JPWO2019201283A5 - - Google Patents
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- Publication number
- JPWO2019201283A5 JPWO2019201283A5 JP2021506031A JP2021506031A JPWO2019201283A5 JP WO2019201283 A5 JPWO2019201283 A5 JP WO2019201283A5 JP 2021506031 A JP2021506031 A JP 2021506031A JP 2021506031 A JP2021506031 A JP 2021506031A JP WO2019201283 A5 JPWO2019201283 A5 JP WO2019201283A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- independently
- heteroaryl
- heterocyclyl
- composition
- 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
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- 150000001875 compounds Chemical class 0.000 claims description 54
- 125000001072 heteroaryl group Chemical group 0.000 claims description 46
- 125000000623 heterocyclic group Chemical group 0.000 claims description 44
- 229910052739 hydrogen Chemical group 0.000 claims description 32
- 239000001257 hydrogen Chemical group 0.000 claims description 32
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 32
- 239000000203 mixture Substances 0.000 claims description 31
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 30
- 125000003107 substituted aryl group Chemical group 0.000 claims description 30
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 28
- 125000005843 halogen group Chemical group 0.000 claims description 22
- 150000003839 salts Chemical class 0.000 claims description 20
- 229910052757 nitrogen Inorganic materials 0.000 claims description 17
- 125000001188 haloalkyl group Chemical group 0.000 claims description 16
- 125000004426 substituted alkynyl group Chemical group 0.000 claims description 14
- 125000005017 substituted alkenyl group Chemical group 0.000 claims description 13
- 239000002246 antineoplastic agent Substances 0.000 claims description 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 12
- 125000000217 alkyl group Chemical group 0.000 claims description 10
- 125000003118 aryl group Chemical group 0.000 claims description 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
- 238000001959 radiotherapy Methods 0.000 claims description 10
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 8
- 125000002619 bicyclic group Chemical group 0.000 claims description 8
- 208000035475 disorder Diseases 0.000 claims description 8
- 125000004450 alkenylene group Chemical group 0.000 claims description 6
- 125000002947 alkylene group Chemical group 0.000 claims description 6
- 125000004419 alkynylene group Chemical group 0.000 claims description 6
- 125000004122 cyclic group Chemical group 0.000 claims description 6
- 125000000262 haloalkenyl group Chemical group 0.000 claims description 6
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 6
- 229910052760 oxygen Inorganic materials 0.000 claims description 6
- 229910052717 sulfur Inorganic materials 0.000 claims description 6
- 125000004429 atom Chemical group 0.000 claims description 4
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 125000002950 monocyclic group Chemical group 0.000 claims description 4
- 239000012453 solvate Substances 0.000 claims description 4
- XDXDZDZNSLXDNA-TZNDIEGXSA-N Idarubicin Chemical compound C1[C@H](N)[C@H](O)[C@H](C)O[C@H]1O[C@@H]1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2C[C@@](O)(C(C)=O)C1 XDXDZDZNSLXDNA-TZNDIEGXSA-N 0.000 claims description 2
- XDXDZDZNSLXDNA-UHFFFAOYSA-N Idarubicin Natural products C1C(N)C(O)C(C)OC1OC1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2CC(O)(C(C)=O)C1 XDXDZDZNSLXDNA-UHFFFAOYSA-N 0.000 claims description 2
- 239000012661 PARP inhibitor Substances 0.000 claims description 2
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 claims description 2
- 230000000259 anti-tumor effect Effects 0.000 claims description 2
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 claims description 2
- 239000003124 biologic agent Substances 0.000 claims description 2
- -1 calikeamycin Substances 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 229960004562 carboplatin Drugs 0.000 claims description 2
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims description 2
- 229960004316 cisplatin Drugs 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 229960000908 idarubicin Drugs 0.000 claims description 2
- 238000009169 immunotherapy Methods 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 2
- 229960001756 oxaliplatin Drugs 0.000 claims description 2
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims description 2
- 239000008177 pharmaceutical agent Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000005717 substituted cycloalkylene group Chemical group 0.000 claims description 2
- 230000009885 systemic effect Effects 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 229960000653 valrubicin Drugs 0.000 claims description 2
- ZOCKGBMQLCSHFP-KQRAQHLDSA-N valrubicin Chemical compound O([C@H]1C[C@](CC2=C(O)C=3C(=O)C4=CC=CC(OC)=C4C(=O)C=3C(O)=C21)(O)C(=O)COC(=O)CCCC)[C@H]1C[C@H](NC(=O)C(F)(F)F)[C@H](O)[C@H](C)O1 ZOCKGBMQLCSHFP-KQRAQHLDSA-N 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 18
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810359447.6A CN110386932A (zh) | 2018-04-20 | 2018-04-20 | 用于抗肿瘤疗法中的双重atm和dna-pk抑制剂 |
| CN201810359447.6 | 2018-04-20 | ||
| US201862665296P | 2018-05-01 | 2018-05-01 | |
| US62/665,296 | 2018-05-01 | ||
| PCT/CN2019/083104 WO2019201283A1 (en) | 2018-04-20 | 2019-04-17 | Dual atm and dna-pk inhibitors for use in anti-tumor therapy |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021522316A JP2021522316A (ja) | 2021-08-30 |
| JPWO2019201283A5 true JPWO2019201283A5 (https=) | 2022-04-22 |
| JP2021522316A5 JP2021522316A5 (https=) | 2022-04-22 |
| JP7366996B2 JP7366996B2 (ja) | 2023-10-23 |
Family
ID=68283636
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021506031A Active JP7366996B2 (ja) | 2018-04-20 | 2019-04-17 | 抗腫瘍療法で使用するためのデュアルａｔｍ及びｄｎａ－ｐｋ阻害剤 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US12187742B2 (https=) |
| EP (2) | EP3784671B1 (https=) |
| JP (1) | JP7366996B2 (https=) |
| KR (1) | KR20210027251A (https=) |
| CN (2) | CN110386932A (https=) |
| BR (1) | BR112020021323A2 (https=) |
| CA (1) | CA3096732A1 (https=) |
| MA (1) | MA52364A (https=) |
| MX (1) | MX2020010942A (https=) |
| SG (1) | SG11202010212RA (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10118890B2 (en) | 2014-10-10 | 2018-11-06 | The Research Foundation For The State University Of New York | Trifluoromethoxylation of arenes via intramolecular trifluoromethoxy group migration |
| WO2019201283A1 (en) | 2018-04-20 | 2019-10-24 | Xrad Therapeutics, Inc. | Dual atm and dna-pk inhibitors for use in anti-tumor therapy |
| WO2021022078A1 (en) * | 2019-07-30 | 2021-02-04 | Xrad Therapeutics, Inc. | Dual atm and dna-pk inhibitors for use in anti-tumor therapy |
| WO2021098734A1 (zh) * | 2019-11-19 | 2021-05-27 | 南京明德新药研发有限公司 | 作为atm抑制剂的有取代的喹啉吡咯酮类合物及其应用 |
| AU2020385513A1 (en) * | 2019-11-22 | 2022-07-14 | Medshine Discovery Inc. | Pyrimidopyrrole spiro compounds and derivatives thereof as DNA-PK inhibitors |
| CN113121538B (zh) * | 2019-12-31 | 2023-04-21 | 成都百裕制药股份有限公司 | 呋喃衍生物及其在医药上的应用 |
| CN115380031A (zh) * | 2020-03-30 | 2022-11-22 | 南京明德新药研发有限公司 | 作为atm抑制剂的喹啉并吡咯烷-2-酮类化合物的晶型及其应用 |
| CN114634521A (zh) * | 2020-12-15 | 2022-06-17 | 首药控股(北京)股份有限公司 | Dna-pk选择性抑制剂及其制备方法和用途 |
| WO2024186805A1 (en) * | 2023-03-06 | 2024-09-12 | Xrad Therapeutics, Inc. | Methods of treating cancer |
| WO2025247391A1 (en) * | 2024-05-31 | 2025-12-04 | Hutchmed Limited | Novel pi3k and/or pikk inhibitors, antibody-drug conjugates comprising the same and uses thereof |
| WO2026006954A1 (en) * | 2024-07-01 | 2026-01-08 | Xrad Holding Cayman Limited | Dual atm and dna-pk inhibitors for use in anti-tumor therapy |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2589935A1 (en) | 2004-12-09 | 2006-06-15 | Regents Of The University Of Minnesota | Nucleosides with antiviral and anticancer activity |
| DK2032535T3 (da) | 2006-06-01 | 2012-11-05 | Sanofi Sa | Spiro-cycliske nitriler som protease-inhibitorer |
| ATE543819T1 (de) | 2006-10-19 | 2012-02-15 | Signal Pharm Llc | Heteroarylverbindungen, zusammensetzungen daraus und behandlungsverfahren damit |
| EP2303890A4 (en) * | 2008-06-19 | 2012-04-11 | Progenics Pharm Inc | INHIBITORS OF PHOSPHATIDYLINOSITE-3-KINASE |
| CN102256966B (zh) * | 2008-10-17 | 2016-02-10 | 白头生物医学研究所 | 可溶性mTOR复合物和其调节剂 |
| CN102803259A (zh) | 2009-06-04 | 2012-11-28 | 诺瓦提斯公司 | 用于治疗增殖性疾病的1H-咪唑并[4,5-c]喹啉酮化合物 |
| EP2509980A1 (en) | 2009-12-07 | 2012-10-17 | Boehringer Ingelheim International GmbH | Heterocyclic compounds containing an indole core |
| CN102399218A (zh) | 2010-09-16 | 2012-04-04 | 和记黄埔医药（上海）有限公司 | 一类并合三杂环及其作为pi3k抑制剂的用途 |
| JP2014504286A (ja) | 2010-12-06 | 2014-02-20 | ピラマル エンタープライジーズ リミテッド | 置換イミダゾキノリン誘導体 |
| JO3003B1 (ar) | 2011-01-14 | 2016-09-05 | Lilly Co Eli | مركب أيميدازو [4، 5 -c ] كينولين-2- واحد واستخدامه كمثبط كيناز PI3/mtor |
| AR089929A1 (es) | 2012-02-10 | 2014-10-01 | Actelion Pharmaceuticals Ltd | Proceso para manufacturar un derivado de naftiridina |
| ES2704744T3 (es) | 2012-06-13 | 2019-03-19 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| CN103936762B (zh) * | 2013-01-17 | 2016-02-24 | 上海汇伦生命科技有限公司 | 吗啉并喹啉类化合物，其制备方法和用途 |
| CN103880844A (zh) | 2014-04-09 | 2014-06-25 | 彭正中 | 一种喹啉酮类新化合物及其制备方法与用途 |
| NO2714752T3 (https=) * | 2014-05-08 | 2018-04-21 | ||
| CN105461711B (zh) * | 2014-06-17 | 2018-11-06 | 正大天晴药业集团股份有限公司 | 作为PI3K抑制剂的吡啶并[1,2-a]嘧啶酮类似物 |
| AU2015276699B2 (en) * | 2014-06-17 | 2019-10-10 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Pyridino[1,2-a]pyrimidone analogue used as PI3K inhibitor |
| CN105461712B (zh) * | 2014-06-17 | 2019-01-29 | 上海嘉坦医药科技有限公司 | 作为mTOR/PI3K抑制剂的吡啶并[1,2-a]嘧啶酮类似物 |
| BR112016029825B1 (pt) | 2014-06-17 | 2020-10-27 | Cisen Pharmaceutical Co., Ltd. | composto |
| US10189810B2 (en) | 2014-09-17 | 2019-01-29 | Verseon Corporation | Pyrazolyl-substituted pyridone compounds as serine protease inhibitors |
| PL3560924T3 (pl) | 2015-04-02 | 2021-10-11 | Merck Patent Gmbh | Imidazolonylochinoliny i ich zastosowanie jako inhibitorów kinazy atm |
| WO2016186453A1 (en) * | 2015-05-20 | 2016-11-24 | Kainos Medicine, Inc. | Quinoline derivatives as bromodomain inhibitors |
| GB201519406D0 (en) * | 2015-11-03 | 2015-12-16 | Astrazeneca Ab | Imidazo[4,5-c]quinolin-2-one compounds and their use in treating cancer |
| GB201519568D0 (en) | 2015-11-05 | 2015-12-23 | Astrazeneca Ab | Imidazo[4,5-c]quinolin-2-one compounds and their use in treating cancer |
| WO2017127430A1 (en) | 2016-01-20 | 2017-07-27 | Biogen Ma Inc. | Irak4 inhibiting agents |
| WO2017162611A1 (en) * | 2016-03-21 | 2017-09-28 | Astrazeneca Ab | Quinoline-3-carboxamide compounds and their use in treating cancer |
| TWI696615B (zh) | 2016-05-05 | 2020-06-21 | 瑞士商伊蘭科動物健康公司 | 雜芳基-1,2,4-三唑及雜芳基-三唑化合物 |
| GB201608227D0 (en) * | 2016-05-11 | 2016-06-22 | Astrazeneca Ab | Imidazo[4,5-c]quinolin-2-one compounds and their use in treating cancer |
| MX391410B (es) * | 2018-09-30 | 2025-03-21 | Medshine Discovery Inc | Derivados de quinolino-pirrolidin-2-ona como inhibidores del gen mutado de ataxia telangiectasia (atm) y el uso de los mismos en el tratamiento de tumores sólidos. |
| WO2021022078A1 (en) | 2019-07-30 | 2021-02-04 | Xrad Therapeutics, Inc. | Dual atm and dna-pk inhibitors for use in anti-tumor therapy |
-
2018
- 2018-04-20 CN CN201810359447.6A patent/CN110386932A/zh active Pending
-
2019
- 2019-04-17 EP EP19787882.0A patent/EP3784671B1/en active Active
- 2019-04-17 MA MA052364A patent/MA52364A/fr unknown
- 2019-04-17 JP JP2021506031A patent/JP7366996B2/ja active Active
- 2019-04-17 KR KR1020207033463A patent/KR20210027251A/ko not_active Withdrawn
- 2019-04-17 BR BR112020021323-3A patent/BR112020021323A2/pt not_active IP Right Cessation
- 2019-04-17 SG SG11202010212RA patent/SG11202010212RA/en unknown
- 2019-04-17 EP EP23202655.9A patent/EP4327877A3/en not_active Withdrawn
- 2019-04-17 CA CA3096732A patent/CA3096732A1/en active Pending
- 2019-04-17 CN CN201980040733.9A patent/CN112469720B/zh active Active
- 2019-04-17 MX MX2020010942A patent/MX2020010942A/es unknown
-
2020
- 2020-10-19 US US17/074,425 patent/US12187742B2/en active Active
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