KR20180041135A - Ret 키나아제 억제제로서 치환된 피라졸로[1,5-a]피리딘 화합물 - Google Patents
Ret 키나아제 억제제로서 치환된 피라졸로[1,5-a]피리딘 화합물 Download PDFInfo
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- KR20180041135A KR20180041135A KR1020187004643A KR20187004643A KR20180041135A KR 20180041135 A KR20180041135 A KR 20180041135A KR 1020187004643 A KR1020187004643 A KR 1020187004643A KR 20187004643 A KR20187004643 A KR 20187004643A KR 20180041135 A KR20180041135 A KR 20180041135A
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- Prior art keywords
- alkyl
- ret
- compound
- optionally substituted
- hetcyc
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- 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
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- 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
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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- 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
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- 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
- A61K31/495—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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- 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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- A—HUMAN NECESSITIES
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-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- 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
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- Health & Medical Sciences (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)
- Veterinary Medicine (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
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- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562193448P | 2015-07-16 | 2015-07-16 | |
| US62/193,448 | 2015-07-16 | ||
| US201562274018P | 2015-12-31 | 2015-12-31 | |
| US62/274,018 | 2015-12-31 | ||
| PCT/US2016/042576 WO2017011776A1 (en) | 2015-07-16 | 2016-07-15 | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20180041135A true KR20180041135A (ko) | 2018-04-23 |
Family
ID=56507905
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020187004643A Withdrawn KR20180041135A (ko) | 2015-07-16 | 2016-07-15 | Ret 키나아제 억제제로서 치환된 피라졸로[1,5-a]피리딘 화합물 |
Country Status (25)
| Country | Link |
|---|---|
| US (7) | US10023570B2 (enExample) |
| EP (1) | EP3322706B1 (enExample) |
| JP (1) | JP6816100B2 (enExample) |
| KR (1) | KR20180041135A (enExample) |
| CN (1) | CN108349969B (enExample) |
| AU (1) | AU2016291676B2 (enExample) |
| BR (1) | BR112018000808A2 (enExample) |
| CA (1) | CA2992586A1 (enExample) |
| CL (1) | CL2018000119A1 (enExample) |
| DK (1) | DK3322706T3 (enExample) |
| EA (1) | EA035049B1 (enExample) |
| ES (1) | ES2857081T3 (enExample) |
| HR (1) | HRP20210177T1 (enExample) |
| HU (1) | HUE053067T2 (enExample) |
| IL (1) | IL256898B (enExample) |
| LT (1) | LT3322706T (enExample) |
| MX (1) | MX378957B (enExample) |
| PH (1) | PH12018500121A1 (enExample) |
| PL (1) | PL3322706T3 (enExample) |
| PT (1) | PT3322706T (enExample) |
| RS (1) | RS61485B1 (enExample) |
| SI (1) | SI3322706T1 (enExample) |
| TN (1) | TN2018000027A1 (enExample) |
| WO (1) | WO2017011776A1 (enExample) |
| ZA (1) | ZA201800771B (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20220008322A (ko) * | 2019-05-14 | 2022-01-20 | 상하이 한서 바이오메디컬 컴퍼니 리미티드 | 2환식 유도체를 포함하는 억제제, 이의 제조방법 및 용도 |
Families Citing this family (79)
| Publication number | Priority date | Publication date | Assignee | Title |
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| EP2918588B1 (en) | 2010-05-20 | 2017-05-03 | Array Biopharma, Inc. | Macrocyclic compounds as TRK kinase 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 |
| EA038890B1 (ru) | 2015-11-02 | 2021-11-03 | Блюпринт Медсинс Корпорейшн | Ингибиторы ret |
| AR107912A1 (es) | 2016-03-17 | 2018-06-28 | Blueprint Medicines Corp | Inhibidores de ret |
| 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 |
| JP2018052878A (ja) | 2016-09-29 | 2018-04-05 | 第一三共株式会社 | ピリジン化合物 |
| JOP20190077A1 (ar) * | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| 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 |
| CA3049136C (en) | 2017-01-18 | 2022-06-14 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| 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 |
| MY201941A (en) | 2017-08-21 | 2024-03-25 | Taiho Pharmaceutical Co Ltd | Fusion protein of dctn1 protein with ret protein |
| 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 |
| TWI783057B (zh) * | 2017-10-10 | 2022-11-11 | 美商絡速藥業公司 | 製備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-甲腈的方法 |
| 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 |
| WO2019143994A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors |
| 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 |
| 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 |
| 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 |
| TW202017927A (zh) * | 2018-09-26 | 2020-05-16 | 大陸商重慶複創醫藥研究有限公司 | 作爲RET激酶抑制劑的取代的[1,2,4]三唑[1,5-a]吡啶化合物 |
| JP2022503932A (ja) * | 2018-09-27 | 2022-01-12 | フォチョン・ファーマシューティカルズ・リミテッド | Retキナーゼ阻害剤としての置換イミダゾ[1,2-a]ピリジン及び[1,2,4]トリアゾロ[1,5-a]ピリジン化合物 |
| WO2020064009A1 (zh) | 2018-09-30 | 2020-04-02 | 北京志健金瑞生物医药科技有限公司 | 取代吡唑稠环类衍生物及其制备方法和应用 |
| US11034669B2 (en) | 2018-11-30 | 2021-06-15 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| EP3878852A4 (en) * | 2018-12-06 | 2021-12-15 | Shenzhen TargetRx, Inc. | SUBSTITUTED PYRAZOLO [1,5-A] PYRIDINE COMPOUND, COMPOSITION THEREOF, AND USE THEREOF |
| JP7457709B2 (ja) * | 2018-12-07 | 2024-03-28 | サンシャイン・レイク・ファーマ・カンパニー・リミテッド | Ret阻害剤、医薬組成物、およびその使用 |
| 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 |
| JP7457708B2 (ja) * | 2018-12-07 | 2024-03-28 | サンシャイン・レイク・ファーマ・カンパニー・リミテッド | Ret阻害剤、医薬組成物およびその使用 |
| CN111592538A (zh) * | 2019-02-21 | 2020-08-28 | 南京明德新药研发有限公司 | 作为ret抑制剂的脂肪环衍生物 |
| CN111635400A (zh) | 2019-03-02 | 2020-09-08 | 察略盛医药科技(上海)有限公司 | 吡唑并[1,5-a]吡啶类衍生物、及其制备方法和用途 |
| AU2020242287A1 (en) | 2019-03-21 | 2021-09-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | A Dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| CN113474343B (zh) * | 2019-04-03 | 2024-01-23 | 广州白云山医药集团股份有限公司白云山制药总厂 | 作为ret抑制剂的吡唑并吡啶类化合物及其应用 |
| 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 |
| CA3142368A1 (en) * | 2019-06-10 | 2020-12-17 | Js Innopharm (Shanghai) Ltd | Heterocyclic compounds as kinase inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof |
| WO2021008455A1 (zh) * | 2019-07-12 | 2021-01-21 | 首药控股(北京)有限公司 | Ret选择性抑制剂及其制备方法和用途 |
| US12338253B2 (en) | 2019-08-05 | 2025-06-24 | Applied Pharmaceutical Science, Inc. | Nitrogen-containing polycyclic fused ring compound, pharmaceutical composition thereof, preparation method therefor and use thereof |
| WO2021043209A1 (zh) * | 2019-09-04 | 2021-03-11 | 广东东阳光药业有限公司 | 一种ret抑制剂、其药物组合物及其用途 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20220008322A (ko) * | 2019-05-14 | 2022-01-20 | 상하이 한서 바이오메디컬 컴퍼니 리미티드 | 2환식 유도체를 포함하는 억제제, 이의 제조방법 및 용도 |
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