EA033237B1 - Новые производные пиразолопиримидина в качестве ингибиторов nik, фармацевтическая композиция и лекарственное средство, содержащее ее - Google Patents

Новые производные пиразолопиримидина в качестве ингибиторов nik, фармацевтическая композиция и лекарственное средство, содержащее ее

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Publication number
EA033237B1
EA033237B1 EA201790907A EA201790907A EA033237B1 EA 033237 B1 EA033237 B1 EA 033237B1 EA 201790907 A EA201790907 A EA 201790907A EA 201790907 A EA201790907 A EA 201790907A EA 033237 B1 EA033237 B1 EA 033237B1
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EA
Eurasian Patent Office
Prior art keywords
medicament
pharmaceutical composition
same
disorders
pyrazolopyrimidine derivatives
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EA201790907A
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English (en)
Other versions
EA201790907A1 (ru
Inventor
Джордж Хинд
Патриция Тисселли
Калум Маклеод
Самьюэль Эдвард Манн
Терри Аарон Панчал
Джон Гари Монтана
Стефен Колин Прайс
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Янссен Фармацевтика Нв
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Application filed by Янссен Фармацевтика Нв filed Critical Янссен Фармацевтика Нв
Publication of EA201790907A1 publication Critical patent/EA201790907A1/ru
Publication of EA033237B1 publication Critical patent/EA033237B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/437—Heterocyclic 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)

Abstract

Изобретение относится к соединениям формулы (I)в которой все переменные указаны в формуле изобретения, применимым для терапии и/или профилактики у млекопитающего, и, в частности, к ингибиторам NF-κB-индуцирующей киназы (NIK, также известной как MAP3K14), применимым для лечения заболеваний, таких как рак, воспалительные нарушения, нарушения метаболизма и аутоиммунные нарушения. Изобретение направлено также на фармацевтические композиции, содержащие такие соединения, а также на применение таких соединений или фармацевтических композиций для предупреждения или лечения заболеваний, таких как рак, воспалительные нарушения, нарушения метаболизма, в том числе ожирение и диабет, а также аутоиммунные нарушения.
EA201790907A 2014-10-23 2015-10-22 Новые производные пиразолопиримидина в качестве ингибиторов nik, фармацевтическая композиция и лекарственное средство, содержащее ее EA033237B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14190073 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
EA201790907A1 EA201790907A1 (ru) 2017-08-31
EA033237B1 true EA033237B1 (ru) 2019-09-30

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EA201790907A EA033237B1 (ru) 2014-10-23 2015-10-22 Новые производные пиразолопиримидина в качестве ингибиторов nik, фармацевтическая композиция и лекарственное средство, содержащее ее

Country Status (13)

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

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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
JP6603713B2 (ja) 2014-10-23 2019-11-06 ヤンセン ファーマシューティカ エヌ．ベー． Ｎｉｋ阻害剤としての新規のチエノピリミジン誘導体
BR112017008045A2 (pt) 2014-10-23 2017-12-19 Janssen Pharmaceutica Nv compostos como inibidores de nik
WO2016062790A1 (en) 2014-10-23 2016-04-28 Janssen Pharmaceutica Nv New pyrazolopyrimidine derivatives as nik inhibitors
US9981962B2 (en) 2014-10-23 2018-05-29 Janssen Pharmaceutica Nv Pyrazole derivatives as NIK inhibitors
EA202092962A1 (ru) * 2018-06-18 2021-09-06 Янссен Фармацевтика Нв Производные пиразола в качестве ингибиторов malt1
CA3123215C (en) 2018-12-19 2024-04-02 Disarm Therapeutics, Inc. Inhibitors of sarm1 in combination with neuroprotective agents
EP3950063A4 (en) * 2019-03-29 2022-11-30 Kowa Company, Ltd. NEW AZAINDOLE DERIVATIVE
SG11202112994WA (en) 2019-05-31 2021-12-30 Janssen Pharmaceutica Nv SMALL MOLECULE INHIBITORS OF NF-kB INDUCING KINASE

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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
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WO2016062790A1 (en) 2014-10-23 2016-04-28 Janssen Pharmaceutica Nv New pyrazolopyrimidine derivatives as nik inhibitors
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JP6603713B2 (ja) 2014-10-23 2019-11-06 ヤンセン ファーマシューティカ エヌ．ベー． Ｎｉｋ阻害剤としての新規のチエノピリミジン誘導体

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Also Published As

Publication number Publication date
IL251778A0 (en) 2017-06-29
MX2017005284A (es) 2017-07-28
WO2016062790A1 (en) 2016-04-28
CN107074882A (zh) 2017-08-18
JP6616412B2 (ja) 2019-12-04
ES2715104T3 (es) 2019-05-31
US10221180B2 (en) 2019-03-05
IL251778B (en) 2020-10-29
US10822342B2 (en) 2020-11-03
CA2960574A1 (en) 2016-04-28
JP2017531678A (ja) 2017-10-26
AU2015334915B2 (en) 2019-09-19
CN107074882B (zh) 2019-07-30
KR20170068489A (ko) 2017-06-19
MX371152B (es) 2020-01-20
US20170334915A1 (en) 2017-11-23
AU2015334915A1 (en) 2017-03-30
EP3209663B1 (en) 2018-12-12
EP3209663A1 (en) 2017-08-30
KR102523405B1 (ko) 2023-04-18
US20190169198A1 (en) 2019-06-06
BR112017007704B1 (pt) 2023-04-11
BR112017007704A2 (pt) 2017-12-19
CA2960574C (en) 2023-03-07
EA201790907A1 (ru) 2017-08-31

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