Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/210.21)
  • Patent number: 12215087
    Abstract: The present disclosure relates to compounds that act as inhibitors of NLRP3 inflammasomes; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with inflammation and inflammaging, including hearing loss and other diseases associated with aging.
    Type: Grant
    Filed: July 17, 2023
    Date of Patent: February 4, 2025
    Assignee: BioAge Labs, Inc.
    Inventors: George Hartman, Paul Humphries, Kevin Edward Leif Wilhelmsen
  • Patent number: 12209086
    Abstract: The present invention provides compounds of the formula: for use in the treatment of systemic sclerosis, fibrosis (e.g. pulmonary fibrosis), achondroplasia, thanatophoric dysplasia (e.g. type I), severe achondroplasia with developmental delay and acanthosis nigricans (SADDAN), muenke syndrome or cancer.
    Type: Grant
    Filed: December 13, 2023
    Date of Patent: January 28, 2025
    Assignee: ELI LILLY AND COMPANY
    Inventors: Adedoyin David Abraham, Desta Doro Bume, Kevin Ronald Condroski, Robert Alan Hazlitt, Timothy Scott Kercher, Andrew Terrance Metcalf, Kaveri Balan Urkalan, Shane Michael Walls, Andrew Karl Dilger
  • Patent number: 12195459
    Abstract: The present disclosure relates to novel pan-KRAS glutarimide-containing compounds with KRAS degradation activities, pharmaceutical compositions containing such compounds, and their use in prevention and treatment diseases and conditions.
    Type: Grant
    Filed: April 24, 2024
    Date of Patent: January 14, 2025
    Assignee: Tiger Biotherapeutics Inc.
    Inventors: Robert Luo, Ji Liu, Pin Huang, Jie Su, Yan Feng, Ke Liu, Jie Fan, Wei He, Yimin Qian
  • Patent number: 12178822
    Abstract: Provided herein are methods of using 2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione, or an enantiomer, a mixture of enantiomers, a tautomer, an isotopolog, or a pharmaceutically acceptable salt thereof, for treating, preventing or managing hematological malignancies.
    Type: Grant
    Filed: May 10, 2023
    Date of Patent: December 31, 2024
    Assignee: Celgene Corporation
    Inventors: Maria Soraya Carrancio Anton, Tonia J. Buchholz, Shailaja Kasibhatla, Antonia Lopez-Girona, Rama Krishna Narla, Michael Pourdehnad
  • Patent number: 12172983
    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: October 29, 2021
    Date of Patent: December 24, 2024
    Assignee: Blueprint Medicines Corporation
    Inventors: John Emmerson Campbell, Thomas A. Dineen, Natasja Brooijmans, Jason D. Brubaker, Meredith Suzanne Eno, Joseph L. Kim, Aysegül Özen, Emanuele Perola, Brett D. Williams, Douglas Wilson, Kevin J. Wilson, Christopher De Savi
  • Patent number: 12162881
    Abstract: The present disclosure provides compounds and compositions thereof which are useful as inhibitors of JAK2 and which exhibit desirable characteristics for the same.
    Type: Grant
    Filed: November 8, 2022
    Date of Patent: December 10, 2024
    Assignee: Ajax Therapeutics, Inc.
    Inventors: Craig E. Masse, Jeremy R. Greenwood, Jiayi Xu, Sayan Mondal, Phani Ghanakota
  • Patent number: 12110291
    Abstract: The present disclosure relates to novel pan-KRAS glutarimide-containing compounds with KRAS degradation activities, pharmaceutical compositions containing such compounds, and their use in prevention and treatment diseases and conditions.
    Type: Grant
    Filed: November 30, 2023
    Date of Patent: October 8, 2024
    Assignee: Tiger Biotherapeutics Inc.
    Inventors: Robert Luo, Ji Liu, Pin Huang, Jie Su, Yan Feng, Ke Liu, Jie Fan, Wei He, Yimin Qian
  • Patent number: 12103923
    Abstract: Provided herein are methods of using 2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione, or an enantiomer, a mixture of enantiomers, a tautomer, an isotopolog, or a pharmaceutically acceptable salt thereof, alone or in combination with rituximab, for treating, preventing or managing non-Hodgkin lymphoma.
    Type: Grant
    Filed: June 24, 2022
    Date of Patent: October 1, 2024
    Assignee: Celgene Corporation
    Inventors: Maria Soraya Carrancio Anton, Tonia J. Buchholz, Antonia Lopez-Girona, Rama Krishna Narla, Michael Pourdehnad
  • Patent number: 12091413
    Abstract: Compounds having activity as inhibitors of NEK7 are provided. The compounds have Structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein, A, X, Y, R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of the NLRP3 inflammasome are also provided.
    Type: Grant
    Filed: May 23, 2023
    Date of Patent: September 17, 2024
    Assignee: Halia Therapeutics, Inc.
    Inventors: David James Bearss, John Sai Keong Kauwe, III, Alexis Henri Abel Mollard
  • Patent number: 12054492
    Abstract: Disclosed are compounds of formula I, II, III, and IV, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of ALK2 kinase. Also provided are pharmaceutical compositions comprising a compound of formula I, II, III, or IV, or pharmaceutically acceptable salt thereof, and methods involving use of the compounds or pharmaceutically acceptable salts thereof and compositions in the treatment and prevention of various diseases and conditions, such as fibrodysplasia ossificans progressiva.
    Type: Grant
    Filed: February 13, 2023
    Date of Patent: August 6, 2024
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Pravin L. Kotian, Yarlagadda S. Babu, V. Satish Kumar, Weihe Zhang, Peng-Cheng Lu, Krishnan Raman
  • Patent number: 12049464
    Abstract: BRD9 protein degradation compounds or pharmaceutically acceptable salts thereof are provided for the treatment of disorders mediated by BRD9, including but not limited to abnormal cellular proliferation.
    Type: Grant
    Filed: September 1, 2022
    Date of Patent: July 30, 2024
    Assignee: C4 Therapeutics, Inc.
    Inventors: Christopher G. Nasveschuk, Rhamy Zeid, Ning Yin, Katrina L. Jackson, Gesine Kerstin Veits, Moses Moustakim, Jeremy L. Yap
  • Patent number: 12049462
    Abstract: The present disclosure relates to tri-substituted aryl and heteroaryl derivatives. pharmaceutical compositions containing them, and methods of using them, including methods for modulating autophagy or preventing, reversing, slowing or inhibiting the PI3K-AKT-MTOR pathway, and methods of treating diseases that are associated with autophagy or the PI3K-AKT-MTOR pathway.
    Type: Grant
    Filed: November 7, 2022
    Date of Patent: July 30, 2024
    Assignee: Neuropore Therapies, Inc.
    Inventors: Emily M. Stocking, Wolfgang J. Wrasidlo
  • Patent number: 12036219
    Abstract: The present disclosure relates generally to methods of treating infections in overweight or obese patients using antibiotics. According to statistics compiled by National Health and Nutrition Examination Survey conducted by the National Center for Health Statistics (NCHS) of the U.S. Centers for Disease Control and Prevention (CDC), in 2009-2010, 35.7% of adults in the United States were found to be obese. Ogden, C.L. NCHS Data Brief 2012, 82, available at http://www.cdc.gov/nchs/data/databiefs/db82.pdf (last visited Mar. 2, 2013).
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: July 16, 2024
    Assignee: MELINTA SUBSIDIARY CORP.
    Inventor: Erin M. Duffy
  • Patent number: 12030896
    Abstract: The present application provides, inter alia, a compound of Formula (I): or a pharmaceutically acceptable salt thereof, wherein Y, Ar, X1, X2, X3, R1, R2, R3, R4, R5, and R6 are as described herein. Methods of making these compounds and methods of using these compound for treating diseases such as cancer are also provided.
    Type: Grant
    Filed: July 1, 2019
    Date of Patent: July 9, 2024
    Assignees: Mayo Foundation for Medical Education and Research, Sanford Burnham Prebys Medical Discovery Institute
    Inventors: Richard J. Bram, Anthony B. Pinkerton, Eduard Serguienko
  • Patent number: 11999728
    Abstract: Compounds of Formula (I) are estrogen receptor alpha modulators, where the variables in Formula (I) are described in the disclosure. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions that are estrogen receptor alpha dependent and/or estrogen receptor alpha mediated, including conditions characterized by excessive cellular proliferation, such as cancer.
    Type: Grant
    Filed: April 4, 2022
    Date of Patent: June 4, 2024
    Assignee: RECURIUM IP HOLDINGS, LLC
    Inventors: Guobao Zhang, Peter Qinhua Huang, Kevin Duane Bunker, Sayee Gajanan Hegde
  • Patent number: 11970493
    Abstract: The present disclosure provides autotaxin (ATX) inhibitor compounds and compositions including said compounds. The present disclosure also provides methods of using said compounds and compositions for inhibiting ATX. Also provided are methods of preparing said compounds and compositions, and synthetic precursors of said compounds.
    Type: Grant
    Filed: October 4, 2021
    Date of Patent: April 30, 2024
    Assignee: ILDONG PHARMACEUTICAL CO., LTD.
    Inventors: Sung-Ku Choi, Yoon-Suk Lee, Sung-Wook Kwon, Kyung-Sun Kim, Jeong-Geun Kim, Jeong-Ah Kim, An-Na Moon, Sun-Young Park, Jun-Su Ban, Dong-Keun Song, Kyu-Sic Jang, Ju-Young Jung, Soo-Jin Lee
  • Patent number: 11931400
    Abstract: Therapeutic compositions and an associated method for improving a Toll-like receptor (TLR)-related condition, including determining a set of peptide sequences associated with a microorganism-related modulator of a TLR, determining a first set of binding parameters for the set of peptide sequences in relation to the TLR, selecting a target subset of peptide sequences from the set of peptide sequences based on the first set of binding parameters, reengineering the target subset of peptide sequences based on mutating amino acid residues of the target subset of peptide sequences, determining a second set of binding parameters for the reengineered target subset of peptide sequences in relation to the TLR, and identifying a first peptide for use in a therapeutic composition for improving the TLR-related condition, based on the second set of binding parameters for the reengineered target subset of peptide sequences.
    Type: Grant
    Filed: March 7, 2018
    Date of Patent: March 19, 2024
    Assignee: PSOMAGEN, INC.
    Inventors: Zachary Apte, Jessica Richman, Daniel Almonacid, Melissa Alegria, Valeria Marquez, Eduardo Morales, Rodrigo Ortiz, Janet Torres, Paulo Covarrubias, Javier Gimpel, Ingrid Araya
  • Patent number: 11919864
    Abstract: Methods are provided for modulating MRGPR X2 generally, or for treating a MRGPR X2 or a MRGPR X2 ortholog dependent condition, more specifically, by contacting the MRGPR X2 or the MRGPR X2 ortholog by administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I): or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein W, Z, R1, R2, R3, R4, R5, R6 and Rx are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.
    Type: Grant
    Filed: September 24, 2021
    Date of Patent: March 5, 2024
    Assignee: ESCIENT PHARMACEUTICALS, INC.
    Inventors: Marion Lanier, Marcus Boehm, Liming Huang, Esther Martinborough, Marcos Sainz, Brandon Selfridge, Adam Yeager
  • Patent number: 11890285
    Abstract: The present invention relates to combination therapies for treating KRas G12C cancers. In particular, the present invention relates to methods of treating cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a combination of a an agent that blocks Programmed Death-1 receptor (PD-1) and Programmed Death Ligand-1 (PD-L1) signaling and a KRAS G12C inhibitor of Formula (I), Formula I-A or Formula I-B, kits comprising the compositions and methods of use therefor.
    Type: Grant
    Filed: September 23, 2020
    Date of Patent: February 6, 2024
    Assignee: Mirati Therapeutics, Inc.
    Inventors: David Briere, James Gail Christensen, Peter Olson
  • Patent number: 11878976
    Abstract: The present invention provides compounds of the formula: for use in the treatment of systemic sclerosis, fibrosis (e.g. pulmonary fibrosis), achondroplasia, thanatophoric dysplasia (e.g. type I), severe achondroplasia with developmental delay and acanthosis nigricans (SADDAN), muenke syndrome or cancer.
    Type: Grant
    Filed: March 3, 2022
    Date of Patent: January 23, 2024
    Assignee: ELI LILLY AND COMPANY
    Inventors: Adedoyin David Abraham, Desta Doro Bume, Kevin Ronald Condroski, Robert Alan Hazlitt, Timothy Scott Kercher, Andrew Terrance Metcalf, Kaveri Balan Urkalan, Shane Michael Walls, Andrew Karl Dilger
  • Patent number: 11858915
    Abstract: Disclosed herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, that are inhibitors of Polo Like Kinase 4 (PLK4). Also disclosed herein are pharmaceutical compositions comprising the compounds of Formula (I), or pharmaceutically acceptable salts thereof, and one or more pharmaceutically acceptable excipients. Further disclosed herein are methods of treating cancer in a subject in need thereof, comprising administering to the subject an amount of a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 27, 2023
    Date of Patent: January 2, 2024
    Assignee: ORIC PHARMACEUTICALS, INC.
    Inventors: Chudi Ndubaku, Jared Thomas Moore, Paul Anthony Gibbons, Jae Hyuk Chang, F. Anthony Romero, Xiaohui Du, Hiroyuki Kawai, Stephane Ciblat, Hong Wang, Vincent Albert, Lea Constantineau-Forget, Hugo De Almeida Silva, Dilan Emine Polat, Amit Nayyar, Daniel Gordon Michael Shore, Kejia Wu, Joanne Tan
  • Patent number: 11819499
    Abstract: Provided are single-dose, ready-to-use formulations and methods for preparing the formulations that include a compound of Formula (I) including pharmaceutically acceptable salts and amorphous and polymorph forms thereof.
    Type: Grant
    Filed: July 26, 2022
    Date of Patent: November 21, 2023
    Assignee: BioSplice Therapeutics, Inc.
    Inventor: Luis A. Dellamary
  • Patent number: 11807650
    Abstract: Disclosed herein, in part, are heteroaromatic compounds and methods of use in treating neuropsychiatric disorders, e.g., schizophrenia and major depressive disorder. Pharmaceutical compositions and methods of making heteroaromatic compounds are provided. The compounds are contemplated to modulate the NMDA receptor.
    Type: Grant
    Filed: January 27, 2022
    Date of Patent: November 7, 2023
    Assignee: Novartis AG
    Inventors: David R. Anderson, Robert Volkmann, Frank Menniti, Christopher Fanger, Yuelian Xu
  • Patent number: 11767312
    Abstract: Disclosed are a phthalazinone compound, and a preparation method therefor and the medical use thereof. In particular, disclosed are a compound as represented by formula (I), and a pharmacodynamically acceptable salt, and the use of the compound as an androgen receptor (AR) for degradation.
    Type: Grant
    Filed: April 5, 2023
    Date of Patent: September 26, 2023
    Assignee: GENENTECH, INC.
    Inventors: Hongfu Lu, Weiqiang Xing, Yongcong Lv, Baojian Qi, Jianbiao Peng, Haibing Guo
  • Patent number: 11713321
    Abstract: Compounds having activity as inhibitors of NEK7 are provided. The compounds have Structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein, A, X, Y, R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of the NLRP3 inflammasome are also provided.
    Type: Grant
    Filed: September 14, 2021
    Date of Patent: August 1, 2023
    Assignee: HALIA THERAPEUTICS, INC.
    Inventors: David James Bearss, John Sai Keong Kauwe, III, Alexis Henri Abel Mollard
  • Patent number: 11708352
    Abstract: This invention provides, among other things, compounds useful for treating diseases such as cancer, pharmaceutical formulations containing such compounds, as well as combinations of these compounds with at least one additional therapeutic agent.
    Type: Grant
    Filed: October 15, 2021
    Date of Patent: July 25, 2023
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Csaba J. Peto, David Jablons, Hassan Lemjabbar-Alaoui
  • Patent number: 11691963
    Abstract: The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
    Type: Grant
    Filed: May 5, 2021
    Date of Patent: July 4, 2023
    Assignee: Ajax Therapeutics, Inc.
    Inventors: Craig E. Masse, Jeremy R. Greenwood, Sayan Mondal, Jiayi Xu, Phani Ghanakota, Fiona Michelle McRobb, Nicholas Boyles
  • Patent number: 11672800
    Abstract: The present disclosure relates to a method of preventing or treating a cancer via administering an EHMT2 inhibitor or a combination comprising an EHMT2 inhibitor compound and one or more additional therapeutic agent disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds or combinations for research or other non-therapeutic purposes.
    Type: Grant
    Filed: April 20, 2018
    Date of Patent: June 13, 2023
    Assignee: Epizyme, Inc.
    Inventors: John Emmerson Campbell, Kenneth William Duncan, Maria Alejandra Raimondi, Christine Klaus, Elayne Penebre
  • Patent number: 11667611
    Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.
    Type: Grant
    Filed: May 6, 2019
    Date of Patent: June 6, 2023
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Ankush Argade, Arvinder Sran, David Carroll, Jeffrey Clough, Kin Tso, Somasekhar Bhamidipati, Sambaiah Thota, Rajinder Singh, Vanessa Taylor, Hui Li, Esteban Masuda
  • Patent number: 11608335
    Abstract: Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.
    Type: Grant
    Filed: February 11, 2019
    Date of Patent: March 21, 2023
    Assignee: CRINETICS PHARMACEUTICALS, INC.
    Inventors: Jian Zhao, Shimiao Wang, Yunfei Zhu
  • Patent number: 11596632
    Abstract: This disclosure relates to JAK1 pathway inhibitors and the use thereof in treating gastrointestinal diseases or disorders such as ulcerative colitis.
    Type: Grant
    Filed: December 19, 2019
    Date of Patent: March 7, 2023
    Assignee: Incyte Corporation
    Inventors: Krishnaswamy Yeleswaram, Paul Smith, Gregory F. Hollis
  • Patent number: 11524957
    Abstract: The present invention provides processes and synthetic intermediates for the synthesis of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4 {3H)-one or a salt, hydrate, or tautomer thereof, or any combination thereof, which are Cdc7 kinase inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with Cdc7 activity.
    Type: Grant
    Filed: April 1, 2019
    Date of Patent: December 13, 2022
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Lei Zhu, John Daniel Bailey, Landon Durak, Joshua David Waetzig, Masahiro Mizuno, Kazuhiro Maeda, Tsuneo Yasuma, Hiroshi Yamaguchi, Koichiro Fukuoka, Kazuyuki Akiyama
  • Patent number: 11512072
    Abstract: The present disclosure provides azetidine compounds of Formula I and their pharmaceutically acceptable salts, their compositions, and methods for their use in determining azetidine compound binding to proteins. The azetidine compounds are useful as probes, for monitoring diacylglycerol kinase activity, and for identifying druggable targets.
    Type: Grant
    Filed: April 19, 2019
    Date of Patent: November 29, 2022
    Assignee: University of Virginia Patent Foundation
    Inventors: Ku-Lung Hsu, Rebecca L. McCloud
  • Patent number: 11512090
    Abstract: Provided herein are compounds which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.
    Type: Grant
    Filed: June 10, 2019
    Date of Patent: November 29, 2022
    Assignee: Pipeline Therapeutics, Inc.
    Inventors: Yifeng Xiong, Thomas Schrader, Austin Chen, Jeffrey Roger Roppe, Jill Melissa Baccei, Yalda Bravo
  • Patent number: 11498920
    Abstract: Novel 4-(1H-imidazol-5-yl)-1H-pyrrolo[2,3-b]pyridine compounds that are useful in the treatment of lymphomas, leukaemias, and solid tumors.
    Type: Grant
    Filed: March 26, 2019
    Date of Patent: November 15, 2022
    Assignee: MASARYKOVA UNIVERZITA
    Inventors: Vitezslav Bryja, Pavlina Janovska, Michaela Gregorova, Vaclav Nemec, Prashant Khirsariya, Kamil Paruch
  • Patent number: 11458123
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.
    Type: Grant
    Filed: November 1, 2017
    Date of Patent: October 4, 2022
    Assignee: ARVINAS OPERATIONS, INC.
    Inventors: Andrew P. Crew, Michael Berlin, Hanqing Dong, Alexey Ishchenko
  • Patent number: 11459327
    Abstract: Cycloalkyl and hetero-cycloalkyl inhibitors, preparation methods therefor, and the use thereof are described. Compounds of the present invention have a structure represented by formula (I). Further disclosed are preparation methods for said compounds, and the use of said compounds as KRASG12C inhibitors. The compounds have an excellent ability to selectively inhibit KRASG12C, improved pharmacodynamic and pharmacokinetic performance, and reduced toxic side effects.
    Type: Grant
    Filed: June 7, 2021
    Date of Patent: October 4, 2022
    Assignees: Suzhou Zelgen Biopharmaceuticals Co., Ltd., Shanghai Zelgen Pharma.Tech Co., Ltd.
    Inventors: Binhua Lv, Dawei Cui, Lianjun Liu, Tao Han, Runqing Wang, Peizhong Ni, Zelin Sheng
  • Patent number: 11459337
    Abstract: Disclosed in the present invention are an IRAK4 inhibitor, and an application thereof in preparation of a drug for treating IRAK4-related diseases. Specifically disclosed are a compound represented by formula (III) and a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 25, 2019
    Date of Patent: October 4, 2022
    Assignee: Chia Tai Tianqing Pharmaceutical Group Co., Inc.
    Inventors: Yang Zhang, Jianfei Wang, Haizhong Tan, Jie Li, Jian Li, Shuhui Chen
  • Patent number: 11446288
    Abstract: Provided are single-dose, ready-to-use formulations and methods for preparing the formulations that include a compound of Formula (I) including pharmaceutically acceptable salts and amorphous and polymorph forms thereof.
    Type: Grant
    Filed: July 27, 2020
    Date of Patent: September 20, 2022
    Assignee: BioSplice Therapeutics, Inc.
    Inventor: Luis A. Dellamary
  • Patent number: 11390617
    Abstract: Provided herein are methods of using 2-(2,6-dioxopiperidin-3-yl)-4-((2-fluoro-4-((3-morpholinoazetidin-1-yl)methyl)benzyl)amino)isoindoline-1,3-dione, or an enantiomer, a mixture of enantiomers, a tautomer, an isotopolog, or a pharmaceutically acceptable salt thereof, alone or in combination with rituximab, for treating, preventing or managing non-Hodgkin lymphoma.
    Type: Grant
    Filed: April 9, 2020
    Date of Patent: July 19, 2022
    Assignee: CELGENE CORPORATION
    Inventors: Maria Soraya Carrancio Anton, Tonia J. Buchholz, Antonia Lopez-Girona, Rama Krishna Narla, Michael Pourdehnad
  • Patent number: 11390632
    Abstract: The present invention relates to a process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one derivatives useful as pharmaceutically active compounds.
    Type: Grant
    Filed: March 19, 2020
    Date of Patent: July 19, 2022
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Michel Adam, Serena Maria Fantasia, Daniel Vincent Fishlock, Fabienne Hoffmann-Emery, Gerard Moine, Christophe Pfleger, Christian Moessner
  • Patent number: 11365250
    Abstract: The present disclosure generally relates to compositions and methods for cancer immunotherapy, as well as hematopoietic recovery following cancer treatment such as chemotherapy or irradiation.
    Type: Grant
    Filed: November 29, 2018
    Date of Patent: June 21, 2022
    Assignee: The Board of Regents of The University of Texas System
    Inventors: Bruce Beutler, Evan Nair-Gill, Xue Zhong, Jinglei Zhang, Pingping Wang
  • Patent number: 11358952
    Abstract: Provided herein are 4-aminoisoindoline-1,3-dione compounds having the following structure: wherein R, Ring A, and n are as defined herein, compositions comprising an effective amount of a 4-aminoisoindoline-1,3-dione compound, and methods for treating or preventing disorders.
    Type: Grant
    Filed: April 22, 2019
    Date of Patent: June 14, 2022
    Assignee: Celgene Corporation
    Inventors: Matthew D. Alexander, Soraya Carranclo, Matthew D. Correa, Virginia Heather Sharron Grant, Joshua Hansen, Roy L. Harris, Dehua Huang, Timothy S. Kercher, Antonia Lopez-Girona, Mark A. Nagy, Veronique Plantevin-Krenitsky
  • Patent number: 11352353
    Abstract: A heterocyclic compound which is an inhibitor of FGFR4 (fibroblast growth factor receptor 4) is described. Specifically, a compound represented by the following formula (I), including an isomer (enantiomer or diastereomer) which may be present, or a pharmaceutically acceptable salt thereof, prodrugs, deuterated derivatives, hydrates, solvates, are described. The definition of each group in the formula (I) is as described in the specification. The compounds have FGFR4 inhibitory activity and can be used for the prevention or treatment of diseases associated with FGFR4 activity or expression, and can also be used in combination with other drugs for the treatment of various related diseases, as described.
    Type: Grant
    Filed: May 27, 2017
    Date of Patent: June 7, 2022
    Assignee: Hangzhou Innogate Pharma Co., Ltd.
    Inventors: Hancheng Zhang, Shifeng Liu, Xiangyang Ye
  • Patent number: 11339162
    Abstract: Compounds of Formula (I) are estrogen receptor alpha modulators, where the variables in Formula (I) are described in the disclosure. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions that are estrogen receptor alpha dependent and/or estrogen receptor alpha mediated, including conditions characterized by excessive cellular proliferation, such as cancer.
    Type: Grant
    Filed: December 20, 2021
    Date of Patent: May 24, 2022
    Assignee: Recurium IP Holdings, LLC
    Inventors: Guobao Zhang, Peter Qinhua Huang, Kevin Duane Bunker, Sayee Gajanan Hegde
  • Patent number: 11319295
    Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (Formula (I)). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Grant
    Filed: October 4, 2018
    Date of Patent: May 3, 2022
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Catherine M. White, Meredeth Ann McGowan, Yongxin Han, Nunzio Sciammetta
  • Patent number: 11306093
    Abstract: A process for preparing the compound of formula I comprising: a) coupling a compound of formula 2 wherein a leaving group O—SO2—R is selected from the triflate group, the tosylate group, the mesylate group, the besylate group, the nosylate group or the brosylate group, with a suitable boronic acid, a trifluoroborate or a boronic acid ester under argon condition and in the presence of a catalyst and a base in a suitable solvent and then isolating the product as an acid addition salt to afford the compound of formula Ia and b) converting the acid addition salt of formula Ia wherein the acid HX comprises suitable organic or inorganic acids into the compound of formula I by treatment with at least a stoichiometric equivalent of a suitable base.
    Type: Grant
    Filed: March 6, 2019
    Date of Patent: April 19, 2022
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Bjoern Bartels, Philipp Cueni, Matthias Koerner, Dieter Muri
  • Patent number: 11306069
    Abstract: Novel benzimidazole enantiomeric derivatives, their process of preparation and their therapeutical uses as dual H1 and H4 receptor ligands are disclosed.
    Type: Grant
    Filed: November 15, 2018
    Date of Patent: April 19, 2022
    Assignee: BIOPROJET
    Inventors: Isabelle Berrebi-Bertrand, Xavier Billot, Thierry Calmels, Marc Capet, Stéphane Krief, Olivier Labeeuw, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Philippe Robert, Jean-Charles Schwartz
  • Patent number: 11279702
    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: October 15, 2021
    Date of Patent: March 22, 2022
    Assignee: KALLYOPE, INC.
    Inventors: Iyassu Sebhat, Shuwen He
  • Patent number: 11274107
    Abstract: Disclosed herein, in part, are heteroaromatic compounds and methods of use in treating neuropsychiatric disorders, e.g., schizophrenia and major depressive disorder. Pharmaceutical compositions and methods of making heteroaromatic compounds are provided. The compounds are contemplated to modulate the NMDA receptor.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: March 15, 2022
    Assignee: Cadent Therapeutics, Inc.
    Inventors: David R. Anderson, Robert A. Volkmann, Frank Menniti, Christopher Fanger, Yuelian Xu