CN105579452B - 作为NIK抑制剂的新型3‑(1H‑吡唑‑4‑基)‑1H‑吡咯并[2,3‑c]吡啶衍生物 - Google Patents

作为NIK抑制剂的新型3‑(1H‑吡唑‑4‑基)‑1H‑吡咯并[2,3‑c]吡啶衍生物 Download PDF

Info

Publication number
CN105579452B
CN105579452B CN201480052798.2A CN201480052798A CN105579452B CN 105579452 B CN105579452 B CN 105579452B CN 201480052798 A CN201480052798 A CN 201480052798A CN 105579452 B CN105579452 B CN 105579452B
Authority
CN
China
Prior art keywords
alkyl
group
hydrogen
substituted
het
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.)
Expired - Fee Related
Application number
CN201480052798.2A
Other languages
English (en)
Chinese (zh)
Other versions
CN105579452A (zh
Inventor
G.海恩德
P.蒂斯塞里
D.E.克拉克
J.J.库拉戈维斯基
C.马克勒奥德
S.E.马恩
F.J.G.劳斯塞
S.C.普赖斯
J.G.蒙塔纳
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.)
Janssen Pharmaceutica NV
Original Assignee
Janssen Pharmaceutica NV
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 Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
Publication of CN105579452A publication Critical patent/CN105579452A/zh
Application granted granted Critical
Publication of CN105579452B publication Critical patent/CN105579452B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Epidemiology (AREA)
CN201480052798.2A 2013-09-26 2014-09-25 作为NIK抑制剂的新型3‑(1H‑吡唑‑4‑基)‑1H‑吡咯并[2,3‑c]吡啶衍生物 Expired - Fee Related CN105579452B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP13186148 2013-09-26
EP13186148.6 2013-09-26
EP14176125 2014-07-08
EP14176125.4 2014-07-08
PCT/EP2014/070489 WO2015044269A1 (en) 2013-09-26 2014-09-25 NEW 3-(1H-PYRAZOL-4-YL)-1H-PYRROLO[2,3-c]PYRIDINE DERIVATIVES AS NIK INHIBITORS

Publications (2)

Publication Number Publication Date
CN105579452A CN105579452A (zh) 2016-05-11
CN105579452B true CN105579452B (zh) 2018-01-23

Family

ID=51626028

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201480052798.2A Expired - Fee Related CN105579452B (zh) 2013-09-26 2014-09-25 作为NIK抑制剂的新型3‑(1H‑吡唑‑4‑基)‑1H‑吡咯并[2,3‑c]吡啶衍生物

Country Status (14)

Country Link
US (1) US9981963B2 (enExample)
EP (1) EP3049412B1 (enExample)
JP (1) JP6404332B2 (enExample)
KR (1) KR102317335B1 (enExample)
CN (1) CN105579452B (enExample)
AU (1) AU2014327235B2 (enExample)
BR (1) BR112016006232B1 (enExample)
CA (1) CA2922633C (enExample)
EA (1) EA028101B1 (enExample)
ES (1) ES2643070T3 (enExample)
IL (1) IL244702B (enExample)
MX (1) MX365739B (enExample)
TW (1) TWI627173B (enExample)
WO (1) WO2015044269A1 (enExample)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI663166B (zh) 2013-04-24 2019-06-21 健生藥品公司 新化合物
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
WO2016062792A1 (en) 2014-10-23 2016-04-28 Janssen Pharmaceutica Nv New compounds as nik inhibitors
AU2015334914B2 (en) 2014-10-23 2019-09-19 Janssen Pharmaceutica Nv New thienopyrimidine derivatives as NIK inhibitors
EA033237B1 (ru) 2014-10-23 2019-09-30 Янссен Фармацевтика Нв Новые производные пиразолопиримидина в качестве ингибиторов nik, фармацевтическая композиция и лекарственное средство, содержащее ее
JP6616411B2 (ja) 2014-10-23 2019-12-04 ヤンセン ファーマシューティカ エヌ．ベー． 新規な、ｎｉｋ阻害剤としてのピラゾール誘導体
US10112924B2 (en) 2015-12-02 2018-10-30 Astraea Therapeutics, Inc. Piperdinyl nociceptin receptor compounds
CN122562777A (zh) * 2015-12-02 2026-08-14 阿斯特来亚治疗有限责任公司 哌啶基痛敏肽受体化合物
HRP20200133T1 (hr) 2016-01-22 2020-05-15 Janssen Pharmaceutica Nv Novi supstituirani derivati cijanoindolina kao inhibitori nik
EP3405464B1 (en) 2016-01-22 2019-12-04 Janssen Pharmaceutica NV New 6-membered heteroaromatic substituted cyanoindoline derivatives as nik inhibitors
WO2018002219A1 (en) 2016-06-30 2018-01-04 Janssen Pharmaceutica Nv Cyanoindoline derivatives as nik inhibitors
EP3478675B1 (en) 2016-06-30 2020-04-22 Janssen Pharmaceutica NV Heteroaromatic derivatives as nik inhibitors
JP7549345B2 (ja) * 2019-02-08 2024-09-11 学校法人近畿大学 悪性腫瘍疾患の改善用組成物
CR20210587A (es) 2019-05-31 2022-02-11 Janssen Pharmaceutica Nv Inhibidores de molécula pequeña de quinasa inductora de nf-kb
CN110156766A (zh) * 2019-06-04 2019-08-23 南京工业大学 一种银催化的氘代五元芳香杂环化合物的制备方法
US20240124430A1 (en) 2020-12-22 2024-04-18 Kinki University Pharmaceutical composition for ameliorating malignant diseases
TW202402269A (zh) * 2022-05-26 2024-01-16 大陸商迪哲（江蘇）醫藥股份有限公司 ＲＯＣＫ（Ｒｈｏ相關激酶）抑制劑及其用途
JPWO2024029528A1 (enExample) 2022-08-02 2024-02-08

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2012123522A1 (en) * 2011-03-16 2012-09-20 F. Hoffmann-La Roche Ag 6,5-heterocyclic propargylic alcohol compounds and uses therefor

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3990061B2 (ja) * 1998-01-05 2007-10-10 エーザイ・アール・アンド・ディー・マネジメント株式会社 プリン誘導体および糖尿病の予防・治療剤としてのアデノシンａ２受容体拮抗剤
DE19948417A1 (de) * 1999-10-07 2001-04-19 Morphochem Ag Imidazol-Derivate und ihre Verwendung als Arzneimittel
BRPI0510319A (pt) 2004-04-26 2007-10-16 Pfizer inibidores da enzima integrase de hiv
TW200736260A (en) * 2005-11-10 2007-10-01 Smithkline Beecham Corp Inhibitors of Akt activity
DE102008005493A1 (de) 2008-01-22 2009-07-23 Merck Patent Gmbh 4-(Pyrrolo[2,3-c] pyridine-3-yl)-pyrimidin-2-yl-amin-derivate
CA2728559A1 (en) 2008-07-03 2010-01-07 Exelixis Inc. Cdk modulators
CN101723936B (zh) 2008-10-27 2014-01-15 上海睿星基因技术有限公司 激酶抑制剂及其在药学中的用途
WO2011050245A1 (en) 2009-10-23 2011-04-28 Yangbo Feng Bicyclic heteroaryls as kinase inhibitors
TWI663166B (zh) 2013-04-24 2019-06-21 健生藥品公司 新化合物
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
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
AU2015334914B2 (en) 2014-10-23 2019-09-19 Janssen Pharmaceutica Nv New thienopyrimidine derivatives as NIK inhibitors
JP6616411B2 (ja) 2014-10-23 2019-12-04 ヤンセン ファーマシューティカ エヌ．ベー． 新規な、ｎｉｋ阻害剤としてのピラゾール誘導体
WO2016062792A1 (en) 2014-10-23 2016-04-28 Janssen Pharmaceutica Nv New compounds as nik inhibitors
EA033237B1 (ru) 2014-10-23 2019-09-30 Янссен Фармацевтика Нв Новые производные пиразолопиримидина в качестве ингибиторов nik, фармацевтическая композиция и лекарственное средство, содержащее ее

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2012123522A1 (en) * 2011-03-16 2012-09-20 F. Hoffmann-La Roche Ag 6,5-heterocyclic propargylic alcohol compounds and uses therefor

Also Published As

Publication number Publication date
EP3049412B1 (en) 2017-07-12
IL244702A0 (en) 2016-04-21
EA028101B1 (ru) 2017-10-31
US9981963B2 (en) 2018-05-29
IL244702B (en) 2019-07-31
TWI627173B (zh) 2018-06-21
EA201690657A1 (ru) 2016-08-31
AU2014327235B2 (en) 2018-02-08
KR102317335B1 (ko) 2021-10-26
TW201602103A (zh) 2016-01-16
AU2014327235A1 (en) 2016-03-17
CA2922633A1 (en) 2015-04-02
US20160229851A1 (en) 2016-08-11
CA2922633C (en) 2022-07-26
BR112016006232A2 (pt) 2017-08-01
MX2016003863A (es) 2016-08-04
BR112016006232B1 (pt) 2022-11-29
JP6404332B2 (ja) 2018-10-10
CN105579452A (zh) 2016-05-11
WO2015044269A1 (en) 2015-04-02
KR20160060054A (ko) 2016-05-27
ES2643070T3 (es) 2017-11-21
JP2016531858A (ja) 2016-10-13
EP3049412A1 (en) 2016-08-03
MX365739B (es) 2019-06-12

Similar Documents

Publication Publication Date Title
TWI627173B (zh) 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
CN105579451B (zh) 作为NIK抑制剂的新型1‑(4‑嘧啶基)‑1H‑吡咯并[3,2‑c]吡啶衍生物
CN107074882B (zh) 作为nik抑制剂的新的吡唑并嘧啶衍生物
CN107074855B (zh) 作为nik抑制剂的新的化合物
EP2989101B1 (en) 3-(2-aminopyrimidin-4-yl)-5-(3-hydroxypropynyl)-1h-pyrrolo[2,3-c]pyridine derivatives as nik inhibitors for the treatment of cancer
CN107074881B (zh) 作为nik抑制剂的新的噻吩并嘧啶衍生物
CN107074818B (zh) 作为nik抑制剂的吡唑衍生物
HK1224664A1 (en) New 3-(1h-pyrazol-4-yl)-1h-pyrrolo(2,3-c) pyridine derivatives as nik inhibitors
HK1224664B (en) New 3-(1h-pyrazol-4-yl)-1h-pyrrolo(2,3-c) pyridine derivatives as nik inhibitors
HK1224295B (en) New 1-(4-pyrimidinyl)-1 h-pyrrolo(3,2-c) pyridine derivatives as nik inhibitors
HK1215430B (en) 3-(2-aminopyrimidin-4-yl)-5-(3-hydroxypropynyl)-1h-pyrrolo[2,3-c]pyridine derivatives as nik inhibitors for the treatment of cancer

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1224664

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1224664

Country of ref document: HK

CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20180123