AU2017239348B2 - Substituted-indole compounds as estrogen receptor down-regulators - Google Patents
Substituted-indole compounds as estrogen receptor down-regulators Download PDFInfo
- Publication number
- AU2017239348B2 AU2017239348B2 AU2017239348A AU2017239348A AU2017239348B2 AU 2017239348 B2 AU2017239348 B2 AU 2017239348B2 AU 2017239348 A AU2017239348 A AU 2017239348A AU 2017239348 A AU2017239348 A AU 2017239348A AU 2017239348 B2 AU2017239348 B2 AU 2017239348B2
- Authority
- AU
- Australia
- Prior art keywords
- compound
- group
- cooh
- alkyl
- pharmaceutically acceptable
- 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.)
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Links
- 0 COCCN1CC(*)(*)C1 Chemical compound COCCN1CC(*)(*)C1 0.000 description 9
- LEKKFGRYFRQEHL-UHFFFAOYSA-N C=Cc1c(C=C)[nH]cc1 Chemical compound C=Cc1c(C=C)[nH]cc1 LEKKFGRYFRQEHL-UHFFFAOYSA-N 0.000 description 1
- PSVHSBJQHOASGA-YBCTUDNBSA-N CC/C(/c(c(C(F)(F)F)c1)ccc1F)=C(\c1cc(cccc2)c2[nH]1)/c1ccc(/C=C/C)cc1 Chemical compound CC/C(/c(c(C(F)(F)F)c1)ccc1F)=C(\c1cc(cccc2)c2[nH]1)/c1ccc(/C=C/C)cc1 PSVHSBJQHOASGA-YBCTUDNBSA-N 0.000 description 1
- JGPVKFUUZGKNIJ-XXHFXVPZSA-N CC/C(/c(cc([s]1)Cl)c1Cl)=C(\c1c(C2NC2)c2ccccc2[nH]1)/c1ccc(/C=C/C(C)=O)cc1 Chemical compound CC/C(/c(cc([s]1)Cl)c1Cl)=C(\c1c(C2NC2)c2ccccc2[nH]1)/c1ccc(/C=C/C(C)=O)cc1 JGPVKFUUZGKNIJ-XXHFXVPZSA-N 0.000 description 1
- DIOOVXCBXOZTDV-HNYWWJJZSA-N CC/C(/c(cc([s]1)Cl)c1Cl)=C(\c1cc2ccccc2[nH]1)/c1ccc(/C=C/C(C)=O)cc1 Chemical compound CC/C(/c(cc([s]1)Cl)c1Cl)=C(\c1cc2ccccc2[nH]1)/c1ccc(/C=C/C(C)=O)cc1 DIOOVXCBXOZTDV-HNYWWJJZSA-N 0.000 description 1
- IZSUBTBIQMAZGC-JEYYALBUSA-N CC/C(/c(cc1C)ccc1Cl)=C(\c([nH]c1ccccc11)c1Cl)/c1ccc(/C=C/C(C)=O)cc1 Chemical compound CC/C(/c(cc1C)ccc1Cl)=C(\c([nH]c1ccccc11)c1Cl)/c1ccc(/C=C/C(C)=O)cc1 IZSUBTBIQMAZGC-JEYYALBUSA-N 0.000 description 1
- URBKMQATJNFDEB-BOXXXNKQSA-N CC/C(/c(ccc(OC)c1)c1Cl)=C(\c1cc(cccc2)c2[nH]1)/c1ccc(/C=C/C)cc1 Chemical compound CC/C(/c(ccc(OC)c1)c1Cl)=C(\c1cc(cccc2)c2[nH]1)/c1ccc(/C=C/C)cc1 URBKMQATJNFDEB-BOXXXNKQSA-N 0.000 description 1
- JWPWOZVUWKLUPZ-UNFRMVJLSA-N CC/C(/c1c(C(F)(F)F)cccc1)=C(\c([nH]c1ccccc11)c1Cl)/c1ccc(/C=C/C)cc1 Chemical compound CC/C(/c1c(C(F)(F)F)cccc1)=C(\c([nH]c1ccccc11)c1Cl)/c1ccc(/C=C/C)cc1 JWPWOZVUWKLUPZ-UNFRMVJLSA-N 0.000 description 1
- KKXPAVFXHDOFNU-UPFVGGGXSA-N CC/C(/c1c[s]c(C)c1)=C(\c([nH]c1ccccc11)c1Cl)/c1ccc(/C=C/C(O)=O)cc1 Chemical compound CC/C(/c1c[s]c(C)c1)=C(\c([nH]c1ccccc11)c1Cl)/c1ccc(/C=C/C(O)=O)cc1 KKXPAVFXHDOFNU-UPFVGGGXSA-N 0.000 description 1
- AUEDHKLGKKFOPX-GKPLWNPISA-N CCC1CN(CCOc(cc2)ccc2/C(/c2cc(cccc3)c3[nH]2)=C(/CC)\c(c(Cl)c2)ccc2F)C1 Chemical compound CCC1CN(CCOc(cc2)ccc2/C(/c2cc(cccc3)c3[nH]2)=C(/CC)\c(c(Cl)c2)ccc2F)C1 AUEDHKLGKKFOPX-GKPLWNPISA-N 0.000 description 1
- BXAAATSLWSMYRK-UHFFFAOYSA-N Cc1c(C(C2)[O]2C(F)(F)F)cccc1 Chemical compound Cc1c(C(C2)[O]2C(F)(F)F)cccc1 BXAAATSLWSMYRK-UHFFFAOYSA-N 0.000 description 1
- ITQTTZVARXURQS-UHFFFAOYSA-N Cc1cccnc1 Chemical compound Cc1cccnc1 ITQTTZVARXURQS-UHFFFAOYSA-N 0.000 description 1
- YTCGOUNVIAWCMG-UHFFFAOYSA-N FC(c1cc(Cl)ccc1)(F)F Chemical compound FC(c1cc(Cl)ccc1)(F)F YTCGOUNVIAWCMG-UHFFFAOYSA-N 0.000 description 1
- VZHJIJZEOCBKRA-UHFFFAOYSA-N Fc1cc(Cl)ccc1 Chemical compound Fc1cc(Cl)ccc1 VZHJIJZEOCBKRA-UHFFFAOYSA-N 0.000 description 1
- CUPOOAWTRIURFT-UHFFFAOYSA-N N#Cc1ccc[s]1 Chemical compound N#Cc1ccc[s]1 CUPOOAWTRIURFT-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- 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
-
- 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
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 |
|---|---|
| AU2017239348A1 AU2017239348A1 (en) | 2018-11-15 |
| AU2017239348B2 true AU2017239348B2 (en) | 2020-03-12 |
Family
ID=59899253
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2017239348A Active AU2017239348B2 (en) | 2016-03-25 | 2017-03-24 | Substituted-indole compounds as estrogen receptor down-regulators |
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 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012037411A2 (en) * | 2010-09-16 | 2012-03-22 | Aragon Pharmaceuticals, Inc. | Estrogen receptor modulators and uses thereof |
Family Cites Families (6)
| 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 |
| 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
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012037411A2 (en) * | 2010-09-16 | 2012-03-22 | Aragon Pharmaceuticals, Inc. | Estrogen receptor modulators and uses thereof |
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 |
| 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 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| DA3 | Amendments made section 104 |
Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE INVENTION TITLE TO READ SUBSTITUTED-INDOLE COMPOUNDS AS ESTROGEN RECEPTOR DOWN-REGULATORS |
|
| HB | Alteration of name in register |
Owner name: LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD. Free format text: FORMER NAME(S): LUOXIN BIOTECHNOLOGY (SHANGHAI) CO., LTD; SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD. Owner name: SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LT Free format text: FORMER NAME(S): LUOXIN BIOTECHNOLOGY (SHANGHAI) CO., LTD; SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD. |
|
| FGA | Letters patent sealed or granted (standard patent) | ||
| PC | Assignment registered |
Owner name: LUOXIN HEALTHCARE SCIENCE AND TECHNOLOGY DEVELOPMENT (BEIJING) LTD. Free format text: FORMER OWNER(S): SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.; LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD. |