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PE20230831A1 - Sintesis de intermedios para inhibidores de mcl-1 macrociclicos mediante un cierre de anillo - Google Patents

Sintesis de intermedios para inhibidores de mcl-1 macrociclicos mediante un cierre de anillo

Info

Publication number
PE20230831A1
PE20230831A1 PE2022002562A PE2022002562A PE20230831A1 PE 20230831 A1 PE20230831 A1 PE 20230831A1 PE 2022002562 A PE2022002562 A PE 2022002562A PE 2022002562 A PE2022002562 A PE 2022002562A PE 20230831 A1 PE20230831 A1 PE 20230831A1
Authority
PE
Peru
Prior art keywords
compound
inhibitors
synthesis
intermediates
mcl
Prior art date
Application number
PE2022002562A
Other languages
English (en)
Inventor
Austin G Smith
Jason S Tedrow
Gabrielle St-Pierre
Oliver Ralf Thiel
Liang Huang
Philipp C Roosen
John T Colyer
Kyle D Baucom
Ari Ericson
Matthew G Beaver
Rahul P Sangodkar
Michael A Lovette
Robert Ronald Milburn
Alan H Cherney
Sheng Cui
Original Assignee
Amgen 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 Amgen Inc filed Critical Amgen Inc
Publication of PE20230831A1 publication Critical patent/PE20230831A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/16—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with two six-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D281/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/08—Bridged 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Epidemiology (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Referido a un compuesto que tiene una estructura de compuesto D, o una de sus sales o solvatos, donde PG es un grupo protector de alcoholes, tal como un eter, un eter sililico, un acetal o cetal, o un acilo. Tambien se refiere a un proceso para sintetizar dicho compuesto D que comprende en mezclar un compuesto C, un agente activante, una base de tipo amina y un compuesto E en presencia de un disolvente; un proceso para sintetizar el compuesto A que comprende en mezclar un catalizador organometalico y un compuesto D en un disolvente, para formar un compuesto F y desprotegerlo para formar el compuesto A; dicho proceso tambien se utiliza para la sintesis de los compuestos intermedios A1 (13',13'-dioxido de (1S,3'R,6'R,7'S,8'E,11'S,12'R)-6-cloro-7'-metoxi-11',12'-dimetil-3,4-dihidro-2H,15'H-espiro[naftalen1,22'[20]oxa[13]tia[1,14]diazatetraciclo[14.7.2.03,6.019,24]pentacosa) y A2 (13',13'-dioxido de (1S,3'R,6'R,7'R,8'E,11'S,12'R)-6-cloro-7'-metoxi-11',12'-dimetil-7'-((9aR)-octahidro-2H-pirido[1,2-a]pirazin-2-ilmetil)-3,4-dihidro-2H,15'H-espiro[naftalen1,22'-[20]oxa[13]tia[1,14]diazatetraciclo[14.7.2.03,6.019,24]pentacosa[8,16,18,24]tetraen]-15'-ona). Dichos compuestos son inhibidores de la proteina de leucemia de celulas mieloides 1 (Mcl-1).
PE2022002562A 2020-05-06 2021-05-05 Sintesis de intermedios para inhibidores de mcl-1 macrociclicos mediante un cierre de anillo PE20230831A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202063020958P 2020-05-06 2020-05-06
PCT/US2021/030780 WO2021226168A1 (en) 2020-05-06 2021-05-05 Ring closing synthesis of macrocyclic mcl-1 inhibitor intermediates

Publications (1)

Publication Number Publication Date
PE20230831A1 true PE20230831A1 (es) 2023-05-19

Family

ID=76076546

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022002562A PE20230831A1 (es) 2020-05-06 2021-05-05 Sintesis de intermedios para inhibidores de mcl-1 macrociclicos mediante un cierre de anillo

Country Status (18)

Country Link
US (1) US20230167130A1 (es)
EP (1) EP4146638A1 (es)
JP (1) JP7585349B2 (es)
KR (1) KR20230008155A (es)
CN (1) CN115485269A (es)
AR (1) AR121999A1 (es)
AU (1) AU2021267335B2 (es)
BR (1) BR112022022434A2 (es)
CA (1) CA3180571A1 (es)
CL (1) CL2022003050A1 (es)
CO (1) CO2022016668A2 (es)
CR (1) CR20220621A (es)
IL (1) IL297457A (es)
MX (1) MX2022013873A (es)
PE (1) PE20230831A1 (es)
TW (1) TWI827924B (es)
UY (1) UY39198A (es)
WO (1) WO2021226168A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2020012137A (es) 2018-05-14 2021-01-29 Gilead Sciences Inc Inhibidores de mcl-1.
TWI778443B (zh) 2019-11-12 2022-09-21 美商基利科學股份有限公司 Mcl1抑制劑
PT4065567T (pt) 2019-11-26 2024-11-08 Gilead Sciences Inc Processos e intermediários para a preparação de inibidores de mcl1
JP2023550612A (ja) 2020-11-19 2023-12-04 ギリアード サイエンシーズ， インコーポレイテッド 大環状ｍｃｌ１阻害剤を調製するための方法及び中間体

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2401563T3 (es) 2009-03-06 2013-04-22 Rutgers, The State University Of New Jersey Derivados de metilendioxibenzo [I]fenantridina usados para tratar el cáncer
JO3474B1 (ar) * 2014-08-29 2020-07-05 Amgen Inc مشتقات تيتراهيدرونافثالين التي تثبط بروتين mcl-1
WO2017147410A1 (en) * 2016-02-25 2017-08-31 Amgen Inc. Compounds that inhibit mcl-1 protein
JP6453507B2 (ja) * 2017-03-30 2019-01-16 アムジエン・インコーポレーテツド Ｍｃｌ−１タンパク質を阻害する化合物
US11691989B2 (en) * 2018-11-22 2023-07-04 Ascentage Pharma (Suzhou) Co., Ltd. Macrocyclic indoles as Mcl-1 inhibitors

Also Published As

Publication number Publication date
CO2022016668A2 (es) 2022-11-29
WO2021226168A1 (en) 2021-11-11
JP2023524264A (ja) 2023-06-09
US20230167130A1 (en) 2023-06-01
EP4146638A1 (en) 2023-03-15
AU2021267335B2 (en) 2024-06-13
TW202208343A (zh) 2022-03-01
CL2022003050A1 (es) 2023-07-07
CR20220621A (es) 2023-01-23
AU2021267335A1 (en) 2022-12-15
KR20230008155A (ko) 2023-01-13
JP7585349B2 (ja) 2024-11-18
TWI827924B (zh) 2024-01-01
UY39198A (es) 2021-11-30
CA3180571A1 (en) 2021-11-11
AR121999A1 (es) 2022-08-03
MX2022013873A (es) 2022-11-30
CN115485269A (zh) 2022-12-16
IL297457A (en) 2022-12-01
BR112022022434A2 (pt) 2022-12-13

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