EA033237B1 - Новые производные пиразолопиримидина в качестве ингибиторов nik, фармацевтическая композиция и лекарственное средство, содержащее ее - Google Patents
Новые производные пиразолопиримидина в качестве ингибиторов nik, фармацевтическая композиция и лекарственное средство, содержащее ееInfo
- Publication number
- EA033237B1 EA033237B1 EA201790907A EA201790907A EA033237B1 EA 033237 B1 EA033237 B1 EA 033237B1 EA 201790907 A EA201790907 A EA 201790907A EA 201790907 A EA201790907 A EA 201790907A EA 033237 B1 EA033237 B1 EA 033237B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- medicament
- pharmaceutical composition
- same
- disorders
- pyrazolopyrimidine derivatives
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- OGEBRHQLRGFBNV-RZDIXWSQSA-N chembl2036808 Chemical class C12=NC(NCCCC)=NC=C2C(C=2C=CC(F)=CC=2)=NN1C[C@H]1CC[C@H](N)CC1 OGEBRHQLRGFBNV-RZDIXWSQSA-N 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 208000023275 Autoimmune disease Diseases 0.000 abstract 2
- 102000019148 NF-kappaB-inducing kinase activity proteins Human genes 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 201000011510 cancer Diseases 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 208000027866 inflammatory disease Diseases 0.000 abstract 2
- 208000030159 metabolic disease Diseases 0.000 abstract 2
- 101001005550 Homo sapiens Mitogen-activated protein kinase kinase kinase 14 Proteins 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 102100025211 Mitogen-activated protein kinase kinase kinase 14 Human genes 0.000 abstract 1
- 108010014632 NF-kappa B kinase Proteins 0.000 abstract 1
- 108040008091 NF-kappaB-inducing kinase activity proteins Proteins 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—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
- A61K31/40—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
- A61K31/435—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
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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)
- 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)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14190073 | 2014-10-23 | ||
| PCT/EP2015/074431 WO2016062790A1 (en) | 2014-10-23 | 2015-10-22 | New pyrazolopyrimidine derivatives as nik inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201790907A1 EA201790907A1 (ru) | 2017-08-31 |
| EA033237B1 true EA033237B1 (ru) | 2019-09-30 |
Family
ID=51846471
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201790907A EA033237B1 (ru) | 2014-10-23 | 2015-10-22 | Новые производные пиразолопиримидина в качестве ингибиторов nik, фармацевтическая композиция и лекарственное средство, содержащее ее |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10221180B2 (enExample) |
| EP (1) | EP3209663B1 (enExample) |
| JP (1) | JP6616412B2 (enExample) |
| KR (1) | KR102523405B1 (enExample) |
| CN (1) | CN107074882B (enExample) |
| AU (1) | AU2015334915B2 (enExample) |
| BR (1) | BR112017007704B1 (enExample) |
| CA (1) | CA2960574C (enExample) |
| EA (1) | EA033237B1 (enExample) |
| ES (1) | ES2715104T3 (enExample) |
| IL (1) | IL251778B (enExample) |
| MX (1) | MX371152B (enExample) |
| WO (1) | WO2016062790A1 (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 |
| CN112839648B (zh) | 2018-06-07 | 2025-04-04 | 达萨玛治疗公司 | Sarm1抑制剂 |
| ES2992431T3 (es) * | 2018-06-18 | 2024-12-12 | Janssen Pharmaceutica Nv | Derivados de pirazol como inhibidores de MALT1 |
| EP3897670A4 (en) | 2018-12-19 | 2022-09-07 | Disarm Therapeutics, Inc. | MRSA1 INHIBITORS IN COMBINATION WITH NEUROPROTECTIVE AGENTS |
| WO2020203950A1 (ja) * | 2019-03-29 | 2020-10-08 | 興和株式会社 | 新規アザインドール誘導体 |
| SMT202400418T1 (it) | 2019-05-31 | 2024-11-15 | Janssen Pharmaceutica Nv | Inibitori a piccola molecola di chinasi che induce nf-κb |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009158011A1 (en) * | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1990007926A1 (en) * | 1989-01-20 | 1990-07-26 | Pfizer Inc. | 3-(1,2,5,6-tetrahydropyridyl)-pyrrolopyridines |
| 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 |
| 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 |
| 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 |
-
2015
- 2015-10-22 KR KR1020177010805A patent/KR102523405B1/ko active Active
- 2015-10-22 MX MX2017005284A patent/MX371152B/es active IP Right Grant
- 2015-10-22 EP EP15784050.5A patent/EP3209663B1/en active Active
- 2015-10-22 WO PCT/EP2015/074431 patent/WO2016062790A1/en not_active Ceased
- 2015-10-22 BR BR112017007704-3A patent/BR112017007704B1/pt not_active IP Right Cessation
- 2015-10-22 CN CN201580057545.9A patent/CN107074882B/zh not_active Expired - Fee Related
- 2015-10-22 JP JP2017522086A patent/JP6616412B2/ja not_active Expired - Fee Related
- 2015-10-22 AU AU2015334915A patent/AU2015334915B2/en not_active Ceased
- 2015-10-22 CA CA2960574A patent/CA2960574C/en active Active
- 2015-10-22 EA EA201790907A patent/EA033237B1/ru not_active IP Right Cessation
- 2015-10-22 ES ES15784050T patent/ES2715104T3/es active Active
- 2015-10-22 US US15/520,346 patent/US10221180B2/en active Active
-
2017
- 2017-04-19 IL IL251778A patent/IL251778B/en active IP Right Grant
-
2019
- 2019-02-01 US US16/265,679 patent/US10822342B2/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009158011A1 (en) * | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| MX2017005284A (es) | 2017-07-28 |
| CA2960574C (en) | 2023-03-07 |
| US10221180B2 (en) | 2019-03-05 |
| CA2960574A1 (en) | 2016-04-28 |
| MX371152B (es) | 2020-01-20 |
| EP3209663B1 (en) | 2018-12-12 |
| JP2017531678A (ja) | 2017-10-26 |
| US10822342B2 (en) | 2020-11-03 |
| US20190169198A1 (en) | 2019-06-06 |
| KR20170068489A (ko) | 2017-06-19 |
| IL251778A0 (en) | 2017-06-29 |
| AU2015334915A1 (en) | 2017-03-30 |
| CN107074882B (zh) | 2019-07-30 |
| IL251778B (en) | 2020-10-29 |
| KR102523405B1 (ko) | 2023-04-18 |
| ES2715104T3 (es) | 2019-05-31 |
| US20170334915A1 (en) | 2017-11-23 |
| BR112017007704A2 (pt) | 2017-12-19 |
| EA201790907A1 (ru) | 2017-08-31 |
| JP6616412B2 (ja) | 2019-12-04 |
| WO2016062790A1 (en) | 2016-04-28 |
| AU2015334915B2 (en) | 2019-09-19 |
| EP3209663A1 (en) | 2017-08-30 |
| CN107074882A (zh) | 2017-08-18 |
| BR112017007704B1 (pt) | 2023-04-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG TJ TM |