IP Library › Granted Patent US 12,624,043
Granted Patent B2
US 12,624,043 · App. 18/382,727 · Granted May 12, 2026

Compositions useful for treating disorders related to kit

Inventor: Brian L. Hodous (Cambridge, MA)
Assignee: Blueprint Medicines Corporation
C07D487/04A61K31/496A61K31/53A61K31/5377A61K45/06C07D401/14C07D403/04C07D403/14C07D413/14C07D417/14
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Quick Facts
Patent No.
US 12,624,043
App. No.
18/382,727
Granted
May 12, 2026
Kind
B2
Abstract

Compounds and compositions useful for treating disorders related to mutant KIT are described herein.

Claims (7)

1 . A compound having the structure:

or a pharmaceutically acceptable salt thereof.

2 . The compound of claim 1 ,

3 . A compound having the structure:

or a pharmaceutically acceptable salt thereof or a tautomer thereof or a pharmaceutically acceptable salt of the tautomer thereof.

4 . The compound of claim 3 ,

or a tautomer thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 19, 2024
From: HODOUS, BRIAN L.; KIM, JOSEPH L.; WILSON, KEVIN J.; WILSON, DOUGLAS; ZHANG, YULIAN
To: BLUEPRINT MEDICINES CORPORATION
Reel/Frame 066176/0761 →
Continuity (9)
Continuation 17983747 · Nov 9, 2022
Continuation 17070556 · Oct 14, 2020
Continuation 15973378 · May 7, 2018
Continuation 14887614 · Oct 20, 2015
Continuation 14515327 · Oct 15, 2014
Provisional Application 61975229 · Apr 4, 2014
Provisional Application 61931204 · Jan 24, 2014
Provisional Application 61892086 · Oct 17, 2013
Related Publication 20240317757A1 · Sep 26, 2024
References Cited (148)
US 6982265B1 · Hunt et al. · 2006 [cited by applicant]
US 7244733B2 · Hunt et al. · 2007 [cited by applicant]
US 8609672B2 · Russu et al. · 2013 [cited by applicant]
US 8802697B2 · Bifulco, Jr. et al. · 2014 [cited by applicant]
US 9126951B2 · Bifulco, Jr. et al. · 2015 [cited by applicant]
US 9200002B2 · Hodous et al. · 2015 [cited by applicant]
US 9334263B2 · Hodous et al. · 2016 [cited by applicant]
US 9340514B2 · Bifulco, Jr. et al. · 2016 [cited by applicant]
US 9434700B2 · Bifulco, Jr. et al. · 2016 [cited by applicant]
US 9499522B2 · DiPietro et al. · 2016 [cited by applicant]
US 9688680B2 · Hodous · 2017 [cited by applicant]
US 9695165B2 · Bifulco, Jr. et al. · 2017 [cited by applicant]
US 9884861B2 · Hodous et al. · 2018 [cited by applicant]
US 9944651B2 · Hodous et al. · 2018 [cited by applicant]
US 9994552B2 · DiPietro et al. · 2018 [cited by applicant]
US 9994575B2 · Hodous et al. · 2018 [cited by applicant]
US 10000490B2 · Bifulco, Jr. et al. · 2018 [cited by applicant]
US 10000496B2 · Hodous et al. · 2018 [cited by applicant]
US 10017512B2 · Wenglowsky et al. · 2018 [cited by applicant]
US 10030005B2 · Brubaker et al. · 2018 [cited by applicant]
US 10035789B2 · Brubaker et al. · 2018 [cited by applicant]
US 10202365B2 · Brooijmans et al. · 2019 [cited by applicant]
US 10227329B2 · Brubaker et al. · 2019 [cited by applicant]
US 10584114B2 · Brubaker et al. · 2020 [cited by applicant]
US 10807985B2 · Hodous et al. · 2020 [cited by applicant]
US 11046697B2 · Wenglowsky et al. · 2021 [cited by applicant]
US 11827642B2 · Hodous et al. · 2023 [cited by applicant]
US 11964980B2 · Waetzig et al. · 2024 [cited by applicant]
US 11999744B2 · Waetzig et al. · 2024 [cited by applicant]
US 20040186140A1 · Cherney et al. · 2004 [cited by applicant]
US 20060211695A1 · Borzilleri et al. · 2006 [cited by applicant]
US 20140187559A1 · Miduturu · 2014 [cited by applicant]
US 20160031892A1 · Hodous · 2016 [cited by applicant]
US 20160102097A1 · Hodous et al. · 2016 [cited by applicant]
US 20170022206A1 · Hodous et al. · 2017 [cited by applicant]
US 20170029409A1 · DiPietro et al. · 2017 [cited by applicant]
US 20170066773A1 · Wenglowsky et al. · 2017 [cited by applicant]
US 20170066812A1 · Bifulco, Jr. et al. · 2017 [cited by applicant]
US 20170119760A1 · Moussy et al. · 2017 [cited by applicant]
US 20170121312A1 · Brubaker et al. · 2017 [cited by applicant]
US 20170145018A1 · Wenglowsky et al. · 2017 [cited by applicant]
US 20170174652A1 · Bifulco, Jr. et al. · 2017 [cited by applicant]
US 20170204104A1 · Hodous et al. · 2017 [cited by applicant]
US 20170253593A1 · Bifulco, Jr. et al. · 2017 [cited by applicant]
US 20170267661A1 · Kim et al. · 2017 [cited by applicant]
US 20170298069A1 · Brooijmans et al. · 2017 [cited by applicant]
US 20180022731A1 · Brooijmans et al. · 2018 [cited by applicant]
US 20180022732A1 · Brubaker et al. · 2018 [cited by applicant]
US 20180362613A1 · Bifulco, Jr. et al. · 2018 [cited by applicant]
US 20190119280A1 · Hodous et al. · 2019 [cited by applicant]
US 20200024280A1 · Hodous et al. · 2020 [cited by applicant]
US 20210147433A1 · Waetzig et al. · 2021 [cited by applicant]
US 20210284645A1 · Hodous et al. · 2021 [cited by applicant]
US 20220010382A1 · Schmidt-Kittler · 2022 [cited by applicant]
US 20220370465A1 · Mar et al. · 2022 [cited by applicant]
US 20230124801A1 · Mar · 2023 [cited by applicant]
US 20240075041A1 · Mar · 2024 [cited by applicant]
CN 101007814A · 2007 [cited by applicant]
CN 102040494A · 2011 [cited by applicant]
CN 103261165A · 2013 [cited by applicant]
CN 105658652A · 2016 [cited by applicant]
CN 108191874A · 2018 [cited by applicant]
CN 110003217A · 2019 [cited by applicant]
CN 110938077A · 2020 [cited by applicant]
CN 110950872A · 2020 [cited by applicant]
CN 112223217A · 2021 [cited by applicant]
EP 0200968A1 · 1986 [cited by applicant]
JP 2003519698A · 2003 [cited by applicant]
JP 2005503372A · 2005 [cited by applicant]
JP 2006519205A · 2006 [cited by applicant]
JP 2007535558A · 2007 [cited by applicant]
JP 2008504366A · 2008 [cited by applicant]
JP 2009514882A · 2009 [cited by applicant]
JP 2009542814A · 2009 [cited by applicant]
JP 2016538257A · 2016 [cited by applicant]
JP 6446040B2 · 2018 [cited by applicant]
JP 2019522051A · 2019 [cited by applicant]
RU 2331640C2 · 2008 [cited by applicant]
WO WO2000071129A1 · 2000 [cited by applicant]
WO WO0071129A1 · 2000 [cited by examiner]
WO WO2001025220A1 · 2001 [cited by applicant]
WO WO200174821A1 · 2001 [cited by applicant]
WO WO2003010158A1 · 2003 [cited by applicant]
WO WO2003090912A1 · 2003 [cited by applicant]
WO WO2004071460A2 · 2004 [cited by applicant]
WO WO2004076450A1 · 2004 [cited by applicant]
WO WO2005117909A2 · 2005 [cited by applicant]
WO WO2006004636A2 · 2006 [cited by applicant]
WO WO2006028524A2 · 2006 [cited by applicant]
WO WO2007056170A2 · 2007 [cited by applicant]
WO WO2007065100A1 · 2007 [cited by applicant]
WO WO2007085188A1 · 2007 [cited by applicant]
WO WO2008005956A2 · 2008 [cited by applicant]
WO WO2009015254A1 · 2009 [cited by applicant]
WO WO2009117157A1 · 2009 [cited by applicant]
WO WO2010002095A2 · 2010 [cited by applicant]
WO WO2010022055A2 · 2010 [cited by applicant]
WO WO2010144345A1 · 2010 [cited by applicant]
WO WO2011005119A1 · 2011 [cited by applicant]
WO WO2011103196A1 · 2011 [cited by applicant]
WO WO2012027495A1 · 2012 [cited by applicant]
WO WO2014039714A2 · 2014 [cited by applicant]
WO WO2014100620A2 · 2014 [cited by applicant]
WO WO2014160521A1 · 2014 [cited by applicant]
WO WO2015057873A1 · 2015 [cited by applicant]
WO WO2015058129A1 · 2015 [cited by applicant]
WO WO2016022569A1 · 2016 [cited by applicant]
WO WO2017019442A1 · 2017 [cited by applicant]
WO WO2018049233A1 · 2018 [cited by applicant]
WO WO2018183712A1 · 2018 [cited by applicant]
WO WO2019034128A1 · 2019 [cited by applicant]
WO WO2019152719A1 · 2019 [cited by applicant]
Antonescu, What lessons can be learned from the GIST paradigm that can be applied to other kinase-driven cancers. J Pathol. Jan. 2011;223(2):251-261. [cited by applicant]
Bennett et al., Cecil Textbook of Medicine, 20th Edition, vol. 1, W.B. Saunders Company, Philadelphia. pp. 1004-1010, (1996). [cited by applicant]
Broesby-Olsen et al., KIT D816V mutation burden does not correlate to clinical manifestations of indolent systemic mastocytosis. J Allergy Clin Immunol. Sep. 2013;132(3):723-728. [cited by applicant]
Cairoli et al., Prognostic impact of c-KIT mutations in core binding factor leukemias: an Italian retrospective study. Blood. May 1, 2006;107(9):3463-8. [cited by applicant]
Cohen, The development and therapeutic potential of protein kinase inhibitors. Curr Opin Chem Biol. Aug. 1999;3(4):459-65. [cited by applicant]
Corti et al., Differential activity of avapritinib in patients with metastases from mucosal melanoma and thymic carcinoma harbouring KIT exon 17 mutations: Initial experience from a Compassionate Use Program in Italy. E… [cited by applicant]
Deininger et al., Avapritinib (BLU-285). a Selective KIT Inhibitor, is Associated with High Response Rate and Tolerable Safety Profile in Advanced Systemic Mastocytosis: Results of a Phase 1 Study. Retrieved online at: … [cited by applicant]
Dermer, Another Anniversary for the War on Cancer. Bio/Technology. Mar. 1994;12:320. [cited by applicant]
Freshney, Culture of Animal Cells, a Manual of Basic Technique. Alan R. Liss, Inc. pp. 1-6, (1983). [cited by applicant]
Kawaguchi et al., Drug and crystal polymorphism. Journal of Human Environmental Engineering. 2002;4(2):310-317. [cited by applicant]
Kluin-Nelemans et al., Prognostic impact of eosinophils in mastocytosis: analysis of 2350 patients collected in the ECNM Registry. Leukemia. Apr. 2020;34(4):1090-1101. [cited by applicant]
Kovalszki et al., Eosinophilia in mast cell disease. Immunol Allergy Clin North Am. May 2014;34(2):357-64. [cited by applicant]
Kuang et al., Biologic Agents for the Treatment of Hypereosinophilic Syndromes. J Allergy Clin Immunol Pract. Nov.-Dec. 2017;5(6):1502-1509. [cited by applicant]
Lee et al., Correlation of imatinib resistance with the mutational status of KIT and PDGFRA genes in gastrointestinal stromal tumors: a meta-analysis. J Gastrointestin Liver Dis. Dec. 2013;22(4):413-8. [cited by applicant]
Lubke et al., Inhibitory effects of midostaurin and avapritinib on myeloid progenitors derived from patients with KIT D816V positive advanced systemic mastocytosis. Leukemia. May 2019;33(5):1195-1205. [cited by applicant]
Martinelli et al., Hypereosinophilic Syndrome and Molecularly Targeted Therapy. Semin Hematol. 2007;44:S4-S16. [cited by applicant]
Mitsuhisa, Approach to Crystal Polymorph in Process Research of New Drugs. Journal of the Society for Synthetic Organic Chemistry. 2007;65(9):907-913. [cited by applicant]
Pardanani, Systemic mastocytosis in adults: 2019 update on diagnosis, risk stratification and management. Am J Hematol. Mar. 2019;94(3):363-377. [cited by applicant]
Paschka et al., Adverse prognostic significance of KIT mutations in adult acute myeloid leukemia with inv(16) and t(8;21): a Cancer and Leukemia Group B Study. J Clin Oncol. Aug. 20, 2006;24(24):3904-11. [cited by applicant]
Pharmaceutical Affairs Bureau No. 568, Establishment of Specifications and Test Methods for New Drugs. 106 pages, May 1, 2001. [cited by applicant]
Quintela et al., A Ready One-pot Preparation for Pyrrolo[2,1-f]-[1,2,4]triazine and Pyrazolo[5, 1-c]pyrimido[4,5-e]-[1,2,4]triazine Derivatives. Tetrahedron. 1996;52(8):3037-3048. [cited by applicant]
Radia, Avapritnib, A Potent and Selective Inhibitor of KIT D816 V, Induces Complete and Durable Responses in Patients (PTS) with Advanced Systemic Mastocytosis (ADVSM). HemaSphere. 2019;3(S1):368-369. [cited by applicant]
Schnittger et al., KIT-D816 mutations in AML1-ETO-positive AML are associated with impaired event-free and overall survival. Blood. 2006;107:1791-1799. [cited by applicant]
Schwaab et al., KIT D816V and JAK2 V617F mutations are seen recurrently in hypereosinophilia of unknown significance. Am J Hematol. Sep. 2015;90(9):774-7. [cited by applicant]
Shallal et al., Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. Eur J Med Chem. Jun. 2011;46(6):2043-57. [cited by applicant]
Vaes et al., Targeted Treatment Options in Mastocytosis. Front Med (Lausanne). Jul. 20, 2017;4:110, 12 pages. [cited by applicant]
Vojvodic et al., Melanoma and Mastocytosis. Open Access Maced J Med Sci. Aug. 30, 2019;7(18):3050-3052. [cited by applicant]
Zhang et al., Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor. Proc Natl Acad Sci U S A. Apr. 2, 2013;110(14):5689-94. [cited by applicant]
Indian Office Action for Application No. 201617009956, dated Nov. 26, 2019, 7 pages. [cited by applicant]
International Search Report and Written Opinion for Application No. PCT/US2014/027008, dated Jul. 24, 2014, 11 pages. [cited by applicant]
International Search Report and Written Opinion for Application No. PCT/US2014/060746, dated Dec. 17, 2014, 8 pages. [cited by applicant]
International Search Report and Written Opinion for Application No. PCT/US2014/061211, dated Dec. 10, 2014, 9 pages. [cited by applicant]
International Search Report and Written Opinion for Application No. PCT/US2015/043624, dated Oct. 6, 2015, 7 pages. [cited by applicant]
International Search Report and Written Opinion for Application No. PCT/US2016/043301, dated Oct. 17, 2016, 10 pages. [cited by applicant]
International Search Report and Written Opinion for Application No. PCT/US2018/025193, dated May 30, 2018, 10 pages. [cited by applicant]
Japanese Office Action for Application No. 2018-224481, dated Mar. 30, 2020, 7 pages. [cited by applicant]