40 patents
Utility
Compounds useful as kinase inhibitors
28 Nov 23
This invention relates to novel compounds.
Nicolas Guisot
Filed: 12 Nov 21
Utility
Compounds Useful As Kinase Inhibitors
23 Nov 23
This invention relates to novel compounds.
Nicolas GUISOT
Filed: 31 Jul 23
Utility
Process for the preparation of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile
7 Nov 23
Charles Todd Eary, Stacey Spencer, Zack Crane, Katelyn Chando, Sylvie Asselin, Weidong Liu, Mike Welch, Adam Cook, Gabrielle R. Kolakowski, Andrew T. Metcalf, David A. Moreno, Tony P. Tang
Filed: 13 Aug 21
Utility
Processes and Intermediates for the Preparation of (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)-1-(1,1,1-TRIFLUOROPROPANE-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE
12 Oct 23
Alonso Jose ARGUELLES DELGADO, Charles Todd EARY, Jared Wade FENNELL, Scott Alan FRANK, Nicholas Andrew MAGNUS, Elizabeth Ann MCFADDIN, Roger Ryan ROTHHAAR, Stacey Renee SPENCER, Radhe Krishan VAID
Filed: 9 Sep 21
Utility
Osimertinib and Selpercatinib Combinations for the Treatment of Egfr- and Ret-associated Cancers
12 Oct 23
The present disclosure provides methods for treating patients with both EGFR- and RET-associated cancers with a combination of osimertinib and selpercatinib, in particular when treatment with the osimertinib leads to the development of fusions or mutations related to RET-associated cancers.
Alexander E. DRILON, Helena A. YU
Filed: 25 Aug 21
Utility
Crystalline Ret Inhibitor
6 Jul 23
Provided herein is a crystalline form of selpercatinib useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders, and methods of making this crystalline form.
Rajni Miglani BHARDWAJ, Jeremy Miles MERRITT, Jon Gordon SELBO, Shekhar Krishna VISWANATH
Filed: 9 Apr 21
Utility
Dosing of a Bruton's Tyrosine Kinase Inhibitor
9 Feb 23
The present invention provides a method of administering doses of the BTK inhibitor, (S)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropane-2-yl)-1H-pyrazole-4-carboxamide or a pharmaceutically acceptable salt thereof for use in treating conditions such as cancer and autoimmune diseases.
Barbara Jean BRANDHUBER, Nora Chien Yee KU, Nisha NANDA, Steven August SMITH, Donald TSAI
Filed: 3 Dec 20
Utility
Liquid formulations of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a] pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
1 Nov 22
A liquid formulation of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutically acceptable salts thereof, or a combination thereof and the use of the liquid formulation in the treatment of pain, cancer, inflammation, and certain infectious diseases are disclosed.
Mark Reynolds, Steven A Smith
Filed: 27 Apr 20
Utility
Compounds useful as kinase inhibitors
18 Oct 22
This invention relates to novel compounds.
Nicolas Guisot
Filed: 15 Dec 20
Utility
Formulations of 6-(2-HYDROXY-2-METHYLPROPOXY)-4-(6-(6-((6-METHOXYPYRIDIN-3-YL)METHYL)-3,6-DIAZABICYCLO[3.1.1]HEPTAN-3-YL)PYRIDIN-3-YL)PYRAZOLO[1,5-A]PYRIDINE-3-CARBONITRILE
30 Jun 22
6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile, or a pharmaceutically acceptable salt, amorphous form, polymorph form, or pharmaceutical composition (including solid formulations or liquid formulations) thereof and the use thereof for treating diseases and disorders which can be treated with a RET kinase inhibitor, such as RET-associated diseases and disorders, e.g., proliferative disorders such as cancers, including hematological cancers and solid tumors, and gastrointestinal disorders such as IBS are disclosed.
Mark REYNOLDS, Charles Todd EARY
Filed: 21 Jan 22
Utility
Formulations of 6-(2-HYDROXY-2-METHYLPROPOXY)-4-(6-(6-((6-METHOXYPYRIDIN-3-YL)METHYL)-3,6-DIAZABICYCLO[3.1.1]HEPTAN-3-YL)PYRIDIN-3-YL)PYRAZOLO[1,5-A]PYRIDINE-3-CARBONITRILE
24 Mar 22
6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile, or a pharmaceutically acceptable salt, amorphous form, polymorph form, or pharmaceutical composition (including solid formulations or liquid formulations) thereof and the use thereof for treating diseases and disorders which can be treated with a RET kinase inhibitor, such as RET-associated diseases and disorders, e.g., proliferative disorders such as cancers, including hematological cancers and solid tumors, and gastrointestinal disorders such as IBS are disclosed.
Mark REYNOLDS, Charles Todd EARY
Filed: 18 Nov 21
Utility
Methods of Diagnosing and Treating Cancer
24 Mar 22
A variety of different point mutations in NTRK1, NTRK2, and NTRK3 were identified in biopsy samples from a subjects having a variety of different cancers.
Brian B. Tuch, Joshua H. Bilenker
Filed: 23 Nov 21
Utility
Compounds Useful As Kinase Inhibitors
3 Mar 22
This invention relates to novel compounds.
Nicolas GUISOT
Filed: 12 Nov 21
Utility
Process for the preparation of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide and salts thereof
4 Jan 22
Mark Reynolds, Charles Todd Eary, Stacey Spencer, Derrick Juengst, Bruno Hache, Yutong Jiang, Julia Haas, Steven W. Andrews
Filed: 18 May 17
Utility
Process for the Preparation of 6-(2-HYDROXY-2-METHYLPROPOXY)-4-(6-(6-((6-METHOXYPYRIDIN-3-YL)METHYL)-3,6-DIAZABICYCLO[3.1.1]HEPTAN-3-YL)PYRIDIN-3-YL)PYRAZOLO[1,5-A]PYRIDINE-3-CARBONITRILE
9 Dec 21
Charles Todd EARY, Stacey SPENCER, Zack CRANE, Katelyn CHANDO, Sylvie ASSELIN, Weidong LIU, Mike WELCH, Adam COOK, Gabrielle R. KOLAKOWSKI, Andrew T. METCALF, David A. MORENO, Tony P. TANG
Filed: 13 Aug 21
Utility
Methods of treating pediatric cancers
7 Dec 21
A method of treating a pediatric cancer in a subject in need thereof.
Michael Cox, Nisha Nanda
Filed: 10 Jan 20
Utility
Spray-dried Dispersions, Formulations, and Polymorphs of (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)-1-(1,1,1-TRIFLUOROPROPAN-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE
28 Oct 21
A spray-dried dispersions and pharmaceutical composition of (S)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1H-pyrazole-4-carboxamide, pharmaceutically acceptable salts thereof, or a combination thereof and the use of the spray-dried dispersion and pharmaceutical composition in the treatment of cancer and autoimmune and inflammatory diseases are disclosed.
Barbara J. Brandhuber, Lauren T. Brent, Charles Todd Eary, Andrew Kenna, Firas Khan, Vivian F.H. Renshaw, Stacey Renee Spencer
Filed: 29 Jul 19
Utility
Process for the preparation of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbontrile
24 Aug 21
Charles Todd Eary, Stacey Spencer, Zack Crane, Katelyn Chando, Sylvie Asselin, Weidong Liu, Mike Welch, Adam Cook, Gabrielle R. Kolakowski, Andrew T. Metcalf, David A. Moreno, Tony P. Tang
Filed: 16 Jun 20
Utility
Process for the preparation of pyrazolo[1,5-a]pyrimidines and salts thereof
17 Aug 21
Qian Zhao, Stacey Spencer, Yutong Jiang, Julia Haas, Charles Todd Eary
Filed: 26 Oct 17
Utility
Point Mutations In TRK Inhibitor-resistant Cancer and Methods Relating to the Same
3 Jun 21
Provided herein are methods of treating a subject having a cancer, methods of selecting a treatment for a subject having a cancer, methods of selecting a subject having a cancer for a treatment that does not include a Trk inhibitor, methods of determining the likelihood that a subject having a cancer will have a positive response to a treatment with a Trk inhibitor, methods of predicting the efficacy of a Trk inhibitor in a subject having cancer, methods of determining a subject's risk for developing a Trk inhibitor-resistant cancer, and methods of determining the presence of a Trk inhibitor-resistant cancer in a subject, based on the detection of a cell from a sample from the subject that has at least one of the point mutations in NTRK1 and/or NTRK2 and/or NTRK3.
Nisha Nanda, Joshua H. Bilenker, James F. Blake, Gabrielle R. Kolakowski, Barbara J. Brandhuber, Steven W. Andrews
Filed: 1 Feb 21