19 patents
Utility
Pyridine, pyrazine, and triazine compounds as allosteric SHP2 inhibitors
18 Jul 23
The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease.
Jie Jack Li, Elena S. Koltun, Adrian Liam Gill, Andreas Buckl, Walter Won, Naing Aay, Kevin Mellem, Christos Tzitzilonis, Ashutosh Jogalekar, James Joseph Cregg
Filed: 10 Apr 20
Utility
Ras inhibitors
4 Jul 23
The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.
Naing Aay, G. Leslie Burnett, James Cregg, Adrian L. Gill, John E. Knox, Elena S. Koltun, Yang Liu, Andreas Buckl, Bianca Jennifer Lee, David E. Wildes, Meghan A. Rice, Mallika Singh
Filed: 15 Sep 21
Utility
C26-linked rapamycin analogs as mTOR inhibitors
27 Jun 23
The present disclosure relates to mTOR inhibitors.
Christopher Michael Semko, Gang Wang, G. Leslie Burnett, James Bradley Aggen, Gert Kiss, James Joseph Cregg, Micah James Evans Gliedt, Jennifer Pitzen, Julie Chu-Li Lee, Walter Won, Arun P. Thottumkara, Adrian Liam Gill
Filed: 30 Oct 20
Utility
2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric SHP2 inhibitors
30 May 23
The present disclosure is directed to inhibitors of SHP2, such as pyrazine compounds, and their use in the treatment of disease associated with SHP2 modulation, such as Noonan Syndrome, Leopard Syndrome, juvenile myelomonocytic leukemias, neuroblastoma, melanoma, acute myeloid leukemia and cancers of the breast, lung and colon.
Elena S. Koltun, Kevin Mellem, Adrian Gill, Gert Kiss, Christopher Semko, Naing Aay, Andreas Buckl, Ashutosh Jogalekar, Walter Won
Filed: 18 Jun 20
Utility
Identifying new therapeutic agents
9 May 23
Disclosed herein are methods for identifying novel drug candidates.
Gregory L. Verdine, David W. White, David M. Armistead, Deborah J. Palestrant, Brian Y. Chow, Chris K. Varma, Mathew Edward Sowa
Filed: 21 Dec 20
Utility
Polycyclic compounds as allosteric SHP2 inhibitors
25 Apr 23
The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease.
Elena S. Koltun, Naing N. Aay, Andreas Buckl, Kevin T. Mellem, Brian R. Blank, Jennifer Pitzen, Gang Wang, Ashutosh S. Jogalekar, Walter S. Won, Christos Tzitzilonis, Jie Jack Li, Adrian Liam Gill, James Joseph Cregg
Filed: 11 Jun 20
Utility
Ras inhibitors
21 Mar 23
The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.
Elena S. Koltun, James Cregg, Adrian L. Gill
Filed: 4 Nov 20
Utility
SHP2 inhibitor compositions and methods for treating cancer
7 Mar 23
The present invention is directed to compositions and methods of treating or preventing diseases or disorders with inhibitors of SHP2, alone, and in combination with other therapeutic agents such as RAS pathway inhibitors (e.g., MEK inhibitors); methods of establishing appropriate treatment plans for subjects based upon the expression of one or more biomarker indicative of SHP2 inhibitor sensitivity; and methods of determining sensitivity to a SHP2 inhibitor based on a phosphorylation status of SHP2.
Robert J. Nichols, Mark A. Goldsmith, Christopher Schulze, Jacqueline Smith, David E. Wildes, Stephen Kelsey, Mallika Singh
Filed: 5 Mar 20
Utility
Ras inhibitors
31 Jan 23
The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.
Elena S. Koltun, James Cregg, Adrian L. Gill, Andreas Buckl, Yang Liu
Filed: 4 Nov 20
Utility
C40-, C28-, and C-32-linked rapamycin analogs as mTOR inhibitors
21 Jun 22
The present disclosure relates to mTOR inhibitors.
Jennifer Pitzen, G. Leslie Burnett, James Bradley Aggen
Filed: 28 Oct 20
Utility
Solid forms of {6-[(2-amino-3-chloropyridin-4-yl)sulfanyl]-3-[(3S,4S)-4-amino-3-methyl-2-oxa-8- azaspiro[4.5]decan-8-yl]-5-methylpyrazin-2-yl} methanol, a SHP2 inhibitor
11 Jan 22
The present disclosure relates to crystalline solid forms of {6-[(2-amino-3-chloropyridin-4-yl)sulfanyl]-3-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-methylpyrazin-2-yl}methanol, or a pharmaceutically acceptable salt thereof, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof.
Shaoling Li, Steven G. Ballmer
Filed: 26 Feb 21
Utility
Bicyclic heteroaryl compounds and uses thereof
9 Nov 21
Adrian L. Gill, Andreas Buckl, Elena S. Koltun, Naing Aay, Arlyn A. Tambo-ong, Severin Thompson, Micah James Gliedt, John E. Knox, James Cregg, Anne V. Edwards, Yang Liu, G. Leslie Burnett
Filed: 23 Dec 20
Utility
Compounds that participate in cooperative binding and uses thereof
13 Jul 21
The invention features compounds (e.g., macrocyclic compounds) capable of modulating biological processes, for ex ample through binding to a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein such as CEP250.
Gregory Lawrence Verdine, Brian Roger Bowman, Mathew Edward Sowa, Joshua Alan Van Dyke Blodgett, Keith Earl Robison, Dylan Talbot Stiles, Jay Paul Morgenstern, Sharon Ann Townson, Uddhav Kumar Shigdel
Filed: 2 Dec 19
Utility
Identifying new therapeutic agents
27 Apr 21
Disclosed herein are methods for identifying novel drug candidates.
Gregory L. Verdine, David W. White, David M. Armistead, Deborah J. Palestrant, Brian Y. Chow, Chris K. Varma, Mathew Edward Sowa
Filed: 20 Dec 18
Utility
Methods and reagents for analyzing protein-protein interfaces
16 Mar 21
The present disclosure provides methods and reagents useful for analyzing protein-protein interfaces such as interfaces between a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein.
Gregory L. Verdine, M. James Nichols, Sharon A. Townson, Uddhav Kumar Shigdel, Seung-Joo Lee, Dylan T. Stiles, Neville J. Anthony
Filed: 9 May 18
Utility
Compositions and methods for the production of compounds
2 Feb 21
The present disclosure provides nucleic acids encoding a Large ATP-binding regulator of the LuxR family (LAL) of transcription factors, vectors and host cells including such nucleic acids, and methods for producing compounds (e.g., polyketides or β-lactam compounds) with such nucleic acids, vectors, and/or host cells.
Brian R. Bowman, Joshua A. V. Blodgett, Gregory L. Verdine, Daniel C. Gray, Jay P. Morgenstern, Lucy Foulston, Keith Robison
Filed: 12 Apr 17
Utility
2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric SHP2 inhibitors
16 Mar 20
The present disclosure is directed to inhibitors of SHP2, such as pyrazine compounds, and their use in the treatment of disease associated with SHP2 modulation, such as Noonan Syndrome, Leopard Syndrome, juvenile myelomonocytic leukemias, neuroblastoma, melanoma, acute myeloid leukemia and cancers of the breast, lung and colon.
Elena S. Koltun, Kevin Mellem, Adrian Gill, Gert Kiss, Christopher Semko, Naing Aay, Andreas Buckl, Ashutosh Jogalekar, Walter Won
Filed: 19 Dec 18
Utility
Compounds that participate in cooperative binding and uses thereof
13 Jan 20
The invention features compounds (e.g., macrocyclic compounds) capable of modulating biological processes, for example through binding to a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein such as CEP250.
Gregory Lawrence Verdine, Brian Roger Bowman, Mathew Edward Sowa, Joshua Alan Van Dyke Blodgett, Keith Earl Robison, Dylan Talbot Stiles, Jay Paul Morgenstern, Sharon Ann Townson, Uddhav Kumar Shigdel
Filed: 7 Jan 16
Utility
Methods and reagents for analyzing protein-protein interfaces
4 Nov 19
The present disclosure provides methods and reagents useful for analyzing protein-protein interfaces such as interfaces between a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein.
Gregory L. Verdine, M. James Nichols, Sharon A. Townson, Uddhav Kumar Shigdel, Seung-Joo Lee, Dylan T. Stiles, Neville J. Anthony
Filed: 8 May 18
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