KR102111792B1 - 에스트로겐 수용체 하향 조절제로서의 치환된 인돌 화합물 - Google Patents
에스트로겐 수용체 하향 조절제로서의 치환된 인돌 화합물 Download PDFInfo
- Publication number
- KR102111792B1 KR102111792B1 KR1020187030877A KR20187030877A KR102111792B1 KR 102111792 B1 KR102111792 B1 KR 102111792B1 KR 1020187030877 A KR1020187030877 A KR 1020187030877A KR 20187030877 A KR20187030877 A KR 20187030877A KR 102111792 B1 KR102111792 B1 KR 102111792B1
- Authority
- KR
- South Korea
- Prior art keywords
- group
- umol
- mmol
- compound
- solution
- 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.)
- Active
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
-
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D405/06—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 only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610180518 | 2016-03-25 | ||
| CN201610180518.7 | 2016-03-25 | ||
| CN201610867918.5 | 2016-09-29 | ||
| CN201610867918 | 2016-09-29 | ||
| PCT/CN2017/078139 WO2017162206A1 (zh) | 2016-03-25 | 2017-03-24 | 作为雌激素受体降解剂的吲哚并取代哌啶类化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20180128456A KR20180128456A (ko) | 2018-12-03 |
| KR102111792B1 true KR102111792B1 (ko) | 2020-05-18 |
Family
ID=59899253
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020187030877A Active KR102111792B1 (ko) | 2016-03-25 | 2017-03-24 | 에스트로겐 수용체 하향 조절제로서의 치환된 인돌 화합물 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US10519143B2 (https=) |
| EP (1) | EP3434668B1 (https=) |
| JP (1) | JP6790222B2 (https=) |
| KR (1) | KR102111792B1 (https=) |
| CN (1) | CN108884035B (https=) |
| AU (1) | AU2017239348B2 (https=) |
| CA (1) | CA3018801C (https=) |
| ES (1) | ES2821407T3 (https=) |
| RU (1) | RU2722441C2 (https=) |
| SG (1) | SG11201808363TA (https=) |
| WO (1) | WO2017162206A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019057201A1 (zh) * | 2017-09-25 | 2019-03-28 | 罗欣生物科技(上海)有限公司 | 一种雌激素受体抑制剂的晶型及其制备方法 |
| CA3109090A1 (en) | 2018-08-17 | 2020-02-20 | F. Hoffmann-La Roche Ag | Diagnostic and therapeutic methods for the treatment of breast cancer |
| CN113166056B (zh) * | 2018-11-28 | 2024-07-05 | 罗欣药业(上海)有限公司 | 一种雌激素受体下调剂的盐型、晶型及其制备方法 |
| JP7716980B2 (ja) * | 2018-12-17 | 2025-08-01 | チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド | エストロゲン受容体拮抗剤 |
| CN116891461A (zh) * | 2022-03-30 | 2023-10-17 | 罗欣药业(上海)有限公司 | 一种serd中间体的合成方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW397821B (en) * | 1996-04-19 | 2000-07-11 | American Home Produits Corp | 3-[4-(2-phenyl-indole-1-ylmethyl)-phenyl]-acrylamides and 2-phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol as well as pharmaceutical compositions of estrogenic agents thereof |
| US20100317635A1 (en) * | 2009-06-16 | 2010-12-16 | Endorecherche, Inc. | Treatment of hot flushes, vasomotor symptoms, and night sweats with sex steroid precursors in combination with selective estrogen receptor modulators |
| GB0917571D0 (en) * | 2009-10-07 | 2009-11-25 | Karobio Ab | Novel estrogen receptor ligands |
| GB2483736B (en) | 2010-09-16 | 2012-08-29 | Aragon Pharmaceuticals Inc | Estrogen receptor modulators and uses thereof |
| SG11201405918XA (en) * | 2012-03-20 | 2014-10-30 | Seragon Pharmaceuticals Inc | Estrogen receptor modulators and uses thereof |
| JP2017507964A (ja) * | 2014-03-13 | 2017-03-23 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | エストロゲン受容体モジュレーターを用いた治療的組合せ |
| CA2941161A1 (en) * | 2014-03-13 | 2015-09-17 | F.Hoffmann-La Roche Ag | Methods and compositions for modulating estrogen receptor mutants |
-
2017
- 2017-03-24 AU AU2017239348A patent/AU2017239348B2/en active Active
- 2017-03-24 RU RU2018135203A patent/RU2722441C2/ru active
- 2017-03-24 CA CA3018801A patent/CA3018801C/en active Active
- 2017-03-24 EP EP17769483.3A patent/EP3434668B1/en active Active
- 2017-03-24 SG SG11201808363TA patent/SG11201808363TA/en unknown
- 2017-03-24 JP JP2019500726A patent/JP6790222B2/ja active Active
- 2017-03-24 KR KR1020187030877A patent/KR102111792B1/ko active Active
- 2017-03-24 US US16/087,861 patent/US10519143B2/en active Active
- 2017-03-24 ES ES17769483T patent/ES2821407T3/es active Active
- 2017-03-24 WO PCT/CN2017/078139 patent/WO2017162206A1/zh not_active Ceased
- 2017-03-24 CN CN201780019970.8A patent/CN108884035B/zh active Active
Also Published As
| Publication number | Publication date |
|---|---|
| RU2018135203A3 (https=) | 2020-04-27 |
| WO2017162206A1 (zh) | 2017-09-28 |
| RU2018135203A (ru) | 2020-04-27 |
| JP6790222B2 (ja) | 2020-11-25 |
| CA3018801A1 (en) | 2017-09-28 |
| ES2821407T3 (es) | 2021-04-26 |
| AU2017239348B2 (en) | 2020-03-12 |
| CN108884035B (zh) | 2020-03-13 |
| CN108884035A (zh) | 2018-11-23 |
| ES2821407T8 (es) | 2022-02-02 |
| US10519143B2 (en) | 2019-12-31 |
| AU2017239348A1 (en) | 2018-11-15 |
| EP3434668A4 (en) | 2019-08-14 |
| RU2722441C2 (ru) | 2020-06-01 |
| EP3434668A1 (en) | 2019-01-30 |
| US20190106414A1 (en) | 2019-04-11 |
| HK1256936A1 (zh) | 2019-10-04 |
| KR20180128456A (ko) | 2018-12-03 |
| SG11201808363TA (en) | 2018-10-30 |
| CA3018801C (en) | 2020-06-23 |
| JP2019512550A (ja) | 2019-05-16 |
| EP3434668B1 (en) | 2020-08-26 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| KR102111792B1 (ko) | 에스트로겐 수용체 하향 조절제로서의 치환된 인돌 화합물 | |
| JP7290638B2 (ja) | Wee1阻害剤としての大環状化合物及びその使用 | |
| JP6717457B2 (ja) | Wee1阻害剤としての1,2−ジヒドロ−3H−ピラゾロ[3,4−d]ピリミジン−3−オン誘導体 | |
| JP2022518591A (ja) | 複素環式化合物であるベンゾピリドンおよびその使用 | |
| IL286352B2 (en) | Novel small molecule inhibitors of TEAD transcription factors | |
| JP7237010B2 (ja) | Hdac6選択的阻害剤およびその製造方法と使用 | |
| KR102244216B1 (ko) | 티오펜 화합물 및 이의 합성 방법과 이의 의약에서의 용도 | |
| CN110139863B (zh) | 作为雌激素受体降解剂的吲哚并取代哌啶类化合物 | |
| CN116867778A (zh) | 苯并七元环类双功能化合物及其应用 | |
| KR102254660B1 (ko) | A2a수용체 억제제로서의 축합 고리 유도체 | |
| CN103910643B (zh) | 一种抗癌活性甲酮衍生物、合成方法及其用途 | |
| CN116438177B (zh) | 靶向嵌合化合物、含其的药物组合物及其制备方法和用途 | |
| KR20240167916A (ko) | 테트라히드로나프탈렌 유도체 | |
| JP7716980B2 (ja) | エストロゲン受容体拮抗剤 | |
| CN100502846C (zh) | 3,4,5-三取代的苯丙烯类衍生物及其制备方法和用途 | |
| WO2019120198A1 (zh) | 一类喹啉衍生物 | |
| RU2772274C2 (ru) | Селективные ингибиторы hdac6, способ их получения и их применение | |
| HK1256936B (en) | Substituted-indole compounds as estrogen receptor down-regulators | |
| JPH07500571A (ja) | Pcpレセプター・リガンドおよびその用途 | |
| HK40080061B (zh) | 具有雌激素受体降解活性的新型色满衍生物及其用途 | |
| HK40009263B (zh) | 氮杂环丁烷衍生物 | |
| JPS61158951A (ja) | 生物体殺滅活性を有する多環状化合物 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
Patent event date: 20181025 Patent event code: PA01051R01D Comment text: International Patent Application |
|
| PG1501 | Laying open of application | ||
| A201 | Request for examination | ||
| A302 | Request for accelerated examination | ||
| PA0201 | Request for examination |
Patent event code: PA02012R01D Patent event date: 20191015 Comment text: Request for Examination of Application |
|
| PA0302 | Request for accelerated examination |
Patent event date: 20191015 Patent event code: PA03022R01D Comment text: Request for Accelerated Examination |
|
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
Comment text: Notification of reason for refusal Patent event date: 20191216 Patent event code: PE09021S01D |
|
| E701 | Decision to grant or registration of patent right | ||
| PE0701 | Decision of registration |
Patent event code: PE07011S01D Comment text: Decision to Grant Registration Patent event date: 20200311 |
|
| GRNT | Written decision to grant | ||
| PR0701 | Registration of establishment |
Comment text: Registration of Establishment Patent event date: 20200511 Patent event code: PR07011E01D |
|
| PR1002 | Payment of registration fee |
Payment date: 20200511 End annual number: 3 Start annual number: 1 |
|
| PG1601 | Publication of registration | ||
| PR1001 | Payment of annual fee |
Payment date: 20230426 Start annual number: 4 End annual number: 4 |
|
| PR1001 | Payment of annual fee |
Payment date: 20240425 Start annual number: 5 End annual number: 5 |