, Ilango Subramanian, Ojas Prakashbhai Doshi
  • Patent number: 11471455
    Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize) the apelin receptor (also referred to herein as the APJ receptor, gene symbol APLNR). This disclosure also features compositions containing the same as well as other methods of using and making the same. The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which a decrease in APJ receptor activity (e.g., repressed or impaired APJ receptor signaling; e.g., repressed or impaired apelin-APJ receptor signaling) or downregulation of endogenous apelin contributes to the pathology and/or symptoms and/or progression of the disease, disorder, or condition.
    Type: Grant
    Filed: January 10, 2022
    Date of Patent: October 18, 2022
    Assignee: ANNAPURNA BIO, INC.
    Inventors: Haifeng Tang, Michael Hanson, Sarah Boyce, Zhe Nie
  • Patent number: 11472817
    Abstract: The present specification relates to a heterocyclic compound represented by Chemical Formula 1, and an organic light emitting device comprising the same.
    Type: Grant
    Filed: September 19, 2019
    Date of Patent: October 18, 2022
    Assignee: LT MATERIALS CO., LTD.
    Inventors: Hyun-Ju La, Yu-Jin Heo, Won-Jang Jeong
  • Patent number: 11464781
    Abstract: Compounds that inhibit phosphodiesterase 1 (PDE1) are useful to treat glaucoma or elevated intraocular pressure. The PDE1 inhibitors may be administered as monotherapy or in combination with additional intraocular-pressure lowering agents. In addition, the invention provides ophthalmic compositions comprising PDE 1 inhibitors and optionally one or more additional intraocular pressure-lowering agents. Topical and systemic therapy may be used.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: October 11, 2022
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Robert Davis, Allen Fienberg
  • Patent number: 11466015
    Abstract: The present disclosure relates to crystalline forms of 8-(2-fluorobenzyl)-6-(3-(trifluoromethyl)-1H-1,2,4-triazol-5-yl)imidazo[1,2-a]pyrazine, depicted below as a compound of Formula (I): which are useful as a stimulator of soluble guanylate cyclase (sGC). The present disclosure also provides pharmaceutically acceptable compositions comprising the crystalline forms and methods of using said compositions in the treatment of various disorders.
    Type: Grant
    Filed: March 7, 2019
    Date of Patent: October 11, 2022
    Assignee: Cyclerion Therapeutics, Inc.
    Inventors: Kwame W. Nti-Addae, Leena Kumari Prasad, Thomas Storz
  • Patent number: 11458149
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: May 29, 2020
    Date of Patent: October 4, 2022
    Assignee: IKENA ONCOLOGY, INC.
    Inventor: Alfredo C. Castro
  • Patent number: 11453683
    Abstract: Compounds that inhibit KRas G12D; in particular, compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor, and in particular, methods of treating cancer. The compounds have a general structure represented by Formula (I): or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 27, 2020
    Date of Patent: September 27, 2022
    Assignees: MIRATI THERAPEUTICS, INC., ARRAY BIOPHARMA INC.
    Inventors: Xiaolun Wang, Aaron Craig Burns, James Gail Christensen, John Michael Ketcham, John David Lawson, Matthew Arnold Marx, Christopher Ronald Smith, Shelley Allen, James F. Blake, Mark Joseph Chicarelli, Joshua Ryan Dahlke, Donghua Dai, Jay Bradford Fell, John Peter Fischer, Macedonio J. Mejia, Brad Newhouse, Phong Nguyen, Jacob Matthew O'Leary, Spencer Pajk, Martha E. Rodriguez, Pavel Savechenkov, Tony P. Tang, Guy P. A. Vigers, Qian Zhao, Dean Russell Kahn, John Gaudino, Michael Christopher Hilton
  • Patent number: 11453673
    Abstract: The present invention provides a compound of Formula I: wherein R1 is methyl, ethyl or cyclopropyl; R2 is hydrogen, methyl, or ethyl; R3 is methyl or AA; and R4 is C2-C4 alkyl, BB; or a pharmaceutically acceptable salt thereof; for use as a PDE1 inhibitor.
    Type: Grant
    Filed: January 13, 2019
    Date of Patent: September 27, 2022
    Assignee: ELI LILLY AND COMPANY
    Inventors: Nicholas Paul Camp, Chafiq Hamdouchi, Jayana Pankaj Lineswala, John Richard Morphy, Qing Shi
  • Patent number: 11447449
    Abstract: The present invention provides a compound of formula (II): an inhibitor of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treatment of proliferative disorders, such as cancer, viral infections and/or autoimmune diseases. Its prodrugs are disclosed.
    Type: Grant
    Filed: January 3, 2019
    Date of Patent: September 20, 2022
    Assignee: Bristol-Myers Squibb Company
    Inventors: James Aaron Balog, Steven P. Seitz, David K. Williams, Murugaiah Andappan Murugaiah Subbaiah
  • Patent number: 11439624
    Abstract: The present invention relates to the use of an Angiotensin II type 1 (AT1) receptor blocker for promoting sleep and/or the treatment of insomnia. It is based, at least in part, on the results of experiments performed using a validated rat model of stress-induced insomnia in which candesartan was found to ameliorate sleep disturbances induced by stress. Further, it was observed that this effect seems to be caused by blockade of AT1 receptors located in several brain regions that are key components of the neural circuitry activated during insomnia. In contrast to currently marketed treatments for insomnia, the AT1 receptor blocker was found to restore normal sleep without inhibiting REM sleep and/or inducing atypical wave components in the EEG.
    Type: Grant
    Filed: September 21, 2020
    Date of Patent: September 13, 2022
    Assignee: University of Pittsburgh—of the Commonwealth System of Higher Education
    Inventors: Georgina Cano, Alan F. Sved
  • Patent number: 11434222
    Abstract: Provided herein are substituted 1,1,1,3,3,3-hexafluoropropan-2-yl 6-azaspiro[2.5]octane-6-carboxylate compounds and pharmaceutical compositions comprising said compounds. The compounds and compositions provided herein are useful as inhibitors of MAGL. Furthermore, the compounds and compositions as provided herein are useful for the treatment of diseases and disorders benefiting from the inhibition of MAGL.
    Type: Grant
    Filed: November 11, 2021
    Date of Patent: September 6, 2022
    Assignee: H. LUNDBECK A/S
    Inventors: John J. M. Wiener, Cheryl A. Grice, Daniel J. Buzard, Justin S. Cisar, Olivia Delene Weber, Amy Allan, Nicholas Raffaele, Jeanne Moody, Michael B. Shaghafi
  • Patent number: 11427589
    Abstract: Described herein are methods for making folic acid derivatives, intermediates, pharmaceutical compositions and uses thereof.
    Type: Grant
    Filed: February 4, 2020
    Date of Patent: August 30, 2022
    Assignee: JSB PHARMA DEVELOPMENT, LLC
    Inventors: Gerald S. Jones, Jr., Joseph P. St. Laurent, Scott A. Goodrich
  • Patent number: 11426472
    Abstract: Excessive deposition of extracellular matrix is a hallmark of Idiopathic pulmonary fibrosis (IPF), it is advantageous to target the cells and the mechanisms associated with this process. By targeting myofibroblasts (specialized contractile fibroblasts) that are key for the development of IPF with drugs conjugated with fibroblast activation protein (FAP), this technology helps minimize the production of extracellular matrix in the lungs and provides a new treatment option for patients diagnosed with IPF.
    Type: Grant
    Filed: October 15, 2019
    Date of Patent: August 30, 2022
    Assignee: Purdue Research Foundation
    Inventors: Philip Stewart Low, Suraj U. Hettiarachchi, Yen-Hsing Li, Jyoti Roy
  • Patent number: 11420975
    Abstract: The present invention relates to a compound of formula I or a pharmaceutically acceptable salt, a solvate, an active metabolite, a polymorph, an ester, an optical isomer or a prodrug thereof, a pharmaceutical composition comprising the compound of formula I, and use of the compound, as a Bruton's tyrosine kinase inhibitor with high selectivity for BTK(C481S) mutant, in the manufacture of a medicament for preventing or treating a heteroimmune disease, an autoimmune disease or a cancer.
    Type: Grant
    Filed: January 13, 2022
    Date of Patent: August 23, 2022
    Assignee: TRANSTHERA SCIENCES (NANJING), INC.
    Inventor: Rongyao Chen
  • Patent number: 11413242
    Abstract: Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP?. Further disclosed are formulations to increase the efficacy of the compounds that activate Tie-2 and inhibit HPTP?.
    Type: Grant
    Filed: June 23, 2020
    Date of Patent: August 16, 2022
    Assignee: EYEPOINT PHARMACEUTICALS, INC.
    Inventor: Kevin Peters
  • Patent number: 11414432
    Abstract: The present invention relates to novel fused bicyclic heterocycle derivatives of formula (I) in which B1, B2, B3, B4, R1, R4, R5, R6 and n have the meanings mentioned above, to agrochemical formulations comprising the compounds of formula (I) and to their use as acaricides and/or insecticides for controlling animal pests, especially arthropods and in particular insects and arachnids.
    Type: Grant
    Filed: March 8, 2019
    Date of Patent: August 16, 2022
    Assignee: BAYER AKTIENGESELLSCHAFT
    Inventors: Dominik Hager, Ruediger Fischer, Laura Hoffmeister, Matthieu Willot, Kerstin Ilg, Ulrich Goergens
  • Patent number: 11401241
    Abstract: Compounds and methods for preventing and/or treating one or more symptoms of sickle cell diseases (SCD) by administering at least one of the compounds are provided. The compounds are based on vanillin which is chemically modified to increase bioavailability and activity, e.g. so that the compounds bind to the F helix of hemoglobin (Hb) and prevent adhesion of red blood cells (RBCs).
    Type: Grant
    Filed: March 18, 2019
    Date of Patent: August 2, 2022
    Assignees: VIRGINIA COMMONWEALTH UNIVERSITY, THE CHILDREN'S HOSPITAL OF PHILADELPHIA
    Inventors: Martin K. Safo, Yan Zhang, Piyusha Pradeep Pagare, Guoyan Xu, Mohini Ghatge, Jurgen Venitz, Osheiza Abdulmalik
  • Patent number: 11389667
    Abstract: A method of generating a strategy for performing a radiotherapy-based treatment and a system for performing the method. During a radiotherapy-based treatment, characteristics of side-effects are monitored and a risk model of the subject modified based on the characteristics. A new treatment strategy for the radiotherapy-based treatment is obtained based on the modified risk model.
    Type: Grant
    Filed: December 18, 2018
    Date of Patent: July 19, 2022
    Assignee: KONINKLIJKE PHILIPS N.V.
    Inventors: Pedro Jorge Da Silva Rodrigues, Alfonso Agatino Isola, Reinhold Wimberger-Friedl, Vanda Lucia de Carvalho Vittorino De Almeida
  • Patent number: 11376246
    Abstract: Methods of treating patients diagnosed with cancer harboring an IDH-1 mutation are provided, including the therapeutic administration of a certain inhibitor of a mutant IDH-1 as a single agent, or in combination with azacitidine (AZA).
    Type: Grant
    Filed: November 25, 2019
    Date of Patent: July 5, 2022
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Patrick F. Kelly, Alan Collis, Jeff Davis, Duncan Walker, Susan Ashwell, Blythe Thomson, Wei Lu
  • Patent number: 11376250
    Abstract: Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: December 1, 2020
    Date of Patent: July 5, 2022
    Assignee: Aptinyx Inc.
    Inventor: M. Amin Khan
  • Patent number: 11358967
    Abstract: The present invention encompasses compounds of the formula (I), wherein the variables are defined herein which are suitable for the modulation of ROR? and the treatment of diseases related to the modulation of ROR?. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
    Type: Grant
    Filed: January 18, 2017
    Date of Patent: June 14, 2022
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Delphine Collin, Johanna Csengery, Robert Owen Hughes, Michael Robert Turner, Lifen Wu
  • Patent number: 11358968
    Abstract: Described here are EET analogs conjugated to folate receptor ligands such as folic acid or folic acid analogs recognized by and selectively bound by folate receptors and other folate binding proteins and the use of such conjugated EET analogs for targeted delivery of therapeutic agents to folate-receptor bearing cell populations. More particularly, provided herein are EET analogs conjugated to folate receptor ligands and uses of such conjugated EET analogs as kidney targeted therapeutics.
    Type: Grant
    Filed: September 14, 2018
    Date of Patent: June 14, 2022
    Assignee: The Medical College of Wisconsin, Inc.
    Inventors: John D. Imig, John R. Falck, Abdul Hye Khan, Adeniyi Adebesin