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)
- 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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2019512550A JP2019512550A (ja) | 2019-05-16 |
| JP2019512550A5 JP2019512550A5 (https=) | 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 (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 |
| 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 |
| KR102111792B1 (ko) | 2020-05-18 |
| 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 |
|---|---|---|
| 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 | |
| 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 | |
| CN116867778A (zh) | 苯并七元环类双功能化合物及其应用 | |
| 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 | |
| JP2020535196A (ja) | A2a受容体アンタゴニストとしての縮合環誘導体 | |
| CN117466870A (zh) | 苯并七元环类双功能化合物及其应用 | |
| CN112168824B (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 | |
| 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 | |
| HK1256936B (en) | Substituted-indole compounds as estrogen receptor down-regulators | |
| WO2019120198A1 (zh) | 一类喹啉衍生物 | |
| 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 | |
| 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 | |
| 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 |