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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CN201580057545.9A
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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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    • 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)
  • 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

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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 (cg-RX-API-DMAC10.html)
EP (1) EP3209663B1 (cg-RX-API-DMAC10.html)
JP (1) JP6616412B2 (cg-RX-API-DMAC10.html)
KR (1) KR102523405B1 (cg-RX-API-DMAC10.html)
CN (1) CN107074882B (cg-RX-API-DMAC10.html)
AU (1) AU2015334915B2 (cg-RX-API-DMAC10.html)
BR (1) BR112017007704B1 (cg-RX-API-DMAC10.html)
CA (1) CA2960574C (cg-RX-API-DMAC10.html)
EA (1) EA033237B1 (cg-RX-API-DMAC10.html)
ES (1) ES2715104T3 (cg-RX-API-DMAC10.html)
IL (1) IL251778B (cg-RX-API-DMAC10.html)
MX (1) MX371152B (cg-RX-API-DMAC10.html)
WO (1) WO2016062790A1 (cg-RX-API-DMAC10.html)

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
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
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
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
JP7478142B2 (ja) 2018-06-07 2024-05-02 ディスアーム セラピューティクス， インコーポレイテッド Ｓａｒｍ１阻害剤
AU2019289223B2 (en) * 2018-06-18 2023-09-21 Janssen Pharmaceutica Nv Pyrazole derivatives as MALT1 inhibitors
CA3123215C (en) 2018-12-19 2024-04-02 Disarm Therapeutics, Inc. Inhibitors of sarm1 in combination with neuroprotective agents
US20220162206A1 (en) * 2019-03-29 2022-05-26 Kowa Company, Ltd. Novel azaindole derivative
CR20210587A (es) 2019-05-31 2022-02-11 Janssen Pharmaceutica Nv Inhibidores de molécula pequeña de quinasa inductora de 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

Family Cites Families (15)

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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
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
AR085908A1 (es) * 2011-03-16 2013-11-06 Hoffmann La Roche DERIVADOS DE 3-BUTIN-2-OL Y DE CARBONITRILO CON ACTIVIDAD INHIBIDORA DE LA QUINASA INDUCTORA DE NF-kB (NIK)
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 (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

Also Published As

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

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Granted publication date: 20190730