JP6790222B2 - エストロゲン受容体ダウンレギュレーターとしての置換インドール化合物 - Google Patents
エストロゲン受容体ダウンレギュレーターとしての置換インドール化合物 Download PDFInfo
- Publication number
- JP6790222B2 JP6790222B2 JP2019500726A JP2019500726A JP6790222B2 JP 6790222 B2 JP6790222 B2 JP 6790222B2 JP 2019500726 A JP2019500726 A JP 2019500726A JP 2019500726 A JP2019500726 A JP 2019500726A JP 6790222 B2 JP6790222 B2 JP 6790222B2
- Authority
- JP
- Japan
- Prior art keywords
- group
- groups
- μmol
- mmol
- compound
- 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)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610180518.7 | 2016-03-25 | ||
| CN201610180518 | 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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2019512550A JP2019512550A (ja) | 2019-05-16 |
| JP2019512550A5 JP2019512550A5 (cg-RX-API-DMAC7.html) | 2019-11-28 |
| JP6790222B2 true JP6790222B2 (ja) | 2020-11-25 |
Family
ID=59899253
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019500726A Active JP6790222B2 (ja) | 2016-03-25 | 2017-03-24 | エストロゲン受容体ダウンレギュレーターとしての置換インドール化合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US10519143B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3434668B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6790222B2 (cg-RX-API-DMAC7.html) |
| KR (1) | KR102111792B1 (cg-RX-API-DMAC7.html) |
| CN (1) | CN108884035B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2017239348B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA3018801C (cg-RX-API-DMAC7.html) |
| ES (1) | ES2821407T3 (cg-RX-API-DMAC7.html) |
| RU (1) | RU2722441C2 (cg-RX-API-DMAC7.html) |
| SG (1) | SG11201808363TA (cg-RX-API-DMAC7.html) |
| WO (1) | WO2017162206A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111032627B (zh) * | 2017-09-25 | 2023-10-20 | 罗欣健康科技发展(北京)有限公司 | 一种雌激素受体抑制剂的晶型及其制备方法 |
| CN113490850B (zh) | 2018-08-17 | 2024-12-06 | 基因泰克公司 | 用于治疗乳腺癌的诊断和治疗方法 |
| KR102858291B1 (ko) * | 2018-11-28 | 2025-09-12 | 뤄신 파마슈티컬 (상하이) 컴퍼니 리미티드 | 에스트로겐 수용체 하향 조절제의 염 형태와 결정형, 및 이의 제조방법 |
| BR112021011728A8 (pt) * | 2018-12-17 | 2023-01-31 | Chia Tai Tianqing Pharmaceutical Group Co Ltd | Antagonista do receptor de estrogênio |
| 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 |
| NZ630124A (en) | 2012-03-20 | 2016-01-29 | Seragon Pharmaceuticals Inc | Estrogen receptor modulators and uses thereof |
| KR20160124909A (ko) * | 2014-03-13 | 2016-10-28 | 에프. 호프만-라 로슈 아게 | 에스트로겐 수용체 조절제를 함유하는 치료 조합물 |
| KR20160132029A (ko) * | 2014-03-13 | 2016-11-16 | 에프. 호프만-라 로슈 아게 | 에스트로젠 수용체 돌연변이체의 조절을 위한 방법 및 조성물 |
-
2017
- 2017-03-24 CA CA3018801A patent/CA3018801C/en active Active
- 2017-03-24 KR KR1020187030877A patent/KR102111792B1/ko active Active
- 2017-03-24 RU RU2018135203A patent/RU2722441C2/ru active
- 2017-03-24 US US16/087,861 patent/US10519143B2/en active Active
- 2017-03-24 SG SG11201808363TA patent/SG11201808363TA/en unknown
- 2017-03-24 EP EP17769483.3A patent/EP3434668B1/en active Active
- 2017-03-24 AU AU2017239348A patent/AU2017239348B2/en active Active
- 2017-03-24 CN CN201780019970.8A patent/CN108884035B/zh active Active
- 2017-03-24 JP JP2019500726A patent/JP6790222B2/ja active Active
- 2017-03-24 WO PCT/CN2017/078139 patent/WO2017162206A1/zh not_active Ceased
- 2017-03-24 ES ES17769483T patent/ES2821407T3/es active Active
Also Published As
| Publication number | Publication date |
|---|---|
| AU2017239348B2 (en) | 2020-03-12 |
| CN108884035B (zh) | 2020-03-13 |
| US10519143B2 (en) | 2019-12-31 |
| EP3434668A4 (en) | 2019-08-14 |
| ES2821407T8 (es) | 2022-02-02 |
| RU2018135203A3 (cg-RX-API-DMAC7.html) | 2020-04-27 |
| CA3018801A1 (en) | 2017-09-28 |
| CN108884035A (zh) | 2018-11-23 |
| KR20180128456A (ko) | 2018-12-03 |
| ES2821407T3 (es) | 2021-04-26 |
| RU2018135203A (ru) | 2020-04-27 |
| HK1256936A1 (zh) | 2019-10-04 |
| US20190106414A1 (en) | 2019-04-11 |
| AU2017239348A1 (en) | 2018-11-15 |
| EP3434668B1 (en) | 2020-08-26 |
| KR102111792B1 (ko) | 2020-05-18 |
| EP3434668A1 (en) | 2019-01-30 |
| RU2722441C2 (ru) | 2020-06-01 |
| SG11201808363TA (en) | 2018-10-30 |
| CA3018801C (en) | 2020-06-23 |
| JP2019512550A (ja) | 2019-05-16 |
| WO2017162206A1 (zh) | 2017-09-28 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| 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 | |
| JP7290638B2 (ja) | Ｗｅｅ１阻害剤としての大環状化合物及びその使用 | |
| CN115003295B (zh) | 具有雌激素受体降解活性的新型色满衍生物及其用途 | |
| CN110963994B (zh) | 异吲哚啉类化合物、其制备方法、药物组合物及用途 | |
| JP6790222B2 (ja) | エストロゲン受容体ダウンレギュレーターとしての置換インドール化合物 | |
| JP2024505735A (ja) | 置換されたピリダジンフェノール系誘導体 | |
| CN110139863B (zh) | 作为雌激素受体降解剂的吲哚并取代哌啶类化合物 | |
| CN110382463B (zh) | Hdac6选择性抑制剂及其制备方法和应用 | |
| JP6836693B2 (ja) | Ａ２ａ受容体アンタゴニストとしての縮合環誘導体 | |
| JP2019519606A (ja) | チオフェン化合物、その合成方法及び医療における応用 | |
| BR112017009012B1 (pt) | Derivados de anel benzo de seis membros como inibidor de dpp-4 e uso dos mesmos | |
| CN117466870A (zh) | 苯并七元环类双功能化合物及其应用 | |
| CN112168824A (zh) | 阿朴菲类化合物的应用 | |
| 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 | |
| CN111527069B (zh) | 一类喹啉衍生物 | |
| CN115594607A (zh) | 一类苯并七元环类化合物及其应用 | |
| JP6951418B2 (ja) | 抗ｈｃｍｖウイルス化合物 | |
| HK1256936B (en) | Substituted-indole compounds as estrogen receptor down-regulators | |
| RU2772274C2 (ru) | Селективные ингибиторы hdac6, способ их получения и их применение | |
| CA3049834C (en) | Hdac6 selective inhibitors, preparation method therefor, and application thereof | |
| JPH07500571A (ja) | Ｐｃｐレセプター・リガンドおよびその用途 | |
| CN120383593A (zh) | 一种识别α-突触核蛋白聚集体的化合物及其用途 | |
| HK40022836A (en) | Macrocyclic compound as a wee1 inhibitor and applications thereof | |
| HK40022836B (zh) | 作为wee1抑制剂的大环类化合物及其应用 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20181126 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20191015 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20191015 |
|
| A871 | Explanation of circumstances concerning accelerated examination |
Free format text: JAPANESE INTERMEDIATE CODE: A871 Effective date: 20191015 |
|
| A975 | Report on accelerated examination |
Free format text: JAPANESE INTERMEDIATE CODE: A971005 Effective date: 20191217 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20191226 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20200128 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20200408 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20200616 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20200826 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20201006 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20201104 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 6790222 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| S111 | Request for change of ownership or part of ownership |
Free format text: JAPANESE INTERMEDIATE CODE: R313113 |
|
| R370 | Written measure of declining of transfer procedure |
Free format text: JAPANESE INTERMEDIATE CODE: R370 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| S111 | Request for change of ownership or part of ownership |
Free format text: JAPANESE INTERMEDIATE CODE: R313113 |
|
| R360 | Written notification for declining of transfer of rights |
Free format text: JAPANESE INTERMEDIATE CODE: R360 |
|
| R370 | Written measure of declining of transfer procedure |
Free format text: JAPANESE INTERMEDIATE CODE: R370 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| S111 | Request for change of ownership or part of ownership |
Free format text: JAPANESE INTERMEDIATE CODE: R313113 |
|
| R350 | Written notification of registration of transfer |
Free format text: JAPANESE INTERMEDIATE CODE: R350 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |