JP2020531447A5 - - Google Patents
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- JP2020531447A5 JP2020531447A5 JP2020508534A JP2020508534A JP2020531447A5 JP 2020531447 A5 JP2020531447 A5 JP 2020531447A5 JP 2020508534 A JP2020508534 A JP 2020508534A JP 2020508534 A JP2020508534 A JP 2020508534A JP 2020531447 A5 JP2020531447 A5 JP 2020531447A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cycloalkyl
- alkoxy
- cancer
- compound according
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 18
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 17
- -1 benzo [d] imidazolyl Chemical group 0.000 claims 17
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 17
- 125000003545 alkoxy group Chemical group 0.000 claims 15
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 11
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 125000001309 chloro group Chemical group Cl* 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 125000004103 aminoalkyl group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000001153 fluoro group Chemical group F* 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 230000007547 defect Effects 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 101000581289 Homo sapiens Microcephalin Proteins 0.000 claims 2
- 102100027632 Microcephalin Human genes 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- 230000033590 base-excision repair Effects 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 208000016691 refractory malignant neoplasm Diseases 0.000 claims 2
- DDZGQYREBDXECY-UHFFFAOYSA-N 1h-pyrazolo[3,4-b]pyrazine Chemical compound C1=CN=C2C=NNC2=N1 DDZGQYREBDXECY-UHFFFAOYSA-N 0.000 claims 1
- 206010004593 Bile duct cancer Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 1
- 102100025064 Cellular tumor antigen p53 Human genes 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 230000005778 DNA damage Effects 0.000 claims 1
- 231100000277 DNA damage Toxicity 0.000 claims 1
- 239000012623 DNA damaging agent Substances 0.000 claims 1
- 102100039524 DNA endonuclease RBBP8 Human genes 0.000 claims 1
- 102100039116 DNA repair protein RAD50 Human genes 0.000 claims 1
- 102100033996 Double-strand break repair protein MRE11 Human genes 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 102100034533 Histone H2AX Human genes 0.000 claims 1
- 101000721661 Homo sapiens Cellular tumor antigen p53 Proteins 0.000 claims 1
- 101000743929 Homo sapiens DNA repair protein RAD50 Proteins 0.000 claims 1
- 101000591400 Homo sapiens Double-strand break repair protein MRE11 Proteins 0.000 claims 1
- 101001067891 Homo sapiens Histone H2AX Proteins 0.000 claims 1
- 101000581326 Homo sapiens Mediator of DNA damage checkpoint protein 1 Proteins 0.000 claims 1
- 101001128138 Homo sapiens NACHT, LRR and PYD domains-containing protein 2 Proteins 0.000 claims 1
- 101000981336 Homo sapiens Nibrin Proteins 0.000 claims 1
- 101000777277 Homo sapiens Serine/threonine-protein kinase Chk2 Proteins 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 102100027643 Mediator of DNA damage checkpoint protein 1 Human genes 0.000 claims 1
- 102100024403 Nibrin Human genes 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 101150097169 RBBP8 gene Proteins 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 102100031075 Serine/threonine-protein kinase Chk2 Human genes 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 102100029538 Structural maintenance of chromosomes protein 1A Human genes 0.000 claims 1
- 102000000504 Tumor Suppressor p53-Binding Protein 1 Human genes 0.000 claims 1
- 108010041385 Tumor Suppressor p53-Binding Protein 1 Proteins 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 208000026900 bile duct neoplasm Diseases 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000004857 imidazopyridinyl group Chemical group N1C(=NC2=C1C=CC=N2)* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000003965 isoxazolidinyl group Chemical group 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 230000019491 signal transduction Effects 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 108010004731 structural maintenance of chromosome protein 1 Proteins 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762546944P | 2017-08-17 | 2017-08-17 | |
| US62/546,944 | 2017-08-17 | ||
| PCT/US2018/046937 WO2019036641A1 (en) | 2017-08-17 | 2018-08-17 | HETEROCYCLIC INHIBITORS OF KINASE ATR |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020531447A JP2020531447A (ja) | 2020-11-05 |
| JP2020531447A5 true JP2020531447A5 (enExample) | 2021-09-24 |
| JP7290627B2 JP7290627B2 (ja) | 2023-06-13 |
Family
ID=65361058
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020508534A Active JP7290627B2 (ja) | 2017-08-17 | 2018-08-17 | Ａｔｒキナーゼの複素環式阻害剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US10800774B2 (enExample) |
| EP (1) | EP3668839B1 (enExample) |
| JP (1) | JP7290627B2 (enExample) |
| CN (1) | CN111886224B (enExample) |
| WO (1) | WO2019036641A1 (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018218197A2 (en) | 2017-05-26 | 2018-11-29 | Board Of Regents, The University Of Texas System | Tetrahydropyrido[4,3-d]pyrimidine inhibitors of atr kinase |
| US10377591B2 (en) | 2017-07-07 | 2019-08-13 | Zebra Technologies Corporation | Input handling for media processing devices |
| CN111867590B (zh) | 2017-07-13 | 2023-11-17 | 德州大学系统董事会 | Atr激酶的杂环抑制剂 |
| CN111886224B (zh) | 2017-08-17 | 2024-07-23 | 德州大学系统董事会 | Atr激酶的杂环抑制剂 |
| JP7235338B2 (ja) * | 2017-09-08 | 2023-03-08 | ニューウェーブ・ファーマスーティカル・インコーポレイテッド | Ａｔｒ阻害剤としての置換ピロロピリジン |
| EP3765008B1 (en) | 2018-03-16 | 2023-06-07 | Board of Regents, The University of Texas System | Heterocyclic inhibitors of atr kinase |
| JP2022510501A (ja) | 2018-10-30 | 2022-01-26 | リペア セラピューティクス インコーポレイテッド | 化合物、医薬組成物、ならびに化合物の調製方法及びａｔｒキナーゼ阻害剤としてのその使用方法 |
| CN118619944A (zh) | 2019-06-06 | 2024-09-10 | 北京泰德制药股份有限公司 | 作为atr激酶抑制剂的2,4,6-三取代的嘧啶化合物 |
| EP4011881B1 (en) | 2019-08-06 | 2025-02-12 | Wuxi Biocity Biopharmaceutics Co., Ltd. | Crystalline forms of an atr inhibitor and use thereof |
| US12448378B2 (en) | 2020-05-29 | 2025-10-21 | Wuxi Life Fountain Biotech Co., Ltd | Fluoropyrrolopyridine compound and application thereof |
| ES3054165T3 (en) * | 2020-10-16 | 2026-01-30 | Shanghai De Novo Pharmatech Co Ltd | Triheterocyclic derivative, and pharmaceutical composition and application thereof |
| CN116178366B (zh) * | 2021-11-26 | 2025-03-18 | 无锡瓴方生物医药科技有限公司 | 氟代吡啶并吡咯类化合物的晶型及其制备方法 |
| WO2025181153A1 (en) | 2024-03-01 | 2025-09-04 | F. Hoffmann-La Roche Ag | Use of atr inhibitors in combination with pi3k alpha inhibitors |
| WO2025217307A1 (en) | 2024-04-09 | 2025-10-16 | Revolution Medicines, Inc. | Methods for predicting response to a ras(on) inhibitor and combination therapies |
| WO2025229051A1 (en) | 2024-05-03 | 2025-11-06 | F. Hoffmann-La Roche Ag | Use of atr inhibitors in combination with antiandrogen agent |
| WO2025233224A1 (en) | 2024-05-09 | 2025-11-13 | F. Hoffmann-La Roche Ag | Use of atr inhibitors in combination with anti-pd(l)1 therapy |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IE49570B1 (en) | 1979-03-30 | 1985-10-30 | Rhone Poulenc Ind | 2-(pyrid-2-yl)tetrahydrothiophene derivatives |
| JO2660B1 (en) | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| US20070244110A1 (en) * | 2006-04-14 | 2007-10-18 | Zenyaku Kogyo Kabushiki Kaisha | Treatment of prostate cancer, melanoma or hepatic cancer |
| JP5534811B2 (ja) | 2006-08-24 | 2014-07-02 | アストラゼネカ アクチボラグ | 増殖性疾患の治療に有用なモルホリノピリミジン誘導体 |
| EP2064203A1 (en) * | 2006-09-14 | 2009-06-03 | AstraZeneca AB | 2-benzimidaz0lyl-6-m0rph0lin0-4-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders |
| BRPI0810646A2 (pt) | 2007-04-12 | 2014-11-04 | Hoffmann La Roche | " compostos farmacêuticos ". |
| US20080292588A1 (en) | 2007-05-17 | 2008-11-27 | Anadys Pharmaceuticals, Inc. | 1-methyl-benzo[1,2,4]thiadiazine 1-oxide derivatives |
| AU2008273892A1 (en) | 2007-07-09 | 2009-01-15 | Astrazeneca Ab | Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases |
| US8138183B2 (en) | 2007-07-09 | 2012-03-20 | Astrazeneca Ab | Morpholino pyrimidine derivatives used in diseases linked to mTOR kinase and/or PI3K |
| BRPI0814818A2 (pt) | 2007-07-09 | 2019-09-10 | Astrazeneca Ab | composto, uso de um composto, métodos para produzir um efeito anti-proliferativo e um efeito inibitório de mtor quinase em uma animal de sangue quente, método para tratar doenças, e, composição farmacêutica |
| JPWO2009110510A1 (ja) | 2008-03-06 | 2011-07-14 | Ｍｓｄ株式会社 | アルキルアミノピリジン誘導体 |
| CA2728559A1 (en) | 2008-07-03 | 2010-01-07 | Exelixis Inc. | Cdk modulators |
| US20110053923A1 (en) | 2008-12-22 | 2011-03-03 | Astrazeneca | Chemical compounds 610 |
| AU2010229468A1 (en) | 2009-03-27 | 2011-10-13 | Vetdc, Inc. | Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy |
| JP2013032290A (ja) | 2009-11-20 | 2013-02-14 | Dainippon Sumitomo Pharma Co Ltd | 新規縮合ピリミジン誘導体 |
| WO2011106276A1 (en) | 2010-02-25 | 2011-09-01 | Merck Sharp & Dohme Corp. | Task channel antagonists |
| WO2011103715A1 (en) | 2010-02-25 | 2011-09-01 | Merck Sharp & Dohme Corp. | Task channel antagonists |
| EP2542536B1 (en) | 2010-03-04 | 2015-01-21 | Cellzome Limited | Morpholino substituted urea derivatives as mtor inhibitors |
| SA111320519B1 (ar) | 2010-06-11 | 2014-07-02 | Astrazeneca Ab | مركبات بيريميدينيل للاستخدام كمثبطات atr |
| UA112517C2 (uk) | 2010-07-06 | 2016-09-26 | Новартіс Аг | Тетрагідропіридопіримідинові похідні |
| WO2012147890A1 (ja) | 2011-04-27 | 2012-11-01 | 持田製薬株式会社 | 新規アゾール誘導体 |
| 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 |
| HUE046727T2 (hu) | 2013-12-06 | 2020-03-30 | Vertex Pharma | Az ATR-kináz inhibitoraként használható vegyület, 2-amino-6-fluoro-N-[5-fluoro-piridin-3-IL]-pirazolo-[1,5-A]-pirimidin-3-karboxamid, ennek elõállítása, különbözõ szilárd formái és ezek radioaktív nyomjelzett származékai |
| WO2015092592A1 (en) | 2013-12-17 | 2015-06-25 | Pfizer Inc. | Novel 3,4-disubstituted-1h-pyrrolo[2,3-b]pyridines and 4,5-disubstituted-7h-pyrrolo[2,3-c]pyridazines as lrrk2 inhibitors |
| CN107074863B (zh) | 2014-06-05 | 2019-12-03 | 沃泰克斯药物股份有限公司 | Atr激酶抑制剂的制备方法及其不同的固体形式 |
| TWI700283B (zh) | 2014-08-04 | 2020-08-01 | 德商拜耳製藥公司 | ２-(嗎啉-４-基)-１,７-萘啶 |
| WO2016061097A1 (en) | 2014-10-13 | 2016-04-21 | Atrin Pharmaceuticals LLC | Ataxia telengiectasia and rad3-related (atr) protein kinase inhibitors |
| GB201514754D0 (en) | 2015-08-19 | 2015-09-30 | Karus Therapeutics Ltd | Compounds |
| CA3023765A1 (en) | 2016-05-24 | 2017-11-30 | Glaxosmithkline Intellectual Property (No. 2) Limited | Pyridine dicarboxamide derivatives as bromodomain inhibitors |
| US10774064B2 (en) * | 2016-06-02 | 2020-09-15 | Cadent Therapeutics, Inc. | Potassium channel modulators |
| WO2018218197A2 (en) | 2017-05-26 | 2018-11-29 | Board Of Regents, The University Of Texas System | Tetrahydropyrido[4,3-d]pyrimidine inhibitors of atr kinase |
| CN111867590B (zh) | 2017-07-13 | 2023-11-17 | 德州大学系统董事会 | Atr激酶的杂环抑制剂 |
| CN111886224B (zh) | 2017-08-17 | 2024-07-23 | 德州大学系统董事会 | Atr激酶的杂环抑制剂 |
| EP3765008B1 (en) | 2018-03-16 | 2023-06-07 | Board of Regents, The University of Texas System | Heterocyclic inhibitors of atr kinase |
-
2018
- 2018-08-17 CN CN201880061041.8A patent/CN111886224B/zh active Active
- 2018-08-17 WO PCT/US2018/046937 patent/WO2019036641A1/en not_active Ceased
- 2018-08-17 JP JP2020508534A patent/JP7290627B2/ja active Active
- 2018-08-17 US US16/104,561 patent/US10800774B2/en active Active
- 2018-08-17 EP EP18845633.9A patent/EP3668839B1/en active Active
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