EP3331530A4 - Mthfd2 inhibitors and uses thereof - Google Patents

Mthfd2 inhibitors and uses thereof Download PDF

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Publication number
EP3331530A4
EP3331530A4 EP16833713.7A EP16833713A EP3331530A4 EP 3331530 A4 EP3331530 A4 EP 3331530A4 EP 16833713 A EP16833713 A EP 16833713A EP 3331530 A4 EP3331530 A4 EP 3331530A4
Authority
EP
European Patent Office
Prior art keywords
mthfd2
inhibitors
mthfd2 inhibitors
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP16833713.7A
Other languages
German (de)
French (fr)
Other versions
EP3331530A1 (en
Inventor
Nello Mainolfi
Mikel MOYER
Eddine Saiah
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Raze Therapeutics Inc
Original Assignee
Raze Therapeutics Inc
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 Raze Therapeutics Inc filed Critical Raze Therapeutics Inc
Publication of EP3331530A1 publication Critical patent/EP3331530A1/en
Publication of EP3331530A4 publication Critical patent/EP3331530A4/en
Withdrawn legal-status Critical Current

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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
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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)
EP16833713.7A 2015-08-03 2016-08-02 Mthfd2 inhibitors and uses thereof Withdrawn EP3331530A4 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562200243P 2015-08-03 2015-08-03
PCT/US2016/045086 WO2017023894A1 (en) 2015-08-03 2016-08-02 Mthfd2 inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
EP3331530A1 EP3331530A1 (en) 2018-06-13
EP3331530A4 true EP3331530A4 (en) 2018-12-19

Family

ID=57943799

Family Applications (1)

Application Number Title Priority Date Filing Date
EP16833713.7A Withdrawn EP3331530A4 (en) 2015-08-03 2016-08-02 Mthfd2 inhibitors and uses thereof

Country Status (2)

Country Link
EP (1) EP3331530A4 (en)
WO (1) WO2017023894A1 (en)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018049191A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridone derivatives as hpk1 modulators and uses thereof for the treatment of cancer
US20180072741A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyrimidine compounds and uses thereof
CN115819417A (en) 2016-09-09 2023-03-21 因赛特公司 Pyrazolopyridine derivatives as HPK1 modulators and their use for the treatment of cancer
WO2018049214A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
JP6970684B2 (en) 2016-11-24 2021-11-24 第一三共株式会社 Sulfonamide derivative with coumarin skeleton
US20180228786A1 (en) 2017-02-15 2018-08-16 Incyte Corporation Pyrazolopyridine compounds and uses thereof
AU2018231120B2 (en) * 2017-03-10 2022-06-23 Rutgers, The State University Of New Jersey Indole derivatives as efflux pump inhibitors
US10722495B2 (en) 2017-09-08 2020-07-28 Incyte Corporation Cyanoindazole compounds and uses thereof
WO2019164847A1 (en) 2018-02-20 2019-08-29 Incyte Corporation Indazole compounds and uses thereof
US10745388B2 (en) 2018-02-20 2020-08-18 Incyte Corporation Indazole compounds and uses thereof
PL3755703T3 (en) 2018-02-20 2022-11-07 Incyte Corporation N-(phenyl)-2-(phenyl)pyrimidine-4-carboxamide derivatives and related compounds as hpk1 inhibitors for treating cancer
US11299473B2 (en) 2018-04-13 2022-04-12 Incyte Corporation Benzimidazole and indole compounds and uses thereof
GB201806349D0 (en) * 2018-04-18 2018-05-30 Thomas Helledays Stiftelse Foer Medicinsk Forskning New compounds and uses
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
EP3856348B1 (en) 2018-09-25 2024-01-03 Incyte Corporation Pyrazolo[4,3-d]pyrimidine compounds as alk2 and/or fgfr modulators
CN111171019A (en) * 2018-11-13 2020-05-19 上海轶诺药业有限公司 Five-membered and six-membered heterocyclic compounds and application thereof as protein receptor kinase inhibitors
AU2020326703A1 (en) 2019-08-06 2022-02-17 Incyte Corporation Solid forms of an HPK1 inhibitor
TW202322824A (en) 2020-02-18 2023-06-16 美商基利科學股份有限公司 Antiviral compounds
WO2022221514A1 (en) 2021-04-16 2022-10-20 Gilead Sciences, Inc. Methods of preparing carbanucleosides using amides

Citations (6)

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Publication number Priority date Publication date Assignee Title
US5834493A (en) * 1993-04-08 1998-11-10 Gil Quintero; Myrna Indole derivatives as 5-HT1A and/or 5-HT2 ligands
US20100317669A1 (en) * 2006-10-27 2010-12-16 Boehringer Ingelheim International Gmbh Novel substituted piperidyl-propane-thiols
WO2012129338A1 (en) * 2011-03-22 2012-09-27 Amgen Inc. Azole compounds as pim inhibitors
WO2012133509A1 (en) * 2011-03-29 2012-10-04 大日本住友製薬株式会社 Novel benzimidazole derivative
WO2014137728A1 (en) * 2013-03-04 2014-09-12 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
WO2015082499A2 (en) * 2013-12-03 2015-06-11 Iomet Pharma Ltd Pharmaceutical compound

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7230011B2 (en) * 2001-01-30 2007-06-12 Eli Lilly And Company Benzenesulfonic acid indol-5-yl esters as antagonists of the 5ht6 receptor
DE10252666A1 (en) * 2002-11-11 2004-08-05 Grünenthal GmbH N-piperidyl-cyclohexane derivatives
US20150152083A1 (en) * 2012-06-06 2015-06-04 Irm Llc, A Delaware Limited Liability Company Compounds and Compositions for Modulating EGFR Activity

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5834493A (en) * 1993-04-08 1998-11-10 Gil Quintero; Myrna Indole derivatives as 5-HT1A and/or 5-HT2 ligands
US20100317669A1 (en) * 2006-10-27 2010-12-16 Boehringer Ingelheim International Gmbh Novel substituted piperidyl-propane-thiols
WO2012129338A1 (en) * 2011-03-22 2012-09-27 Amgen Inc. Azole compounds as pim inhibitors
WO2012133509A1 (en) * 2011-03-29 2012-10-04 大日本住友製薬株式会社 Novel benzimidazole derivative
WO2014137728A1 (en) * 2013-03-04 2014-09-12 Merck Sharp & Dohme Corp. Compounds inhibiting leucine-rich repeat kinase enzyme activity
WO2015082499A2 (en) * 2013-12-03 2015-06-11 Iomet Pharma Ltd Pharmaceutical compound

Non-Patent Citations (9)

* Cited by examiner, † Cited by third party
Title
CHO ET AL.: "Conformational Refinement of Hydroxamate-Based Histone Deacetylase Inhibitors and Exploration of 3-Piperidin-3-ylindole Analogues of Dacinostat (LAQ824)", J. MED. CHEM., vol. 53, no. 7, 1 January 2010 (2010-01-01), pages 2952 - 2963, XP002624311, ISSN: 0022-2623, [retrieved on 20100305], DOI: 10.1021/JM100007M *
DATABASE REAXYS [online] Elsevier Life Sciences IP Limited; 10 November 1998 (1998-11-10), QUINTER ET AL.: "Indole derivtives as 5-HT1A and/or 5-HT2 ligands", XP002786181, Database accession no. 13589235 (XRN) *
GRAY: "Reductive Alkylation of Indole with Pyridinecarboxaldehydes", J. ORG. CHEM., vol. 23, no. 10, 1 October 1958 (1958-10-01), pages 1453 - 1454, XP055520241, ISSN: 0022-3263, DOI: 10.1021/jo01104a012 *
MLADENOVA ET AL.: "First-in-Class, Dual-Action, 3,5-Disubstituted Indole Derivatives Having Human Nitric Oxide Synthase (nNOS) and Norepinephrine Reuptake Inhibitory (NERI) Activity for the Treatment of Neuropathic Pain", J. MED. CHEM., vol. 55, no. 7, 4 April 2012 (2012-04-04), pages 3488 - 3501, XP055520349, ISSN: 0022-2623, DOI: 10.1021/jm300138g *
PRATT; BOTIMER: "Disproportionative Condensations. IV. The 3-Alkylation of Indoles by Primary and Secondary Alcohols 1", J. AM. CHEM. SOC., vol. 79, no. 19, 1 October 1957 (1957-10-01), pages 5248 - 5250, XP055520239, ISSN: 0002-7863, DOI: 10.1021/ja01576a049 *
See also references of WO2017023894A1 *
TEDESCHI ET AL.: "Mitochondrial Methylenetetrahydrofolate Dehydrogenase (MTHFD2) Overexpression Is Associated with Tumor Cell Proliferation and Is a Novel Target for Drug Development", MOL. CANCER RES., vol. 13, no. 10, 22 June 2015 (2015-06-22), US, pages 1361 - 1366, XP055520438, ISSN: 1541-7786, DOI: 10.1158/1541-7786.MCR-15-0117 *
YANG ET AL.: "Highly Enantioselective Ring-Opening Reactions of Aziridines with Indole and Its Application in the Building of C 3 -Halogenated Pyrroloindolines", CHEMISTRY - A EUROPEAN JOURNAL, vol. 20, no. 50, 8 December 2014 (2014-12-08), DE, pages 16478 - 16483, XP055520223, ISSN: 0947-6539, DOI: 10.1002/chem.201404354 *
ZAYTSEV ET AL.: "Searching for Dual Inhibitors of the MDM2-p53 and MDMX-p53 Protein-Protein Interaction by a Scaffold-Hopping Approach", CHEM. BIOL. DRUG DES., vol. 86, no. 2, 11 November 2014 (2014-11-11), GB, pages 180 - 189, XP055520311, ISSN: 1747-0277, DOI: 10.1111/cbdd.12474 *

Also Published As

Publication number Publication date
EP3331530A1 (en) 2018-06-13
WO2017023894A1 (en) 2017-02-09

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RIC1 Information provided on ipc code assigned before grant

Ipc: C07D 401/04 20060101ALI20181107BHEP

Ipc: A61P 35/00 20060101ALI20181107BHEP

Ipc: C07D 413/12 20060101ALI20181107BHEP

Ipc: C07D 403/12 20060101AFI20181107BHEP

Ipc: A61K 31/497 20060101ALI20181107BHEP

Ipc: C07D 401/12 20060101ALI20181107BHEP

Ipc: C07D 209/14 20060101ALI20181107BHEP

Ipc: C07D 405/12 20060101ALI20181107BHEP

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