AU2017289317B2 - Cyanoindoline derivatives as NIK inhibitors - Google Patents

Cyanoindoline derivatives as NIK inhibitors Download PDF

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Publication number
AU2017289317B2
AU2017289317B2 AU2017289317A AU2017289317A AU2017289317B2 AU 2017289317 B2 AU2017289317 B2 AU 2017289317B2 AU 2017289317 A AU2017289317 A AU 2017289317A AU 2017289317 A AU2017289317 A AU 2017289317A AU 2017289317 B2 AU2017289317 B2 AU 2017289317B2
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substituted
4alkyl
ring
alkyl
optionally
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AU2017289317A1 (en
Inventor
Simon Richard Green
Gerhard Max GROSS
George Hynd
Edgar Jacoby
Janusz Jozef Kulagowski
Yannick Aime Eddy Ligny
Calum Macleod
Samuel Edward MANN
Lieven Meerpoel
Olivier Alexis Georges Querolle
Ian Stansfield
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5365—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2017289317A 2016-06-30 2017-06-29 Cyanoindoline derivatives as NIK inhibitors Active AU2017289317B2 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
EP16177131.6 2016-06-30
EP16177147 2016-06-30
EP16177131 2016-06-30
EP16177142 2016-06-30
EP16177142.3 2016-06-30
EP16177147.2 2016-06-30
PCT/EP2017/066125 WO2018002219A1 (en) 2016-06-30 2017-06-29 Cyanoindoline derivatives as nik inhibitors

Publications (2)

Publication Number Publication Date
AU2017289317A1 AU2017289317A1 (en) 2019-01-17
AU2017289317B2 true AU2017289317B2 (en) 2021-04-01

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Family Applications (1)

Application Number Title Priority Date Filing Date
AU2017289317A Active AU2017289317B2 (en) 2016-06-30 2017-06-29 Cyanoindoline derivatives as NIK inhibitors

Country Status (8)

Country Link
US (2) US20190119299A1 (cg-RX-API-DMAC7.html)
EP (1) EP3478673B1 (cg-RX-API-DMAC7.html)
JP (1) JP6936814B2 (cg-RX-API-DMAC7.html)
KR (1) KR102587619B1 (cg-RX-API-DMAC7.html)
CN (1) CN109689645B (cg-RX-API-DMAC7.html)
AU (1) AU2017289317B2 (cg-RX-API-DMAC7.html)
ES (1) ES2837157T3 (cg-RX-API-DMAC7.html)
WO (1) WO2018002219A1 (cg-RX-API-DMAC7.html)

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WO2017125534A1 (en) 2016-01-22 2017-07-27 Janssen Pharmaceutica Nv New 6-membered heteroaromatic substituted cyanoindoline derivatives as nik inhibitors
JP6910359B2 (ja) 2016-01-22 2021-07-28 ヤンセン ファーマシューティカ エヌ．ベー． Ｎｉｋ阻害剤としての新たな置換されたシアノインドリン誘導体
JP6936815B2 (ja) 2016-06-30 2021-09-22 ヤンセン ファーマシューティカ エヌ．ベー． Ｎｉｋ阻害剤としてのヘテロ芳香族誘導体
AU2017289317B2 (en) 2016-06-30 2021-04-01 Janssen Pharmaceutica Nv Cyanoindoline derivatives as NIK inhibitors
FI3976597T3 (fi) 2019-05-31 2024-09-25 Janssen Pharmaceutica Nv Nf-kb:tä indusoivan kinaasin pienimolekyylisiä estäjiä
EP3994133A4 (en) * 2019-07-04 2023-11-22 Qilu Regor Therapeutics Inc. Hpk1 inhibitors and uses thereof
TW202304906A (zh) * 2021-04-08 2023-02-01 大陸商杭州阿諾生物醫藥科技有限公司 高活性hpk1激酶抑制劑
CN114380806B (zh) * 2022-03-24 2022-06-10 中国药科大学 2-氨基-4-吲哚基嘧啶类化合物及其制备方法与应用

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JP6936815B2 (ja) 2016-06-30 2021-09-22 ヤンセン ファーマシューティカ エヌ．ベー． Ｎｉｋ阻害剤としてのヘテロ芳香族誘導体

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WO2002079197A1 (en) * 2001-03-29 2002-10-10 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
WO2010042337A1 (en) * 2008-10-07 2010-04-15 Merck Sharp & Dohme Corp. Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity
WO2014174021A1 (en) * 2013-04-24 2014-10-30 Janssen Pharmaceutica Nv 3-(2-aminopyrimidin-4-yl)-5-(3-hydroxypropynyl)-1h-pyrrolo[2,3-c]pyridine derivatives as nik inhibitors for the treatment of cancer
WO2015044267A1 (en) * 2013-09-26 2015-04-02 Janssen Pharmaceutica Nv NEW 1-(4-PYRIMIDINYL)-1H-PYRROLO[3,2-c]PYRIDINE DERIVATIVES AS NIK INHIBITORS
WO2015044269A1 (en) * 2013-09-26 2015-04-02 Janssen Pharmaceutica Nv NEW 3-(1H-PYRAZOL-4-YL)-1H-PYRROLO[2,3-c]PYRIDINE DERIVATIVES AS NIK INHIBITORS

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EP3478673A1 (en) 2019-05-08
CN109689645B (zh) 2022-06-03
KR102587619B1 (ko) 2023-10-11
EP3478673B1 (en) 2020-09-16
AU2017289317A1 (en) 2019-01-17
WO2018002219A1 (en) 2018-01-04
US11186589B2 (en) 2021-11-30
ES2837157T3 (es) 2021-06-29
JP2019524646A (ja) 2019-09-05
CA3027418A1 (en) 2018-01-04
US20210032267A1 (en) 2021-02-04
US20190119299A1 (en) 2019-04-25
KR20190025949A (ko) 2019-03-12
JP6936814B2 (ja) 2021-09-22
CN109689645A (zh) 2019-04-26

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Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ STANSFIELD, IAN; QUEROLLE, OLIVIER ALEXIS GEORGES; LIGNY, YANNICK AIME EDDY; GROSS, GERHARD MAX; JACOBY, EDGAR; MEERPOEL, LIEVEN; GREEN, SIMON RICHARD; HYND, GEORGE; KULAGOWSKI, JANUSZ JOZEF; MACLEOD, CALUM AND MANN, SAMUEL EDWARD

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