CN110891573A - Ret抑制剂和mtorc1抑制剂的组合及其用于治疗由异常ret活性介导的癌症的用途 - Google Patents
Ret抑制剂和mtorc1抑制剂的组合及其用于治疗由异常ret活性介导的癌症的用途 Download PDFInfo
- Publication number
- CN110891573A CN110891573A CN201880046867.7A CN201880046867A CN110891573A CN 110891573 A CN110891573 A CN 110891573A CN 201880046867 A CN201880046867 A CN 201880046867A CN 110891573 A CN110891573 A CN 110891573A
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- China
- Prior art keywords
- cancer
- ret
- inhibitor
- leu
- ser
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- 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.)
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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
- A61K31/495—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
- A61K31/435—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
- A61K31/436—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 six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
-
- 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
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Enzymes And Modification Thereof (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762506334P | 2017-05-15 | 2017-05-15 | |
| US62/506,334 | 2017-05-15 | ||
| US201862652284P | 2018-04-03 | 2018-04-03 | |
| US62/652,284 | 2018-04-03 | ||
| US201862656297P | 2018-04-11 | 2018-04-11 | |
| US62/656,297 | 2018-04-11 | ||
| US201862657605P | 2018-04-13 | 2018-04-13 | |
| US62/657,605 | 2018-04-13 | ||
| PCT/US2018/032794 WO2018213329A1 (en) | 2017-05-15 | 2018-05-15 | Combinations of ret inhibitors and mtorc1 inhibitors and uses thereof for the treatment of cancer mediated by aberrant ret activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN110891573A true CN110891573A (zh) | 2020-03-17 |
Family
ID=62567777
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880046867.7A Pending CN110891573A (zh) | 2017-05-15 | 2018-05-15 | Ret抑制剂和mtorc1抑制剂的组合及其用于治疗由异常ret活性介导的癌症的用途 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20210290620A1 (https=) |
| EP (1) | EP3624802A1 (https=) |
| JP (1) | JP2020519672A (https=) |
| CN (1) | CN110891573A (https=) |
| WO (1) | WO2018213329A1 (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116867492A (zh) * | 2020-11-20 | 2023-10-10 | 赫尔森保健股份公司 | 使用4-氨基-n-[4-(甲氧基甲基)苯基]-7-(1-甲基环丙基)-6-(3-吗啉代丙-1-炔-1-基)-7h-吡咯并[2,3-d]嘧啶-5-羧酰胺治疗肿瘤的方法 |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
| PL3371171T3 (pl) | 2015-11-02 | 2024-03-25 | Blueprint Medicines Corporation | Inhibitory RET |
| SI3773589T1 (sl) * | 2018-04-03 | 2024-03-29 | Blueprint Medicines Corporation | Inhibitor RET za uporabo pri zdravljenju raka, ki ima RET spremembo |
| CN111961034A (zh) * | 2019-05-20 | 2020-11-20 | 浙江同源康医药股份有限公司 | 用作ret激酶抑制剂的化合物及其应用 |
| JP2023501757A (ja) * | 2020-05-29 | 2023-01-18 | ブループリント メディシンズ コーポレイション | プラルセチニブ薬学的組成物 |
| JP2023527412A (ja) | 2020-05-29 | 2023-06-28 | ブループリント メディシンズ コーポレイション | プラルセチニブの固体形態 |
| EP4687905A1 (en) | 2023-03-30 | 2026-02-11 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (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 |
| 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 |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| 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 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013170159A1 (en) * | 2012-05-10 | 2013-11-14 | Synta Pharmaceuticals Corp. | Treating cancer with hsp90 inhibitory compounds |
| WO2017079140A1 (en) * | 2015-11-02 | 2017-05-11 | Blueprint Medicines Corporation | Inhibitors of ret |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006128042A2 (en) | 2005-05-26 | 2006-11-30 | The Johns Hopkins University | Methods of identifying mutations in nucleic acid |
| US20090012045A1 (en) * | 2007-06-26 | 2009-01-08 | Rigel Pharmaceuticals, Inc. | Methods of Treating Cell Proliferative Disorders |
| WO2009100536A1 (en) | 2008-02-15 | 2009-08-20 | Methylgene Inc. | Inhibitors of kinase activity with 1,2-di-cyclyl substituted alkyne structures |
| EP2740742B1 (en) | 2011-08-04 | 2018-03-14 | National Cancer Center | Fusion gene of kif5b gene and ret gene, and method for determining effectiveness of cancer treatment targeting fusion gene |
| EP3564261B1 (en) | 2011-08-23 | 2024-11-13 | Foundation Medicine, Inc. | Kif5b-ret fusion molecules and uses thereof |
| US20130096136A1 (en) | 2011-09-30 | 2013-04-18 | Methylgene Inc. | Inhibitors of Protein Tyrosine Kinase Activity |
| JP2015109806A (ja) | 2012-03-22 | 2015-06-18 | アステラス製薬株式会社 | 新規ret融合体の検出法 |
| US20150177246A1 (en) | 2012-07-26 | 2015-06-25 | Lsip, Llc | Fusion gene of cep55 gene and ret gene |
| SI2902029T1 (sl) | 2012-09-25 | 2018-11-30 | Chugai Seiyaku Kabushiki Kaisha | Inhibitor ret |
| BR112015023618A2 (pt) | 2013-03-15 | 2017-07-18 | Glaxosmithkline Ip Dev Ltd | derivados de piridina como inibidores de quinase reorganizada durante a transfecção (ret) |
| WO2015006875A1 (en) | 2013-07-18 | 2015-01-22 | Methylgene Inc. | Process for the preparation of substituted pyrimidines |
| US20150057335A1 (en) | 2013-08-20 | 2015-02-26 | National Cancer Center | Novel fusion genes identified in lung cancer |
| GB201321146D0 (en) | 2013-11-29 | 2014-01-15 | Cancer Rec Tech Ltd | Quinazoline compounds |
| EA032030B1 (ru) | 2014-09-10 | 2019-03-29 | Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Соединения в качестве ингибиторов реаранжированной во время трансфекции (ret) киназы |
| PE20170705A1 (es) | 2014-09-10 | 2017-05-21 | Glaxosmithkline Ip Dev Ltd | Nuevos compuestos como inhibidores de ret (reorganizado durante la transfeccion) |
| ES2792036T3 (es) | 2014-11-14 | 2020-11-06 | Nerviano Medical Sciences Srl | Derivados de 6-amino-7-biciclo-7-deaza-purina como inhibidores de cinasa |
| US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
| BR112018000808A2 (pt) | 2015-07-16 | 2018-09-04 | Array Biopharma Inc | compostos de pirazolo[1,5-a]piridina substituída como inibidores de ret cinase |
| CN105255927B (zh) | 2015-09-30 | 2018-07-27 | 温州医科大学附属第一医院 | 一种kiaa1217-ret融合基因 |
| TW201738228A (zh) | 2016-03-17 | 2017-11-01 | 藍圖醫藥公司 | Ret之抑制劑 |
| US10227329B2 (en) | 2016-07-22 | 2019-03-12 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
| WO2018022761A1 (en) | 2016-07-27 | 2018-02-01 | Blueprint Medicines Corporation | Substituted cyclopentane-amides for treating disorders related to ret |
-
2018
- 2018-05-15 JP JP2019563217A patent/JP2020519672A/ja not_active Withdrawn
- 2018-05-15 US US16/613,625 patent/US20210290620A1/en not_active Abandoned
- 2018-05-15 CN CN201880046867.7A patent/CN110891573A/zh active Pending
- 2018-05-15 EP EP18730519.8A patent/EP3624802A1/en not_active Withdrawn
- 2018-05-15 WO PCT/US2018/032794 patent/WO2018213329A1/en not_active Ceased
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013170159A1 (en) * | 2012-05-10 | 2013-11-14 | Synta Pharmaceuticals Corp. | Treating cancer with hsp90 inhibitory compounds |
| WO2017079140A1 (en) * | 2015-11-02 | 2017-05-11 | Blueprint Medicines Corporation | Inhibitors of ret |
Non-Patent Citations (1)
| Title |
|---|
| VIVEK SUBBIAH 等: "Systemic and CNS activity of the RET inhibitor vandetanib combined with the mTOR inhibitor everolimus in KIF5B-RET re-arranged non-small cell lung cancer with brain metastases", 《LUNG CANCER》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116867492A (zh) * | 2020-11-20 | 2023-10-10 | 赫尔森保健股份公司 | 使用4-氨基-n-[4-(甲氧基甲基)苯基]-7-(1-甲基环丙基)-6-(3-吗啉代丙-1-炔-1-基)-7h-吡咯并[2,3-d]嘧啶-5-羧酰胺治疗肿瘤的方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2018213329A1 (en) | 2018-11-22 |
| JP2020519672A (ja) | 2020-07-02 |
| EP3624802A1 (en) | 2020-03-25 |
| US20210290620A1 (en) | 2021-09-23 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20200317 |
|
| WD01 | Invention patent application deemed withdrawn after publication |