AU2015334915B2 - New pyrazolopyrimidine derivatives as NIK inhibitors - Google Patents
New pyrazolopyrimidine derivatives as NIK inhibitors Download PDFInfo
- Publication number
- AU2015334915B2 AU2015334915B2 AU2015334915A AU2015334915A AU2015334915B2 AU 2015334915 B2 AU2015334915 B2 AU 2015334915B2 AU 2015334915 A AU2015334915 A AU 2015334915A AU 2015334915 A AU2015334915 A AU 2015334915A AU 2015334915 B2 AU2015334915 B2 AU 2015334915B2
- Authority
- AU
- Australia
- Prior art keywords
- substituted
- 4alkyl
- group
- hydrogen
- fluoro
- 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
- ANSIOVHKPLAOPM-UHFFFAOYSA-N CC(C)(C)OC([n](cc(B1OC(C)(C)C(C)(C)O1)c1c2)c1cnc2Br)=C Chemical compound CC(C)(C)OC([n](cc(B1OC(C)(C)C(C)(C)O1)c1c2)c1cnc2Br)=C ANSIOVHKPLAOPM-UHFFFAOYSA-N 0.000 description 1
- 0 CC(C*)(C#CC(*1=C(C)C1C1N2*)=C(C*)C1C(C(C1=NC)=[*+]C(N)=*C1=C)=C2I)O Chemical compound CC(C*)(C#CC(*1=C(C)C1C1N2*)=C(C*)C1C(C(C1=NC)=[*+]C(N)=*C1=C)=C2I)O 0.000 description 1
- CEPCNHUDSNMACE-UHFFFAOYSA-N COCCC[n](cc(c1c2)-c3nc(Cl)nc4c[n](C5CC5)nc34)c1cnc2Br Chemical compound COCCC[n](cc(c1c2)-c3nc(Cl)nc4c[n](C5CC5)nc34)c1cnc2Br CEPCNHUDSNMACE-UHFFFAOYSA-N 0.000 description 1
- LUYQBWQJCFIINX-UHFFFAOYSA-N Cc(cc1)ccc1S([n]1c2cc(F)c(C)cc2cc1)(=C)=O Chemical compound Cc(cc1)ccc1S([n]1c2cc(F)c(C)cc2cc1)(=C)=O LUYQBWQJCFIINX-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- 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
-
- 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 (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14190073.8 | 2014-10-23 | ||
| 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 |
|---|---|
| AU2015334915A1 AU2015334915A1 (en) | 2017-03-30 |
| AU2015334915B2 true AU2015334915B2 (en) | 2019-09-19 |
Family
ID=51846471
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2015334915A Ceased AU2015334915B2 (en) | 2014-10-23 | 2015-10-22 | New pyrazolopyrimidine derivatives as NIK inhibitors |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10221180B2 (OSRAM) |
| EP (1) | EP3209663B1 (OSRAM) |
| JP (1) | JP6616412B2 (OSRAM) |
| KR (1) | KR102523405B1 (OSRAM) |
| CN (1) | CN107074882B (OSRAM) |
| AU (1) | AU2015334915B2 (OSRAM) |
| BR (1) | BR112017007704B1 (OSRAM) |
| CA (1) | CA2960574C (OSRAM) |
| EA (1) | EA033237B1 (OSRAM) |
| ES (1) | ES2715104T3 (OSRAM) |
| IL (1) | IL251778B (OSRAM) |
| MX (1) | MX371152B (OSRAM) |
| WO (1) | WO2016062790A1 (OSRAM) |
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 |
| 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 |
| US9981962B2 (en) | 2014-10-23 | 2018-05-29 | Janssen Pharmaceutica Nv | Pyrazole derivatives 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). |
| BR112017007704B1 (pt) | 2014-10-23 | 2023-04-11 | Janssen Pharmaceutica N.V | Derivados de pirazolopirimidina como inibidores de nik, seu uso e composição farmacêutica que os compreende |
| ES2718557T3 (es) | 2014-10-23 | 2019-07-02 | Janssen Pharmaceutica Nv | Nuevos compuestos como inhibidores de nik |
| US12448374B2 (en) | 2018-06-07 | 2025-10-21 | Disarm Therapeutics, Inc. | Inhibitors of SARM1 |
| EA202092962A1 (ru) * | 2018-06-18 | 2021-09-06 | Янссен Фармацевтика Нв | Производные пиразола в качестве ингибиторов malt1 |
| CN113164508B (zh) | 2018-12-19 | 2025-07-08 | 达萨玛治疗公司 | 与神经保护剂组合的sarm1抑制剂 |
| SG11202109997PA (en) * | 2019-03-29 | 2021-10-28 | Kowa Co | Novel azaindole derivative |
| ES2989387T3 (es) | 2019-05-31 | 2024-11-26 | Janssen Pharmaceutica Nv | Pequeñas moléculas inhibidoras de la quinasa inductora de nf-kb |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5169947A (en) * | 1989-01-20 | 1992-12-08 | Pfizer Inc. | 3-(1,2,5,6-tetrahydropyridyl)-pyrrolopyridines |
| WO2009158011A1 (en) * | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA06012449A (es) | 2004-04-26 | 2007-01-17 | Pfizer | Inhibidores de la enzima integrasa de vih. |
| 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 |
| CA2728559A1 (en) | 2008-07-03 | 2010-01-07 | Exelixis Inc. | Cdk modulators |
| US20110183975A1 (en) | 2008-10-07 | 2011-07-28 | Yasuhiro Goto | 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 |
| KR20130133051A (ko) | 2011-03-16 | 2013-12-05 | 에프. 호프만-라 로슈 아게 | 6,5-헤테로사이클릭 프로파길릭 알콜 화합물 및 이의 용도 |
| 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 |
| 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). |
| BR112017007704B1 (pt) | 2014-10-23 | 2023-04-11 | Janssen Pharmaceutica N.V | Derivados de pirazolopirimidina como inibidores de nik, seu uso e composição farmacêutica que os compreende |
| US9981962B2 (en) | 2014-10-23 | 2018-05-29 | Janssen Pharmaceutica Nv | Pyrazole derivatives as NIK inhibitors |
| ES2718557T3 (es) | 2014-10-23 | 2019-07-02 | Janssen Pharmaceutica Nv | Nuevos compuestos como inhibidores de nik |
-
2015
- 2015-10-22 BR BR112017007704-3A patent/BR112017007704B1/pt not_active IP Right Cessation
- 2015-10-22 ES ES15784050T patent/ES2715104T3/es active Active
- 2015-10-22 KR KR1020177010805A patent/KR102523405B1/ko active Active
- 2015-10-22 CN CN201580057545.9A patent/CN107074882B/zh not_active Expired - Fee Related
- 2015-10-22 AU AU2015334915A patent/AU2015334915B2/en not_active Ceased
- 2015-10-22 WO PCT/EP2015/074431 patent/WO2016062790A1/en not_active Ceased
- 2015-10-22 EP EP15784050.5A patent/EP3209663B1/en active Active
- 2015-10-22 EA EA201790907A patent/EA033237B1/ru not_active IP Right Cessation
- 2015-10-22 CA CA2960574A patent/CA2960574C/en active Active
- 2015-10-22 US US15/520,346 patent/US10221180B2/en active Active
- 2015-10-22 JP JP2017522086A patent/JP6616412B2/ja not_active Expired - Fee Related
- 2015-10-22 MX MX2017005284A patent/MX371152B/es active IP Right Grant
-
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 (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5169947A (en) * | 1989-01-20 | 1992-12-08 | Pfizer Inc. | 3-(1,2,5,6-tetrahydropyridyl)-pyrrolopyridines |
| CN1025998C (zh) * | 1989-01-20 | 1994-09-28 | 美国辉瑞有限公司 | 3-(1，2，5，6-四氢吡啶基)-吡咯并吡啶类的制备方法 |
| WO2009158011A1 (en) * | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2960574C (en) | 2023-03-07 |
| CN107074882A (zh) | 2017-08-18 |
| JP2017531678A (ja) | 2017-10-26 |
| US10822342B2 (en) | 2020-11-03 |
| US20170334915A1 (en) | 2017-11-23 |
| AU2015334915A1 (en) | 2017-03-30 |
| CN107074882B (zh) | 2019-07-30 |
| US10221180B2 (en) | 2019-03-05 |
| ES2715104T3 (es) | 2019-05-31 |
| CA2960574A1 (en) | 2016-04-28 |
| KR20170068489A (ko) | 2017-06-19 |
| EP3209663A1 (en) | 2017-08-30 |
| MX371152B (es) | 2020-01-20 |
| BR112017007704B1 (pt) | 2023-04-11 |
| BR112017007704A2 (pt) | 2017-12-19 |
| EA033237B1 (ru) | 2019-09-30 |
| US20190169198A1 (en) | 2019-06-06 |
| IL251778B (en) | 2020-10-29 |
| EP3209663B1 (en) | 2018-12-12 |
| WO2016062790A1 (en) | 2016-04-28 |
| KR102523405B1 (ko) | 2023-04-18 |
| MX2017005284A (es) | 2017-07-28 |
| JP6616412B2 (ja) | 2019-12-04 |
| EA201790907A1 (ru) | 2017-08-31 |
| IL251778A0 (en) | 2017-06-29 |
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| AU2014327233B2 (en) | New 1-(4-pyrimidinyl)-1H-pyrrolo[3,2-c]pyridine derivatives as NIK inhibitors | |
| AU2015334914B2 (en) | New thienopyrimidine derivatives as NIK inhibitors | |
| AU2014259477B2 (en) | 3-(2-aminopyrimidin-4-yl)-5-(3-hydroxypropynyl)-1H-pyrrolo[2,3-c]pyridine derivatives as NIK inhibitors for the treatment of cancer | |
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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 |