WO2012078519A3 - 3-acylidene-2-oxoindole derivatives for inhibition of transglutaminase 2 - Google Patents

3-acylidene-2-oxoindole derivatives for inhibition of transglutaminase 2 Download PDF

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Publication number
WO2012078519A3
WO2012078519A3 PCT/US2011/063312 US2011063312W WO2012078519A3 WO 2012078519 A3 WO2012078519 A3 WO 2012078519A3 US 2011063312 W US2011063312 W US 2011063312W WO 2012078519 A3 WO2012078519 A3 WO 2012078519A3
Authority
WO
WIPO (PCT)
Prior art keywords
transglutaminase
acylidene
inhibition
derivatives
oxoindole
Prior art date
Application number
PCT/US2011/063312
Other languages
French (fr)
Other versions
WO2012078519A2 (en
Inventor
John Griffin
Brian Raimundo
Peter Madrid
Chaitan Khosla
Xi JIN
Cornelius Kloeck
Original Assignee
Numerate, Inc.
The Board Of Trustees Of The Leland Stanford Junior University
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 Numerate, Inc., The Board Of Trustees Of The Leland Stanford Junior University filed Critical Numerate, Inc.
Publication of WO2012078519A2 publication Critical patent/WO2012078519A2/en
Publication of WO2012078519A3 publication Critical patent/WO2012078519A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32—Oxygen atoms
    • C07D209/34—Oxygen atoms in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (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)

Abstract

Provided herein are acylidene oxoindole derivatives, compositions including them, and methods of inhibiting transglutaminase 2 and treating diseases mediated by transglutaminase 2 by administering such derivatives and compositions.
PCT/US2011/063312 2010-12-06 2011-12-05 3-acylidene-2-oxoindole derivatives for inhibition of transglutaminase 2 WO2012078519A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US42021610P 2010-12-06 2010-12-06
US61/420,216 2010-12-06

Publications (2)

Publication Number Publication Date
WO2012078519A2 WO2012078519A2 (en) 2012-06-14
WO2012078519A3 true WO2012078519A3 (en) 2012-08-02

Family

ID=46207668

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2011/063312 WO2012078519A2 (en) 2010-12-06 2011-12-05 3-acylidene-2-oxoindole derivatives for inhibition of transglutaminase 2

Country Status (1)

Country Link
WO (1) WO2012078519A2 (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ723971A (en) 2012-04-12 2018-01-26 Univ Georgetown Methods and compositions for treating ewings sarcoma family of tumors
CN111777596A (en) 2014-10-09 2020-10-16 英克特诺治疗公司 Indolone compounds and use thereof
CN104496885B (en) * 2015-01-12 2017-08-25 中国药科大学 A kind of preparation method of the Nitroisatoic of 4 amino of N methyl 5
CN109219594B (en) 2016-03-31 2022-10-11 英克特诺治疗公司 Indoline analogue and application thereof
CA3029851A1 (en) 2016-07-29 2018-02-01 Oncternal Therapeutics, Inc. Uses of indoline compounds such as tk216 for the treatment of cancer
TWI825144B (en) * 2018-08-10 2023-12-11 美商思達利醫藥公司 Transglutaminase 2 (tg2) inhibitors

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004056769A2 (en) * 2002-12-20 2004-07-08 Ciba Specialty Chemicals Holding Inc. Synthesis of amines and intermediates for the synthesis thereof
US20060052308A1 (en) * 2003-11-18 2006-03-09 The Board Of Trustees Of The Leland Stanford Junior University Transglutaminase inhibitors and methods of use thereof
WO2009123080A1 (en) * 2008-04-01 2009-10-08 アステラス製薬株式会社 Indolinone compound

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004056769A2 (en) * 2002-12-20 2004-07-08 Ciba Specialty Chemicals Holding Inc. Synthesis of amines and intermediates for the synthesis thereof
US20060052308A1 (en) * 2003-11-18 2006-03-09 The Board Of Trustees Of The Leland Stanford Junior University Transglutaminase inhibitors and methods of use thereof
WO2009123080A1 (en) * 2008-04-01 2009-10-08 アステラス製薬株式会社 Indolinone compound

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
CASSABDRA L. WOODARD ET AL.: "Oxindole-based compounds are selective inhibitors of Plasmodium falciparum cyclin dependent protein kinase", JOURNAL OF MEDICINAL CHEMISTRY, vol. 46, no. 18, 2003, pages 3877 - 3883 *
CORNELIUS KLOECK ET AL.: "Acylideneoxoindoles: A new class of reversible inhibitors of human transglutaminase 2", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, vol. 21, no. 9, 16 December 2010 (2010-12-16), pages 2692 - 2696, XP002751380, DOI: doi:10.1016/J.BMCL.2010.12.037 *
LINDSEY J. MACPHERSON ET AL.: "Noxious compounds activate TRPA1 ion channels through covalent modification of cysteines", NATURE, vol. 445, 2007, pages 541 - 545, XP009149873, DOI: doi:10.1038/nature05544 *
STANLEY REHN ET AL.: "The reaction between 3-aminocrotonates and oxindole- 3-ylidene derivatives: synthesis of highly substituted pyrroles", TETRAHEDRON, vol. 61, no. 12, 2005, pages 3115 - 3123 *

Also Published As

Publication number Publication date
WO2012078519A2 (en) 2012-06-14

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