TW201524958A - 用作轉染期間重排抑制劑之新穎化合物 - Google Patents
用作轉染期間重排抑制劑之新穎化合物 Download PDFInfo
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- TW201524958A TW201524958A TW103109315A TW103109315A TW201524958A TW 201524958 A TW201524958 A TW 201524958A TW 103109315 A TW103109315 A TW 103109315A TW 103109315 A TW103109315 A TW 103109315A TW 201524958 A TW201524958 A TW 201524958A
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- Prior art keywords
- alkyl
- ethoxy
- fluorophenyl
- trifluoromethyl
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Classifications
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
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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
-
- 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
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/62—Oxygen or sulfur atoms
- C07D213/69—Two or more oxygen atoms
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
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- 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Peptides Or Proteins (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
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| CN2014072449 | 2014-02-24 |
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| TW201524958A true TW201524958A (zh) | 2015-07-01 |
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| TWI757256B (zh) * | 2015-11-02 | 2022-03-11 | 美商纜圖藥品公司 | 轉染過程重排之抑制劑 |
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| BR122019024201B1 (pt) | 2010-05-20 | 2021-08-03 | Array Biopharma Inc | Composto macrocíclico como inibidores de trk quinase, seu uso, e composição farmacêutica |
| AU2015313894A1 (en) * | 2014-09-08 | 2017-03-23 | Glaxosmithkline Intellectual Property Development Limited | Crystalline forms of 2-(4-(4-ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-n-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)acetamide |
| BR112017004897A2 (pt) * | 2014-09-10 | 2017-12-12 | Glaxosmithkline Ip Dev Ltd | compostos inovadores como inibidores rearranjados durante a transfecção (ret) |
| EP3517526B1 (en) | 2014-09-10 | 2020-08-19 | GlaxoSmithKline Intellectual Property Development Limited | Pyridinones as rearranged during transfection (ret) inhibitors |
| US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
| CA2992586A1 (en) | 2015-07-16 | 2017-01-19 | Array Biopharma, Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors |
| US10829484B2 (en) | 2015-07-28 | 2020-11-10 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| 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 |
| US10160747B2 (en) | 2016-03-16 | 2018-12-25 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| AR107912A1 (es) | 2016-03-17 | 2018-06-28 | Blueprint Medicines Corp | Inhibidores de ret |
| EP3454886A1 (en) | 2016-05-13 | 2019-03-20 | Instituto de Medicina Molecular | 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 |
| JP2018052878A (ja) | 2016-09-29 | 2018-04-05 | 第一三共株式会社 | ピリジン化合物 |
| TWI752098B (zh) | 2016-10-10 | 2022-01-11 | 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 |
| 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 |
| JP6888101B2 (ja) | 2017-01-18 | 2021-06-16 | アレイ バイオファーマ インコーポレイテッド | ＲＥＴキナーゼ阻害剤としての置換ピラゾロ［１，５−ａ］ピラジン化合物 |
| 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 |
| US20210290620A1 (en) | 2017-05-15 | 2021-09-23 | Blueprint Medicines Corporation | Combinations of RET Inhibitors and mTORC1 Inhibitors and Uses Thereof for the Treatment of Cancer Mediated by Aberrant RET Activity |
| US10093648B1 (en) * | 2017-09-22 | 2018-10-09 | Celgene Corporation | Crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate, compositions and methods of use thereof |
| TWI876442B (zh) | 2017-10-10 | 2025-03-11 | 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 |
| 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 |
| SG11202009681YA (en) | 2018-04-03 | 2020-10-29 | Blueprint Medicines Corp | Ret inhibitor for use in treating cancer having a ret alteration |
| CN109096264B (zh) * | 2018-08-28 | 2019-08-23 | 山东理工职业学院 | Ret抑制剂及其制备方法、组合物和用途 |
| ES2922314T3 (es) | 2018-09-10 | 2022-09-13 | Array Biopharma Inc | Compuestos heterocíclicos condensados como inhibidores de cinasa RET |
| EP3956330A4 (en) | 2019-04-18 | 2023-01-18 | The Johns Hopkins University | SUBSTITUTED 2-AMINO-PYRAZOLYL-[1,2,4]TRIAZOLO[1,5A]PYRIDINE DERIVATIVES AND THEIR USE |
| JP7461605B2 (ja) * | 2020-02-20 | 2024-04-04 | 広州白雲山医薬集団股▲フン▼有限公司白雲山制薬総廠 | キノリン系化合物 |
| TWI777509B (zh) * | 2020-04-27 | 2022-09-11 | 美商美國禮來大藥廠 | 用於抑制ret激酶之化合物 |
| WO2021243192A1 (en) | 2020-05-29 | 2021-12-02 | Blueprint Medicines Corporation | Solid forms of pralsetinib |
| CR20220666A (es) | 2020-05-29 | 2023-05-05 | Blueprint Medicines Corp | Composiciones farmacéuticas de pralsetinib |
| TWI786742B (zh) * | 2020-07-23 | 2022-12-11 | 大陸商深圳晶泰科技有限公司 | 吡啶酮類化合物及其製備方法和應用 |
| IL301817A (en) | 2020-10-13 | 2023-06-01 | Univ Johns Hopkins | Modified 4-([4,2,1]triazolo[5,1-a]pyridin-6-yl)thiophene-2-carboxamide histories and their use |
| KR20230104146A (ko) * | 2020-11-06 | 2023-07-07 | 일라이 릴리 앤드 캄파니 | Ret 키나제 억제제로서의 피라졸 유도체 |
| EP4347645A1 (en) | 2021-06-03 | 2024-04-10 | Fundação D. Anna de Sommer Champalimaud e Dr. Carlos Montez Champalimaud Foundation | Neuro-mesenchyme units control ilc2 and obesity via a brain-adipose circuit |
| CN115626880B (zh) * | 2022-11-15 | 2023-11-14 | 常州大学 | 3-硝基-5-氰基三氟甲苯的合成方法 |
| CN116925023B (zh) * | 2023-07-18 | 2025-11-21 | 江苏桐孚高新材料有限公司 | 2-全氟烷基-4h-吡喃-4-酮衍生物的改进合成方法 |
| EP4650002A1 (en) * | 2024-05-15 | 2025-11-19 | Ludwig-Maximilians-Universität | Aniline-based modulators of the nuclear receptor tlx (nr2e1) |
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| MXPA02001498A (es) | 1999-08-12 | 2003-07-21 | Pharmacia & Italia S P A | Derivados de 3(5)-amino-pirazol, procedimiento para la preparacion de los mismos y usos como agentes antitumorales. |
| AU2002215053A1 (en) * | 2000-11-27 | 2002-06-24 | Pharmacia Italia S.P.A. | Phenylacetamido- pyrazole derivatives and their use as antitumor agents |
| DE10201764A1 (de) | 2002-01-18 | 2003-07-31 | Bayer Cropscience Ag | Substituierte 4-Aminopyridin-Derivate |
| US7968574B2 (en) | 2004-12-28 | 2011-06-28 | Kinex Pharmaceuticals, Llc | Biaryl compositions and methods for modulating a kinase cascade |
| CN101558068A (zh) * | 2006-10-16 | 2009-10-14 | 诺瓦提斯公司 | 用作蛋白激酶抑制剂的苯乙酰胺类 |
| PL2848610T3 (pl) * | 2006-11-15 | 2018-01-31 | Ym Biosciences Australia Pty | Inhibitory aktywności kinazy |
| KR20120059558A (ko) | 2009-08-19 | 2012-06-08 | 암비트 바이오사이언시즈 코포레이션 | 바이아릴 화합물 및 이의 사용 방법 |
| EP2651930B1 (en) | 2010-12-16 | 2015-10-28 | Boehringer Ingelheim International GmbH | Biarylamide inhibitors of leukotriene production |
| AR095308A1 (es) | 2013-03-15 | 2015-10-07 | Glaxosmithkline Ip Dev Ltd | Compuesto de 2-piridona, composición farmacéutica que lo comprende y su uso para preparar un medicamento |
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2014
- 2014-03-14 MX MX2015012286A patent/MX2015012286A/es unknown
- 2014-03-14 PT PT147135982T patent/PT2970191T/pt unknown
- 2014-03-14 US US14/775,772 patent/US9382238B2/en not_active Expired - Fee Related
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- 2014-03-14 UY UY0001035465A patent/UY35465A/es unknown
- 2014-03-14 TW TW103109315A patent/TW201524958A/zh unknown
- 2014-03-14 PE PE2015001878A patent/PE20151538A1/es not_active Application Discontinuation
- 2014-03-14 UA UAA201510041A patent/UA115264C2/uk unknown
- 2014-03-14 LT LTEP14713598.2T patent/LT2970191T/lt unknown
- 2014-03-14 WO PCT/IB2014/059817 patent/WO2014141187A1/en not_active Ceased
- 2014-03-14 HR HRP20170363TT patent/HRP20170363T1/hr unknown
- 2014-03-14 SM SM20170152T patent/SMT201700152T1/it unknown
- 2014-03-14 BR BR112015023618A patent/BR112015023618A2/pt not_active IP Right Cessation
- 2014-03-14 PL PL14713598T patent/PL2970191T3/pl unknown
- 2014-03-14 JP JP2015562529A patent/JP2016516026A/ja active Pending
- 2014-03-14 HU HUE14713598A patent/HUE033423T2/en unknown
- 2014-03-14 DK DK14713598.2T patent/DK2970191T3/en active
- 2014-03-14 AU AU2014229233A patent/AU2014229233B2/en not_active Ceased
- 2014-03-14 EP EP14713598.2A patent/EP2970191B1/en active Active
- 2014-03-14 CN CN201480015907.3A patent/CN105051027A/zh active Pending
- 2014-03-14 NZ NZ628388A patent/NZ628388A/en not_active IP Right Cessation
- 2014-03-14 EA EA201591738A patent/EA029296B1/ru not_active IP Right Cessation
- 2014-03-14 CA CA2905627A patent/CA2905627A1/en not_active Abandoned
- 2014-03-14 ME MEP-2017-60A patent/ME02664B/me unknown
- 2014-03-14 ES ES14713598.2T patent/ES2616655T3/es active Active
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2015
- 2015-09-03 IL IL241161A patent/IL241161A0/en unknown
- 2015-09-08 CL CL2015002514A patent/CL2015002514A1/es unknown
- 2015-09-10 PH PH12015502044A patent/PH12015502044A1/en unknown
- 2015-09-14 CR CR20150490A patent/CR20150490A/es unknown
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2016
- 2016-06-02 US US15/171,229 patent/US9789100B2/en not_active Expired - Fee Related
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI757256B (zh) * | 2015-11-02 | 2022-03-11 | 美商纜圖藥品公司 | 轉染過程重排之抑制劑 |
| TWI787018B (zh) * | 2015-11-02 | 2022-12-11 | 美商纜圖藥品公司 | 轉染過程重排之抑制劑 |
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