CL2020003354A1 - Compuestos - Google Patents

Compuestos

Info

Publication number
CL2020003354A1
CL2020003354A1 CL2020003354A CL2020003354A CL2020003354A1 CL 2020003354 A1 CL2020003354 A1 CL 2020003354A1 CL 2020003354 A CL2020003354 A CL 2020003354A CL 2020003354 A CL2020003354 A CL 2020003354A CL 2020003354 A1 CL2020003354 A1 CL 2020003354A1
Authority
CL
Chile
Prior art keywords
compounds
manufacture
pharmaceutical compositions
active substances
provides compounds
Prior art date
Application number
CL2020003354A
Other languages
English (en)
Inventor
Martin Duplessis
Annick Goergler
Georg Jaeschke
Buelent Kocer
Bernd Kuhn
Kiel Lazarski
Yanke Liang
Yvonne Alice Nagel
Sander Ulrike Obst
Antonio Ricci
Daniel Rueher
Sandra Steiner
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of CL2020003354A1 publication Critical patent/CL2020003354A1/es

Links

Classifications

    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816—Wall or shell material
    • A61K9/4825—Proteins, e.g. gelatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/485—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4875—Compounds of unknown constitution, e.g. material from plants or animals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Botany (AREA)
  • Zoology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Dermatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

La presente invención proporciona compuestos que son inhibidores alostéricos selectivos de mutantes de EGFR que contienen T790M/L858R, T790M/L858R/C797S, L858R, L858R/C797S, su fabricación, composiciones farmacéuticas que los contienen y su utilización como sustancias terapéuticamente activas.
CL2020003354A 2018-06-29 2020-12-22 Compuestos CL2020003354A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP18180758 2018-06-29

Publications (1)

Publication Number Publication Date
CL2020003354A1 true CL2020003354A1 (es) 2021-07-19

Family

ID=62837714

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2020003354A CL2020003354A1 (es) 2018-06-29 2020-12-22 Compuestos

Country Status (20)

Country Link
US (1) US12209091B2 (es)
EP (1) EP3814351A1 (es)
JP (1) JP7411588B2 (es)
KR (1) KR20210025535A (es)
CN (1) CN112437774A (es)
AR (1) AR115663A1 (es)
AU (1) AU2019294414B2 (es)
BR (1) BR112020026450A2 (es)
CA (1) CA3103166A1 (es)
CL (1) CL2020003354A1 (es)
CR (1) CR20200625A (es)
IL (1) IL279800B2 (es)
MA (1) MA53003A (es)
MX (1) MX2020014085A (es)
PE (1) PE20211388A1 (es)
PH (1) PH12020552154A1 (es)
SG (1) SG11202011818YA (es)
TW (1) TWI833773B (es)
WO (1) WO2020002487A1 (es)
ZA (1) ZA202007956B (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2019291050A1 (en) 2018-06-22 2020-12-24 F. Hoffmann-La Roche Ag Oligonucleotides for modulating SCN9A expression
WO2020254565A1 (en) 2019-06-21 2020-12-24 F. Hoffmann-La Roche Ag Egfr inhibitors for the treatment of cancer
AR121167A1 (es) * 2019-06-21 2022-04-27 Hoffmann La Roche DERIVADOS DE PIRROLO[1,2-c]IMIDAZOL COMO INHIBIDORES DE EGFR
IL326872A (en) 2019-11-11 2026-04-01 Dana Farber Cancer Inst Inc EGFR allosteric inhibitors and methods of using them
AR120799A1 (es) * 2019-12-20 2022-03-16 Hoffmann La Roche 2-[4-cloro-6-[2-[4-[[4-(hidroximetil)-1-piperidil]metil]fenil]etinil]-1-oxoisoindolin-2-il]-2-(6,7-dihidro-5h-pirrolo[1,2-c]imidazol-1-il)-n-tiazol-2-il-acetamida como inhibidor de egfr
EP4681715A3 (en) 2019-12-20 2026-01-28 C4 Therapeutics, Inc. Isoindolinone and indazole compounds for the degradation of egfr
JP7785701B2 (ja) * 2020-06-09 2025-12-15 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド アロステリックｅｇｆｒ阻害剤及びその使用方法
WO2022117475A1 (en) * 2020-12-01 2022-06-09 F. Hoffmann-La Roche Ag New indazole derivatives
WO2022117487A1 (en) * 2020-12-01 2022-06-09 F. Hoffmann-La Roche Ag New indazole derivatives
US20240002390A1 (en) 2020-12-01 2024-01-04 Hoffmann-La Roche Inc. New indazole acetylene derivatives
JP2024521791A (ja) * 2021-05-26 2024-06-04 シーフォー セラピューティクス， インコーポレイテッド 脳又はｃｎｓへの癌転移を治療するためのｅｇｆｒデグレーダー
US20250129047A1 (en) 2021-07-04 2025-04-24 Newave Pharmaceutical Inc. Isoquinoline derivatives as mutant egfr modulators and uses thereof
EP4410307A4 (en) 2021-09-30 2026-05-06 Jiangsu Hengrui Pharmaceuticals Co Ltd PYRROLO BENZODIAZEPINE DERIVATIVE AND CONJUGATE, PROCESS FOR THEIR PREPARATION AND USE
EP4648765A1 (en) * 2023-01-11 2025-11-19 Dana-Farber Cancer Institute, Inc. Mutant-selective egfr inhibitors

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200804313A (en) * 2006-05-25 2008-01-16 Synta Pharmaceuticals Corp Triazole compounds that modulate HSP90 activity
JP5386350B2 (ja) 2006-05-31 2014-01-15 タケダ カリフォルニア インコーポレイテッド グルコキナーゼ活性剤としての、インダゾールおよびイソインドール誘導体
WO2009158369A1 (en) 2008-06-25 2009-12-30 Schering Corporation Synthesis and use of heterocyclic antibacterial agents
SG10201501062SA (en) 2010-02-11 2015-04-29 Celgene Corp Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
US8420661B2 (en) 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
CN102093339B (zh) 2010-12-09 2013-06-12 天津药物研究院 一类嘧啶衍生物的制备及用途
CN102060848B (zh) 2010-12-09 2013-09-18 天津药物研究院 芳香胺取代的嘧啶衍生物的制备及用途
EP3294705B1 (en) 2015-05-14 2021-07-21 The Wistar Institute Of Anatomy And Biology Ebna1 inhibitors and methods using same
CA2987914C (en) * 2015-06-30 2022-09-13 Dana-Farber Cancer Institute, Inc. Inhibitors of egfr and methods of use thereof
TW201834651A (zh) * 2016-12-22 2018-10-01 瑞士商赫孚孟拉羅股份公司 化合物
AR113299A1 (es) * 2017-06-02 2020-04-08 Hoffmann La Roche Compuestos de isoindolina

Also Published As

Publication number Publication date
CR20200625A (es) 2021-02-05
IL279800B1 (en) 2023-10-01
ZA202007956B (en) 2021-10-27
AU2019294414A1 (en) 2020-12-24
MA53003A (fr) 2021-05-05
CN112437774A (zh) 2021-03-02
IL279800A (en) 2021-03-01
TW202019930A (zh) 2020-06-01
JP7411588B2 (ja) 2024-01-11
MX2020014085A (es) 2021-03-09
CA3103166A1 (en) 2020-01-02
KR20210025535A (ko) 2021-03-09
JP2021529775A (ja) 2021-11-04
PH12020552154A1 (en) 2021-07-05
AU2019294414B2 (en) 2023-06-29
US20210079005A1 (en) 2021-03-18
IL279800B2 (en) 2024-02-01
BR112020026450A2 (pt) 2021-03-23
EP3814351A1 (en) 2021-05-05
WO2020002487A1 (en) 2020-01-02
AR115663A1 (es) 2021-02-10
TWI833773B (zh) 2024-03-01
SG11202011818YA (en) 2020-12-30
US12209091B2 (en) 2025-01-28
PE20211388A1 (es) 2021-07-27

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