Plural Hetero Atoms In The Bicyclo Ring System Patents (Class 514/300)
  • Patent number: 12029814
    Abstract: Compound formulations and methods for preventing or treating upper respiratory virus infections, such as influenza, respiratory syncytia virus (RSV), SARS, and SARS-COV-2, in human and animal species are disclosed. The compounds may exhibit antiviral, antimicrobial, anti-inflammatory, or cytoprotective activities. Liquid formulations comprising one or more compounds may be administered into the outer canal of the ear for delivery to the nasal and oral cavities, nasopharynx, posterior pharynx and laryngopharynx, the primary sites of upper respiratory infections, located across the tympanic membrane (or eardrum) and eustachian tube, of the individuals infected with one or more upper respiratory viruses or other pathogens. Methods to facilitate trans-tympanic membrane translocation of the compounds by thermal, electrical or electromagnetic impulse, manual or mechanical muscle contraction or stimulation of muscles, nerves or tissues proximate to the eardrum are disclosed.
    Type: Grant
    Filed: October 17, 2023
    Date of Patent: July 9, 2024
    Inventors: Subhash Dhawan, Yashi Dhawan
  • Patent number: 11998545
    Abstract: Provided herein are compounds of the Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E 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 RET-associated diseases and disorders.
    Type: Grant
    Filed: June 27, 2023
    Date of Patent: June 4, 2024
    Assignee: Array Biopharma Inc.
    Inventors: Steven W. Andrews, Sean Aronow, James F. Blake, Barbara J. Brandhuber, Adam Cook, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Elizabeth A. McFaddin, Megan L. McKenney, Oren T. McNulty, Andrew T. Metcalf, David A. Moreno, Tony P. Tang, Li Ren
  • Patent number: 11952378
    Abstract: Novel pyrrolo[2,3-c]isoquinoline-1,2-dione, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrrolo[2,3-c]isoquinoline-1,2-dione compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.
    Type: Grant
    Filed: December 14, 2023
    Date of Patent: April 9, 2024
    Assignee: KING FAISAL UNIVERSITY
    Inventors: Christophe Tratrat, Michelyne Haroun
  • Patent number: 11919898
    Abstract: A crystal form of an azaindole derivative and a preparation method thereof are disclosed.
    Type: Grant
    Filed: January 15, 2021
    Date of Patent: March 5, 2024
    Assignee: SHENZHEN LINGFANG BIOTECH CO., LTD.
    Inventors: Zhengxia Chen, Meibi Dai, Yang Zhang
  • Patent number: 11912723
    Abstract: Provided herein are KRAS modulating compounds, such as compounds of Formula (I), (II), (II*), (III) or pharmaceutically acceptable salts, solvates, stereoisomers, atom labelled, or tautomers of any of the foregoing, useful for modulating KRAS GD12 and/or other G12 mutants.
    Type: Grant
    Filed: July 31, 2023
    Date of Patent: February 27, 2024
    Assignee: QUANTA THERAPEUTICS, INC.
    Inventors: Hong Lin, Juan Luengo, Neil Johnson, Audrey Hospital
  • Patent number: 11897879
    Abstract: Provided is a compound that can have an effect of inhibiting MALT1 and is expected as useful as a prophylactic or therapeutic drug for cancer, etc. A compound represented by formula (I) [wherein each symbol is as defined in the description], a salt thereof, or a cocrystal, a hydrate or a solvate of the same.
    Type: Grant
    Filed: November 17, 2021
    Date of Patent: February 13, 2024
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Takaharu Hirayama, Yoshiteru Ito, Noriyuki Nii, Youichi Kawakita, Shinichi Imamura
  • Patent number: 11891390
    Abstract: Pyrrolo[2,3-c][2,7]naphthyridine-2-carboxylic acid compounds are provided. The pyrrolo[2,3-c][2,7]naphthyridine-2-carboxylic acid compounds have the general formula: where R1 is H, C1-C6 alkyl, or C3-C6 cycloalkyl, and R2 is C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 cyanoalkyl, (CH2)2-3NR3R4, (CH2)1-2aryl, (CH2)1-2heteroaryl, C(O)—(CH2)2-3NR3R4, C(O)aryl, C(O)heteroaryl, S(O)2—(CH2)2-3NR3R4, S(O)2aryl, S(O)2heteroaryl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C3-C6 cyanocycloalkyl, aryl, or 5- or 6-membered heteroaryl. The pyrrolo[2,3-c[2,7]naphthyridine-2-carboxylic acid compounds inhibit protein kinase CK2 activity and may be used as anticancer agents, as well as agents for treating inflammation, pain, immunological disorders, diabetes, viral infections, and neurodegenerative diseases.
    Type: Grant
    Filed: August 30, 2023
    Date of Patent: February 6, 2024
    Assignee: KING FAISAL UNIVERSITY
    Inventors: Michelyne Haroun, Christophe Tratrat
  • Patent number: 11840533
    Abstract: Described herein are pyridinone-based compounds, derivatives thereof, and pharmaceutical formulations thereof. In some aspects, the pyridinone-based compounds, derivatives thereof, and/or pharmaceutical formulations thereof can be administered to a subject in need thereof. In some aspects, pyridinone-based compounds, derivatives thereof, and/or pharmaceutical formulations thereof can modulate an activity and/or a function of a BRD protein and/or BET protein.
    Type: Grant
    Filed: May 16, 2022
    Date of Patent: December 12, 2023
    Assignee: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Gregory R. Thatcher, Rui Xiong, Jiong Zhao, Yangfeng Li
  • Patent number: 11827633
    Abstract: The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula (I), in which A, E, G, R1 to R6 and R10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: August 23, 2021
    Date of Patent: November 28, 2023
    Assignee: Sanofi
    Inventors: Dirk Gretzke, Olaf Ritzeler, Uwe Heinelt, Volkmar Wehner, Friedemann Schmidt
  • Patent number: 11820772
    Abstract: The present invention relates to polymorphs of the hydrochloride salt of 5-{2-[({8-[(2,6-dimethylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyridine-6-yl}carbonyl)-amino]ethoxy}-5-oxopentanoic acid (linaprazan glurate), more specifically Form 1 and Form 2 of the HCl salt of linaprazan glurate. The invention also relates to a process for the preparation of such polymorphs, to pharmaceutical compositions comprising such polymorphs, and to the use of these polymorphs in the treatment or prevention of gastrointestinal inflammatory diseases or gastric acid related diseases, in particular erosive gastroesophageal reflux disease (eGERD).
    Type: Grant
    Filed: April 3, 2023
    Date of Patent: November 21, 2023
    Assignee: Cinclus Pharma Holding AB (Publ)
    Inventors: Kjell Jarring, Thomas Larsson, Xingbang Lin, Dan Wang, Mikael Hillgren
  • Patent number: 11801237
    Abstract: Provided herein is an amorphous compound represented by Formula (I): and compositions thereof, which are useful in the treatment of disorders related to the activity of the c-KIT and PDGFR? kinases, and oncogenic forms thereof.
    Type: Grant
    Filed: May 9, 2023
    Date of Patent: October 31, 2023
    Assignee: Deciphera Pharmaceuticals, LLC
    Inventors: Michael D. Kaufman, Scott Bone, Corey Bloom, Fred Jordan
  • Patent number: 11802125
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: March 15, 2021
    Date of Patent: October 31, 2023
    Inventors: Joseph D. Panarese, Dexter Davis, Nathaniel Thomas Kenton, Samuel Bartlett, Yat Sun Or
  • Patent number: 11780852
    Abstract: Disclosed are methods for treating Crohn's disease using a compound of the formula: or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: February 10, 2021
    Date of Patent: October 10, 2023
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Ryan Hudson, Jennifer Kozak, Dante D. Podesto, Xiaojun Huang, Venkat R. Thalladi
  • Patent number: 11767319
    Abstract: The present disclosure relates generally to various forms and compositions of N-(5-(5-((1R,2S)-2-fluorocyclopropyl)-1,2,4-oxadiazol-3-yl)-2-methylphenyl)imidazo[1,2-a]pyridine-3-carboxamide useful as a selective inhibitor of c-kit kinase and uses of the same in the treatment of c-kit kinase associated diseases.
    Type: Grant
    Filed: July 15, 2021
    Date of Patent: September 26, 2023
    Assignee: Third Harmonic Bio, Inc.
    Inventors: Gregg F. Keaney, Leonard Walter Rozamus, Jr., Jonathan James Loughrey, Jaclyn Raeburn, Yuxiang Song
  • Patent number: 11760756
    Abstract: The present invention relates to crystalline forms of the PD-1/PD-L1 inhibitor (R)-1-((7-cyano-2-(3?-(3-(((R)-3-hydroxypyrrolidin-1-yl)methyl)-1,7-naphthyridin-8-ylamino)-2,2?-dimethylbiphenyl-3-yl)benzo[d]oxazol-5-yl)methyl)pyrrolidine-3-carboxylic acid, including methods of preparation thereof, and related synthetic intermediates, where the compound is useful in the treatment of various diseases including infectious diseases and cancer.
    Type: Grant
    Filed: November 5, 2021
    Date of Patent: September 19, 2023
    Assignee: Incyte Corporation
    Inventors: Zhongjiang Jia, Shili Chen, Mei Li, Pingli Liu, Yongchun Pan, Yongzhong Wu, Jiacheng Zhou
  • Patent number: 11744823
    Abstract: The present disclosure relates generally to pharmaceutical compositions of N-(5-(5-((1R,2S)-2-fluorocyclopropyl)-1,2,4-oxadiazol-3-yl)-2-methylphenyl)imidazo[1,2-a]pyridine-3-carboxamide useful as a selective inhibitor of c-kit kinase and uses of the same in the treatment of c-kit kinase associated diseases.
    Type: Grant
    Filed: November 19, 2021
    Date of Patent: September 5, 2023
    Assignee: Third Harmonic Bio, Inc.
    Inventors: Gregg F. Keaney, Elizabeth Kwong
  • Patent number: 11731986
    Abstract: Protein tyrosine phosphatases (PTPs) are key regulators of metabolism and insulin signaling. As a negative regulator of insulin signaling, the low molecular weight protein tyrosine phosphatase (LMPTP) is a target for insulin resistance and related conditions. Described herein are compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and compositions, and methods of using these compounds and compositions.
    Type: Grant
    Filed: June 8, 2021
    Date of Patent: August 22, 2023
    Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
    Inventors: Anthony B. Pinkerton, Robert J. Ardecky, Jiwen Zou
  • Patent number: 11691971
    Abstract: The present application provides naphthyridinone compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.
    Type: Grant
    Filed: June 17, 2021
    Date of Patent: July 4, 2023
    Assignee: Incyte Corporation
    Inventors: Stacey Shepard, Lixin Shao, Liangxing Wu, Wenqing Yao
  • Patent number: 11684616
    Abstract: This invention relates to compounds of general Formula I and pharmaceutically acceptable salts thereof, in which R1, R2, R3a, R3b, and R4 are as defined herein, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
    Type: Grant
    Filed: April 30, 2021
    Date of Patent: June 27, 2023
    Assignee: PFIZER INC.
    Inventors: Joyann Barber, Sujin Cho-Schultz, Matthew L. Del Bel, Rebecca Anne Gallego, Mingying He, Mehran Jalaie, Robert Steven Kania, Michele Ann McTigue, Sajiv Krishnan Nair, Anne-Marie Dechert Schmitt, Jamison Bryce Tuttle, Dahui Zhou, Ru Zhou
  • Patent number: 11584745
    Abstract: Disclosed are an aromatic heterocyclic compound, an intermediate thereof, a preparation method therefor, and a pharmaceutical composition and use thereof. The aromatic heterocyclic compound of the present invention is a new ALK5 inhibitor, and is used for treating and/or preventing various ALK5-mediated diseases.
    Type: Grant
    Filed: December 28, 2018
    Date of Patent: February 21, 2023
    Assignee: SHANGHAI YINGLI PHARMACEUTICAL CO., LTD
    Inventors: Zusheng Xu, Yangtong Lou, Li Chen, Kun Zeng, Qingrui Sun, Xiaoli Lei
  • Patent number: 11548892
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit transglutaminase 2 (TG2). Also described herein are methods for using such TG2 inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from TG2 inhibition.
    Type: Grant
    Filed: May 20, 2022
    Date of Patent: January 10, 2023
    Assignee: Sitari Pharma, Inc.
    Inventors: David Campbell, Justin Chapman, Thomas R. Diraimondo, Sergio G. Duron
  • Patent number: 11542261
    Abstract: Some embodiments of the invention include inventive compounds (e.g., compounds of Formula (I)) and compositions (e.g., pharmaceutical compositions) which can be used for treating, for example, certain diseases. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating (e.g., diseases such as head and neck squamous cell carcinoma (HNSCC), cancer, blood disorders, etc.). Additional embodiments provide synergistic combinations of a BCL2 inhibitor with an IRAK inhibiting compound, and methods of using same.
    Type: Grant
    Filed: February 28, 2020
    Date of Patent: January 3, 2023
    Assignees: CHILDREN'S HOSPITAL MEDICAL CENTER, THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPT. OF HEALTH AND HUMAN SERVICES
    Inventors: Daniel T. Starczynowski, Craig J. Thomas, Garrett Rhyasen, Katelyn Melgar, Morgan MacKenzie Walker, Jian-kang Jiang
  • Patent number: 11534431
    Abstract: Disclosed herein is a pharmaceutical combination for use in the prevention, delay of progression or treatment of cancer, wherein the pharmaceutical combination exhibits a synergistic efficacy. The pharmaceutical combination comprises a humanized antagonist monoclonal antibody against PD- and a RAF inhibitor. Also disclosed herein is a combination for use in the prevention, delay of progression or treatment of cancer in a subject, comprising administering to the subject a therapeutically effective amount of a humanized antagonist monoclonal antibody against PD-1 and a therapeutically effective amount of a RAF inhibitor.
    Type: Grant
    Filed: November 16, 2020
    Date of Patent: December 27, 2022
    Assignee: BEIGENE SWITZERLAND GMBH
    Inventors: Jing Song, Lai Wang, Kang Li, Tong Zhang, Lusong Luo, Min Wei, Zhiyu Tang, Guoliang Zhang, Changyou Zhou
  • Patent number: 11524031
    Abstract: The present invention concerns the use of a combination consisting of D-aspartic and L-aspartic acids or L-aspartic acid used alone to stimulate the procreative activity in the man by increment of spermatozoon number and motility.
    Type: Grant
    Filed: July 8, 2019
    Date of Patent: December 13, 2022
    Assignee: MERCK SERONO S.P.A.
    Inventors: Salvatore D'Aniello, Enrico D'Aniello
  • Patent number: 11472801
    Abstract: The present disclosure relates to solid forms of N-{[2?-(2,6-difluoro-3,5-dimethoxyphenyl)-3?-oxo-2?,3?-dihydro-1?H-spiro[cyclopropane-1,4?-[2,7]naphthyridin]-6?-yl]methyl}acrylamide, methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of the FGFR-associated or mediated diseases such as cancer.
    Type: Grant
    Filed: February 6, 2020
    Date of Patent: October 18, 2022
    Assignee: Incyte Corporation
    Inventors: Yongchun Pan, Chongsheng Eric Shi, Ming Tao, Wayne Han, Michael Xia, Dengjin Wang, Zhongjiang Jia, Jiacheng Zhou, Qun Li
  • Patent number: 11439628
    Abstract: The present invention relates to non-steriodal mineralocorticoid receptor (MR) and the pharmacology of mineralocorticoid receptor antagonists (MR Antagonists, MRAs). In particular, the invention relates to the use of MRAs alone and in combination preferably in combination with sGC stimulators and/or sGC activators for preparation of medicaments for the prevention and/or treatment of muscular or neuromuscular diseases, especially for the treatment of Duchenne Muscular Dystrophy (DMD).
    Type: Grant
    Filed: May 10, 2019
    Date of Patent: September 13, 2022
    Assignee: BAYER AKTIENGESELLSCHAFT
    Inventors: Peter Sandner, Peter Kolkhof, Ilka Mathar, Stefanie Breitenstein
  • Patent number: 11426412
    Abstract: Heterocyclic compounds of Formula (I), (II), and (III) are described herein along with their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof. The compounds described herein, their polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosis, cutaneous lupus erythematosis, ulcerative colitis, cancer, cystic fibrosis, asthma, multiple sclerosis and psoriasis.
    Type: Grant
    Filed: October 16, 2018
    Date of Patent: August 30, 2022
    Assignee: JUBILANT EPIPAD LLC
    Inventors: Gurulingappa Hallur, Athisayamani Jeyaraj Duraiswamy, Buchi Reddy Purra, N.V.S.K. Rao, Sridharan Rajagopal, Rajendra Kristam
  • Patent number: 11384085
    Abstract: Compounds useful in the modulation of ion channel activity in cells are disclosed herein. This disclosure also relates to use of these compounds in the treatment of pain, and pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Grant
    Filed: May 17, 2019
    Date of Patent: July 12, 2022
    Assignee: BIONOMICS LIMITED
    Inventors: Belinda Huff, Courtney Hollis, Hamish Toop, Nathan Kuchel, Lorna Helen Mitchell, Rajinder Singh
  • Patent number: 11376241
    Abstract: The present invention relates to compounds which can act as aryl hydrocarbon receptor (AhR) modulators and, in particular, as AhR antagonists. The invention further relates to the use of the compounds for the treatment and/or prophylaxis of diseases and/or conditions through binding of said aryl hydrocarbon receptor by said compounds.
    Type: Grant
    Filed: February 1, 2018
    Date of Patent: July 5, 2022
    Assignee: PHENEX PHARMACEUTICALS AG
    Inventors: Christoph Steeneck, Ulrich Deuschle, Michael Albers, Thomas Hoffmann
  • Patent number: 11377698
    Abstract: Provided herein, among other things, is a method of treating a cancer patient without the need for a tissue biopsy. In some embodiments, the method may comprise (a) performing or having performed a sequencing assay on cell-free DNA (cfDNA) from a sample of blood from the patient to determine if the cell-free DNA comprises actionable and/or non-actionable sequence variations in one or more target genes, and (b) treating the patient using the following method: i. administering a therapy that is targeted to an actionable sequence variation if the patient is identified as having the actionable sequence variation, and ii. administering a non-targeted therapy in the absence of any follow-up genetic testing on DNA extracted from a tissue biopsy if one or more non-actionable sequence variations and no actionable sequence variations are identified.
    Type: Grant
    Filed: September 4, 2019
    Date of Patent: July 5, 2022
    Assignee: INIVATA LTD.
    Inventors: Clive Morris, Vincent Plagnol, Tim Forshew
  • Patent number: 11370803
    Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
    Type: Grant
    Filed: September 17, 2020
    Date of Patent: June 28, 2022
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Nikolaos Papaioannou, Jeremy Mark Travins, Sarah Jocelyn Fink, John Mark Ellard, Alastair Rae
  • Patent number: 11351227
    Abstract: The present disclosure generally provides compositions and methods related to the field of immunology. Specifically, disclosed herein are chemokine binding proteins and methods of use thereof.
    Type: Grant
    Filed: April 27, 2018
    Date of Patent: June 7, 2022
    Assignee: Washington University
    Inventors: Daved Fremont, Olga Lubman, Andrew E. Gelman, Yun Hsuan Lu
  • Patent number: 11352355
    Abstract: Disclosed are chemical entities which are inhibitors of spleen tyrosine kinase (SYK), namely, chemical entities comprising 6-((1R,2S)-2-aminocyclohexylamino)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,4-c]pyridine-3(2H)-one and certain solid state forms thereof. Also disclosed are methods of using the chemical entities to treat disorders such as a cancer.
    Type: Grant
    Filed: May 8, 2020
    Date of Patent: June 7, 2022
    Assignee: Calithera Biosciences, Inc.
    Inventors: Rongliang Chen, Tomonori Ichibakase, Chunrong Ma, Christopher F. Matthews, Hajime Motoyoshi, Colin O'Bryan, Kentaro Yaji, Naoki Yoshikawa
  • Patent number: 11319318
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R9, X1 and X2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, e.g. cancer, pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Grant
    Filed: March 4, 2016
    Date of Patent: May 3, 2022
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Laetitia Martin, Steffen Steurer, Xiao-Ling Cockcroft
  • Patent number: 11306084
    Abstract: The present disclosure provides pharmaceutical agents, including those of the formula: (I) wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods of using the pharmaceutical agents are also provided. The compounds may be used for the inhibition or antagonism of integrins ???? and/or ?5??. In some embodiments, the compounds provided herein exhibit reduced inhibitory or antagonistic activity of integrins ???3, ???5, ???6, ???8, and/or ?IIb?3.
    Type: Grant
    Filed: December 28, 2017
    Date of Patent: April 19, 2022
    Assignees: Saint Louis University, Indalo Therapeutics, Inc.
    Inventors: Peter G. Ruminski, David W. Griggs, Scott Seiwert
  • Patent number: 11273150
    Abstract: The invention provides compositions and methods for the treatment of presbyopia. The methods preferably comprise storing an aceclidine composition in a container having a headspace at a temperature from about 2 to about 8 degrees Celsius. The methods further comprise filling the container under an inert gas overlay and/or enclosing the container an anti-leaching material or disposing the container in a second container containing an anti-leaching material.
    Type: Grant
    Filed: October 13, 2020
    Date of Patent: March 15, 2022
    Assignee: LENZ THERAPEUTICS, INC.
    Inventor: Gerald Horn
  • Patent number: 11273147
    Abstract: This invention provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
    Type: Grant
    Filed: August 30, 2019
    Date of Patent: March 15, 2022
    Assignee: University of Tennessee Research Foundation
    Inventors: Ramesh Narayanan, Duane D. Miller, Thamarai Ponnusamy, Dong-Jin Hwang, Yali He, Jayaprakash Pagadala, Christopher C. Coss, James T. Dalton, Charles B. Duke
  • Patent number: 11254667
    Abstract: Some embodiments of the invention include inventive compounds (e.g., compounds of Formula (I)). Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions (e.g., pharmaceutical compositions) for treating, for example, certain diseases using the inventive compounds. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating (e.g., diseases such as cancer or blood disorders). Further embodiments include methods for making the inventive compounds. Additional embodiments of the invention are also discussed herein.
    Type: Grant
    Filed: August 16, 2017
    Date of Patent: February 22, 2022
    Assignees: CHILDREN'S HOSPITAL MEDICAL CENTER, THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY, DEPT. OF HEALTH AND HUMAN SERVICES
    Inventors: Daniel T. Starczynowski, Craig J. Thomas, Garrett Rhyasen, Katelyn Melgar, Morgan MacKenzie Walker, Jian-kang Jiang
  • Patent number: 11242342
    Abstract: Isoquinoline amine compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
    Type: Grant
    Filed: November 8, 2017
    Date of Patent: February 8, 2022
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Andrew Felts
  • Patent number: 11180494
    Abstract: The invention relates to compounds of formula (I): or a salt thereof, wherein R1, G, L1, L2, L3, and Y are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are inhibitors of one, or both of, ?v?1 integrin and ?v?6 integrin that are useful for treating fibrosis such as in nonalcoholic steatohepatitis (NASH), idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
    Type: Grant
    Filed: October 8, 2019
    Date of Patent: November 23, 2021
    Assignee: Pliant Therapeutics, Inc.
    Inventors: Jacob Cha, Manuel Munoz, Maureen Reilly, Nicole Cooper, Katerina Leftheris, David J. Morgans, Jr., Timothy Hom, Yajun Zheng
  • Patent number: 11155546
    Abstract: The present disclosure relates to 4,6,7-trisubstituted 1,2-dihydropyrrolo[3,4-c]pyridin/pyrimidin-3-one derivatives, and their preparations and medicinal use. Specifically, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof, wherein the definition of each group is as described in the specification and claims.
    Type: Grant
    Filed: March 27, 2020
    Date of Patent: October 26, 2021
    Assignees: SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD., YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Shuchun Guo, Fusheng Zhou, Xiang Chen, Jinzhu Zhao, Dong Huang, Jing Xie, Changjiang Qiao, Wan He, Kai Zhang, Xi Chen, Jiong Lan
  • Patent number: 11130755
    Abstract: The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula (I), in which A, E, G, R1 to R6 and R10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: November 2, 2017
    Date of Patent: September 28, 2021
    Assignee: SANOFI
    Inventors: Dirk Gretzke, Olaf Ritzeler, Uwe Heinelt, Volkmar Wehner, Friedemann Schmidt
  • Patent number: 11110092
    Abstract: The present application relates to treatment of hematologic cancers, which treatments can include, e.g., administration of a purine nucleoside phosphorylase (PNP) inhibitor, an alkylating agent and/or an anti-CD20 agent, and related compositions and kits.
    Type: Grant
    Filed: May 1, 2019
    Date of Patent: September 7, 2021
    Assignee: BIOCRYST PHARMACEUTICALS, INC.
    Inventors: Shanta Bantia, Philip Breitfeld, Yarlagadda S Babu
  • Patent number: 11098043
    Abstract: This disclosure relates to compounds that are CBP inhibitor and methods of using such compounds in the treatment and diagnosis of diseases and disorders.
    Type: Grant
    Filed: July 13, 2018
    Date of Patent: August 24, 2021
    Assignee: University of Massachusetts
    Inventors: Wei Zhang, Alex Mugwiria Muthengi, Hailemichael O. Yosief
  • Patent number: 11083198
    Abstract: In crop production in the fields of agriculture, horticulture and the like, the damage caused by insect pests etc. is still immense, and insect pests resistant to existing insecticides have emerged. Under such circumstances, the development of novel agricultural and horticultural insecticides is desired. The present invention provides an agricultural and horticultural insecticide comprising a 4H-pyrrolopyridine compound represented by the general formula (1): {wherein R1 represents a halogen atom, R2 and R3 each represent a haloalkyl group, Q represents Q-A, Q-B or Q-C, X represents a nitrogen atom, R4 and R7 each represent a hydrogen atom, R2 and R3 each represent a halogen atom, a haloalkyl group or a substituted phenyl group, and m represents 2} or a salt thereof as an active ingredient; and a method for using the insecticide.
    Type: Grant
    Filed: December 26, 2017
    Date of Patent: August 10, 2021
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Ikki Yonemura, Yusuke Sano, Naoto Shimizu, Akihiro Miyasaka, Akiyuki Suwa, Shunpei Fujie, Ryosuke Tanaka
  • Patent number: 11072611
    Abstract: The present invention discloses compounds according to Formula I: Wherein R1a, R1b, R2, R4, R5, R6a, R6b, R8, W, X, Cy, and the subscript a are as defined herein. The present invention relates to compounds inhibiting autotaxin (NPP2 or ENPP2), methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, proliferative diseases, inflammatory diseases, autoimmune diseases, respiratory diseases, cardiovascular diseases, neurodegenerative diseases, dermatological disorders, and/or abnormal angiogenesis associated diseases by administering the compound of the invention.
    Type: Grant
    Filed: November 13, 2019
    Date of Patent: July 27, 2021
    Assignee: GALAPAGOS NV
    Inventors: Nicolas Desroy, Bertrand Heckmann, Reginald Christophe Xavier Brys, Agnès Marie Joncour, Christophe Peixoto, Xavier Marie Bock
  • Patent number: 11046669
    Abstract: Disclosed are small molecule inhibitors of ?v?6 integrin, and methods of using them to treat a number of diseases and conditions.
    Type: Grant
    Filed: June 26, 2019
    Date of Patent: June 29, 2021
    Assignee: Morphic Therapeutic, Inc.
    Inventors: Bryce A. Harrison, Matthew G. Bursavich, Mark Brewer, Aleksey I. Gerasyuto, Kristopher N. Hahn, Kyle D. Konze, Fu-Yang Lin, Blaise S. Lippa, Alexey A. Lugovskoy, Bruce N. Rogers, Mats A. Svensson, Dawn M. Troast
  • Patent number: 11040027
    Abstract: The invention relates to MKK4 (mitogen-activated protein kinase 4) and their use in promoting liver regeneration or reducing or preventing hepatocyte death. The MKK4 inhibitors selectively inhibit protein kinase MKK4 over protein kinases JNK and MKK7.
    Type: Grant
    Filed: January 17, 2018
    Date of Patent: June 22, 2021
    Assignee: Heparegenix GMBH
    Inventors: Wolfgang Albrecht, Stefan Laufer, Roland Selig, Phillip Klövekorn, Bent Präfke
  • Patent number: 11026954
    Abstract: The present invention provides the steroid compound 3beta-hydroxy-5alpha-pregnan-20-one for use in treatment of Tourette's syndrome, obsessive compulsive disorder and/or gambling disorder, as well as methods for treating said disorders and pharmaceutical compositions for use in treatment of said disorders.
    Type: Grant
    Filed: September 2, 2018
    Date of Patent: June 8, 2021
    Assignee: ASARINA PHARMA AB
    Inventor: Torbjörn Bäckström
  • Patent number: RE49575
    Abstract: The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and also the preparation and use of the crystalline polymorph I of (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I).
    Type: Grant
    Filed: August 25, 2020
    Date of Patent: July 11, 2023
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Johannes Platzek, Gunnar Garke, Alfons Grunenberg