JPWO2022132652A5 - - Google Patents
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- JPWO2022132652A5 JPWO2022132652A5 JP2023535799A JP2023535799A JPWO2022132652A5 JP WO2022132652 A5 JPWO2022132652 A5 JP WO2022132652A5 JP 2023535799 A JP2023535799 A JP 2023535799A JP 2023535799 A JP2023535799 A JP 2023535799A JP WO2022132652 A5 JPWO2022132652 A5 JP WO2022132652A5
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- 238000000034 method Methods 0.000 claims description 127
- 150000001875 compounds Chemical class 0.000 claims description 126
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- AHJRHEGDXFFMBM-UHFFFAOYSA-N palbociclib Chemical compound N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 AHJRHEGDXFFMBM-UHFFFAOYSA-N 0.000 claims description 43
- 230000000392 somatic effect Effects 0.000 claims description 39
- 206010028980 Neoplasm Diseases 0.000 claims description 37
- 230000035772 mutation Effects 0.000 claims description 35
- 150000003839 salts Chemical class 0.000 claims description 34
- -1 glidants Substances 0.000 claims description 23
- 229910052739 hydrogen Inorganic materials 0.000 claims description 16
- 239000001257 hydrogen Substances 0.000 claims description 16
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 14
- 229940124297 CDK 4/6 inhibitor Drugs 0.000 claims description 12
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- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 9
- 229910052799 carbon Inorganic materials 0.000 claims description 9
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 9
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- PIMQWRZWLQKKBJ-SFHVURJKSA-N 2-[(2S)-1-[3-ethyl-7-[(1-oxido-3-pyridin-1-iumyl)methylamino]-5-pyrazolo[1,5-a]pyrimidinyl]-2-piperidinyl]ethanol Chemical compound C=1C(N2[C@@H](CCCC2)CCO)=NC2=C(CC)C=NN2C=1NCC1=CC=C[N+]([O-])=C1 PIMQWRZWLQKKBJ-SFHVURJKSA-N 0.000 claims description 6
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- PDGKHKMBHVFCMG-UHFFFAOYSA-N 2-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]spiro[7,8-dihydropyrazino[5,6]pyrrolo[1,2-d]pyrimidine-9,1'-cyclohexane]-6-one Chemical compound C1CN(C)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C2N3C4(CCCCC4)CNC2=O)C3=N1 PDGKHKMBHVFCMG-UHFFFAOYSA-N 0.000 claims description 6
- UELIMKCXGLIYCY-UHFFFAOYSA-N 4-[(2,6-dichlorobenzoyl)amino]-n-piperidin-4-yl-1h-pyrazole-5-carboxamide;methanesulfonic acid Chemical compound CS(O)(=O)=O.ClC1=CC=CC(Cl)=C1C(=O)NC1=CNN=C1C(=O)NC1CCNCC1 UELIMKCXGLIYCY-UHFFFAOYSA-N 0.000 claims description 6
- SGJLSPUSUBJWHO-UHFFFAOYSA-N 6-acetyl-8-cyclopentyl-5-methyl-2-[(5-piperidin-4-ylpyridin-2-yl)amino]pyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2N(C3CCCC3)C(=O)C(C(=O)C)=C(C)C2=CN=C1NC(N=C1)=CC=C1C1CCNCC1 SGJLSPUSUBJWHO-UHFFFAOYSA-N 0.000 claims description 6
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- 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 claims description 6
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- DUYNJNWVGIWJRI-LJAQVGFWSA-N acolbifene Chemical compound C1=CC([C@H]2C(=C(C3=CC=C(O)C=C3O2)C)C=2C=CC(O)=CC=2)=CC=C1OCCN1CCCCC1 DUYNJNWVGIWJRI-LJAQVGFWSA-N 0.000 claims description 6
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- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 claims description 6
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| KR20240063185A (ko) | 2016-12-01 | 2024-05-10 | 아비나스 오퍼레이션스, 인코포레이티드 | 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체 |
| WO2021041348A1 (en) | 2019-08-26 | 2021-03-04 | Arvinas Operations, Inc. | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
| JP2025526290A (ja) * | 2022-07-12 | 2025-08-13 | リージェンツ オブ ザ ユニバーシティー オブ ミシガン | エストロゲン受容体分解剤としてのテトラヒドロナフタレン誘導体 |
| TWI866427B (zh) * | 2022-08-31 | 2024-12-11 | 美商亞文納營運公司 | 雌激素受體降解劑之給藥方案 |
| WO2024196053A1 (ko) * | 2023-03-17 | 2024-09-26 | 재단법인 대구경북첨단의료산업진흥재단 | 에스트로겐-연관 수용체 감마 억제제 및 항암제의 병용요법용 조성물 |
| TW202440096A (zh) * | 2023-03-24 | 2024-10-16 | 美商亞文納營運公司 | 雌激素受體降解劑之給藥方案 |
| WO2024246825A1 (en) * | 2023-06-02 | 2024-12-05 | Pfizer Inc. | Combinations of estrogen receptor degraders and cdk4 inhibitors |
| TW202448458A (zh) * | 2023-06-02 | 2024-12-16 | 美商亞文納營運公司 | 雌激素受體降解劑與ａｋｔ抑制劑之組合 |
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| JP7504097B2 (ja) * | 2018-12-06 | 2024-06-21 | ラジウス ファーマシューティカルズ，インコーポレイテッド | Ｃｄｋ４／６阻害剤に耐性の癌を治療するための方法 |
| WO2021041348A1 (en) * | 2019-08-26 | 2021-03-04 | Arvinas Operations, Inc. | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
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