KR102317335B1 - NIK 억제제로서의 신규 3-(1H-피라졸-4-일)-1H-피롤로[2,3-c]피리딘 유도체 - Google Patents
NIK 억제제로서의 신규 3-(1H-피라졸-4-일)-1H-피롤로[2,3-c]피리딘 유도체 Download PDFInfo
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- KR102317335B1 KR102317335B1 KR1020167007902A KR20167007902A KR102317335B1 KR 102317335 B1 KR102317335 B1 KR 102317335B1 KR 1020167007902 A KR1020167007902 A KR 1020167007902A KR 20167007902 A KR20167007902 A KR 20167007902A KR 102317335 B1 KR102317335 B1 KR 102317335B1
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- 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
-
- 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
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- 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
-
- 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
- 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)
- 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)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Epidemiology (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13186148.6 | 2013-09-26 | ||
| EP13186148 | 2013-09-26 | ||
| EP14176125.4 | 2014-07-08 | ||
| EP14176125 | 2014-07-08 | ||
| PCT/EP2014/070489 WO2015044269A1 (en) | 2013-09-26 | 2014-09-25 | NEW 3-(1H-PYRAZOL-4-YL)-1H-PYRROLO[2,3-c]PYRIDINE DERIVATIVES AS NIK INHIBITORS |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20160060054A KR20160060054A (ko) | 2016-05-27 |
| KR102317335B1 true KR102317335B1 (ko) | 2021-10-26 |
Family
ID=51626028
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020167007902A Expired - Fee Related KR102317335B1 (ko) | 2013-09-26 | 2014-09-25 | NIK 억제제로서의 신규 3-(1H-피라졸-4-일)-1H-피롤로[2,3-c]피리딘 유도체 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9981963B2 (https=) |
| EP (1) | EP3049412B1 (https=) |
| JP (1) | JP6404332B2 (https=) |
| KR (1) | KR102317335B1 (https=) |
| CN (1) | CN105579452B (https=) |
| AU (1) | AU2014327235B2 (https=) |
| BR (1) | BR112016006232B1 (https=) |
| CA (1) | CA2922633C (https=) |
| EA (1) | EA028101B1 (https=) |
| ES (1) | ES2643070T3 (https=) |
| IL (1) | IL244702B (https=) |
| MX (1) | MX365739B (https=) |
| TW (1) | TWI627173B (https=) |
| WO (1) | WO2015044269A1 (https=) |
Families Citing this family (19)
| 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 |
| AU2015334917B2 (en) | 2014-10-23 | 2019-08-29 | Janssen Pharmaceutica Nv | New compounds as NIK inhibitors |
| JP6616412B2 (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. | Nik阻害剤としての新規のピラゾロピリミジン誘導体 |
| BR112017008039B1 (pt) | 2014-10-23 | 2023-04-11 | Janssen Pharmaceutica N.V. | Derivados de pirazol como inibidores de nik, seu uso no tratamento ou prevenção de câncer e composição farmacêutica que os compreende |
| MX371151B (es) | 2014-10-23 | 2020-01-20 | Janssen Pharmaceutica Nv | NUEVOS DERIVADOS DE TIENOPIRIMIDINA EN CALIDAD DE INHIBIDORES DE LA CINASA INDUCTORA DE NF-kB (NIK). |
| JP7011596B2 (ja) * | 2015-12-02 | 2022-02-10 | アストライア セラピューティクス, エルエルシー | ピペリジニルノシセプチン受容体化合物 |
| 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 |
| ES2775449T3 (es) | 2016-01-22 | 2020-07-27 | Janssen Pharmaceutica Nv | Nuevos derivados de cianoindolina sustituida como inhibidores de nik |
| WO2018002217A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Heteroaromatic derivatives as nik inhibitors |
| ES2837157T3 (es) | 2016-06-30 | 2021-06-29 | Janssen Pharmaceutica Nv | Derivados de cianoindolina como inhibidores de NIK |
| WO2020162638A1 (ja) * | 2019-02-08 | 2020-08-13 | 学校法人近畿大学 | 悪性腫瘍疾患の改善用組成物 |
| CN114222737B (zh) | 2019-05-31 | 2024-07-26 | 詹森药业有限公司 | NF-κB诱导激酶的小分子抑制剂 |
| CN110156766A (zh) * | 2019-06-04 | 2019-08-23 | 南京工业大学 | 一种银催化的氘代五元芳香杂环化合物的制备方法 |
| WO2022138735A1 (ja) | 2020-12-22 | 2022-06-30 | 学校法人近畿大学 | 悪性腫瘍疾患の改善用医薬組成物 |
| 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 |
| WO2024029528A1 (ja) | 2022-08-02 | 2024-02-08 | 学校法人近畿大学 | アレルギー性疾患の改善用医薬組成物 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009158011A1 (en) | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| WO2010042337A1 (en) | 2008-10-07 | 2010-04-15 | Merck Sharp & Dohme Corp. | Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity |
| WO2012123522A1 (en) | 2011-03-16 | 2012-09-20 | F. Hoffmann-La Roche Ag | 6,5-heterocyclic propargylic alcohol compounds and uses therefor |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3990061B2 (ja) * | 1998-01-05 | 2007-10-10 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | プリン誘導体および糖尿病の予防・治療剤としてのアデノシンa2受容体拮抗剤 |
| DE19948417A1 (de) * | 1999-10-07 | 2001-04-19 | Morphochem Ag | Imidazol-Derivate und ihre Verwendung als Arzneimittel |
| WO2005103003A2 (en) | 2004-04-26 | 2005-11-03 | Pfizer Inc. | Pyrrolopyridine derivatives and their use as hiv-integrase inhibitors |
| 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 |
| CN102143746A (zh) | 2008-07-03 | 2011-08-03 | 埃克塞利希斯股份有限公司 | Cdk 调节剂 |
| 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 |
| BR112017008039B1 (pt) | 2014-10-23 | 2023-04-11 | Janssen Pharmaceutica N.V. | Derivados de pirazol como inibidores de nik, seu uso no tratamento ou prevenção de câncer e composição farmacêutica que os compreende |
| AU2015334917B2 (en) | 2014-10-23 | 2019-08-29 | Janssen Pharmaceutica Nv | New compounds as NIK inhibitors |
| MX371151B (es) | 2014-10-23 | 2020-01-20 | Janssen Pharmaceutica Nv | NUEVOS DERIVADOS DE TIENOPIRIMIDINA EN CALIDAD DE INHIBIDORES DE LA CINASA INDUCTORA DE NF-kB (NIK). |
| JP6616412B2 (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. | Nik阻害剤としての新規のピラゾロピリミジン誘導体 |
-
2014
- 2014-09-24 TW TW103132895A patent/TWI627173B/zh not_active IP Right Cessation
- 2014-09-25 AU AU2014327235A patent/AU2014327235B2/en not_active Ceased
- 2014-09-25 ES ES14776635.6T patent/ES2643070T3/es active Active
- 2014-09-25 EA EA201690657A patent/EA028101B1/ru not_active IP Right Cessation
- 2014-09-25 BR BR112016006232-9A patent/BR112016006232B1/pt not_active IP Right Cessation
- 2014-09-25 JP JP2016516870A patent/JP6404332B2/ja not_active Expired - Fee Related
- 2014-09-25 CN CN201480052798.2A patent/CN105579452B/zh not_active Expired - Fee Related
- 2014-09-25 CA CA2922633A patent/CA2922633C/en active Active
- 2014-09-25 MX MX2016003863A patent/MX365739B/es active IP Right Grant
- 2014-09-25 WO PCT/EP2014/070489 patent/WO2015044269A1/en not_active Ceased
- 2014-09-25 US US15/024,724 patent/US9981963B2/en active Active
- 2014-09-25 EP EP14776635.6A patent/EP3049412B1/en active Active
- 2014-09-25 KR KR1020167007902A patent/KR102317335B1/ko not_active Expired - Fee Related
-
2016
- 2016-03-22 IL IL244702A patent/IL244702B/en active IP Right Grant
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009158011A1 (en) | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| WO2010042337A1 (en) | 2008-10-07 | 2010-04-15 | Merck Sharp & Dohme Corp. | Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity |
| WO2012123522A1 (en) | 2011-03-16 | 2012-09-20 | F. Hoffmann-La Roche Ag | 6,5-heterocyclic propargylic alcohol compounds and uses therefor |
Also Published As
| Publication number | Publication date |
|---|---|
| US9981963B2 (en) | 2018-05-29 |
| EA201690657A1 (ru) | 2016-08-31 |
| JP6404332B2 (ja) | 2018-10-10 |
| EP3049412B1 (en) | 2017-07-12 |
| CA2922633A1 (en) | 2015-04-02 |
| AU2014327235B2 (en) | 2018-02-08 |
| IL244702A0 (en) | 2016-04-21 |
| BR112016006232A2 (pt) | 2017-08-01 |
| KR20160060054A (ko) | 2016-05-27 |
| EP3049412A1 (en) | 2016-08-03 |
| MX2016003863A (es) | 2016-08-04 |
| CA2922633C (en) | 2022-07-26 |
| US20160229851A1 (en) | 2016-08-11 |
| TWI627173B (zh) | 2018-06-21 |
| MX365739B (es) | 2019-06-12 |
| EA028101B1 (ru) | 2017-10-31 |
| BR112016006232B1 (pt) | 2022-11-29 |
| IL244702B (en) | 2019-07-31 |
| JP2016531858A (ja) | 2016-10-13 |
| CN105579452B (zh) | 2018-01-23 |
| ES2643070T3 (es) | 2017-11-21 |
| TW201602103A (zh) | 2016-01-16 |
| CN105579452A (zh) | 2016-05-11 |
| WO2015044269A1 (en) | 2015-04-02 |
| AU2014327235A1 (en) | 2016-03-17 |
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