CN107074882B - 作为nik抑制剂的新的吡唑并嘧啶衍生物 - Google Patents

作为nik抑制剂的新的吡唑并嘧啶衍生物 Download PDF

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Publication number
CN107074882B
CN107074882B CN201580057545.9A CN201580057545A CN107074882B CN 107074882 B CN107074882 B CN 107074882B CN 201580057545 A CN201580057545 A CN 201580057545A CN 107074882 B CN107074882 B CN 107074882B
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alkyl
group
hydrogen
compound
acid
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Expired - Fee Related
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Chinese (zh)
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CN107074882A (zh
Inventor
G.海恩德
P.蒂斯塞里
C.马勒奥德
S.E.曼恩
T.A.潘查
J.G.蒙塔纳
S.C.普里塞
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201580057545.9A 2014-10-23 2015-10-22 作为nik抑制剂的新的吡唑并嘧啶衍生物 Expired - Fee Related CN107074882B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14190073 2014-10-23
EP14190073.8 2014-10-23
PCT/EP2015/074431 WO2016062790A1 (en) 2014-10-23 2015-10-22 New pyrazolopyrimidine derivatives as nik inhibitors

Publications (2)

Publication Number Publication Date
CN107074882A CN107074882A (zh) 2017-08-18
CN107074882B true CN107074882B (zh) 2019-07-30

Family

ID=51846471

Family Applications (1)

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CN201580057545.9A Expired - Fee Related CN107074882B (zh) 2014-10-23 2015-10-22 作为nik抑制剂的新的吡唑并嘧啶衍生物

Country Status (13)

Country Link
US (2) US10221180B2 (enExample)
EP (1) EP3209663B1 (enExample)
JP (1) JP6616412B2 (enExample)
KR (1) KR102523405B1 (enExample)
CN (1) CN107074882B (enExample)
AU (1) AU2015334915B2 (enExample)
BR (1) BR112017007704B1 (enExample)
CA (1) CA2960574C (enExample)
EA (1) EA033237B1 (enExample)
ES (1) ES2715104T3 (enExample)
IL (1) IL251778B (enExample)
MX (1) MX371152B (enExample)
WO (1) WO2016062790A1 (enExample)

Families Citing this family (12)

* 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
ES2704749T3 (es) 2014-10-23 2019-03-19 Janssen Pharmaceutica Nv Nuevos derivados de pirazol en calidad de inhibidores de nik
CN107074882B (zh) 2014-10-23 2019-07-30 詹森药业有限公司 作为nik抑制剂的新的吡唑并嘧啶衍生物
KR102500071B1 (ko) 2014-10-23 2023-02-14 얀센 파마슈티카 엔.브이. Nik 억제제로서의 신규 화합물
EA033238B1 (ru) 2014-10-23 2019-09-30 Янссен Фармацевтика Нв Новые производные тиенопиримидина в качестве ингибиторов nik
WO2019236884A1 (en) 2018-06-07 2019-12-12 Disarm Therapeutics, Inc. Inhibitors of sarm1
JP7296407B2 (ja) * 2018-06-18 2023-06-22 ヤンセン ファーマシューティカ エヌ.ベー. Malt1阻害剤としてのピラゾール誘導体
CA3123215C (en) 2018-12-19 2024-04-02 Disarm Therapeutics, Inc. Inhibitors of sarm1 in combination with neuroprotective agents
MX2021011923A (es) * 2019-03-29 2021-11-03 Kowa Co Novedoso derivado de azaindol.
MA56038B1 (fr) 2019-05-31 2024-11-29 Janssen Pharmaceutica Nv Inhibiteurs à petite molécule de kinase induisant nf-kb

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1025998C (zh) * 1989-01-20 1994-09-28 美国辉瑞有限公司 3-(1,2,5,6-四氢吡啶基)-吡咯并吡啶类的制备方法
WO2009158011A1 (en) * 2008-06-26 2009-12-30 Amgen Inc. Alkynyl alcohols as kinase inhibitors

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CA2564356A1 (en) 2004-04-26 2005-11-03 Pfizer Inc. Pyrrolopyridine derivatives and their use as hiv-integrase inhibitors
AR056786A1 (es) 2005-11-10 2007-10-24 Smithkline Beecham Corp Compuesto de 1h- imidazo ( 4,5-c) piridin-2-ilo, composicion farmaceutica que lo comprende, procedimiento para preparar dicha composicion, su uso para preparar unmedicamento, uso de una combinacion que omprende al compuesto y al menos un agente antineoplasico para preparar un medicamento y dicha com
DE102008005493A1 (de) 2008-01-22 2009-07-23 Merck Patent Gmbh 4-(Pyrrolo[2,3-c] pyridine-3-yl)-pyrimidin-2-yl-amin-derivate
EP2320895A2 (en) 2008-07-03 2011-05-18 Exelixis, Inc. Cdk modulators
WO2010042337A1 (en) 2008-10-07 2010-04-15 Merck Sharp & Dohme Corp. Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity
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
TW201247650A (en) 2011-03-16 2012-12-01 Hoffmann La Roche 6,5-heterocyclic propargylic alcohol compounds and uses therefor
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
KR102500071B1 (ko) 2014-10-23 2023-02-14 얀센 파마슈티카 엔.브이. Nik 억제제로서의 신규 화합물
CN107074882B (zh) 2014-10-23 2019-07-30 詹森药业有限公司 作为nik抑制剂的新的吡唑并嘧啶衍生物
EA033238B1 (ru) 2014-10-23 2019-09-30 Янссен Фармацевтика Нв Новые производные тиенопиримидина в качестве ингибиторов nik
ES2704749T3 (es) 2014-10-23 2019-03-19 Janssen Pharmaceutica Nv Nuevos derivados de pirazol en calidad de inhibidores de nik

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1025998C (zh) * 1989-01-20 1994-09-28 美国辉瑞有限公司 3-(1,2,5,6-四氢吡啶基)-吡咯并吡啶类的制备方法
WO2009158011A1 (en) * 2008-06-26 2009-12-30 Amgen Inc. Alkynyl alcohols as kinase inhibitors

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Publication number Publication date
BR112017007704A2 (pt) 2017-12-19
MX2017005284A (es) 2017-07-28
ES2715104T3 (es) 2019-05-31
EP3209663A1 (en) 2017-08-30
MX371152B (es) 2020-01-20
KR102523405B1 (ko) 2023-04-18
EA033237B1 (ru) 2019-09-30
IL251778B (en) 2020-10-29
US20170334915A1 (en) 2017-11-23
US10822342B2 (en) 2020-11-03
US20190169198A1 (en) 2019-06-06
JP6616412B2 (ja) 2019-12-04
WO2016062790A1 (en) 2016-04-28
AU2015334915A1 (en) 2017-03-30
CN107074882A (zh) 2017-08-18
CA2960574C (en) 2023-03-07
EA201790907A1 (ru) 2017-08-31
BR112017007704B1 (pt) 2023-04-11
AU2015334915B2 (en) 2019-09-19
IL251778A0 (en) 2017-06-29
JP2017531678A (ja) 2017-10-26
US10221180B2 (en) 2019-03-05
KR20170068489A (ko) 2017-06-19
CA2960574A1 (en) 2016-04-28
EP3209663B1 (en) 2018-12-12

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Granted publication date: 20190730