PE20210662A1 - Activadores de la respuesta a proteinas desplegadas - Google Patents

Activadores de la respuesta a proteinas desplegadas

Info

Publication number
PE20210662A1
PE20210662A1 PE2020002206A PE2020002206A PE20210662A1 PE 20210662 A1 PE20210662 A1 PE 20210662A1 PE 2020002206 A PE2020002206 A PE 2020002206A PE 2020002206 A PE2020002206 A PE 2020002206A PE 20210662 A1 PE20210662 A1 PE 20210662A1
Authority
PE
Peru
Prior art keywords
halo
independently
compound
orc
orb
Prior art date
Application number
PE2020002206A
Other languages
English (en)
Inventor
David J Shapiro
Paul J Hergenrother
Matthew W Boudreau
Original Assignee
Univ Illinois
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 Univ Illinois filed Critical Univ Illinois
Publication of PE20210662A1 publication Critical patent/PE20210662A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32Oxygen atoms
    • C07D209/34Oxygen atoms in position 2
    • 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
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Referido a un compuesto de formula (I); en donde R1, R2, R3 y R4 son, independientemente, H, halo, -ORA, -SRA, entre otros; A1, A2, A3 y A4 son, independiente, H, halo, o alquilo; G1 es halo, -ORB, -SRB, entre otros; G2 es halo, -ORC, -SRC, entre otros; X y Z son, independientemente, O, S, o -NRD; y RA, RB, RC y RD son, independientemente, H o alquilo; en donde, cuando estan presentes, -ORB y -ORC no son ambos -OH. Un compuesto seleccionado es (S)- o (R)- 3-(4-hidroxifenil)-3-(4-metoxifenil)-7-(trifluorometil)indolin-2-ona. Dichos compuestos inhiben la proliferacion de las celulas cancerosas y destruyen las celulas cancerosas de mama, ovario y endometrio ER alfa positivas, lo que evita la reactivacion de los tumores anos despues. Tambien refiere una composicion farmaceutica que comprende dicho compuesto, siendo util en el tratamiento del cancer ER alfa positivo resistentes a la terapia en comparacion con BHPI y otras terapias convencionales (terapias endocrinas, tamoxifeno y fulvestrant/ICI).
PE2020002206A 2018-07-03 2019-07-01 Activadores de la respuesta a proteinas desplegadas PE20210662A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862693641P 2018-07-03 2018-07-03
PCT/US2019/040058 WO2020009958A1 (en) 2018-07-03 2019-07-01 Activators of the unfolded protein response

Publications (1)

Publication Number Publication Date
PE20210662A1 true PE20210662A1 (es) 2021-03-31

Family

ID=69059783

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2020002206A PE20210662A1 (es) 2018-07-03 2019-07-01 Activadores de la respuesta a proteinas desplegadas

Country Status (22)

Country Link
US (3) US20210276951A1 (es)
EP (1) EP3817741A4 (es)
JP (1) JP2021529757A (es)
KR (1) KR20210027382A (es)
CN (1) CN112423743A (es)
AU (1) AU2019299221A1 (es)
BR (1) BR112020025591A2 (es)
CA (1) CA3103958A1 (es)
CL (1) CL2020003423A1 (es)
CO (1) CO2020016690A2 (es)
CR (1) CR20210060A (es)
DO (1) DOP2020000256A (es)
EA (1) EA202190146A1 (es)
EC (1) ECSP20084330A (es)
IL (1) IL279429A (es)
JO (1) JOP20200344A1 (es)
MA (1) MA53105A (es)
MX (1) MX2021000043A (es)
PE (1) PE20210662A1 (es)
PH (1) PH12020552223A1 (es)
SG (1) SG11202012902WA (es)
WO (1) WO2020009958A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2021000043A (es) 2018-07-03 2021-03-25 Univ Illinois Activadores de la respuesta a proteinas desplegadas.
WO2021222738A1 (en) * 2020-05-01 2021-11-04 The Board Of Trustees Of The University Of Illinois Compounds for estrogen receptor positive cancers
WO2022020605A1 (en) * 2020-07-23 2022-01-27 The Board Of Trustees Of The University Of Illinois Treatment of metastasized estrogen receptor positive breast cancer
WO2022032146A1 (en) * 2020-08-07 2022-02-10 Systems Oncology, Llc Methods for inhibiting growth of era positive cancers
US20230391721A1 (en) * 2020-10-23 2023-12-07 The Board Of Trustees Of The University Of Illinois Anticancer compounds selective for er-positive cancers

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006508893A (ja) 2002-03-15 2006-03-16 イーライ・リリー・アンド・カンパニー ステロイドホルモン核内レセプターモジュレーターとしてのジヒドロインドール−2−オン誘導体
US20050070718A1 (en) 2003-09-30 2005-03-31 Abbott Gmbh & Co. Kg Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing them
JP4989976B2 (ja) * 2004-02-13 2012-08-01 プレジデント アンド フェロウズ オブ ハーバード カレッジ 翻訳開始阻害剤としての3−3−二置換オキシインドール
US7517899B2 (en) 2004-03-30 2009-04-14 Wyeth Phenylaminopropanol derivatives and methods of their use
US20070299102A1 (en) * 2004-04-08 2007-12-27 Topo Target A/S Diphenyl Ox-Indol-2-One Compounds and Their Use in the Treatment of Cancer
US20070072897A1 (en) 2005-09-29 2007-03-29 Wyeth Phenylaminopropanol derivatives and methods of their use
TW200817382A (en) 2006-08-24 2008-04-16 Wyeth Corp Process for preparing indolinone phenylaminopropanol derivatives
JP2010512355A (ja) 2006-12-11 2010-04-22 トポターゲット・アクティーゼルスカブ 癌の処置のためのジフェニルオキシ−インドール−2−オン化合物のプロドラッグ
AU2008240599A1 (en) * 2007-04-24 2008-10-30 Topotarget A/S Substituted 3-(4-hydroxyphenyl)-indolin-2-one-compounds
EP2520561B1 (en) 2007-06-08 2016-02-10 MannKind Corporation IRE-1A Inhibitors
WO2010109008A1 (en) 2009-03-26 2010-09-30 Topotarget A/S Prodrugs of substituted 3-(4-hydroxyphenyl)-indolin-2-ones
US20160106711A1 (en) 2012-09-20 2016-04-21 President And Fellows Of Harvard College 3-3-Di-Substituted-Oxindoles as Inhibitors of Translation Initiation
US9316631B1 (en) 2012-10-19 2016-04-19 Whitehead Institute For Biomedical Research ER-stress inducing compounds and methods of use thereof
WO2014113820A1 (en) * 2013-01-18 2014-07-24 Shapiro David J Estrogen receptor inhibitors
JP6806562B2 (ja) 2013-03-15 2021-01-06 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア eIF2α経路の調節因子
EP3004090B1 (en) 2013-05-28 2017-10-25 Astrazeneca AB Chemical compounds
MX2021000043A (es) 2018-07-03 2021-03-25 Univ Illinois Activadores de la respuesta a proteinas desplegadas.

Also Published As

Publication number Publication date
IL279429A (en) 2021-01-31
JOP20200344A1 (ar) 2020-12-31
MX2021000043A (es) 2021-03-25
CR20210060A (es) 2021-04-08
AU2019299221A1 (en) 2021-02-04
US20200190029A1 (en) 2020-06-18
DOP2020000256A (es) 2021-03-15
JP2021529757A (ja) 2021-11-04
US11584718B2 (en) 2023-02-21
CN112423743A (zh) 2021-02-26
US20210276951A1 (en) 2021-09-09
BR112020025591A2 (pt) 2021-03-23
SG11202012902WA (en) 2021-01-28
PH12020552223A1 (en) 2021-06-28
MA53105A (fr) 2021-05-12
CO2020016690A2 (es) 2021-01-18
WO2020009958A1 (en) 2020-01-09
EA202190146A1 (ru) 2021-04-27
EP3817741A1 (en) 2021-05-12
US11046647B2 (en) 2021-06-29
KR20210027382A (ko) 2021-03-10
CL2020003423A1 (es) 2021-05-14
EP3817741A4 (en) 2022-07-06
ECSP20084330A (es) 2021-01-29
CA3103958A1 (en) 2020-01-09
US20210340100A1 (en) 2021-11-04

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