CA3003721C - Inhibitors of ret to treat cancer - Google Patents
Inhibitors of ret to treat cancer Download PDFInfo
- Publication number
- CA3003721C CA3003721C CA3003721A CA3003721A CA3003721C CA 3003721 C CA3003721 C CA 3003721C CA 3003721 A CA3003721 A CA 3003721A CA 3003721 A CA3003721 A CA 3003721A CA 3003721 C CA3003721 C CA 3003721C
- Authority
- CA
- Canada
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- hydrogen
- alkyl
- 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.)
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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)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (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)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (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 |
|---|---|
| CA3003721A1 CA3003721A1 (en) | 2017-05-11 |
| CA3003721C true CA3003721C (en) | 2024-02-06 |
Family
ID=57286889
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3003721A Active CA3003721C (en) | 2015-11-02 | 2016-11-01 | Inhibitors of ret to treat cancer |
Country Status (31)
| Country | Link |
|---|---|
| US (5) | US10030005B2 (OSRAM) |
| EP (3) | EP4292594A3 (OSRAM) |
| JP (3) | JP6807385B2 (OSRAM) |
| KR (1) | KR20180073689A (OSRAM) |
| CN (2) | CN108473468B (OSRAM) |
| AU (1) | AU2016348402B2 (OSRAM) |
| BR (1) | BR112018008877B1 (OSRAM) |
| CA (1) | CA3003721C (OSRAM) |
| CL (1) | CL2018001181A1 (OSRAM) |
| DK (1) | DK3371171T3 (OSRAM) |
| EA (1) | EA038890B1 (OSRAM) |
| ES (1) | ES2969185T3 (OSRAM) |
| FI (1) | FI3371171T3 (OSRAM) |
| FR (1) | FR24C1016I1 (OSRAM) |
| HR (1) | HRP20231681T1 (OSRAM) |
| HU (1) | HUE064659T2 (OSRAM) |
| IL (3) | IL288519B2 (OSRAM) |
| LT (1) | LT3371171T (OSRAM) |
| MX (1) | MX384884B (OSRAM) |
| MY (1) | MY194262A (OSRAM) |
| NZ (1) | NZ742351A (OSRAM) |
| PH (1) | PH12018500907A1 (OSRAM) |
| PL (1) | PL3371171T3 (OSRAM) |
| PT (1) | PT3371171T (OSRAM) |
| RS (1) | RS65069B1 (OSRAM) |
| SA (1) | SA518391496B1 (OSRAM) |
| SG (1) | SG11201803653QA (OSRAM) |
| SI (1) | SI3371171T1 (OSRAM) |
| TW (2) | TWI787018B (OSRAM) |
| WO (1) | WO2017079140A1 (OSRAM) |
| ZA (1) | ZA201803050B (OSRAM) |
Families Citing this family (69)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2918588B1 (en) | 2010-05-20 | 2017-05-03 | Array Biopharma, Inc. | Macrocyclic compounds as TRK kinase inhibitors |
| US8802697B2 (en) | 2012-07-11 | 2014-08-12 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| WO2014160521A1 (en) | 2013-03-15 | 2014-10-02 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| ES2683127T3 (es) | 2013-10-17 | 2018-09-25 | Blueprint Medicines Corporation | Composiciones útiles para tratar trastornos relacionados con la KIT |
| AU2014339972B9 (en) | 2013-10-25 | 2019-05-30 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
| DK3322706T3 (da) | 2015-07-16 | 2021-02-01 | Array Biopharma Inc | Substituerede pyrazolo[1,5-a]pyridin-forbindelser som ret-kinaseinhibitorer |
| MX2018001032A (es) | 2015-07-24 | 2018-11-09 | Blueprint Medicines Corp | Compuestos utiles para el tratamiento de trastornos relacionados con kit y pdgfr. |
| CN108137607B (zh) | 2015-08-26 | 2021-04-06 | 缆图药品公司 | 适用于治疗与ntrk相关的病症的化合物和组合物 |
| EA038890B1 (ru) | 2015-11-02 | 2021-11-03 | Блюпринт Медсинс Корпорейшн | Ингибиторы ret |
| CA3005741A1 (en) | 2015-11-19 | 2017-05-26 | Blueprint Medicines Corporation | Compounds and compositions useful for treating disorders related to ntrk |
| AR107912A1 (es) | 2016-03-17 | 2018-06-28 | Blueprint Medicines Corp | Inhibidores de ret |
| EP3442977B1 (en) | 2016-04-15 | 2023-06-28 | Blueprint Medicines Corporation | Inhibitors of activin receptor-like kinase |
| JP7000349B2 (ja) | 2016-05-13 | 2022-02-04 | インスティテュート デ メディシナ モレキュラー ジョアオ ロボ アントゥネス | Ｉｌｃ３細胞に関連する疾患を処置する方法 |
| WO2018017983A1 (en) * | 2016-07-22 | 2018-01-25 | 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 |
| 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 |
| WO2018183712A1 (en) | 2017-03-31 | 2018-10-04 | Blueprint Medicines Corporation | Pyrrolo[1,2-b]pyridazine compounds and compositions useful for treating disorders related to kit and pdgfr |
| WO2018213329A1 (en) | 2017-05-15 | 2018-11-22 | Blueprint Medicines Corporation | Combinations of ret inhibitors and mtorc1 inhibitors and uses thereof for the treatment of cancer mediated by aberrant ret activity |
| 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 |
| 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 |
| CN111566102B (zh) | 2017-10-18 | 2023-09-08 | 缆图药品公司 | 作为激活素受体样激酶抑制剂的取代的吡咯并吡啶 |
| CA3087578C (en) | 2018-01-18 | 2023-08-08 | Array Biopharma Inc. | Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors |
| CA3087354C (en) | 2018-01-18 | 2023-01-03 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| WO2019143994A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| CA3096043A1 (en) | 2018-04-03 | 2019-10-10 | Blueprint Medicines Corporation | Ret inhibitor for use in treating cancer having a ret alteration |
| EP3833372A4 (en) | 2018-08-10 | 2022-06-08 | 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 |
| CN112996794A (zh) | 2018-09-10 | 2021-06-18 | 阿雷生物药品公司 | 作为ret激酶抑制剂的稠合杂环化合物 |
| 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 |
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| PH12021552004A1 (en) | 2019-02-19 | 2022-09-05 | Sichuan Kelun Biotech Biopharmaceutical Co Ltd | Heterocyclic compound, pharmaceutical composition comprising same, preparation method therefor, and use thereof |
| 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 |
| LT3856341T (lt) | 2019-04-12 | 2023-12-27 | Blueprint Medicines Corporation | (s)-1-(4-fluorfenil)-1-(2-(4-(6-(1-metil-1h-pirazol-4-il)pirolo[2,1-f] [1,2,4]triazin-4-il)piperazinil)-pirimidin-5-il)etan-1-amino kristalinės formos ir gamybos būdai |
| 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 |
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| 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 |
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| WO2022117448A1 (en) | 2020-12-03 | 2022-06-09 | Sandoz Ag | Crystalline forms of pralsetinib |
| EP4255892A1 (en) * | 2020-12-04 | 2023-10-11 | 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 |
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