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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Immunology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14190072.0 | 2014-10-23 | ||
| EP14190072 | 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 |
| WO2016062789A1 (en) | 2014-10-23 | 2016-04-28 | Janssen Pharmaceutica Nv | New thienopyrimidine derivatives as nik inhibitors |
| WO2016062790A1 (en) | 2014-10-23 | 2016-04-28 | Janssen Pharmaceutica Nv | New pyrazolopyrimidine derivatives as nik inhibitors |
| JP6676048B2 (ja) | 2014-10-23 | 2020-04-08 | 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化合物 |
| MX371150B (es) | 2014-10-23 | 2020-01-20 | Janssen Pharmaceutica Nv | NUEVOS DERIVADOS DE PIRAZOL EN CALIDAD DE INHIBIDORES DE LA CINASA INDUCTORA DE NF-kB (NIK). |
| WO2017096323A1 (en) * | 2015-12-02 | 2017-06-08 | Astraea Therapeutics, Llc | Piperidinyl nociceptin receptor compounds |
| US10112924B2 (en) | 2015-12-02 | 2018-10-30 | Astraea Therapeutics, Inc. | Piperdinyl nociceptin receptor compounds |
| US11001569B2 (en) * | 2016-01-22 | 2021-05-11 | Janssen Pharmaceutica Nv | 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors |
| PH12021553011A1 (en) | 2019-05-31 | 2022-11-07 | Janssen Pharmaceutica Nv | SMALL MOLECULE INHIBITORS OF NF-kB INDUCING KINASE |
| 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 |
| 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 |
| WO2009158011A1 (en) * | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| US20110201599A1 (en) | 2008-07-03 | 2011-08-18 | 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 |
| 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 |
| 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 |
| WO2016062790A1 (en) | 2014-10-23 | 2016-04-28 | Janssen Pharmaceutica Nv | New pyrazolopyrimidine derivatives as nik inhibitors |
| WO2016062789A1 (en) | 2014-10-23 | 2016-04-28 | Janssen Pharmaceutica Nv | New thienopyrimidine derivatives as nik inhibitors |
| JP6676048B2 (ja) | 2014-10-23 | 2020-04-08 | 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化合物 |
| MX371150B (es) | 2014-10-23 | 2020-01-20 | Janssen Pharmaceutica Nv | NUEVOS DERIVADOS DE PIRAZOL EN CALIDAD DE INHIBIDORES DE LA CINASA INDUCTORA DE NF-kB (NIK). |
-
2015
- 2015-10-22 MX MX2017005283A patent/MX371150B/es active IP Right Grant
- 2015-10-22 BR BR112017008039-7A patent/BR112017008039B1/pt not_active IP Right Cessation
- 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 EP EP15784360.8A patent/EP3209654B1/en active Active
- 2015-10-22 KR KR1020177010800A patent/KR102499862B1/ko active Active
- 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 ES ES15784360T patent/ES2704749T3/es active Active
- 2015-10-22 CA CA2960335A patent/CA2960335C/en active Active
- 2015-10-22 WO PCT/EP2015/074433 patent/WO2016062791A1/en not_active Ceased
- 2015-10-22 AU AU2015334916A patent/AU2015334916B2/en not_active Ceased
-
2017
- 2017-04-19 IL IL251777A patent/IL251777B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MX2017005283A (es) | 2017-08-15 |
| KR102499862B1 (ko) | 2023-02-13 |
| EA033236B1 (ru) | 2019-09-30 |
| EP3209654B1 (en) | 2018-10-03 |
| ES2704749T3 (es) | 2019-03-19 |
| MX371150B (es) | 2020-01-20 |
| AU2015334916A1 (en) | 2017-03-23 |
| JP2017531677A (ja) | 2017-10-26 |
| EA201790904A1 (ru) | 2017-08-31 |
| BR112017008039B1 (pt) | 2023-04-11 |
| US20170334900A1 (en) | 2017-11-23 |
| CA2960335A1 (en) | 2016-04-28 |
| BR112017008039A2 (pt) | 2017-12-19 |
| WO2016062791A1 (en) | 2016-04-28 |
| CN107074818B (zh) | 2020-04-17 |
| IL251777A0 (en) | 2017-06-29 |
| EP3209654A1 (en) | 2017-08-30 |
| CN107074818A (zh) | 2017-08-18 |
| AU2015334916B2 (en) | 2020-02-06 |
| US9981962B2 (en) | 2018-05-29 |
| KR20170068488A (ko) | 2017-06-19 |
| IL251777B (en) | 2021-09-30 |
| CA2960335C (en) | 2023-09-19 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6404332B2 (ja) | 新規な、ＮＩＫ阻害剤としての３−（１Ｈ−ピラゾール−４−イル）−１Ｈ−ピロロ［２，３−ｃ］ピリジン誘導体 | |
| JP6616411B2 (ja) | 新規な、ｎｉｋ阻害剤としてのピラゾール誘導体 | |
| JP6402179B2 (ja) | 新規な、ＮＩＫ阻害剤としての１−（４−ピリミジニル）−１Ｈ−ピロロ［３，２−ｃ］ピリジン誘導体 | |
| EP2989101B1 (en) | 3-(2-aminopyrimidin-4-yl)-5-(3-hydroxypropynyl)-1h-pyrrolo[2,3-c]pyridine derivatives as nik inhibitors for the treatment of cancer | |
| JP6616412B2 (ja) | Ｎｉｋ阻害剤としての新規のピラゾロピリミジン誘導体 | |
| JP6603713B2 (ja) | Ｎｉｋ阻害剤としての新規のチエノピリミジン誘導体 | |
| JP2017531681A (ja) | Ｎｉｋ阻害剤としての新規化合物 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20181019 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20190711 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20190723 |
|
| A524 | Written submission of copy of amendment under article 19 pct |
Free format text: JAPANESE INTERMEDIATE CODE: A524 Effective date: 20191008 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20191105 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20191107 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6616411 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| LAPS | Cancellation because of no payment of annual fees |