CN109689645B - 作为nik抑制剂的氰基吲哚啉衍生物 - Google Patents
作为nik抑制剂的氰基吲哚啉衍生物 Download PDFInfo
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- CN109689645B CN109689645B CN201780053613.3A CN201780053613A CN109689645B CN 109689645 B CN109689645 B CN 109689645B CN 201780053613 A CN201780053613 A CN 201780053613A CN 109689645 B CN109689645 B CN 109689645B
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—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
- A61K31/495—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
- A61K31/5365—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 ortho- or peri-condensed with heterocyclic ring 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
- A61K31/535—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
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- C07D403/02—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
- C07D403/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D405/02—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 two hetero rings
- C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16177147.2 | 2016-06-30 | ||
| EP16177142 | 2016-06-30 | ||
| EP16177147 | 2016-06-30 | ||
| EP16177131 | 2016-06-30 | ||
| EP16177131.6 | 2016-06-30 | ||
| EP16177142.3 | 2016-06-30 | ||
| PCT/EP2017/066125 WO2018002219A1 (en) | 2016-06-30 | 2017-06-29 | Cyanoindoline derivatives as nik inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN109689645A CN109689645A (zh) | 2019-04-26 |
| CN109689645B true CN109689645B (zh) | 2022-06-03 |
Family
ID=59227756
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780053613.3A Active CN109689645B (zh) | 2016-06-30 | 2017-06-29 | 作为nik抑制剂的氰基吲哚啉衍生物 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US20190119299A1 (https=) |
| EP (1) | EP3478673B1 (https=) |
| JP (1) | JP6936814B2 (https=) |
| KR (1) | KR102587619B1 (https=) |
| CN (1) | CN109689645B (https=) |
| AU (1) | AU2017289317B2 (https=) |
| ES (1) | ES2837157T3 (https=) |
| WO (1) | WO2018002219A1 (https=) |
Families Citing this family (8)
| 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 |
| 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 |
| IL289612B2 (en) * | 2019-07-04 | 2026-02-01 | Qilu Regor Therapeutics Inc | HPK1 inhibitors and their uses |
| TW202304906A (zh) * | 2021-04-08 | 2023-02-01 | 大陸商杭州阿諾生物醫藥科技有限公司 | 高活性hpk1激酶抑制劑 |
| CN114380806B (zh) * | 2022-03-24 | 2022-06-10 | 中国药科大学 | 2-氨基-4-吲哚基嘧啶类化合物及其制备方法与应用 |
Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002079197A1 (en) * | 2001-03-29 | 2002-10-10 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| 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 |
| CN101039919A (zh) * | 2004-10-13 | 2007-09-19 | 惠氏公司 | 经n-苯磺酰基取代的苯胺基嘧啶类似物 |
| 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 |
| CN105143223A (zh) * | 2013-04-24 | 2015-12-09 | 詹森药业有限公司 | 3-(2-氨基嘧啶-4-基)-5-(3-羟丙炔基)-1h-吡咯并[2,3-c]吡啶衍生物作为nik抑制剂用于治疗癌症 |
| CN105579452A (zh) * | 2013-09-26 | 2016-05-11 | 詹森药业有限公司 | 作为NIK抑制剂的新型3-(1H-吡唑-4-基)-1H-吡咯并[2,3-c]吡啶衍生物 |
| CN105579451A (zh) * | 2013-09-26 | 2016-05-11 | 詹森药业有限公司 | 作为NIK抑制剂的新型1-(4-嘧啶基)-1H-吡咯并[3,2-c]吡啶衍生物 |
Family Cites Families (20)
| 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 |
| 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 |
| 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 |
| AR093580A1 (es) | 2013-08-30 | 2015-06-10 | Ptc Therapeutics Inc | Inhibidores bmi-1 de pirimidina sustituidos |
| 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
- 2017-06-29 ES ES17733469T patent/ES2837157T3/es active Active
- 2017-06-29 KR KR1020197002912A patent/KR102587619B1/ko active Active
- 2017-06-29 EP EP17733469.5A patent/EP3478673B1/en active Active
- 2017-06-29 US US16/309,080 patent/US20190119299A1/en not_active Abandoned
- 2017-06-29 CN CN201780053613.3A patent/CN109689645B/zh active Active
- 2017-06-29 WO PCT/EP2017/066125 patent/WO2018002219A1/en not_active Ceased
- 2017-06-29 AU AU2017289317A patent/AU2017289317B2/en not_active Ceased
- 2017-06-29 JP JP2018562323A patent/JP6936814B2/ja active Active
-
2020
- 2020-02-06 US US16/783,810 patent/US11186589B2/en active Active
Patent Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002079197A1 (en) * | 2001-03-29 | 2002-10-10 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| 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 |
| CN101039919A (zh) * | 2004-10-13 | 2007-09-19 | 惠氏公司 | 经n-苯磺酰基取代的苯胺基嘧啶类似物 |
| 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 |
| CN105143223A (zh) * | 2013-04-24 | 2015-12-09 | 詹森药业有限公司 | 3-(2-氨基嘧啶-4-基)-5-(3-羟丙炔基)-1h-吡咯并[2,3-c]吡啶衍生物作为nik抑制剂用于治疗癌症 |
| CN105579452A (zh) * | 2013-09-26 | 2016-05-11 | 詹森药业有限公司 | 作为NIK抑制剂的新型3-(1H-吡唑-4-基)-1H-吡咯并[2,3-c]吡啶衍生物 |
| CN105579451A (zh) * | 2013-09-26 | 2016-05-11 | 詹森药业有限公司 | 作为NIK抑制剂的新型1-(4-嘧啶基)-1H-吡咯并[3,2-c]吡啶衍生物 |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2018002219A1 (en) | 2018-01-04 |
| EP3478673A1 (en) | 2019-05-08 |
| CA3027418A1 (en) | 2018-01-04 |
| EP3478673B1 (en) | 2020-09-16 |
| US20210032267A1 (en) | 2021-02-04 |
| ES2837157T3 (es) | 2021-06-29 |
| AU2017289317A1 (en) | 2019-01-17 |
| US11186589B2 (en) | 2021-11-30 |
| KR102587619B1 (ko) | 2023-10-11 |
| JP2019524646A (ja) | 2019-09-05 |
| AU2017289317B2 (en) | 2021-04-01 |
| US20190119299A1 (en) | 2019-04-25 |
| CN109689645A (zh) | 2019-04-26 |
| JP6936814B2 (ja) | 2021-09-22 |
| KR20190025949A (ko) | 2019-03-12 |
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| GR01 | Patent grant |