AU2017221472B2 - Methods and compounds for restoring mutant p53 function - Google Patents

Methods and compounds for restoring mutant p53 function Download PDF

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AU2017221472B2
AU2017221472B2 AU2017221472A AU2017221472A AU2017221472B2 AU 2017221472 B2 AU2017221472 B2 AU 2017221472B2 AU 2017221472 A AU2017221472 A AU 2017221472A AU 2017221472 A AU2017221472 A AU 2017221472A AU 2017221472 B2 AU2017221472 B2 AU 2017221472B2
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amino
methyl
prop
indol
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AU2017221472A1 (en
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Romyr Dominique
Hongju Li
Binh Vu
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PMV Pharmaceuticals Inc
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PMV Pharmaceuticals Inc
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    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/575—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/5758—Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumours, cancers or neoplasias, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides or metabolites
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    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
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    • 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
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/536—Immunoassay; Biospecific binding assay; Materials therefor with immune complex formed in liquid phase
    • G01N33/542—Immunoassay; Biospecific binding assay; Materials therefor with immune complex formed in liquid phase with steric inhibition or signal modification, e.g. fluorescent quenching
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    • G01N2333/46—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans from vertebrates
    • G01N2333/47—Assays involving proteins of known structure or function as defined in the subgroups
    • G01N2333/4701—Details
    • G01N2333/4748—Details p53

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  • Indole Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
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AU2017221472A 2016-02-19 2017-02-17 Methods and compounds for restoring mutant p53 function Active AU2017221472B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662297450P 2016-02-19 2016-02-19
US62/297,450 2016-02-19
PCT/US2017/018511 WO2017143291A1 (en) 2016-02-19 2017-02-17 METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION

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AU2017221472A1 AU2017221472A1 (en) 2018-07-26
AU2017221472B2 true AU2017221472B2 (en) 2023-01-05

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US (4) US10138219B2 (enExample)
EP (1) EP3416638A4 (enExample)
JP (1) JP6956098B2 (enExample)
KR (1) KR102868217B1 (enExample)
CN (2) CN119161324B (enExample)
AU (1) AU2017221472B2 (enExample)
CA (2) CA3215564C (enExample)
IL (2) IL286839B (enExample)
MX (1) MX383904B (enExample)
WO (1) WO2017143291A1 (enExample)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX383904B (es) 2016-02-19 2025-03-14 Pmv Pharmaceuticals Inc Métodos y composiciones para restablecer la función de p53 mutante.
US11814373B2 (en) * 2019-09-23 2023-11-14 Pmv Pharmaceuticals, Inc. Methods and compounds for restoring mutant p53 function
EP4149459A4 (en) * 2020-05-12 2024-05-22 PMV Pharmaceuticals, Inc. METHODS AND COMPOUNDS FOR RESTORING MUTANT P53 FUNCTION
CN111686127B (zh) * 2020-06-04 2022-02-15 华南理工大学 锌铁纳米材料在降解突变p53蛋白中的应用
CN113750246B (zh) * 2020-06-04 2023-12-05 华南理工大学 ZIF-8纳米材料在降解广谱突变p53蛋白中的应用
US12570645B2 (en) 2020-06-22 2026-03-10 Pmv Pharmaceuticals, Inc. Uses of p53 x-ray co-crystal structures
WO2021262596A1 (en) * 2020-06-22 2021-12-30 Pmv Pharmaceuticals, Inc. Methods and compounds for restoring mutant p53 function
EP4168411A4 (en) * 2020-06-22 2024-07-24 PMV Pharmaceuticals, Inc. METHODS AND COMPOUNDS FOR RESTORING FUNCTION IN P53 MUTANTS
CN116249689A (zh) * 2020-06-24 2023-06-09 皮姆维制药公司 用于再激活突变p53的化合物的伴随诊断工具
WO2021262483A1 (en) * 2020-06-24 2021-12-30 Pmv Pharmaceuticals, Inc. METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
CA3183081A1 (en) * 2020-06-24 2021-12-30 Arnold Levine Combination therapy for treatment of cancer
US11667636B2 (en) 2020-12-24 2023-06-06 Escient Pharmaceuticals, Inc. Modulators of Mas-related G-protein receptor X2 and related products and methods
WO2022213975A1 (en) * 2021-04-08 2022-10-13 Jacobio Pharmaceuticals Co., Ltd. Compounds targeting y220c mutant of p53
UY39890A (es) * 2021-08-10 2023-03-31 Jacobio Pharmaceuticals Co Ltd Compuestos con diana en mutante de p53
CN117916230A (zh) * 2021-08-27 2024-04-19 杭州紫晶医药科技有限公司 作为p53调节剂的化合物
WO2023147419A2 (en) 2022-01-27 2023-08-03 Pmv Pharmaceuticals, Inc. Deuterated compounds for restoring mutant p53 function
WO2024017384A1 (zh) * 2022-07-22 2024-01-25 深圳众格生物科技有限公司 恢复p53突变功能的化合物及其应用
WO2024041503A1 (en) * 2022-08-22 2024-02-29 Jacobio Pharmaceuticals Co., Ltd. Compounds targeting y220c mutant of p53
WO2024083223A1 (zh) * 2022-10-21 2024-04-25 正大天晴药业集团股份有限公司 大环类化合物及其医药用途
CN120265637A (zh) * 2022-12-08 2025-07-04 北京加科思新药研发有限公司 靶向p53突变体的化合物
WO2025031471A1 (zh) * 2023-08-09 2025-02-13 德睿智药(苏州)新药研发有限公司 用于调节p53功能的新型杂环类化合物
AU2024295989B2 (en) 2023-10-20 2026-08-13 Nutshell Therapeutics (Shanghai) Co., Ltd. N-sulfonamide nitrogen-containing fused heterocyclic compound, and application thereof
WO2025242903A1 (en) * 2024-05-24 2025-11-27 Onco3R Therapeutics Bv Compounds and pharmaceutical compositions thereof for the treatment of proliferative diseases
WO2026025042A1 (en) 2024-07-26 2026-01-29 Dana-Farber Cancer Institute, Inc. P53 targeting compounds and uses thereof
WO2026067649A1 (zh) * 2024-09-27 2026-04-02 奇树医药公司 恢复p53突变功能的化合物及其应用

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000032175A2 (en) * 1998-12-02 2000-06-08 Pfizer Products Inc. METHODS AND COMPOSITIONS FOR RESTORING CONFORMATIONAL STABILITY OF A PROTEIN OF THE p53 FAMILY
US20120258920A1 (en) * 2008-03-13 2012-10-11 Universita' Degli Studi Di Trieste Peptides and aptamers thereof as specific modulators of mutant p53 function
WO2012175962A1 (en) * 2011-06-20 2012-12-27 Medical Research Council COMPOUNDS FOR USE IN STABILISING p53 MUTANTS
WO2013036208A1 (en) * 2011-09-09 2013-03-14 Agency For Science, Technology And Research P53 activating peptides
CN104672241A (zh) * 2015-01-29 2015-06-03 王磊 吡咯并[2,3-d]嘧啶类化合物及其用途
WO2016004513A1 (en) * 2014-07-11 2016-01-14 Simon Fraser University Anti-bacterial pyruvate kinase modulator compounds, compositions, uses and methods

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6770652B2 (en) * 2001-10-18 2004-08-03 Duquesne University Of The Holy Ghost Multiple acting anti-angiogenic and cytotoxic compounds and methods for using the same
EP1689710A1 (en) * 2003-11-25 2006-08-16 Novo Nordisk A/S Indole derivatives for use as chemical uncoupler
US7601714B2 (en) 2004-07-08 2009-10-13 Boehringer Ingelheim Pharmaceuticals, Inc. Pyrimidine derivatives useful as inhibitors of PKC-theta
WO2006136823A1 (en) 2005-06-21 2006-12-28 Astex Therapeutics Limited Heterocyclic containing amines as kinase b inhibitors
RS54165B1 (sr) * 2008-04-16 2015-12-31 Karo Bio Ab Novi ligandi za estrogenski receptor
GB0808282D0 (en) * 2008-05-07 2008-06-11 Medical Res Council Compounds for use in stabilizing p53 mutants
HUE027755T2 (en) * 2009-03-27 2016-11-28 Merck Sharp & Dohme Inhibitors of hepatitis C virus replication
DE102010049877A1 (de) 2010-11-01 2012-05-03 Merck Patent Gmbh 7-((1,2,3)Triazol-4-yl)-pyrrolo(2,3) pyrazinderivate
RU2598842C2 (ru) 2011-01-20 2016-09-27 Мерк Шарп Энд Домэ Корп. Антагонисты рецептора минералокортикоидов
WO2013101911A2 (en) 2011-12-28 2013-07-04 Allergan, Inc. Benzimidazole derivatives as selective blockers of persistent sodium current
US8822689B2 (en) 2012-09-19 2014-09-02 Merial Limited Aryloazol-2-yl cyanoethylamino compounds, method of making and method of using thereof
EP3145512B1 (en) * 2014-05-19 2019-07-17 Jiangsu Hengrui Medicine Co., Ltd. Substituted ethynyl heterobicyclic compounds as tyrosine kinase inhibitors
MX383904B (es) 2016-02-19 2025-03-14 Pmv Pharmaceuticals Inc Métodos y composiciones para restablecer la función de p53 mutante.

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000032175A2 (en) * 1998-12-02 2000-06-08 Pfizer Products Inc. METHODS AND COMPOSITIONS FOR RESTORING CONFORMATIONAL STABILITY OF A PROTEIN OF THE p53 FAMILY
US20120258920A1 (en) * 2008-03-13 2012-10-11 Universita' Degli Studi Di Trieste Peptides and aptamers thereof as specific modulators of mutant p53 function
WO2012175962A1 (en) * 2011-06-20 2012-12-27 Medical Research Council COMPOUNDS FOR USE IN STABILISING p53 MUTANTS
WO2013036208A1 (en) * 2011-09-09 2013-03-14 Agency For Science, Technology And Research P53 activating peptides
WO2016004513A1 (en) * 2014-07-11 2016-01-14 Simon Fraser University Anti-bacterial pyruvate kinase modulator compounds, compositions, uses and methods
CN104672241A (zh) * 2015-01-29 2015-06-03 王磊 吡咯并[2,3-d]嘧啶类化合物及其用途

Non-Patent Citations (8)

* Cited by examiner, † Cited by third party
Title
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 29 May 2019 (2019-05-29), BILBAO, NEREA ET AL: "Two-Dimensional Nanoporous Networks Formed by Liquid-to-Solid Transfer of Hydrogen-Bonded Macrocycles Built from DNA Bases", XP002791700, retrieved from STN *
Dell'acqua M et al (2015) "MediaChrom: Discovering a Class of Pyrimidoindolone-Based Polarity-Sensitive Dyes", Journal of Organic Chemistry, vol. 80, no. 21, pages 10939 - 10954 *
FIANDANESE, V. BOTTALICO, D. MARCHESE, G. PUNZI, A.: "A straightforward synthesis of indole and benzofuran derivatives", TETRAHEDRON, ELSEVIER SIENCE PUBLISHERS, AMSTERDAM, NL, vol. 64, no. 1, 1 November 2007 (2007-11-01), AMSTERDAM, NL , pages 53 - 60, XP022361251, ISSN: 0040-4020, DOI: 10.1016/j.tet.2007.10.100 *
Guo Z et al (2014) "PIM inhibitors target CD25-positive AML cells through concomitant suppression of STAT5 activation and degradation of MYC oncogene", Blood, vol. 124, no. 11, pages 1777 - 1789 *
Leblanc et al (2002) Homogeneous time-resolved fluorescence assay for identifying p53 interactions with its protein partners, directly in a cellular extract, Analytical Biochemistry, Vol. 308, Issue 2, 2002, Pages 247-254 *
Selivanova et al (2007) "Reactivation of mutant p53: molecular mechanisms and therapeutic potential", Oncogene, vol. 26, no. 15, pages 2243 - 2254 *
Shinohara Y et al (2010) Design of environmentally sensitive fluorescent 2-deoxyguanosine containing arylethynyl moieties: Distinction of thymine base by base-discriminating fluorescent (BDF) probe, Bioorg & Med Chem Ltrs, 20(9), pp2817-20 *
Tolnai GL, et al (2013) "C2-Selective Direct Alkynylation of Indoles", Organic Letters, vol. 15, no. 1, pages 112 - 115 *

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