AU2015334915B2 - New pyrazolopyrimidine derivatives as NIK inhibitors - Google Patents

New pyrazolopyrimidine derivatives as NIK inhibitors Download PDF

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Publication number
AU2015334915B2
AU2015334915B2 AU2015334915A AU2015334915A AU2015334915B2 AU 2015334915 B2 AU2015334915 B2 AU 2015334915B2 AU 2015334915 A AU2015334915 A AU 2015334915A AU 2015334915 A AU2015334915 A AU 2015334915A AU 2015334915 B2 AU2015334915 B2 AU 2015334915B2
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AU
Australia
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substituted
4alkyl
group
hydrogen
fluoro
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AU2015334915A
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AU2015334915A1 (en
Inventor
George Hynd
Calum Macleod
Samuel Edward MANN
John Gary Montana
Terry Aaron PANCHAL
Stephen Colin PRICE
Patrizia Tisselli
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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
    • 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
    • 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
    • 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
    • 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)
AU2015334915A 2014-10-23 2015-10-22 New pyrazolopyrimidine derivatives as NIK inhibitors Ceased AU2015334915B2 (en)

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
AU2015334915A1 AU2015334915A1 (en) 2017-03-30
AU2015334915B2 true AU2015334915B2 (en) 2019-09-19

Family

ID=51846471

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2015334915A Ceased AU2015334915B2 (en) 2014-10-23 2015-10-22 New pyrazolopyrimidine derivatives as NIK inhibitors

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
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
US5169947A (en) * 1989-01-20 1992-12-08 Pfizer Inc. 3-(1,2,5,6-tetrahydropyridyl)-pyrrolopyridines
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5169947A (en) * 1989-01-20 1992-12-08 Pfizer Inc. 3-(1,2,5,6-tetrahydropyridyl)-pyrrolopyridines
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
CN107074882B (zh) 2019-07-30
MX2017005284A (es) 2017-07-28
EA033237B1 (ru) 2019-09-30
JP6616412B2 (ja) 2019-12-04
MX371152B (es) 2020-01-20
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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