WO2024010817A3 - Selective androgen receptor degrader (sard) o-linked ligands - Google Patents

Selective androgen receptor degrader (sard) o-linked ligands Download PDF

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Publication number
WO2024010817A3
WO2024010817A3 PCT/US2023/026942 US2023026942W WO2024010817A3 WO 2024010817 A3 WO2024010817 A3 WO 2024010817A3 US 2023026942 W US2023026942 W US 2023026942W WO 2024010817 A3 WO2024010817 A3 WO 2024010817A3
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WO
WIPO (PCT)
Prior art keywords
androgen receptor
prostate cancer
sard
selective androgen
receptor degrader
Prior art date
Application number
PCT/US2023/026942
Other languages
French (fr)
Other versions
WO2024010817A2 (en
Inventor
Ramesh Narayanan
Duane D. Miller
Thamarai PONNUSAMY
Yali He
Dong-Jin Hwang
Original Assignee
University Of Tennessee Research Foundation
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Filing date
Publication date
Application filed by University Of Tennessee Research Foundation filed Critical University Of Tennessee Research Foundation
Publication of WO2024010817A2 publication Critical patent/WO2024010817A2/en
Publication of WO2024010817A3 publication Critical patent/WO2024010817A3/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61K31/075—Ethers or acetals
    • A61K31/085—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
    • A61K31/09—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/54—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

This disclosure is directed to selective androgen receptor degrader (SARD) compounds, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, spinal (and) bulbar muscular atrophy (SBMA), amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
PCT/US2023/026942 2022-07-07 2023-07-05 Selective androgen receptor degrader (sard) o-linked ligands and methods of use thereof WO2024010817A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202263359126P 2022-07-07 2022-07-07
US63/359,126 2022-07-07

Publications (2)

Publication Number Publication Date
WO2024010817A2 WO2024010817A2 (en) 2024-01-11
WO2024010817A3 true WO2024010817A3 (en) 2024-02-29

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2023/026942 WO2024010817A2 (en) 2022-07-07 2023-07-05 Selective androgen receptor degrader (sard) o-linked ligands and methods of use thereof

Country Status (1)

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WO (1) WO2024010817A2 (en)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005102990A1 (en) * 2004-04-22 2005-11-03 Warner-Lambert Company Llc Androgen modulators
WO2006055184A2 (en) * 2004-11-16 2006-05-26 Janssen Pharmaceutica N.V. Novel heterocycle derivatives useful as selective androgen receptor modulators (sarms)
US20080255124A1 (en) * 2004-10-13 2008-10-16 Smithkline Beecham Corporation Chemical Compounds
US20170368003A1 (en) * 2016-06-10 2017-12-28 University Of Tennessee Research Foundation Selective androgen receptor degrader (sard) ligands and methods of use thereof

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005102990A1 (en) * 2004-04-22 2005-11-03 Warner-Lambert Company Llc Androgen modulators
US20080255124A1 (en) * 2004-10-13 2008-10-16 Smithkline Beecham Corporation Chemical Compounds
WO2006055184A2 (en) * 2004-11-16 2006-05-26 Janssen Pharmaceutica N.V. Novel heterocycle derivatives useful as selective androgen receptor modulators (sarms)
US20170368003A1 (en) * 2016-06-10 2017-12-28 University Of Tennessee Research Foundation Selective androgen receptor degrader (sard) ligands and methods of use thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MOHLER, ML ET AL.: "An Overview of Next-Generation Androgen Receptor-Targeted Therapeutics in Development for the Treatment of Prostate Cancer", INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, vol. 22, no. 4, 20 February 2021 (2021-02-20), pages 1 - 20, XP093145318, DOI: 10.3390/ijms22042124 *

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Publication number Publication date
WO2024010817A2 (en) 2024-01-11

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