KR102523405B1 - Nik 억제제로서의 신규 피라졸로피리미딘 유도체 - Google Patents

Nik 억제제로서의 신규 피라졸로피리미딘 유도체 Download PDF

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KR102523405B1
KR102523405B1 KR1020177010805A KR20177010805A KR102523405B1 KR 102523405 B1 KR102523405 B1 KR 102523405B1 KR 1020177010805 A KR1020177010805 A KR 1020177010805A KR 20177010805 A KR20177010805 A KR 20177010805A KR 102523405 B1 KR102523405 B1 KR 102523405B1
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KR20170068489A (ko
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조지 하인드
패트리지아 티셀리
칼럼 맥클레오드
사무엘 에드워드 만
테리 아론 판챨
존 게리 몬타나
스티븐 콜린 프라이스
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얀센 파마슈티카 엔.브이.
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    • 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
    • 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
    • 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)
KR1020177010805A 2014-10-23 2015-10-22 Nik 억제제로서의 신규 피라졸로피리미딘 유도체 Active KR102523405B1 (ko)

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
KR20170068489A KR20170068489A (ko) 2017-06-19
KR102523405B1 true KR102523405B1 (ko) 2023-04-18

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KR1020177010805A Active KR102523405B1 (ko) 2014-10-23 2015-10-22 Nik 억제제로서의 신규 피라졸로피리미딘 유도체

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 (3)

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JP2011525915A (ja) 2008-06-26 2011-09-29 アムジエン・インコーポレーテツド キナーゼ阻害薬としてのアルキニルアルコール類
JP2014508183A (ja) 2011-03-16 2014-04-03 エフ.ホフマン−ラ ロシュ アーゲー 6,5−複素環式プロパルギルアルコール化合物及びこれらの使用
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

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WO1990007926A1 (en) * 1989-01-20 1990-07-26 Pfizer Inc. 3-(1,2,5,6-tetrahydropyridyl)-pyrrolopyridines
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
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011525915A (ja) 2008-06-26 2011-09-29 アムジエン・インコーポレーテツド キナーゼ阻害薬としてのアルキニルアルコール類
JP2014508183A (ja) 2011-03-16 2014-04-03 エフ.ホフマン−ラ ロシュ アーゲー 6,5−複素環式プロパルギルアルコール化合物及びこれらの使用
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

Also Published As

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
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
CN107074882B (zh) 2019-07-30
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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