JP7805363B2 - EGFR阻害薬としての置換1H-ピラゾロ[4,3-c]及び誘導体 - Google Patents
EGFR阻害薬としての置換1H-ピラゾロ[4,3-c]及び誘導体Info
- Publication number
- JP7805363B2 JP7805363B2 JP2023526609A JP2023526609A JP7805363B2 JP 7805363 B2 JP7805363 B2 JP 7805363B2 JP 2023526609 A JP2023526609 A JP 2023526609A JP 2023526609 A JP2023526609 A JP 2023526609A JP 7805363 B2 JP7805363 B2 JP 7805363B2
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- membered heterocyclyl
- cycloalkyl
- haloalkyl
- 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.)
- Active
Links
Classifications
-
- 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
- A61K31/435—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/4995—Pyrazines or piperazines forming part of bridged 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
-
- 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
- A61K31/495—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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- 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
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP20205297.3 | 2020-11-02 | ||
| EP20205297 | 2020-11-02 | ||
| PCT/EP2021/080151 WO2022090481A1 (en) | 2020-11-02 | 2021-10-29 | Substituted 1h-pyrazolo[4,3-c]pyridines and derivatives as egfr inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023550591A JP2023550591A (ja) | 2023-12-04 |
| JP2023550591A5 JP2023550591A5 (enExample) | 2024-11-05 |
| JP7805363B2 true JP7805363B2 (ja) | 2026-01-23 |
Family
ID=73059474
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023526609A Active JP7805363B2 (ja) | 2020-11-02 | 2021-10-29 | EGFR阻害薬としての置換1H-ピラゾロ[4,3-c]及び誘導体 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US12064421B2 (enExample) |
| EP (1) | EP4237423B1 (enExample) |
| JP (1) | JP7805363B2 (enExample) |
| CN (1) | CN116507627B (enExample) |
| AR (1) | AR123977A1 (enExample) |
| TW (1) | TW202233637A (enExample) |
| WO (1) | WO2022090481A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW202309022A (zh) | 2021-04-13 | 2023-03-01 | 美商努法倫特公司 | 用於治療具egfr突變之癌症之胺基取代雜環 |
| WO2024181803A1 (ko) * | 2023-02-28 | 2024-09-06 | 보로노이 주식회사 | 헤테로아릴 유도체 및 이의 용도 |
| KR20240152239A (ko) * | 2023-04-11 | 2024-10-21 | 보로노이 주식회사 | 피라졸로피리딘 유도체 화합물 및 이의 용도 |
| CN117069746B (zh) * | 2023-08-17 | 2025-10-21 | 苏州共康医药科技有限公司 | 取代的吡唑并吡啶类化合物作为4代egfr抑制剂 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015521645A (ja) | 2012-06-27 | 2015-07-30 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | 5−アザインダゾール化合物及び使用方法 |
| WO2016133935A1 (en) | 2015-02-17 | 2016-08-25 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| JP2017524703A (ja) | 2014-07-25 | 2017-08-31 | シャンハイ ハイヤン ファーマシューティカル テクノロジー カンパニー リミテッドShanghai Haiyan Pharmaceutical Technology Co., Ltd. | 2,4−二置換7H−ピロロ[2,3−d]ピリミジン誘導体、その製造方法および医薬における使用 |
| WO2019162323A1 (en) | 2018-02-21 | 2019-08-29 | Boehringer Ingelheim International Gmbh | New benzimidazole compounds and derivatives as egfr inhibitors |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2003220970A1 (en) | 2002-03-01 | 2003-09-16 | Smithkline Beecham Corporation | Diamino-pyrimidines and their use as angiogenesis inhibitors |
| US20050154202A1 (en) | 2002-04-05 | 2005-07-14 | Hagmann William K. | Substituted aryl amides |
| NZ543482A (en) | 2003-05-21 | 2009-02-28 | Prosidion Ltd | Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phoshorylase |
| US7557211B2 (en) | 2004-11-12 | 2009-07-07 | Bristol-Myers Squibb Company | 8H-imidazo[4,5-D]thiazolo[4,5-B]pyridine based tricyclic compounds and pharmaceutical compositions comprising same |
| US7737279B2 (en) | 2005-05-10 | 2010-06-15 | Bristol-Myers Squibb Company | 1,6-dihydro-1,3,5,6-tetraaza-as-indacene based tricyclic compounds and pharmaceutical compositions comprising same |
| TW200803855A (en) | 2006-02-24 | 2008-01-16 | Kalypsys Inc | Quinolones useful as inducible nitric oxide synthase inhibitors |
| EP2114916A2 (en) | 2007-02-02 | 2009-11-11 | NeuroSearch A/S | Pyridinyl-pyrazole derivatives and their use as potassium channel modulators |
| US8865732B2 (en) | 2008-03-21 | 2014-10-21 | Novartis Ag | Heterocyclic compounds and uses thereof |
| TWI501967B (zh) | 2010-12-16 | 2015-10-01 | Janssen R&D Ireland | 作為呼吸道融合病毒抗病毒劑之氮雜吲哚類 |
| US9527925B2 (en) | 2011-04-01 | 2016-12-27 | Boehringer Ingelheim International Gmbh | Bispecific binding molecules binding to VEGF and ANG2 |
| WO2013056679A1 (en) | 2011-10-21 | 2013-04-25 | Beijing Hanmi Pharmaceutical Co., Ltd | Novel heteroaryl-amino derivatives |
| AR090151A1 (es) | 2012-03-07 | 2014-10-22 | Lilly Co Eli | Compuestos inhibidores de raf |
| JO3300B1 (ar) | 2012-06-06 | 2018-09-16 | Novartis Ag | مركبات وتركيبات لتعديل نشاط egfr |
| US20150152083A1 (en) | 2012-06-06 | 2015-06-04 | Irm Llc, A Delaware Limited Liability Company | Compounds and Compositions for Modulating EGFR Activity |
| RU2660429C2 (ru) | 2012-09-28 | 2018-07-06 | Мерк Шарп И Доум Корп. | Новые соединения, которые являются ингибиторами erk |
| WO2014081718A1 (en) | 2012-11-20 | 2014-05-30 | Genentech, Inc. | Aminopyrimidine compounds as inhibitors of t790m containing egfr mutants |
| US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| WO2014210354A1 (en) | 2013-06-28 | 2014-12-31 | Genentech, Inc. | Azaindazole compounds as inhibitors of t790m containing egfr mutants |
| CN105658639A (zh) | 2013-08-22 | 2016-06-08 | 豪夫迈·罗氏有限公司 | 炔基醇和应用方法 |
| CN104418858B (zh) | 2013-08-30 | 2018-12-11 | 浙江医药股份有限公司新昌制药厂 | 2,6-二含氮取代的嘌呤衍生物及其制备方法和其药物组合物与应用 |
| WO2015094929A1 (en) | 2013-12-18 | 2015-06-25 | Merck Sharp & Dohme Corp. | Erk inhibitors |
| LT3466955T (lt) | 2014-01-13 | 2021-02-25 | Aurigene Discovery Technologies Limited | Oksazol[4,5-b]piridino ir tiazol[4,5-b]piridino darinių, kaip irak4 inhibitorių, skirtų vėžio gydymui, gamybos būdas |
| JP6568926B2 (ja) | 2014-03-20 | 2019-08-28 | カペラ セラピューティクス,インコーポレーテッド | 癌の治療のためのerbbチロシンキナーゼ阻害剤としてのベンゾイミダゾール誘導体 |
| CA2943220C (en) | 2014-03-20 | 2024-01-16 | Capella Therapeutics, Inc. | Benzimidazole derivatives as erbb tyrosine kinase inhibitors for the treatment of cancer |
| CN108012529A (zh) | 2015-05-15 | 2018-05-08 | 诺华股份有限公司 | 治疗egfr突变的癌症的方法 |
| UA124090C2 (uk) | 2015-06-03 | 2021-07-21 | Прінсіпіа Байофарма Інк. | Інгібітори тирозинкінази |
| JP6845165B2 (ja) | 2015-06-30 | 2021-03-17 | デイナ ファーバー キャンサー インスティチュート,インコーポレイテッド | Egfr阻害剤およびその使用方法 |
| EP3347353B1 (en) | 2015-09-11 | 2019-07-17 | Boehringer Ingelheim International GmbH | Pyrazolyl-substituted heteroaryls and their use as medicaments |
| TWI726968B (zh) | 2016-01-07 | 2021-05-11 | 開曼群島商Cs醫藥技術公司 | Egfr酪胺酸激酶之臨床重要突變體之選擇性抑制劑 |
| EP3535258B1 (en) | 2016-11-03 | 2021-11-24 | Bristol-Myers Squibb Company | Substituted bicycle heterocyclic derivatives useful as romk channel inhibitors |
| US11198726B2 (en) | 2017-06-02 | 2021-12-14 | Boerhinger Ingelheim International Gmbh | Anti-cancer combination therapy |
| EP3717471B1 (en) | 2017-12-02 | 2022-01-05 | Galapagos NV | Novel compounds and pharmaceutical compositions thereof for the treatment of diseases |
| WO2020178316A1 (en) * | 2019-03-05 | 2020-09-10 | Aziende Chimiche Riunite Angelini Francesco - A.C.R.A.F. S.P.A. | 5- or 7-azaindazoles as beta-lactamase inhibitors |
-
2021
- 2021-10-29 US US17/514,145 patent/US12064421B2/en active Active
- 2021-10-29 JP JP2023526609A patent/JP7805363B2/ja active Active
- 2021-10-29 EP EP21799061.3A patent/EP4237423B1/en active Active
- 2021-10-29 WO PCT/EP2021/080151 patent/WO2022090481A1/en not_active Ceased
- 2021-10-29 CN CN202180073462.4A patent/CN116507627B/zh active Active
- 2021-11-01 AR ARP210103034A patent/AR123977A1/es not_active Application Discontinuation
- 2021-11-01 TW TW110140534A patent/TW202233637A/zh unknown
-
2024
- 2024-06-27 US US18/756,533 patent/US20240358688A1/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015521645A (ja) | 2012-06-27 | 2015-07-30 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | 5−アザインダゾール化合物及び使用方法 |
| JP2017524703A (ja) | 2014-07-25 | 2017-08-31 | シャンハイ ハイヤン ファーマシューティカル テクノロジー カンパニー リミテッドShanghai Haiyan Pharmaceutical Technology Co., Ltd. | 2,4−二置換7H−ピロロ[2,3−d]ピリミジン誘導体、その製造方法および医薬における使用 |
| WO2016133935A1 (en) | 2015-02-17 | 2016-08-25 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| WO2019162323A1 (en) | 2018-02-21 | 2019-08-29 | Boehringer Ingelheim International Gmbh | New benzimidazole compounds and derivatives as egfr inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2023550591A (ja) | 2023-12-04 |
| US20220133734A1 (en) | 2022-05-05 |
| EP4237423A1 (en) | 2023-09-06 |
| AR123977A1 (es) | 2023-02-01 |
| CN116507627B (zh) | 2026-01-23 |
| CN116507627A (zh) | 2023-07-28 |
| EP4237423B1 (en) | 2024-12-11 |
| US20240358688A1 (en) | 2024-10-31 |
| WO2022090481A1 (en) | 2022-05-05 |
| TW202233637A (zh) | 2022-09-01 |
| US12064421B2 (en) | 2024-08-20 |
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