ES2643164T3 - Indol 7-sustituido como inhibidores de Mcl-1 - Google Patents

Indol 7-sustituido como inhibidores de Mcl-1 Download PDF

Info

Publication number
ES2643164T3
ES2643164T3 ES08745970T ES08745970T ES2643164T3 ES 2643164 T3 ES2643164 T3 ES 2643164T3 ES 08745970 T ES08745970 T ES 08745970T ES 08745970 T ES08745970 T ES 08745970T ES 2643164 T3 ES2643164 T3 ES 2643164T3
Authority
ES
Spain
Prior art keywords
mcl
inhibitors
substituted indole
indole
substituted
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES08745970T
Other languages
English (en)
Inventor
Steven W. Elmore
Andrew J. Souers
Milan Bruncko
Xiaohong Song
Xilu Wang
Lisa A. Hasvold
Le Wang
Aaron R. Kunzer
Cheol-Min Park
Michael D. Wendt
Zhi-Fu Tao
David Madar
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
AbbVie Inc
Original Assignee
AbbVie 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 AbbVie Inc filed Critical AbbVie Inc
Application granted granted Critical
Publication of ES2643164T3 publication Critical patent/ES2643164T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/113Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
ES08745970T 2007-04-16 2008-04-16 Indol 7-sustituido como inhibidores de Mcl-1 Active ES2643164T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US91203807P 2007-04-16 2007-04-16
US94965007P 2007-07-13 2007-07-13
PCT/US2008/060472 WO2008131000A2 (en) 2007-04-16 2008-04-16 7-substituted indole mcl-1 inhibitors

Publications (1)

Publication Number Publication Date
ES2643164T3 true ES2643164T3 (es) 2017-11-21

Family

ID=39791546

Family Applications (2)

Application Number Title Priority Date Filing Date
ES17174968T Active ES2705599T3 (es) 2007-04-16 2008-04-16 Indoles sustituidos en la posición 7 como inhibidores de mcl-1
ES08745970T Active ES2643164T3 (es) 2007-04-16 2008-04-16 Indol 7-sustituido como inhibidores de Mcl-1

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES17174968T Active ES2705599T3 (es) 2007-04-16 2008-04-16 Indoles sustituidos en la posición 7 como inhibidores de mcl-1

Country Status (18)

Country Link
US (3) US8445679B2 (es)
EP (2) EP2134684B1 (es)
JP (2) JP5496877B2 (es)
KR (1) KR101511074B1 (es)
CN (1) CN101743224A (es)
AU (1) AU2008242983B2 (es)
BR (1) BRPI0810365A2 (es)
CA (1) CA2682356C (es)
CO (1) CO6220947A2 (es)
CR (1) CR11107A (es)
DO (1) DOP2009000246A (es)
ES (2) ES2705599T3 (es)
IL (1) IL201432A0 (es)
MX (1) MX2009011211A (es)
MY (1) MY162157A (es)
NZ (1) NZ579833A (es)
WO (1) WO2008131000A2 (es)
ZA (1) ZA200906956B (es)

Families Citing this family (94)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7981888B2 (en) 2007-04-16 2011-07-19 Abbott Laboratories 1-oxyalkyl-2-carboxyl-7-nonsubstituted indole derivatives
ES2705599T3 (es) 2007-04-16 2019-03-26 Abbvie Inc Indoles sustituidos en la posición 7 como inhibidores de mcl-1
WO2009143578A1 (en) * 2008-05-28 2009-12-03 The Council Of The Queensland Institute Of Medical Research Cancer drug target and methods of diagnosis and therapy
NZ593536A (en) * 2008-12-19 2013-07-26 Genentech Inc Quinoline derivatives and methods of use
NZ593537A (en) * 2008-12-19 2013-07-26 Genentech Inc Isoquinoline derivatives and methods of use
EP3138838A1 (en) * 2010-01-29 2017-03-08 Dana-Farber Cancer Institute, Inc. Small molecules for the modulation of mcl-1 and methods of modulating cell death, cell division, cell differentiation and methods of treating disorders
ES2659763T3 (es) 2011-02-14 2018-03-19 The Regents Of The University Of Michigan Composiciones y procedimientos para el tratamiento de obesidad y trastornos relacionados
JP2014122161A (ja) * 2011-03-31 2014-07-03 Astellas Pharma Inc ピラゾール化合物
US9102673B2 (en) 2011-07-12 2015-08-11 Merck Sharp & Dohme Corp. Substituted pyrrolo[3,2-c]pyridines as TrkA kinase inhibitors
FR2986002B1 (fr) 2012-01-24 2014-02-21 Servier Lab Nouveaux derives d'indolizine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US9926306B2 (en) 2012-03-20 2018-03-27 Dana-Farber Cancer Institute, Inc. Inhibition of MCL-1 and/or BFL-1/A1
WO2013149124A1 (en) 2012-03-29 2013-10-03 The Regents Of The University Of Michigan Small molecule inhibitors of mcl-1 and uses thereof
WO2014047427A2 (en) * 2012-09-21 2014-03-27 Vanderbilt University Substituted benzofuran, benzothiophene and indole mcl-1 inhibitors
AU2013326867B2 (en) * 2012-10-05 2018-03-08 Rigel Pharmaceuticals, Inc. GDF-8 inhibitors
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
US9365581B2 (en) 2013-05-02 2016-06-14 The Regents Of The University Of Michigan Deuterated amlexanox
FR3008977A1 (fr) 2013-07-23 2015-01-30 Servier Lab Nouveaux derives d'isoindoline ou d'isoquinoline, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
FR3008976A1 (fr) 2013-07-23 2015-01-30 Servier Lab "nouveaux derives d'indolizine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent"
FR3008979B1 (fr) * 2013-07-23 2015-07-24 Servier Lab Nouveaux derives phosphates, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
CA2922341C (en) 2013-08-28 2022-06-07 Vanderbilt University Substituted indole mcl-1 inhibitors
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
JP6757312B2 (ja) 2014-03-27 2020-09-16 ヴァンダービルト ユニバーシティー 置換インドールmcl−1阻害剤
ES2763527T3 (es) 2014-04-04 2020-05-29 Univ Michigan Regents Inhibidores de molécula pequeña de mcl-1 y usos de los mismos
JO3474B1 (ar) 2014-08-29 2020-07-05 Amgen Inc مشتقات تيتراهيدرونافثالين التي تثبط بروتين mcl-1
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
JP2017528498A (ja) 2014-09-25 2017-09-28 アラクセス ファーマ エルエルシー Kras g12c変異体タンパク質のインヒビター
US9949965B2 (en) 2014-10-17 2018-04-24 Vanderbilt University Tricyclic indole Mcl-1 inhibitors and uses thereof
ES2803581T3 (es) 2014-10-29 2021-01-28 Walter & Eliza Hall Inst Medical Res Inhibidores de Mcl-1 para su uso en el tratamiento de enfermedades provocadas por neovascularización patológica
CN104557665B (zh) * 2015-01-09 2016-11-30 华东师范大学 光学活性3-取代吲哚衍生物及其合成方法和应用
MX382355B (es) 2015-04-10 2025-03-13 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos.
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
US10463649B2 (en) 2015-06-08 2019-11-05 Texas Tech University System Inhibitors of Mc1-1 as drugs to overcome resistance to BRAF inhibitors and MEK inhibitors
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058792A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017070256A2 (en) 2015-10-19 2017-04-27 Araxes Pharma Llc Method for screening inhibitors of ras
US11866409B2 (en) 2015-11-02 2024-01-09 Carmel-Haifa University Economic Corporation Ltd. Apoptosis related protein in the tgf-beta signaling pathway (ARTS) mimetic compounds, compositions, methods and uses thereof in induction of differentiation and/or apoptosis of premalignant and malignant cells, thereby restoring their normal-like phenotype
EP3377481A1 (en) 2015-11-16 2018-09-26 Araxes Pharma LLC 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
GB201521059D0 (en) * 2015-11-30 2016-01-13 Isis Innovation Inhibitors of metallo-beta-lactamases
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
EP3407974A4 (en) 2016-01-29 2019-08-28 The Regents Of The University Of Michigan Amlexanox Analogs
WO2017147410A1 (en) 2016-02-25 2017-08-31 Amgen Inc. Compounds that inhibit mcl-1 protein
AU2017228385B2 (en) 2016-03-04 2021-11-04 Vanderbilt University Substituted indole Mcl-1 inhibitors
KR101885084B1 (ko) 2016-03-24 2018-08-03 기초과학연구원 N-아실 인돌 유도체의 아민화 방법
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
SMT202000249T1 (it) * 2016-04-22 2020-07-08 Astrazeneca Ab Inibitori di mcl1 macrociclici per il trattamento di cancro
US10981932B2 (en) * 2016-05-19 2021-04-20 Bayer Aktiengesellschaft Macrocyclic indole derivatives
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
EP3519402A1 (en) 2016-09-29 2019-08-07 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
WO2018140513A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
US11358959B2 (en) 2017-01-26 2022-06-14 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
CN110382482A (zh) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 稠合的杂-杂二环化合物及其使用方法
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
TW201904976A (zh) * 2017-03-31 2019-02-01 瑞典商阿斯特捷利康公司 Mcl-1抑制劑及其使用方法
JP2020521741A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー がんの処置のための化合物およびその使用の方法
CN110831933A (zh) 2017-05-25 2020-02-21 亚瑞克西斯制药公司 喹唑啉衍生物作为突变kras、hras或nras的调节剂
CN110869358A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 Kras的共价抑制剂
MA49908A (fr) 2017-08-18 2021-04-28 Amgen Inc Composés inhibant la protéine mcl-1
EP3668876B1 (en) 2017-08-18 2024-01-24 Cothera Bioscience, Inc. Polymorphic form of tg02
US11279712B2 (en) 2017-08-29 2022-03-22 Amgen Inc. Macrocyclic compounds that inhibit MCL-1 protein
US11447504B2 (en) 2017-11-17 2022-09-20 Bayer Aktiengesellschaft Macrocyclic chlorine substituted indole derivatives
AR113886A1 (es) 2017-11-17 2020-06-24 Broad Inst Inc Derivados de indol macrocíclicos
US11286263B2 (en) 2017-11-17 2022-03-29 The Broad Institute, Inc. Macrocyclic fluorine substituted indole derivatives
TWI810220B (zh) 2017-11-17 2023-08-01 德商拜耳廠股份有限公司 經取代之巨環吲哚衍生物
WO2019096905A1 (en) 2017-11-17 2019-05-23 Bayer Aktiengesellschaft Macrocyclic chlorine substituted indole derivatives
MA54985A (fr) 2018-03-05 2021-12-29 Amgen Inc Pharmacophores d'acide alpha-hydroxy phénylacétique ou antagonistes de la protéine bio-isostère mcl-1
BR112021001709A2 (pt) 2018-08-01 2021-05-04 Araxes Pharma Llc compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer
AU2019347963A1 (en) * 2018-09-30 2021-05-27 Jiangsu Hengrui Medicine Co., Ltd. Indole macrocyclic derivative, preparation method therefor and application thereof in medicine
US12319703B2 (en) 2019-01-23 2025-06-03 Ascentage Pharma (Suzhou) Co., Ltd. Macrocyclic fused pyrazoles as Mcl-1 inhibitors
CN113574058B (zh) * 2019-04-30 2024-04-16 江苏恒瑞医药股份有限公司 吲哚类大环衍生物、其制备方法及其在医药上的应用
US12338250B2 (en) 2019-05-17 2025-06-24 The Broad Institute, Inc. Methods of preparing macrocyclic indoles
KR20220044721A (ko) * 2019-08-06 2022-04-11 도메인 테라퓨틱스 신경펩타이드 ff 수용체 길항제로서의 5-헤테로아릴-피리딘-2-아민 화합물
MX2022006179A (es) 2019-11-21 2022-06-14 Janssen Pharmaceutica Nv Derivados macrociclicos de indol como inhibidores de mcl-1.
MX2022006180A (es) 2019-11-21 2022-06-14 Janssen Pharmaceutica Nv Derivados macrociclicos de sulfonilo como inhibidores de mcl-1.
CN112898224B (zh) * 2019-12-04 2023-02-17 中国科学院上海药物研究所 一种烯丙基醇支撑的大环内酯化合物及其用途
TWI827924B (zh) 2020-05-06 2024-01-01 美商安進公司 大環Mcl-1抑制劑中間體的閉環合成
KR20230017823A (ko) 2020-05-29 2023-02-06 얀센 파마슈티카 엔.브이. Mcl-1의 억제제로서의 마크로사이클릭 7-피라졸-5-일-인돌 유도체
AU2021291056A1 (en) 2020-06-19 2023-02-23 Janssen Pharmaceutica Nv N-linked macrocyclic 7-(pyrazol-5-yl)-indole derivatives as inhibitors of MCL-1
ES2994690T3 (en) * 2020-06-19 2025-01-30 Janssen Pharmaceutica Nv N-linked macrocyclic 4-(pyrazol-5-yl)-indole derivatives as inhibitors of mcl-1
WO2022255888A1 (en) * 2021-06-01 2022-12-08 Captor Therapeutics S.A. Targeted protein degradation using bifunctional compounds that bind ubiquitin ligase and target mcl-1 protein
JP7673255B2 (ja) 2021-06-11 2025-05-08 ギリアード サイエンシーズ, インコーポレイテッド Mcl-1阻害剤と抗体薬物コンジュゲートとの組み合わせ
TWI910028B (zh) 2021-06-11 2025-12-21 美商基利科學股份有限公司 Mcl-1抑制劑與抗癌劑之組合
EP4630414A1 (en) * 2022-12-06 2025-10-15 Captor Therapeutics S.A. Targeted protein degradation using bifunctional compounds that bind ubiquitin ligase and target mcl-1 protein
WO2024123195A1 (en) * 2022-12-06 2024-06-13 Captor Therapeutics S.A. Targeted protein degradation using prodrugs of bifunctional compounds that bind ubiquitin ligase and target mcl-1 protein

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB888426A (en) * 1957-08-02 1962-01-31 Lab Francais Chimiotherapie Tryptamine-2-carboxylic acid derivatives and their preparation
US3303195A (en) * 1957-10-31 1967-02-07 Roussel Uclaf Methylated deserpidine
US3578669A (en) * 1969-09-16 1971-05-11 Sterling Drug Inc 1-((2 - substituted - 3 - indolyl) - lower-alkanoyl) - cycloalkyl - lower-alkylpiperidines and 1 - ((2 - hydroxymethyl-3 - indolyl)-lower-alkayl)-cycloalkyl-lower-alkylpiperidines
AR205437A1 (es) * 1972-09-25 1976-05-07 Hoffmann La Roche Procedimiento para la preparacion de derivados de indoloquinolinona
US4014883A (en) 1973-09-10 1977-03-29 Hoffmann-La Roche Inc. Indoloquinolines, intermediates and processes
CA1299174C (en) 1987-02-02 1992-04-21 Michael Edward Flaugh Alkylmelatonins
CS270491B1 (cs) * 1988-10-20 1990-06-13 Magdalena Ing Stankova Způsob výroby kyseliny 7-ethyl-2-karboxyindol- -3—yloclové
FR2662713B1 (fr) * 1990-05-29 1994-04-08 Oreal Procede de teinture de fibres keratiniques avec un aminoindole associe a un derive quinonique.
JP3545461B2 (ja) * 1993-09-10 2004-07-21 エーザイ株式会社 二環式ヘテロ環含有スルホンアミド誘導体
PT673937E (pt) * 1993-09-10 2004-04-30 Eisai Co Ltd Derivados biciclicos heterociclicos de sulfonamida e de ester sulfonico
WO1997006141A1 (en) * 1995-08-04 1997-02-20 Otsuka Kagaku Kabushiki Kaisha Indole-2-carboxylic ester derivatives and agricultural and horticultural bacteriocides containing the same as the active ingredient
US6077812A (en) * 1997-02-26 2000-06-20 Fmc Corporation Cycloimido-substituted benzofused heterocyclic herbicides
GB9716657D0 (en) 1997-08-07 1997-10-15 Zeneca Ltd Chemical compounds
CO4970713A1 (es) 1997-09-19 2000-11-07 Sanofi Synthelabo Derivados de carboxamidotiazoles, su preparacion, composiciones farmaceuticas que los contienen
DE60113865T2 (de) 2000-07-31 2006-07-20 Vernalis Research Ltd., Winnersh Piperazin derivate
JP2004529855A (ja) * 2000-10-10 2004-09-30 スミスクライン ビーチャム コーポレーション 置換インドール類、そのような置換インドール類を含む医薬組成物及びPPAR−γ結合剤としてのそれらの使用
EP1314733A1 (en) 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
SE0302035D0 (sv) 2003-07-09 2003-07-09 Biolipox Ab New compound
CA2528626A1 (en) * 2003-07-09 2005-01-20 Biolipox Ab Indoles useful in the treatment of inflammation
CN102358738A (zh) 2003-07-30 2012-02-22 里格尔药品股份有限公司 2,4-嘧啶二胺化合物及其预防和治疗自体免疫疾病的用途
EP1663242B1 (en) 2003-08-07 2011-04-27 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and uses as anti-proliferative agents
US7268159B2 (en) 2003-09-25 2007-09-11 Wyeth Substituted indoles
WO2005049593A2 (en) 2003-11-13 2005-06-02 Abbott Laboratories N-acylsulfonamide apoptosis promoters
WO2006041961A1 (en) 2004-10-05 2006-04-20 GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTHAND HUMAN SERVICES Arylthioindole tubulin polymerization inhibitors and methods of treating or preventing cancer using same
JP5024039B2 (ja) 2005-02-25 2012-09-12 小野薬品工業株式会社 インドール化合物およびその用途
JP4415896B2 (ja) * 2005-04-20 2010-02-17 トヨタ自動車株式会社 車両用空調装置
JP5094394B2 (ja) * 2005-04-20 2012-12-12 武田薬品工業株式会社 縮合複素環化合物
DE102005022977A1 (de) 2005-05-19 2006-12-07 Merck Patent Gmbh Phenylchinazolinderivate
JP5193861B2 (ja) * 2005-07-07 2013-05-08 アボット・ラボラトリーズ アポトーシス促進剤
UA95788C2 (en) 2005-12-15 2011-09-12 Ф. Хоффманн-Ля Рош Аг Fused pyrrole derivatives
UA97257C2 (en) * 2006-10-19 2012-01-25 Такеда Фармасьютикал Компани Лимитед Indole derivatives
US20100183658A1 (en) * 2007-03-30 2010-07-22 The Brigham And Women's Hospital, Inc. Novel Compounds for Enhancing MHC Class II Therapies
ES2705599T3 (es) 2007-04-16 2019-03-26 Abbvie Inc Indoles sustituidos en la posición 7 como inhibidores de mcl-1
US7981888B2 (en) 2007-04-16 2011-07-19 Abbott Laboratories 1-oxyalkyl-2-carboxyl-7-nonsubstituted indole derivatives

Also Published As

Publication number Publication date
US9035047B2 (en) 2015-05-19
US20140051683A1 (en) 2014-02-20
ES2705599T3 (es) 2019-03-26
NZ579833A (en) 2012-11-30
IL201432A0 (en) 2010-05-31
CA2682356C (en) 2016-06-14
DOP2009000246A (es) 2009-11-15
EP3243814A1 (en) 2017-11-15
ZA200906956B (en) 2011-03-30
WO2008131000A3 (en) 2008-12-18
US8445679B2 (en) 2013-05-21
US20150284328A1 (en) 2015-10-08
MX2009011211A (es) 2009-10-30
AU2008242983B2 (en) 2013-07-11
CR11107A (es) 2010-02-09
EP2134684A2 (en) 2009-12-23
AU2008242983A1 (en) 2008-10-30
MY162157A (en) 2017-05-31
JP5745661B2 (ja) 2015-07-08
RU2009141986A (ru) 2011-05-27
BRPI0810365A2 (pt) 2014-10-29
JP5496877B2 (ja) 2014-05-21
CN101743224A (zh) 2010-06-16
US20090054402A1 (en) 2009-02-26
KR20090130137A (ko) 2009-12-17
US9359296B2 (en) 2016-06-07
JP2014129399A (ja) 2014-07-10
EP3243814B1 (en) 2018-10-17
CA2682356A1 (en) 2008-10-30
EP2134684B1 (en) 2017-08-02
KR101511074B1 (ko) 2015-04-13
CO6220947A2 (es) 2010-11-19
JP2010524956A (ja) 2010-07-22
WO2008131000A2 (en) 2008-10-30

Similar Documents

Publication Publication Date Title
IL201432A0 (en) 7 - substituted indole mcl - 1 inhibitors
BRPI0811065A2 (pt) Indazóis 5-heteroaril substituídos como inibidores de quinase
BRPI0715324A2 (pt) Composto de indol
PT2134685E (pt) Derivados de índole não substituídos na posição 7 como inibidores de mcl-1
DOP2012000282A (es) Indoles sustituidos como inhibidores ezh2
BRPI0809221A2 (pt) indol carboxamidas como inibidores de ikk2
BRPI0914942A2 (pt) Compostos de oxindol
BRPI1008749A2 (pt) Derivados de benzodiazepina
BRPI0812825A2 (pt) Derivados ftalazinona como inibidores de parp-1
BR112012006630A2 (pt) derivados em indol como moduladores dos canais de cálcio ativados para liberação de cálcio (crac)
BRPI0920135A2 (pt) imidazopiridazinacarbonitrilos úteis como inibidores de quinase
BRPI0913879A2 (pt) fenilpirazinonas como inibidores de quinase
PT2860179T (pt) Derivados de pirazolo-piridina como inibidores de nadph-oxidase
ATE549340T1 (de) Spiroindolinon-derivate als mdm2-p53 inhibitoren
BRPI1008855A2 (pt) derivados de indol como agentes anticâncer
IL207684A0 (en) Substituted indole derivatives
EP2079466A4 (en) SUBSTITUTED INDOLE COMPOUNDS
BRPI0912234A2 (pt) derivados de salinosporamida como inibidores de proteassomas
BRPI0818338A2 (pt) Composto de pirimidil indolina
GB0905328D0 (en) Indole derivatives
DE112009000578A5 (de) Reibahle
CR10879A (es) Cyclized derivatives as eg-5 inhibitors
BRPI0915887A2 (pt) derivados de indol macrocíclicos úteis como inibidores do vírus da hepatite c
ATE545635T1 (de) Substituierte n-oxidpyrazinderivate
BR112013013037A2 (pt) derivados de indol como moduladores dos receptores de s1p