JPWO2021139756A5 - - Google Patents
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- Publication number
- JPWO2021139756A5 JPWO2021139756A5 JP2022540980A JP2022540980A JPWO2021139756A5 JP WO2021139756 A5 JPWO2021139756 A5 JP WO2021139756A5 JP 2022540980 A JP2022540980 A JP 2022540980A JP 2022540980 A JP2022540980 A JP 2022540980A JP WO2021139756 A5 JPWO2021139756 A5 JP WO2021139756A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- heterocyclyl
- cycloalkyl
- alkyl
- halogen
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 84
- 125000000753 cycloalkyl group Chemical group 0.000 claims 63
- 125000000623 heterocyclic group Chemical group 0.000 claims 60
- 125000003118 aryl group Chemical group 0.000 claims 41
- 125000001072 heteroaryl group Chemical group 0.000 claims 41
- 229910052736 halogen Inorganic materials 0.000 claims 40
- 150000002367 halogens Chemical class 0.000 claims 40
- 125000003545 alkoxy group Chemical group 0.000 claims 37
- 150000001875 compounds Chemical class 0.000 claims 35
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 34
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 33
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 31
- 125000004093 cyano group Chemical group *C#N 0.000 claims 30
- 125000003277 amino group Chemical group 0.000 claims 25
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 25
- 239000000203 mixture Substances 0.000 claims 23
- 150000003839 salts Chemical class 0.000 claims 23
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 20
- 125000001188 haloalkyl group Chemical group 0.000 claims 20
- 125000001424 substituent group Chemical group 0.000 claims 19
- -1 cyano, amino Chemical group 0.000 claims 13
- XOJVVFBFDXDTEG-UHFFFAOYSA-N pristane Chemical compound CC(C)CCCC(C)CCCC(C)CCCC(C)C XOJVVFBFDXDTEG-UHFFFAOYSA-N 0.000 claims 13
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 230000007547 defect Effects 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 5
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 229910052805 deuterium Inorganic materials 0.000 claims 5
- 206010046766 uterine cancer Diseases 0.000 claims 5
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 4
- 125000003172 aldehyde group Chemical group 0.000 claims 4
- 125000004431 deuterium atom Chemical group 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000006239 protecting group Chemical group 0.000 claims 4
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 206010014733 Endometrial cancer Diseases 0.000 claims 3
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 3
- 206010033128 Ovarian cancer Diseases 0.000 claims 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 102000015694 estrogen receptors Human genes 0.000 claims 3
- 108010038795 estrogen receptors Proteins 0.000 claims 3
- 208000032839 leukemia Diseases 0.000 claims 3
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- 125000004434 sulfur atom Chemical group 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000001494 2-propynyl group Chemical group [H]C#CC([H])([H])* 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 2
- 208000013452 Fallopian tube neoplasm Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 1
- 208000031220 Hemophilia Diseases 0.000 claims 1
- 208000009292 Hemophilia A Diseases 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 125000003262 carboxylic acid ester group Chemical group [H]C([H])([*:2])OC(=O)C([H])([H])[*:1] 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 230000000593 degrading effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000002834 estrogen receptor modulator Substances 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 208000026278 immune system disease Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000003340 mental effect Effects 0.000 claims 1
- 230000002503 metabolic effect Effects 0.000 claims 1
- 230000000926 neurological effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 230000001850 reproductive effect Effects 0.000 claims 1
Applications Claiming Priority (13)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202010025118 | 2020-01-10 | ||
| CN202010025118.5 | 2020-01-10 | ||
| CN202010036802 | 2020-01-14 | ||
| CN202010036802.3 | 2020-01-14 | ||
| CN202010273891.3 | 2020-04-09 | ||
| CN202010273891 | 2020-04-09 | ||
| CN202010680491.4 | 2020-07-15 | ||
| CN202010680491 | 2020-07-15 | ||
| CN202010819555 | 2020-08-14 | ||
| CN202010819555.4 | 2020-08-14 | ||
| CN202010971693.4 | 2020-09-16 | ||
| CN202010971693 | 2020-09-16 | ||
| PCT/CN2021/070826 WO2021139756A1 (zh) | 2020-01-10 | 2021-01-08 | 三环四氢异喹啉类衍生物、其制备方法及其在医药上的应用 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2023509944A JP2023509944A (ja) | 2023-03-10 |
| JP2023509944A5 JP2023509944A5 (https=) | 2024-01-17 |
| JPWO2021139756A5 true JPWO2021139756A5 (https=) | 2024-01-17 |
| JP7657807B2 JP7657807B2 (ja) | 2025-04-07 |
Family
ID=76787742
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022540980A Active JP7657807B2 (ja) | 2020-01-10 | 2021-01-08 | 三環式テトラヒドロイソキノリン誘導体、その調製方法及びその医薬的応用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US12428428B2 (https=) |
| EP (1) | EP4089094A4 (https=) |
| JP (1) | JP7657807B2 (https=) |
| KR (1) | KR20220125272A (https=) |
| CN (2) | CN114746424B (https=) |
| AU (1) | AU2021205156A1 (https=) |
| BR (1) | BR112022013322A2 (https=) |
| CA (1) | CA3164166A1 (https=) |
| MX (1) | MX2022008091A (https=) |
| TW (1) | TWI882060B (https=) |
| WO (1) | WO2021139756A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114746424B (zh) | 2020-01-10 | 2023-06-16 | 江苏恒瑞医药股份有限公司 | 三环四氢异喹啉类衍生物、其制备方法及其在医药上的应用 |
| WO2023280309A1 (zh) | 2021-07-09 | 2023-01-12 | 江苏恒瑞医药股份有限公司 | 一种三环四氢异喹啉类衍生物的盐型 |
| CN117813288A (zh) | 2021-07-15 | 2024-04-02 | 西藏海思科制药有限公司 | 芳氨基衍生物雌激素受体调节剂及其用途 |
| JP2025529974A (ja) | 2022-09-09 | 2025-09-09 | サノフイ | 置換テトラヒドロシクロヘプタ［ｅ］インドール誘導体、それらの調製のプロセス及びその治療的使用 |
| TW202547495A (zh) * | 2024-04-01 | 2025-12-16 | 大陸商山東盛迪醫藥有限公司 | 一種選擇性雌激素受體降解劑的製備方法 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1113007A1 (en) | 1999-12-24 | 2001-07-04 | Pfizer Inc. | Tetrahydroisoquinoline compounds as estrogen agonists/antagonists |
| AU2007336811A1 (en) | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CN104066732B (zh) | 2011-11-15 | 2016-04-13 | 韩国化学硏究院 | 新型抗病毒吡咯并吡啶衍生物及其制备方法 |
| US20150336977A1 (en) | 2013-01-07 | 2015-11-26 | B.G. Negev Technologies And Applications Ltd. | Coumestan, Coumestrol, Coumestan Derivatives and Processes of Making the Same and Uses of Same |
| WO2014141292A2 (en) | 2013-03-04 | 2014-09-18 | Intas Pharmaceuticals Limited | Endoxifen citrate polymorph and process for preparing the same |
| ZA201401636B (en) | 2013-03-05 | 2014-11-26 | Cipla Ltd | Oxalic acid addition salts and/or solvates of a selective estrogen receptor modulator |
| JP2016517420A (ja) | 2013-03-14 | 2016-06-16 | セラゴン ファーマシューティカルズ， インク． | 多環式エストロゲン受容体モジュレーター及びその使用 |
| EP2981530B1 (en) | 2013-04-04 | 2020-02-12 | The Administrators of the Tulane Educational Fund | Enhanced osteogenic activity of daidzein analogs on human mesenchymal stem cells |
| TWI653235B (zh) | 2013-05-28 | 2019-03-11 | 阿斯特捷利康公司 | 作為抗癌劑之吲哚衍生物 |
| WO2015092634A1 (en) * | 2013-12-16 | 2015-06-25 | Novartis Ag | 1,2,3,4-tetrahydroisoquinoline compounds and compositions as selective estrogen receptor antagonists and degraders |
| KR20180012853A (ko) * | 2015-06-16 | 2018-02-06 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 피페리딘 유도체 및 이의 제조 방법 및 약학적 용도 |
| EP3328999B1 (en) | 2015-07-30 | 2020-03-25 | Arcis Biotechnology Holdings Limited | Method using a quaternary ammonium compound |
| US9969732B2 (en) * | 2016-04-08 | 2018-05-15 | Genentech, Inc. | Tetrahydroisoquinoline estrogen receptor modulators and uses thereof |
| TWI735681B (zh) | 2016-10-24 | 2021-08-11 | 瑞典商阿斯特捷利康公司 | 化合物 |
| 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 |
| WO2019002442A1 (en) * | 2017-06-29 | 2019-01-03 | Astrazeneca Ab | CHEMICAL COMPOUNDS |
| US11236088B2 (en) * | 2017-11-14 | 2022-02-01 | Kind Pharmaceutical | Heterocyclic compounds and their application in medicine |
| 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 |
| WO2019228443A1 (en) * | 2018-05-30 | 2019-12-05 | Dizal (Jiangsu) Pharmaceutical Co., Ltd. | Selective estrogen receptor downregulators and uses thereof |
| CN114746424B (zh) | 2020-01-10 | 2023-06-16 | 江苏恒瑞医药股份有限公司 | 三环四氢异喹啉类衍生物、其制备方法及其在医药上的应用 |
-
2021
- 2021-01-08 CN CN202180006879.9A patent/CN114746424B/zh active Active
- 2021-01-08 JP JP2022540980A patent/JP7657807B2/ja active Active
- 2021-01-08 KR KR1020227026103A patent/KR20220125272A/ko active Pending
- 2021-01-08 BR BR112022013322A patent/BR112022013322A2/pt unknown
- 2021-01-08 MX MX2022008091A patent/MX2022008091A/es unknown
- 2021-01-08 AU AU2021205156A patent/AU2021205156A1/en active Pending
- 2021-01-08 CA CA3164166A patent/CA3164166A1/en active Pending
- 2021-01-08 EP EP21738824.8A patent/EP4089094A4/en active Pending
- 2021-01-08 TW TW110100844A patent/TWI882060B/zh active
- 2021-01-08 US US17/790,110 patent/US12428428B2/en active Active
- 2021-01-08 WO PCT/CN2021/070826 patent/WO2021139756A1/zh not_active Ceased
- 2021-01-08 CN CN202310574384.7A patent/CN116731064A/zh active Pending
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