JP2019514878A5 - - Google Patents
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- Publication number
- JP2019514878A5 JP2019514878A5 JP2018555185A JP2018555185A JP2019514878A5 JP 2019514878 A5 JP2019514878 A5 JP 2019514878A5 JP 2018555185 A JP2018555185 A JP 2018555185A JP 2018555185 A JP2018555185 A JP 2018555185A JP 2019514878 A5 JP2019514878 A5 JP 2019514878A5
- Authority
- JP
- Japan
- Prior art keywords
- dimethyl
- methyl
- oxy
- amino
- alkyl
- 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.)
- Pending
Links
- -1 cyano, hydroxyl Chemical group 0.000 claims 50
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 31
- IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 claims 23
- 125000000217 alkyl group Chemical group 0.000 claims 20
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 20
- 150000003839 salts Chemical class 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 17
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 14
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 12
- 239000003814 drug Substances 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 101001109137 Homo sapiens Receptor-interacting serine/threonine-protein kinase 2 Proteins 0.000 claims 10
- 102100022502 Receptor-interacting serine/threonine-protein kinase 2 Human genes 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 9
- 125000005647 linker group Chemical group 0.000 claims 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- 201000010099 disease Diseases 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 125000005843 halogen group Chemical group 0.000 claims 7
- 230000001404 mediated effect Effects 0.000 claims 7
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000004429 atom Chemical group 0.000 claims 6
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical group C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 229940124597 therapeutic agent Drugs 0.000 claims 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical group [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 3
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 3
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 3
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 125000000437 thiazol-2-yl group Chemical group [H]C1=C([H])N=C(*)S1 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000004939 6-pyridyl group Chemical group N1=CC=CC=C1* 0.000 claims 1
- 101000733257 Homo sapiens Rho guanine nucleotide exchange factor 28 Proteins 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000005036 alkoxyphenyl group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- PCDHSSHKDZYLLI-UHFFFAOYSA-N butan-1-one Chemical compound CCC[C]=O PCDHSSHKDZYLLI-UHFFFAOYSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 229940043355 kinase inhibitor Drugs 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662324944P | 2016-04-20 | 2016-04-20 | |
| US62/324,944 | 2016-04-20 | ||
| PCT/EP2017/059090 WO2017182418A1 (en) | 2016-04-20 | 2017-04-18 | Conjugates comprising ripk2 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019514878A JP2019514878A (ja) | 2019-06-06 |
| JP2019514878A5 true JP2019514878A5 (https=) | 2020-05-28 |
Family
ID=58548715
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018555185A Pending JP2019514878A (ja) | 2016-04-20 | 2017-04-18 | Ｒｉｐｋ２阻害剤を含むコンジュゲート |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US10781205B2 (https=) |
| EP (1) | EP3445759A1 (https=) |
| JP (1) | JP2019514878A (https=) |
| KR (1) | KR20180135038A (https=) |
| CN (1) | CN109311867A (https=) |
| AU (1) | AU2017253560B2 (https=) |
| BR (1) | BR112018071408A2 (https=) |
| CA (1) | CA3020792A1 (https=) |
| RU (1) | RU2018134981A (https=) |
| WO (1) | WO2017182418A1 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201506872D0 (en) * | 2015-04-22 | 2015-06-03 | Ge Oil & Gas Uk Ltd | Novel compounds |
| PT3500299T (pt) | 2016-08-19 | 2024-02-21 | Beigene Switzerland Gmbh | Combinação de zanubrutinib com um anticorpo anti-cd20 ou anti-pd-1 para utilização no tratamento do cancro |
| TW202515616A (zh) | 2017-06-26 | 2025-04-16 | 英屬開曼群島商百濟神州有限公司 | 抗pd-1抗體或其抗原結合片段在製備治療用於患有肝細胞癌(hcc)之藥物的用途 |
| CN111801334B (zh) | 2017-11-29 | 2023-06-09 | 百济神州瑞士有限责任公司 | 使用包含btk抑制剂的组合治疗惰性或侵袭性b-细胞淋巴瘤 |
| JP2021527137A (ja) * | 2018-06-13 | 2021-10-11 | アンフィスタ セラピューティクス リミテッド | Ｒｐｎ１１を標的化するための二機能性分子 |
| WO2020027225A1 (ja) | 2018-07-31 | 2020-02-06 | ファイメクス株式会社 | 複素環化合物 |
| WO2020043122A1 (zh) * | 2018-08-28 | 2020-03-05 | 南京明德新药研发有限公司 | 作为rip2激酶抑制剂的喹唑啉类衍生物 |
| KR20210141554A (ko) | 2019-03-21 | 2021-11-23 | 코디악 바이오사이언시즈, 인크. | 세포외 소포 접합체 및 이의 용도 |
| WO2020191369A1 (en) | 2019-03-21 | 2020-09-24 | Codiak Biosciences, Inc. | Process for preparing extracellular vesicles |
| JP2021024787A (ja) | 2019-07-31 | 2021-02-22 | ファイメクス株式会社 | 複素環化合物 |
| WO2021020585A1 (ja) | 2019-07-31 | 2021-02-04 | ファイメクス株式会社 | 複素環化合物 |
| WO2021237100A1 (en) | 2020-05-21 | 2021-11-25 | Codiak Biosciences, Inc. | Methods of targeting extracellular vesicles to lung |
| US20240241020A1 (en) | 2020-09-23 | 2024-07-18 | Lonza Sales Ag | Process for preparing extracellular vesicles |
| US20240165243A1 (en) | 2021-02-10 | 2024-05-23 | Beigene Switzerland Gmbh | Egfr degraders and methods of use |
| CN114014890A (zh) * | 2021-03-12 | 2022-02-08 | 爱科诺生物医药(香港)有限公司 | 具有rip2激酶抑制活性的化合物，包含其的药物组合物，及其应用 |
| AU2022424178A1 (en) | 2021-12-30 | 2024-07-11 | Beone Medicines I Gmbh | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| WO2024071371A1 (ja) * | 2022-09-30 | 2024-04-04 | ユビエンス株式会社 | 複素環式化合物 |
| WO2024240858A1 (en) | 2023-05-23 | 2024-11-28 | Valerio Therapeutics | Protac molecules directed against dna damage repair system and uses thereof |
| AU2024281173A1 (en) | 2023-05-31 | 2025-12-04 | Beone Medicines I Gmbh | Compounds for the degradation of egfr kinase |
| WO2025092821A1 (zh) * | 2023-11-01 | 2025-05-08 | 成都赜灵生物医药科技有限公司 | 喹唑啉衍生物类ripk2抑制剂及其用途 |
| WO2025126115A1 (en) | 2023-12-13 | 2025-06-19 | Beigene Switzerland Gmbh | Degradation of irak4 by conjugation of irak4 inhibitors with e3 ligase ligands and methods of use |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20110220A1 (es) | 2006-08-02 | 2011-04-11 | Novartis Ag | DERIVADOS DE 2-OXO-ETIL-AMINO-PROPIONAMIDA-PIRROLIDIN-2-IL-SUSTITUIDOS COMO INHIBIDORES DEL ENLACE DE LA PROTEINA Smac AL INHIBIDOR DE LA PROTEINA DE APOPTOSIS |
| WO2008128171A2 (en) | 2007-04-13 | 2008-10-23 | The Regents Of The University Of Michigan | Diazo bicyclic smac mimetics and the uses thereof |
| US9750729B2 (en) * | 2008-05-16 | 2017-09-05 | Dana-Farber Cancer Institute, Inc. | Immunomodulation by IAP inhibitors |
| PE20121132A1 (es) | 2009-08-12 | 2012-09-04 | Novartis Ag | Formulaciones orales solidas y formas cristalinas de un inhibidor de la proteina de apoptosis |
| EP2566477B1 (en) | 2010-05-07 | 2015-09-02 | GlaxoSmithKline Intellectual Property Development Limited | Amino-quinolines as kinase inhibitors |
| UY33549A (es) | 2010-08-10 | 2012-01-31 | Glaxo Group Ltd | Quinolil aminas como agentes inhibidores de las quinasas |
| SG192769A1 (en) | 2011-03-04 | 2013-09-30 | Glaxosmithkline Ip No 2 Ltd | Amino-quinolines as kinase inhibitors |
| GB201106817D0 (en) | 2011-04-21 | 2011-06-01 | Astex Therapeutics Ltd | New compound |
| TWI547494B (zh) * | 2011-08-18 | 2016-09-01 | 葛蘭素史克智慧財產發展有限公司 | 作為激酶抑制劑之胺基喹唑啉類 |
| CA2861066C (en) | 2012-01-12 | 2024-01-02 | Yale University | Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an e3 ubiquitin ligase |
| ES2654623T3 (es) | 2012-08-23 | 2018-02-14 | The Regents Of The University Of Michigan | Inhibidores bivalentes de proteínas IAP y métodos terapéuticos que los usan |
| AR092530A1 (es) | 2012-09-13 | 2015-04-22 | Glaxosmithkline Llc | Compuesto de amino-quinolina, composicion farmaceutica que lo comprende y uso de dicho compuesto para la preparacion de un medicamento |
| WO2014047024A1 (en) | 2012-09-18 | 2014-03-27 | Bristol-Myers Squibb Company | Iap antagonists |
| US9603889B2 (en) | 2012-10-02 | 2017-03-28 | Bristol-Myers Squibb Company | IAP antagonists |
| GB201218850D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| GB201218864D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| GB201218862D0 (en) | 2012-10-19 | 2012-12-05 | Astex Therapeutics Ltd | Bicyclic heterocycle compounds and their uses in therapy |
| AU2013357493A1 (en) | 2012-12-11 | 2015-04-30 | F. Hoffmann-La Roche Ag | Dimeric compounds |
| KR101335240B1 (ko) | 2012-12-13 | 2013-11-29 | 전호건 | 수평 연속 방식의 탄화장치 |
| RU2662810C2 (ru) | 2013-02-21 | 2018-07-31 | Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед | Хиназолины в качестве ингибиторов киназы |
| GB201311891D0 (en) * | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| GB201311888D0 (en) * | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| ES2883289T3 (es) | 2013-12-20 | 2021-12-07 | Astex Therapeutics Ltd | Compuestos heterocíclicos bicíclicos y sus usos en terapia |
| GB201506871D0 (en) * | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201506872D0 (en) * | 2015-04-22 | 2015-06-03 | Ge Oil & Gas Uk Ltd | Novel compounds |
-
2017
- 2017-04-18 CA CA3020792A patent/CA3020792A1/en not_active Abandoned
- 2017-04-18 KR KR1020187033631A patent/KR20180135038A/ko not_active Withdrawn
- 2017-04-18 WO PCT/EP2017/059090 patent/WO2017182418A1/en not_active Ceased
- 2017-04-18 AU AU2017253560A patent/AU2017253560B2/en not_active Ceased
- 2017-04-18 US US16/094,564 patent/US10781205B2/en not_active Expired - Fee Related
- 2017-04-18 CN CN201780036566.1A patent/CN109311867A/zh active Pending
- 2017-04-18 EP EP17717721.9A patent/EP3445759A1/en not_active Withdrawn
- 2017-04-18 JP JP2018555185A patent/JP2019514878A/ja active Pending
- 2017-04-18 RU RU2018134981A patent/RU2018134981A/ru not_active Application Discontinuation
- 2017-04-18 BR BR112018071408A patent/BR112018071408A2/pt not_active Application Discontinuation
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