JP2019504890A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2019504890A5 JP2019504890A5 JP2018560447A JP2018560447A JP2019504890A5 JP 2019504890 A5 JP2019504890 A5 JP 2019504890A5 JP 2018560447 A JP2018560447 A JP 2018560447A JP 2018560447 A JP2018560447 A JP 2018560447A JP 2019504890 A5 JP2019504890 A5 JP 2019504890A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- pharmaceutically acceptable
- compound
- acceptable salt
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 81
- 150000003839 salts Chemical class 0.000 claims description 73
- 125000000217 alkyl group Chemical group 0.000 claims description 44
- 229910052739 hydrogen Inorganic materials 0.000 claims description 38
- 239000001257 hydrogen Substances 0.000 claims description 38
- 150000002431 hydrogen Chemical class 0.000 claims description 26
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 22
- 229910052801 chlorine Inorganic materials 0.000 claims description 22
- 239000000460 chlorine Substances 0.000 claims description 22
- 229910052736 halogen Inorganic materials 0.000 claims description 22
- 150000002367 halogens Chemical class 0.000 claims description 22
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 20
- 239000011737 fluorine Substances 0.000 claims description 20
- 229910052731 fluorine Inorganic materials 0.000 claims description 20
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 16
- 125000000623 heterocyclic group Chemical group 0.000 claims description 16
- 206010028980 Neoplasm Diseases 0.000 claims description 13
- 125000001072 heteroaryl group Chemical group 0.000 claims description 12
- 201000011510 cancer Diseases 0.000 claims description 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 10
- 125000004429 atom Chemical group 0.000 claims description 10
- 201000010099 disease Diseases 0.000 claims description 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
- 125000003118 aryl group Chemical group 0.000 claims description 8
- -1 -OR A Chemical group 0.000 claims description 5
- 230000002062 proliferating effect Effects 0.000 claims description 5
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 3
- 208000026310 Breast neoplasm Diseases 0.000 claims description 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 201000007281 estrogen-receptor positive breast cancer Diseases 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 238000000034 method Methods 0.000 description 4
- 210000000481 breast Anatomy 0.000 description 2
- 206010005003 Bladder cancer Diseases 0.000 description 1
- 206010008342 Cervix carcinoma Diseases 0.000 description 1
- 208000002250 Hematologic Neoplasms Diseases 0.000 description 1
- 206010046431 Urethral cancer Diseases 0.000 description 1
- 206010046458 Urethral neoplasms Diseases 0.000 description 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 description 1
- 206010047741 Vulval cancer Diseases 0.000 description 1
- 208000004354 Vulvar Neoplasms Diseases 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 201000010881 cervical cancer Diseases 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
- 206010046885 vaginal cancer Diseases 0.000 description 1
- 208000013139 vaginal neoplasm Diseases 0.000 description 1
- 201000005102 vulva cancer Diseases 0.000 description 1
- 208000028010 vulval Paget disease Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662291921P | 2016-02-05 | 2016-02-05 | |
| US62/291,921 | 2016-02-05 | ||
| PCT/US2017/016452 WO2017136688A1 (en) | 2016-02-05 | 2017-02-03 | Selective estrogen receptor degraders and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019504890A JP2019504890A (ja) | 2019-02-21 |
| JP2019504890A5 true JP2019504890A5 (enExample) | 2020-02-27 |
| JP6905539B2 JP6905539B2 (ja) | 2021-07-21 |
Family
ID=59501091
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018560447A Active JP6905539B2 (ja) | 2016-02-05 | 2017-02-03 | 選択的エストロゲン受容体分解剤およびその使用 |
Country Status (15)
| Country | Link |
|---|---|
| US (4) | US10647724B2 (enExample) |
| EP (1) | EP3411034B1 (enExample) |
| JP (1) | JP6905539B2 (enExample) |
| KR (1) | KR102479822B1 (enExample) |
| CN (2) | CN109362222B (enExample) |
| AU (1) | AU2017213614B2 (enExample) |
| BR (1) | BR112018015419B1 (enExample) |
| CA (1) | CA3012078C (enExample) |
| DK (1) | DK3411034T3 (enExample) |
| ES (1) | ES2842579T3 (enExample) |
| IL (1) | IL260789B (enExample) |
| MX (1) | MX387596B (enExample) |
| RU (1) | RU2734501C2 (enExample) |
| WO (1) | WO2017136688A1 (enExample) |
| ZA (1) | ZA201805573B (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20171330A1 (es) | 2014-12-18 | 2017-09-13 | Hoffmann La Roche | Tetrahidro-pirido[3,4-b]indoles moduladores de receptores de estrogenos y usos de los mismos |
| CA3011391C (en) * | 2015-11-12 | 2021-02-09 | Zhejiang Hisun Pharmaceutical Co., Ltd. | Acrylic acid derivative, preparation method and use in medicine thereof |
| DK3411034T3 (da) | 2016-02-05 | 2021-01-11 | Inventisbio Inc | Selektiv østrogenreceptornedbrydere og anvendelser deraf |
| JP6733872B2 (ja) * | 2016-02-26 | 2020-08-05 | ロンザ ウォーカーズヴィル，インコーポレーテッド | 肝細胞を寄せ集める方法 |
| EP3442971B1 (en) | 2016-04-01 | 2024-09-25 | Recurium IP Holdings, LLC | Estrogen receptor modulators |
| JP7018026B2 (ja) * | 2016-06-16 | 2022-02-09 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | ヘテロアリールエストロゲン受容体モジュレーター及びその使用 |
| CN107814798B (zh) * | 2016-09-14 | 2020-11-03 | 四川科伦博泰生物医药股份有限公司 | 3-取代丙烯酸类化合物及其制备方法和用途 |
| WO2018130124A1 (zh) * | 2017-01-11 | 2018-07-19 | 南京圣和药业股份有限公司 | 作为选择性雌激素受体下调剂的三环类化合物及其应用 |
| JP7348906B2 (ja) | 2018-02-28 | 2023-09-21 | フェロ セラピューティクス， インコーポレイテッド | フェロトーシス誘導活性を有する化合物およびそれらの使用方法 |
| CN111770924B (zh) * | 2018-04-04 | 2023-05-09 | 深圳福沃药业有限公司 | 用于治疗乳腺癌的雌激素受体降解剂 |
| WO2019222272A1 (en) | 2018-05-14 | 2019-11-21 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| EP3810283B1 (en) | 2018-06-21 | 2023-06-14 | F. Hoffmann-La Roche AG | Solid forms of the tartrate salt of 3-((1r,3r)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2h-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, process for their preparation and methods of their use in treating cancers |
| 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 |
| MX2021007687A (es) * | 2018-12-24 | 2021-10-13 | Inventisbio Co Ltd | Sales novedosas de degradadores selectivos de receptores de estrogeno. |
| US11040964B2 (en) | 2019-02-27 | 2021-06-22 | Ferro Therapeutics, Inc. | Compounds and methods of use |
| WO2020232119A1 (en) | 2019-05-14 | 2020-11-19 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| CN114929696A (zh) * | 2019-05-24 | 2022-08-19 | 浙江海正药业股份有限公司 | 丙烯酸类衍生物的晶型及其制备方法和用途 |
| JP2022543832A (ja) | 2019-08-06 | 2022-10-14 | リキュリウム アイピー ホールディングス リミテッド ライアビリティー カンパニー | 変異体を治療するためのエストロゲン受容体調節剤 |
| WO2021253380A1 (en) * | 2020-06-19 | 2021-12-23 | InventisBio Co., Ltd. | Oral formulations and uses thereof |
| US12345153B2 (en) | 2022-08-12 | 2025-07-01 | Saudi Arabian Oil Company | Distributed fiber-optic telemetry for data transmission and real-time location of downhole autonomous sensing devices |
| CN119907798A (zh) * | 2022-08-25 | 2025-04-29 | 赛诺菲 | 新颖的取代的2,3,4,9-四氢-1h-吡啶并[3,4-b]吲哚甲酸衍生物、其制备方法及其治疗用途 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005516967A (ja) | 2002-01-18 | 2005-06-09 | ザ ジェネティクス カンパニー インコーポレーティッド | β−セクレターゼインヒビター |
| US20030225132A1 (en) * | 2002-04-11 | 2003-12-04 | Dininno Frank P. | Estrogen receptor modulators |
| WO2004091488A2 (en) | 2003-04-14 | 2004-10-28 | Merck & Co., Inc. | Estrogen receptor modulators |
| PL1737461T3 (pl) | 2004-03-15 | 2013-05-31 | Ptc Therapeutics Inc | Pochodne karbolinowe użyteczne w hamowaniu angiogenezy |
| TW200930369A (en) | 2007-11-15 | 2009-07-16 | Astrazeneca Ab | Bis-(sulfonylamino) derivatives in therapy |
| US8703726B2 (en) * | 2009-05-27 | 2014-04-22 | Ptc Therapeutics, Inc. | Methods for treating prostate conditions |
| WO2010138706A1 (en) * | 2009-05-27 | 2010-12-02 | Ptc Therapeutics, Inc. | Methods for treating breast cancer |
| JP2013508397A (ja) * | 2009-10-22 | 2013-03-07 | ポリメディックス・インコーポレーテッド | 高分子化合物の調製方法 |
| DK2580210T5 (en) | 2010-06-10 | 2017-06-19 | Seragon Pharmaceuticals Inc | ESTROGEN RECEPTOR MODULATORS AND APPLICATIONS THEREOF |
| TWI560172B (en) * | 2011-11-02 | 2016-12-01 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
| EP2791133B1 (en) * | 2011-12-14 | 2019-04-17 | Seragon Pharmaceuticals, Inc. | Fluorinated estrogen receptor modulators and uses thereof |
| US20140122109A1 (en) * | 2012-10-29 | 2014-05-01 | Consuli, Inc. | Clinical diagnosis objects interaction |
| KR20150129723A (ko) * | 2013-03-14 | 2015-11-20 | 세라곤 파마슈티컬스, 인크. | 다환형 에스트로겐 수용체 조절제 및 이의 용도 |
| PE20160874A1 (es) | 2013-05-28 | 2016-09-04 | Astrazeneca Ab | Compuestos quimicos |
| CA2915534A1 (en) * | 2013-06-19 | 2014-12-24 | Seragon Pharmaceuticals, Inc. | Azetidine estrogen receptor modulators and uses thereof |
| CA2941161A1 (en) * | 2014-03-13 | 2015-09-17 | F.Hoffmann-La Roche Ag | Methods and compositions for modulating estrogen receptor mutants |
| EP3156054A4 (en) | 2014-06-12 | 2018-03-14 | ONO Pharmaceutical Co., Ltd. | Medicine for preventing and/or treating stress-induced diseases |
| PE20171330A1 (es) * | 2014-12-18 | 2017-09-13 | Hoffmann La Roche | Tetrahidro-pirido[3,4-b]indoles moduladores de receptores de estrogenos y usos de los mismos |
| AU2016279330B2 (en) | 2015-06-16 | 2020-05-14 | Jiangsu Hengrui Medicine Co., Ltd. | Piperidine derivative and preparation method and pharmaceutical use thereof |
| EP3355884B1 (en) | 2015-10-01 | 2021-04-28 | Olema Pharmaceuticals, Inc. | TETRAHYDRO-1H-PYRIDO[3,4-b]INDOLE ANTI-ESTROGENIC DRUGS |
| CA3011391C (en) * | 2015-11-12 | 2021-02-09 | Zhejiang Hisun Pharmaceutical Co., Ltd. | Acrylic acid derivative, preparation method and use in medicine thereof |
| DK3411034T3 (da) | 2016-02-05 | 2021-01-11 | Inventisbio Inc | Selektiv østrogenreceptornedbrydere og anvendelser deraf |
| EP3442971B1 (en) | 2016-04-01 | 2024-09-25 | Recurium IP Holdings, LLC | Estrogen receptor modulators |
| CN109843882A (zh) | 2016-06-16 | 2019-06-04 | 豪夫迈·罗氏有限公司 | 四氢-吡啶并[3,4-b]吲哚雌激素受体调节剂及其用途 |
| JP7018026B2 (ja) | 2016-06-16 | 2022-02-09 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | ヘテロアリールエストロゲン受容体モジュレーター及びその使用 |
| US20180002344A1 (en) | 2016-06-16 | 2018-01-04 | Genentech, Inc. | Heteroaryl estrogen receptor modulators and uses thereof |
| US10149839B2 (en) | 2016-07-25 | 2018-12-11 | Astrazeneca Ab | Chemical compounds |
| US10774081B2 (en) | 2016-10-28 | 2020-09-15 | Luoxin Pharmaceutical (Shanghai) Co., Ltd. | Indolo substituted piperidine compound as estrogen receptor down-regulator |
| WO2018130124A1 (zh) | 2017-01-11 | 2018-07-19 | 南京圣和药业股份有限公司 | 作为选择性雌激素受体下调剂的三环类化合物及其应用 |
| UA125043C2 (uk) | 2017-01-30 | 2021-12-29 | Астразенека Аб | Модулятори рецептора естрогену |
| MX2021007687A (es) * | 2018-12-24 | 2021-10-13 | Inventisbio Co Ltd | Sales novedosas de degradadores selectivos de receptores de estrogeno. |
-
2017
- 2017-02-03 DK DK17748247.8T patent/DK3411034T3/da active
- 2017-02-03 RU RU2018128318A patent/RU2734501C2/ru active
- 2017-02-03 WO PCT/US2017/016452 patent/WO2017136688A1/en not_active Ceased
- 2017-02-03 JP JP2018560447A patent/JP6905539B2/ja active Active
- 2017-02-03 CA CA3012078A patent/CA3012078C/en active Active
- 2017-02-03 MX MX2018009496A patent/MX387596B/es unknown
- 2017-02-03 CN CN201780008535.5A patent/CN109362222B/zh active Active
- 2017-02-03 AU AU2017213614A patent/AU2017213614B2/en active Active
- 2017-02-03 US US16/073,673 patent/US10647724B2/en active Active
- 2017-02-03 CN CN202110236070.7A patent/CN113004273A/zh active Pending
- 2017-02-03 EP EP17748247.8A patent/EP3411034B1/en active Active
- 2017-02-03 BR BR112018015419-9A patent/BR112018015419B1/pt active IP Right Grant
- 2017-02-03 ES ES17748247T patent/ES2842579T3/es active Active
- 2017-02-03 KR KR1020187025594A patent/KR102479822B1/ko active Active
-
2018
- 2018-07-26 IL IL260789A patent/IL260789B/en active IP Right Grant
- 2018-08-21 ZA ZA2018/05573A patent/ZA201805573B/en unknown
-
2019
- 2019-10-17 US US16/655,689 patent/US11014936B2/en active Active
-
2021
- 2021-04-27 US US17/241,722 patent/US20210253592A1/en not_active Abandoned
-
2023
- 2023-07-11 US US18/220,484 patent/US12187736B2/en active Active