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WO2025024311A3 - G9a/glp inhibitors and methods of use - Google Patents

G9a/glp inhibitors and methods of use Download PDF

Info

Publication number
WO2025024311A3
WO2025024311A3 PCT/US2024/038842 US2024038842W WO2025024311A3 WO 2025024311 A3 WO2025024311 A3 WO 2025024311A3 US 2024038842 W US2024038842 W US 2024038842W WO 2025024311 A3 WO2025024311 A3 WO 2025024311A3
Authority
WO
WIPO (PCT)
Prior art keywords
glp
methods
inhibitors
glp inhibitors
isopropylpiperidin
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.)
Pending
Application number
PCT/US2024/038842
Other languages
French (fr)
Other versions
WO2025024311A2 (en
Inventor
Jian Jin
Yan Xiong
Kwang-Su Park
Julia VELEZ
Jing Liu
Xian Chen
Juan SONG
Ling Xie
Ryan N. SHEEHY
Yonghui JIANG
Sung-Eun WANG
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.)
Yale University
University of North Carolina at Chapel Hill
Icahn School of Medicine at Mount Sinai
Original Assignee
Yale University
University of North Carolina at Chapel Hill
Icahn School of Medicine at Mount Sinai
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 Yale University, University of North Carolina at Chapel Hill, Icahn School of Medicine at Mount Sinai filed Critical Yale University
Publication of WO2025024311A2 publication Critical patent/WO2025024311A2/en
Publication of WO2025024311A3 publication Critical patent/WO2025024311A3/en
Pending legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Described is small molecule N-(l-isopropylpiperidin-4-yl)-6-methoxy-2-morpholino-7- (3-(pyrrolidin-l-yl)propoxy)quinolin-4-amine)) (MS 1262) that inhibits methyltransferases G9a/GLP. This inhibitor can be used for the treatment of patients with G9a/GLP related diseases such as Alzheimer's Disease and Prader-Willi Syndrome.
PCT/US2024/038842 2023-07-21 2024-07-19 G9a/glp inhibitors and methods of use Pending WO2025024311A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202363515010P 2023-07-21 2023-07-21
US63/515,010 2023-07-21

Publications (2)

Publication Number Publication Date
WO2025024311A2 WO2025024311A2 (en) 2025-01-30
WO2025024311A3 true WO2025024311A3 (en) 2025-04-17

Family

ID=94375713

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2024/038842 Pending WO2025024311A2 (en) 2023-07-21 2024-07-19 G9a/glp inhibitors and methods of use

Country Status (1)

Country Link
WO (1) WO2025024311A2 (en)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080033000A1 (en) * 2006-05-15 2008-02-07 Senex Biotechnology, Inc. Identification of CDKI pathway inhibitors
US20080318971A1 (en) * 2007-06-01 2008-12-25 Wyeth Treatment of imatinib resistant leukemia
WO2013134047A2 (en) * 2012-03-07 2013-09-12 The Mclean Hospital Corporation Aminoquinoline derivatives and uses thereof
US20220388962A1 (en) * 2019-08-22 2022-12-08 Biohaven Therapeutics Ltd. Molecules that bind to tdp-43 for the treatment of amyotrophic lateral sclerosis and related disorders

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080033000A1 (en) * 2006-05-15 2008-02-07 Senex Biotechnology, Inc. Identification of CDKI pathway inhibitors
US20080318971A1 (en) * 2007-06-01 2008-12-25 Wyeth Treatment of imatinib resistant leukemia
WO2013134047A2 (en) * 2012-03-07 2013-09-12 The Mclean Hospital Corporation Aminoquinoline derivatives and uses thereof
US20220388962A1 (en) * 2019-08-22 2022-12-08 Biohaven Therapeutics Ltd. Molecules that bind to tdp-43 for the treatment of amyotrophic lateral sclerosis and related disorders

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DATABASE PUBCHEM COMPOUND 4 August 2019 (2019-08-04), XP093304833, Database accession no. 137631913 *

Also Published As

Publication number Publication date
WO2025024311A2 (en) 2025-01-30

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