JP5998223B2 - キナーゼ阻害剤としての置換３，４−ジヒドロピロロ［１，２−ａ］ピラジン−１（２Ｈ）−オン誘導体 - Google Patents
キナーゼ阻害剤としての置換３，４−ジヒドロピロロ［１，２−ａ］ピラジン−１（２Ｈ）−オン誘導体 Download PDFInfo
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- JP5998223B2 JP5998223B2 JP2014533881A JP2014533881A JP5998223B2 JP 5998223 B2 JP5998223 B2 JP 5998223B2 JP 2014533881 A JP2014533881 A JP 2014533881A JP 2014533881 A JP2014533881 A JP 2014533881A JP 5998223 B2 JP5998223 B2 JP 5998223B2
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- pyrazin
- oxo
- tetrahydropyrrolo
- acetamide
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Classifications
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
- A61N5/00—Radiation therapy
- A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
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- General Health & Medical Sciences (AREA)
- Public Health (AREA)
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- General Chemical & Material Sciences (AREA)
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- Radiology & Medical Imaging (AREA)
- Pathology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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| EP11184337.1 | 2011-10-07 | ||
| EP11184337 | 2011-10-07 | ||
| PCT/EP2012/069586 WO2013050446A1 (en) | 2011-10-07 | 2012-10-04 | SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS |
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| JP2014528433A JP2014528433A (ja) | 2014-10-27 |
| JP2014528433A5 JP2014528433A5 (cg-RX-API-DMAC7.html) | 2015-11-19 |
| JP5998223B2 true JP5998223B2 (ja) | 2016-09-28 |
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| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| WO2013032718A1 (en) * | 2011-08-31 | 2013-03-07 | Dow Global Technologies Llc | Method for preparing flexible polyurethane foam with hydrolysable silane compounds |
| WO2014110574A1 (en) | 2013-01-14 | 2014-07-17 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
| UA121098C2 (uk) | 2013-01-15 | 2020-04-10 | Інсайт Холдинґс Корпорейшн | Тіазолкарбоксаміди і піридинкарбоксаміди, які використовуються як інгібітори рім-кінази |
| WO2015027124A1 (en) | 2013-08-23 | 2015-02-26 | Incyte Corporation | Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
| US10301306B2 (en) | 2014-12-15 | 2019-05-28 | Bristol-Myers Squibb Company | Substituted dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-ones as RIPK3 inhibitors |
| WO2016196244A1 (en) | 2015-05-29 | 2016-12-08 | Incyte Corporation | Pyridineamine compounds useful as pim kinase inhibitors |
| EA035049B1 (ru) | 2015-07-16 | 2020-04-22 | Аррэй Байофарма Инк. | СОЕДИНЕНИЯ ЗАМЕЩЕННОГО ПИРАЗОЛО[1,5-a]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ RET КИНАЗЫ |
| TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Ｐｉｍ激酶抑制劑之鹽 |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| TN2019000271A1 (en) | 2015-10-26 | 2021-01-07 | Univ Colorado Regents | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| EP3439663B1 (en) | 2016-04-04 | 2024-07-17 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| TN2018000335A1 (en) | 2016-04-04 | 2020-01-16 | Loxo Oncology Inc | Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| SI3800189T1 (sl) | 2016-05-18 | 2023-11-30 | Loxo Oncology, Inc. | Priprava (s)-n-(5-((r)-2-(2,5-difluorofenil)pirolidin-1-il)pirazolo (1,5-a)pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida |
| 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 |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| 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 |
| 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 |
| AR113922A1 (es) | 2017-12-08 | 2020-07-01 | Incyte Corp | Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas |
| 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 |
| WO2019191667A1 (en) | 2018-03-29 | 2019-10-03 | Board Of Regents, The University Of Texas System | Imidazopiperazine inhibitors of transcription activating proteins |
| WO2019195846A1 (en) * | 2018-04-06 | 2019-10-10 | Board Of Regents, The University Of Texas System | Imidazopiperazinone inhibitors of transcription activating proteins |
| KR102653681B1 (ko) | 2018-07-31 | 2024-04-03 | 록쏘 온콜로지, 인코포레이티드 | (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의분무-건조된 분산물 및 제제 |
| ES2922314T3 (es) | 2018-09-10 | 2022-09-13 | Array Biopharma Inc | Compuestos heterocíclicos condensados como inhibidores de cinasa RET |
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| WO2020238776A1 (zh) * | 2019-05-24 | 2020-12-03 | 江苏恒瑞医药股份有限公司 | 取代的稠合双环类衍生物、其制备方法及其在医药上的应用 |
| WO2021113492A1 (en) | 2019-12-06 | 2021-06-10 | Schrödinger, Inc. | Cyclic compounds and methods of using same |
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| GB0520958D0 (en) | 2005-10-14 | 2005-11-23 | Cyclacel Ltd | Compound |
| WO2009118411A2 (en) * | 2008-03-28 | 2009-10-01 | Nerviano Medical Sciences S.R.L. | 3,4-dihydro-2h-pyrazino[1,2-a]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| ES2536730T3 (es) * | 2008-09-19 | 2015-05-28 | Nerviano Medical Sciences S.R.L. | Derivados de 3,4-dihidro-2H-pirrolo[1,2-a]pirazin-1-ona |
| ES2524576T3 (es) * | 2010-01-29 | 2014-12-10 | Nerviano Medical Sciences S.R.L. | Derivados de 6,7-dihidroimidazo[1,5-a]pirazin-8(5H)-ona como moduladores de proteína cinasa |
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2012
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Also Published As
| Publication number | Publication date |
|---|---|
| US20140243347A1 (en) | 2014-08-28 |
| EP2788351A1 (en) | 2014-10-15 |
| EP2788351B1 (en) | 2017-06-28 |
| JP2014528433A (ja) | 2014-10-27 |
| US9145418B2 (en) | 2015-09-29 |
| WO2013050446A1 (en) | 2013-04-11 |
| ES2639064T3 (es) | 2017-10-25 |
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