Patents by Inventor Nathanael S. Gray

Nathanael S. Gray has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20240034726
    Abstract: Provided herein are 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 disclosed compounds or compositions for treating and/or preventing diseases (e.g., inflammatory diseases, neurological diseases (e.g., Alzheimer's disease), infectious diseases (e.g., viral infections (e.g., infections caused by viral human hepatitis (e.g., hepatitis B), a flaviviridae family virus (e.g., a flavivims (e.g., Zika virus)))), and proliferative diseases (e.g., cancer (e.g., lung cancer, prostate cancer, skin cancer, thyroid cancer, pancreatic cancer, colorectal cancer, liver cancer, leukemia, or lymphoma)) in a subject. Provided are methods of inhibiting a protein kinase (e.g., MAP2K (e.g., MKK7)) in a subject. Also provided are methods of inhibiting MKK7 in a subject in need thereof.
    Type: Application
    Filed: February 25, 2021
    Publication date: February 1, 2024
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Steven P. Treon, Jinhua Wang, Li Tan, Guang Yang
  • Patent number: 11878019
    Abstract: The present disclosure provides methods of increasing skin pigmentation in a subject in need thereof using salt-inducible kinase (SIK) inhibitors, such as macrocyclic compounds of Formula (I), bicyclic urea compounds of Formula (II), (III), and (IV), and compounds of Formula (V), (VI), (VI-A), or (VII). Also provided are pharmaceutical compositions, methods, and uses that include or involve a compound described herein.
    Type: Grant
    Filed: November 22, 2021
    Date of Patent: January 23, 2024
    Assignees: The General Hospital Corporation, Dana-Farber Cancer Institute, Inc.
    Inventors: David E. Fisher, Nisma Mujahid, Ryo Murakami, Nathanael S. Gray, Yanke Liang, Hwan Geun Choi
  • Patent number: 11858897
    Abstract: The application relates to a compound of Formula (I): which modulates the activity of ALK or SRPK, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which ALK or SRPK plays a role.
    Type: Grant
    Filed: June 15, 2021
    Date of Patent: January 2, 2024
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: John Hatcher, Nathanael S. Gray, Hwangeun Choi, Pasi Janne, Tinghu Zhang
  • Publication number: 20230399304
    Abstract: The present disclosure relates to compounds that are capable of inhibiting creatine kinase. The present disclosure also relates to methods of treating cancer, such as hematological malignancies.
    Type: Application
    Filed: October 22, 2021
    Publication date: December 14, 2023
    Inventors: Nathanael S. Gray, Edward Chouchani, Tinghu Zhang, Narek Darabedian, Wenzhi JI, Jianwei Che
  • Publication number: 20230391768
    Abstract: The present disclosure provides compounds of Formula (I?) (e.g., compounds of Formula (I)), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be kinase (e.g., Janus kinase (JAK), e.g., Janus kinase 2 (JAK2)) inhibitors. Also provided are pharmaceutical compositions and kits including the provided compounds. Further provided are methods of using the provided compounds, pharmaceutical compositions, and kits (e.g., for treating a disease (e.g., proliferative disease) in a subject in need thereof).
    Type: Application
    Filed: November 7, 2019
    Publication date: December 7, 2023
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Tinghu Zhang, Yao Liu, Zhixiang He, Mingfeng Hao, David Weinstock, Loretta Sze-Mun Li
  • Patent number: 11827636
    Abstract: The present application provides bifunctional compounds of Formula (Ia) or (Ib): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 8 (CDK8). The present application also relates to methods for the targeted degradation of CDK8 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK8 which can be utilized in the treatment of disorders modulated by CDK8.
    Type: Grant
    Filed: December 23, 2021
    Date of Patent: November 28, 2023
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Tinghu Zhang, Calla M. Olson, Yanke Liang, Nicholas Kwiatkowski
  • Patent number: 11826365
    Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
    Type: Grant
    Filed: June 4, 2020
    Date of Patent: November 28, 2023
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Hwan Geun Choi, Xianming Deng, Jianming Zhang
  • Publication number: 20230365620
    Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts thereof are provided and methods involving compounds of Formula (I) as effective inhibitors of CDK8 and/or CDK19 are also provided.
    Type: Application
    Filed: May 8, 2023
    Publication date: November 16, 2023
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, John Hatcher
  • Patent number: 11814379
    Abstract: The application relates to a compound having Formula I: which modulates the activity of HER2 and/or a mutant thereof, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which HER2 and/or a mutant thereof plays a role.
    Type: Grant
    Filed: June 14, 2019
    Date of Patent: November 14, 2023
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Jaebong Jang, Pasi Janne, Jieun Son
  • Publication number: 20230357222
    Abstract: Disclosed are bispecific compounds (degraders) that target cereblon (CRBN) for degradation. Also disclosed are pharmaceutical compositions containing the degraders and methods of using the compounds as research tools and to reduce adverse side effects associated with a cereblon targeted therapy.
    Type: Application
    Filed: March 16, 2021
    Publication date: November 9, 2023
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Zhixiang He, Tinghu Zhang, Chelsea Powell, Eric S. Fischer, Jonathan Bushman, Guangyan Du
  • Patent number: 11807606
    Abstract: DCAF15 is a substrate recognition (adaptor) protein of E3 ubiquitin ligase. Disclosed herein are compounds that recruit ubiquitin ligase CRL4DCAF15, to a target RNA recognition motif (RRM), causing its degradation. Also disclosed herein are compositions and methods of use in treating associated disorders and diseases.
    Type: Grant
    Filed: January 24, 2019
    Date of Patent: November 7, 2023
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Eric Fischer, Hojong Yoon, Tinghu Zhang, Tyler Faust, Katherine Donovan, Quan Cai, Zhengnian Li
  • Publication number: 20230348434
    Abstract: The application relates to a compound having Formula (I): which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role.
    Type: Application
    Filed: April 28, 2023
    Publication date: November 2, 2023
    Inventors: Nathanael S. Gray, Pasi Janne, Hwan Geun Choi, Jaebong Jang
  • Publication number: 20230338551
    Abstract: The present application provides bifunctional compounds of Formula (X): or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for Bruton's tyrosine kinase (BTK). The present application also relates to methods for the targeted degradation of BTK through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BTK which can be utilized in the treatment of disorders modulated by BTK.
    Type: Application
    Filed: June 27, 2023
    Publication date: October 26, 2023
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Dennis Dobrovolsky, Hai-Tsang Huang
  • Publication number: 20230339865
    Abstract: The present disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be kinase (e.g., HCK, BTK, LYN) inhibitors. Also provided are pharmaceutical compositions and kits including the provided compounds. Further provided are methods of using the provided compounds, pharmaceutical compositions, and kits (e.g., for treating diseases (e.g., proliferative diseases) in a subject in need thereof).
    Type: Application
    Filed: June 3, 2021
    Publication date: October 26, 2023
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Steven P. Treon, Sara Jean Buhrlage, Guang Yang, Jinhua Wang, Li Tan, Zachary R. Hunter
  • Publication number: 20230339922
    Abstract: The disclosure relates to compounds that act as covalent inhibitors of epidermal growth factor receptor (EGFR); pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.
    Type: Application
    Filed: March 28, 2023
    Publication date: October 26, 2023
    Inventors: NATHANAEL S. GRAY, ZHENGNIAN LI, JIANWEI CHE, TINGHU ZHANG
  • Publication number: 20230331721
    Abstract: Disclosed are to compounds, compositions, and methods for treating diseases or conditions mediated by aberrant serine-arginine protein kinase (SRPK) 1 and SRPK2 activity.
    Type: Application
    Filed: October 5, 2021
    Publication date: October 19, 2023
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, John Hatcher
  • Publication number: 20230295137
    Abstract: The disclosure relates to compounds that act as covalent inhibitors of epidermal growth factor receptor (EGFR); pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.
    Type: Application
    Filed: March 28, 2023
    Publication date: September 21, 2023
    Inventors: ZHENGNIAN LI, JIANWEI CHE, TINGHU ZHANG, NATHANAEL S. GRAY
  • Publication number: 20230295167
    Abstract: Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that that are potent and selective inhibitors of HER2. Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds to treat diseases and disorders associated with HER2.
    Type: Application
    Filed: October 4, 2021
    Publication date: September 21, 2023
    Inventors: Nathanael S. Gray, John M. Hatcher, Alyssa Verano
  • Publication number: 20230271932
    Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds of Formula (I) are useful for activating uncoupling protein 1 (UCP1) dependent thermogenesis. Also disclosed herein are methods of treating obesity or metabolic disorders such as diabetes using a compound of Formula (I).
    Type: Application
    Filed: June 16, 2021
    Publication date: August 31, 2023
    Inventors: Nathanael S. Gray, Mengyang Fan, Martha Ordonez, Edward Chouchani, Tinghu Zhang, Zhengnian LI, Jianwei Che
  • Patent number: 11730818
    Abstract: The present application provides bifunctional compounds of Formula (X): or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for Bruton's tyrosine kinase (BTK). The present application also relates to methods for the targeted degradation of BTK through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BTK which can be utilized in the treatment of disorders modulated by BTK.
    Type: Grant
    Filed: December 16, 2020
    Date of Patent: August 22, 2023
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Dennis Dobrovolsky, Hai-Tsang Huang