JP2020530490A5 - - Google Patents
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- Publication number
- JP2020530490A5 JP2020530490A5 JP2020529797A JP2020529797A JP2020530490A5 JP 2020530490 A5 JP2020530490 A5 JP 2020530490A5 JP 2020529797 A JP2020529797 A JP 2020529797A JP 2020529797 A JP2020529797 A JP 2020529797A JP 2020530490 A5 JP2020530490 A5 JP 2020530490A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- hydroxyl
- halogen
- ethyl
- 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
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- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 76
- 125000000217 alkyl group Chemical group 0.000 claims 73
- 229910052736 halogen Inorganic materials 0.000 claims 46
- 150000002367 halogens Chemical class 0.000 claims 46
- 125000003545 alkoxy group Chemical group 0.000 claims 29
- 150000001875 compounds Chemical class 0.000 claims 28
- 125000000753 cycloalkyl group Chemical group 0.000 claims 26
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 24
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 19
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- -1 chloro, difluoromethyl Chemical group 0.000 claims 11
- 229910052799 carbon Inorganic materials 0.000 claims 10
- 125000001153 fluoro group Chemical group F* 0.000 claims 10
- 125000003282 alkyl amino group Chemical group 0.000 claims 9
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 7
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 7
- 125000001309 chloro group Chemical group Cl* 0.000 claims 6
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 4
- 125000002883 imidazolyl group Chemical group 0.000 claims 4
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 4
- 125000006584 (C3-C10) heterocycloalkyl group Chemical group 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000001246 bromo group Chemical group Br* 0.000 claims 2
- 239000000470 constituent Substances 0.000 claims 2
- 125000006001 difluoroethyl group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- AHHWIHXENZJRFG-UHFFFAOYSA-N oxetane Chemical compound C1COC1 AHHWIHXENZJRFG-UHFFFAOYSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 1
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 239000003098 androgen Substances 0.000 claims 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 150000004678 hydrides Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 125000004458 methylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])[H] 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 0 CCCN=Cc(cc(*(C)C*C)cc1*)c1NCC Chemical compound CCCN=Cc(cc(*(C)C*C)cc1*)c1NCC 0.000 description 5
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710667860.4 | 2017-08-07 | ||
| CN201710667860 | 2017-08-07 | ||
| CN201810333652 | 2018-04-13 | ||
| CN201810333652.5 | 2018-04-13 | ||
| PCT/CN2018/099161 WO2019029521A1 (zh) | 2017-08-07 | 2018-08-07 | 用作雄激素受体拮抗剂的二芳基硫代乙内酰脲化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020530490A JP2020530490A (ja) | 2020-10-22 |
| JP2020530490A5 true JP2020530490A5 (https=) | 2021-09-09 |
| JP7285838B2 JP7285838B2 (ja) | 2023-06-02 |
Family
ID=65270909
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020529797A Active JP7285838B2 (ja) | 2017-08-07 | 2018-08-07 | アンドロゲン受容体拮抗薬として使用されるジアリールチオヒダントイン化合物 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US11332465B2 (https=) |
| EP (1) | EP3666772A4 (https=) |
| JP (1) | JP7285838B2 (https=) |
| KR (1) | KR102658095B1 (https=) |
| CN (3) | CN113563311A (https=) |
| AU (1) | AU2018314980B2 (https=) |
| CA (1) | CA3072269A1 (https=) |
| WO (1) | WO2019029521A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3666772A4 (en) | 2017-08-07 | 2021-01-20 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | DIARYLTHIOHYDANTOIN COMPOUND AS ANDROGEN RECEPTOR ANTAGONIST |
| CN109422737B (zh) * | 2017-08-22 | 2021-07-30 | 上海时莱生物技术有限公司 | 咪唑酮类雄激素受体拮抗剂、其制备方法和用途 |
| BR112021015122A2 (pt) * | 2019-02-01 | 2021-09-28 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd | Cristal de composto de diariltio-hidantoína |
| CN110452166A (zh) * | 2019-09-06 | 2019-11-15 | 浙江朗华制药有限公司 | 一种5-异硫氰酰基-3-三氟甲基-2-氰基吡啶的制备方法 |
| CN114929702B (zh) * | 2020-01-19 | 2024-05-31 | 正大天晴药业集团股份有限公司 | 作为ar拮抗剂的二芳基硫代乙内酰脲化合物 |
| CN120112517A (zh) * | 2022-10-28 | 2025-06-06 | 南京明德新药研发有限公司 | 桥环类化合物及其在药学上的应用 |
| CN115724759B (zh) * | 2022-11-23 | 2024-06-25 | 爱斯特（成都）生物制药股份有限公司 | 一种恩扎卢胺中间体的制备方法 |
| CN116444444A (zh) * | 2023-03-27 | 2023-07-18 | 盐城工业职业技术学院 | 一种制备2-取代喹唑啉酮类化合物的方法 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT2656842T (lt) * | 2006-03-27 | 2016-09-26 | The Regents Of The University Of California | Androgeno receptoriaus moduliatorius, skirtas prostatos vėžio ir su androgeno receptoriumi susijusių ligų gydymui |
| CN101817787B (zh) * | 2009-02-26 | 2013-07-24 | 童友之 | 抗前列腺癌的雄性激素受体拮抗剂 |
| WO2011103202A2 (en) | 2010-02-16 | 2011-08-25 | Aragon Pharmaceuticals, Inc. | Androgen receptor modulators and uses thereof |
| WO2013084138A1 (en) | 2011-12-05 | 2013-06-13 | Novartis Ag | Cyclic urea derivatives as androgen receptor antagonists |
| CN103804358B (zh) | 2012-11-14 | 2016-06-29 | 上海医药集团股份有限公司 | 一类二芳基乙内酰脲衍生物、其制备方法、药物组合物和应用 |
| WO2015018356A1 (zh) | 2013-08-08 | 2015-02-12 | 上海医药集团股份有限公司 | 二芳基乙内酰脲衍生物、其制备方法、药物组合物和应用 |
| CN104341352A (zh) * | 2013-08-09 | 2015-02-11 | 南京衡杰生物科技有限公司 | 作为雄激素受体拮抗剂的二芳基乙内酰脲化合物及其应用 |
| CN104341342B (zh) | 2014-10-23 | 2016-04-13 | 中国电子科技集团公司第四十六研究所 | 一种高产率、高纯度的dast源粉合成工艺 |
| CN106146474A (zh) * | 2015-04-24 | 2016-11-23 | 成都贝斯凯瑞生物科技有限公司 | 硫代咪唑二酮和咪唑二酮类化合物及其用途 |
| TWI726969B (zh) * | 2016-01-11 | 2021-05-11 | 比利時商健生藥品公司 | 用作雄性激素受體拮抗劑之經取代之硫尿囊素衍生物 |
| CN110023297A (zh) | 2016-07-08 | 2019-07-16 | 詹森药业有限公司 | 作为雄性激素受体拮抗剂的取代的乙内酰脲和硫代己内酰脲衍生物 |
| RU2019108092A (ru) * | 2016-08-22 | 2020-09-22 | Янссен Фармацевтика Нв | Тиогидантоиновые антагонисты андрогеновых рецепторов для лечения рака |
| EP3666772A4 (en) | 2017-08-07 | 2021-01-20 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | DIARYLTHIOHYDANTOIN COMPOUND AS ANDROGEN RECEPTOR ANTAGONIST |
| CN109422737B (zh) * | 2017-08-22 | 2021-07-30 | 上海时莱生物技术有限公司 | 咪唑酮类雄激素受体拮抗剂、其制备方法和用途 |
| BR112021015122A2 (pt) | 2019-02-01 | 2021-09-28 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd | Cristal de composto de diariltio-hidantoína |
| CN114929702B (zh) * | 2020-01-19 | 2024-05-31 | 正大天晴药业集团股份有限公司 | 作为ar拮抗剂的二芳基硫代乙内酰脲化合物 |
-
2018
- 2018-08-07 EP EP18844090.3A patent/EP3666772A4/en active Pending
- 2018-08-07 JP JP2020529797A patent/JP7285838B2/ja active Active
- 2018-08-07 AU AU2018314980A patent/AU2018314980B2/en active Active
- 2018-08-07 CN CN202110901351.XA patent/CN113563311A/zh active Pending
- 2018-08-07 CA CA3072269A patent/CA3072269A1/en active Pending
- 2018-08-07 US US16/637,236 patent/US11332465B2/en active Active
- 2018-08-07 CN CN202110900404.6A patent/CN113582977B/zh active Active
- 2018-08-07 WO PCT/CN2018/099161 patent/WO2019029521A1/zh not_active Ceased
- 2018-08-07 KR KR1020207006521A patent/KR102658095B1/ko active Active
- 2018-08-07 CN CN201880055633.9A patent/CN111032644B/zh active Active
-
2021
- 2021-10-15 US US17/503,141 patent/US11866433B2/en active Active
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