JP2017531041A5 - - Google Patents
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- Publication number
- JP2017531041A5 JP2017531041A5 JP2017538930A JP2017538930A JP2017531041A5 JP 2017531041 A5 JP2017531041 A5 JP 2017531041A5 JP 2017538930 A JP2017538930 A JP 2017538930A JP 2017538930 A JP2017538930 A JP 2017538930A JP 2017531041 A5 JP2017531041 A5 JP 2017531041A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- alkyl
- macrocyclic compound
- alkenyl
- aralkyl
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 19
- 238000000034 method Methods 0.000 claims description 5
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 201000011510 cancer Diseases 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 150000002678 macrocyclic compounds Chemical class 0.000 claims 26
- 125000000217 alkyl group Chemical group 0.000 claims 17
- 125000003342 alkenyl group Chemical group 0.000 claims 15
- 125000003710 aryl alkyl group Chemical group 0.000 claims 15
- 125000003118 aryl group Chemical group 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- 125000000304 alkynyl group Chemical group 0.000 claims 13
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims 13
- 125000000623 heterocyclic group Chemical group 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 13
- -1 oxazoyl Chemical group 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 239000002552 dosage form Substances 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000004434 sulfur atom Chemical group 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 239000012623 DNA damaging agent Substances 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 125000004452 carbocyclyl group Chemical group 0.000 claims 2
- 125000005884 carbocyclylalkyl group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 150000003462 sulfoxides Chemical class 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 125000001931 aliphatic group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 229960000397 bevacizumab Drugs 0.000 claims 1
- GXJABQQUPOEUTA-RDJZCZTQSA-N bortezomib Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)B(O)O)NC(=O)C=1N=CC=NC=1)C1=CC=CC=C1 GXJABQQUPOEUTA-RDJZCZTQSA-N 0.000 claims 1
- 229960001467 bortezomib Drugs 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 1
- 229960004316 cisplatin Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims 1
- 229960004768 irinotecan Drugs 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- FAQDUNYVKQKNLD-UHFFFAOYSA-N olaparib Chemical group FC1=CC=C(CC2=C3[CH]C=CC=C3C(=O)N=N2)C=C1C(=O)N(CC1)CCN1C(=O)C1CC1 FAQDUNYVKQKNLD-UHFFFAOYSA-N 0.000 claims 1
- 229960000572 olaparib Drugs 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 229960001592 paclitaxel Drugs 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 150000003457 sulfones Chemical class 0.000 claims 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 0 C*(C)c1nc(*)c(*)nc1***(*)I** Chemical compound C*(C)c1nc(*)c(*)nc1***(*)I** 0.000 description 20
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 description 4
- 239000003909 protein kinase inhibitor Substances 0.000 description 4
- 102000010583 ATR Human genes 0.000 description 1
- 206010003591 Ataxia Diseases 0.000 description 1
- 101000904787 Homo sapiens Serine/threonine-protein kinase ATR Proteins 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462063176P | 2014-10-13 | 2014-10-13 | |
| US62/063,176 | 2014-10-13 | ||
| US201562104274P | 2015-01-16 | 2015-01-16 | |
| US62/104,274 | 2015-01-16 | ||
| PCT/US2015/055317 WO2016061097A1 (en) | 2014-10-13 | 2015-10-13 | Ataxia telengiectasia and rad3-related (atr) protein kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017531041A JP2017531041A (ja) | 2017-10-19 |
| JP2017531041A5 true JP2017531041A5 (Direct) | 2018-11-15 |
| JP6678679B2 JP6678679B2 (ja) | 2020-04-08 |
Family
ID=55654998
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017538930A Active JP6678679B2 (ja) | 2014-10-13 | 2015-10-13 | 毛細血管拡張性運動失調症およびＲａｄ３関連（ＡＴＲ）プロテインキナーゼ阻害剤 |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US9663535B2 (Direct) |
| EP (1) | EP3207031B1 (Direct) |
| JP (1) | JP6678679B2 (Direct) |
| KR (1) | KR102569226B1 (Direct) |
| CN (1) | CN107108527B (Direct) |
| AU (1) | AU2015333738B2 (Direct) |
| BR (1) | BR112017007708B8 (Direct) |
| CA (1) | CA2963973C (Direct) |
| ES (1) | ES2879441T3 (Direct) |
| IL (1) | IL251595B (Direct) |
| MX (1) | MX389198B (Direct) |
| WO (1) | WO2016061097A1 (Direct) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3207031B1 (en) | 2014-10-13 | 2021-04-14 | Atrin Pharmaceuticals LLC | Ataxia telengiectasia and rad3-related (atr) protein kinase inhibitors |
| US10301324B2 (en) | 2016-04-12 | 2019-05-28 | Atrin Pharmaceuticals LLC | Ataxia telengiectasia and rad3-related (ATR) inhibitors and methods of their use |
| 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 |
| ES2974334T3 (es) | 2017-07-13 | 2024-06-26 | Univ Texas | Inhibidores heterocíclicos de ATR cinasa |
| 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 |
| US11267809B2 (en) | 2017-09-14 | 2022-03-08 | The Board Of Trustees Of The Leland Stanford Junior University | BAF complex modulating compounds and methods of using the same |
| EP3765008B1 (en) | 2018-03-16 | 2023-06-07 | Board of Regents, The University of Texas System | Heterocyclic inhibitors of atr kinase |
| CN110357905B (zh) * | 2018-03-26 | 2021-10-01 | 武汉誉祥医药科技有限公司 | 作为蛋白激酶抑制剂的大环类衍生物及其制备方法和用途 |
| US11980613B2 (en) | 2018-07-12 | 2024-05-14 | The Board Of Trustees Of The Leland Stanford Junior University | Methods for reversing HIV latency using BAF complex modulating compounds |
| CN110950890B (zh) * | 2018-09-27 | 2022-07-01 | 北京赛林泰医药技术有限公司 | 取代的咪唑并[4,5-c]喹啉大环化合物作为多靶点激酶抑制剂 |
| CR20210281A (es) | 2018-10-30 | 2021-10-25 | Repare Therapeutics Inc | Compuestos, composiciones farmacéuticas y métodos de preparación de compuestos y de uso como inhibidores de la cinasa atr |
| CN114369096A (zh) | 2020-10-16 | 2022-04-19 | 上海迪诺医药科技有限公司 | 三杂环衍生物、其药物组合物及应用 |
| CN119585285A (zh) | 2022-04-14 | 2025-03-07 | 阿普里治疗股份有限公司 | Atr抑制剂 |
| CA3258066A1 (en) | 2022-06-15 | 2023-12-21 | Astrazeneca Ab | Polytherapy for the treatment of cancer |
| WO2025181153A1 (en) | 2024-03-01 | 2025-09-04 | F. Hoffmann-La Roche Ag | Use of atr inhibitors in combination with pi3k alpha inhibitors |
| 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 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA05009063A (es) * | 2003-02-26 | 2005-12-12 | Sugen Inc | Compuestos de aminoheteroarilo como inhibidores de proteina cinasa. |
| US7163939B2 (en) * | 2003-11-05 | 2007-01-16 | Abbott Laboratories | Macrocyclic kinase inhibitors |
| NZ593969A (en) * | 2008-12-19 | 2013-11-29 | Vertex Pharma | Pyrazine derivatives useful as inhibitors of atr kinase |
| JP2013526540A (ja) * | 2010-05-12 | 2013-06-24 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ａｔｒキナーゼ阻害剤として有用な化合物 |
| EP2686323A1 (en) | 2011-03-16 | 2014-01-22 | Cephalon, Inc. | Macrocyclic compounds as alk, fak and jak2 inhibitors |
| KR101692600B1 (ko) * | 2012-03-06 | 2017-01-03 | 화이자 인코포레이티드 | 증식성 질환 치료용 거대환형 유도체 |
| DK2836485T3 (en) * | 2012-03-17 | 2018-04-23 | Polyphor Ag | CONFORMITY LIMITED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS |
| CN104513253A (zh) * | 2013-10-01 | 2015-04-15 | 南京波尔泰药业科技有限公司 | 用于治疗增殖性疾病的大环化合物 |
| EP3207031B1 (en) | 2014-10-13 | 2021-04-14 | Atrin Pharmaceuticals LLC | Ataxia telengiectasia and rad3-related (atr) protein kinase inhibitors |
-
2015
- 2015-10-13 EP EP15850553.7A patent/EP3207031B1/en active Active
- 2015-10-13 BR BR112017007708A patent/BR112017007708B8/pt active Search and Examination
- 2015-10-13 ES ES15850553T patent/ES2879441T3/es active Active
- 2015-10-13 AU AU2015333738A patent/AU2015333738B2/en active Active
- 2015-10-13 WO PCT/US2015/055317 patent/WO2016061097A1/en not_active Ceased
- 2015-10-13 JP JP2017538930A patent/JP6678679B2/ja active Active
- 2015-10-13 CN CN201580067182.7A patent/CN107108527B/zh active Active
- 2015-10-13 US US14/881,680 patent/US9663535B2/en active Active
- 2015-10-13 CA CA2963973A patent/CA2963973C/en active Active
- 2015-10-13 MX MX2017004515A patent/MX389198B/es unknown
- 2015-10-13 KR KR1020177012838A patent/KR102569226B1/ko active Active
-
2017
- 2017-04-05 IL IL251595A patent/IL251595B/en unknown
- 2017-04-27 US US15/498,631 patent/US9981989B2/en active Active
-
2018
- 2018-04-12 US US15/951,302 patent/US10196405B2/en active Active
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