CN108697710B - 作为nik抑制剂的新颖的经取代的氰基吲哚啉衍生物 - Google Patents
作为nik抑制剂的新颖的经取代的氰基吲哚啉衍生物 Download PDFInfo
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- CN108697710B CN108697710B CN201780007786.1A CN201780007786A CN108697710B CN 108697710 B CN108697710 B CN 108697710B CN 201780007786 A CN201780007786 A CN 201780007786A CN 108697710 B CN108697710 B CN 108697710B
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- 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
- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- C07D403/02—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
- C07D403/10—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 linked by a carbon chain containing aromatic 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
- 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
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/535—Organo-phosphoranes
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16152416.0 | 2016-01-22 | ||
| EP16152416 | 2016-01-22 | ||
| EP16159651 | 2016-03-10 | ||
| EP16159651.5 | 2016-03-10 | ||
| PCT/EP2017/051150 WO2017125530A1 (en) | 2016-01-22 | 2017-01-20 | New substituted cyanoindoline derivatives as nik inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN108697710A CN108697710A (zh) | 2018-10-23 |
| CN108697710B true CN108697710B (zh) | 2022-02-18 |
Family
ID=57868252
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780007786.1A Active CN108697710B (zh) | 2016-01-22 | 2017-01-20 | 作为nik抑制剂的新颖的经取代的氰基吲哚啉衍生物 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US11180487B2 (https=) |
| EP (1) | EP3405196B1 (https=) |
| JP (1) | JP6910359B2 (https=) |
| KR (1) | KR102784966B1 (https=) |
| CN (1) | CN108697710B (https=) |
| AU (1) | AU2017209935B2 (https=) |
| BR (1) | BR112018014675B1 (https=) |
| CA (1) | CA3011880A1 (https=) |
| DK (1) | DK3405196T3 (https=) |
| ES (1) | ES2775449T3 (https=) |
| HR (1) | HRP20200133T1 (https=) |
| HU (1) | HUE047684T2 (https=) |
| IL (1) | IL260500B (https=) |
| LT (1) | LT3405196T (https=) |
| MX (1) | MX2018008974A (https=) |
| PH (1) | PH12018501567A1 (https=) |
| SI (1) | SI3405196T1 (https=) |
| TW (1) | TWI739783B (https=) |
| WO (1) | WO2017125530A1 (https=) |
| ZA (1) | ZA201804688B (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2775449T3 (es) | 2016-01-22 | 2020-07-27 | Janssen Pharmaceutica Nv | Nuevos derivados de cianoindolina sustituida como inhibidores de nik |
| EP3405464B1 (en) | 2016-01-22 | 2019-12-04 | Janssen Pharmaceutica NV | New 6-membered heteroaromatic substituted cyanoindoline derivatives as nik inhibitors |
| ES2837157T3 (es) | 2016-06-30 | 2021-06-29 | Janssen Pharmaceutica Nv | Derivados de cianoindolina como inhibidores de NIK |
| WO2018002217A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Heteroaromatic derivatives as nik inhibitors |
| JP6740452B2 (ja) * | 2016-07-26 | 2020-08-12 | 深▲セン▼市塔吉瑞生物医▲薬▼有限公司Ｓｈｅｎｚｈｅｎ ＴａｒｇｅｔＲｘ，Ｉｎｃ． | プロテインチロシンキナーゼの活性を阻害するためのアミノピリミジン系化合物 |
| KR102704889B1 (ko) * | 2017-09-30 | 2024-09-10 | 하이헤 바이오파마 컴패니 리미티드 | Erk 키나제 억제 활성을 갖는 화합물 및 그의 용도 |
| TW202045008A (zh) | 2019-02-01 | 2020-12-16 | 印度商皮埃企業有限公司 | 4-取代的異噁唑/異噁唑啉(雜)芳基脒化合物、及其製備與用途 |
| US20220177459A1 (en) * | 2019-04-02 | 2022-06-09 | Hinova Pharmaceuticals Inc. | Aromatic amine compound and use thereof in preparation of ar and brd4 dual inhibitors and regulators |
| CN114222737B (zh) | 2019-05-31 | 2024-07-26 | 詹森药业有限公司 | NF-κB诱导激酶的小分子抑制剂 |
| ES2991366T3 (es) | 2020-05-08 | 2024-12-03 | Halia Therapeutics Inc | Inhibidores de NEK7 cinasa |
| US20240285599A1 (en) | 2021-08-23 | 2024-08-29 | Osaka University | Mature-Hepatocyte Transdifferentiation Suppressing Composition |
| US20240158394A1 (en) | 2022-09-14 | 2024-05-16 | Halia Therapeutics, Inc. | Nek7 inhibitors |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009158011A1 (en) * | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| WO2010042337A1 (en) * | 2008-10-07 | 2010-04-15 | Merck Sharp & Dohme Corp. | Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001025220A1 (en) | 1999-10-07 | 2001-04-12 | Amgen Inc. | Triazine kinase inhibitors |
| EP1257546A1 (en) | 2000-02-17 | 2002-11-20 | Amgen Inc. | Kinase inhibitors |
| AU2001250783A1 (en) | 2000-02-29 | 2001-09-12 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| EP1373257B9 (en) | 2001-03-29 | 2008-10-15 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| JP2005500294A (ja) | 2001-06-19 | 2005-01-06 | ブリストル−マイヤーズ スクイブ カンパニー | ホスホジエステラーゼ７に対するピリミジン阻害剤 |
| WO2003030909A1 (en) | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
| TWI546290B (zh) | 2008-06-27 | 2016-08-21 | 賽基艾維洛米斯研究股份有限公司 | 雜芳基化合物及其用途 |
| KR101906146B1 (ko) | 2009-08-17 | 2018-10-10 | 메모리얼 슬로안-케터링 캔서 센터 | 열 충격 단백질 결합 화합물, 조성물, 및 이의 제조 방법 및 사용 방법 |
| WO2011153553A2 (en) | 2010-06-04 | 2011-12-08 | The Regents Of The University Of California | Methods and compositions for kinase inhibition |
| BR112013002112B1 (pt) | 2010-07-29 | 2021-04-06 | Rigel Pharmaceuticals, Inc. | Composto, composição farmacêutica, e, uso de um composto, ou de um respectivo sal farmaceuticamente aceitável, ou de uma composição |
| WO2012142329A1 (en) | 2011-04-12 | 2012-10-18 | Myrexis, Inc. | Compositions and therapeutic uses of ikk-related kinase epsilon and tankbinding kinase 1 inhibitors |
| TWI663166B (zh) | 2013-04-24 | 2019-06-21 | 健生藥品公司 | 新化合物 |
| AR093580A1 (es) | 2013-08-30 | 2015-06-10 | Ptc Therapeutics Inc | Inhibidores bmi-1 de pirimidina sustituidos |
| 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 |
| CN106458990B (zh) | 2014-04-04 | 2019-06-07 | 希洛斯医药品股份有限公司 | 细胞周期蛋白依赖性激酶7(cdk7)的抑制剂 |
| JP2017520526A (ja) | 2014-05-22 | 2017-07-27 | ザ・ユニバーシティ・オブ・シドニー | オメガ−３類似体 |
| WO2016022645A1 (en) | 2014-08-06 | 2016-02-11 | Merck Sharp & Dohme Corp. | Heterocyclic cgrp receptor antagonists |
| NZ729618A (en) | 2014-09-26 | 2018-07-27 | Gilead Sciences Inc | Aminotriazine derivatives useful as tank-binding kinase inhibitor compounds |
| CN106928216A (zh) | 2015-12-31 | 2017-07-07 | 中国科学院上海药物研究所 | 具有erk激酶抑制活性的化合物、其制备方法和用途 |
| EP3405464B1 (en) | 2016-01-22 | 2019-12-04 | Janssen Pharmaceutica NV | New 6-membered heteroaromatic substituted cyanoindoline derivatives as nik inhibitors |
| ES2775449T3 (es) | 2016-01-22 | 2020-07-27 | Janssen Pharmaceutica Nv | Nuevos derivados de cianoindolina sustituida como inhibidores de nik |
| CN109152784B (zh) | 2016-03-16 | 2021-12-28 | 库拉肿瘤学公司 | 经取代的menin-mll抑制剂及使用方法 |
| WO2018002217A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Heteroaromatic derivatives as nik inhibitors |
| ES2837157T3 (es) | 2016-06-30 | 2021-06-29 | Janssen Pharmaceutica Nv | Derivados de cianoindolina como inhibidores de NIK |
-
2017
- 2017-01-20 ES ES17701110T patent/ES2775449T3/es active Active
- 2017-01-20 CN CN201780007786.1A patent/CN108697710B/zh active Active
- 2017-01-20 SI SI201730183T patent/SI3405196T1/sl unknown
- 2017-01-20 BR BR112018014675-7A patent/BR112018014675B1/pt active IP Right Grant
- 2017-01-20 US US16/071,192 patent/US11180487B2/en active Active
- 2017-01-20 HR HRP20200133TT patent/HRP20200133T1/hr unknown
- 2017-01-20 MX MX2018008974A patent/MX2018008974A/es unknown
- 2017-01-20 WO PCT/EP2017/051150 patent/WO2017125530A1/en not_active Ceased
- 2017-01-20 KR KR1020187024257A patent/KR102784966B1/ko active Active
- 2017-01-20 CA CA3011880A patent/CA3011880A1/en active Pending
- 2017-01-20 EP EP17701110.3A patent/EP3405196B1/en active Active
- 2017-01-20 DK DK17701110.3T patent/DK3405196T3/da active
- 2017-01-20 TW TW105143703A patent/TWI739783B/zh not_active IP Right Cessation
- 2017-01-20 HU HUE17701110A patent/HUE047684T2/hu unknown
- 2017-01-20 AU AU2017209935A patent/AU2017209935B2/en active Active
- 2017-01-20 LT LTEP17701110.3T patent/LT3405196T/lt unknown
- 2017-01-20 JP JP2018535876A patent/JP6910359B2/ja active Active
-
2018
- 2018-07-09 IL IL260500A patent/IL260500B/en active IP Right Grant
- 2018-07-13 ZA ZA2018/04688A patent/ZA201804688B/en unknown
- 2018-07-23 PH PH12018501567A patent/PH12018501567A1/en unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009158011A1 (en) * | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| 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 |
|---|---|
| JP6910359B2 (ja) | 2021-07-28 |
| JP2019504067A (ja) | 2019-02-14 |
| LT3405196T (lt) | 2020-02-25 |
| US20210087182A1 (en) | 2021-03-25 |
| IL260500B (en) | 2021-01-31 |
| WO2017125530A1 (en) | 2017-07-27 |
| KR102784966B1 (ko) | 2025-03-20 |
| HRP20200133T1 (hr) | 2020-05-15 |
| ZA201804688B (en) | 2022-03-30 |
| DK3405196T3 (en) | 2020-03-09 |
| KR20180100441A (ko) | 2018-09-10 |
| EP3405196B1 (en) | 2019-12-04 |
| PH12018501567A1 (en) | 2019-01-28 |
| BR112018014675A2 (pt) | 2018-12-11 |
| AU2017209935B2 (en) | 2021-04-01 |
| SI3405196T1 (sl) | 2020-03-31 |
| AU2017209935A1 (en) | 2018-08-09 |
| TW201728577A (zh) | 2017-08-16 |
| EP3405196A1 (en) | 2018-11-28 |
| ES2775449T3 (es) | 2020-07-27 |
| HUE047684T2 (hu) | 2020-05-28 |
| BR112018014675B1 (pt) | 2023-12-19 |
| TWI739783B (zh) | 2021-09-21 |
| CA3011880A1 (en) | 2017-07-27 |
| CN108697710A (zh) | 2018-10-23 |
| MX2018008974A (es) | 2018-11-09 |
| US11180487B2 (en) | 2021-11-23 |
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