Patents Examined by Douglas M Willis
  • Substituted imidazo[4,5-c][1,8]naphthyridines as phosphodiesterase inhibitors
    Patent number: 11673889
    Abstract: The invention provides compounds of Formula (A) that may inhibit ENPP1, and that are accordingly useful for treatment of disorders related to ENPP1. The invention further provides pharmaceutical compositions containing these compounds and methods of using these compounds to treat or prevent disorders related to ENPP1.
    Type: Grant
    Filed: March 23, 2022
    Date of Patent: June 13, 2023
    Assignee: NANJING ZHENGXIANG PHARMACEUTICALS CO., LTD.
    Inventor: Xiaolin Hao
  • Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4,4-dimethylpent-2-enenitrile
    Patent number: 11667641
    Abstract: Crystalline forms of Compound (I): are disclosed. Pharmaceutical compositions comprising the same, methods of inhibiting BTK using the same, and methods for making crystalline forms of Compound (I) are also disclosed.
    Type: Grant
    Filed: January 7, 2021
    Date of Patent: June 6, 2023
    Assignee: Principia Biopharma Inc.
    Inventors: Pasit Phiasivongsa, Jiang Zhu, Kolbot By, Mohammad Reza Masjedizadeh
  • Phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds for the treatment of pancreatic cancer
    Patent number: 11655214
    Abstract: The present invention provides phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds, such as compounds of formula I: pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat physiological disorders such as pancreatic cancer.
    Type: Grant
    Filed: April 11, 2018
    Date of Patent: May 23, 2023
    Assignee: ELI LILLY AND COMPANY
    Inventors: Marta Maria Cifuentes-Garcia, Maria Cristina Garcia Paredes
  • Substituted piperazines as BTK inhibitors
    Patent number: 11655254
    Abstract: Provided are heteroaryl heterocyclic compounds of formula (I), pharmaceutical compositions comprising same, methods for preparing same, and uses thereof, wherein the variables are as defined in the description. The compounds are Btk inhibitors.
    Type: Grant
    Filed: April 25, 2022
    Date of Patent: May 23, 2023
    Assignee: HUTCHISON MEDIPHARMA LIMITED
    Inventors: Guangxiu Dai, Kun Xiao
  • Crystal form a of (5-amino-8-(2-methyl-6-(trifluoromethyl)pyridin-4-yl)-7-phenyl-[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)methanol (compound 1)
    Patent number: 11649239
    Abstract: Disclosed in the present invention are a crystal form of a [1,2,4]triazolo[1,5-c]pyrimidine compound and a preparation method thereof. Further disclosed is a use of the crystal form in the preparation of a medicament for treating A2A receptor related diseases.
    Type: Grant
    Filed: April 28, 2019
    Date of Patent: May 16, 2023
    Assignee: Medshine Discovery Inc.
    Inventors: Kevin X. Chen, Yanxin Yu, Xinde Chen, Li Zhang, Zhaoguo Chen, Cheng Xie
  • Substituted pyrido[2,3-d]pyrimidines as inhibitors of Ras pathway signaling
    Patent number: 11648254
    Abstract: The present disclosure provides compounds represented by Formula (I-1): and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic proteins.
    Type: Grant
    Filed: March 2, 2022
    Date of Patent: May 16, 2023
    Assignee: Kumquat Biosciences Inc.
    Inventors: Baogen Wu, Xiangzhu Wang, Xiaoming Li, Zhiyong Chen, Pingda Ren, Yi Liu
  • Substituted imidazo[1,5-a]pyrazines for IRE1 inhibition
    Patent number: 11649237
    Abstract: Provided herein, inter alia, are substituted imidazo[1,5-?]pyrazine compounds, compositions and methods for treating or preventing an IRE1?-related disease or disorder. In certain embodiments, the disease or disorder is selected from the group consisting of a neurodegenerative disease, a demyelinating disease, cancer, an eye disease, a fibrotic disease, and diabetes.
    Type: Grant
    Filed: August 31, 2018
    Date of Patent: May 16, 2023
    Assignees: Optikira LLC, The Regents of the University of California
    Inventors: Richard M. Keenan, Bradley J. Backes, Dustin J. Maly, Charles Reynolds, Ben Whittaker, Jamie Knight, Jonathan Mark Sutton, George Hynd, Feroz R. Papa, Scott A. Oakes
  • Substituted pyrazolo[1,5-a]pyrimidines as PI4K inhibitors
    Patent number: 11649238
    Abstract: The invention relates to compounds of formula (I) which are inhibitors of kinase activity, pharmaceutical formulations containing the compounds and their uses in treating and preventing viral infections and disorders caused or exacerbated by the viral infection wherein R1, R2, R3, R4a, R4b, R4c, R5, W, X, Y and Z are defined herein.
    Type: Grant
    Filed: January 15, 2019
    Date of Patent: May 16, 2023
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Nicholas Paul Barton, Sophie Marie Bertrand, Kenneth David Down, Matthew Gray
  • Substituted 1?,2?-dihydro-3?H-spiro[cyclohexane-1,4?-pyrimido[5?,4?:4,5]pyrrolo[2,1-c][1,2,4]triazin]-3?-ones as cyclin-dependent kinase inhibitors
    Patent number: 11643416
    Abstract: This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.
    Type: Grant
    Filed: May 11, 2022
    Date of Patent: May 9, 2023
    Assignee: G1 Therapeutics, Inc.
    Inventor: Jay Copeland Strum
  • Substituted imidazo[1,2-a]pyrazines and pyrazino[1,2-a]pyrimidines as topical agents for dermatological applications
    Patent number: 11639356
    Abstract: Provided are compounds of formula (I): or cosmeceutically acceptable or pharmaceutically acceptable salts thereof. Additionally provided are cosmeceutical and/or pharmaceutical compositions comprising the compounds of formula (I), or the cosmeceutically acceptable or pharmaceutically acceptable salts thereof. Also provided are therapeutic and/or cosmetic methods using the cosmeceutical and/or pharmaceutical compositions comprising the compounds of formula (I), or the cosmeceutically acceptable or pharmaceutically acceptable salts thereof, for modulating cyclic adenosine monophosphate response element binding (CREB)-binding protein (CBP)/?-catenin mediated signaling in treating skin related diseases, conditions, or disorders mediated by aberrant CBP/?-catenin signaling and cosmetic methods for treating skin conditions mediated by aberrant CBP/?-catenin signaling.
    Type: Grant
    Filed: October 1, 2021
    Date of Patent: May 2, 2023
    Assignee: Genesis Molecular Technologies, Inc.
    Inventor: Fuqiang Ruan
  • Substituted pyrrolo[3,4-d]imidazoles as MDM2-p53 inhibitors
    Patent number: 11639355
    Abstract: Disclosed is a novel class of MDM2-p53 inhibitor compounds having an imidaxopyrolone structure, and specifically disclosed are compounds represented by formulas (I-1) and (I-2) and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 12, 2019
    Date of Patent: May 2, 2023
    Assignees: LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD., SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD., MEDSHINE DISCOVERY INC.
    Inventors: Kevin X Chen, Xiaobing Yan, Jianglei Huang, Yuekun Nie, Guoping Hu, Jian Li, Shuhui Chen, Jiaqiang Dong, Tie-Lin Wang
  • Substituted pyrazolo[1,5-a]pyrimidines as inhibitors of interferon signaling
    Patent number: 11634423
    Abstract: The present invention provides a compound of Formula I: wherein R is or a pharmaceutically acceptable salt thereof, useful for treating psoriasis, systemic lupus erythematosus, or type 1 diabetes.
    Type: Grant
    Filed: February 5, 2021
    Date of Patent: April 25, 2023
    Assignee: Eli Lilly and Company
    Inventors: Thomas John Bleisch, Zhaogen Chen, Theodore Curtis Jessop
  • Substituted pyrazolo[1,5-a]pyrazines as negative allosteric modulators of group II metabotropic glutamate receptor
    Patent number: 11633395
    Abstract: Provided are a compound that is useful for the prevention of and/or as a treatment agent for a disease in which a group II mGlu receptor is involved; and a medical application of said compound. Provided is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 22, 2018
    Date of Patent: April 25, 2023
    Assignee: SUMITOMO PHARMA CO., LTD.
    Inventors: Yohei Ikuma, Kengo Tojo, Ryo Fukazawa, Shuji Masumoto
  • Process for the synthesis of linker-drug vc-seco-DUBA
    Patent number: 11633492
    Abstract: The compound of formula (II) is an advantageous intermediate for improving the process of synthesizing the linker-drug vc-seco-DUBA, as well as for the overall process for preparing an antibody-drug conjugate comprising the vc-seco-DUBA linker-drug. The methods of making the compound of formula (II) can include recovery of the compound as a solid, such as via crystallization, in high yields and purity.
    Type: Grant
    Filed: November 22, 2018
    Date of Patent: April 25, 2023
    Assignee: Byondis B.V.
    Inventors: Vladimir Janousek, Martin Kas
  • Substituted pyrrolo[3,4-d]imidazoles as JAK inhibitors
    Patent number: 11629148
    Abstract: The present disclosure relates to substituted pyrrollo[3,4-D]imidazoles as JAK inhibitor compounds and uses thereof. Specifically, the present disclosure discloses a compound represented by formula (I), optical isomer thereof, geometric isomer thereof, a tautomer thereof or a mixture of various isomers, or a pharmaceutically acceptable salt thereof, or a prodrug thereof, or a metabolite thereof. The present disclosure also relates to the application of the compounds in the treatment of JAK-related diseases or disorders.
    Type: Grant
    Filed: August 24, 2021
    Date of Patent: April 18, 2023
    Assignee: HENAN MEDINNO PHARMACEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Liang Lu, Hai Huang, Longzheng Zhang, Saisai Zhao, Jixuan Zhang
  • Antibody-drug conjugates comprising substituted benzo[e]pyrrolo[1,2-?][1,4]diazepines
    Patent number: 11628223
    Abstract: A novel antibody-pyrrolodiazepine derivative and a novel antibody-pyrrolodiazepine derivative conjugate using the same, comprising substituted benzo[e]pyrrolo[1,2-a][1,4]diazepines represented by the [Formula 24], [Formula 25], [Formula 26], and/or [Formula 27].
    Type: Grant
    Filed: September 28, 2018
    Date of Patent: April 18, 2023
    Assignee: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Narihiro Toda, Yusuke Ota, Fuminao Doi, Masaki Meguro, Ichiro Hayakawa, Shinji Ashida, Takeshi Masuda, Takashi Nakada, Mitsuhiro Iwamoto, Naoya Harada, Tomoko Terauchi, Daisuke Okajima, Kensuke Nakamura, Hiroaki Uchida, Hirofumi Hamada
  • Substituted [1,2,4]triazolo[4,3-a]pyrazines as modulators of sodium channel activity
    Patent number: 11629146
    Abstract: The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.
    Type: Grant
    Filed: November 28, 2017
    Date of Patent: April 18, 2023
    Assignee: PRAXIS PRECISION MEDICINES, INC.
    Inventors: Kiran Reddy, Gabriel Martinez Botella, Andrew Mark Griffin, Brian Edward Marron
  • Substituted [1,2,4]triazolo[1,5-a]pyrimidines for stabilizing microtubules
    Patent number: 11623927
    Abstract: The present disclosure provides compounds of formula (I) or (II) or a pharmaceutically acceptable salt or stereoisomer thereof, wherein Rx-R8 are defined herein. Also provided are compositions comprising a compound described herein and a pharmaceutically effective excipient, methods of stabilizing microtubules in a patient comprising administering to the patient a microtubule-stabilizing amount of a compound described herein, methods of treating cancer in a patient comprising administering to the patient a therapeutically effective amount of a compound described herein, and methods of treating a neurodegenerative disease in a patient comprising administering to the patient a therapeutically effective amount of a compound described herein.
    Type: Grant
    Filed: February 28, 2019
    Date of Patent: April 11, 2023
    Assignees: The Trustees of the University of Pennsylvania, The Regents of the University of California
    Inventors: Kurt R. Brunden, Virginia M. Y. Lee, John Q. Trojanowski, Carlo Ballatore, Killian Oukoloff, Amos B. Smith, III
  • Aminopyrrolotriazines as kinase inhibitors
    Patent number: 11618753
    Abstract: The disclosure relates to compounds of formula I which are useful as kinase modulators including RIPK 1 modulation. The disclosure also provides methods of making and using the compounds for example in treatments related to necrosis or inflammation as well as other indications.
    Type: Grant
    Filed: January 24, 2019
    Date of Patent: April 4, 2023
    Assignee: Bristol-Myers Squibb Company
    Inventors: Scott Hunter Watterson, Murugaiah Andappan Murugaiah Subbaiah, Carolyn Diane Dzierba, Hua Gong, Jason M. Guernon, Junqing Guo, Amy C. Hart, Guanglin Luo, John E. Macor, William J. Pitts, Jianliang Shi, Brian Lee Venables, Carolyn A. Weigelt, Yong-Jin Wu, Zhizhen Barbara Zheng, Sing-Yuen Sit, Jie Chen
  • Substituted imidazo[1,5-a]pyrazines for modulation of IRE1
    Patent number: 11613544
    Abstract: Described herein, inter alia, are certain substituted imidazo[1,5-a]pyrazines of formula (I) and methods of using the same for modulating the activity of Ire1.
    Type: Grant
    Filed: September 24, 2020
    Date of Patent: March 28, 2023
    Assignees: The Regents of the University of California, University of Washington Through Its Center For Commercialization
    Inventors: Bradley J. Backes, Dustin J. Maly, Scott A. Oakes, Feroz R. Papa, Gayani Perera, Likun Wang