PE20221588A1 - Degradador selectivo del receptor de estrogeno - Google Patents
Degradador selectivo del receptor de estrogenoInfo
- Publication number
- PE20221588A1 PE20221588A1 PE2022000135A PE2022000135A PE20221588A1 PE 20221588 A1 PE20221588 A1 PE 20221588A1 PE 2022000135 A PE2022000135 A PE 2022000135A PE 2022000135 A PE2022000135 A PE 2022000135A PE 20221588 A1 PE20221588 A1 PE 20221588A1
- Authority
- PE
- Peru
- Prior art keywords
- estrogen receptor
- selective estrogen
- receptor degrader
- chromen
- azetidin
- Prior art date
Links
- 229940125944 selective estrogen receptor degrader Drugs 0.000 title abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- DVZLOPUYTKPWHJ-MPWQXXDYSA-N (2S)-3-(3,5-difluorophenyl)-2-[4-[(E)-3-[3-(fluoromethyl)azetidin-1-yl]prop-1-enyl]phenyl]-4-methyl-2H-chromen-7-ol Chemical compound FC=1C=C(C=C(C=1)F)C=1[C@@H](OC2=CC(=CC=C2C=1C)O)C1=CC=C(C=C1)\C=C\CN1CC(C1)CF DVZLOPUYTKPWHJ-MPWQXXDYSA-N 0.000 abstract 1
- 206010006187 Breast cancer Diseases 0.000 abstract 1
- 208000026310 Breast neoplasm Diseases 0.000 abstract 1
- 101100521345 Mus musculus Prop1 gene Proteins 0.000 abstract 1
- 108700017836 Prophet of Pit-1 Proteins 0.000 abstract 1
- 125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 102000015694 estrogen receptors Human genes 0.000 abstract 1
- 108010038795 estrogen receptors Proteins 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic 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
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un degradador selectivo del receptor de estrogeno (SERD), un compuesto 3-(3,5-difluorofenil)-2-[4-[(E)-3-[3-(fluorometil)azetidin-1-il]prop-1-enil]fenil]-4-metil-2H-cromen-7-ol y su enantiomero S, (2S)-3-(3,5-difluorofenil)-2-[4-[(E)-3-[3-(fluorometil)azetidin-1-il]prop-1-enil]fenil]-4-metil-2H-cromen-7-ol, o sales farmaceuticamente aceptables de estos. Tambien se proporcionan procesos para su preparacion. Tambien se proporciona el uso de estos compuestos para el tratamiento de enfermedades relacionadas con la modulacion de los receptores de estrogeno, tales como el cancer de mama positivo para ER.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN201921029554 | 2019-07-22 | ||
| PCT/IB2020/056914 WO2021014386A1 (en) | 2019-07-22 | 2020-07-22 | Selective estrogen receptor degrader |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20221588A1 true PE20221588A1 (es) | 2022-10-10 |
Family
ID=71842730
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2022000135A PE20221588A1 (es) | 2019-07-22 | 2020-07-22 | Degradador selectivo del receptor de estrogeno |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US11014915B2 (es) |
| EP (1) | EP4003525A1 (es) |
| JP (1) | JP2022541938A (es) |
| KR (1) | KR20220046586A (es) |
| CN (1) | CN114302879A (es) |
| AU (1) | AU2020317099A1 (es) |
| BR (1) | BR112022001285A2 (es) |
| CA (1) | CA3148592A1 (es) |
| CL (1) | CL2022000156A1 (es) |
| IL (1) | IL290036A (es) |
| MX (1) | MX2022001013A (es) |
| PE (1) | PE20221588A1 (es) |
| PH (1) | PH12022550182A1 (es) |
| WO (1) | WO2021014386A1 (es) |
| ZA (1) | ZA202201157B (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3111466A1 (en) * | 2018-09-07 | 2020-03-12 | Sanofi | Salts of methyl 6-(2,4-dichlorophenyl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulene-2-carboxylate and preparation process thereof |
| MX420421B (es) | 2019-07-22 | 2025-02-10 | Boehringer Ingelheim Int | Derivados de n-(6-metoxi)pirizadin-3-il) amina, n-metilo como moduladores de autotaxina (atx) para el tratamiento de enfermedades inflamatorias de las vias respiratorias o fibroticas |
| PE20221588A1 (es) * | 2019-07-22 | 2022-10-10 | Sun Pharma Advanced Res Co Ltd | Degradador selectivo del receptor de estrogeno |
| AU2023216654B2 (en) * | 2022-02-01 | 2025-09-25 | Eli Lilly And Company | Processes for the preparation of selective estrogen receptor degraders |
| CN119176799B (zh) * | 2024-09-19 | 2025-10-03 | 晨伫(杭州)生物科技有限责任公司 | 色烯衍生物及其应用 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5395842A (en) | 1988-10-31 | 1995-03-07 | Endorecherche Inc. | Anti-estrogenic compounds and compositions |
| DE69023906T2 (de) | 1990-08-09 | 1996-04-11 | Council Scient Ind Res | Benzopyrane und Verfahren zu deren Herstellung. |
| US6060503A (en) | 1991-12-02 | 2000-05-09 | Endorecherche, Inc. | Benzopyran-containing compounds and method for their use |
| US5407947A (en) | 1993-11-05 | 1995-04-18 | Eli Lilly And Company | Methods for inhibiting bone loss using pyrolidine and piperidine substituted benzopyrans |
| US5389646A (en) | 1993-12-30 | 1995-02-14 | Zymogenetics, Inc. | Methods for treatment and prevention of bone loss using 2,3-benzopyrans |
| WO1999002512A1 (en) | 1997-07-09 | 1999-01-21 | Novo Nordisk A/S | Dl-2,3-diaryl-2h-1-benzopyrans |
| DE10013782A1 (de) | 2000-03-15 | 2001-10-18 | Schering Ag | 4-Fluoralkyl-2H-benzopyrane mit antiestrogener Wirksamkeit, Verfahren zu ihrer Herstellung, pharmazeutische Präparate, die diese enthalten sowie deren Verwendung zur Herstellung von Arzneimitteln |
| MX2012014431A (es) | 2010-06-10 | 2013-02-26 | Aragon Pharmaceuticals Inc | Modulares del receptor de estrogenos y usos de los mismos. |
| JP2015500346A (ja) | 2011-12-14 | 2015-01-05 | セラゴン ファーマシューティカルズ,インク. | エストロゲン受容体モジュレーターおよびその使用 |
| MX2014007198A (es) | 2011-12-16 | 2014-10-13 | Olema Pharmaceuticals Inc | Compuestos novedosos de benzopirano, composiciones y usos de los mismos. |
| BR112015030595A2 (pt) | 2013-06-19 | 2017-07-25 | Seragon Pharmaceuticals Inc | moduladores de receptor de estrogênio de azetidina e usos dos mesmos |
| EA031077B1 (ru) | 2013-06-19 | 2018-11-30 | Серагон Фармасьютикалз, Инк. | Модулятор рецептора эстрогена и его применения |
| WO2014203132A1 (en) | 2013-06-19 | 2014-12-24 | Olema Pharmaceuticals, Inc. | Substituted benzopyran compounds, compositions and uses thereof |
| CN103879283B (zh) * | 2014-03-10 | 2019-01-15 | 浙江吉利汽车研究院有限公司 | 一种电动车辆 |
| JP2017538727A (ja) * | 2014-12-18 | 2017-12-28 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | 癌の治療に有用な2,3−ジフェニルクロメンの誘導体 |
| WO2016174551A1 (en) | 2015-04-27 | 2016-11-03 | Pfizer Inc. | Anti-estrogenic compounds |
| EP3303326B1 (en) | 2015-05-26 | 2020-12-16 | H. Hoffnabb-La Roche Ag | Heterocyclic estrogen receptor modulators and uses thereof |
| ES2916223T3 (es) * | 2015-10-27 | 2022-06-29 | Sun Pharma Advanced Res Co Ltd | Nuevos antiestrógenos heterocíclicos |
| PE20221588A1 (es) * | 2019-07-22 | 2022-10-10 | Sun Pharma Advanced Res Co Ltd | Degradador selectivo del receptor de estrogeno |
-
2020
- 2020-07-22 PE PE2022000135A patent/PE20221588A1/es unknown
- 2020-07-22 KR KR1020227005904A patent/KR20220046586A/ko not_active Ceased
- 2020-07-22 AU AU2020317099A patent/AU2020317099A1/en not_active Abandoned
- 2020-07-22 CA CA3148592A patent/CA3148592A1/en active Pending
- 2020-07-22 PH PH1/2022/550182A patent/PH12022550182A1/en unknown
- 2020-07-22 US US16/936,022 patent/US11014915B2/en active Active
- 2020-07-22 BR BR112022001285A patent/BR112022001285A2/pt not_active IP Right Cessation
- 2020-07-22 WO PCT/IB2020/056914 patent/WO2021014386A1/en not_active Ceased
- 2020-07-22 JP JP2022504655A patent/JP2022541938A/ja active Pending
- 2020-07-22 EP EP20747136.8A patent/EP4003525A1/en not_active Withdrawn
- 2020-07-22 MX MX2022001013A patent/MX2022001013A/es unknown
- 2020-07-22 CN CN202080053315.6A patent/CN114302879A/zh active Pending
-
2021
- 2021-05-05 US US17/308,501 patent/US20210261534A1/en not_active Abandoned
-
2022
- 2022-01-22 CL CL2022000156A patent/CL2022000156A1/es unknown
- 2022-01-23 IL IL290036A patent/IL290036A/en unknown
- 2022-01-25 ZA ZA2022/01157A patent/ZA202201157B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PH12022550182A1 (en) | 2022-11-14 |
| JP2022541938A (ja) | 2022-09-28 |
| US20210261534A1 (en) | 2021-08-26 |
| EP4003525A1 (en) | 2022-06-01 |
| CA3148592A1 (en) | 2021-01-28 |
| BR112022001285A2 (pt) | 2022-03-22 |
| IL290036A (en) | 2022-03-01 |
| KR20220046586A (ko) | 2022-04-14 |
| WO2021014386A1 (en) | 2021-01-28 |
| CL2022000156A1 (es) | 2022-11-18 |
| US11014915B2 (en) | 2021-05-25 |
| US20210024504A1 (en) | 2021-01-28 |
| CN114302879A (zh) | 2022-04-08 |
| AU2020317099A1 (en) | 2022-02-24 |
| MX2022001013A (es) | 2022-02-22 |
| ZA202201157B (en) | 2023-07-26 |
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