CL2021000045A1 - Degradadores selectivos del receptor de estrógeno - Google Patents
Degradadores selectivos del receptor de estrógenoInfo
- Publication number
- CL2021000045A1 CL2021000045A1 CL2021000045A CL2021000045A CL2021000045A1 CL 2021000045 A1 CL2021000045 A1 CL 2021000045A1 CL 2021000045 A CL2021000045 A CL 2021000045A CL 2021000045 A CL2021000045 A CL 2021000045A CL 2021000045 A1 CL2021000045 A1 CL 2021000045A1
- Authority
- CL
- Chile
- Prior art keywords
- estrogen receptor
- selective estrogen
- breakers
- degradators
- serds
- Prior art date
Links
- 102000015694 estrogen receptors Human genes 0.000 title abstract 2
- 108010038795 estrogen receptors Proteins 0.000 title abstract 2
- 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
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- 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
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- 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)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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 novedosos degradadores selectivos del receptor de estrógeno (SERD) de acuerdo con la fórmula (I); 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 |
|---|---|
| CL2021000045A1 true CL2021000045A1 (es) | 2021-07-19 |
Family
ID=67470734
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2021000045A CL2021000045A1 (es) | 2018-07-12 | 2021-01-07 | Degradadores selectivos del receptor de estrógeno |
Country Status (40)
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017059139A1 (en) | 2015-10-01 | 2017-04-06 | Olema Pharmaceuticals, Inc. | TETRAHYDRO-1H-PYRIDO[3,4-b]INDOLE ANTI-ESTROGENIC DRUGS |
| 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 |
| MD3820874T2 (ro) * | 2018-07-12 | 2023-05-31 | Lilly Co Eli | Degradanți selectivi ai receptorului estrogen |
| CA3144791A1 (en) | 2019-07-07 | 2021-01-14 | Olema Pharmaceuticals, Inc. | Regimens of estrogen receptor antagonists |
| WO2021063967A1 (en) | 2019-10-01 | 2021-04-08 | Sanofi | Novel substituted 6,7-dihydro-5h-benzo[7]annulene compounds, processes for their preparation and therapeutic uses thereof |
| CA3160897A1 (en) | 2019-12-09 | 2021-06-17 | Sanofi | 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 |
| IL302153B1 (en) | 2020-10-19 | 2026-07-01 | Sanofi Sa | 6,7-DIHYDRO-5H-BENZO[7]ANNULENE COMPOUNDS AND THEIR DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THEIR THERAPEUTIC USES |
| IL302152B1 (en) | 2020-10-19 | 2026-07-01 | Sanofi Sa | 6,7-DIHYDRO-5H-BENZO[7]ANNULENE COMPOUNDS AND THEIR DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THEIR THERAPEUTIC USES |
| WO2022106711A1 (en) * | 2020-11-23 | 2022-05-27 | Sanofi | 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 |
| JP7846700B2 (ja) * | 2021-02-16 | 2026-04-15 | ジェネンテック， インコーポレイテッド | Ｇｄｃ－９５４５とアベマシクリブ又はリボシクリブとを含む併用療法を使用する乳がんの治療 |
| 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 |
| 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 |
| 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 |
| 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 |
| US20240199629A1 (en) * | 2022-02-01 | 2024-06-20 | Eli Lilly And Company | Processes for the preparation of selective estrogen receptor degraders |
| PE20241731A1 (es) * | 2022-02-01 | 2024-08-19 | Lilly Co Eli | Procesos para la preparacion de degradadores selectivos del receptor de estrogeno |
| WO2024083716A1 (en) | 2022-10-17 | 2024-04-25 | Astrazeneca Ab | Combinations of a serd for the treatment of cancer |
| AU2023373671A1 (en) | 2022-11-02 | 2025-05-15 | Petra Pharma Corporation | Allosteric chromenone inhibitors of phosphoinositide 3-kinase (pi3k) for the treatment of disease |
| JP2025539034A (ja) | 2022-11-11 | 2025-12-03 | アストラゼネカ・アクチエボラーグ | 癌の治療のための併用療法 |
| US20240180893A1 (en) | 2022-11-17 | 2024-06-06 | Astrazeneca Ab | Methods of treatment of breast cancer |
| WO2024233256A1 (en) | 2023-05-05 | 2024-11-14 | 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 |
| JP2026515235A (ja) | 2023-05-11 | 2026-05-14 | アストラゼネカ・アクチエボラーグ | 癌を治療するためのｐａｒｐ１阻害剤と選択的エストロゲン分解薬の併用 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6756388B1 (en) * | 1993-10-12 | 2004-06-29 | Pfizer Inc. | Benzothiophenes and related compounds as estrogen agonists |
| 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 |
| CA2480800C (en) * | 2002-04-08 | 2008-09-23 | Mark T. Bilodeau | Inhibitors of akt activity |
| CA2482986A1 (en) * | 2002-04-19 | 2003-10-30 | Signal Pharmaceuticals, Inc. | Benzopyranone compounds, compositions thereof, and methods of treatment therewith |
| EA012262B1 (ru) * | 2004-01-22 | 2009-08-28 | Эли Лилли Энд Компани | Селективные модуляторы рецепторов эстрогена для лечения вазомоторных симптомов |
| US20080221163A1 (en) * | 2005-01-18 | 2008-09-11 | Jeffrey Alan Dodge | Selective Estrogen Receptor Modulators |
| AR088082A1 (es) * | 2011-10-13 | 2014-05-07 | Lilly Co Eli | Moduladores selectivos del receptor androgeno |
| BR112015030595A2 (pt) * | 2013-06-19 | 2017-07-25 | Seragon Pharmaceuticals Inc | moduladores de receptor de estrogênio de azetidina e usos dos mesmos |
| TWI784255B (zh) | 2014-12-18 | 2022-11-21 | 瑞士商赫孚孟拉羅股份公司 | 四氫-吡啶并[3,4-b]吲哚雌激素受體調節劑及其用途 |
| WO2016097071A1 (en) * | 2014-12-18 | 2016-06-23 | F. Hoffmann-La Roche Ag | Estrogen receptor modulators and uses thereof |
| WO2017127442A1 (en) * | 2016-01-18 | 2017-07-27 | The Regents Of The University Of California | Methods for treating cancer with rorgamma inhibitors |
| TW201803870A (zh) * | 2016-04-20 | 2018-02-01 | 阿斯特捷利康公司 | 化學化合物 |
| 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 |
| 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 |
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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 ES ES19745925T patent/ES2933980T3/es active Active
- 2019-07-11 AU AU2019299947A patent/AU2019299947B2/en active Active
- 2019-07-11 MY MYPI2021000056A patent/MY198962A/en unknown
- 2019-07-11 KR KR1020227044200A patent/KR102589886B1/ko active Active
- 2019-07-11 SI SI201930406T patent/SI3820873T1/sl unknown
- 2019-07-11 MX MX2021000375A patent/MX2021000375A/es unknown
- 2019-07-11 CN CN201980046849.3A patent/CN112638916B/zh active Active
- 2019-07-11 PE PE2020002017A patent/PE20210400A1/es unknown
- 2019-07-11 MA MA53126A patent/MA53126B1/fr unknown
- 2019-07-11 BR BR122023025061-3A patent/BR122023025061A2/pt not_active Application Discontinuation
- 2019-07-11 EP EP19745925.8A patent/EP3820873B1/en active Active
- 2019-07-11 US US16/508,745 patent/US10654866B2/en active Active
- 2019-07-11 PT PT197459258T patent/PT3820873T/pt unknown
- 2019-07-11 UA UAA202100102A patent/UA127507C2/uk unknown
- 2019-07-11 CR CR20210007A patent/CR20210007A/es unknown
- 2019-07-11 EA EA202092975A patent/EA202092975A1/ru unknown
- 2019-07-11 MA MA53124A patent/MA53124B1/fr unknown
- 2019-07-11 WO PCT/US2019/041334 patent/WO2020014435A1/en not_active Ceased
- 2019-07-11 EP EP22201995.2A patent/EP4155310A1/en active Pending
- 2019-07-11 KR KR1020237034781A patent/KR102783756B1/ko active Active
- 2019-07-11 HU HUE19745925A patent/HUE060963T2/hu unknown
- 2019-07-11 LT LTEPPCT/US2019/041334T patent/LT3820873T/lt unknown
- 2019-07-11 FI FIEP19745925.8T patent/FI3820873T3/fi active
- 2019-07-11 KR KR1020217000466A patent/KR102550538B1/ko active Active
- 2019-07-11 MD MDE20210462T patent/MD3820873T2/ro unknown
- 2019-07-11 SG SG11202100148TA patent/SG11202100148TA/en unknown
- 2019-07-11 IL IL289871A patent/IL289871B2/en unknown
- 2019-07-11 DK DK19745925.8T patent/DK3820873T3/da active
- 2019-07-11 CN CN202311312431.7A patent/CN117379428A/zh active Pending
- 2019-07-11 JP JP2021500536A patent/JP6995241B2/ja active Active
- 2019-07-11 RS RS20221142A patent/RS63809B1/sr unknown
- 2019-07-11 HR HRP20230009TT patent/HRP20230009T1/hr unknown
- 2019-07-11 PL PL19745925.8T patent/PL3820873T3/pl unknown
- 2019-07-11 CA CA3105501A patent/CA3105501C/en active Active
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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 JO JOJO/P/2021/0005A patent/JOP20210005B1/ar active
- 2021-01-10 IL IL280065A patent/IL280065B/en unknown
- 2021-01-11 MX MX2023006047A patent/MX2023006047A/es unknown
- 2021-01-12 EC ECSENADI20211770A patent/ECSP21001770A/es unknown
- 2021-01-12 SA SA521421008A patent/SA521421008B1/ar 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
- 2024-11-22 AR ARP240103229A patent/AR134662A2/es unknown
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2025
- 2025-09-17 JP JP2025154293A patent/JP2025186400A/ja active Pending
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2026
- 2026-04-07 FI FIC20260010C patent/FIC20260010I1/fi unknown
- 2026-04-15 FR FR26C1020C patent/FR26C1020I1/fr active Active
- 2026-04-21 NO NO2026021C patent/NO2026021I1/no unknown
- 2026-05-08 LT LTPA2026519C patent/LTPA2026519I1/lt unknown
- 2026-05-18 NL NL301383C patent/NL301383I2/nl unknown
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