JP2019515026A5 - - Google Patents
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- Publication number
- JP2019515026A5 JP2019515026A5 JP2019503398A JP2019503398A JP2019515026A5 JP 2019515026 A5 JP2019515026 A5 JP 2019515026A5 JP 2019503398 A JP2019503398 A JP 2019503398A JP 2019503398 A JP2019503398 A JP 2019503398A JP 2019515026 A5 JP2019515026 A5 JP 2019515026A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- optionally substituted
- formula
- 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
- GDGULTXZDPTNNZ-NSCUHMNNSA-N methyl (E)-3-(3,5-difluoro-4-formylphenyl)prop-2-enoate Chemical compound COC(=O)\C=C\c1cc(F)c(C=O)c(F)c1 GDGULTXZDPTNNZ-NSCUHMNNSA-N 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 claims 37
- 150000003839 salts Chemical class 0.000 claims 23
- 239000008194 pharmaceutical composition Substances 0.000 claims 11
- 206010028980 Neoplasm Diseases 0.000 claims 9
- 201000011510 cancer Diseases 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 150000002431 hydrogen Chemical class 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 4
- 108010007005 Estrogen Receptor alpha Proteins 0.000 claims 3
- 102100038595 Estrogen receptor Human genes 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- OFBQJSOFQDEBGM-UHFFFAOYSA-N Pentane Chemical compound CCCCC OFBQJSOFQDEBGM-UHFFFAOYSA-N 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- HUMNYLRZRPPJDN-UHFFFAOYSA-N benzaldehyde Chemical compound O=CC1=CC=CC=C1 HUMNYLRZRPPJDN-UHFFFAOYSA-N 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- -1 difluorocyclobutyl Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 150000002440 hydroxy compounds Chemical class 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims 2
- 125000004211 3,5-difluorophenyl group Chemical group [H]C1=C(F)C([H])=C(*)C([H])=C1F 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002357 endometrial effect Effects 0.000 claims 1
- 201000010255 female reproductive organ cancer Diseases 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 230000003301 hydrolyzing effect Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000007918 intramuscular administration Methods 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- QNGNSVIICDLXHT-UHFFFAOYSA-N para-ethylbenzaldehyde Natural products CCC1=CC=C(C=O)C=C1 QNGNSVIICDLXHT-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 0 C**1*(C2)C2CC1 Chemical compound C**1*(C2)C2CC1 0.000 description 3
- HCOFVGDDABFNJB-UHFFFAOYSA-N CCCCc1ccccc1NCC Chemical compound CCCCc1ccccc1NCC HCOFVGDDABFNJB-UHFFFAOYSA-N 0.000 description 1
- RSVHQPLZYJNYJP-SVMLNYGMSA-N C[C@H](C1)N2C3(CC4C3)C4c3cc(/C=C/C(OC)=O)cc(F)c3[C@@H]2c2c1c(cccc1)c1[nH]2 Chemical compound C[C@H](C1)N2C3(CC4C3)C4c3cc(/C=C/C(OC)=O)cc(F)c3[C@@H]2c2c1c(cccc1)c1[nH]2 RSVHQPLZYJNYJP-SVMLNYGMSA-N 0.000 description 1
- BVOINHANKYWPHF-OPGSHWCFSA-N C[C@H](Cc1c[nH]c2ccccc12)NC1(C2)CC2C1 Chemical compound C[C@H](Cc1c[nH]c2ccccc12)NC1(C2)CC2C1 BVOINHANKYWPHF-OPGSHWCFSA-N 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021127863A JP2021176911A (ja) | 2016-04-01 | 2021-08-04 | エストロゲン受容体調節薬 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662317254P | 2016-04-01 | 2016-04-01 | |
| US62/317,254 | 2016-04-01 | ||
| PCT/US2017/024809 WO2017172957A1 (en) | 2016-04-01 | 2017-03-29 | Estrogen receptor modulators |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021127863A Division JP2021176911A (ja) | 2016-04-01 | 2021-08-04 | エストロゲン受容体調節薬 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019515026A JP2019515026A (ja) | 2019-06-06 |
| JP2019515026A5 true JP2019515026A5 (enExample) | 2020-05-07 |
| JP6926189B2 JP6926189B2 (ja) | 2021-08-25 |
Family
ID=59966438
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019503398A Active JP6926189B2 (ja) | 2016-04-01 | 2017-03-29 | エストロゲン受容体調節薬 |
| JP2021127863A Pending JP2021176911A (ja) | 2016-04-01 | 2021-08-04 | エストロゲン受容体調節薬 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021127863A Pending JP2021176911A (ja) | 2016-04-01 | 2021-08-04 | エストロゲン受容体調節薬 |
Country Status (15)
| Country | Link |
|---|---|
| US (5) | US20190142811A1 (enExample) |
| EP (1) | EP3442971B1 (enExample) |
| JP (2) | JP6926189B2 (enExample) |
| KR (2) | KR20220071293A (enExample) |
| CN (4) | CN112679495B (enExample) |
| AR (1) | AR108011A1 (enExample) |
| AU (3) | AU2017242027B2 (enExample) |
| CA (1) | CA3017388C (enExample) |
| ES (1) | ES2991862T3 (enExample) |
| IL (3) | IL295050A (enExample) |
| MX (2) | MX392461B (enExample) |
| RU (1) | RU2738646C2 (enExample) |
| SG (1) | SG11201807708SA (enExample) |
| TW (2) | TW202235418A (enExample) |
| WO (1) | WO2017172957A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6905539B2 (ja) | 2016-02-05 | 2021-07-21 | インベンティスバイオ リミテッド ライアビリティ カンパニー | 選択的エストロゲン受容体分解剤およびその使用 |
| CN112679495B (zh) | 2016-04-01 | 2023-03-28 | 里科瑞尔姆Ip控股有限责任公司 | 雌激素受体调节剂 |
| 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 |
| EP3665142A4 (en) | 2017-09-11 | 2021-04-28 | Recurium IP Holdings, LLC | CONTINUOUS CURRENT PROCESS FOR THE PRODUCTION OF BICYCLIC CONNECTIONS |
| JP2021503448A (ja) * | 2017-11-16 | 2021-02-12 | ノバルティス アーゲー | Ｌｓｚ１０２及びリボシクリブを含む医薬組合せ |
| WO2020238733A1 (zh) * | 2019-05-24 | 2020-12-03 | 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 |
| MX2022001149A (es) * | 2019-08-06 | 2022-04-06 | Recurium Ip Holdings Llc | Moduladores del receptor de estrógeno para el tratamiento de mutantes. |
| MX2022005139A (es) * | 2019-11-04 | 2022-06-24 | Recurium Ip Holdings Llc | Sales y formas de un modulador de receptores estrogénicos. |
| WO2021127042A1 (en) * | 2019-12-20 | 2021-06-24 | Recurium Ip Holdings, Llc | Combinations |
| AU2020407573A1 (en) * | 2019-12-20 | 2022-07-14 | Recurium Ip Holdings, Llc | Combinations |
| MX2022007627A (es) | 2019-12-20 | 2022-08-16 | Recurium Ip Holdings Llc | Combinaciones. |
| KR20220119418A (ko) * | 2019-12-20 | 2022-08-29 | 리커리엄 아이피 홀딩스, 엘엘씨 | 조합물 |
| WO2021127046A1 (en) * | 2019-12-20 | 2021-06-24 | Recurium Ip Holdings, Llc | Combinations |
| IL297448A (en) * | 2020-04-22 | 2022-12-01 | Recurium Ip Holdings Llc | Preparation of an selective estrogen receptor degrader |
| WO2021253380A1 (en) * | 2020-06-19 | 2021-12-23 | InventisBio Co., Ltd. | Oral formulations and uses thereof |
| AU2021343525A1 (en) * | 2020-09-20 | 2023-05-18 | Tactogen Inc | Advantageous tryptamine compositions for mental disorders or enhancement |
| WO2022133446A1 (en) * | 2020-12-16 | 2022-06-23 | Recurium Ip Holdings, Llc | Combinations |
| EP4267578A4 (en) * | 2020-12-23 | 2024-11-20 | Recurium IP Holdings, LLC | ESTROGEN RECEPTOR MODULATORS |
| WO2022153268A1 (en) | 2021-01-15 | 2022-07-21 | Beckley Psytech Limited | Tryptamine analogues |
| EP4366734A4 (en) * | 2021-07-08 | 2025-05-21 | Olema Pharmaceuticals, Inc. | METHODS OF TREATING DISEASES ASSOCIATED WITH ESTROGEN RECEPTOR |
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| GB9604996D0 (en) | 1996-03-08 | 1996-05-08 | Black James Foundation | Benzodiazonine derivatives |
| EP1113007A1 (en) * | 1999-12-24 | 2001-07-04 | Pfizer Inc. | Tetrahydroisoquinoline compounds as estrogen agonists/antagonists |
| EP1438310B1 (en) | 2001-10-19 | 2006-12-20 | TransTech Pharma Inc. | Beta-carbolin derivatives as ptp-inhibitors |
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| WO2007002051A1 (en) | 2005-06-22 | 2007-01-04 | Smithkline Beecham Corporation | Carboline derivatives and their use as inhibitors of flaviviridae infections |
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| KR101997592B1 (ko) | 2014-10-09 | 2019-07-08 | 광동 쫑성 파마세티컬 컴패니, 리미티드 | 히드록시퓨린계 화합물 및 이의 응용 |
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| JP6905539B2 (ja) * | 2016-02-05 | 2021-07-21 | インベンティスバイオ リミテッド ライアビリティ カンパニー | 選択的エストロゲン受容体分解剤およびその使用 |
| CN112679495B (zh) | 2016-04-01 | 2023-03-28 | 里科瑞尔姆Ip控股有限责任公司 | 雌激素受体调节剂 |
| JP6956747B2 (ja) | 2016-06-10 | 2021-11-02 | ユニバーシティ オブ テネシー リサーチ ファウンデーション | 選択的アンドロゲン受容体分解剤（ｓａｒｄ）リガンドおよびその使用方法 |
| CN109415361B (zh) * | 2016-06-29 | 2022-03-08 | 浙江海正药业股份有限公司 | 丙烯酸类衍生物及其制备方法和其在医药上的用途 |
| CN110139674B (zh) * | 2016-10-05 | 2023-05-16 | 豪夫迈·罗氏有限公司 | 制备抗体药物缀合物的方法 |
| 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 |
-
2017
- 2017-03-29 CN CN202011582762.9A patent/CN112679495B/zh active Active
- 2017-03-29 JP JP2019503398A patent/JP6926189B2/ja active Active
- 2017-03-29 CN CN201780033815.1A patent/CN109311870B/zh active Active
- 2017-03-29 RU RU2018132037A patent/RU2738646C2/ru active
- 2017-03-29 MX MX2018011419A patent/MX392461B/es unknown
- 2017-03-29 AU AU2017242027A patent/AU2017242027B2/en active Active
- 2017-03-29 KR KR1020227016946A patent/KR20220071293A/ko not_active Ceased
- 2017-03-29 SG SG11201807708SA patent/SG11201807708SA/en unknown
- 2017-03-29 IL IL295050A patent/IL295050A/en unknown
- 2017-03-29 CA CA3017388A patent/CA3017388C/en active Active
- 2017-03-29 CN CN202011582784.5A patent/CN112745316A/zh active Pending
- 2017-03-29 WO PCT/US2017/024809 patent/WO2017172957A1/en not_active Ceased
- 2017-03-29 ES ES17776574T patent/ES2991862T3/es active Active
- 2017-03-29 CN CN202111035485.4A patent/CN113717170A/zh active Pending
- 2017-03-29 KR KR1020187030841A patent/KR102401841B1/ko active Active
- 2017-03-29 US US16/086,434 patent/US20190142811A1/en not_active Abandoned
- 2017-03-29 IL IL285318A patent/IL285318B/en unknown
- 2017-03-29 EP EP17776574.0A patent/EP3442971B1/en active Active
- 2017-03-30 TW TW110145253A patent/TW202235418A/zh unknown
- 2017-03-30 TW TW106110662A patent/TWI746535B/zh active
- 2017-03-30 AR ARP170100788A patent/AR108011A1/es unknown
-
2018
- 2018-09-06 IL IL261654A patent/IL261654B/en unknown
- 2018-09-24 MX MX2022005780A patent/MX2022005780A/es unknown
-
2020
- 2020-05-05 US US16/866,995 patent/US10959989B2/en active Active
- 2020-05-05 US US16/867,017 patent/US11065234B2/en active Active
- 2020-05-05 US US16/866,900 patent/US11065233B2/en active Active
- 2020-12-22 AU AU2020294196A patent/AU2020294196B2/en active Active
-
2021
- 2021-07-06 US US17/305,369 patent/US20210330651A1/en not_active Abandoned
- 2021-08-04 JP JP2021127863A patent/JP2021176911A/ja active Pending
-
2022
- 2022-06-09 AU AU2022204025A patent/AU2022204025A1/en not_active Abandoned
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