WO2014176475A3 - Egfr inhibitors and uses thereof - Google Patents

Egfr inhibitors and uses thereof Download PDF

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Publication number
WO2014176475A3
WO2014176475A3 PCT/US2014/035391 US2014035391W WO2014176475A3 WO 2014176475 A3 WO2014176475 A3 WO 2014176475A3 US 2014035391 W US2014035391 W US 2014035391W WO 2014176475 A3 WO2014176475 A3 WO 2014176475A3
Authority
WO
WIPO (PCT)
Prior art keywords
egfr inhibitors
egfr
hsp90
proteins
inhibit
Prior art date
Application number
PCT/US2014/035391
Other languages
French (fr)
Other versions
WO2014176475A2 (en
Inventor
Mulkesh K. NYATI
Christopher Whitehead
Theodore S. LAWRENCE
Alnawaz RHEMTULLA
Original Assignee
The Regents Of The University Of Michigan
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by The Regents Of The University Of Michigan filed Critical The Regents Of The University Of Michigan
Publication of WO2014176475A2 publication Critical patent/WO2014176475A2/en
Publication of WO2014176475A3 publication Critical patent/WO2014176475A3/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Compounds that inhibit the interaction between HSP90 and proteins having an M-5 loop, such as EGFR, are disclosed, as are their use in treating EGFR-related diseases, including cancers and solid tumors.
PCT/US2014/035391 2013-04-26 2014-04-25 Egfr inhibitors and uses thereof WO2014176475A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361816476P 2013-04-26 2013-04-26
US61/816,476 2013-04-26

Publications (2)

Publication Number Publication Date
WO2014176475A2 WO2014176475A2 (en) 2014-10-30
WO2014176475A3 true WO2014176475A3 (en) 2015-11-26

Family

ID=51792515

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2014/035391 WO2014176475A2 (en) 2013-04-26 2014-04-25 Egfr inhibitors and uses thereof

Country Status (1)

Country Link
WO (1) WO2014176475A2 (en)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2015374118B2 (en) 2014-12-29 2020-07-23 The Trustees Of The University Of Pennsylvania Small molecule inhibitors of lactate dehydrogenase and methods of use thereof
CA3091834A1 (en) 2018-02-23 2019-08-29 The Regents Of The University Of Michigan Egfr dimer disruptors and use of the same
CA3150759A1 (en) * 2019-08-22 2021-02-25 The Regents Of The Universtiy Of Michigan Method of treating kras-associated cancers
IL296091A (en) * 2020-03-05 2022-11-01 Univ Michigan Regents Inhibitors of egfr, kras, braf, and other targets and use of the same
IL301532A (en) 2020-09-23 2023-05-01 Scorpion Therapeutics Inc Pyrrolo[3,2-c]pyridin-4-one derivatives useful in the treatment of cancer
WO2022072632A1 (en) 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Bicyclic compounds for use in the treatment cancer
WO2022072645A2 (en) 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Methods for treating cancer
WO2022072634A1 (en) 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Bicyclic compounds for use in the treatment cancer
WO2022077154A1 (en) * 2020-10-12 2022-04-21 The Regents Of The University Of Michigan Synthesis of egfr modulators
WO2022094271A1 (en) 2020-10-30 2022-05-05 Scorpion Therapeutics, Inc. Methods for treating cancer
WO2022098992A1 (en) 2020-11-05 2022-05-12 Scorpion Therapeutics, Inc. Use of macrocyclic compounds in methods of treating cancer
WO2022197913A1 (en) 2021-03-18 2022-09-22 Scorpion Therapeutics, Inc. Bicyclic derivatives which can be used to treat cancer
WO2023081967A1 (en) * 2021-11-10 2023-05-19 The University Of Western Australia Compounds and uses therefor
WO2023173083A1 (en) 2022-03-11 2023-09-14 Scorpion Therapeutics, Inc. Tetrahydroindole derivatives as egfr and/or her2 inhibtors useful for the treatment of cancer

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120208828A1 (en) * 2009-06-05 2012-08-16 Oslo University Hospital Hf Azole Derivatives as WTN Pathway Inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120208828A1 (en) * 2009-06-05 2012-08-16 Oslo University Hospital Hf Azole Derivatives as WTN Pathway Inhibitors

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BAI ET AL.: "Discovery of novel selective inhibitors for EFGR-T790M/L858R.", BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS, vol. 22, no. 3, 2012, pages 1365 - 1370, XP028887016, Retrieved from the Internet <URL:http://www.researchgate.net/publication/221731124_Discovery_of_novel_selective_inhibitors_for_EGFR-T790ML858R> [retrieved on 20140807] *
DATABASE PUBCHEM 9 July 2005 (2005-07-09), XP055238352, Database accession no. 866670 *

Also Published As

Publication number Publication date
WO2014176475A2 (en) 2014-10-30

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