KR102784966B1 - Nik 억제제로서 신규 치환된 시아노인돌린 유도체 - Google Patents

Nik 억제제로서 신규 치환된 시아노인돌린 유도체 Download PDF

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KR102784966B1
KR102784966B1 KR1020187024257A KR20187024257A KR102784966B1 KR 102784966 B1 KR102784966 B1 KR 102784966B1 KR 1020187024257 A KR1020187024257 A KR 1020187024257A KR 20187024257 A KR20187024257 A KR 20187024257A KR 102784966 B1 KR102784966 B1 KR 102784966B1
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cycloalkyl
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KR20180100441A (ko
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이안 스탠스필드
올리비에 알렉시스 조르쥬 퀘롤
버지니 소피 퐁슬레
게르하르트 맥스 그로스
에드가 야코비
리벤 미어푈
리벤 미어?O
자너즈 조제프 쿨라고프스키
칼룸 매클레오드
사무엘 에드워드 만
시몬 리차드 그린
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잔센파마슈티카엔.브이.
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    • 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/10—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 carbon chain containing aromatic 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
    • C07D403/14—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
    • C07D405/14—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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/535—Organo-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)
  • 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)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020187024257A 2016-01-22 2017-01-20 Nik 억제제로서 신규 치환된 시아노인돌린 유도체 Active KR102784966B1 (ko)

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)

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KR20180100441A KR20180100441A (ko) 2018-09-10
KR102784966B1 true KR102784966B1 (ko) 2025-03-20

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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)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI739783B (zh) 2016-01-22 2021-09-21 比利時商健生藥品公司 作為nik抑制劑的新穎的經取代氰基吲哚啉衍生物
US11001569B2 (en) 2016-01-22 2021-05-11 Janssen Pharmaceutica Nv 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors
CN109641882B (zh) 2016-06-30 2022-10-28 杨森制药有限公司 作为nik抑制剂的杂芳族衍生物
KR102587619B1 (ko) 2016-06-30 2023-10-11 잔센파마슈티카엔.브이. Nik 억제제로서의 시아노인돌린 유도체
CN108602802B (zh) 2016-07-26 2020-01-21 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
CN111793031B (zh) * 2019-04-02 2021-06-22 海创药业股份有限公司 芳香胺类化合物及其在制备ar和brd4双重抑制剂和调控剂中的用途
MA56038B1 (fr) 2019-05-31 2024-11-29 Janssen Pharmaceutica Nv Inhibiteurs à petite molécule de kinase induisant nf-kb
WO2021242505A1 (en) 2020-05-08 2021-12-02 Halia Therapeutics, Inc. Inhibitors of nek7 kinase
WO2023026794A1 (ja) 2021-08-23 2023-03-02 国立大学法人大阪大学 成熟肝細胞の分化転換抑制用組成物
US20240158394A1 (en) 2022-09-14 2024-05-16 Halia Therapeutics, Inc. Nek7 inhibitors

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002079197A1 (en) 2001-03-29 2002-10-10 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
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
WO2009158011A1 (en) 2008-06-26 2009-12-30 Amgen Inc. Alkynyl alcohols as kinase inhibitors
WO2010042337A1 (en) 2008-10-07 2010-04-15 Merck Sharp & Dohme Corp. Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE396978T1 (de) 1999-10-07 2008-06-15 Amgen Inc Triazin-kinase-hemmer
JP2003532635A (ja) 2000-02-17 2003-11-05 アムジエン・インコーポレーテツド キナーゼ阻害薬
ATE311366T1 (de) 2000-02-29 2005-12-15 Millennium Pharm Inc Benzamide und ähnliche inhibitoren vom faktor xa
EP1397142A4 (en) 2001-06-19 2004-11-03 Bristol Myers Squibb Co PYRIMIDINE PHOSPHODIESTERASE (PDE) INHIBITORS 7
US8450335B2 (en) 2008-06-27 2013-05-28 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
EP3205647B1 (en) 2009-08-17 2020-05-13 Memorial Sloan-Kettering Cancer Center 2-(pyrimidin-5-yl)-thiopyrimidine derivatives as hsp70 and hsc70 modulators for the treatment of proliferative disorders
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
ES2823350T3 (es) 2010-07-29 2021-05-06 Rigel Pharmaceuticals Inc Compuestos heterocíclicos que activan AMPK y métodos de uso de los mismos
AU2012242777A1 (en) 2011-04-12 2013-10-31 Alzheimer's Institute Of America, Inc. Compositions and therapeutic uses of IKK-related kinase epsilon and TANKbinding kinase 1 inhibitors
TWI663166B (zh) 2013-04-24 2019-06-21 健生藥品公司 新化合物
CA2922657C (en) 2013-08-30 2022-04-12 Ptc Therapeutics, Inc. Substituted pyrimidine bmi-1 inhibitors
TWI704146B (zh) 2013-09-26 2020-09-11 比利時商健生藥品公司 用作ＮＩＫ抑制劑之新的1-(４-嘧啶基)-１Ｈ-吡唑並[３,２-ｃ]吡啶衍生物
TWI627173B (zh) 2013-09-26 2018-06-21 比利時商健生藥品公司 作為ＮＩＫ抑制劑的新穎３－（１Ｈ－吡唑－４－基）－１Ｈ－吡咯并［２，３－ｃ］吡啶衍生物
RS58175B1 (sr) 2014-04-04 2019-03-29 Syros Pharmaceuticals Inc Inhibitori ciklin-zavisne kinaze 7 (cdk7)
JP2017520526A (ja) 2014-05-22 2017-07-27 ザ・ユニバーシティ・オブ・シドニー オメガ−３類似体
WO2016022645A1 (en) 2014-08-06 2016-02-11 Merck Sharp & Dohme Corp. Heterocyclic cgrp receptor antagonists
EP3517536B1 (en) 2014-09-26 2021-05-05 Gilead Sciences, Inc. Aminotriazine derivatives useful as tank-binding kinase inhibitor compounds
CN106928216A (zh) * 2015-12-31 2017-07-07 中国科学院上海药物研究所 具有erk激酶抑制活性的化合物、其制备方法和用途
TWI739783B (zh) 2016-01-22 2021-09-21 比利時商健生藥品公司 作為nik抑制劑的新穎的經取代氰基吲哚啉衍生物
US11001569B2 (en) 2016-01-22 2021-05-11 Janssen Pharmaceutica Nv 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors
RS64261B1 (sr) 2016-03-16 2023-07-31 Kura Oncology Inc Supstituisani derivati tieno[2,3-d]pirimidina kao inhibitori menin-mll i načini upotrebe
KR102587619B1 (ko) 2016-06-30 2023-10-11 잔센파마슈티카엔.브이. Nik 억제제로서의 시아노인돌린 유도체
CN109641882B (zh) 2016-06-30 2022-10-28 杨森制药有限公司 作为nik抑制剂的杂芳族衍生物

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002079197A1 (en) 2001-03-29 2002-10-10 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
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
WO2009158011A1 (en) 2008-06-26 2009-12-30 Amgen Inc. Alkynyl alcohols as kinase inhibitors
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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IL260500B (en) 2021-01-31
BR112018014675A2 (pt) 2018-12-11
LT3405196T (lt) 2020-02-25
US11180487B2 (en) 2021-11-23
BR112018014675B1 (pt) 2023-12-19
PH12018501567A1 (en) 2019-01-28
WO2017125530A1 (en) 2017-07-27
KR20180100441A (ko) 2018-09-10
HUE047684T2 (hu) 2020-05-28
HRP20200133T1 (hr) 2020-05-15
AU2017209935B2 (en) 2021-04-01
CN108697710B (zh) 2022-02-18
MX2018008974A (es) 2018-11-09
TW201728577A (zh) 2017-08-16
CN108697710A (zh) 2018-10-23
EP3405196B1 (en) 2019-12-04
AU2017209935A1 (en) 2018-08-09
DK3405196T3 (en) 2020-03-09
ZA201804688B (en) 2022-03-30
EP3405196A1 (en) 2018-11-28
SI3405196T1 (sl) 2020-03-31
ES2775449T3 (es) 2020-07-27
TWI739783B (zh) 2021-09-21
US20210087182A1 (en) 2021-03-25
CA3011880A1 (en) 2017-07-27
JP2019504067A (ja) 2019-02-14
JP6910359B2 (ja) 2021-07-28

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