AU2017209935B2 - New substituted cyanoindoline derivatives as NIK inhibitors - Google Patents

New substituted cyanoindoline derivatives as NIK inhibitors Download PDF

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Publication number
AU2017209935B2
AU2017209935B2 AU2017209935A AU2017209935A AU2017209935B2 AU 2017209935 B2 AU2017209935 B2 AU 2017209935B2 AU 2017209935 A AU2017209935 A AU 2017209935A AU 2017209935 A AU2017209935 A AU 2017209935A AU 2017209935 B2 AU2017209935 B2 AU 2017209935B2
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4alkyl
substituted
alkyl
het
optionally
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AU2017209935A1 (en
Inventor
Simon Richard Green
Gerhard Max GROSS
George Hynd
Edgar Jacoby
Janusz Jozef Kulagowski
Calum Macleod
Samuel Edward MANN
Lieven Meerpoel
Virginie Sophie Poncelet
Olivier Alexis Georges Querolle
Ian Stansfield
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • 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
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/535Organo-phosphoranes

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2017209935A 2016-01-22 2017-01-20 New substituted cyanoindoline derivatives as NIK inhibitors Active AU2017209935B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP16152416 2016-01-22
EP16152416.0 2016-01-22
EP16159651.5 2016-03-10
EP16159651 2016-03-10
PCT/EP2017/051150 WO2017125530A1 (en) 2016-01-22 2017-01-20 New substituted cyanoindoline derivatives as nik inhibitors

Publications (2)

Publication Number Publication Date
AU2017209935A1 AU2017209935A1 (en) 2018-08-09
AU2017209935B2 true AU2017209935B2 (en) 2021-04-01

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AU2017209935A Active AU2017209935B2 (en) 2016-01-22 2017-01-20 New substituted cyanoindoline derivatives as NIK inhibitors

Country Status (20)

Country Link
US (1) US11180487B2 (enExample)
EP (1) EP3405196B1 (enExample)
JP (1) JP6910359B2 (enExample)
KR (1) KR102784966B1 (enExample)
CN (1) CN108697710B (enExample)
AU (1) AU2017209935B2 (enExample)
BR (1) BR112018014675B1 (enExample)
CA (1) CA3011880A1 (enExample)
DK (1) DK3405196T3 (enExample)
ES (1) ES2775449T3 (enExample)
HR (1) HRP20200133T1 (enExample)
HU (1) HUE047684T2 (enExample)
IL (1) IL260500B (enExample)
LT (1) LT3405196T (enExample)
MX (1) MX2018008974A (enExample)
PH (1) PH12018501567A1 (enExample)
SI (1) SI3405196T1 (enExample)
TW (1) TWI739783B (enExample)
WO (1) WO2017125530A1 (enExample)
ZA (1) ZA201804688B (enExample)

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CN108697710B (zh) 2016-01-22 2022-02-18 杨森制药有限公司 作为nik抑制剂的新颖的经取代的氰基吲哚啉衍生物
US11001569B2 (en) 2016-01-22 2021-05-11 Janssen Pharmaceutica Nv 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors
US11136311B2 (en) 2016-06-30 2021-10-05 Janssen Pharmaceutica Nv Heteroaromatic derivatives as NIK inhibitors
AU2017289317B2 (en) 2016-06-30 2021-04-01 Janssen Pharmaceutica Nv Cyanoindoline derivatives as NIK inhibitors
WO2018019204A1 (zh) 2016-07-26 2018-02-01 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物
AU2018339722B2 (en) * 2017-09-30 2022-06-30 Haihe Biopharma Co., Ltd Compound having ERK kinase inhibitory activity and use thereof
TW202045008A (zh) 2019-02-01 2020-12-16 印度商皮埃企業有限公司 4-取代的異噁唑/異噁唑啉(雜)芳基脒化合物、及其製備與用途
CA3135929A1 (en) * 2019-04-02 2020-10-08 Hinova Pharmaceuticals Inc. Aromatic amine compound and use thereof in preparation of ar and brd4 dual inhibitors and regulators
PE20220768A1 (es) 2019-05-31 2022-05-16 Janssen Pharmaceutica Nv Inhibidores de molecula pequena de quinasa inductora de nf-kb
HUE068185T2 (hu) 2020-05-08 2024-12-28 Halia Therapeutics Inc NEK7-kináz inhibitorok
EP4393508A4 (en) * 2021-08-23 2024-12-04 Osaka University COMPOSITION FOR SUPPRESSING TRANSDIFFERENTIATION OF MATURE HEPATOCYTES
US20240158394A1 (en) 2022-09-14 2024-05-16 Halia Therapeutics, Inc. Nek7 inhibitors

Citations (1)

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WO2010042337A1 (en) * 2008-10-07 2010-04-15 Merck Sharp & Dohme Corp. Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity

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CA2441733A1 (en) * 2001-03-29 2002-10-10 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
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WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
EP2315751A1 (en) 2008-06-26 2011-05-04 Amgen Inc. Alkynyl alcohols as kinase inhibitors
TWI546290B (zh) 2008-06-27 2016-08-21 賽基艾維洛米斯研究股份有限公司 雜芳基化合物及其用途
CN102753177A (zh) 2009-08-17 2012-10-24 纪念斯隆-凯特琳癌症中心 热休克蛋白结合化合物、组合物以及其制备和使用方法
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
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US11001569B2 (en) 2016-01-22 2021-05-11 Janssen Pharmaceutica Nv 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors
CN108697710B (zh) 2016-01-22 2022-02-18 杨森制药有限公司 作为nik抑制剂的新颖的经取代的氰基吲哚啉衍生物
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Also Published As

Publication number Publication date
US11180487B2 (en) 2021-11-23
IL260500B (en) 2021-01-31
CN108697710B (zh) 2022-02-18
MX2018008974A (es) 2018-11-09
PH12018501567A1 (en) 2019-01-28
HUE047684T2 (hu) 2020-05-28
EP3405196A1 (en) 2018-11-28
CN108697710A (zh) 2018-10-23
KR102784966B1 (ko) 2025-03-20
EP3405196B1 (en) 2019-12-04
DK3405196T3 (en) 2020-03-09
JP6910359B2 (ja) 2021-07-28
TW201728577A (zh) 2017-08-16
AU2017209935A1 (en) 2018-08-09
BR112018014675B1 (pt) 2023-12-19
KR20180100441A (ko) 2018-09-10
SI3405196T1 (sl) 2020-03-31
BR112018014675A2 (pt) 2018-12-11
WO2017125530A1 (en) 2017-07-27
ES2775449T3 (es) 2020-07-27
TWI739783B (zh) 2021-09-21
ZA201804688B (en) 2022-03-30
HRP20200133T1 (hr) 2020-05-15
JP2019504067A (ja) 2019-02-14
CA3011880A1 (en) 2017-07-27
LT3405196T (lt) 2020-02-25
US20210087182A1 (en) 2021-03-25

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