TWI863110B - 用於製備選擇性雌激素受體降解劑之方法 - Google Patents

用於製備選擇性雌激素受體降解劑之方法 Download PDF

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Publication number
TWI863110B
TWI863110B TW112103450A TW112103450A TWI863110B TW I863110 B TWI863110 B TW I863110B TW 112103450 A TW112103450 A TW 112103450A TW 112103450 A TW112103450 A TW 112103450A TW I863110 B TWI863110 B TW I863110B
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TW
Taiwan
Prior art keywords
compound
salt
formula
trifluoromethyl
phenyl
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TW112103450A
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English (en)
Chinese (zh)
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TW202346300A (zh
Inventor
德爾加多 阿隆索 喬瑟 阿蓋爾
道格拉斯 派頓 可吉爾
尼可拉斯 安德魯 馬格努斯
寶麗斯 阿諾多維奇 茲凱斯
麥 坎 古元 霍克
陸愈
大衛 麥可 雷米克
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美商美國禮來大藥廠
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4741Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having oxygen as a ring hetero atom, e.g. tubocuraran derivatives, noscapine, bicuculline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B01PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01JCHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J23/00Catalysts comprising metals or metal oxides or hydroxides, not provided for in group B01J21/00
    • B01J23/38Catalysts comprising metals or metal oxides or hydroxides, not provided for in group B01J21/00 of noble metals
    • B01J23/40Catalysts comprising metals or metal oxides or hydroxides, not provided for in group B01J21/00 of noble metals of the platinum group metals
    • B01J23/44Palladium
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/022Boron compounds without C-boron linkages

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Materials Engineering (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Steroid Compounds (AREA)
TW112103450A 2022-02-01 2023-02-01 用於製備選擇性雌激素受體降解劑之方法 TWI863110B (zh)

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

Publications (2)

Publication Number Publication Date
TW202346300A TW202346300A (zh) 2023-12-01
TWI863110B true TWI863110B (zh) 2024-11-21

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TW112103450A TWI863110B (zh) 2022-02-01 2023-02-01 用於製備選擇性雌激素受體降解劑之方法
TW113140271A TW202523669A (zh) 2022-02-01 2023-02-01 用於製備選擇性雌激素受體降解劑之方法

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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)

* Cited by examiner, † Cited by third party
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10654866B2 (en) * 2018-07-12 2020-05-19 Eli Lilly And Company Selective estrogen receptor degraders

Family Cites Families (13)

* Cited by examiner, † Cited by third party
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
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10654866B2 (en) * 2018-07-12 2020-05-19 Eli Lilly And Company Selective estrogen receptor degraders

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JP7387926B2 (ja) 2023-11-28
MX2024009453A (es) 2024-08-09
CA3243621A1 (en) 2023-08-10
EP4472982A1 (en) 2024-12-11
US11926634B2 (en) 2024-03-12
JP2023112696A (ja) 2023-08-14
KR102743629B1 (ko) 2024-12-17
AU2025234145A1 (en) 2025-10-02
KR20250006312A (ko) 2025-01-10
US20230242545A1 (en) 2023-08-03
DOP2024000150A (es) 2024-08-30
AU2023216654B2 (en) 2025-09-25
JOP20240169A1 (ar) 2024-07-30
TW202523669A (zh) 2025-06-16
KR20240135862A (ko) 2024-09-12
CO2024009411A2 (es) 2024-07-29
JP2023162334A (ja) 2023-11-08
IL313886A (en) 2024-08-01
CR20240283A (es) 2024-09-03
WO2023150056A1 (en) 2023-08-10
JP7805336B2 (ja) 2026-01-23
TW202346300A (zh) 2023-12-01
PE20241731A1 (es) 2024-08-19
AU2023216654A1 (en) 2024-07-11
JP2025183283A (ja) 2025-12-16

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