KR102499862B1 - Ｎｉｋ 억제제로서의 신규 피라졸 유도체 - Google Patents

Ｎｉｋ 억제제로서의 신규 피라졸 유도체 Download PDF

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KR102499862B1
KR102499862B1 KR1020177010800A KR20177010800A KR102499862B1 KR 102499862 B1 KR102499862 B1 KR 102499862B1 KR 1020177010800 A KR1020177010800 A KR 1020177010800A KR 20177010800 A KR20177010800 A KR 20177010800A KR 102499862 B1 KR102499862 B1 KR 102499862B1
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alkyl
hydrogen
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substituted
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KR20170068488A (ko
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조지 하인드
패트리지아 티셀리
야뉴스 죠제프 쿠라고프스키
칼럼 맥클레오드
사무엘 에드워드 만
존 게리 몬타나
스티븐 콜린 프라이스
파비앙 장 기슬랭 루셀
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얀센 파마슈티카 엔.브이.
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020177010800A 2014-10-23 2015-10-22 Ｎｉｋ 억제제로서의 신규 피라졸 유도체 Active KR102499862B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14190072 2014-10-23
EP14190072.0 2014-10-23
PCT/EP2015/074433 WO2016062791A1 (en) 2014-10-23 2015-10-22 New pyrazole derivatives as nik inhibitors

Publications (2)

Publication Number Publication Date
KR20170068488A KR20170068488A (ko) 2017-06-19
KR102499862B1 true KR102499862B1 (ko) 2023-02-13

Family

ID=51865980

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KR1020177010800A Active KR102499862B1 (ko) 2014-10-23 2015-10-22 Ｎｉｋ 억제제로서의 신규 피라졸 유도체

Country Status (13)

Country Link
US (1) US9981962B2 (enExample)
EP (1) EP3209654B1 (enExample)
JP (1) JP6616411B2 (enExample)
KR (1) KR102499862B1 (enExample)
CN (1) CN107074818B (enExample)
AU (1) AU2015334916B2 (enExample)
BR (1) BR112017008039B1 (enExample)
CA (1) CA2960335C (enExample)
EA (1) EA033236B1 (enExample)
ES (1) ES2704749T3 (enExample)
IL (1) IL251777B (enExample)
MX (1) MX371150B (enExample)
WO (1) WO2016062791A1 (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
CN122562777A (zh) * 2015-12-02 2026-08-14 阿斯特来亚治疗有限责任公司 哌啶基痛敏肽受体化合物
US10112924B2 (en) 2015-12-02 2018-10-30 Astraea Therapeutics, Inc. Piperdinyl nociceptin receptor compounds
EP3405464B1 (en) * 2016-01-22 2019-12-04 Janssen Pharmaceutica NV New 6-membered heteroaromatic substituted cyanoindoline derivatives as nik inhibitors
CR20210587A (es) 2019-05-31 2022-02-11 Janssen Pharmaceutica Nv Inhibidores de molécula pequeña de quinasa inductora de nf-kb
TW202402269A (zh) * 2022-05-26 2024-01-16 大陸商迪哲（江蘇）醫藥股份有限公司 ＲＯＣＫ（Ｒｈｏ相關激酶）抑制劑及其用途

Citations (2)

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WO2009158011A1 (en) 2008-06-26 2009-12-30 Amgen Inc. Alkynyl alcohols as kinase inhibitors
US20120214762A1 (en) 2011-03-16 2012-08-23 Genentech, Inc. 6,5-heterocyclic propargylic alcohol compounds and uses therefor

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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
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
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
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009158011A1 (en) 2008-06-26 2009-12-30 Amgen Inc. Alkynyl alcohols as kinase inhibitors
US20120214762A1 (en) 2011-03-16 2012-08-23 Genentech, Inc. 6,5-heterocyclic propargylic alcohol compounds and uses therefor

Also Published As

Publication number Publication date
US9981962B2 (en) 2018-05-29
CN107074818B (zh) 2020-04-17
AU2015334916B2 (en) 2020-02-06
JP6616411B2 (ja) 2019-12-04
IL251777B (en) 2021-09-30
EA201790904A1 (ru) 2017-08-31
WO2016062791A1 (en) 2016-04-28
MX2017005283A (es) 2017-08-15
AU2015334916A1 (en) 2017-03-23
EP3209654B1 (en) 2018-10-03
ES2704749T3 (es) 2019-03-19
KR20170068488A (ko) 2017-06-19
US20170334900A1 (en) 2017-11-23
EA033236B1 (ru) 2019-09-30
JP2017531677A (ja) 2017-10-26
EP3209654A1 (en) 2017-08-30
CA2960335C (en) 2023-09-19
CN107074818A (zh) 2017-08-18
MX371150B (es) 2020-01-20
IL251777A0 (en) 2017-06-29
CA2960335A1 (en) 2016-04-28
BR112017008039A2 (pt) 2017-12-19
BR112017008039B1 (pt) 2023-04-11

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