1,4-diazine As One Of The Cyclos Patents (Class 514/249)
  • Patent number: 12023336
    Abstract: The present invention relates to compounds and pharmaceutical composition having antiviral effects. Over 1200 molecules were screened and 55 molecules having statistically significant anti-HIV activity were identified and selected. The compound Methotrexate (MTX-HYD) and its analogues, the combinations thereof and their combination with other anti-retrovirals were selected for repurposing the compounds as anti-HIV drugs. The present invention may further relate to pharmaceutical composition comprising compounds in combination with active drugs having anti-HIV activity.
    Type: Grant
    Filed: May 10, 2019
    Date of Patent: July 2, 2024
    Assignee: NATIONAL CENTRE FOR CELL SCIENCE
    Inventors: Debashis Mitra, Jay Trivedi
  • Patent number: 12023335
    Abstract: A method for treating pancreatic cancer in a subject in need thereof comprising, administering to the subject an effective amount of a tubulin polymerization inhibitor compound is described herein. More particularly, a method for treating pancreatic ductal adenocarcinoma in a subject in need thereof comprising, administering to the subject an effective amount of a substituted reverse pyrimidine tubulin polymerization inhibitor compound alone or in combination with other chemo-therapeutic agents is described herein.
    Type: Grant
    Filed: August 17, 2019
    Date of Patent: July 2, 2024
    Assignee: PTC THERAPEUTICS, INC.
    Inventors: Marla L. Weetall, Liangxian Cao, Thomas W. Davis, Melissa L. Dumble, Jaime A. Eberle-Singh, Kenneth P. Olive
  • Patent number: 12012394
    Abstract: The present invention generally relates to various compounds that are useful as ?-synuclein ligands. The invention further relates to methods of using these compounds and their radiolabeled analogs for the detection of synucleinopathies, including Parkinson's disease (PD).
    Type: Grant
    Filed: February 15, 2019
    Date of Patent: June 18, 2024
    Assignee: Washington University
    Inventors: Zhude Tu, Paul T. Kotzbauer, Xuyi Yue, Dhruva D. Dhavale
  • Patent number: 12012410
    Abstract: A prophylactic or therapeutic agent for spinal muscular atrophy according to the present invention includes a compound represented by the formula (I) or a salt thereof: the variables are described herein.
    Type: Grant
    Filed: June 27, 2019
    Date of Patent: June 18, 2024
    Assignee: REBORNA BIOSCIENCES, INC.
    Inventors: Koji Fuji, Takeshi Yamasaki, Shunya Suzuki, Koji Ono, Hiroki Takahagi
  • Patent number: 11974999
    Abstract: Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I):
    Type: Grant
    Filed: January 1, 2021
    Date of Patent: May 7, 2024
    Assignees: Suzhou Baijibugong Pharmaceutical Technology Co., Ltd.
    Inventors: Xibin Liao, Jia Li, Zhijian Lu, Yubo Zhou, Anhui Gao
  • Patent number: 11970498
    Abstract: The present disclosure provides a compound represented by structural Formula (I): or a pharmaceutically acceptable salt thereof useful for treating a cancer.
    Type: Grant
    Filed: February 8, 2023
    Date of Patent: April 30, 2024
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Douglas Wilson, Neil Bifulco, Jr., Natasja Brooijmans, Joseph L. Kim, Philip D. Ramsden, Richard Vargas, Steven Mark Wenglowsky
  • Patent number: 11969410
    Abstract: The present invention provides relatively low pH, stable, pharmaceutically acceptable and ophthalmologically suitable compositions comprising effective amounts of pilocarpine and brimonidine compounds for treating an ocular condition, wherein compositions demonstrate a significant difference in the amount or rate of one or more pharmaceutical ingredient(s) absorbed or retained by ocular tissue or compared to reference composition(s) with similar compositional characteristics but having a significantly higher pH. In aspects compositions are characterizable by other elements, e.g., the inclusion of benzalkonium chloride, a limited amount of sodium chloride, or both. In embodiments, compositions are free of both a borate and a citrate buffer. Compositions provided by the invention surprisingly demonstrate pharmaceutically acceptable stability when stored under controlled room temperature conditions for an extended period of time.
    Type: Grant
    Filed: February 9, 2023
    Date of Patent: April 30, 2024
    Assignee: Somerset Therapeutics, LLC
    Inventors: Mandar V. Shah, Ilango Subramanian, Veerappan Subramanian, Aman Trehan
  • Patent number: 11964989
    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: July 20, 2022
    Date of Patent: April 23, 2024
    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: 11964965
    Abstract: The present disclosure relates to synthesizing and utilizing fluorescent dye compounds or pharmaceutically acceptable salts thereof. Conjugation of amino acid groups to the fluorescent dyes increase specificity and detection of the compound. Methods of manufacture and synthesis of the compounds for use thereof in diagnostic imaging are contemplated.
    Type: Grant
    Filed: May 20, 2020
    Date of Patent: April 23, 2024
    Assignee: On Target Laboratories, LLC
    Inventors: Sumith A. Kularatne, Pravin Gagare
  • Patent number: 11963939
    Abstract: The present disclosure describes methods of treating a central nervous system condition associated with oxidative stress using a 5-lipoxigenase activating protein (FLAP) inhibitor, for example, N-acetylcysteine or nordihydroguaiaretic acid. The present disclosure also describes methods of treating a central nervous system condition with N-acetylcysteine and a second therapeutic agent such as prostaglandin E2.
    Type: Grant
    Filed: January 13, 2023
    Date of Patent: April 23, 2024
    Assignees: Neuronasal, Inc., Burke Neurological Institute
    Inventors: Rajiv R. Ratan, Saravanan Karuppagounder, Thomas I. Bradshaw
  • Patent number: 11963960
    Abstract: This invention relates to compounds for treating acute myeloid leukemia or inhibiting recurrence of acute myeloid leukemia and for inhibiting growth of and/or killing leukemic stem cells.
    Type: Grant
    Filed: March 15, 2021
    Date of Patent: April 23, 2024
    Assignee: Flash Therapeutics, LLC
    Inventors: Michael Serrano-Wu, Zhixiong Ye, Kejia Ding
  • Patent number: 11958840
    Abstract: The present disclosure relates generally to eukaryotic initiation factor 2B modulators, or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers, or prodrug thereof, and methods of making and using thereof.
    Type: Grant
    Filed: March 23, 2022
    Date of Patent: April 16, 2024
    Assignee: Denali Therapeutics Inc.
    Inventors: Robert A. Craig, II, Javier de Vicente Fidalgo, Anthony A. Estrada, Jianwen A. Feng, Brian M. Fox, Maksim Osipov, Arun Thottumkara
  • Patent number: 11951109
    Abstract: The present disclosure relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and one or more other therapeutic agents, particularly anticancer agents such as prednisone, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.
    Type: Grant
    Filed: November 15, 2021
    Date of Patent: April 9, 2024
    Assignee: Epizyme, Inc.
    Inventors: Heike Keilhack, Sarah Kathleen Knutson, Danielle Johnston Blackwell
  • Patent number: 11952381
    Abstract: Provided are compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2A, R2B, R3, R4, and R5 are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 4, 2022
    Date of Patent: April 9, 2024
    Assignee: CYTOKINETICS, INC.
    Inventors: Chihyuan Chuang, Bradley P. Morgan, Mark Vanderwal, Luke W. Ashcraft, Kevin Lau
  • Patent number: 11944622
    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: July 13, 2022
    Date of Patent: April 2, 2024
    Assignee: Annapurna Bio, Inc.
    Inventors: Haifeng Tang, Michael Hanson, Sarah Boyce, Zhe Nie
  • Patent number: 11938198
    Abstract: The present invention provides a method of treating heart failure with reduced ejection fraction, by administering to a patient at risk of such damage, a pharmaceutically effective amount of a composition which inhibits the anchoring of PP2A to mAKAP?. This composition is preferably in the form of a viral based gene therapy vector that encodes a fragment of mAKAP? to which PP2A binds.
    Type: Grant
    Filed: March 13, 2020
    Date of Patent: March 26, 2024
    Assignees: University of Miami, The Board of Trustees of the Leland Stanford Junior University
    Inventors: Michael S. Kapiloff, Jinliang Li
  • Patent number: 11932648
    Abstract: The present disclosure provides a compound represented by structural Formula (I): or a pharmaceutically acceptable salt thereof useful for treating a cancer.
    Type: Grant
    Filed: June 27, 2022
    Date of Patent: March 19, 2024
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Douglas Wilson, Neil Bifulco, Jr., Natasja Brooijmans, Joseph L. Kim, Emanuele Perola, Philip D. Ramsden, Richard Vargas, Steven Mark Wenglowsky
  • Patent number: 11908549
    Abstract: The invention relates to a computer-implemented Bayesian inference method for performing Bayesian inference in a Bayesian network, which includes a continuous child node (3) and its discrete parent node (2) having two states. Being provided with a calibrated continuous probability distribution of the observations of the child node (3) for each of the two states of the parent node (2), the inferring for a new observation of the child node (3) for which the state of the parent node (2) is not known of the probability of at least a first state of the parent node (2) makes use of masses of portions of the probability distributions that depend on a locational relationship of the probability distributions and the value of the new observation. This may ensure that the inferred probability of the first state of the parent node (2) monotonically changes with monotonically changing values of the new observation.
    Type: Grant
    Filed: September 21, 2018
    Date of Patent: February 20, 2024
    Assignee: KONINKLIJKE PHILIPS N.V.
    Inventors: Martijn Theodorus Lambert Akse, Wilhelmus Franciscus Johannes Verhaegh
  • Patent number: 11905511
    Abstract: A method of measuring immunocompetence is described. This method provides a means for assessing the effects of diseases or conditions that compromise the immune system and of therapies aimed to reconstitute it. This method is based on quantifying T-cell diversity by calculating the number of diverse T-cell receptor (TCR) beta chain variable regions from blood cells.
    Type: Grant
    Filed: June 29, 2018
    Date of Patent: February 20, 2024
    Assignee: Fred Hutchinson Cancer Center
    Inventors: Harlan S. Robins, Edus H. Warren, Christopher Scott Carlson
  • Patent number: 11905291
    Abstract: Disclosed herein are WD40 repeat domain protein 5 (WDR5) degradation/disruption compounds including a WDR5 ligand, a degradation/disruption tag, and a linker, and methods of using such compounds in the treatment of WDR5-mediated diseases.
    Type: Grant
    Filed: June 21, 2019
    Date of Patent: February 20, 2024
    Assignees: Icahn School of Medicine at Mount Sinai, The University of North Carolina at Chapel Hill
    Inventors: Jian Jin, Gang Wang, Jing Liu, Xufen Yu, Dongxu Li
  • Patent number: 11891405
    Abstract: The present application belongs to the field of pharmaceutical chemistry, and relates to a furo[3,4-b]pyrrole-containing BTK inhibitor, and in particular, to a compound of formula (I), a stereisomer or pharmacologically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition containing the compound, and use thereof in treating BTK-related diseases.
    Type: Grant
    Filed: September 12, 2019
    Date of Patent: February 6, 2024
    Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Yinsheng Zhang, Hongjiang Xu, Jing Ren, Qinglin Wang, Zheyang Wu, Chao Jin, Wei Shi, Xiaojin Wang, Xiangyi He, Xiayun Chang, Jie Wang, Tianxiao Zhao
  • Patent number: 11894116
    Abstract: An apparatus for extending longevity, wherein the apparatus includes at least a processor and a memory communicatively connected to the at least a processor. The memory containing instructions configuring at least a processor to receive a longevity measurement pertaining to a user. The memory containing instructions further configuring the processor to select a target longevity factor as a function of the longevity measurement and then identify a longevity treatment plan as a function of the target longevity factor. The memory containing instructions further configuring the processor to generate a longevity treatment protocol as a function of the longevity treatment and the longevity measurement.
    Type: Grant
    Filed: December 1, 2022
    Date of Patent: February 6, 2024
    Inventor: Jeffrey Gladden
  • Patent number: 11884683
    Abstract: The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, R3, R4, R5, R6 and n are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: May 31, 2019
    Date of Patent: January 30, 2024
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Tao Yu, Alan Whitehead, Yili Chen, Chunrui Sun, Zhiyong Hu, Kake Zhao, Ronald M. Kim, John A. McCauley
  • Patent number: 11883400
    Abstract: Methods and formulations are provided for the treatment and prevention of portal hypertension.
    Type: Grant
    Filed: October 21, 2019
    Date of Patent: January 30, 2024
    Assignee: Noorik Biopharmaceuticals AG
    Inventor: Iker Navarro
  • Patent number: 11883491
    Abstract: Methods and compositions using an inhibitor of EGFR signaling for prevention or an inhibitor of EGFR signaling and a nucleic acid molecule encoding an atonal-associated factor for treatment of hearing loss are described.
    Type: Grant
    Filed: April 30, 2018
    Date of Patent: January 30, 2024
    Assignee: St. Jude Children's Research Hospital, Inc.
    Inventors: Jian Zuo, Fei Zheng, Tetsuji Yamashita, Zoe Kellard, Tal Teitz, Jaeki Min, Taosheng Chen
  • Patent number: 11872234
    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 10, 2023
    Date of Patent: January 16, 2024
    Assignee: Par Pharmaceutical, Inc.
    Inventors: Joseph Prabahar Koilpillai, Sayuj Nath, Satish Patil, Somasundaram Muthuramalingam, Selvakumar Viruthagiri, Mohankumar Lakshmanan
  • Patent number: 11857539
    Abstract: The present invention provides, stable, pharmaceutically acceptable and ophthalmologically suitable gel compositions comprising therapeutically effective amounts of both a pilocarpine compound and a brimonidine compound and effective amount(s) of at least one polyethoxylated castor oil, which in aspects is/are present in a defined ratio with one or more active pharmaceutical ingredients. In aspects, such compositions are formulated as gel compositions. In certain embodiments, provided compositions are free of both a borate buffer and a citrate buffer. Compositions provided by the invention demonstrate stability, e.g., pH and active pharmaceutical ingredient stability, when stored under controlled room temperature conditions for an extended period of time. Further, the invention provides methods of manufacturing such compositions and methods of their use in treating ocular conditions, such as presbyopia.
    Type: Grant
    Filed: February 9, 2023
    Date of Patent: January 2, 2024
    Assignee: Somerset Therapeutics, LLC
    Inventors: Mandar V. Shah, Ilango Subramanian, Veerappan Subramanian, Aman Trehan
  • Patent number: 11858939
    Abstract: This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula I, II or any of Compounds 100-128 or any of those in Tables 2 or 3) accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or impairment.
    Type: Grant
    Filed: December 28, 2020
    Date of Patent: January 2, 2024
    Assignee: Alkermes, Inc.
    Inventors: Martin R. Jefson, John A. Lowe, III, Fabian Dey, Andreas Bergmann, Andreas Schoop, Nathan Oliver Fuller
  • Patent number: 11851434
    Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.
    Type: Grant
    Filed: October 29, 2021
    Date of Patent: December 26, 2023
    Assignee: Array BioPharma Inc.
    Inventors: Steven W. Andrews, James F. Blake, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, David A. Moreno, Li Ren, Shane M. Walls
  • Patent number: 11850249
    Abstract: Disclosed herein are pharmacologically acceptable and ophthalmologically suitable compositions and methods of their use in treating ophthalmic diseases or related conditions. In aspects, the invention provides compositions comprising effective amounts of carbonic anhydrase inhibitor(s) and alpha-2-adrenergic agonist(s). In facets, compositions comprise a penetration enhancer component comprising one or more penetration enhancer compound(s)/molecule(s). In aspects, the invention provides compositions comprising effective amounts of brimonidine compound(s) and brinzolamide compound(s) capable of being administered once or twice daily for the treatment of elevated intraocular pressure, but which provide similar efficacy to a similar or substantially identical reference product requiring administration three times per day.
    Type: Grant
    Filed: October 5, 2021
    Date of Patent: December 26, 2023
    Assignee: Somerset Therapeutics, LLC
    Inventors: Mandar V. Shah, Ilango Subramanian, Veerappan Subramanian, Aman Trehan
  • Patent number: 11844792
    Abstract: A method is provided for identifying a patient having a respiratory illness and administering to the patient a combination of an anti-inflammatory agent and a leukotriene inhibitor. The method may include treating respiratory illness associated with a coronavirus, and may it may further include reducing or preventing an inflammatory response or cytokine storm for those patients without impairing their immune response against the underlying pathogen.
    Type: Grant
    Filed: July 9, 2021
    Date of Patent: December 19, 2023
    Inventor: Sean Downing
  • Patent number: 11845752
    Abstract: Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 13, 2021
    Date of Patent: December 19, 2023
    Assignee: Aligos Therapeutics, Inc.
    Inventors: Sandrine Vendeville, Yannick Debing, Antitsa Dimitrova Stoycheva, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 11833142
    Abstract: The present disclosure provides a compound of Formula (I?): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein Ra, Rb, Rx, R1, R2, X2, and q are as defined herein, and methods of making and using same.
    Type: Grant
    Filed: October 4, 2021
    Date of Patent: December 5, 2023
    Assignee: Novartis AG
    Inventors: Rohan Eric John Beckwith, Simone Bonazzi, Artiom Cernijenko, Fupeng Ma, Nathaniel F. Ware
  • Patent number: 11833137
    Abstract: The present invention includes substituted chromenones that are useful to inhibit the IRE1/XBP-1 pathway. In certain embodiments, the compounds of the invention inhibit IRE1's RNase activity. In other embodiments, the compounds of the invention are useful to treat or prevent a cancer that involve activation of the ER stress response. The invention also relates, in certain aspects, to the discovery that secretory IgM (sIgM) can orchestrate an immunosuppressive microenvironment by recruiting myeloid-derived suppressor cells (MDSCs) into different tumor models, such as but not limited to solid tumors (such as but not limited to lung cancer) and tumors that have high levels of secreted IgM. In certain embodiments, sIgM produced by B cells or CLL cells can contribute to the accumulation of MDSCs in a tumor. In other embodiments, inhibition of the IRE1/XBP-1 pathway can ablate, minimize, or reduce MDSC levels in a tumor.
    Type: Grant
    Filed: April 1, 2019
    Date of Patent: December 5, 2023
    Assignees: The Wistar Institute, University of South Florida
    Inventors: Chih-Chi Andrew Hu, Juan R. Del Valle
  • Patent number: 11834424
    Abstract: Compounds and pharmaceutically acceptable salts thereof of Formula I are disclosed. Certain compounds and salts of Formula I are active as CMA modulators. The disclosure provides pharmaceutical compositions containing a compound of Formula I.
    Type: Grant
    Filed: August 30, 2018
    Date of Patent: December 5, 2023
    Assignee: ALBERT EINSTEIN COLLEGE OF MEDICINE
    Inventors: Ana Maria Cuervo, Evripidis Gavathiotis
  • Patent number: 11826429
    Abstract: A sterile aqueous formulation of a carbonic anhydrase inhibitor such as brinzolamide in combination with polymers like Soluplus® and a surfactant like polysorbate 80, as well as methods of preparation thereof, is disclosed. The formulation relates to the highly solubilized or an amorphous form of poorly insoluble drugs/active ingredient(s) to improve its bio-availability and manufacturability.
    Type: Grant
    Filed: March 6, 2020
    Date of Patent: November 28, 2023
    Assignee: SENTISS PHARMA PRIVATE LIMITED
    Inventors: Mandar V. Shah, Deepak Bahri
  • Patent number: 11826336
    Abstract: This disclosure relates to nutritional formulas and uses for treating or preventing a gastrointestinal condition and/or motor-planning speech and/or coordinator difficulties. In certain embodiments, this disclosure relates to a nutritional formula comprising medium chain fatty acids, or esters thereof (such as and tri-, di-, mono-glycerides, or alkyl esters), unsaturated fatty acids, and a vitamin E and optionally other nutrients. In certain embodiments, any of the compounds or nutrients may be in alternative salt forms.
    Type: Grant
    Filed: June 1, 2021
    Date of Patent: November 28, 2023
    Assignees: Emory University, Children's Healthcare of Atlanta, Inc.
    Inventor: Claudia R. Morris
  • Patent number: 11820777
    Abstract: In some embodiments, the invention relates to crystalline solid forms, including hydrates, polymorphs, and salt forms, of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention relates to amorphous solid forms of (S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide. In some embodiments, the invention also relates to pharmaceutical compositions containing the solid forms, and methods for treating conditions or disorders by administering to a subject a pharmaceutical composition that includes the forms, including pharmaceutical compositions and methods for overcoming the effects of acid reducing agents.
    Type: Grant
    Filed: January 27, 2022
    Date of Patent: November 21, 2023
    Assignee: Acerta Pharma B.V.
    Inventors: Fritz Blatter, Tim Ingallinera, Tjeerd Barf, Edwin Aret, Cecile Krejsa, Jerry Evarts
  • Patent number: 11804301
    Abstract: Embodiments in accordance with the present disclosure are directed to systems and methods for managing hot flashes and/or menopause symptoms. An example system includes sensor circuitry and logic circuitry. The sensor circuitry obtains a physical measurement associated with a user and communicates the physical measurement. The logic circuitry generates a predictive model that indicates a probability of the user having a hot flash at a date and time based on a plurality of input parameters, revises the probability based on the physical measurement using the predictive model, and communicates data indicative of an action in response to the revised probability being outside a threshold, such as providing cooling relief.
    Type: Grant
    Filed: July 3, 2019
    Date of Patent: October 31, 2023
    Assignee: SRI International
    Inventors: Massimiliano de Zambotti, Fiona C. Baker, Mohamad Forouzanfar, Bhaskar Ramamurthy, Laurie Menoud
  • Patent number: 11795216
    Abstract: The invention relates to neutralizing antibodies of GM-CSF and compositions comprising the same for use in the treatment of inflammatory disorders such as rheumatoid arthritis according to specific dosing regimen. The invention relates also to neutralizing antibodies of GM-CSF and compositions comprising the same for use in the treatment of pain, e.g. pain experienced in inflammatory disorders such as rheumatoid arthritis, according to specific dosage regimen.
    Type: Grant
    Filed: August 17, 2020
    Date of Patent: October 24, 2023
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Thomas Wagner, Malin Carlsson, Margit Staum Kaltoft
  • Patent number: 11798300
    Abstract: A microscopic object characterization system comprises a computer system, a microscope with a computing unit connected to the computer system, and an object characterization program executable in the computer system configured to receive refractive index data representing at least a spatial distribution of measured values of refractive index (RI) or values correlated to refractive index of the microscopic object. The object characterization program is operable to execute an algorithm applying a plurality of transformations on the refractive index data. The transformations generate a distribution of two or more parameters used to characterize features of the microscopic object.
    Type: Grant
    Filed: April 16, 2021
    Date of Patent: October 24, 2023
    Assignee: NANOLIVE SA
    Inventors: Yann Cotte, Sebastien Equis, Bastian Dalla Piazza, Sorin Pop, Luca Clario, Christopher Tremblay, Pierre-Alain Cotte
  • Patent number: 11787808
    Abstract: The invention relates to crystalline folate salts. The salt consists of a folate anion and an organic cation. The folate anion is 5-methyl-(6S)-tetrahydrofolic acid, and the cation is an organic compound which is an alkanolamine selected from the group consisting of choline, N-methylaminoethanol, 2-amino-2-methylpropanol and 2-dimethylaminoethanol.
    Type: Grant
    Filed: October 31, 2019
    Date of Patent: October 17, 2023
    Assignee: APROFOL AG
    Inventors: Martin Ulmann, Gerd Wiesler, Arthur Bodenmüller, Markus Müller
  • Patent number: 11786538
    Abstract: The present invention relates to ophthalmic compositions comprising from 0.005% to 0.02% bimatoprost by weight, less than 100 ppm benzalkonium chloride, and a secondary penetration enhancer that detectably enhances penetration of bimatoprost into a mammalian eye such that elevated intraocular pressure is effectively reduced to an extent statistically comparable to compositions comprising higher amounts of bimatoprost and benzalkonium chloride. Further, the invention also provides a process of preparing such compositions and methods of their use for lowering intraocular pressure and treating glaucoma.
    Type: Grant
    Filed: December 8, 2020
    Date of Patent: October 17, 2023
    Assignee: Somerset Therapeutics, LLC
    Inventors: Mandar V. Shah, Veerappan Subramanian, Ilango Subramanian, Aman Trehan
  • Patent number: 11767325
    Abstract: The present invention is directed to, in part, fused heteroaryl compounds of Formula (II-II): and compositions thereof, 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 neurological disorders (e.g., Dravet syndrome, epilepsy), pain, and neuromuscular disorders are also provided herein.
    Type: Grant
    Filed: November 25, 2020
    Date of Patent: September 26, 2023
    Assignee: PRAXIS PRECISION MEDICINES, INC.
    Inventors: Kiran Reddy, Gabriel Martinez Botella, Andrew Mark Griffin, Brian Edward Marron, Carlos Loya
  • Patent number: 11760733
    Abstract: Compositions comprising small molecule mitofusin agonists are described. The mitofusin modulating agents are useful for treating diseases or disorders associated with a mitochondria-associated disease, disorder, or condition such as diseases or disorders associated with mitofusin 1 (Mfn1) and/or mitofusin 2 (Mfn2), or mitochondrial dysfunction. Methods of treatment, pharmaceutical formulations, and screening methods for identifying compounds that regulate mitochondrial function are also described.
    Type: Grant
    Filed: April 20, 2018
    Date of Patent: September 19, 2023
    Assignee: Washington University
    Inventor: Gerald W. Dorn, II
  • Patent number: 11753409
    Abstract: The present invention is related to crystalline salts of N-(3-(5-((1-ethylpiperidin-4-yl)(methyl)amino)-3-(pyrimidin-5-yl)-1H-pyrrolo[3,2-b]pyridin-1-yl)-2,4-difluorophenyl)propane-1-sulfonamide, a RAF kinase Inhibitor, useful in the treatment of cancer and other diseases.
    Type: Grant
    Filed: March 11, 2022
    Date of Patent: September 12, 2023
    Assignee: Xynomic Pharmaceuticals, Inc.
    Inventors: Ulrike Werthmann, Gerd-Michael Maier, Bodo Betzemeier, Otmar Schaaf
  • Patent number: 11752154
    Abstract: The present invention features pharmaceutical compositions including sepiapterin, or a pharmaceutically acceptable salt and/or co-crystal thereof, and methods for the treatment of tetrahydrobiopterin-related disorders (e.g., tetrahydrobiopterin deficiency or phenylketonuria) with such compositions.
    Type: Grant
    Filed: October 31, 2019
    Date of Patent: September 12, 2023
    Assignee: PTC Therapeutics MP, Inc.
    Inventor: Daniel E. Levy
  • Patent number: 11739093
    Abstract: The present disclosure is directed to compounds of Formula IV: as inhibitors of SHP2 and their use in the treatment of diseases associated with SHP2. Also disclosed are pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: July 22, 2019
    Date of Patent: August 29, 2023
    Assignee: REVOLUTION MEDICINES, INC.
    Inventors: Brian R. Blank, Jennifer Pitzen, Gang Wang, Walter S. Won, Christos Tzitzilonis, Jie Jack Li, Elena S. Koltun, Naing Aay, Andreas Buckl, Kevin Mellem, Christopher Semko, Ash Jogalekar, Gert Kiss, Adrian Gill
  • Patent number: 11717522
    Abstract: The present invention relates to a method for preparing a lyophilized solid pharmaceutical composition comprising a) a compound having the formula (I): and/or a compound having the formula (II): ?and b) two different sodium phosphate salts, wherein the two different sodium phosphate salts are NaH2PO4·2H2O and Na2HPO4·2H2O, and wherein the quantity of the NaH2PO4·2H2O and Na2HPO4·2H2O present in the composition is chosen such that the molar ratio of both NaH2PO4·2H2O and Na2HPO4·2H2O to compound (I) or compound (II) ranges from 0.02 to 0.5.
    Type: Grant
    Filed: January 20, 2021
    Date of Patent: August 8, 2023
    Assignee: VASOPHARM GMBH
    Inventors: Peter Scheurer, Frank Tegtmeier, Reinhard Schinzel
  • Patent number: 11707463
    Abstract: Disclosed herein are methods of treating cholangiocarcinoma in a patient comprising: evaluating a biological sample from the patient for the presence of one or more FGFR mutants including at least the FGFR2 SNP C383R; and treating the patient with an FGFR inhibitor if one or more FGFR mutants including at least the FGFR2 SNP C383R are present in the sample.
    Type: Grant
    Filed: June 1, 2018
    Date of Patent: July 25, 2023
    Assignee: Janssen Pharmaceutica NV
    Inventor: Jacqueline Cirillo Bussolari