JP6468611B2 - キナーゼ阻害のためのヘテロアリール化合物 - Google Patents
キナーゼ阻害のためのヘテロアリール化合物 Download PDFInfo
- Publication number
- JP6468611B2 JP6468611B2 JP2016567502A JP2016567502A JP6468611B2 JP 6468611 B2 JP6468611 B2 JP 6468611B2 JP 2016567502 A JP2016567502 A JP 2016567502A JP 2016567502 A JP2016567502 A JP 2016567502A JP 6468611 B2 JP6468611 B2 JP 6468611B2
- Authority
- JP
- Japan
- Prior art keywords
- amino
- alkyl
- methyl
- compound
- dihydro
- 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.)
- Expired - Fee Related
Links
Classifications
-
- 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
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
-
- 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
- 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
- C07D471/06—Peri-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
- C07D487/06—Peri-condensed systems
-
- 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
- C07D498/06—Peri-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (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 |
|---|---|---|---|
| US201461992742P | 2014-05-13 | 2014-05-13 | |
| US61/992,742 | 2014-05-13 | ||
| PCT/US2015/030522 WO2015175632A1 (en) | 2014-05-13 | 2015-05-13 | Heteroaryl compounds for kinase inhibition |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017518282A JP2017518282A (ja) | 2017-07-06 |
| JP2017518282A5 JP2017518282A5 (enExample) | 2018-06-21 |
| JP6468611B2 true JP6468611B2 (ja) | 2019-02-13 |
Family
ID=54480594
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016567502A Expired - Fee Related JP6468611B2 (ja) | 2014-05-13 | 2015-05-13 | キナーゼ阻害のためのヘテロアリール化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20170166598A1 (enExample) |
| EP (1) | EP3143015B1 (enExample) |
| JP (1) | JP6468611B2 (enExample) |
| CN (1) | CN106687457B (enExample) |
| WO (1) | WO2015175632A1 (enExample) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103501612B (zh) | 2011-05-04 | 2017-03-29 | 阿里亚德医药股份有限公司 | 抑制表皮生长因子受体导致的癌症中细胞增殖的化合物 |
| JP6469567B2 (ja) | 2012-05-05 | 2019-02-13 | アリアド・ファーマシューティカルズ・インコーポレイテッド | Egfr発動性がんの細胞増殖阻害用化合物 |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| AP2017009690A0 (en) * | 2014-06-19 | 2017-01-31 | Ariad Pharma Inc | Heteroaryl compounds for kinase inhibition |
| WO2016054987A1 (zh) | 2014-10-11 | 2016-04-14 | 上海翰森生物医药科技有限公司 | Egfr抑制剂及其制备和应用 |
| CN105085489B (zh) | 2014-11-05 | 2019-03-01 | 益方生物科技(上海)有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| CA2984586C (en) * | 2015-04-29 | 2021-02-16 | Guangdong Zhongsheng Pharmaceutical Co., Ltd. | Fused-ring or tricyclic aryl pyrimidine compound used as kinase inhibitor |
| JP6863901B2 (ja) * | 2015-05-13 | 2021-04-28 | アリアド ファーマシューティカルズ, インコーポレイテッド | キナーゼ阻害のためのヘテロアリール化合物 |
| CN106810553B (zh) * | 2015-11-30 | 2020-03-17 | 江苏正大丰海制药有限公司 | 3-(4,5-取代氨基嘧啶)苯基衍生物及其应用 |
| JP2019501222A (ja) | 2016-01-07 | 2019-01-17 | シーエス ファーマテック リミテッド | Egfrチロシンキナーゼの臨床的に重要な変異体の選択的阻害薬 |
| CN107344934B (zh) * | 2016-05-04 | 2019-08-23 | 江苏正大丰海制药有限公司 | 药物活性物质的固体形式 |
| JP6746794B2 (ja) * | 2016-09-19 | 2020-08-26 | 南京創特医薬科技有限公司Nanjing Chuangte Pharmaceutical Technology Co., Ltd | 重水素化3−(4,5−置換アミノピリミジン)フェニル誘導体及びその使用 |
| JOP20190073A1 (ar) | 2016-10-31 | 2019-04-07 | Taiho Pharmaceutical Co Ltd | مثبط انتقائي لمستقبل عامل نمو بشروي (egfr) لطافر إدخال exon 20 |
| CN110753693A (zh) | 2016-12-23 | 2020-02-04 | 阿尔维纳斯运营股份有限公司 | Egfr蛋白水解靶向嵌合分子和相关使用方法 |
| AR111469A1 (es) | 2017-04-21 | 2019-07-17 | Yuhan Corp | Sal de un compuesto del derivado de aminopiridina, una forma cristalina de la misma, y un proceso para preparar la misma |
| MD3658552T2 (ro) | 2017-07-28 | 2024-02-29 | Yuhan Corp | Procedeu de obținere a N-(5-((4-(4-((dimetilamino)metil)-3-fenil-1H-pirazol-1-il)pirimidin-2-il)amino)-4-metoxi-2-morfolinofenil)acrilamidei prin prin reacţia aminei corespunzătoare cu clorură de 3-halo-propionil |
| FI3677266T3 (fi) | 2017-09-01 | 2024-03-22 | Taiho Pharmaceutical Co Ltd | Eksoni 18- ja/tai eksoni 21 -egfr-mutantille selektiivinen inhibiittori |
| EP3613738A1 (en) * | 2018-08-23 | 2020-02-26 | Lead Discovery Center GmbH | 4-substituted pyrrolo[2,3-b]pyridine as erbb modulators useful for treating cancer |
| FI3902548T3 (fi) | 2018-12-28 | 2025-07-17 | Taiho Pharmaceutical Co Ltd | Hoitoresistentin L718- ja/tai L792-mutaation omaavan EGFR:n inhibiittori käytettäväksi syövän hoitamisessa |
| US12157730B2 (en) | 2019-03-19 | 2024-12-03 | Voronoi Inc. | Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component |
| MA55380A (fr) | 2019-03-19 | 2022-01-26 | B2Sbio Inc | Dérivé hétéroaryle, son procédé de production et composition pharmaceutique le comprenant en tant que constituant efficace |
| CN117986251A (zh) * | 2019-04-24 | 2024-05-07 | 拜耳股份有限公司 | 4H-吡咯并[3,2-c]吡啶-4-酮化合物 |
| US12433597B2 (en) * | 2019-06-04 | 2025-10-07 | Trisalus Life Sciences, Inc. | Atraumatic occlusive system with compartment for measurement of vascular pressure change |
| JP7724210B2 (ja) | 2019-09-13 | 2025-08-15 | ホリスティック・メディカル | 医療用インプラント、送達装置、医療用インプラントを製造する方法、および医療用インプラントを送達する方法 |
| CN110746307B (zh) * | 2019-11-01 | 2021-07-06 | 韶远科技(上海)有限公司 | 一种1-硝基-2-乙基-4-氟苯的制备方法 |
| US20210161897A1 (en) | 2019-11-12 | 2021-06-03 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| MX2022005708A (es) * | 2019-11-14 | 2022-06-08 | Amgen Inc | Sintesis mejorada del compuesto inhibidor de g12c de kras. |
| JP2023510426A (ja) | 2020-01-20 | 2023-03-13 | アストラゼネカ・アクチエボラーグ | 癌を治療するための上皮細胞増殖因子受容体チロシンキナーゼ阻害剤 |
| JP7626773B2 (ja) | 2020-02-03 | 2025-02-04 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | HER2阻害薬としての[1,3]ジアジノ[5,4-d]ピリミジン |
| EP4100412A1 (en) * | 2020-02-03 | 2022-12-14 | Boehringer Ingelheim International GmbH | [1,3]diazino[5,4-d]pyrimidines as her2 inhibitors |
| US11608343B2 (en) * | 2020-04-24 | 2023-03-21 | Boehringer Ingelheim International Gmbh | Substituted pyrimido[5,4-d]pyrimidines as HER2 inhibitors |
| US20210369709A1 (en) | 2020-05-27 | 2021-12-02 | Astrazeneca Ab | EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER |
| MX2023003362A (es) | 2020-09-23 | 2023-05-30 | Scorpion Therapeutics Inc | Derivados de pirrolo[3,2-c]piridin-4-ona utiles en el tratamiento del cancer. |
| TW202229282A (zh) | 2020-09-30 | 2022-08-01 | 美商史考皮恩治療有限公司 | 治療癌症之方法 |
| WO2022072632A1 (en) | 2020-09-30 | 2022-04-07 | Scorpion Therapeutics, Inc. | Bicyclic compounds for use in the treatment cancer |
| WO2022072645A2 (en) | 2020-09-30 | 2022-04-07 | Scorpion Therapeutics, Inc. | Methods for treating cancer |
| WO2022076831A2 (en) | 2020-10-09 | 2022-04-14 | Scorpion Therapeutics, Inc. | Methods for treating cancer |
| WO2022094271A1 (en) | 2020-10-30 | 2022-05-05 | Scorpion Therapeutics, Inc. | Methods for treating cancer |
| WO2022098992A1 (en) | 2020-11-05 | 2022-05-12 | Scorpion Therapeutics, Inc. | Use of macrocyclic compounds in methods of treating cancer |
| WO2022197913A1 (en) | 2021-03-18 | 2022-09-22 | Scorpion Therapeutics, Inc. | Bicyclic derivatives which can be used to treat cancer |
| BR112023021111A2 (pt) | 2021-04-13 | 2023-12-19 | Nuvalent Inc | Composto, composição farmacêutica, método de tratamento de câncer, método para inibir seletivamente her2, método de regulação de um nível de her2, método para aumentar um nível de her2, método de diminuição da fosforilação de her2 |
| WO2023173083A1 (en) | 2022-03-11 | 2023-09-14 | Scorpion Therapeutics, Inc. | Tetrahydroindole derivatives as egfr and/or her2 inhibtors useful for the treatment of cancer |
| WO2023187037A1 (en) | 2022-03-31 | 2023-10-05 | Astrazeneca Ab | Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer |
| CN114957224B (zh) * | 2022-05-17 | 2024-03-19 | 浙大城市学院 | 一种肿瘤低氧靶向的egfr抑制剂及其应用 |
| IL317733A (en) | 2022-06-27 | 2025-02-01 | Astrazeneca Ab | Combinations involving epidermal growth factor receptor tyrosine kinase inhibitors for cancer treatment |
| CA3261476A1 (en) | 2022-07-08 | 2024-01-11 | Astrazeneca Ab | Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Combination with HGF Receptor Inhibitors for the Treatment of Cancer |
| CN120359211A (zh) * | 2022-12-08 | 2025-07-22 | 盐野义制药株式会社 | 具有血清素受体结合活性的含氮杂环和碳环衍生物 |
| WO2024254266A1 (en) | 2023-06-08 | 2024-12-12 | Scorpion Therapeutics, Inc. | A 1,5-dihydro-4h-pyrrolo[3,2-c] pyridin-4-one for use in the treatment of cancer |
| WO2024254298A1 (en) | 2023-06-08 | 2024-12-12 | Scorpion Therapeutics, Inc. | A 1,5-dihydro-4h-pyrrolo[3,2-c] pyridin-4-one for use in the treatment of cancer |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0311274D0 (en) * | 2003-05-16 | 2003-06-18 | Astrazeneca Ab | Chemical compounds |
| EP1948180B1 (en) * | 2005-11-11 | 2013-03-13 | Boehringer Ingelheim International GmbH | Combination treatment of cancer comprising egfr/her2 inhibitors |
| CA3006428A1 (en) * | 2007-06-08 | 2008-12-18 | Genentech, Inc. | Gene expression markers of tumor resistance to her2 inhibitor treatment |
| US8450335B2 (en) * | 2008-06-27 | 2013-05-28 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| 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 |
| JP5918693B2 (ja) * | 2009-05-05 | 2016-05-18 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Egfr阻害剤及び疾患の治療方法 |
| WO2011082266A2 (en) * | 2009-12-30 | 2011-07-07 | Arqule, Inc. | Substituted heterocyclic compounds |
| ME02887B (me) * | 2011-07-27 | 2018-04-20 | Astrazeneca Ab | 2-(2,4,5-supstituisani-anilino) pirimidinski derivati kao egfr modulatori korisni za tretman raka |
-
2015
- 2015-05-13 JP JP2016567502A patent/JP6468611B2/ja not_active Expired - Fee Related
- 2015-05-13 US US15/310,349 patent/US20170166598A1/en not_active Abandoned
- 2015-05-13 CN CN201580037958.0A patent/CN106687457B/zh not_active Expired - Fee Related
- 2015-05-13 EP EP15792086.9A patent/EP3143015B1/en active Active
- 2015-05-13 WO PCT/US2015/030522 patent/WO2015175632A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| EP3143015A4 (en) | 2017-11-01 |
| EP3143015B1 (en) | 2019-02-20 |
| CN106687457A (zh) | 2017-05-17 |
| WO2015175632A1 (en) | 2015-11-19 |
| EP3143015A1 (en) | 2017-03-22 |
| CN106687457B (zh) | 2020-01-10 |
| US20170166598A1 (en) | 2017-06-15 |
| JP2017518282A (ja) | 2017-07-06 |
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