AR115694A1 - Degradadores selectivos del receptor de estrógeno - Google Patents
Degradadores selectivos del receptor de estrógenoInfo
- Publication number
- AR115694A1 AR115694A1 ARP190101886A ARP190101886A AR115694A1 AR 115694 A1 AR115694 A1 AR 115694A1 AR P190101886 A ARP190101886 A AR P190101886A AR P190101886 A ARP190101886 A AR P190101886A AR 115694 A1 AR115694 A1 AR 115694A1
- Authority
- AR
- Argentina
- Prior art keywords
- degradators
- selective
- receptor
- strogen
- strogen receptor
- Prior art date
Links
- 102000015694 estrogen receptors Human genes 0.000 abstract 1
- 108010038795 estrogen receptors Proteins 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/4353—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic 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
- C07D491/02—Heterocyclic 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
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4741—Quinolines; 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Finger-Pressure Massage (AREA)
- Orthopedics, Nursing, And Contraception (AREA)
Abstract
Se proporcionan degradadores selectivos del receptor de estrógeno (SERD) de acuerdo con la fórmula (1), sales aceptables desde el punto de vista farmacéutico de estos y composiciones farmacéuticas de estos, en donde ya sea R¹ o R² se selecciona independientemente de Cl, F, -CF₃, o -CH₃, y el otro es hidrógeno, y métodos para su uso.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862697100P | 2018-07-12 | 2018-07-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR115694A1 true AR115694A1 (es) | 2021-02-17 |
Family
ID=67470734
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190101886A AR115694A1 (es) | 2018-07-12 | 2019-07-03 | Degradadores selectivos del receptor de estrógeno |
| ARP240103228A AR134487A2 (es) | 2018-07-12 | 2024-11-22 | Degradadores selectivos del receptor de estrógeno |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP240103228A AR134487A2 (es) | 2018-07-12 | 2024-11-22 | Degradadores selectivos del receptor de estrógeno |
Country Status (37)
| Country | Link |
|---|---|
| US (4) | US10654866B2 (es) |
| EP (2) | EP4155310A1 (es) |
| JP (6) | JP6995241B2 (es) |
| KR (3) | KR102783756B1 (es) |
| CN (2) | CN112638916B (es) |
| AR (2) | AR115694A1 (es) |
| AU (2) | AU2019299947B2 (es) |
| BR (1) | BR122023025061A2 (es) |
| CA (1) | CA3105501C (es) |
| CL (1) | CL2021000045A1 (es) |
| CO (1) | CO2021000043A2 (es) |
| CR (1) | CR20210007A (es) |
| DK (1) | DK3820873T3 (es) |
| EA (1) | EA202092975A1 (es) |
| EC (1) | ECSP21001770A (es) |
| ES (1) | ES2933980T3 (es) |
| FI (1) | FI3820873T3 (es) |
| HR (1) | HRP20230009T1 (es) |
| HU (1) | HUE060963T2 (es) |
| IL (3) | IL289871B2 (es) |
| JO (1) | JOP20210005A1 (es) |
| LT (1) | LT3820873T (es) |
| MA (2) | MA53124B1 (es) |
| MD (1) | MD3820873T2 (es) |
| MX (2) | MX2021000375A (es) |
| MY (1) | MY198962A (es) |
| PE (1) | PE20210400A1 (es) |
| PH (1) | PH12021550049A1 (es) |
| PL (1) | PL3820873T3 (es) |
| PT (1) | PT3820873T (es) |
| RS (1) | RS63809B1 (es) |
| SA (1) | SA521421008B1 (es) |
| SG (1) | SG11202100148TA (es) |
| SI (1) | SI3820873T1 (es) |
| TW (1) | TWI702219B (es) |
| UA (1) | UA127507C2 (es) |
| WO (1) | WO2020014435A1 (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA122346C2 (uk) | 2015-10-01 | 2020-10-26 | Олема Фармасьютикалз, Інк. | ТЕТРАГІДРО-1H-ПІРИДО[3,4-b]ІНДОЛЬНІ АНТИЕСТРОГЕННІ ЛІКАРСЬКІ ПРЕПАРАТИ |
| WO2020014440A1 (en) * | 2018-07-12 | 2020-01-16 | Eli Lilly And Company | Selective estrogen receptor degraders |
| 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 |
| JP7616794B2 (ja) | 2019-07-07 | 2025-01-17 | オレマ ファーマシューティカルズ インク． | エストロゲン受容体アンタゴニストのレジメン |
| IL293252A (en) | 2019-12-09 | 2022-07-01 | Sanofi Sa | Crystalline form of a 7h-benzo[7]annulene-2-carboxylic acid derivative |
| TW202146007A (zh) | 2020-02-27 | 2021-12-16 | 法商賽諾菲公司 | 包含阿培利司（ａｌｐｅｌｉｓｉｂ）與６－（２，４－二氯苯基）－５－［４－［（３ｓ）－１－（３－氟丙基）吡咯啶－３－基］氧苯基］－８，９－二氫－７ｈ－苯并［７］輪烯－２－羧酸之組合 |
| IL303041A (en) * | 2020-11-23 | 2023-07-01 | Sanofi Sa | Combination comprising abemaciclib and 6-(2,4-dichlorophenyl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulene-2-carboxylic acid |
| AU2022222660A1 (en) * | 2021-02-16 | 2023-07-27 | Genentech, Inc. | Treatment of breast cancer using combination therapies comprising gdc-9545 and abemaciclib or ribociclib |
| CN114957114A (zh) * | 2021-02-26 | 2022-08-30 | 冷志 | 一种4-溴-3-氯-7-甲氧基喹啉的合成方法 |
| CN117042771A (zh) * | 2021-03-09 | 2023-11-10 | 伊莱利利公司 | 使用serd给药方案的组合治疗癌症的方法 |
| 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 |
| AU2023216654B2 (en) * | 2022-02-01 | 2025-09-25 | Eli Lilly And Company | Processes for the preparation of selective estrogen receptor degraders |
| TW202430176A (zh) | 2022-10-17 | 2024-08-01 | 瑞典商阿斯特捷利康公司 | 用於治療癌症之組合療法 |
| CN120456897A (zh) | 2022-11-02 | 2025-08-08 | 佩特拉制药公司 | 用于治疗疾病的磷酸肌醇3-激酶(pi3k)变构色原酮抑制剂 |
| CN120187416A (zh) | 2022-11-11 | 2025-06-20 | 阿斯利康(瑞典)有限公司 | 用于治疗癌症的组合疗法 |
| US20240180893A1 (en) | 2022-11-17 | 2024-06-06 | Astrazeneca Ab | Methods of treatment of breast cancer |
| AU2024268541A1 (en) | 2023-05-05 | 2025-11-20 | Eli Lilly And Company | Imlunestrant or salts thereof for use in treating and preventing central nervous system (cns) metastases in subjects having er+ breast cancer |
| AU2024268579A1 (en) | 2023-05-11 | 2026-01-15 | Astrazeneca Ab | Combination of a parp1 inhibitor and a selective estrogen degrader for treating cancer |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1395563B1 (en) * | 2001-05-22 | 2006-03-29 | Eli Lilly And Company | 2-substituted 1,2,3,4-tetrahydroquinolines and derivatives thereof, compositions and methods |
| US7329654B2 (en) * | 2001-12-19 | 2008-02-12 | Janssen Pharmaceutica N.V. | Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators |
| MXPA04010433A (es) * | 2002-04-19 | 2005-08-19 | Signal Pharm Inc | Compuestos benzopiranona, composiciones de estos y los metodos para el tratamiento con estos. |
| US20090023917A1 (en) * | 2004-01-22 | 2009-01-22 | 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 |
| BR112015030595A2 (pt) | 2013-06-19 | 2017-07-25 | Seragon Pharmaceuticals Inc | moduladores de receptor de estrogênio de azetidina e usos dos mesmos |
| EP3233828B1 (en) * | 2014-12-18 | 2020-03-04 | F. Hoffmann-La Roche AG | Estrogen receptor modulators and uses thereof |
| IL301960B2 (en) * | 2014-12-18 | 2024-08-01 | Hoffmann La Roche | Tetrahydro-pyrido[3, 4-b]indole estrogen receptor modulators and their uses |
| WO2018108954A1 (en) | 2016-12-12 | 2018-06-21 | F. Hoffmann-La Roche Ag | Process for the preparation of 2-(3-(fluoromethyl)azetidin-1-yl)ethan-1-ol |
| WO2020014440A1 (en) * | 2018-07-12 | 2020-01-16 | Eli Lilly And Company | Selective estrogen receptor degraders |
| 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 |
-
2019
- 2019-07-02 TW TW108123257A patent/TWI702219B/zh active
- 2019-07-03 AR ARP190101886A patent/AR115694A1/es active IP Right Grant
- 2019-07-11 SG SG11202100148TA patent/SG11202100148TA/en unknown
- 2019-07-11 BR BR122023025061-3A patent/BR122023025061A2/pt not_active Application Discontinuation
- 2019-07-11 EP EP22201995.2A patent/EP4155310A1/en active Pending
- 2019-07-11 FI FIEP19745925.8T patent/FI3820873T3/fi active
- 2019-07-11 MY MYPI2021000056A patent/MY198962A/en unknown
- 2019-07-11 MA MA53124A patent/MA53124B1/fr unknown
- 2019-07-11 ES ES19745925T patent/ES2933980T3/es active Active
- 2019-07-11 EP EP19745925.8A patent/EP3820873B1/en active Active
- 2019-07-11 CR CR20210007A patent/CR20210007A/es unknown
- 2019-07-11 MX MX2021000375A patent/MX2021000375A/es unknown
- 2019-07-11 JP JP2021500536A patent/JP6995241B2/ja active Active
- 2019-07-11 AU AU2019299947A patent/AU2019299947B2/en active Active
- 2019-07-11 PE PE2020002017A patent/PE20210400A1/es unknown
- 2019-07-11 SI SI201930406T patent/SI3820873T1/sl unknown
- 2019-07-11 DK DK19745925.8T patent/DK3820873T3/da active
- 2019-07-11 EA EA202092975A patent/EA202092975A1/ru unknown
- 2019-07-11 LT LTEPPCT/US2019/041334T patent/LT3820873T/lt unknown
- 2019-07-11 IL IL289871A patent/IL289871B2/en unknown
- 2019-07-11 HU HUE19745925A patent/HUE060963T2/hu unknown
- 2019-07-11 UA UAA202100102A patent/UA127507C2/uk unknown
- 2019-07-11 KR KR1020237034781A patent/KR102783756B1/ko active Active
- 2019-07-11 PL PL19745925.8T patent/PL3820873T3/pl unknown
- 2019-07-11 PT PT197459258T patent/PT3820873T/pt unknown
- 2019-07-11 KR KR1020227044200A patent/KR102589886B1/ko active Active
- 2019-07-11 JO JOP/2021/0005A patent/JOP20210005A1/ar unknown
- 2019-07-11 CA CA3105501A patent/CA3105501C/en active Active
- 2019-07-11 MA MA53126A patent/MA53126B1/fr unknown
- 2019-07-11 US US16/508,745 patent/US10654866B2/en active Active
- 2019-07-11 CN CN201980046849.3A patent/CN112638916B/zh active Active
- 2019-07-11 WO PCT/US2019/041334 patent/WO2020014435A1/en not_active Ceased
- 2019-07-11 HR HRP20230009TT patent/HRP20230009T1/hr unknown
- 2019-07-11 RS RS20221142A patent/RS63809B1/sr unknown
- 2019-07-11 MD MDE20210462T patent/MD3820873T2/ro unknown
- 2019-07-11 KR KR1020217000466A patent/KR102550538B1/ko active Active
- 2019-07-11 CN CN202311312431.7A patent/CN117379428A/zh active Pending
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2020
- 2020-05-18 US US16/876,819 patent/US11117902B2/en active Active
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2021
- 2021-01-06 CO CONC2021/0000043A patent/CO2021000043A2/es unknown
- 2021-01-07 CL CL2021000045A patent/CL2021000045A1/es unknown
- 2021-01-08 PH PH12021550049A patent/PH12021550049A1/en unknown
- 2021-01-10 IL IL280065A patent/IL280065B/en unknown
- 2021-01-11 MX MX2023006047A patent/MX2023006047A/es unknown
- 2021-01-12 SA SA521421008A patent/SA521421008B1/ar unknown
- 2021-01-12 EC ECSENADI20211770A patent/ECSP21001770A/es unknown
- 2021-09-02 US US17/465,066 patent/US11634426B2/en active Active
- 2021-12-14 JP JP2021202668A patent/JP7009672B1/ja active Active
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2022
- 2022-01-12 JP JP2022003022A patent/JP7241211B2/ja active Active
- 2022-06-08 AU AU2022203969A patent/AU2022203969B2/en active Active
- 2022-08-14 IL IL295598A patent/IL295598B2/en unknown
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2023
- 2023-03-06 JP JP2023033486A patent/JP7557564B2/ja active Active
- 2023-03-15 US US18/121,667 patent/US11993608B2/en active Active
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2024
- 2024-09-13 JP JP2024159222A patent/JP7746496B2/ja active Active
- 2024-11-22 AR ARP240103228A patent/AR134487A2/es unknown
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2025
- 2025-09-17 JP JP2025154293A patent/JP2025186400A/ja active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |