CO2022018532A2 - Compuestos macrocíclicos y métodos de uso de los mismos - Google Patents

Compuestos macrocíclicos y métodos de uso de los mismos

Info

Publication number
CO2022018532A2
CO2022018532A2 CONC2022/0018532A CO2022018532A CO2022018532A2 CO 2022018532 A2 CO2022018532 A2 CO 2022018532A2 CO 2022018532 A CO2022018532 A CO 2022018532A CO 2022018532 A2 CO2022018532 A2 CO 2022018532A2
Authority
CO
Colombia
Prior art keywords
methods
macrocyclic
binding motif
same
macrocyclic compounds
Prior art date
Application number
CONC2022/0018532A
Other languages
English (en)
Inventor
Jakob Fuhrmann
Wayne Fairbrother
Hao Wu
Jeremy Murray
Original Assignee
Genentech 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 Genentech Inc filed Critical Genentech Inc
Publication of CO2022018532A2 publication Critical patent/CO2022018532A2/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64Cyclic peptides containing only normal peptide links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K19/00Hybrid peptides, i.e. peptides covalently bound to nucleic acids, or non-covalently bound protein-protein complexes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02Linear peptides containing at least one abnormal peptide link
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/50Cyclic peptides containing at least one abnormal peptide link
    • C07K7/52Cyclic peptides containing at least one abnormal peptide link with only normal peptide links in the ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Se proveen compuestos macrocíclicos que comprenden un motivo de unión a la ubiquitina ligasa E3 (EULBM) y al menos un aminoácido, y métodos para preparar y usar tales EULBM macrocíclicos para el tratamiento del cáncer o de una condición fibrótica. También se proveen inductores químicos heterobifuncionales macrocíclicos de degradación (CIDE) que comprenden un motivo de unión a la ubiquitina ligasa E3 (EULBM) y un motivo de unión a la proteína diana (TPBM) unidos por al menos un aminoácido.
CONC2022/0018532A 2020-06-23 2022-12-21 Compuestos macrocíclicos y métodos de uso de los mismos CO2022018532A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202063043071P 2020-06-23 2020-06-23
PCT/US2021/038503 WO2021262731A2 (en) 2020-06-23 2021-06-22 Macrocyclic compounds and methods of use thereof

Publications (1)

Publication Number Publication Date
CO2022018532A2 true CO2022018532A2 (es) 2022-12-30

Family

ID=77207221

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2022/0018532A CO2022018532A2 (es) 2020-06-23 2022-12-21 Compuestos macrocíclicos y métodos de uso de los mismos

Country Status (17)

Country Link
US (1) US20220106361A1 (es)
EP (1) EP4168121A2 (es)
JP (1) JP2023532233A (es)
KR (1) KR20230026461A (es)
CN (1) CN115702026A (es)
AR (1) AR122707A1 (es)
AU (1) AU2021297799A1 (es)
BR (1) BR112022026364A2 (es)
CA (1) CA3185149A1 (es)
CL (2) CL2022003643A1 (es)
CO (1) CO2022018532A2 (es)
CR (1) CR20220658A (es)
IL (1) IL299163A (es)
MX (1) MX2022016454A (es)
PE (1) PE20230617A1 (es)
TW (1) TW202219056A (es)
WO (1) WO2021262731A2 (es)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2024020159A1 (en) * 2022-07-21 2024-01-25 Merck Sharp & Dohme Llc Macrocyclic peptides targeting kras

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4144233A (en) 1977-02-16 1979-03-13 The Dow Chemical Company Method for preparing benzo-(1,3,4)-benzotriazepines
US5185331A (en) 1991-05-14 1993-02-09 Merck & Co., Inc. Triazolobenzodiazepines
DK1107981T3 (da) * 1998-08-20 2005-05-30 Lilly Co Eli Syntese af ringmodificerede, cykliske peptidanaloger
JP5159305B2 (ja) 2005-05-30 2013-03-06 田辺三菱製薬株式会社 チエノトリアゾロジアゼピン化合物及びその医薬としての用途
KR101600634B1 (ko) 2007-12-28 2016-03-07 미쓰비시 타나베 파마 코퍼레이션 항암제
HUE026967T2 (en) 2009-11-05 2016-07-28 Glaxosmithkline Llc Benzodiazepine Bromodomain inhibitor
EP2722334B1 (en) 2009-11-05 2016-01-13 GlaxoSmithKline LLC Benzodiazepine bromodomain inhibitor
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
ES2606958T3 (es) 2010-05-14 2017-03-28 Dana-Farber Cancer Institute, Inc. Compuestos de tienotriazolodiazepina para tratar una neoplasia
JP5913292B2 (ja) 2010-05-14 2016-04-27 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド 代謝を調節する組成物および方法
US9085582B2 (en) 2010-06-22 2015-07-21 Glaxosmithkline Llc Benzotriazolodiazepine compounds inhibitors of bromodomains
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
WO2013106646A2 (en) 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
CA2996245C (en) 2015-09-02 2023-10-17 Glaxosmithkline Intellectual Property (No.2) Limited Pyridinone dicarboxamide for use as bromodomain inhibitors
CA3078682A1 (en) * 2017-12-15 2019-06-20 Dana-Farber Cancer Institute, Inc. Stabilized peptide-mediated targeted protein degradation

Also Published As

Publication number Publication date
CN115702026A (zh) 2023-02-14
CL2023002555A1 (es) 2024-01-26
CA3185149A1 (en) 2021-12-30
CR20220658A (es) 2023-04-26
KR20230026461A (ko) 2023-02-24
CL2022003643A1 (es) 2023-05-26
BR112022026364A2 (pt) 2023-01-17
TW202219056A (zh) 2022-05-16
US20220106361A1 (en) 2022-04-07
AU2021297799A1 (en) 2022-12-22
EP4168121A2 (en) 2023-04-26
WO2021262731A2 (en) 2021-12-30
WO2021262731A3 (en) 2022-02-24
JP2023532233A (ja) 2023-07-27
PE20230617A1 (es) 2023-04-14
MX2022016454A (es) 2023-03-06
AR122707A1 (es) 2022-09-28
IL299163A (en) 2023-02-01

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