AU2016348402B2 - Inhibitors of RET - Google Patents
Inhibitors of RET Download PDFInfo
- Publication number
- AU2016348402B2 AU2016348402B2 AU2016348402A AU2016348402A AU2016348402B2 AU 2016348402 B2 AU2016348402 B2 AU 2016348402B2 AU 2016348402 A AU2016348402 A AU 2016348402A AU 2016348402 A AU2016348402 A AU 2016348402A AU 2016348402 B2 AU2016348402 B2 AU 2016348402B2
- Authority
- AU
- Australia
- Prior art keywords
- compound
- alkyl
- hydrogen
- pharmaceutically acceptable
- acceptable salt
- 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.)
- Ceased, expires
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- 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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/30—Halogen atoms or nitro radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/34—One oxygen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/34—One oxygen atom
- C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/38—One sulfur atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D403/02—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 two hetero rings
- C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562249784P | 2015-11-02 | 2015-11-02 | |
| US62/249,784 | 2015-11-02 | ||
| US201662367960P | 2016-07-28 | 2016-07-28 | |
| US62/367,960 | 2016-07-28 | ||
| PCT/US2016/059879 WO2017079140A1 (en) | 2015-11-02 | 2016-11-01 | Inhibitors of ret |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2016348402A1 AU2016348402A1 (en) | 2018-05-31 |
| AU2016348402B2 true AU2016348402B2 (en) | 2021-05-13 |
Family
ID=57286889
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2016348402A Ceased AU2016348402B2 (en) | 2015-11-02 | 2016-11-01 | Inhibitors of RET |
Country Status (31)
Families Citing this family (70)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT3205654T (pt) | 2010-05-20 | 2019-04-22 | Array Biopharma Inc | Compostos macrocíclicos como inibidores de cinases trk |
| BR112015000653A2 (pt) | 2012-07-11 | 2019-11-05 | Blueprint Medicines Corp | compostos inibidores do receptor de fator de crescimento de fibroblasto, sua composição farmacêutica e seus usos |
| WO2014160521A1 (en) | 2013-03-15 | 2014-10-02 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| PL3409674T3 (pl) | 2013-10-17 | 2022-09-26 | Blueprint Medicines Corporation | Sposób wytwarzania kompozycji użytecznych do leczenia zaburzeń związanych z KIT |
| PH12016500739B1 (en) | 2013-10-25 | 2022-04-29 | Blueprint Medicines Corp | Inhibitors of the fibrolast growth factor receptor |
| US9695165B2 (en) | 2014-01-15 | 2017-07-04 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
| EA035049B1 (ru) | 2015-07-16 | 2020-04-22 | Аррэй Байофарма Инк. | СОЕДИНЕНИЯ ЗАМЕЩЕННОГО ПИРАЗОЛО[1,5-a]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ RET КИНАЗЫ |
| MX2018001032A (es) | 2015-07-24 | 2018-11-09 | Blueprint Medicines Corp | Compuestos utiles para el tratamiento de trastornos relacionados con kit y pdgfr. |
| WO2017035354A1 (en) | 2015-08-26 | 2017-03-02 | Blueprint Medicines Corporation | Compounds and compositions useful for treating disorders related to ntrk |
| EP3371171B1 (en) | 2015-11-02 | 2023-10-25 | Blueprint Medicines Corporation | Inhibitors of ret |
| CN108431008A (zh) | 2015-11-19 | 2018-08-21 | 蓝图药品公司 | 可用于治疗与ntrk相关的病症的化合物和组合物 |
| UY37155A (es) | 2016-03-17 | 2017-10-31 | Blueprint Medicines Corp | Inhibidores de ret |
| PL3442977T3 (pl) | 2016-04-15 | 2024-03-04 | Blueprint Medicines Corporation | Inhibitory kinazy podobnej do receptora aktywiny |
| US20190142868A1 (en) | 2016-05-13 | 2019-05-16 | Instituto de Medicina Moleccular | Methods of treating diseases associated with ilc3 cells |
| WO2018017983A1 (en) * | 2016-07-22 | 2018-01-25 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to ret |
| US10035789B2 (en) | 2016-07-27 | 2018-07-31 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| CA3049136C (en) | 2017-01-18 | 2022-06-14 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| US11040979B2 (en) | 2017-03-31 | 2021-06-22 | Blueprint Medicines Corporation | Substituted pyrrolo[1,2-b]pyridazines for treating disorders related to KIT and PDGFR |
| EP3624802A1 (en) | 2017-05-15 | 2020-03-25 | Blueprint Medicines Corporation | Combinations of ret inhibitors and mtorc1 inhibitors and uses thereof for the treatment of cancer mediated by aberrant ret activity |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| TWI812649B (zh) | 2017-10-10 | 2023-08-21 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| EP3697786B1 (en) | 2017-10-18 | 2022-08-31 | Blueprint Medicines Corporation | Substituted pyrrolopyridines as inhibitors of activin receptor-like kinase |
| EP3740486A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| CN111630054B (zh) | 2018-01-18 | 2023-05-09 | 奥瑞生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物 |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| WO2019195471A1 (en) | 2018-04-03 | 2019-10-10 | Blueprint Medicines Corporation | Ret inhibitor for use in treating cancer having a ret alteration |
| WO2020033838A2 (en) | 2018-08-10 | 2020-02-13 | Blueprint Medicines Corporation | Treatment of egfr-mutant cancer |
| CN112566907A (zh) * | 2018-08-17 | 2021-03-26 | 南京明德新药研发有限公司 | 作为ret抑制剂的吡唑衍生物 |
| ES2922314T3 (es) | 2018-09-10 | 2022-09-13 | Array Biopharma Inc | Compuestos heterocíclicos condensados como inhibidores de cinasa RET |
| WO2020114474A1 (zh) * | 2018-12-06 | 2020-06-11 | 苏州信诺维医药科技有限公司 | 一种杂环化合物、其应用及含其的药物组合物 |
| CN111285882B (zh) * | 2018-12-07 | 2022-12-02 | 四川科伦博泰生物医药股份有限公司 | 稠环化合物、包含其的药物组合物及其制备方法和用途 |
| CN111484479B (zh) * | 2019-01-25 | 2023-06-13 | 四川科伦博泰生物医药股份有限公司 | 氮杂环化合物、包含其的药物组合物及其制备方法和用途 |
| CN111499613B (zh) * | 2019-01-31 | 2023-05-12 | 浙江海正药业股份有限公司 | N-甲酰胺衍生物、其制备方法及其在医药上的用途 |
| EP3929198A4 (en) | 2019-02-19 | 2022-11-16 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | HETEROCYCLIC COMPOUND, PHARMACEUTICAL COMPOSITION THEREOF, PROCESS FOR THEIR PRODUCTION AND ITS USE |
| EP3950688B1 (en) * | 2019-04-03 | 2025-01-15 | Guangzhou Baiyunshan Pharmaceutical Holdings Co., Ltd. Baiyunshan Pharmaceutical General Factory | Nitrogen-containing spiro derivative as ret inhibitor |
| CN111808077B (zh) | 2019-04-12 | 2023-05-02 | 浙江海正药业股份有限公司 | 哌嗪酰胺衍生物，其制备方法及其在医药上的用途 |
| EP4302761A3 (en) | 2019-04-12 | 2024-03-27 | Blueprint Medicines Corporation | Crystalline forms of (s)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1h-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazinyl)-pyrimidin-5-yl)ethan-1-amine and methods of making |
| 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 |
| US11666570B2 (en) * | 2019-07-11 | 2023-06-06 | The Board Of Trustees Of The Leland Stanford Junior University | Diagnosis and regulation of epidermal differentiation and cancer cell activity |
| CN113121524B (zh) | 2019-12-31 | 2023-04-25 | 南京创济生物医药有限公司 | 杂环亚砜亚胺化合物及其中间体、制备方法和应用 |
| CN113135896B (zh) * | 2020-01-18 | 2024-12-06 | 正大天晴药业集团股份有限公司 | 作为ret抑制剂的甲基吡唑类衍生物 |
| CN111362923A (zh) * | 2020-03-25 | 2020-07-03 | 魏威 | 制备ret抑制剂普拉塞替尼的方法、以及普拉塞替尼的中间体及其制备方法 |
| CN111440151A (zh) * | 2020-03-25 | 2020-07-24 | 魏威 | 制备抗肿瘤药普拉赛替尼的方法 |
| CN111269229B (zh) * | 2020-03-27 | 2021-02-12 | 苏州信诺维医药科技有限公司 | 一种治疗癌症的化合物 |
| CN113698390B (zh) * | 2020-05-20 | 2022-09-27 | 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 |
| PE20231425A1 (es) * | 2020-05-29 | 2023-09-13 | Blueprint Medicines Corp | Composiciones farmaceuticas de pralsetinib |
| CA3183728A1 (en) * | 2020-05-29 | 2021-12-02 | Blueprint Medicines Corporation | Solid forms of pralsetinib |
| CN111777595A (zh) * | 2020-07-22 | 2020-10-16 | 上海希迈医药科技有限公司 | 一种环己烷甲酰胺类化合物的新晶型及其制备方法 |
| WO2022086899A1 (en) | 2020-10-19 | 2022-04-28 | Teva Pharmaceuticals International Gmbh | Solid state forms of pralsetinib and process for preparation thereof |
| WO2022117448A1 (en) | 2020-12-03 | 2022-06-09 | Sandoz Ag | Crystalline forms of pralsetinib |
| AU2021390534A1 (en) * | 2020-12-04 | 2023-06-22 | Blueprint Medicines Corporation | Method of preparing pralsetinib |
| CN113072541B (zh) * | 2021-04-02 | 2022-07-08 | 山东四环药业股份有限公司 | 一种靶向药物blu-667的制备方法 |
| JP2024522938A (ja) | 2021-06-03 | 2024-06-21 | フンダサン デー．アンナ ジ ソーメル チャンパリマウド エー ドクトル カルロス モンテス チャンパリマウド | 脳－脂肪回路を介してｉｌｃ２および肥満度を制御する神経－間葉単位 |
| TW202345806A (zh) | 2022-03-31 | 2023-12-01 | 美商艾伯維有限公司 | 噻唑并〔５，４－ｂ〕吡啶ｍａｌｔ－１抑制劑 |
| CN115057822B (zh) * | 2022-07-14 | 2023-05-02 | 上海优合贝德医药科技有限公司 | 一种普拉替尼中间体2097133-31-6的新合成方法 |
| CN117466901A (zh) * | 2022-07-23 | 2024-01-30 | 浙江海正药业股份有限公司 | 哌嗪酰胺衍生物的晶型及其制备方法和用途 |
| CN119768181A (zh) | 2022-08-24 | 2025-04-04 | 东丽株式会社 | 用于癌的治疗和/或预防的药品 |
| KR20250164828A (ko) | 2023-03-30 | 2025-11-25 | 레볼루션 메디슨즈, 인크. | Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도 |
| IT202300006819A1 (it) | 2023-04-06 | 2024-10-06 | Olon Spa | Processo per preparare pralsetinib in forma amorfa, e relativi intermedi in forma cristallina. |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | 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 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004009087A1 (en) * | 2002-07-24 | 2004-01-29 | University Of Cincinnati | 4-4(methylpiperazin-1-ylmethyl)-n-[4-methyl-3-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide for treating mutated-ret kinase associated diseases |
| WO2007124221A1 (en) * | 2006-04-18 | 2007-11-01 | Rigel Pharmaceuticals, Inc. | Methods of treating cell proliferative disorders by using pyrimidinediamine compounds |
| WO2008061201A1 (en) * | 2006-11-15 | 2008-05-22 | Rigel Pharmaceuticals, Inc. | Methods for treating renal tumors using 2,4-pyrimidinediamine drug and prodrug compounds |
| WO2009003136A1 (en) * | 2007-06-26 | 2008-12-31 | Rigel Pharmaceuticals, Inc. | Substituted pyrimidine-2, 4 -diamines for treating cell proliferative disorders |
Family Cites Families (80)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA02007957A (es) | 2000-02-17 | 2002-11-29 | Amgen Inc | Inhibidores de cinasas. |
| JP5138938B2 (ja) | 2003-12-19 | 2013-02-06 | プレキシコン インコーポレーテッド | Ｒｅｔ調節剤の開発のための化合物および方法 |
| WO2006128042A2 (en) | 2005-05-26 | 2006-11-30 | The Johns Hopkins University | Methods of identifying mutations in nucleic acid |
| WO2007023382A2 (en) | 2005-08-25 | 2007-03-01 | Pfizer Inc. | Pyrimidine amino pyrazole compounds, potent kinase inhibitors |
| US20090227598A1 (en) | 2006-01-24 | 2009-09-10 | Buser-Doepner Carolyn A | Ret Tyrosine Kinase Inhibition |
| BRPI0814818A2 (pt) | 2007-07-09 | 2019-09-10 | Astrazeneca Ab | composto, uso de um composto, métodos para produzir um efeito anti-proliferativo e um efeito inibitório de mtor quinase em uma animal de sangue quente, método para tratar doenças, e, composição farmacêutica |
| MY150032A (en) | 2007-07-19 | 2013-11-29 | Merck Sharp & Dohme | Heterocyclic amide compounds as protein kinase inhibitors |
| NZ582879A (en) * | 2007-07-31 | 2012-03-30 | Vertex Pharma | Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof |
| WO2009100536A1 (en) | 2008-02-15 | 2009-08-20 | Methylgene Inc. | Inhibitors of kinase activity with 1,2-di-cyclyl substituted alkyne structures |
| EP2313091A4 (en) | 2008-07-14 | 2012-04-04 | Univ Kingston | PHARMACEUTICAL COMPOSITIONS WITH RET-HEMMERN AND METHOD FOR THE TREATMENT OF CANCER |
| CN102497863A (zh) * | 2009-03-24 | 2012-06-13 | Msdk.K.公司 | 具有Aurora A选择性抑制作用的新型氨基吡啶衍生物 |
| CA2765044A1 (en) * | 2009-06-09 | 2010-12-16 | California Capital Equity, Llc | Benzyl substituted triazine derivatives and their therapeutical applications |
| EA201290255A1 (ru) | 2009-10-30 | 2013-04-30 | Ариад Фармасьютикалз, Инк. | Способы и композиции для лечения рака |
| EP2498607B1 (en) | 2009-11-13 | 2016-02-17 | Genosco | Kinase inhibitors |
| 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 |
| BR112014004213A2 (pt) | 2011-08-23 | 2017-06-20 | Found Medicine Inc | novas moléculas de fusão kif5b-ret e usos das mesmas |
| EP2751112B1 (en) | 2011-09-02 | 2019-10-09 | The Regents of The University of California | Substituted pyrazolo[3,4-d]pyrimidines and uses thereof |
| US20130096136A1 (en) | 2011-09-30 | 2013-04-18 | Methylgene Inc. | Inhibitors of Protein Tyrosine Kinase Activity |
| US10023855B2 (en) | 2011-10-31 | 2018-07-17 | Macrogen, Inc. | Fusion protein comprising C-terminal domain of RET protein and use thereof as a diagnosing marker |
| EP2776420A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
| 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 |
| ES2645984T3 (es) * | 2012-04-25 | 2017-12-11 | Raqualia Pharma Inc | Derivados de pirrolopiridinona como bloqueadores de TTX-S |
| WO2013170159A1 (en) | 2012-05-10 | 2013-11-14 | Synta Pharmaceuticals Corp. | Treating cancer with hsp90 inhibitory compounds |
| BR112015000653A2 (pt) | 2012-07-11 | 2019-11-05 | Blueprint Medicines Corp | compostos inibidores do receptor de fator de crescimento de fibroblasto, sua composição farmacêutica e seus usos |
| WO2014017491A1 (ja) | 2012-07-26 | 2014-01-30 | 独立行政法人国立がん研究センター | Ｃｅｐ５５遺伝子とｒｅｔ遺伝子との融合遺伝子 |
| WO2014039971A1 (en) | 2012-09-07 | 2014-03-13 | Exelixis, Inc. | Inhibitors of met, vegfr and ret for use in the treatment of lung adenocarcinoma |
| JP5759568B2 (ja) * | 2012-09-25 | 2015-08-05 | 中外製薬株式会社 | Ｒｅｔ阻害剤 |
| US9604980B2 (en) | 2012-11-07 | 2017-03-28 | Nerviano Medical Sciences S.R.L. | Substituted pyrimidinyl and pyridinyl-pyrrolopyridinones, process for their preparation and their use as kinase inhibitors |
| TWI629266B (zh) | 2012-12-28 | 2018-07-11 | 藍印藥品公司 | 纖維母細胞生長因子受體之抑制劑 |
| EA027861B1 (ru) | 2013-02-25 | 2017-09-29 | Бристол-Майерс Сквибб Компани | C-3 алкил- и алкенилмодифицированные производные бетулиновой кислоты или их фармацевтические соли, противовирусная фармацевтическая композиция и фармацевтическая композиция для лечения вич на их основе |
| ES2616655T3 (es) | 2013-03-15 | 2017-06-13 | Glaxosmithkline Intellectual Property Development Limited | Derivados de piridina como inhibidores de quinasa reorganizada durante la transfección (RET) |
| WO2014160521A1 (en) | 2013-03-15 | 2014-10-02 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| WO2015006875A1 (en) | 2013-07-18 | 2015-01-22 | Methylgene Inc. | Process for the preparation of substituted pyrimidines |
| WO2015025866A1 (ja) | 2013-08-20 | 2015-02-26 | 独立行政法人国立がん研究センター | 肺がんで見出された新規融合遺伝子 |
| PL3409674T3 (pl) | 2013-10-17 | 2022-09-26 | Blueprint Medicines Corporation | Sposób wytwarzania kompozycji użytecznych do leczenia zaburzeń związanych z KIT |
| US9334263B2 (en) | 2013-10-17 | 2016-05-10 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| PH12016500739B1 (en) | 2013-10-25 | 2022-04-29 | Blueprint Medicines Corp | Inhibitors of the fibrolast growth factor receptor |
| GB201321146D0 (en) | 2013-11-29 | 2014-01-15 | Cancer Rec Tech Ltd | Quinazoline compounds |
| US9695165B2 (en) | 2014-01-15 | 2017-07-04 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| WO2016022569A1 (en) | 2014-08-04 | 2016-02-11 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| WO2016037578A1 (en) | 2014-09-10 | 2016-03-17 | Glaxosmithkline Intellectual Property Development Limited | Novel compounds as rearranged during transfection (ret) inhibitors |
| EP3517526B1 (en) | 2014-09-10 | 2020-08-19 | GlaxoSmithKline Intellectual Property Development Limited | Pyridinones as rearranged during transfection (ret) inhibitors |
| 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 |
| EA035049B1 (ru) | 2015-07-16 | 2020-04-22 | Аррэй Байофарма Инк. | СОЕДИНЕНИЯ ЗАМЕЩЕННОГО ПИРАЗОЛО[1,5-a]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ RET КИНАЗЫ |
| MX2018001032A (es) | 2015-07-24 | 2018-11-09 | Blueprint Medicines Corp | Compuestos utiles para el tratamiento de trastornos relacionados con kit y pdgfr. |
| WO2017035354A1 (en) | 2015-08-26 | 2017-03-02 | Blueprint Medicines Corporation | Compounds and compositions useful for treating disorders related to ntrk |
| 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 |
| EP3371171B1 (en) | 2015-11-02 | 2023-10-25 | Blueprint Medicines Corporation | Inhibitors of ret |
| MX2018005517A (es) | 2015-11-02 | 2018-11-09 | Five Prime Therapeutics Inc | Polipeptidos del dominio extracelular de cd80 y su uso en el tratamiento del cancer. |
| JP2018534933A (ja) | 2015-11-02 | 2018-11-29 | ヤンセン ファーマシューティカ エヌ．ベー． | 抗ｉｌ１ｒａｐ抗体、ｉｌ１ｒａｐとｃｄ３を結合する二重特異性抗原結合分子、及びその使用 |
| CN108431008A (zh) | 2015-11-19 | 2018-08-21 | 蓝图药品公司 | 可用于治疗与ntrk相关的病症的化合物和组合物 |
| WO2017145050A1 (en) | 2016-02-23 | 2017-08-31 | Glaxosmithkline Intellectual Property Development Limited | Pyridylpyridone derivative useful as a ret kinase inhibitor in the treatment of ibs and cancer |
| UY37155A (es) | 2016-03-17 | 2017-10-31 | Blueprint Medicines Corp | Inhibidores de ret |
| BR112018070163A2 (pt) | 2016-04-01 | 2019-01-29 | Signal Pharm Llc | compostos de aminopurina substituída, composições e métodos de tratamento |
| JP6943876B2 (ja) | 2016-04-15 | 2021-10-06 | キャンサー・リサーチ・テクノロジー・リミテッドＣａｎｃｅｒ Ｒｅｓｅａｒｃｈ Ｔｅｃｈｎｏｌｏｇｙ Ｌｉｍｉｔｅｄ | Ｒｅｔキナーゼ阻害剤としての複素環化合物 |
| SMT202200348T1 (it) | 2016-04-15 | 2022-11-18 | Cancer Research Tech Ltd | Composti eterociclici come inibitori della chinasi ret |
| PL3442977T3 (pl) | 2016-04-15 | 2024-03-04 | Blueprint Medicines Corporation | Inhibitory kinazy podobnej do receptora aktywiny |
| WO2018017983A1 (en) | 2016-07-22 | 2018-01-25 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to ret |
| US10035789B2 (en) | 2016-07-27 | 2018-07-31 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
| WO2018049233A1 (en) | 2016-09-08 | 2018-03-15 | Nicolas Stransky | Inhibitors of the fibroblast growth factor receptor in combination with cyclin-dependent kinase inhibitors |
| JP2018052878A (ja) | 2016-09-29 | 2018-04-05 | 第一三共株式会社 | ピリジン化合物 |
| CN106749231B (zh) | 2016-10-09 | 2019-03-01 | 南京纳丁菲医药科技有限公司 | 萘啶化合物和药物组合物及它们的应用 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| US10799503B2 (en) | 2016-12-01 | 2020-10-13 | Ignyta, Inc. | Methods for the treatment of cancer |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| CA3049136C (en) | 2017-01-18 | 2022-06-14 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors |
| US11040979B2 (en) | 2017-03-31 | 2021-06-22 | Blueprint Medicines Corporation | Substituted pyrrolo[1,2-b]pyridazines for treating disorders related to KIT and PDGFR |
| GB201705971D0 (en) | 2017-04-13 | 2017-05-31 | Cancer Res Tech Ltd | Inhibitor compounds |
| EP3624802A1 (en) | 2017-05-15 | 2020-03-25 | Blueprint Medicines Corporation | Combinations of ret inhibitors and mtorc1 inhibitors and uses thereof for the treatment of cancer mediated by aberrant ret activity |
| WO2018237134A1 (en) | 2017-06-23 | 2018-12-27 | San Diego State University Research Foundation | Atropisomerism for enhanced kinase inhibitor selectivity |
| CN109180677A (zh) | 2017-06-30 | 2019-01-11 | 厦门大学 | 取代芳基醚类化合物、其制备方法、药用组合物及其应用 |
| EP4095258A1 (en) | 2017-07-07 | 2022-11-30 | Nipd Genetics Public Company Limited | Target-enriched multiplexed parallel analysis for assesment of tumor biomarkers |
| CN111511746B (zh) | 2017-12-19 | 2024-01-09 | 特普医药公司 | 用于治疗疾病的巨环化合物 |
| EP3740491A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| CN111630054B (zh) | 2018-01-18 | 2023-05-09 | 奥瑞生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物 |
| EP3740486A1 (en) | 2018-01-18 | 2020-11-25 | Array Biopharma, Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| WO2019195471A1 (en) | 2018-04-03 | 2019-10-10 | Blueprint Medicines Corporation | Ret inhibitor for use in treating cancer having a ret alteration |
| WO2020033838A2 (en) | 2018-08-10 | 2020-02-13 | Blueprint Medicines Corporation | Treatment of egfr-mutant cancer |
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004009087A1 (en) * | 2002-07-24 | 2004-01-29 | University Of Cincinnati | 4-4(methylpiperazin-1-ylmethyl)-n-[4-methyl-3-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide for treating mutated-ret kinase associated diseases |
| WO2007124221A1 (en) * | 2006-04-18 | 2007-11-01 | Rigel Pharmaceuticals, Inc. | Methods of treating cell proliferative disorders by using pyrimidinediamine compounds |
| WO2008061201A1 (en) * | 2006-11-15 | 2008-05-22 | Rigel Pharmaceuticals, Inc. | Methods for treating renal tumors using 2,4-pyrimidinediamine drug and prodrug compounds |
| WO2009003136A1 (en) * | 2007-06-26 | 2008-12-31 | Rigel Pharmaceuticals, Inc. | Substituted pyrimidine-2, 4 -diamines for treating cell proliferative disorders |
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