CA2870837C - 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof - Google Patents
5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof Download PDFInfo
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- CA2870837C CA2870837C CA2870837A CA2870837A CA2870837C CA 2870837 C CA2870837 C CA 2870837C CA 2870837 A CA2870837 A CA 2870837A CA 2870837 A CA2870837 A CA 2870837A CA 2870837 C CA2870837 C CA 2870837C
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Classifications
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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
- A61K31/505—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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- A61K31/33—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
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- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—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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- A—HUMAN NECESSITIES
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- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
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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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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
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- 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
- 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
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Molecular Biology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Nutrition Science (AREA)
- Physiology (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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| US201261647200P | 2012-05-15 | 2012-05-15 | |
| US61/647,200 | 2012-05-15 | ||
| PCT/GB2013/051233 WO2013171470A1 (en) | 2012-05-15 | 2013-05-14 | 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof |
Publications (2)
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| CA2870837A1 CA2870837A1 (en) | 2013-11-21 |
| CA2870837C true CA2870837C (en) | 2022-05-10 |
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| SG (1) | SG11201407238VA (OSRAM) |
| WO (1) | WO2013171470A1 (OSRAM) |
| ZA (1) | ZA201408452B (OSRAM) |
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| ES2709003T3 (es) | 2011-11-09 | 2019-04-12 | Cancer Research Tech Ltd | Compuestos de 5-(piridin-2-il-amino)-pirazina-2-carbonitrilo y su uso terapéutico |
| SG11201407238VA (en) * | 2012-05-15 | 2014-12-30 | Cancer Rec Tech Ltd | 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof |
| SMT202000713T1 (it) | 2012-12-07 | 2021-03-15 | Vertex Pharma | Pirazolo [1,5-a] pirimidine utili come inibitori dell'atr chinasi per il trattamento di malattie del cancro |
| US9663519B2 (en) | 2013-03-15 | 2017-05-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| ES2768678T3 (es) | 2013-12-06 | 2020-06-23 | Vertex Pharma | Compuesto de 2-amino-6-fluoro-N-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inhibidor de la ATR quinasa, su preparación, diferentes formas sólidas y derivados radiomarcados de las mismas |
| SG10201902206QA (en) | 2014-06-05 | 2019-04-29 | Vertex Pharma | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
| AU2015277212B2 (en) * | 2014-06-17 | 2020-07-02 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of Chk1 and ATR inhibitors |
| RU2768621C1 (ru) | 2015-09-30 | 2022-03-24 | Вертекс Фармасьютикалз Инкорпорейтед | Способ лечения рака с использованием комбинации повреждающих днк средств и ингибиторов atr |
| WO2018094325A1 (en) * | 2016-11-18 | 2018-05-24 | The Trustees Of Columbia University In The City Of New York | Therapeutic modulation of oncogenes by pharmacologic top2 targeting for cancer |
| MX2019011506A (es) * | 2017-03-31 | 2019-11-01 | Seattle Genetics Inc | Inhibicion de cinasa 1 de punto de control (chk1) para el tratamiento de cancer. |
| WO2018191299A1 (en) * | 2017-04-10 | 2018-10-18 | Sierra Oncology, Inc. | Chk1(sra737)wee1 inhibitor combination methods of inhibiting tumor growth |
| CN116999564A (zh) * | 2017-04-10 | 2023-11-07 | 塞拉肿瘤学公司 | 抑制肿瘤生长的CHK1(SRA737)/PARPi组合方法 |
| US20200157638A1 (en) * | 2017-06-01 | 2020-05-21 | Sierra Oncology, Inc. | Biomarkers and patient selection strategies |
| CN107266897B (zh) * | 2017-08-04 | 2019-05-14 | 上海跃贝新材料科技股份有限公司 | 一种低粘度矿物增强pc/pet合金材料及其制备方法 |
| KR20200126388A (ko) * | 2018-02-26 | 2020-11-06 | 시에라 온코로지, 인코퍼레이티드 | Chk1 저해제를 포함하는 암의 치료 방법 |
| JP2022523028A (ja) * | 2019-01-25 | 2022-04-21 | ヌメディー， インコーポレイテッド | 特発性肺線維症を処置するための方法 |
| CA3135165A1 (en) * | 2019-03-28 | 2020-10-01 | Sierra Oncology, Inc. | Methods of treating cancer with chk1 inhibitors |
| CN114072526A (zh) * | 2019-05-14 | 2022-02-18 | 塞拉肿瘤学公司 | 使用chk1抑制剂治疗癌症的方法 |
| CN110872277B (zh) * | 2019-11-14 | 2021-06-04 | 浙江大学 | N-取代芳环-2-氨基嘧啶类化合物及用途 |
| CN110684083B (zh) * | 2019-12-06 | 2020-05-15 | 北京诺赛启研再生医学研究院有限公司 | 抑制黑色素合成的偶联物ii及其在药品和化妆品中的应用 |
| CN110680928B (zh) * | 2019-12-06 | 2020-04-28 | 深圳前海港影生物科技有限公司 | 抑制黑色素合成的偶联物及其在药品和化妆品中的应用 |
| TW202204348A (zh) * | 2020-04-07 | 2022-02-01 | 美商西爾拉癌症醫學公司 | Ｃｈｋ１抑制劑之合成方法 |
| CN117858870A (zh) * | 2021-08-17 | 2024-04-09 | 葛兰素史密斯克莱知识产权(第3号)有限公司 | P2x3拮抗剂的制备 |
| TW202519226A (zh) | 2023-11-08 | 2025-05-16 | 美商艾克塞里克斯公司 | 使用抑制ｐｋｍｙｔ１之化合物治療癌症之方法 |
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| US7776865B2 (en) | 2005-10-06 | 2010-08-17 | Schering Corporation | Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| GB0616747D0 (en) * | 2006-08-24 | 2006-10-04 | Astrazeneca Ab | Novel compounds |
| WO2008077554A1 (en) | 2006-12-27 | 2008-07-03 | Sanofi-Aventis | Cycloalkylamine substituted isoquinoline derivatives |
| CN103588704B (zh) * | 2007-03-16 | 2016-09-14 | 斯克里普斯研究学院 | 粘着斑激酶抑制剂 |
| WO2008117050A1 (en) | 2007-03-27 | 2008-10-02 | Astrazeneca Ab | Pyrazolyl-amino-substituted pyrazines and their use for the treatment of cancer |
| US8618121B2 (en) | 2007-07-02 | 2013-12-31 | Cancer Research Technology Limited | 9H-pyrimido[4,5-B]indoles, 9H-pyrido[4',3':4,5]pyrrolo[2,3-D]pyridines, and 9H 1,3,6,9 tetraaza-fluorenes as CHK1 kinase function inhibitors |
| GB0719644D0 (en) * | 2007-10-05 | 2007-11-14 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| GB0803018D0 (en) | 2008-02-19 | 2008-03-26 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| ES2709003T3 (es) | 2011-11-09 | 2019-04-12 | Cancer Research Tech Ltd | Compuestos de 5-(piridin-2-il-amino)-pirazina-2-carbonitrilo y su uso terapéutico |
| SG11201407238VA (en) | 2012-05-15 | 2014-12-30 | Cancer Rec Tech Ltd | 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof |
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