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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- 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) | KR20240142622A (enExample) |
| CN (2) | CN113248494A (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 (2) | RU2745742C1 (enExample) |
| SI (1) | SI3355884T1 (enExample) |
| SM (1) | SMT202100433T1 (enExample) |
| UA (1) | UA122346C2 (enExample) |
| WO (1) | WO2017059139A1 (enExample) |
Families Citing this family (40)
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| EA032311B1 (ru) | 2014-12-18 | 2019-05-31 | Ф. Хоффманн-Ля Рош Аг | Тетрагидро-пиридо[3,4-b]индоловые модуляторы эстрогеновых рецепторов и их применение |
| HUE055321T2 (hu) * | 2015-10-01 | 2021-11-29 | Olema Pharmaceuticals Inc | Tetrahidro-1H-pirido[3,4-b]indol anti-ösztrogén hatóanyagok |
| CA3008020C (en) | 2015-12-09 | 2024-02-20 | The Board Of Trustees Of The University Of Illinois | Benzothiophene-based selective estrogen receptor downregulators |
| ES2842579T3 (es) * | 2016-02-05 | 2021-07-14 | Inventisbio Llc | Degradadores de los receptores de estrógenos selectivos y sus usos |
| US10125135B2 (en) | 2016-04-20 | 2018-11-13 | Astrazeneca Ab | Chemical compounds |
| WO2018019793A1 (en) * | 2016-07-25 | 2018-02-01 | Astrazeneca Ab | N-(2-(4-((1r,3r)-3-methyl-2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indol-1-yl)phenoxy)ethyl)propan-1-amine derivatives and related compounds as selective down-regulators of the estrogen receptor for treating cancer |
| WO2018049042A1 (en) * | 2016-09-07 | 2018-03-15 | The Wistar Institute Of Anatomy And Biology | Methods and compositions for treating cancers by inhibiting estrogen signaling in myeloid-derived suppressor cells |
| WO2018081168A2 (en) | 2016-10-24 | 2018-05-03 | The Board Of Trustees Of The University Of Illinois | Benzothiophene-based selective mixed estrogen receptor downregulators |
| JP6744489B2 (ja) | 2016-10-24 | 2020-08-19 | アストラゼネカ・アクチエボラーグＡｓｔｒａｚｅｎｅｃａ Ａｋｔｉｅｂｏｌａｇ | 癌の治療において有用な６，７，８，９−テトラヒドロ−３Ｈ−ピラゾロ［４，３−ｆ］イソキノリン誘導体 |
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| WO2019192533A1 (zh) * | 2018-04-04 | 2019-10-10 | 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 |
| EP3793608A4 (en) | 2018-05-14 | 2022-04-20 | Nuvation Bio Inc. | COMPOUNDS TARGETING ANTICANCER NUCLEAR HORMONE RECEPTORS |
| CN118239948A (zh) | 2018-06-21 | 2024-06-25 | 豪夫迈·罗氏有限公司 | 固体形式及制备稠合三环化合物的方法，包括其使用方法 |
| CA3123321A1 (en) * | 2018-12-24 | 2020-07-02 | InventisBio Co., Ltd. | Novel salts of selective estrogen receptor degraders |
| SG11202111402PA (en) * | 2019-05-14 | 2021-11-29 | Nuvation Bio Inc | Anti-cancer nuclear hormone receptor-targeting compounds |
| CA3144791A1 (en) * | 2019-07-07 | 2021-01-14 | Olema Pharmaceuticals, Inc. | Regimens of estrogen receptor antagonists |
| EP4058464A1 (en) | 2019-11-13 | 2022-09-21 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| AU2021230588A1 (en) * | 2020-03-06 | 2022-08-25 | Olema Pharmaceuticals, Inc. | Methods of treating estrogen receptor-associated diseases |
| KR20230005270A (ko) | 2020-04-24 | 2023-01-09 | 아스트라제네카 아베 | 약학적 제형 |
| AU2021260829B2 (en) | 2020-04-24 | 2024-01-11 | Astrazeneca Ab | Dosage regimen for the treatment of cancer |
| US11848549B2 (en) * | 2020-09-15 | 2023-12-19 | Easy Solar Products, Inc. | Junction box with flashing for a tile surface |
| EP4267578A4 (en) | 2020-12-23 | 2024-11-20 | Recurium IP Holdings, LLC | ESTROGEN RECEPTOR MODULATORS |
| 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 |
| JP2024516024A (ja) | 2021-05-03 | 2024-04-11 | 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 |
| WO2023283329A1 (en) * | 2021-07-08 | 2023-01-12 | Olema Pharmaceuticals, Inc. | Methods of treating estrogen receptor-associated diseases |
| WO2023091550A1 (en) * | 2021-11-18 | 2023-05-25 | Olema Pharmaceuticals, Inc. | Methods of treating estrogen receptor-associated diseases |
| WO2023221122A1 (en) * | 2022-05-20 | 2023-11-23 | Olema Pharmaceuticals, Inc. | Salts and solid forms of an estrogen receptor antagonist |
| WO2023221123A1 (en) * | 2022-05-20 | 2023-11-23 | Olema Pharmaceuticals, Inc. | Crystalline forms of an estrogen receptor antagonist |
| CA3262155A1 (en) | 2022-08-11 | 2024-02-15 | Evexta Bio | COMPOUNDS FOR CANCER TREATMENT |
| WO2024039860A1 (en) | 2022-08-19 | 2024-02-22 | Olema Pharmaceuticals, Inc. | 2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indole derivatives as estrogen receptor modulators for the treatment of cancer |
| WO2024039858A1 (en) | 2022-08-19 | 2024-02-22 | Olema Pharmaceuticals, Inc. | Estrogen receptor modulators and uses thereof |
| CA3262231A1 (en) | 2022-08-19 | 2024-02-22 | Olema Pharmaceuticals, Inc. | Estrogen receptor modulators and uses thereof |
| AU2023356291A1 (en) * | 2022-10-05 | 2025-04-17 | Novartis Ag | Methods of treating estrogen receptor-mediated disorders |
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| JP6266177B2 (ja) * | 2014-10-31 | 2018-01-24 | カーステン マニュファクチュアリング コーポレーション | ゴルフクラブヘッドの溝及びゴルフクラブヘッドの溝を製造する方法 |
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| EA032311B1 (ru) * | 2014-12-18 | 2019-05-31 | Ф. Хоффманн-Ля Рош Аг | Тетрагидро-пиридо[3,4-b]индоловые модуляторы эстрогеновых рецепторов и их применение |
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| US20180002344A1 (en) | 2016-06-16 | 2018-01-04 | Genentech, Inc. | Heteroaryl estrogen receptor modulators and uses thereof |
| 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 |
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| MY210254A (en) | 2018-07-12 | 2025-09-04 | Lilly Co Eli | Selective estrogen receptor degraders |
| TWI702219B (zh) | 2018-07-12 | 2020-08-21 | 美商美國禮來大藥廠 | 選擇性雌激素受體降解劑 |
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