Exactly Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/303)
  • Patent number: 12122773
    Abstract: Provided herein is a crystalline hydrate of the compound of formula 1: Also provides herein are pharmaceutical compositions comprising such crystalline hydrate, methods of using such crystalline hydrate to treat respiratory diseases, and processes useful for preparing such crystalline hydrate.
    Type: Grant
    Filed: May 31, 2023
    Date of Patent: October 22, 2024
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventor: Gene Timothy Fass
  • Patent number: 12110290
    Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.
    Type: Grant
    Filed: July 6, 2023
    Date of Patent: October 8, 2024
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guanglin Luo, Jie Chen, Carolyn Diane Dzierba, David B. Frennesson, Junqing Guo, Amy C. Hart, Xirui Hu, Michael E. Mertzman, Matthew Reiser Patton, Jianliang Shi, Steven H. Spergel, Brian Lee Venables, Yong-Jin Wu, Zili Xiao, Michael G. Yang
  • Patent number: 12103925
    Abstract: The present application provides a crystalline form of tolebrutinib, an amorphous form, and a method of preparation thereof and a use thereof, and the crystalline form of tolebrutinib provided in the present application has at least one of the following advantages: good stability, low moisture attraction, uniform particle size distribution, solubility meeting the requirements for medicinal use, stable storage, avoiding phase transformation of the drug in the process of development and in storage, and a reliable method for the preparation thereof, which has a great development value. The amorphous form of tolebrutinib provided in this application, while possessing better solubility than that of tolebrutinib in the crystalline state, still possesses good stability of placement and acceptable hygroscopicity, and has high medicinal value.
    Type: Grant
    Filed: September 27, 2023
    Date of Patent: October 1, 2024
    Assignee: HANGZHOU SOLIPHARMA CO., LTD.
    Inventors: Xiaohong Sheng, Xiaoxia Sheng, Yu Dai
  • Patent number: 12024522
    Abstract: The present application provides processes for preparing (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, which is useful as an inhibitor phosphoinositide 3-kinase-delta (PI3K?), as well as a salt form and intermediates related thereto.
    Type: Grant
    Filed: July 1, 2021
    Date of Patent: July 2, 2024
    Assignees: Incyte Corporation, Incyte Holdings Corporation
    Inventors: Lei Qiao, Lingkai Weng, Chongsheng Eric Shi, David Meloni, Qiyan Lin, Michael Xia, Vaqar Sharief, William Frietze, Zhongjiang Jia, Yongchun Pan, Pingli Liu, Tai-Yuen Yue, Jiacheng Zhou, Jianji Wang
  • Patent number: 12018016
    Abstract: Compounds of formula (A) are provided which are useful in the treatment of diseases or conditions modulated at least in part by CCR6:
    Type: Grant
    Filed: August 17, 2022
    Date of Patent: June 25, 2024
    Assignee: AMGEN INC.
    Inventors: Penglie Zhang, Daniel R. Marshall, Howard S. Roth, Aubrie Harland, Ju Yang, Christopher W. Lange, Rebecca M. Lui, Antoni Krasinski
  • Patent number: 12012401
    Abstract: Provided herein is a synthetic process for preparing a compound of Formula (1). The disclosure also provides useful intermediates and salts, amorphous and polymorph forms of the compound of Formula (1). These compounds are useful for various disease including cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, and osteoarthritis as well as Wnt-related diseases.
    Type: Grant
    Filed: March 18, 2021
    Date of Patent: June 18, 2024
    Assignee: BioSplice Therapeutics, Inc.
    Inventor: Sunil Kumar KC
  • Patent number: 11976064
    Abstract: The present invention relates to imidazo-pyridinyl compounds, or a pharmaceutically acceptable salt thereof, 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, in a subject.
    Type: Grant
    Filed: May 6, 2022
    Date of Patent: May 7, 2024
    Assignee: Pfizer Inc.
    Inventors: Omar Ahmad, Andrew Fensome, Erik Alphie LaChapelle, Ethan Lawrence Fisher, Rayomand J. Unwalla, Jun Xiao, Lei Zhang
  • Patent number: 11969412
    Abstract: The invention provides a p38 MAPK inhibitor of Formula I, or a pharmaceutically acceptable salt or solvate thereof: for use in the treatment or prevention of hypercytokinemia in a human patient; wherein R is C1-3alkyl, optionally substituted by one or more halo, NR1R2 or hydroxy, and R1and R2 are independently H, halo or C1-3alkyl, optionally substituted by one or more F. Also provided are compositions for use in the treatment or prevention of hypercytokinemia comprising the p38 MAPK inhibitor of Formula I; and methods for treating or preventing hypercytokinemia in a human patient in need thereof comprising administering to the patient a therapeutically or prophylactically effective amount of a p38 MAPK inhibitor of Formula I. The invention also provides a p38 MAPK inhibitor and an antimicrobial agent, such as an antiviral agent, for use in the treatment or prevention of hypercytokinemia.
    Type: Grant
    Filed: September 23, 2022
    Date of Patent: April 30, 2024
    Assignee: Poolbeg Pharma (UK) Limited
    Inventors: Adrian Huw Davies, Pui-Man Choy, Vinay Saunders, Basma Bahsoun, Surender Vashist, Neil Edward Torbett, Paul Andrew Whittaker
  • Patent number: 11926626
    Abstract: This disclosure relates to GLP-1 agonists of Formula (I), including pharmaceutically acceptable salts and solvates thereof, and pharmaceutical compositions including the same.
    Type: Grant
    Filed: September 21, 2022
    Date of Patent: March 12, 2024
    Assignee: Gasherbrum Bio, Inc.
    Inventors: Qinghua Meng, Weiqiang Xing, Haizhen Zhang, Xichen Lin, Hui Lei, Andrew Jennings
  • Patent number: 11925624
    Abstract: The present disclosure relates to methods of administering Compound I for treating fibrotic disorders, inflammatory disorders or autoimmune disorders.
    Type: Grant
    Filed: November 17, 2021
    Date of Patent: March 12, 2024
    Assignee: GENENTECH, INC.
    Inventors: Lin Pan, Dorothy Sze-Wing Cheung, Jeffrey Mark Harris, Indiana Strombom
  • Patent number: 11925631
    Abstract: The present disclosure relates generally to certain 6-azabenzimidazole compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.
    Type: Grant
    Filed: May 27, 2021
    Date of Patent: March 12, 2024
    Assignee: Gilead Sciences, Inc.
    Inventors: Gayatri Balan, Mark J. Bartlett, Jayaraman Chandrasekhar, Julian A. Codelli, John H. Conway, Jennifer L. Cosman, Rao V. Kalla, Musong Kim, Seung H. Lee, Jennifer R. Lo, Jennifer A. Loyer-Drew, Scott A. Mitchell, Thao D. Perry, Gary B. Phillips, Patrick J. Salvo, Joshua J. Van Veldhuizen, Suet C. Yeung, Jeff Zablocki
  • Patent number: 11866422
    Abstract: This invention is directed to novel carbocyclic prolinamide derivatives of Formula (I), and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of age-related macular degeneration (AMD) and related diseases of the eye. These diseases include dry-AMD, wet-AMD, geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells. The invention disclosed herein is further directed to methods of prevention, slowing the progress of, and treatment of dry-AMD, wet-AMD, and geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or photoreceptor cells, comprising: administration of a therapeutically effective amount of compound of the invention.
    Type: Grant
    Filed: July 14, 2021
    Date of Patent: January 9, 2024
    Assignee: Orion Ophthalmology LLC
    Inventors: Robert Gomez, Jinyue Ding, Renata Marcella Oballa, David Andrew Powell
  • Patent number: 11851429
    Abstract: This disclosure is directed, at least in part, to AMPK activators useful for the treatment of conditions or disorders associated with AMPK. In some embodiments, the condition or disorder is associated with the gut-brain axis. In some embodiments, condition or disorder is associated with systemic infection and inflammation from having a leaky gut barrier. In some embodiments, the AMPK activators are gut-restricted compounds. In some embodiments, the AMPK activators are agonists or partial agonists.
    Type: Grant
    Filed: January 26, 2022
    Date of Patent: December 26, 2023
    Assignee: KALLYOPE, INC.
    Inventors: Iyassu Sebhat, Shuwen He, Ann Weber, Nancy Thornberry, Lisa Krug, Paul Richards, Brett Lauring
  • Patent number: 11833138
    Abstract: Certain embodiments of the present disclosure provide liquid pharmaceutical formulations, suitable for oral administration, that contain glycerol and an amount of apixaban in the solution phase of the formulations of from 0.5 mg/ml to 6 mg/ml.
    Type: Grant
    Filed: January 30, 2023
    Date of Patent: December 5, 2023
    Assignee: TaP Pharmaceuticals AG
    Inventors: Nilesh Parikh, William Hite
  • Patent number: 11767322
    Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.
    Type: Grant
    Filed: October 18, 2021
    Date of Patent: September 26, 2023
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guanglin Luo, Jie Chen, Carolyn Diane Dzierba, David B. Frennesson, Junqing Guo, Amy C. Hart, Xirui Hu, Michael C. Mertzman, Matthew Reiser Patton, Jianliang Shi, Steven H. Spergel, Brian Lee Venables, Yong-Jin Wu, Zili Xiao, Michael G. Yang
  • Patent number: 11739090
    Abstract: Disclosed are a class of BTK kinase inhibitor compounds with a high activity and a high selectivity and the use thereof in the preparation of a drug for treating BTK target-related diseases. Specifically, disclosed are a compound shown as formula (I), and an isomer and a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 25, 2020
    Date of Patent: August 29, 2023
    Assignee: JUMBO DRUG BANK CO., LTD.
    Inventors: Chunli Shen, XiaWei Wei, Chengde Wu, Guoping Hu, Ning Jiang, Wei Zheng, Jian Li, Shuhui Chen
  • Patent number: 11702415
    Abstract: Provided herein is a crystalline hydrate of the compound of formula 1: Also provides herein are pharmaceutical compositions comprising such crystalline hydrate, methods of using such crystalline hydrate to treat respiratory diseases, and processes useful for preparing such crystalline hydrate.
    Type: Grant
    Filed: March 1, 2021
    Date of Patent: July 18, 2023
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventor: Gene Timothy Fass
  • Patent number: 11647748
    Abstract: The present invention provides novel sulphonamide inhibitors of cystathionin gamma synthase (CGS), their use as selective and non-selective herbicides, agricultural and non-agricultural herbicides, herbicides in integrated pest management, herbicides for gardening, clearing waste ground, clearing industrial or constructions sites, clearing railways and railway embankments, pesticide, fungicide, agricultural plant stimulant or antimicrobial agent. Also provided is a method for the control of undesired vegetation or clearing areas from the undesired vegetation comprising applying to the locus of said undesired vegetation, to the undesired plants or to a habitat thereof, a herbicidally effective amount of the compound of the present invention.
    Type: Grant
    Filed: July 1, 2020
    Date of Patent: May 16, 2023
    Assignee: MIGAL—GALILEE RESEARCH INSTITUTE LTD.
    Inventors: Itai Bloch, Elad Cohen, Rachel Amir, Maayan Gal
  • Patent number: 11607405
    Abstract: The invention provides methods for treating triple negative breast cancer (TNBC), by co-administration of a BET bromodomain inhibitor selected from 1-benzyl-6-(3,5-dimethylisoxazol-4-yl)-N-methyl-1H-imidazo[4,5-b]pyridin-2-amine (Compound I), 1-benzyl-6-(3,5-dimethylisoxazol-4-yl)-1H-imidazo[4,5-b]pyridin-2-amine, and pharmaceutically acceptable salts/co-crystals thereof, and a second therapeutic agent to a subject in need thereof. The second therapeutic agent can be a PARP inhibitor, such as, e.g., talazoparib, olaparib or veliparib.
    Type: Grant
    Filed: September 13, 2019
    Date of Patent: March 21, 2023
    Assignee: Zenith Epigenetics Ltd.
    Inventors: Eric Campeau, Laura Tsujikawa, Sanjay Lakhotia
  • Patent number: 11590112
    Abstract: The invention provides a p38 MAPK inhibitor of Formula I, or a pharmaceutically acceptable salt or solvate thereof: Formula I for use in the treatment or prevention of hypercytokinemia in a human patient; wherein R is C1-3alkyl, optionally substituted by one or more halo, NR1R2 or hydroxy, and R1 and R2 are independently H, halo or C1-3alkyl, optionally substituted by one or more F. Also provided are compositions for use in the treatment or prevention of hypercytokinemia comprising the p38 MAPK inhibitor of Formula I; and methods for treating or preventing hypercytokinemia in a human patient in need thereof comprising administering to the patient a therapeutically or prophylactically effective amount of a p38 MAPK inhibitor of Formula I. The invention also provides a p38 MAPK inhibitor and an antimicrobial agent, such as an antiviral agent, for use in the treatment or prevention of hypercytokinemia.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: February 28, 2023
    Assignee: Orph Pharma IP Company Limited
    Inventors: Adrian Huw Davies, Pui-Man Choy, Vinay Saunders, Basma Bahsoun, Surender Vashist, Neil Edward Torbett, Paul Andrew Whittaker
  • Patent number: 11560378
    Abstract: Provided are compositions and methods for treating osteoarthritis including intra-articular administration of a compound of Formula (I) including amorphous and polymorph forms thereof.
    Type: Grant
    Filed: December 1, 2020
    Date of Patent: January 24, 2023
    Assignee: BioSplice Therapeutics, Inc.
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC, Yusuf Yazici, Christopher Swearingen, Luis A Dellamary
  • Patent number: 11491140
    Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (1) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
    Type: Grant
    Filed: July 30, 2020
    Date of Patent: November 8, 2022
    Assignee: H. Lundbeck A/S
    Inventors: Jan Kehler, Karsten Juhl, Mauro Marigo, Paulo Jorge Vieira Vital, Mikkel Jessing, Morten Langgård, Lars Kyhn Rasmussen, Carl Martin Sebastian Clementson
  • Patent number: 11427569
    Abstract: Described are benzoimidazole indolyl methane compounds, pharmaceutical compositions containing them, and use of the compounds to inhibit PCSK9-mediated ailments.
    Type: Grant
    Filed: February 13, 2020
    Date of Patent: August 30, 2022
    Assignee: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Weiping Tang, Gabrielle N. Winston-McPherson, Haibo Xie, Alan D. Attie, Mark Patrick Keller, Ka Yang
  • Patent number: 11427581
    Abstract: Disclosed in the present application are a class of compounds as JAK inhibitors and use thereof in the preparation of medicaments for treating JAK and TYK2 related diseases. Specifically, a compound represented by formula (I), an isomer thereof or a pharmaceutically acceptable salt thereof is disclosed.
    Type: Grant
    Filed: January 31, 2019
    Date of Patent: August 30, 2022
    Assignee: ZHUHAI UNITED LABORATORIES CO., LTD.
    Inventors: Weiwei Mao, Hao Wu, Xuejian Zheng, Guoping Hu, Changqing Wei, Jian Li, Shuhui Chen
  • Patent number: 11414433
    Abstract: Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
    Type: Grant
    Filed: December 29, 2020
    Date of Patent: August 16, 2022
    Assignee: Incyte Corporation
    Inventors: Liangxing Wu, Kaijiong Xiao, Wenqing Yao
  • Patent number: 11407767
    Abstract: This invention related to compounds that are inhibitors of the CDK12 kinase. The compounds are useful in the treatment of disorders mediated by the CDK12 kinase including myotonic dystrophy type 1 (DM1) and other disorders caused by the generation of RNA repeat expansion transcripts. In particular, the invention relates to compounds of the formula (I), or a pharmaceutically acceptable salts or N-oxides thereof, wherein R1a, R2, R3, R4a, R4b and R4c are as defined herein.
    Type: Grant
    Filed: September 21, 2018
    Date of Patent: August 9, 2022
    Inventors: David Brook, Chris Hayes, Nicholas Bennett, Matthew Palframan, Sue Cramp, Richard Bull, Michael Bodnarchuk
  • Patent number: 11401256
    Abstract: The present invention provides dihydroquinolinone compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.
    Type: Grant
    Filed: March 4, 2020
    Date of Patent: August 2, 2022
    Assignee: C4 Therapeutics, Inc.
    Inventors: Roger Norcross, Adrian Britschgi, Fabian Dey, Annick Goergler, Eric Andre Kusznir, Moreno Attilio Wichert
  • Patent number: 11377443
    Abstract: A compound which is an arylimidazolyl isoxazole of formula (I): (Formula (I)) or a pharmaceutically acceptable salt thereof. The compound has activity in modulating the activity of p300 and/or CBP and is used to treat cancer, particularly prostate cancer.
    Type: Grant
    Filed: May 14, 2020
    Date of Patent: July 5, 2022
    Assignee: CELLCENTRIC LIMITED
    Inventors: Neil Anthony Pegg, Stuart Thomas Onions, David Michel Adrien Taddei, Jonathan Shannon, Silvia Paoletta, Richard James Brown, Don Smyth, Gareth Harbottle
  • Patent number: 11325907
    Abstract: Disclosed are a crystal form of 1H-imidazo[4,5-b]pyridine-2(3H)-one compound and a preparation process therefor, and use of the crystal form in the manufacture of a medicament for treating a disease associated with PDE4 receptor.
    Type: Grant
    Filed: January 29, 2019
    Date of Patent: May 10, 2022
    Assignee: Medshine Discovery Inc.
    Inventors: Maoyi Lei, Yu Xu, Yunfu Luo
  • Patent number: 11312713
    Abstract: The present invention provides novel imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof I wherein R1, R2 and R3 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
    Type: Grant
    Filed: March 6, 2018
    Date of Patent: April 26, 2022
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Thomas Allen Chappie, Jinshan Michael Chen, Jotham Wadsworth Coe, Karen Jean Coffman, Paul Galatsis, Michelle Renee Garnsey, Christopher John Helal, Jaclyn Louise Henderson, Bethany Lyn Kormos, Ravi G. Kurumbail, Luis Angel Martinez-Alsina, Martin Youngjin Pettersson, Matthew Richard Reese, Colin Richard Rose, Antonia Friederike Stepan, Patrick Robert Verhoest, Travis T. Wager, Joseph Scott Warmus, Yuan Zhang
  • Patent number: 11274123
    Abstract: The present invention relates to compounds of formula (I), compositions, methods and uses involving the said formula (I) that inhibit CD47 signaling pathway. The present invention also relates to methods of making such compounds and their uses for the treatment of diseases or disorders mediated by CD47.
    Type: Grant
    Filed: January 11, 2019
    Date of Patent: March 15, 2022
    Assignee: AURIGENE DISCOVERY TECHNOLOGIES LIMITED
    Inventors: Pottayil Govindan Nair Sasikumar, Muralidhara Ramachandra, Seetharamaiah Setty Sudarshan Naremaddepalli, Chennakrishnareddy Gundala
  • Patent number: 11274100
    Abstract: The present invention provides a compound having excellent histone acetyl transferase inhibitory activity against EP300 and/or CREBBP, or a pharmacologically acceptable salt thereof. The compound is represented by the following formula (1) or a pharmacologically acceptable salt thereof: wherein ring Q1, ring Q2, R1, R2, R3 and R4 respectively have the same meanings as defined in the specification.
    Type: Grant
    Filed: June 21, 2018
    Date of Patent: March 15, 2022
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Hiroyuki Naito, Yoshiko Kagoshima, Hideaki Funami, Akifumi Nakamura, Masayoshi Asano, Makoto Haruta, Takashi Suzuki, Jun Watanabe, Ryutaro Kanada, Saito Higuchi, Kentaro Ito, Akiko Egami, Katsuhiro Kobayashi
  • Patent number: 11236087
    Abstract: The present invention relates generally to novel antiviral agents. Specifically, the present invention relates to compounds which can inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV replication cycle, compositions comprising such compounds, methods for inhibiting HBV viral replication, methods for treating or preventing HBV infection, and processes and intermediates for making the compounds.
    Type: Grant
    Filed: November 2, 2018
    Date of Patent: February 1, 2022
    Assignee: AiCuris GmbH & Co. KG
    Inventors: Alastair Donald, Andreas Urban, Susanne Bonsmann, Anita Wegert, Jasper Springer
  • Patent number: 11203591
    Abstract: The present disclosure relates generally to certain 6-azabenzimidazole compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.
    Type: Grant
    Filed: October 30, 2019
    Date of Patent: December 21, 2021
    Assignee: Gilead Sciences, Inc.
    Inventors: Gayatri Balan, Mark J. Bartlett, Jayaraman Chandrasekhar, Julian A. Codelli, John H. Conway, Jennifer L. Cosman, Rao V. Kalla, Zachary A. Kasun, Musong Kim, Seung H. Lee, Jennifer R. Lo, Jennifer A. Loyer-Drew, Scott A. Mitchell, Thao D. Perry, Gary B. Phillips, Patrick J. Salvo, Sundaramoorthi Swaminathan, Joshua J. Van Veldhuizen, Suet C. Yeung, Jeff Zablocki
  • Patent number: 11179376
    Abstract: The present invention provides salts of pyrazolo[1,5-?]pyridine derivative and use thereof. The invention also relates to a pharmaceutically acceptable composition comprising such salts and a method of using the salts and the pharmaceutically acceptable composition to prevent or treat a proliferative disorder or pulmonary fibrosis in a patient.
    Type: Grant
    Filed: December 15, 2018
    Date of Patent: November 23, 2021
    Assignee: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Ning Xi, Mingming Sun
  • Patent number: 11130759
    Abstract: Disclosed herein are certain 2-oxoquinazoline derivatives of Formula (IA): that are methionine adenosyltransferase 2A (MAT2A) inhibitors. Also disclosed are pharmaceutical compositions comprising such compounds and methods of treating diseases treatable by inhibition of MAT2A such as cancer, including cancers characterized by reduced or absence of methylthioadenosine phosphorylase (MTAP) activity.
    Type: Grant
    Filed: February 12, 2021
    Date of Patent: September 28, 2021
    Assignee: IDEAYA BIOSCIENCE, INC.
    Inventors: Muzaffar Alam, Leah Cleary, Melissa Fleury, Zhonghua Pei, Richard Steel, James Sutton, John E. Knox, Zachary E. R. Newby
  • Patent number: 11083724
    Abstract: Disclosed are methods of treating CGRP related disorders, e.g., migraine, by administering to a patient in need thereof rimegepant or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions comprising rimegepant and kits including the pharmaceutical compositions and instructions are also disclosed.
    Type: Grant
    Filed: May 27, 2020
    Date of Patent: August 10, 2021
    Assignee: Biohaven Pharmaceutical Ireland DAC
    Inventors: Vladimir Coric, Robert Croop
  • Patent number: 10973834
    Abstract: The present invention provides use of an agent that inhibits EP4 activity and an immuno-oncology agent, or a composition thereof, for treatment of a cancer.
    Type: Grant
    Filed: April 16, 2019
    Date of Patent: April 13, 2021
    Assignees: Arrys Therapeutics, Inc., AskAt Inc.
    Inventors: Mark Manfredi, Jeffrey Ecsedy, Atsushi Nagahisa, Yukinori Take, Takako Okumura
  • Patent number: 10968215
    Abstract: The present invention provides a pyrido five-element aromatic ring compound, and a preparation method therefor and a use thereof. The compound provided in the present invention has an inhibitory effect on wild-type and/or mutant EZH2, and is well positioned to become a novel anti-tumor drug or a drug for the treatment of autoimmune diseases.
    Type: Grant
    Filed: September 6, 2017
    Date of Patent: April 6, 2021
    Assignees: SHANGHAI HAIHE PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Xuxing Chen, Meiyu Geng, Lei Jiang, Yi Chen, Jianhua Cao, Qingyun Jiang, Qianqian Shen, Jian Ding, Yucai Yao, Zhao Zhao, Yuanfang Xiong
  • Patent number: 10961217
    Abstract: Crystals of a compound that exhibits an analgesic action against neuropathic pain and/or fibromyalgia syndrome are useful as pharmaceuticals. The crystals may be of (S)-1-(4-(dimethylamino)piperidin-1-yl)-3-hydroxy-3-(1-methyl-1H-imidazol-2-yl)propan-1-one or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: August 25, 2017
    Date of Patent: March 30, 2021
    Assignee: Toray Industries, Inc.
    Inventors: Hirozumi Takahashi, Yoko Baba, Yasuhiro Morita, Katsuhiko Iseki, Naoki Izumimoto
  • Patent number: 10947228
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: July 22, 2019
    Date of Patent: March 16, 2021
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • Patent number: 10946071
    Abstract: This disclosure is directed to methods of alleviating the negative effects of, treating, or slowing the progression of progressive multiple sclerosis in human patients using ibudilast and interferon-beta.
    Type: Grant
    Filed: October 8, 2019
    Date of Patent: March 16, 2021
    Assignee: MediciNova, Inc.
    Inventor: Kazuko Matsuda
  • Patent number: 10947235
    Abstract: This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.
    Type: Grant
    Filed: February 27, 2020
    Date of Patent: March 16, 2021
    Assignee: AskAt Inc.
    Inventors: Yukinori Take, Shinichi Koizumi, Takako Okumura, Kazuhiko Nonomura
  • Patent number: 10913746
    Abstract: The present invention provides a compound having the structure: wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; and B is a substituted or unsubstituted heterobicycle, wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 24, 2019
    Date of Patent: February 9, 2021
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Konstantin Petrukhin, Christopher Cioffi, Graham Johnson, Rando Allikmets, Emily Freeman, Ping Chen, Michael Conlon, Lei Zhu
  • Patent number: 10889583
    Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: January 12, 2021
    Assignee: Syngenta Participations AG
    Inventors: Pierre Joseph Marcel Jung, Vikas Sikervar, Indira Sen, Girish Rawal, Michel Muehlebach, Andrew Edmunds, Sebastian Rendler, Daniel Emery
  • Patent number: 10882859
    Abstract: There are provided compounds of formula I, wherein X, Ak, s, A, R1 and R2 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of the JAK family) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Grant
    Filed: December 11, 2019
    Date of Patent: January 5, 2021
    Assignee: TOPIVERT PHARMA LIMITED
    Inventor: Matthew Colin Thor Fyfe
  • Patent number: 10882860
    Abstract: Provided are compositions and methods for treating osteoarthritis including intra-articular administration of a compound of Formula (I) including amorphous and polymorph forms thereof.
    Type: Grant
    Filed: December 11, 2019
    Date of Patent: January 5, 2021
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC, Yusuf Yazici, Christopher Swearingen, Luis A Dellamary
  • Patent number: 10875854
    Abstract: The present invention relates to compounds of formula wherein HetAr is a five or six membered hetaryl group, containing one, two or three heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen or lower alkoxy; R2 is lower alkyl substituted by halogen; R3 is hydrogen, lower alkyl substituted by halogen, lower alkyl or lower alkyl substituted by hydroxy; Y is R4 is lower alkoxy, lower alkoxy substituted by halogen or CN; or to pharmaceutically active acid addition salts thereof, to racemic mixtures or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
    Type: Grant
    Filed: December 18, 2018
    Date of Patent: December 29, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bjoern Bartels, Roland Jakob-Roetne, Anja Limberg, Werner Neidhart, Hasane Ratni, Rosa Maria Rodriguez Sarmiento
  • Patent number: 10870651
    Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g.
    Type: Grant
    Filed: December 23, 2015
    Date of Patent: December 22, 2020
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Yanke Liang, Tinghu Zhang, Nicholas Paul Kwiatkowski
  • Patent number: 10836727
    Abstract: The present invention provides novel crystalline forms of 4-[3-Chloro-4-(N?-cyclopropylureido)phenoxy]-7-methoxyquinoline-6-carboxamide methanesulfonate, as well as methods for their preparation.
    Type: Grant
    Filed: September 15, 2017
    Date of Patent: November 17, 2020
    Assignee: Indena S.P.A.
    Inventors: Nicola Sardone, Stefano Luca Giaffreda, Andrea Gambini, Alex Petrolati, Pietro Allegrini, Enrico Modena