AU2021218739A1 - Inhibitors of ULK1/2 and methods of using same - Google Patents

Inhibitors of ULK1/2 and methods of using same Download PDF

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Publication number
AU2021218739A1
AU2021218739A1 AU2021218739A AU2021218739A AU2021218739A1 AU 2021218739 A1 AU2021218739 A1 AU 2021218739A1 AU 2021218739 A AU2021218739 A AU 2021218739A AU 2021218739 A AU2021218739 A AU 2021218739A AU 2021218739 A1 AU2021218739 A1 AU 2021218739A1
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AU
Australia
Prior art keywords
substituted
compound
unsubstituted
alkyl
independently
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Pending
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AU2021218739A
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English (en)
Inventor
Nicole A. Bakas
Sonja N. BRUN
Nicholas D.P. Cosford
Allison S. LIMPERT
Reuben J. Shaw
Mitchell VAMOS
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.)
Sanford Burnham Prebys Medical Discovery Institute
Salk Institute for Biological Studies
Original Assignee
Sanford Burnham Prebys Medical Discovery Institute
Salk Institute for Biological Studies
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Application filed by Sanford Burnham Prebys Medical Discovery Institute, Salk Institute for Biological Studies filed Critical Sanford Burnham Prebys Medical Discovery Institute
Publication of AU2021218739A1 publication Critical patent/AU2021218739A1/en
Pending legal-status Critical Current

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    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen 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
    • C07D401/14—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
    • 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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AU2021218739A 2020-02-14 2021-02-12 Inhibitors of ULK1/2 and methods of using same Pending AU2021218739A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202062977040P 2020-02-14 2020-02-14
US62/977,040 2020-02-14
PCT/US2021/018040 WO2021163629A1 (en) 2020-02-14 2021-02-12 Inhibitors of ulk1/2 and methods of using same

Publications (1)

Publication Number Publication Date
AU2021218739A1 true AU2021218739A1 (en) 2022-09-22

Family

ID=77292760

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2021218739A Pending AU2021218739A1 (en) 2020-02-14 2021-02-12 Inhibitors of ULK1/2 and methods of using same

Country Status (8)

Country Link
US (1) US20230135635A1 (https=)
EP (1) EP4103182A4 (https=)
JP (1) JP2023513794A (https=)
KR (1) KR20220153581A (https=)
CN (1) CN115515589A (https=)
AU (1) AU2021218739A1 (https=)
CA (1) CA3171187A1 (https=)
WO (1) WO2021163629A1 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220153582A (ko) 2020-02-14 2022-11-18 솔크 인스티튜트 포 바이올로지칼 스터디즈 마크로시클릭 ulk1/2 억제제
WO2022072668A1 (en) * 2020-09-30 2022-04-07 Salk Institute For Biological Studies Patient selection biomarkers for treatment with ulk inhibitors
WO2023134582A1 (zh) * 2022-01-14 2023-07-20 上海立森印迹医药技术有限公司 一种嘧啶-2,4-二胺衍生物及其制备方法和用途
WO2024140401A1 (zh) * 2022-12-30 2024-07-04 捷思英达控股有限公司 作为激酶抑制剂的杂环化合物以及包括其的组合物
CN116768885B (zh) * 2023-03-14 2026-03-24 浙江大学 N2-取代双环-2-氨基嘧啶类衍生物、其制备方法及医药用途
WO2024233766A1 (en) * 2023-05-10 2024-11-14 Erasca, Inc. Macrocyclic ulk1/2 inhibitors and their use thereof
WO2025045182A1 (zh) * 2023-09-01 2025-03-06 深圳众格生物科技有限公司 Ulk1抑制剂及其制备方法和用途

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6939874B2 (en) * 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
WO2006129100A1 (en) * 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
WO2007028445A1 (en) * 2005-07-15 2007-03-15 Glaxo Group Limited 6-indolyl-4-yl-amino-5-halogeno-2-pyrimidinyl-amino derivatives
EP2089369B1 (en) * 2006-10-19 2011-02-02 Rigel Pharmaceuticals, Inc. 2,4 -pyrimidinediamine derivatives as inhibitors of jak kinases for the treatment of autoimmune diseases
BRPI0810641A2 (pt) * 2007-04-12 2019-09-24 Hoffmann La Roche "compostos farmacêuticos".
CA2693594A1 (en) * 2007-07-17 2009-01-22 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as pkc inhibitors
EA201100078A1 (ru) * 2008-06-25 2011-08-30 Айрм Ллк Производные пиримидина в качестве ингибиторов киназы
WO2014197680A1 (en) * 2013-06-05 2014-12-11 Salk Institute For Biological Studies Vitamin d receptor agonists to treat diseases involving cxcl12 activity
US10300058B2 (en) * 2014-04-18 2019-05-28 Xuanzhu Pharma Co., Ltd. Tyrosine kinase inhibitor and uses thereof
CA2952787A1 (en) * 2014-06-17 2015-12-23 Korea Research Institute Of Chemical Technology Pyrimidine-2,4-diamine derivative and anticancer pharmaceutical composition comprising same as effective ingredient
DK3185868T3 (da) * 2014-08-25 2022-05-23 Salk Inst For Biological Studi Hidtil ukendte ULK1-inhibitorer og fremgangsmåder til anvendelse af samme
KR20250081944A (ko) * 2014-09-24 2025-06-05 솔크 인스티튜트 포 바이올로지칼 스터디즈 종양 살상 바이러스 및 이의 사용방법
CN105524045B (zh) * 2014-10-22 2020-04-10 山东轩竹医药科技有限公司 四环类间变性淋巴瘤激酶抑制剂
WO2016090079A1 (en) * 2014-12-05 2016-06-09 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
CN106188029B (zh) * 2015-05-05 2018-09-18 山东轩竹医药科技有限公司 二并环类间变性淋巴瘤激酶抑制剂
EP3528814B1 (en) * 2016-10-18 2024-08-14 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and methods of treating dclk1/2-mediated disorders
US11180482B2 (en) * 2016-11-30 2021-11-23 Ariad Pharmaceuticals, Inc. Anilinopyrimidines as haematopoietic progenitor kinase 1 (HPK1) inhibitors
EP3620457A4 (en) * 2017-05-02 2021-01-06 Korea Research Institute of Chemical Technology PYRIMIDE-DERIVATIVE COMPOUND, OPTICAL ISOMER THEREOF, OR PHARMACEUTICAL SALT THEREOF AND COMPOSITION FOR THE PREVENTION OR TREATMENT OF TYRO-3 RELATED DISEASES THEREOF AS ACTIVE SUBSTANCE

Also Published As

Publication number Publication date
CN115515589A (zh) 2022-12-23
KR20220153581A (ko) 2022-11-18
EP4103182A1 (en) 2022-12-21
US20230135635A1 (en) 2023-05-04
CA3171187A1 (en) 2021-08-19
EP4103182A4 (en) 2024-02-21
WO2021163629A1 (en) 2021-08-19
JP2023513794A (ja) 2023-04-03

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