TWI739783B - 作為nik抑制劑的新穎的經取代氰基吲哚啉衍生物 - Google Patents

作為nik抑制劑的新穎的經取代氰基吲哚啉衍生物 Download PDF

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TWI739783B
TWI739783B TW105143703A TW105143703A TWI739783B TW I739783 B TWI739783 B TW I739783B TW 105143703 A TW105143703 A TW 105143703A TW 105143703 A TW105143703 A TW 105143703A TW I739783 B TWI739783 B TW I739783B
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heterocyclic group
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TW105143703A
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TW201728577A (zh
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斯坦斯菲爾德 伊恩
凱羅勒 奧利弗亞歷西斯喬治
彭賽列 維吉尼亞蘇菲
葛洛斯 格哈德麥克斯
雅可比 埃德加
梅爾波 理文
庫拉格斯基 雅努什約瑟夫
麥克勞德 卡倫
曼 山缪愛德華
格林 賽門理查
海因德 喬治
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比利時商健生藥品公司
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    • 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
    • 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
    • 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)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW105143703A 2016-01-22 2017-01-20 作為nik抑制劑的新穎的經取代氰基吲哚啉衍生物 TWI739783B (zh)

Applications Claiming Priority (4)

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

Publications (2)

Publication Number Publication Date
TW201728577A TW201728577A (zh) 2017-08-16
TWI739783B true TWI739783B (zh) 2021-09-21

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TW105143703A TWI739783B (zh) 2016-01-22 2017-01-20 作為nik抑制劑的新穎的經取代氰基吲哚啉衍生物

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

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SI3405196T1 (sl) 2016-01-22 2020-03-31 Janssen Pharmaceutica Nv Novi substituirani derivati cianoindolina kot inhibitorji NIK
KR102720461B1 (ko) 2016-01-22 2024-10-21 잔센파마슈티카엔.브이. Nik 억제제로서의 신규 6원 헤테로방향족 치환된 시아노인돌린 유도체
ES2837157T3 (es) 2016-06-30 2021-06-29 Janssen Pharmaceutica Nv Derivados de cianoindolina como inhibidores de NIK
CA3027416A1 (en) 2016-06-30 2018-01-04 Janssen Pharmaceutica Nv Heteroaromatic 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
BR112020006294A2 (pt) * 2017-09-30 2020-10-06 Shanghai Haihe Pharmaceutical Co., Ltd. composto com atividade inibidora da erk quinase e seu uso
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
BR112021019508A2 (pt) * 2019-04-02 2022-02-01 Hinova Pharmaceuticals Inc Composto de amina aromática e uso do mesmo na preparação de reguladores e inibidores duplos de ar e brd4
RS66105B1 (sr) 2019-05-31 2024-11-29 Janssen Pharmaceutica Nv Inhibitori malih molekula nf-kb koji indukuju kinazu
WO2021242505A1 (en) 2020-05-08 2021-12-02 Halia Therapeutics, Inc. Inhibitors of nek7 kinase
US20240285599A1 (en) * 2021-08-23 2024-08-29 Osaka University Mature-Hepatocyte Transdifferentiation Suppressing Composition
WO2024059200A1 (en) 2022-09-14 2024-03-21 Halia Therapeutics, Inc. Nek7 inhibitors

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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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KR102720461B1 (ko) 2016-01-22 2024-10-21 잔센파마슈티카엔.브이. Nik 억제제로서의 신규 6원 헤테로방향족 치환된 시아노인돌린 유도체
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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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BR112018014675A2 (pt) 2018-12-11
CN108697710A (zh) 2018-10-23
JP6910359B2 (ja) 2021-07-28
MX2018008974A (es) 2018-11-09
HUE047684T2 (hu) 2020-05-28
AU2017209935A1 (en) 2018-08-09
EP3405196A1 (en) 2018-11-28
ZA201804688B (en) 2022-03-30
HRP20200133T1 (hr) 2020-05-15
PH12018501567A1 (en) 2019-01-28
SI3405196T1 (sl) 2020-03-31
DK3405196T3 (en) 2020-03-09
IL260500B (en) 2021-01-31
KR20180100441A (ko) 2018-09-10
LT3405196T (lt) 2020-02-25
US20210087182A1 (en) 2021-03-25
KR102784966B1 (ko) 2025-03-20
ES2775449T3 (es) 2020-07-27
BR112018014675B1 (pt) 2023-12-19
AU2017209935B2 (en) 2021-04-01
TW201728577A (zh) 2017-08-16
EP3405196B1 (en) 2019-12-04
US11180487B2 (en) 2021-11-23
CA3011880A1 (en) 2017-07-27
WO2017125530A1 (en) 2017-07-27
CN108697710B (zh) 2022-02-18
JP2019504067A (ja) 2019-02-14

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