JP2018530549A5 - - Google Patents
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- JP2018530549A5 JP2018530549A5 JP2018516524A JP2018516524A JP2018530549A5 JP 2018530549 A5 JP2018530549 A5 JP 2018530549A5 JP 2018516524 A JP2018516524 A JP 2018516524A JP 2018516524 A JP2018516524 A JP 2018516524A JP 2018530549 A5 JP2018530549 A5 JP 2018530549A5
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- Prior art keywords
- compound
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- alkyl
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 110
- 229910052739 hydrogen Inorganic materials 0.000 claims description 39
- 239000001257 hydrogen Substances 0.000 claims description 39
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 28
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 25
- 125000000217 alkyl group Chemical group 0.000 claims description 23
- 150000003839 salts Chemical class 0.000 claims description 16
- 239000000203 mixture Substances 0.000 claims description 12
- 150000002431 hydrogen Chemical class 0.000 claims description 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 7
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- 229940011871 estrogen Drugs 0.000 claims description 3
- 239000000262 estrogen Substances 0.000 claims description 3
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims description 2
- 206010005949 Bone cancer Diseases 0.000 claims description 2
- 208000018084 Bone neoplasm Diseases 0.000 claims description 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 2
- 206010014733 Endometrial cancer Diseases 0.000 claims description 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 2
- 201000009273 Endometriosis Diseases 0.000 claims description 2
- 229940102550 Estrogen receptor antagonist Drugs 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 208000002495 Uterine Neoplasms Diseases 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 102000015694 estrogen receptors Human genes 0.000 claims description 2
- 108010038795 estrogen receptors Proteins 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 206010046766 uterine cancer Diseases 0.000 claims description 2
- 206010046885 vaginal cancer Diseases 0.000 claims description 2
- 208000013139 vaginal neoplasm Diseases 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims 4
- -1 salt compound Chemical class 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 8
- 238000000034 method Methods 0.000 description 7
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 6
- 125000005843 halogen group Chemical group 0.000 description 5
- 125000001153 fluoro group Chemical group F* 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 3
- VWUXBMIQPBEWFH-WCCTWKNTSA-N Fulvestrant Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC2=C1 VWUXBMIQPBEWFH-WCCTWKNTSA-N 0.000 description 2
- 229960002258 fulvestrant Drugs 0.000 description 2
- IPBQTKXTHVMANC-XHCCPWGMSA-N C[C@H](Cc1c2[nH]c3ccccc13)N(CC(C)(C)F)[C@@H]2c(cc1)ccc1OCCN1CC(CF)C1 Chemical compound C[C@H](Cc1c2[nH]c3ccccc13)N(CC(C)(C)F)[C@@H]2c(cc1)ccc1OCCN1CC(CF)C1 IPBQTKXTHVMANC-XHCCPWGMSA-N 0.000 description 1
- 208000017657 Menopausal disease Diseases 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 230000005907 cancer growth Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000014509 gene expression Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562235900P | 2015-10-01 | 2015-10-01 | |
| US62/235,900 | 2015-10-01 | ||
| PCT/US2016/054549 WO2017059139A1 (en) | 2015-10-01 | 2016-09-29 | TETRAHYDRO-1H-PYRIDO[3,4-b]INDOLE ANTI-ESTROGENIC DRUGS |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020169604A Division JP7277424B2 (ja) | 2015-10-01 | 2020-10-07 | テトラヒドロ－１Ｈ－ピリド［３，４－ｂ］インドール抗エストロゲン薬物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018530549A JP2018530549A (ja) | 2018-10-18 |
| JP2018530549A5 true JP2018530549A5 (enExample) | 2019-11-07 |
| JP6776348B2 JP6776348B2 (ja) | 2020-10-28 |
Family
ID=58427985
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018516524A Active JP6776348B2 (ja) | 2015-10-01 | 2016-09-29 | テトラヒドロ−１Ｈ−ピリド［３，４−ｂ］インドール抗エストロゲン薬物 |
| JP2020169604A Active JP7277424B2 (ja) | 2015-10-01 | 2020-10-07 | テトラヒドロ－１Ｈ－ピリド［３，４－ｂ］インドール抗エストロゲン薬物 |
| JP2023076673A Active JP7650316B2 (ja) | 2015-10-01 | 2023-05-08 | テトラヒドロ－１Ｈ－ピリド［３，４－ｂ］インドール抗エストロゲン薬物 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020169604A Active JP7277424B2 (ja) | 2015-10-01 | 2020-10-07 | テトラヒドロ－１Ｈ－ピリド［３，４－ｂ］インドール抗エストロゲン薬物 |
| JP2023076673A Active JP7650316B2 (ja) | 2015-10-01 | 2023-05-08 | テトラヒドロ－１Ｈ－ピリド［３，４－ｂ］インドール抗エストロゲン薬物 |
Country Status (26)
| Country | Link |
|---|---|
| US (5) | US10292971B2 (enExample) |
| EP (2) | EP3355884B1 (enExample) |
| JP (3) | JP6776348B2 (enExample) |
| KR (2) | KR102710603B1 (enExample) |
| CN (2) | CN108366996B (enExample) |
| AU (4) | AU2016331065B2 (enExample) |
| BR (2) | BR112018006121B1 (enExample) |
| CA (1) | CA3000410A1 (enExample) |
| CL (1) | CL2018000827A1 (enExample) |
| CY (1) | CY1124669T1 (enExample) |
| DK (1) | DK3355884T3 (enExample) |
| ES (1) | ES2881398T3 (enExample) |
| HR (1) | HRP20211124T1 (enExample) |
| HU (1) | HUE055321T2 (enExample) |
| IL (3) | IL310489A (enExample) |
| LT (1) | LT3355884T (enExample) |
| MX (2) | MX382269B (enExample) |
| NZ (1) | NZ779654A (enExample) |
| PL (1) | PL3355884T3 (enExample) |
| PT (1) | PT3355884T (enExample) |
| RS (1) | RS62133B1 (enExample) |
| RU (1) | RU2745742C1 (enExample) |
| SI (1) | SI3355884T1 (enExample) |
| SM (1) | SMT202100433T1 (enExample) |
| UA (1) | UA122346C2 (enExample) |
| WO (1) | WO2017059139A1 (enExample) |
Families Citing this family (41)
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| CN112375078B (zh) | 2014-12-18 | 2023-12-19 | 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 |
| KR102710603B1 (ko) | 2015-10-01 | 2024-09-27 | 올레마 파마슈티컬스 인코포레이티드 | 테트라히드로-1H-피리도[3,4-b]인돌 항에스트로겐 약물 |
| NZ743651A (en) | 2015-12-09 | 2023-07-28 | Univ Illinois | Benzothiophene-based selective estrogen receptor downregulators |
| WO2017136688A1 (en) | 2016-02-05 | 2017-08-10 | Inventisbio Inc. | Selective estrogen receptor degraders and uses thereof |
| US10125135B2 (en) | 2016-04-20 | 2018-11-13 | Astrazeneca Ab | Chemical compounds |
| US10149839B2 (en) | 2016-07-25 | 2018-12-11 | Astrazeneca Ab | Chemical compounds |
| US20190201526A1 (en) * | 2016-09-07 | 2019-07-04 | The Wistar Institute Of Anatomy And Biology | Methods and Compositions for Treating Cancers by Inhibiting Estrogen Signaling in Myeloid-Derived Suppressor Cells |
| LT3640251T (lt) | 2016-10-24 | 2022-03-10 | Astrazeneca Ab | 6,7,8,9-tetrahidro-3h-pirazolo[4,3-f]izochinolino dariniai, tinkami vėžio gydymui |
| WO2018081168A2 (en) | 2016-10-24 | 2018-05-03 | The Board Of Trustees Of The University Of Illinois | Benzothiophene-based selective mixed estrogen receptor downregulators |
| TWI823845B (zh) | 2017-01-06 | 2023-12-01 | 美商G1治療公司 | 用於治療癌症的組合療法 |
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| IL278063B2 (en) | 2018-06-21 | 2025-08-01 | Hoffmann La Roche | Solid forms 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 and processes for preparing fused tricyclic compounds comprising a substituted phenyl or pyridinyl moiety, including methods of their use |
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| JP2022532342A (ja) | 2019-05-14 | 2022-07-14 | ニューベイション・バイオ・インコーポレイテッド | 抗がん核内ホルモン受容体標的化化合物 |
| JP7616794B2 (ja) * | 2019-07-07 | 2025-01-17 | オレマ ファーマシューティカルズ インク． | エストロゲン受容体アンタゴニストのレジメン |
| TW202131930A (zh) | 2019-11-13 | 2021-09-01 | 美商諾維雪碧歐公司 | 抗癌核荷爾蒙受體標靶化合物 |
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| IL297216A (en) | 2020-04-24 | 2022-12-01 | Astrazeneca Ab | Dosage regimen for the treatment of cancer |
| JP7719796B2 (ja) | 2020-04-24 | 2025-08-06 | アストラゼネカ・アクチエボラーグ | 医薬製剤 |
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| WO2022166983A1 (zh) * | 2021-02-08 | 2022-08-11 | 贝达药业股份有限公司 | 杂芳基并哌啶类衍生物及其药物组合物和应用 |
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| JP2025526784A (ja) | 2022-08-11 | 2025-08-15 | イヴクスタ・バイオ | 癌を処置するための化合物 |
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