ES2805976T3 - Derivados heteroaromáticos en calidad de inhibidores de NIK - Google Patents
Derivados heteroaromáticos en calidad de inhibidores de NIK Download PDFInfo
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- ES2805976T3 ES2805976T3 ES17739902T ES17739902T ES2805976T3 ES 2805976 T3 ES2805976 T3 ES 2805976T3 ES 17739902 T ES17739902 T ES 17739902T ES 17739902 T ES17739902 T ES 17739902T ES 2805976 T3 ES2805976 T3 ES 2805976T3
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- alkyl
- substituted
- cycloalkyl
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- 125000001072 heteroaryl group Chemical group 0.000 title claims abstract description 95
- 239000003112 inhibitor Substances 0.000 title description 13
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 772
- 125000001424 substituent group Chemical group 0.000 claims abstract description 262
- 150000001875 compounds Chemical class 0.000 claims abstract description 256
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract description 197
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- 125000005843 halogen group Chemical group 0.000 claims abstract description 161
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- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims abstract description 109
- 239000001257 hydrogen Substances 0.000 claims abstract description 109
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- 229910052757 nitrogen Inorganic materials 0.000 claims abstract description 91
- 125000005842 heteroatom Chemical group 0.000 claims abstract description 75
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- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims abstract description 43
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract description 41
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Classifications
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
- 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
- C07D405/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
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- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
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| EP16177104 | 2016-06-30 | ||
| PCT/EP2017/066120 WO2018002217A1 (en) | 2016-06-30 | 2017-06-29 | Heteroaromatic derivatives as nik inhibitors |
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| AU (1) | AU2017289315B2 (enExample) |
| CA (1) | CA3027416A1 (enExample) |
| ES (1) | ES2805976T3 (enExample) |
| WO (1) | WO2018002217A1 (enExample) |
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| HUE047684T2 (hu) | 2016-01-22 | 2020-05-28 | Janssen Pharmaceutica Nv | Új szubsztituált cianoindolin származékok mint NIK inhibitorok |
| US11001569B2 (en) | 2016-01-22 | 2021-05-11 | Janssen Pharmaceutica Nv | 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors |
| WO2018002219A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Cyanoindoline derivatives as nik inhibitors |
| KR102517352B1 (ko) | 2016-06-30 | 2023-03-31 | 잔센파마슈티카엔.브이. | Nik 억제제로서의 헤테로방향족 유도체 |
| KR102797697B1 (ko) | 2018-05-25 | 2025-04-22 | 에이2에이 파마수티칼스, 잉크. | 신종 항암제 후보로서, 매우 강력한 tacc3 억제제 |
| KR101954370B1 (ko) * | 2018-07-25 | 2019-03-05 | 한미약품 주식회사 | 피리미딘 화합물 및 이를 포함하는 암의 예방 또는 치료용 약학 조성물 |
| WO2020171646A1 (ko) | 2019-02-22 | 2020-08-27 | 한미약품 주식회사 | Flt3 저해제 및 저메틸화제를 포함하는 급성 골수성 백혈병의 치료를 위한 약학적 조성물 |
| ES2989387T3 (es) | 2019-05-31 | 2024-11-26 | Janssen Pharmaceutica Nv | Pequeñas moléculas inhibidoras de la quinasa inductora de nf-kb |
| CN113993859B (zh) * | 2019-06-25 | 2024-07-02 | 益方生物科技(上海)股份有限公司 | 杂环化合物、其制备方法及其使用方法 |
| CA3145391A1 (en) | 2019-06-27 | 2020-12-30 | Hanmi Pharm. Co., Ltd. | Pharmaceutical composition for treating acute myeloid leukemia, containing flt3 inhibitor and chemotherapeutic agents |
| WO2022221194A1 (en) * | 2021-04-12 | 2022-10-20 | A2A Pharmaceuticals, Inc. | Compositions and methods for treating cancer |
| EP4499625A4 (en) | 2022-03-24 | 2026-03-18 | A2A Pharmaceuticals Inc | CANCER COMPOSITIONS AND TREATMENT METHODS |
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| HUP0301117A3 (en) | 2000-02-17 | 2004-01-28 | Amgen Inc Thousand Oaks | Imidazole derivatives kinase inhibitors, their use, process for their preparation and pharmaceutical compositions containing them |
| ES2254385T3 (es) | 2000-02-29 | 2006-06-16 | Millennium Pharmaceuticals, Inc. | Benzamidas e inhibidores relacionados del factor xa. |
| ES2292753T4 (es) | 2001-03-29 | 2009-02-16 | Vertex Pharmaceuticals Incorporated | Inhibidores de quinasas n-terminales c-jun (jnk) y otras proteina quinasas. |
| WO2002102313A2 (en) | 2001-06-19 | 2002-12-27 | Bristol-Myers Squibb Company | Pyrimidine inhibitors of phosphodiesterase (pde) 7 |
| 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 |
| US20110086834A1 (en) * | 2008-06-26 | 2011-04-14 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| NZ603525A (en) | 2008-06-27 | 2015-02-27 | Celgene Avilomics Res Inc | Pyrimidine based compound and uses thereof |
| US20110183975A1 (en) * | 2008-10-07 | 2011-07-28 | Yasuhiro Goto | Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity |
| NZ598262A (en) | 2009-08-17 | 2014-05-30 | Sloan Kettering Inst Cancer | Heat shock protein binding compounds, compositions, and methods for making and using same |
| WO2011153553A2 (en) | 2010-06-04 | 2011-12-08 | The Regents Of The University Of California | Methods and compositions for kinase inhibition |
| KR101764952B1 (ko) | 2010-07-29 | 2017-08-03 | 리겔 파마슈티칼스, 인크. | Ａｍｐｋ-활성화 헤테로시클릭 화합물 및 그의 사용 방법 |
| BR112013026202A2 (pt) | 2011-04-12 | 2017-07-25 | Myrexis Inc | composições e usos terapêuticos de inibidores quinase epsilon relacionado a ikk e quinase i de ligação a tank |
| TWI663166B (zh) | 2013-04-24 | 2019-06-21 | 健生藥品公司 | 新化合物 |
| KR102232595B1 (ko) | 2013-08-30 | 2021-03-26 | 피티씨 테라퓨틱스, 인크. | 치환된 피리미딘 bmi-1 저해제 |
| 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 |
| RU2016141934A (ru) | 2014-04-04 | 2018-05-07 | Сирос Фармасьютикалз, Инк. | Ингибиторы циклин-зависимой киназы 7 (cdk7) |
| WO2015176135A1 (en) | 2014-05-22 | 2015-11-26 | The University Of Sydney | Omega-3 analogues |
| 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 |
| HUE047684T2 (hu) | 2016-01-22 | 2020-05-28 | Janssen Pharmaceutica Nv | Új szubsztituált cianoindolin származékok mint NIK inhibitorok |
| US11001569B2 (en) | 2016-01-22 | 2021-05-11 | Janssen Pharmaceutica Nv | 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors |
| EP3429591B1 (en) | 2016-03-16 | 2023-03-15 | Kura Oncology, Inc. | Substituted thieno[2,3-d]pyrimidine derivatives as inhibitors of menin-mll and methods of use |
| KR102517352B1 (ko) | 2016-06-30 | 2023-03-31 | 잔센파마슈티카엔.브이. | Nik 억제제로서의 헤테로방향족 유도체 |
| WO2018002219A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Cyanoindoline derivatives as nik inhibitors |
-
2017
- 2017-06-29 KR KR1020197002588A patent/KR102517352B1/ko active Active
- 2017-06-29 EP EP17739902.9A patent/EP3478675B1/en active Active
- 2017-06-29 CN CN201780053583.6A patent/CN109641882B/zh active Active
- 2017-06-29 ES ES17739902T patent/ES2805976T3/es active Active
- 2017-06-29 AU AU2017289315A patent/AU2017289315B2/en not_active Ceased
- 2017-06-29 WO PCT/EP2017/066120 patent/WO2018002217A1/en not_active Ceased
- 2017-06-29 CA CA3027416A patent/CA3027416A1/en active Pending
- 2017-06-29 JP JP2018562331A patent/JP6936815B2/ja active Active
- 2017-06-29 US US16/309,059 patent/US11136311B2/en active Active
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| AU2017289315A1 (en) | 2019-01-24 |
| AU2017289315B2 (en) | 2021-04-01 |
| EP3478675B1 (en) | 2020-04-22 |
| WO2018002217A1 (en) | 2018-01-04 |
| KR102517352B1 (ko) | 2023-03-31 |
| CA3027416A1 (en) | 2018-01-04 |
| US20190359598A1 (en) | 2019-11-28 |
| CN109641882B (zh) | 2022-10-28 |
| CN109641882A (zh) | 2019-04-16 |
| KR20190025644A (ko) | 2019-03-11 |
| JP2019521097A (ja) | 2019-07-25 |
| JP6936815B2 (ja) | 2021-09-22 |
| US11136311B2 (en) | 2021-10-05 |
| EP3478675A1 (en) | 2019-05-08 |
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