JP6616411B2 - 新規な、ｎｉｋ阻害剤としてのピラゾール誘導体 - Google Patents
新規な、ｎｉｋ阻害剤としてのピラゾール誘導体 Download PDFInfo
- Publication number
- JP6616411B2 JP6616411B2 JP2017522072A JP2017522072A JP6616411B2 JP 6616411 B2 JP6616411 B2 JP 6616411B2 JP 2017522072 A JP2017522072 A JP 2017522072A JP 2017522072 A JP2017522072 A JP 2017522072A JP 6616411 B2 JP6616411 B2 JP 6616411B2
- Authority
- JP
- Japan
- Prior art keywords
- group
- alkyl
- substituted
- het
- hydrogen atom
- 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.)
- Expired - Fee Related
Links
Classifications
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Oncology (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2017531677A JP2017531677A (ja) | 2017-10-26 |
| JP2017531677A5 JP2017531677A5 (enExample) | 2019-11-21 |
| JP6616411B2 true JP6616411B2 (ja) | 2019-12-04 |
Family
ID=51865980
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017522072A Expired - Fee Related JP6616411B2 (ja) | 2014-10-23 | 2015-10-22 | 新規な、ｎｉｋ阻害剤としてのピラゾール誘導体 |
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)
| 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 |
| 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 |
| EA033238B1 (ru) | 2014-10-23 | 2019-09-30 | Янссен Фармацевтика Нв | Новые производные тиенопиримидина в качестве ингибиторов nik |
| CN107074855B (zh) | 2014-10-23 | 2019-11-05 | 詹森药业有限公司 | 作为nik抑制剂的新的化合物 |
| ES2704749T3 (es) | 2014-10-23 | 2019-03-19 | Janssen Pharmaceutica Nv | Nuevos derivados de pirazol en calidad de inhibidores de nik |
| KR102523405B1 (ko) | 2014-10-23 | 2023-04-18 | 얀센 파마슈티카 엔.브이. | Ｎｉｋ 억제제로서의 신규 피라졸로피리미딘 유도체 |
| US10112924B2 (en) | 2015-12-02 | 2018-10-30 | Astraea Therapeutics, Inc. | Piperdinyl nociceptin receptor compounds |
| EP3383390A4 (en) * | 2015-12-02 | 2019-11-20 | Astraea Therapeutics, LLC | PIPERIDINYL-nociceptin RECEPTOR COMPOUNDS |
| CN109311846B (zh) * | 2016-01-22 | 2021-03-19 | 杨森制药有限公司 | 作为nik抑制剂的新的6元杂芳族取代的氰基吲哚衍生物 |
| SMT202400418T1 (it) | 2019-05-31 | 2024-11-15 | Janssen Pharmaceutica Nv | Inibitori a piccola molecola di chinasi che induce nf-κb |
| 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 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0510319A (pt) | 2004-04-26 | 2007-10-16 | Pfizer | inibidores da enzima integrase de hiv |
| 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 |
| WO2009158011A1 (en) * | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| JP2011526931A (ja) | 2008-07-03 | 2011-10-20 | エグゼリクシス， インコーポレイテッド | Ｃｄｋモジュレーター |
| 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 |
| CA2827161A1 (en) * | 2011-03-16 | 2012-09-20 | F. Hoffmann-La Roche Ag | 6,5-heterocyclic propargylic alcohol compounds and uses therefor |
| 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 |
| CN107074855B (zh) | 2014-10-23 | 2019-11-05 | 詹森药业有限公司 | 作为nik抑制剂的新的化合物 |
| EA033238B1 (ru) | 2014-10-23 | 2019-09-30 | Янссен Фармацевтика Нв | Новые производные тиенопиримидина в качестве ингибиторов nik |
| ES2704749T3 (es) | 2014-10-23 | 2019-03-19 | Janssen Pharmaceutica Nv | Nuevos derivados de pirazol en calidad de inhibidores de nik |
| KR102523405B1 (ko) | 2014-10-23 | 2023-04-18 | 얀센 파마슈티카 엔.브이. | Ｎｉｋ 억제제로서의 신규 피라졸로피리미딘 유도체 |
-
2015
- 2015-10-22 ES ES15784360T patent/ES2704749T3/es active Active
- 2015-10-22 WO PCT/EP2015/074433 patent/WO2016062791A1/en not_active Ceased
- 2015-10-22 MX MX2017005283A patent/MX371150B/es active IP Right Grant
- 2015-10-22 KR KR1020177010800A patent/KR102499862B1/ko active Active
- 2015-10-22 BR BR112017008039-7A patent/BR112017008039B1/pt not_active IP Right Cessation
- 2015-10-22 CA CA2960335A patent/CA2960335C/en active Active
- 2015-10-22 CN CN201580057462.XA patent/CN107074818B/zh not_active Expired - Fee Related
- 2015-10-22 JP JP2017522072A patent/JP6616411B2/ja not_active Expired - Fee Related
- 2015-10-22 US US15/520,342 patent/US9981962B2/en active Active
- 2015-10-22 EA EA201790904A patent/EA033236B1/ru not_active IP Right Cessation
- 2015-10-22 AU AU2015334916A patent/AU2015334916B2/en not_active Ceased
- 2015-10-22 EP EP15784360.8A patent/EP3209654B1/en active Active
-
2017
- 2017-04-19 IL IL251777A patent/IL251777B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN107074818A (zh) | 2017-08-18 |
| EP3209654B1 (en) | 2018-10-03 |
| KR20170068488A (ko) | 2017-06-19 |
| CN107074818B (zh) | 2020-04-17 |
| WO2016062791A1 (en) | 2016-04-28 |
| JP2017531677A (ja) | 2017-10-26 |
| EP3209654A1 (en) | 2017-08-30 |
| US20170334900A1 (en) | 2017-11-23 |
| IL251777A0 (en) | 2017-06-29 |
| ES2704749T3 (es) | 2019-03-19 |
| CA2960335A1 (en) | 2016-04-28 |
| MX371150B (es) | 2020-01-20 |
| CA2960335C (en) | 2023-09-19 |
| US9981962B2 (en) | 2018-05-29 |
| MX2017005283A (es) | 2017-08-15 |
| BR112017008039B1 (pt) | 2023-04-11 |
| IL251777B (en) | 2021-09-30 |
| AU2015334916A1 (en) | 2017-03-23 |
| AU2015334916B2 (en) | 2020-02-06 |
| BR112017008039A2 (pt) | 2017-12-19 |
| EA033236B1 (ru) | 2019-09-30 |
| KR102499862B1 (ko) | 2023-02-13 |
| EA201790904A1 (ru) | 2017-08-31 |
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