JP2023112696A5 - - Google Patents
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- Publication number
- JP2023112696A5 JP2023112696A5 JP2023013779A JP2023013779A JP2023112696A5 JP 2023112696 A5 JP2023112696 A5 JP 2023112696A5 JP 2023013779 A JP2023013779 A JP 2023013779A JP 2023013779 A JP2023013779 A JP 2023013779A JP 2023112696 A5 JP2023112696 A5 JP 2023112696A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- salt
- preparing
- reacting
- acid
- 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 21
- 238000000034 method Methods 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 12
- 239000003054 catalyst Substances 0.000 claims 5
- 239000003638 chemical reducing agent Substances 0.000 claims 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims 3
- 239000002904 solvent Substances 0.000 claims 3
- -1 (R)-2-(4-(2-hydroxy-8-(trifluoromethyl)-5H-chromeno[4,3-c]quinolin-5-yl)phenoxy)ethane-1,1-diol Chemical compound 0.000 claims 2
- WMFOQBRAJBCJND-UHFFFAOYSA-M Lithium hydroxide Chemical compound [Li+].[OH-] WMFOQBRAJBCJND-UHFFFAOYSA-M 0.000 claims 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- UORVGPXVDQYIDP-UHFFFAOYSA-N borane Chemical compound B UORVGPXVDQYIDP-UHFFFAOYSA-N 0.000 claims 2
- FJDQFPXHSGXQBY-UHFFFAOYSA-L caesium carbonate Chemical compound [Cs+].[Cs+].[O-]C([O-])=O FJDQFPXHSGXQBY-UHFFFAOYSA-L 0.000 claims 2
- YCIMNLLNPGFGHC-UHFFFAOYSA-N catechol Chemical compound OC1=CC=CC=C1O YCIMNLLNPGFGHC-UHFFFAOYSA-N 0.000 claims 2
- GGSUCNLOZRCGPQ-UHFFFAOYSA-N diethylaniline Chemical compound CCN(CC)C1=CC=CC=C1 GGSUCNLOZRCGPQ-UHFFFAOYSA-N 0.000 claims 2
- 239000003446 ligand Substances 0.000 claims 2
- 239000012279 sodium borohydride Substances 0.000 claims 2
- 229910000033 sodium borohydride Inorganic materials 0.000 claims 2
- MFRIHAYPQRLWNB-UHFFFAOYSA-N sodium tert-butoxide Chemical compound [Na+].CC(C)(C)[O-] MFRIHAYPQRLWNB-UHFFFAOYSA-N 0.000 claims 2
- 229910052723 transition metal Inorganic materials 0.000 claims 2
- 150000003624 transition metals Chemical class 0.000 claims 2
- GQHTUMJGOHRCHB-UHFFFAOYSA-N 2,3,4,6,7,8,9,10-octahydropyrimido[1,2-a]azepine Chemical compound C1CCCCN2CCCN=C21 GQHTUMJGOHRCHB-UHFFFAOYSA-N 0.000 claims 1
- QMMFVYPAHWMCMS-UHFFFAOYSA-N Dimethyl sulfide Chemical compound CSC QMMFVYPAHWMCMS-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 229910010084 LiAlH4 Inorganic materials 0.000 claims 1
- 239000012448 Lithium borohydride Substances 0.000 claims 1
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 1
- 125000006241 alcohol protecting group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 229910000085 borane Inorganic materials 0.000 claims 1
- NNTOJPXOCKCMKR-UHFFFAOYSA-N boron;pyridine Chemical compound [B].C1=CC=NC=C1 NNTOJPXOCKCMKR-UHFFFAOYSA-N 0.000 claims 1
- 229910000024 caesium carbonate Inorganic materials 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 238000006880 cross-coupling reaction Methods 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 239000012280 lithium aluminium hydride Substances 0.000 claims 1
- 229940098779 methanesulfonic acid Drugs 0.000 claims 1
- ZRLVQFQTCMUIRM-UHFFFAOYSA-N potassium;2-methylbutan-2-olate Chemical compound [K+].CCC(C)(C)[O-] ZRLVQFQTCMUIRM-UHFFFAOYSA-N 0.000 claims 1
- 229910000104 sodium hydride Inorganic materials 0.000 claims 1
- 239000012321 sodium triacetoxyborohydride Substances 0.000 claims 1
- CGRKYEALWSRNJS-UHFFFAOYSA-N sodium;2-methylbutan-2-olate Chemical compound [Na+].CCC(C)(C)[O-] CGRKYEALWSRNJS-UHFFFAOYSA-N 0.000 claims 1
- 235000011149 sulphuric acid Nutrition 0.000 claims 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical class CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 1
- YNJBWRMUSHSURL-UHFFFAOYSA-N trichloroacetic acid Chemical compound OC(=O)C(Cl)(Cl)Cl YNJBWRMUSHSURL-UHFFFAOYSA-N 0.000 claims 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-N triflic acid Chemical compound OS(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-N 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023138310A JP7805336B2 (ja) | 2022-02-01 | 2023-08-28 | 選択的エストロゲン受容体分解剤の調製のためのプロセス |
| JP2025146941A JP2025183283A (ja) | 2022-02-01 | 2025-09-04 | 選択的エストロゲン受容体分解剤の調製のためのプロセス |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202263305520P | 2022-02-01 | 2022-02-01 | |
| US63/305,520 | 2022-02-01 | ||
| US202263409060P | 2022-09-22 | 2022-09-22 | |
| US63/409,060 | 2022-09-22 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023138310A Division JP7805336B2 (ja) | 2022-02-01 | 2023-08-28 | 選択的エストロゲン受容体分解剤の調製のためのプロセス |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023112696A JP2023112696A (ja) | 2023-08-14 |
| JP2023112696A5 true JP2023112696A5 (https=) | 2023-09-05 |
| JP7387926B2 JP7387926B2 (ja) | 2023-11-28 |
Family
ID=85382684
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023013779A Active JP7387926B2 (ja) | 2022-02-01 | 2023-02-01 | 選択的エストロゲン受容体分解剤の調製のためのプロセス |
| JP2023138310A Active JP7805336B2 (ja) | 2022-02-01 | 2023-08-28 | 選択的エストロゲン受容体分解剤の調製のためのプロセス |
| JP2025146941A Pending JP2025183283A (ja) | 2022-02-01 | 2025-09-04 | 選択的エストロゲン受容体分解剤の調製のためのプロセス |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023138310A Active JP7805336B2 (ja) | 2022-02-01 | 2023-08-28 | 選択的エストロゲン受容体分解剤の調製のためのプロセス |
| JP2025146941A Pending JP2025183283A (ja) | 2022-02-01 | 2025-09-04 | 選択的エストロゲン受容体分解剤の調製のためのプロセス |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US11926634B2 (https=) |
| EP (1) | EP4472982A1 (https=) |
| JP (3) | JP7387926B2 (https=) |
| KR (2) | KR20250006312A (https=) |
| AU (2) | AU2023216654B2 (https=) |
| CA (1) | CA3243621A1 (https=) |
| CO (1) | CO2024009411A2 (https=) |
| CR (1) | CR20240283A (https=) |
| DO (1) | DOP2024000150A (https=) |
| IL (1) | IL313886A (https=) |
| JO (1) | JOP20240169A1 (https=) |
| MX (1) | MX2024009453A (https=) |
| PE (1) | PE20241731A1 (https=) |
| TW (2) | TWI863110B (https=) |
| WO (1) | WO2023150056A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2020137965A (ja) * | 2019-03-01 | 2020-09-03 | 株式会社三洋物産 | 遊技機 |
| US20240199629A1 (en) * | 2022-02-01 | 2024-06-20 | Eli Lilly And Company | Processes for the preparation of selective estrogen receptor degraders |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1709021B1 (en) | 2004-01-22 | 2010-08-04 | Eli Lilly And Company | Selective estrogen receptor modulators for the treatment of vasomotor symptoms |
| US20080221163A1 (en) | 2005-01-18 | 2008-09-11 | Jeffrey Alan Dodge | Selective Estrogen Receptor Modulators |
| EP2343287A1 (en) * | 2009-12-10 | 2011-07-13 | Almirall, S.A. | New 2-aminothiadiazole derivatives |
| CN103582637B (zh) * | 2011-05-17 | 2015-08-12 | 弗·哈夫曼-拉罗切有限公司 | 酪氨酸激酶抑制剂 |
| BR112015030595A2 (pt) | 2013-06-19 | 2017-07-25 | Seragon Pharmaceuticals Inc | moduladores de receptor de estrogênio de azetidina e usos dos mesmos |
| CN107406424B (zh) | 2014-12-18 | 2020-08-25 | 豪夫迈·罗氏有限公司 | 雌激素受体调节剂及其用途 |
| MD3820874T2 (ro) | 2018-07-12 | 2023-05-31 | Lilly Co Eli | Degradanți selectivi ai receptorului estrogen |
| TWI702219B (zh) | 2018-07-12 | 2020-08-21 | 美商美國禮來大藥廠 | 選擇性雌激素受體降解劑 |
| US11014915B2 (en) * | 2019-07-22 | 2021-05-25 | Sun Pharma Advanced Research Company Limited | Selective estrogen receptor degrader |
| CN115175679A (zh) | 2020-03-06 | 2022-10-11 | 奥列马制药公司 | 治疗雌激素受体相关疾病的方法 |
| CN115867282B (zh) * | 2020-03-26 | 2025-05-27 | 奈克斯拉制药英国有限公司 | 用于抗癌的5-氨基-8-(4-吡啶基)-[1,2,4]三唑并[4,3-c]嘧啶-3-酮化合物 |
| AR123185A1 (es) * | 2020-08-10 | 2022-11-09 | Novartis Ag | Compuestos y composiciones para inhibir ezh2 |
| TWI837605B (zh) | 2021-03-09 | 2024-04-01 | 美商美國禮來大藥廠 | 使用serd組合給藥方案治療癌症之方法 |
| TWI894443B (zh) | 2021-03-16 | 2025-08-21 | 美商美國禮來大藥廠 | 選擇性雌激素受體降解劑 |
-
2023
- 2023-01-27 EP EP23707540.3A patent/EP4472982A1/en active Pending
- 2023-01-27 PE PE2024001567A patent/PE20241731A1/es unknown
- 2023-01-27 WO PCT/US2023/011671 patent/WO2023150056A1/en not_active Ceased
- 2023-01-27 AU AU2023216654A patent/AU2023216654B2/en active Active
- 2023-01-27 CA CA3243621A patent/CA3243621A1/en active Pending
- 2023-01-27 MX MX2024009453A patent/MX2024009453A/es unknown
- 2023-01-27 CR CR20240283A patent/CR20240283A/es unknown
- 2023-01-27 KR KR1020247041076A patent/KR20250006312A/ko active Pending
- 2023-01-27 KR KR1020247028876A patent/KR102743629B1/ko active Active
- 2023-01-27 US US18/160,457 patent/US11926634B2/en active Active
- 2023-01-27 IL IL313886A patent/IL313886A/en unknown
- 2023-02-01 TW TW112103450A patent/TWI863110B/zh active
- 2023-02-01 TW TW113140271A patent/TW202523669A/zh unknown
- 2023-02-01 JP JP2023013779A patent/JP7387926B2/ja active Active
- 2023-08-28 JP JP2023138310A patent/JP7805336B2/ja active Active
-
2024
- 2024-07-16 CO CONC2024/0009411A patent/CO2024009411A2/es unknown
- 2024-07-30 JO JOJO/P/2024/0169A patent/JOP20240169A1/ar unknown
- 2024-07-31 DO DO2024000150A patent/DOP2024000150A/es unknown
-
2025
- 2025-09-04 JP JP2025146941A patent/JP2025183283A/ja active Pending
- 2025-09-16 AU AU2025234145A patent/AU2025234145A1/en active Pending
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