AU2014327235B2 - New 3-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-c]pyridine derivatives as NIK inhibitors - Google Patents
New 3-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-c]pyridine derivatives as NIK inhibitors Download PDFInfo
- Publication number
- AU2014327235B2 AU2014327235B2 AU2014327235A AU2014327235A AU2014327235B2 AU 2014327235 B2 AU2014327235 B2 AU 2014327235B2 AU 2014327235 A AU2014327235 A AU 2014327235A AU 2014327235 A AU2014327235 A AU 2014327235A AU 2014327235 B2 AU2014327235 B2 AU 2014327235B2
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- Australia
- Prior art keywords
- alkyl
- group
- hydrogen
- substituted
- het
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
Links
- 0 *C(*)(C#Cc1nc(*)c2[n]c(*)c(-c3c(*)[n]nc3*)c2c1*)O Chemical compound *C(*)(C#Cc1nc(*)c2[n]c(*)c(-c3c(*)[n]nc3*)c2c1*)O 0.000 description 5
- DHWXHYCQFFUPSD-UHFFFAOYSA-N CC1CCN(CCF)CC1 Chemical compound CC1CCN(CCF)CC1 DHWXHYCQFFUPSD-UHFFFAOYSA-N 0.000 description 1
- YHRWOLBOIFIGBI-AQTBWJFISA-N CCNNC(C)C(C#CC(C)(C)O)/N=C\C(N(CC)C=C)=C Chemical compound CCNNC(C)C(C#CC(C)(C)O)/N=C\C(N(CC)C=C)=C YHRWOLBOIFIGBI-AQTBWJFISA-N 0.000 description 1
- IUWCXBOKQILJGJ-UHFFFAOYSA-N CC[n](cc(-c1c[nH]nc1)c1c2)c1cnc2C#CC(C)(C1CC1)O Chemical compound CC[n](cc(-c1c[nH]nc1)c1c2)c1cnc2C#CC(C)(C1CC1)O IUWCXBOKQILJGJ-UHFFFAOYSA-N 0.000 description 1
- GVEAZZHRPKVKOU-UHFFFAOYSA-N CC[n](cc(-c1c[nH]nc1)c1c2)c1cnc2C#CC(C)(c1n[o]c(C)c1)O Chemical compound CC[n](cc(-c1c[nH]nc1)c1c2)c1cnc2C#CC(C)(c1n[o]c(C)c1)O GVEAZZHRPKVKOU-UHFFFAOYSA-N 0.000 description 1
- MPHNXUKZXHHZPF-UHFFFAOYSA-N CC[n](cc(-c1c[nH]nc1)c1c2)c1cnc2C#CC1(CCCC1)O Chemical compound CC[n](cc(-c1c[nH]nc1)c1c2)c1cnc2C#CC1(CCCC1)O MPHNXUKZXHHZPF-UHFFFAOYSA-N 0.000 description 1
- RCOFKRJSFYLYAU-UHFFFAOYSA-N CC[n](cc(-c1c[nH]nc1N)c1c2)c1cnc2C#CC(C)(C)O Chemical compound CC[n](cc(-c1c[nH]nc1N)c1c2)c1cnc2C#CC(C)(C)O RCOFKRJSFYLYAU-UHFFFAOYSA-N 0.000 description 1
- PUHHKTBWNDEVCS-SSDOTTSWSA-N C[C@H]1CN(CCC(F)(F)F)CC1 Chemical compound C[C@H]1CN(CCC(F)(F)F)CC1 PUHHKTBWNDEVCS-SSDOTTSWSA-N 0.000 description 1
- YFNGCWGJKJYAST-UHFFFAOYSA-N C[Si+](C)(C)CCOC[n]1ncc(-c(c2c3)c[n](C4CCNCC4)c2cnc3Br)c1 Chemical compound C[Si+](C)(C)CCOC[n]1ncc(-c(c2c3)c[n](C4CCNCC4)c2cnc3Br)c1 YFNGCWGJKJYAST-UHFFFAOYSA-N 0.000 description 1
- PWDFMFLOPPHBJG-UHFFFAOYSA-N C[n](cc(-c1c[n](COCC[Si+](C)(C)C)nc1)c1c2)c1cnc2Br Chemical compound C[n](cc(-c1c[n](COCC[Si+](C)(C)C)nc1)c1c2)c1cnc2Br PWDFMFLOPPHBJG-UHFFFAOYSA-N 0.000 description 1
- QTTHKCAWADJVAA-UHFFFAOYSA-N Cc(cc1)ccc1S([n](cc(-c1c[n](COCC[Si](C)(C)C)nc1)c1c2)c1cnc2Br)(=O)=O Chemical compound Cc(cc1)ccc1S([n](cc(-c1c[n](COCC[Si](C)(C)C)nc1)c1c2)c1cnc2Br)(=O)=O QTTHKCAWADJVAA-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (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 |
|---|---|
| AU2014327235A1 AU2014327235A1 (en) | 2016-03-17 |
| AU2014327235B2 true AU2014327235B2 (en) | 2018-02-08 |
Family
ID=51626028
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2014327235A Ceased AU2014327235B2 (en) | 2013-09-26 | 2014-09-25 | New 3-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-c]pyridine derivatives as NIK inhibitors |
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 |
| KR102523405B1 (ko) | 2014-10-23 | 2023-04-18 | 얀센 파마슈티카 엔.브이. | Ｎｉｋ 억제제로서의 신규 피라졸로피리미딘 유도체 |
| CA2960336C (en) | 2014-10-23 | 2023-03-07 | Janssen Pharmaceutica Nv | Compounds as nik inhibitors |
| EP3209654B1 (en) | 2014-10-23 | 2018-10-03 | Janssen Pharmaceutica N.V. | New pyrazole derivatives as nik inhibitors |
| EA033238B1 (ru) | 2014-10-23 | 2019-09-30 | Янссен Фармацевтика Нв | Новые производные тиенопиримидина в качестве ингибиторов nik |
| CN108883103A (zh) * | 2015-12-02 | 2018-11-23 | 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 |
| JP6910359B2 (ja) | 2016-01-22 | 2021-07-28 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｎｉｋ阻害剤としての新たな置換されたシアノインドリン誘導体 |
| KR102720461B1 (ko) | 2016-01-22 | 2024-10-21 | 잔센파마슈티카엔.브이. | Nik 억제제로서의 신규 6원 헤테로방향족 치환된 시아노인돌린 유도체 |
| WO2018002219A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Cyanoindoline derivatives as nik inhibitors |
| ES2805976T3 (es) | 2016-06-30 | 2021-02-16 | Janssen Pharmaceutica Nv | Derivados heteroaromáticos en calidad de 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 |
| UA130430C2 (uk) | 2019-05-31 | 2026-02-18 | Янссен Фармацевтика Нв | НИЗЬКОМОЛЕКУЛЯРНІ ІНГІБІТОРИ КІНАЗИ, ЩО ІНДУКУЄ NF-kB |
| 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 |
| EP4253372A4 (en) | 2020-12-22 | 2024-11-13 | Kinki University | PHARMACEUTICAL COMPOSITION FOR THE RELIEF OF MALIGNANT DISEASES |
| 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 (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010042337A1 (en) * | 2008-10-07 | 2010-04-15 | Merck Sharp & Dohme Corp. | Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity |
Family Cites Families (17)
| 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 |
| CA2564356A1 (en) | 2004-04-26 | 2005-11-03 | Pfizer Inc. | Pyrrolopyridine derivatives and their use as hiv-integrase inhibitors |
| AR056786A1 (es) | 2005-11-10 | 2007-10-24 | Smithkline Beecham Corp | Compuesto de 1h- imidazo ( 4,5-c) piridin-2-ilo, composicion farmaceutica que lo comprende, procedimiento para preparar dicha composicion, su uso para preparar unmedicamento, uso de una combinacion que omprende al compuesto y al menos un agente antineoplasico para preparar un medicamento y dicha com |
| DE102008005493A1 (de) | 2008-01-22 | 2009-07-23 | Merck Patent Gmbh | 4-(Pyrrolo[2,3-c] pyridine-3-yl)-pyrimidin-2-yl-amin-derivate |
| JP2011525915A (ja) * | 2008-06-26 | 2011-09-29 | アムジエン・インコーポレーテツド | キナーゼ阻害薬としてのアルキニルアルコール類 |
| US20110201599A1 (en) | 2008-07-03 | 2011-08-18 | Exelixis, Inc. | CDK Modulators |
| 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 |
| MX2013010513A (es) | 2011-03-16 | 2013-10-07 | Hoffmann La Roche | Compuestos de alcohol 6,5-heterociclil-propargilico y usos de los mismos. |
| 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 |
| KR102523405B1 (ko) | 2014-10-23 | 2023-04-18 | 얀센 파마슈티카 엔.브이. | Ｎｉｋ 억제제로서의 신규 피라졸로피리미딘 유도체 |
| EP3209654B1 (en) | 2014-10-23 | 2018-10-03 | Janssen Pharmaceutica N.V. | New pyrazole derivatives as nik inhibitors |
| CA2960336C (en) | 2014-10-23 | 2023-03-07 | Janssen Pharmaceutica Nv | Compounds as nik inhibitors |
| EA033238B1 (ru) | 2014-10-23 | 2019-09-30 | Янссен Фармацевтика Нв | Новые производные тиенопиримидина в качестве ингибиторов nik |
-
2014
- 2014-09-24 TW TW103132895A patent/TWI627173B/zh not_active IP Right Cessation
- 2014-09-25 CA CA2922633A patent/CA2922633C/en active Active
- 2014-09-25 EP EP14776635.6A patent/EP3049412B1/en active Active
- 2014-09-25 EA EA201690657A patent/EA028101B1/ru not_active IP Right Cessation
- 2014-09-25 AU AU2014327235A patent/AU2014327235B2/en not_active Ceased
- 2014-09-25 WO PCT/EP2014/070489 patent/WO2015044269A1/en not_active Ceased
- 2014-09-25 JP JP2016516870A patent/JP6404332B2/ja not_active Expired - Fee Related
- 2014-09-25 BR BR112016006232-9A patent/BR112016006232B1/pt not_active IP Right Cessation
- 2014-09-25 MX MX2016003863A patent/MX365739B/es active IP Right Grant
- 2014-09-25 ES ES14776635.6T patent/ES2643070T3/es active Active
- 2014-09-25 US US15/024,724 patent/US9981963B2/en active Active
- 2014-09-25 KR KR1020167007902A patent/KR102317335B1/ko not_active Expired - Fee Related
- 2014-09-25 CN CN201480052798.2A patent/CN105579452B/zh not_active Expired - Fee Related
-
2016
- 2016-03-22 IL IL244702A patent/IL244702B/en active IP Right Grant
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010042337A1 (en) * | 2008-10-07 | 2010-04-15 | Merck Sharp & Dohme Corp. | Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity |
Also Published As
| Publication number | Publication date |
|---|---|
| EA201690657A1 (ru) | 2016-08-31 |
| EP3049412B1 (en) | 2017-07-12 |
| MX365739B (es) | 2019-06-12 |
| ES2643070T3 (es) | 2017-11-21 |
| BR112016006232B1 (pt) | 2022-11-29 |
| CA2922633C (en) | 2022-07-26 |
| IL244702A0 (en) | 2016-04-21 |
| AU2014327235A1 (en) | 2016-03-17 |
| EA028101B1 (ru) | 2017-10-31 |
| MX2016003863A (es) | 2016-08-04 |
| TW201602103A (zh) | 2016-01-16 |
| WO2015044269A1 (en) | 2015-04-02 |
| JP2016531858A (ja) | 2016-10-13 |
| BR112016006232A2 (pt) | 2017-08-01 |
| US20160229851A1 (en) | 2016-08-11 |
| KR20160060054A (ko) | 2016-05-27 |
| IL244702B (en) | 2019-07-31 |
| CA2922633A1 (en) | 2015-04-02 |
| JP6404332B2 (ja) | 2018-10-10 |
| TWI627173B (zh) | 2018-06-21 |
| KR102317335B1 (ko) | 2021-10-26 |
| CN105579452A (zh) | 2016-05-11 |
| US9981963B2 (en) | 2018-05-29 |
| CN105579452B (zh) | 2018-01-23 |
| EP3049412A1 (en) | 2016-08-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) | ||
| MK14 | Patent ceased section 143(a) (annual fees not paid) or expired |