CR20220621A - Síntesis de intermedios para inhibidores de mcl-1 macrocíclicos mediante un cierre de anillo - Google Patents

Síntesis de intermedios para inhibidores de mcl-1 macrocíclicos mediante un cierre de anillo

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Publication number
CR20220621A
CR20220621A CR20220621A CR20220621A CR20220621A CR 20220621 A CR20220621 A CR 20220621A CR 20220621 A CR20220621 A CR 20220621A CR 20220621 A CR20220621 A CR 20220621A CR 20220621 A CR20220621 A CR 20220621A
Authority
CR
Costa Rica
Prior art keywords
eqn
prod
style
shape
sum
Prior art date
Application number
CR20220621A
Other languages
English (en)
Inventor
Philipp C Roosen
Alan H Cherney
Rahul P Sangodkar
Oliver Ralf Thiel
John T Colyer
Kyle D Baucom
Matthew G Beaver
Robert Ronald Milburn
Austin G Smith
Sheng Cui
Jason S Tedrow
Gabrielle St-Pierre
Liang Huang
Ari Ericson
Michael A Lovette
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 CR20220621A publication Critical patent/CR20220621A/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D267/00Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02Seven-membered rings
    • C07D267/08Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D267/00Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02Seven-membered rings
    • C07D267/08Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/16Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with two six-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D281/00Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/08Bridged systems
    • 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
    • A61K31/553Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

Landscapes

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

Abstract

En la presente se proporcionan procesos para sintetizar inhibidores de Mcl-1 e intermedios tales como el compuesto F que se pueden utilizar para prepararlos donde el PG variable es como se define en la presente. En particular, en la presente se proporcionan procesos para sintetizar el compuesto A1, y sus sales o solvatos, y el compuesto A2, y sus sales y solvatos. <!--[if gte vml 1]><v:shapetype id="_x0000_t75" coordsize="21600,21600" o:spt="75" o:preferrelative="t" path="m@4@5l@4@11@9@11@9@5xe" filled="f" stroked="f"> <v:stroke joinstyle="miter"/> <v:formulas> <v:f eqn="if lineDrawn pixelLineWidth 0"/> <v:f eqn="sum @0 1 0"/> <v:f eqn="sum 0 0 @1"/> <v:f eqn="prod @2 1 2"/> <v:f eqn="prod @3 21600 pixelWidth"/> <v:f eqn="prod @3 21600 pixelHeight"/> <v:f eqn="sum @0 0 1"/> <v:f eqn="prod @6 1 2"/> <v:f eqn="prod @7 21600 pixelWidth"/> <v:f eqn="sum @8 21600 0"/> <v:f eqn="prod @7 21600 pixelHeight"/> <v:f eqn="sum @10 21600 0"/> </v:formulas> <v:path o:extrusionok="f" gradientshapeok="t" o:connecttype="rect"/> <o:lock v:ext="edit" aspectratio="t"/></v:shapetype><v:shape id="Picture_x0020_3" o:spid="_x0000_i1027" type="#_x0000_t75" style='width:156.75pt;height:103.5pt;visibility:visible;mso-wrap-style:square'> <v:imagedata o:title=""/></v:shape><![endif]--> (F),<!--[if gte vml 1]><v:shape id="Picture_x0020_2" o:spid="_x0000_i1026" type="#_x0000_t75" style='width:159pt; height:102pt;visibility:visible;mso-wrap-style:square'> <v:imagedata o:title=""/></v:shape><![endif]--> (A1) <!--[if gte vml 1]><v:shape id="Picture_x0020_1" o:spid="_x0000_i1025" type="#_x0000_t75" style='width:156.75pt;height:125.25pt; visibility:visible;mso-wrap-style:square'> <v:imagedata o:title=""/></v:shape><![endif]--> (A2).<br />
CR20220621A 2020-05-06 2021-05-05 Síntesis de intermedios para inhibidores de mcl-1 macrocíclicos mediante un cierre de anillo CR20220621A (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
CR20220621A true CR20220621A (es) 2023-01-23

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CR20220621A CR20220621A (es) 2020-05-06 2021-05-05 Síntesis de intermedios para inhibidores de mcl-1 macrocíclicos mediante un cierre de anillo

Country Status (19)

Country Link
US (1) US12441741B2 (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)
JO (1) JOP20220289A1 (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 (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102551319B1 (ko) 2018-05-14 2023-07-05 길리애드 사이언시즈, 인코포레이티드 Mcl-1 억제제
TWI778443B (zh) 2019-11-12 2022-09-21 美商基利科學股份有限公司 Mcl1抑制劑
AU2020391106B2 (en) 2019-11-26 2024-03-21 Gilead Sciences, Inc. Processes and intermediates for preparing MCL1 inhibitors
EP4146205A4 (en) 2020-05-05 2024-05-29 Nuvalent, Inc. HETEROAROMATIC MACROCYCLIC ETHERS AS CHEMOTHERAPEUTIC AGENTS
WO2022108984A1 (en) 2020-11-19 2022-05-27 Gilead Sciences, Inc. Processes and intermediates for preparing macrocyclic mcl1 inhibitors

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY162157A (en) 2007-04-16 2017-05-31 Abbott Lab Substituted indole mcl-1 inhibitors
DK2403856T3 (da) 2009-03-06 2013-04-08 Univ Rutgers Methylendioxybenzo[i]phenanthridinderivater anvendt til behandling af cancer
JO3474B1 (ar) * 2014-08-29 2020-07-05 Amgen Inc مشتقات تيتراهيدرونافثالين التي تثبط بروتين mcl-1
US11306107B2 (en) * 2016-02-25 2022-04-19 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
EP3781570A4 (en) * 2018-11-22 2021-06-02 Ascentage Pharma (Suzhou) Co., Ltd. MACROCYCLIC INDOLES SERVING AS MCL-1 INHIBITORS

Also Published As

Publication number Publication date
BR112022022434A2 (pt) 2022-12-13
CO2022016668A2 (es) 2022-11-29
TWI827924B (zh) 2024-01-01
UY39198A (es) 2021-11-30
CL2022003050A1 (es) 2023-07-07
TW202208343A (zh) 2022-03-01
AU2021267335B2 (en) 2024-06-13
US20230167130A1 (en) 2023-06-01
WO2021226168A1 (en) 2021-11-11
US12441741B2 (en) 2025-10-14
JP2023524264A (ja) 2023-06-09
EP4146638A1 (en) 2023-03-15
AU2021267335A1 (en) 2022-12-15
CN115485269A (zh) 2022-12-16
JP7585349B2 (ja) 2024-11-18
KR20230008155A (ko) 2023-01-13
IL297457A (en) 2022-12-01
PE20230831A1 (es) 2023-05-19
JOP20220289A1 (ar) 2022-11-01
AR121999A1 (es) 2022-08-03
MX2022013873A (es) 2022-11-30
CA3180571A1 (en) 2021-11-11

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