JP2024535380A - Egfr阻害剤の多形形態 - Google Patents
Egfr阻害剤の多形形態 Download PDFInfo
- Publication number
- JP2024535380A JP2024535380A JP2024518581A JP2024518581A JP2024535380A JP 2024535380 A JP2024535380 A JP 2024535380A JP 2024518581 A JP2024518581 A JP 2024518581A JP 2024518581 A JP2024518581 A JP 2024518581A JP 2024535380 A JP2024535380 A JP 2024535380A
- Authority
- JP
- Japan
- Prior art keywords
- compound
- polymorph
- cancer
- suspension
- equilibration
- 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.)
- Pending
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Classifications
-
- 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
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163247774P | 2021-09-23 | 2021-09-23 | |
| US63/247,774 | 2021-09-23 | ||
| PCT/US2022/044475 WO2023049312A1 (en) | 2021-09-23 | 2022-09-23 | Egfr inhibitor polymorph forms |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2024535380A true JP2024535380A (ja) | 2024-09-30 |
| JP2024535380A5 JP2024535380A5 (https=) | 2025-09-29 |
Family
ID=85721153
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024518581A Pending JP2024535380A (ja) | 2021-09-23 | 2022-09-23 | Egfr阻害剤の多形形態 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US12545686B2 (https=) |
| EP (1) | EP4405360A4 (https=) |
| JP (1) | JP2024535380A (https=) |
| KR (1) | KR20250005041A (https=) |
| CN (1) | CN119343350A (https=) |
| AU (1) | AU2022350669A1 (https=) |
| CA (1) | CA3233057A1 (https=) |
| IL (1) | IL311616A (https=) |
| MX (1) | MX2024003495A (https=) |
| WO (1) | WO2023049312A1 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102809395B1 (ko) * | 2019-03-15 | 2025-05-16 | 더 리전트 오브 더 유니버시티 오브 캘리포니아 | 암을 치료하기 위한 조성물 및 방법 |
| EP4405360A4 (en) | 2021-09-23 | 2025-08-20 | Erasca Inc | POLYMORPHIC FORMS OF EGFR INHIBITOR |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ras相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ras抑制劑 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Family Cites Families (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5538325A (en) | 1978-09-11 | 1980-03-17 | Sankyo Co Ltd | 4-anilinoquinazoline derivative and its preparation |
| GB9323290D0 (en) | 1992-12-10 | 1994-01-05 | Zeneca Ltd | Quinazoline derivatives |
| GB9510757D0 (en) | 1994-09-19 | 1995-07-19 | Wellcome Found | Therapeuticaly active compounds |
| DE69536015D1 (de) | 1995-03-30 | 2009-12-10 | Pfizer Prod Inc | Chinazolinone Derivate |
| US5747498A (en) | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
| GB9514265D0 (en) | 1995-07-13 | 1995-09-13 | Wellcome Found | Hetrocyclic compounds |
| CA2258548C (en) | 1996-06-24 | 2005-07-26 | Pfizer Inc. | Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases |
| US6706721B1 (en) | 1998-04-29 | 2004-03-16 | Osi Pharmaceuticals, Inc. | N-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine mesylate anhydrate and monohydrate |
| KR100397792B1 (ko) | 2001-06-28 | 2003-09-13 | 한국과학기술연구원 | 4-(페닐아미노)-[1,4]디옥사노[2,3-g]퀴나졸린 유도체 및그의 제조방법 |
| EP1491211A4 (en) | 2002-03-29 | 2010-01-13 | Astellas Pharma Inc | DRUG AGAINST GLIOBLASTOMA |
| CN101219992B (zh) * | 2003-02-12 | 2011-08-31 | 日产化学工业株式会社 | 匹伐他汀钙的晶形 |
| EP1687308B1 (en) * | 2003-11-17 | 2019-06-12 | Merck & Cie | Process for preparating (6R)-L-erythrotetrahydrobiopterin hydrochloride crystalline form B from other crystalline forms |
| CN1854130B (zh) | 2005-04-15 | 2011-04-20 | 中国医学科学院药物研究所 | 喹唑啉衍生物、及其制法和药物组合物与用途 |
| EP1960552A2 (en) | 2005-12-16 | 2008-08-27 | Genentech, Inc. | Method for diagnosing, prognosing and treating glioma |
| JP2010501572A (ja) | 2006-08-22 | 2010-01-21 | コンサート ファーマシューティカルズ インコーポレイテッド | 4−アミノキナゾリン誘導体およびその使用方法 |
| WO2008046242A1 (fr) | 2006-10-16 | 2008-04-24 | Institute Of Mataria Medica, Chinese Academy Of Medical Sciences | Nouveaux dérivés quinazolines, leurs procédés de préparation et leurs utilisations |
| JP2008308491A (ja) | 2007-05-11 | 2008-12-25 | Gunma Univ | がん治療用の遊走阻害剤 |
| TW201019961A (en) | 2008-10-17 | 2010-06-01 | Genentech Inc | Combination therapy |
| WO2011035540A1 (zh) | 2009-09-28 | 2011-03-31 | 齐鲁制药有限公司 | 作为酪氨酸激酶抑制剂的4-(取代苯胺基)喹唑啉衍生物 |
| EA021439B1 (ru) | 2009-11-03 | 2015-06-30 | ГЛЭКСОСМИТКЛАЙН ЭлЭлСи | Хиназолиновые соединения |
| BRPI1003128A2 (pt) | 2010-08-06 | 2012-04-10 | Unicamp | processo de sìntese dos compostos meta e para-4-arilaminoquinazolìnicos para inibição da atividade tirosina-quinase do fator de crescimento epidérmico (egfrk) |
| ITPD20110091A1 (it) | 2011-03-24 | 2012-09-25 | Univ Padova | Inibitori multitirosinchinasi utili per le patologie correlate: modelli farmacoforici, composti identificati tramite questi modelli, metodi per la loro preparazione, la loro formulazione e il loro impiego terapeutico. |
| WO2013013614A1 (zh) | 2011-07-28 | 2013-01-31 | 南京英派药业有限公司 | 4-(3-杂芳基芳基氨基)喹唑啉和1-(3-杂芳基芳基氨基)异喹啉作为Hedgehog通路抑制剂及其应用 |
| CN103965211A (zh) | 2013-02-02 | 2014-08-06 | 江苏奥赛康药业股份有限公司 | 含喹唑啉结构的三环类衍生物及其制备方法和用途 |
| CN103965213A (zh) | 2013-02-02 | 2014-08-06 | 江苏奥赛康药业股份有限公司 | 7,8-二氢-6H-[1,4]噁嗪[3,2-g]喹唑啉类衍生物及其制备方法和用途 |
| CN103965212A (zh) | 2013-02-02 | 2014-08-06 | 江苏奥赛康药业股份有限公司 | 6,7,8,9-四氢-[1,4]氧氮杂卓[3,2-g]喹唑啉类衍生物及其制备方法和用途 |
| MX367772B (es) | 2013-04-04 | 2019-09-05 | Janssen Pharmaceutica Nv | Derivados de n-(2,3-dihidro-1h-pirrolo[2,3,b]piridin-5-il)-4-quina zolinamina y n-(2,3-dihidro-1h-indol-5-il)-4-quinazolinamina novedosos como inhibidores de perk. |
| NZ732511A (en) * | 2014-12-15 | 2018-11-30 | Univ Michigan Regents | Small molecule inhibitors of egfr and pi3k |
| CA2974442A1 (en) | 2015-02-03 | 2016-08-11 | Trillium Therapeutics Inc. | Novel fluorinated derivatives as egfr inhibitors useful for treating cancers |
| HUE054065T2 (hu) | 2015-08-04 | 2021-08-30 | Dc Europa Ltd | Szerek glióma kezelésében történõ alkalmazásra |
| CN105017163A (zh) | 2015-08-25 | 2015-11-04 | 佛山市赛维斯医药科技有限公司 | 双乙氧基苯并喹唑啉类酪氨酸激酶抑制剂、制备方法及其用途 |
| AU2017204973A1 (en) | 2016-01-06 | 2018-07-12 | Trillium Therapeutics Inc. | Novel fluorinated quinazoline derivatives as EGFR inhibitors |
| CN106432202B (zh) | 2016-09-22 | 2019-04-02 | 郑州大学第一附属医院 | 喹唑啉类衍生物及其应用 |
| CN111868039A (zh) * | 2017-09-26 | 2020-10-30 | 加利福尼亚大学董事会 | 用于治疗癌症的组合物和方法 |
| KR102809395B1 (ko) | 2019-03-15 | 2025-05-16 | 더 리전트 오브 더 유니버시티 오브 캘리포니아 | 암을 치료하기 위한 조성물 및 방법 |
| US20240058340A1 (en) | 2020-09-21 | 2024-02-22 | The Regents Of The University Of California | Compositions and methods for treating cancer |
| WO2022061201A1 (en) | 2020-09-21 | 2022-03-24 | The Regents Of The University Of California | Compositions and methods for treating cancer |
| WO2022061299A1 (en) | 2020-09-21 | 2022-03-24 | The Regents Of The University Of California | Non-invasive functional companion assays for oncogene targeted therapy for brain cancer |
| EP4405360A4 (en) | 2021-09-23 | 2025-08-20 | Erasca Inc | POLYMORPHIC FORMS OF EGFR INHIBITOR |
| WO2023244639A1 (en) | 2022-06-14 | 2023-12-21 | The Regents Of The University Of California | Methods of predicting cns cancer response to treatment with egfr inhibitors |
| WO2024081447A1 (en) | 2022-10-14 | 2024-04-18 | The Regents Of The University Of California | Egfr inhibitors for treating lung cancer |
| WO2024102177A1 (en) | 2022-11-08 | 2024-05-16 | The Regents Of The University Of California | Combination therapies for the treatment of brain cancer |
-
2022
- 2022-09-23 EP EP22873607.0A patent/EP4405360A4/en active Pending
- 2022-09-23 IL IL311616A patent/IL311616A/en unknown
- 2022-09-23 KR KR1020247013445A patent/KR20250005041A/ko active Pending
- 2022-09-23 CA CA3233057A patent/CA3233057A1/en active Pending
- 2022-09-23 WO PCT/US2022/044475 patent/WO2023049312A1/en not_active Ceased
- 2022-09-23 CN CN202280077001.9A patent/CN119343350A/zh active Pending
- 2022-09-23 AU AU2022350669A patent/AU2022350669A1/en active Pending
- 2022-09-23 JP JP2024518581A patent/JP2024535380A/ja active Pending
-
2024
- 2024-03-20 MX MX2024003495A patent/MX2024003495A/es unknown
- 2024-03-22 US US18/614,458 patent/US12545686B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US12545686B2 (en) | 2026-02-10 |
| CN119343350A (zh) | 2025-01-21 |
| AU2022350669A1 (en) | 2024-04-04 |
| EP4405360A1 (en) | 2024-07-31 |
| CA3233057A1 (en) | 2023-03-30 |
| EP4405360A4 (en) | 2025-08-20 |
| IL311616A (en) | 2024-05-01 |
| MX2024003495A (es) | 2025-01-09 |
| US20240287088A1 (en) | 2024-08-29 |
| WO2023049312A1 (en) | 2023-03-30 |
| KR20250005041A (ko) | 2025-01-09 |
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