JP2020100659A5 - - Google Patents
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- JP2020100659A5 JP2020100659A5 JP2020033150A JP2020033150A JP2020100659A5 JP 2020100659 A5 JP2020100659 A5 JP 2020100659A5 JP 2020033150 A JP2020033150 A JP 2020033150A JP 2020033150 A JP2020033150 A JP 2020033150A JP 2020100659 A5 JP2020100659 A5 JP 2020100659A5
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- JP
- Japan
- Prior art keywords
- inhibitor
- pharmaceutical composition
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- pharmaceutically acceptable
- stereoisomer
- 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.)
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- 239000003112 inhibitor Substances 0.000 claims 16
- 239000008194 pharmaceutical composition Substances 0.000 claims 14
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 239000002246 antineoplastic agent Substances 0.000 claims 8
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 8
- -1 acorbifene Chemical compound 0.000 claims 6
- 229960001603 tamoxifen Drugs 0.000 claims 6
- 230000000155 isotopic effect Effects 0.000 claims 5
- 108010012934 Albumin-Bound Paclitaxel Proteins 0.000 claims 4
- GAGWJHPBXLXJQN-UORFTKCHSA-N Capecitabine Chemical compound C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](C)O1 GAGWJHPBXLXJQN-UORFTKCHSA-N 0.000 claims 4
- GAGWJHPBXLXJQN-UHFFFAOYSA-N Capecitabine Natural products C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1C1C(O)C(O)C(C)O1 GAGWJHPBXLXJQN-UHFFFAOYSA-N 0.000 claims 4
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 4
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims 4
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 4
- 229930012538 Paclitaxel Natural products 0.000 claims 4
- 229940028652 abraxane Drugs 0.000 claims 4
- 229960004117 capecitabine Drugs 0.000 claims 4
- 229960003668 docetaxel Drugs 0.000 claims 4
- 229960005167 everolimus Drugs 0.000 claims 4
- 229960001592 paclitaxel Drugs 0.000 claims 4
- LKJPYSCBVHEWIU-KRWDZBQOSA-N (R)-bicalutamide Chemical compound C([C@@](O)(C)C(=O)NC=1C=C(C(C#N)=CC=1)C(F)(F)F)S(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-KRWDZBQOSA-N 0.000 claims 2
- FSPQCTGGIANIJZ-UHFFFAOYSA-N 2-[[(3,4-dimethoxyphenyl)-oxomethyl]amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide Chemical group C1=C(OC)C(OC)=CC=C1C(=O)NC1=C(C(N)=O)C(CCCC2)=C2S1 FSPQCTGGIANIJZ-UHFFFAOYSA-N 0.000 claims 2
- RHXHGRAEPCAFML-UHFFFAOYSA-N 7-cyclopentyl-n,n-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 RHXHGRAEPCAFML-UHFFFAOYSA-N 0.000 claims 2
- 229940126638 Akt inhibitor Drugs 0.000 claims 2
- 229940123877 Aurora kinase inhibitor Drugs 0.000 claims 2
- 239000012664 BCL-2-inhibitor Substances 0.000 claims 2
- 229940123711 Bcl2 inhibitor Drugs 0.000 claims 2
- 108010037003 Buserelin Proteins 0.000 claims 2
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims 2
- QXRSDHAAWVKZLJ-OXZHEXMSSA-N Epothilone B Natural products O=C1[C@H](C)[C@H](O)[C@@H](C)CCC[C@@]2(C)O[C@H]2C[C@@H](/C(=C\c2nc(C)sc2)/C)OC(=O)C[C@H](O)C1(C)C QXRSDHAAWVKZLJ-OXZHEXMSSA-N 0.000 claims 2
- 229940111980 Focal adhesion kinase inhibitor Drugs 0.000 claims 2
- 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 2
- 108010069236 Goserelin Proteins 0.000 claims 2
- 101000617830 Homo sapiens Sterol O-acyltransferase 1 Proteins 0.000 claims 2
- JJKOTMDDZAJTGQ-DQSJHHFOSA-N Idoxifene Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN2CCCC2)=CC=1)/C1=CC=C(I)C=C1 JJKOTMDDZAJTGQ-DQSJHHFOSA-N 0.000 claims 2
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims 2
- 239000003798 L01XE11 - Pazopanib Substances 0.000 claims 2
- 102000008135 Mechanistic Target of Rapamycin Complex 1 Human genes 0.000 claims 2
- 108010035196 Mechanistic Target of Rapamycin Complex 1 Proteins 0.000 claims 2
- 101100520074 Oryza sativa subsp. japonica PIK-1 gene Proteins 0.000 claims 2
- 239000012661 PARP inhibitor Substances 0.000 claims 2
- 229940116355 PI3 kinase inhibitor Drugs 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 claims 2
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 2
- 101710151245 Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 2
- 102100021993 Sterol O-acyltransferase 1 Human genes 0.000 claims 2
- 101000697584 Streptomyces lavendulae Streptothricin acetyltransferase Proteins 0.000 claims 2
- BPEGJWRSRHCHSN-UHFFFAOYSA-N Temozolomide Chemical compound O=C1N(C)N=NC2=C(C(N)=O)N=CN21 BPEGJWRSRHCHSN-UHFFFAOYSA-N 0.000 claims 2
- 108010050144 Triptorelin Pamoate Proteins 0.000 claims 2
- 229940124674 VEGF-R inhibitor Drugs 0.000 claims 2
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims 2
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims 2
- 229950001573 abemaciclib Drugs 0.000 claims 2
- 239000003719 aurora kinase inhibitor Substances 0.000 claims 2
- 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 2
- 229960000397 bevacizumab Drugs 0.000 claims 2
- 229960000997 bicalutamide Drugs 0.000 claims 2
- CUWODFFVMXJOKD-UVLQAERKSA-N buserelin Chemical compound CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](COC(C)(C)C)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H]1NC(=O)CC1)CC1=CC=C(O)C=C1 CUWODFFVMXJOKD-UVLQAERKSA-N 0.000 claims 2
- 229960002719 buserelin Drugs 0.000 claims 2
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical compound C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims 2
- 229940127093 camptothecin Drugs 0.000 claims 2
- 229960004562 carboplatin Drugs 0.000 claims 2
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 2
- 229960004316 cisplatin Drugs 0.000 claims 2
- 239000002875 cyclin dependent kinase inhibitor Substances 0.000 claims 2
- 229940043378 cyclin-dependent kinase inhibitor Drugs 0.000 claims 2
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 claims 2
- ZWAOHEXOSAUJHY-ZIYNGMLESA-N doxifluridine Chemical compound O[C@@H]1[C@H](O)[C@@H](C)O[C@H]1N1C(=O)NC(=O)C(F)=C1 ZWAOHEXOSAUJHY-ZIYNGMLESA-N 0.000 claims 2
- 229960004679 doxorubicin Drugs 0.000 claims 2
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 2
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 2
- HESCAJZNRMSMJG-HGYUPSKWSA-N epothilone A Natural products O=C1[C@H](C)[C@H](O)[C@H](C)CCC[C@H]2O[C@H]2C[C@@H](/C(=C\c2nc(C)sc2)/C)OC(=O)C[C@H](O)C1(C)C HESCAJZNRMSMJG-HGYUPSKWSA-N 0.000 claims 2
- QXRSDHAAWVKZLJ-PVYNADRNSA-N epothilone B Chemical compound C/C([C@@H]1C[C@@H]2O[C@]2(C)CCC[C@@H]([C@@H]([C@@H](C)C(=O)C(C)(C)[C@@H](O)CC(=O)O1)O)C)=C\C1=CSC(C)=N1 QXRSDHAAWVKZLJ-PVYNADRNSA-N 0.000 claims 2
- 229960001433 erlotinib Drugs 0.000 claims 2
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 2
- VJJPUSNTGOMMGY-MRVIYFEKSA-N etoposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@H](C)OC[C@H]4O3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 VJJPUSNTGOMMGY-MRVIYFEKSA-N 0.000 claims 2
- 229960005420 etoposide Drugs 0.000 claims 2
- MKXKFYHWDHIYRV-UHFFFAOYSA-N flutamide Chemical compound CC(C)C(=O)NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 MKXKFYHWDHIYRV-UHFFFAOYSA-N 0.000 claims 2
- 229960002074 flutamide Drugs 0.000 claims 2
- 229960002258 fulvestrant Drugs 0.000 claims 2
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims 2
- 229960005277 gemcitabine Drugs 0.000 claims 2
- 229960003690 goserelin acetate Drugs 0.000 claims 2
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims 2
- 229940121372 histone deacetylase inhibitor Drugs 0.000 claims 2
- 229950002248 idoxifene Drugs 0.000 claims 2
- 229960005386 ipilimumab Drugs 0.000 claims 2
- 229940043355 kinase inhibitor Drugs 0.000 claims 2
- GXESHMAMLJKROZ-IAPPQJPRSA-N lasofoxifene Chemical compound C1([C@@H]2[C@@H](C3=CC=C(C=C3CC2)O)C=2C=CC(OCCN3CCCC3)=CC=2)=CC=CC=C1 GXESHMAMLJKROZ-IAPPQJPRSA-N 0.000 claims 2
- 229960002367 lasofoxifene Drugs 0.000 claims 2
- BLCLNMBMMGCOAS-UHFFFAOYSA-N n-[1-[[1-[[1-[[1-[[1-[[1-[[1-[2-[(carbamoylamino)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[(2-methylpropan-2-yl)oxy]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amin Chemical compound C1CCC(C(=O)NNC(N)=O)N1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)C(COC(C)(C)C)NC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 BLCLNMBMMGCOAS-UHFFFAOYSA-N 0.000 claims 2
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 2
- UZWDCWONPYILKI-UHFFFAOYSA-N n-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine Chemical compound C1CN(CC)CCN1CC(C=N1)=CC=C1NC1=NC=C(F)C(C=2C=C3N(C(C)C)C(C)=NC3=C(F)C=2)=N1 UZWDCWONPYILKI-UHFFFAOYSA-N 0.000 claims 2
- XWXYUMMDTVBTOU-UHFFFAOYSA-N nilutamide Chemical compound O=C1C(C)(C)NC(=O)N1C1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 XWXYUMMDTVBTOU-UHFFFAOYSA-N 0.000 claims 2
- 229960002653 nilutamide Drugs 0.000 claims 2
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims 2
- 229960001756 oxaliplatin Drugs 0.000 claims 2
- WRUUGTRCQOWXEG-UHFFFAOYSA-N pamidronate Chemical compound NCCC(O)(P(O)(O)=O)P(O)(O)=O WRUUGTRCQOWXEG-UHFFFAOYSA-N 0.000 claims 2
- 229940046231 pamidronate Drugs 0.000 claims 2
- CUIHSIWYWATEQL-UHFFFAOYSA-N pazopanib Chemical compound C1=CC2=C(C)N(C)N=C2C=C1N(C)C(N=1)=CC=NC=1NC1=CC=C(C)C(S(N)(=O)=O)=C1 CUIHSIWYWATEQL-UHFFFAOYSA-N 0.000 claims 2
- 229960000639 pazopanib Drugs 0.000 claims 2
- QOFFJEBXNKRSPX-ZDUSSCGKSA-N pemetrexed Chemical compound C1=N[C]2NC(N)=NC(=O)C2=C1CCC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 QOFFJEBXNKRSPX-ZDUSSCGKSA-N 0.000 claims 2
- 229960005079 pemetrexed Drugs 0.000 claims 2
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 2
- 239000003197 protein kinase B inhibitor Substances 0.000 claims 2
- 229960004622 raloxifene Drugs 0.000 claims 2
- GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 claims 2
- 229950003687 ribociclib Drugs 0.000 claims 2
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- 229960000303 topotecan Drugs 0.000 claims 2
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims 2
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- VXKHXGOKWPXYNA-PGBVPBMZSA-N triptorelin Chemical compound C([C@@H](C(=O)N[C@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)NCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 VXKHXGOKWPXYNA-PGBVPBMZSA-N 0.000 claims 2
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Families Citing this family (165)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| JP6817962B2 (ja) | 2015-01-20 | 2021-01-20 | アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． | ターゲティングされたアンドロゲン受容体分解のための化合物および方法 |
| WO2016197114A1 (en) | 2015-06-05 | 2016-12-08 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| EP3319944A4 (en) | 2015-07-10 | 2019-04-24 | Arvinas, Inc. | MDM2-BASED MODULATORS OF PROTEOLYSIS AND RELATED USE METHODS |
| EP3337476A4 (en) | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| US20170281784A1 (en) | 2016-04-05 | 2017-10-05 | Arvinas, Inc. | Protein-protein interaction inducing technology |
| CN109562113A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的螺环降解决定子体 |
| CN109562107A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的杂环降解决定子体 |
| CN121974842A (zh) | 2016-05-10 | 2026-05-05 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| WO2017197046A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
| EP3512842B1 (en) | 2016-09-15 | 2024-01-17 | Arvinas, Inc. | Indole derivatives as estrogen receptor degraders |
| WO2018067702A1 (en) | 2016-10-04 | 2018-04-12 | Massachusetts Institute Of Technology | Bottlebrush copolymers and uses thereof |
| MX2019005007A (es) | 2016-11-01 | 2019-07-18 | Arvinas Inc | Protac dirigidos a la proteína tau y métodos asociados de uso. |
| IL266842B (en) | 2016-12-01 | 2022-09-01 | Arvinas Operations Inc | History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists |
| US10806737B2 (en) | 2016-12-23 | 2020-10-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| IL325835A (en) | 2016-12-23 | 2026-03-01 | Univ Yale | Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| CN110753693A (zh) | 2016-12-23 | 2020-02-04 | 阿尔维纳斯运营股份有限公司 | Egfr蛋白水解靶向嵌合分子和相关使用方法 |
| US11191741B2 (en) | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| IL300417A (en) | 2017-01-26 | 2023-04-01 | Arvinas Operations Inc | Bifunctional benzothiophene compounds, preparations containing them and their use in therapy |
| IL319363A (en) | 2017-01-31 | 2025-05-01 | Arvinas Operations Inc | Cervalon ligands and bifunctional compounds containing them |
| EP4717317A3 (en) | 2017-06-20 | 2026-06-03 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| WO2019043217A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROBENZIMIDAZOLONES |
| WO2019043208A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROQUINOLINONES |
| CN118108706A (zh) | 2017-09-04 | 2024-05-31 | C4医药公司 | 戊二酰亚胺 |
| EP3710002A4 (en) | 2017-11-16 | 2021-07-07 | C4 Therapeutics, Inc. | DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION |
| US11065231B2 (en) | 2017-11-17 | 2021-07-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides |
| JP2021512153A (ja) | 2018-01-26 | 2021-05-13 | イエール ユニバーシティ | タンパク質分解のイミド系モジュレーターおよび使用方法 |
| CN111902141A (zh) | 2018-03-26 | 2020-11-06 | C4医药公司 | 用于ikaros降解的羟脑苷脂结合剂 |
| US12539292B2 (en) | 2018-04-01 | 2026-02-03 | Arvinas Operations, Inc. | BRM targeting compounds and associated methods of use |
| BR112020020307A2 (pt) | 2018-04-04 | 2021-01-12 | Arvinas Operations, Inc. | Moduladores de proteólise e métodos de uso associados |
| EP3778590A4 (en) | 2018-04-09 | 2021-12-22 | ShanghaiTech University | ANTI PROTEIN DEGRADATION COMPOUND, ANTITUMOR APPLICATION, INTERMEDIATE THEREOF, AND INTERMEDIATE USE |
| CA3095912A1 (en) * | 2018-04-13 | 2019-10-17 | Arvinas Operations, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| WO2019204354A1 (en) | 2018-04-16 | 2019-10-24 | C4 Therapeutics, Inc. | Spirocyclic compounds |
| CN118344338A (zh) | 2018-04-23 | 2024-07-16 | 细胞基因公司 | 取代的4-氨基异吲哚啉-1,3-二酮化合物以及它们用于治疗淋巴瘤的用途 |
| EP3578561A1 (en) | 2018-06-04 | 2019-12-11 | F. Hoffmann-La Roche AG | Spiro compounds |
| AR116109A1 (es) | 2018-07-10 | 2021-03-31 | Novartis Ag | Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos |
| BR122022012697B1 (pt) | 2018-07-10 | 2023-04-04 | Novartis Ag | Usos de derivados de 3-(5-hidróxi-1-oxoisoindolin-2-il)piperidina-2,6- diona, e kit |
| WO2020027225A1 (ja) | 2018-07-31 | 2020-02-06 | ファイメクス株式会社 | 複素環化合物 |
| US11707452B2 (en) | 2018-08-20 | 2023-07-25 | Arvinas Operations, Inc. | Modulators of alpha-synuclein proteolysis and associated methods of use |
| WO2020051235A1 (en) | 2018-09-04 | 2020-03-12 | C4 Therapeutics, Inc. | Compounds for the degradation of brd9 or mth1 |
| SG11202105256QA (en) * | 2018-11-21 | 2021-06-29 | Accutar Biotechnology Inc | Novel compounds having estrogen receptor alpha degradation activity and uses thereof |
| AU2019402189B2 (en) * | 2018-12-20 | 2023-04-13 | Novartis Ag | Dosing regimen and pharmaceutical combination comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives |
| EP3897631A4 (en) | 2018-12-20 | 2022-11-23 | C4 Therapeutics, Inc. | TARGETED PROTEIN BREAKDOWN |
| KR20210136973A (ko) * | 2019-01-03 | 2021-11-17 | 더 리젠츠 오브 더 유니버시티 오브 미시간 | 에스트로겐 수용체 단백질 분해제 |
| WO2020160192A1 (en) | 2019-01-29 | 2020-08-06 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| WO2020160193A2 (en) | 2019-01-29 | 2020-08-06 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| KR102876423B1 (ko) * | 2019-02-07 | 2025-10-24 | 한국화학연구원 | 표적 단백질 ｅｅｄ 분해 유도 데그라듀서, 이의 제조방법 및 이를 유효성분으로 함유하는 ｅｅｄ, ｅｚｈ2, 또는 ｐｒｃ2 관련 질환의 예방 또는 치료용 약학적 조성물 |
| CA3123519A1 (en) * | 2019-02-15 | 2020-08-20 | Novartis Ag | Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| EP3924054B1 (en) * | 2019-02-15 | 2025-04-02 | Novartis AG | 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| EP3932922A4 (en) | 2019-02-25 | 2022-05-11 | ShanghaiTech University | SULPHUR-CONTAINING COMPOUND BASED ON A GLUTARIMIDE FRAMEWORK AND ITS USE |
| ES2995214T3 (en) | 2019-03-06 | 2025-02-07 | C4 Therapeutics Inc | Heterocyclic compounds for medical treatment |
| EP3941607A1 (en) | 2019-03-21 | 2022-01-26 | Codiak BioSciences, Inc. | Process for preparing extracellular vesicles |
| KR20210141554A (ko) | 2019-03-21 | 2021-11-23 | 코디악 바이오사이언시즈, 인크. | 세포외 소포 접합체 및 이의 용도 |
| TW202102497A (zh) | 2019-03-29 | 2021-01-16 | 瑞典商阿斯特捷利康公司 | 化合物及它們在治療癌症中之用途 |
| WO2020214555A1 (en) | 2019-04-16 | 2020-10-22 | Northwestern University | Bifunctional compounds comprising apcin-a and their use in the treatment of cancer |
| US12331061B2 (en) | 2019-04-18 | 2025-06-17 | Accutar Biotechnology Inc. | Compounds having BET, estrogen receptor, and androgen receptor degradation activity and uses thereof |
| JP2022533147A (ja) * | 2019-05-17 | 2022-07-21 | ヒノバ ファーマシューティカルズ インコーポレイテッド | 芳香族アミン類のａｒ及びｂｅｔを標的とするタンパク質分解キメラ化合物及び使用 |
| US12558427B2 (en) | 2019-07-17 | 2026-02-24 | Kymera Therapeutics, Inc. | IRAK degraders and uses thereof |
| EP3999182A1 (en) | 2019-07-17 | 2022-05-25 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| WO2021018118A1 (en) * | 2019-07-29 | 2021-02-04 | Janssen Pharmaceutica Nv | Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 1 proteins |
| WO2021022163A2 (en) | 2019-07-31 | 2021-02-04 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| WO2021023233A1 (zh) | 2019-08-05 | 2021-02-11 | 上海科技大学 | Egfr蛋白降解剂及其抗肿瘤应用 |
| WO2021041348A1 (en) * | 2019-08-26 | 2021-03-04 | Arvinas Operations, Inc. | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
| EP3795570B1 (en) * | 2019-09-23 | 2022-02-23 | Accutar Biotechnology Inc. | Substituted quinoline-8-carbonitrile derivatives having androgen receptor degradation activity and uses thereof |
| CN112574278B (zh) * | 2019-09-29 | 2024-08-23 | 江西济民可信集团有限公司 | 作为蛋白降解剂杂环类化合物及其制备方法和医药应用 |
| MX2022004526A (es) | 2019-10-17 | 2022-07-21 | Arvinas Operations Inc | Moléculas bifuncionales que contienen una porción de unión a la ligasa de ubiquitina e3 unida a una porción de direccionamiento a bcl6. |
| JP7629459B2 (ja) | 2019-11-19 | 2025-02-13 | ブリストル－マイヤーズ スクイブ カンパニー | Ｈｅｌｉｏｓタンパク質の阻害剤として有用な化合物 |
| IL293481A (en) * | 2019-12-06 | 2022-08-01 | Celgene Corp | Processes for the preparation of 2-(4-chlorophenyl)-n-((2-(2,6-dioxypyridin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide |
| CN115003295B (zh) * | 2019-12-12 | 2025-05-06 | 冰洲石生物科技公司 | 具有雌激素受体降解活性的新型色满衍生物及其用途 |
| JP7871189B2 (ja) * | 2019-12-17 | 2026-06-08 | オリオニス バイオサイエンシズ，インコーポレイテッド | タンパク質の動員および／または分解を調節する化合物 |
| US20230099031A1 (en) * | 2019-12-17 | 2023-03-30 | Orionis Biosciences, Inc. | Bifunctional agents for protein recruitment and/or degradation |
| PH12022551482A1 (en) | 2019-12-18 | 2023-11-29 | Novartis Ag | 3-(5-methoxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| WO2021127443A1 (en) | 2019-12-19 | 2021-06-24 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| CN116234803B (zh) * | 2019-12-23 | 2026-06-30 | 冰洲石生物科技公司 | 用于治疗癌症的雌激素受体降解剂和细胞周期蛋白依赖性激酶抑制剂的组合 |
| WO2021141662A1 (en) * | 2020-01-10 | 2021-07-15 | Massachusetts Institute Of Technology | Proteolysis targeting chimeric molecules (protacs) with functional handles and uses thereof |
| US12528825B2 (en) | 2020-01-29 | 2026-01-20 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| MX2022009308A (es) * | 2020-01-29 | 2022-08-22 | Foghorn Therapeutics Inc | Compuestos y usos de estos. |
| AU2021226514B2 (en) * | 2020-02-25 | 2023-10-19 | Shanghaitech University | Glutarimide skeleton-based compounds and application thereof |
| CN119823124A (zh) | 2020-03-05 | 2025-04-15 | C4医药公司 | 用于brd9的靶向降解的化合物 |
| TW202140441A (zh) * | 2020-03-23 | 2021-11-01 | 美商必治妥美雅史谷比公司 | 經取代之側氧基異吲哚啉化合物 |
| CN111393409A (zh) * | 2020-03-27 | 2020-07-10 | 苏州昊帆生物股份有限公司 | 蛋白降解靶向嵌合体化合物、应用及其制备方法 |
| US20220370416A1 (en) * | 2020-04-06 | 2022-11-24 | Arvinas Operations, Inc. | Compounds and methods for targeted degradation of kras |
| WO2021237100A1 (en) | 2020-05-21 | 2021-11-25 | Codiak Biosciences, Inc. | Methods of targeting extracellular vesicles to lung |
| WO2021255212A1 (en) | 2020-06-19 | 2021-12-23 | F. Hoffmann-La Roche Ag | Braf degraders |
| CN115916769B (zh) * | 2020-06-28 | 2024-09-10 | 深圳扬厉医药技术有限公司 | 并环吲唑类化合物 |
| CN116490186B (zh) | 2020-08-05 | 2025-10-31 | C4医药公司 | 用于ret的靶向降解的化合物 |
| WO2022047145A1 (en) | 2020-08-28 | 2022-03-03 | Arvinas Operations, Inc. | Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| AU2021342287A1 (en) * | 2020-09-14 | 2023-04-13 | Arvinas Operations, Inc. | Crystalline forms of a compound for the targeted degradation of estrogen receptor |
| CN112094275A (zh) * | 2020-09-16 | 2020-12-18 | 迪嘉药业集团有限公司 | 一种（右）佐匹克隆光降解杂质的制备方法 |
| WO2022066928A2 (en) | 2020-09-23 | 2022-03-31 | Codiak Biosciences, Inc. | Process for preparing extracellular vesicles |
| WO2022099117A1 (en) | 2020-11-06 | 2022-05-12 | Prelude Therapeutics Incorporated | Brm targeting compounds and associated methods of use |
| US20240058318A1 (en) * | 2020-12-10 | 2024-02-22 | Mayo Foundation For Medical Education And Research | Degrading pkcb1 to treat cancer |
| IL303143A (en) | 2020-12-14 | 2023-07-01 | Arvinas Operations Inc | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
| CN117242060B (zh) | 2021-01-13 | 2026-07-17 | 蒙特罗莎治疗股份有限公司 | 异吲哚啉酮化合物 |
| CN116438177B (zh) * | 2021-01-28 | 2025-09-16 | 江苏亚虹医药科技股份有限公司 | 靶向嵌合化合物、含其的药物组合物及其制备方法和用途 |
| US12655135B2 (en) | 2021-02-04 | 2026-06-16 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Benzo seven-membered ring bifunctional compound and application thereof |
| MX2023009178A (es) | 2021-02-15 | 2023-08-21 | Kymera Therapeutics Inc | Degradadores de la cinasa 4 asociada al receptor de interleucina 1 (irak4) y usos de los mismos. |
| JP2024512544A (ja) * | 2021-03-29 | 2024-03-19 | 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司 | テトラヒドロナフタレン系化合物、その製造方法及びその医薬的応用 |
| EP4320125A1 (en) | 2021-04-05 | 2024-02-14 | Bristol-Myers Squibb Company | Pyridinyl substituted oxoisoindoline compounds for the treatment of cancer |
| PE20231941A1 (es) | 2021-04-06 | 2023-12-05 | Bristol Myers Squibb Co | Compuestos de oxoisoindolina sustituidos con piridinilo |
| CN118388454A (zh) | 2021-04-16 | 2024-07-26 | 阿尔维纳斯运营股份有限公司 | Bcl6蛋白水解的调节剂和其相关使用方法 |
| MX2023012981A (es) * | 2021-05-03 | 2024-01-11 | Nurix Therapeutics Inc | Compuestos para inhibir o degradar proteinas objetivo, composiciones que los comprenden, metodos para su preparacion y metodos para usarlos. |
| US20240287076A1 (en) | 2021-05-05 | 2024-08-29 | Biogen Ma Inc. | Compounds for targeting degradation of bruton's tyrosine kinase |
| WO2022254362A1 (en) | 2021-06-03 | 2022-12-08 | Novartis Ag | 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and medical uses thereof |
| CA3224732A1 (en) | 2021-07-07 | 2023-01-12 | Kevin M. Guckian | Compounds for targeting degradation of irak4 proteins |
| WO2023283372A1 (en) | 2021-07-07 | 2023-01-12 | Biogen Ma Inc. | Compounds for targeting degradation of irak4 proteins |
| CN115611909A (zh) * | 2021-07-12 | 2023-01-17 | 江苏恒瑞医药股份有限公司 | 四氢萘类化合物、其制备方法及其在医药上的应用 |
| KR20240040769A (ko) * | 2021-07-26 | 2024-03-28 | 아비나스 오퍼레이션스, 인코포레이티드 | 이작용성 화합물을 제조하는 방법 |
| US20240368121A1 (en) * | 2021-08-20 | 2024-11-07 | Biotheryx, Inc. | Estrogen receptor degraders, pharmaceutical compositions thereof, and their therapeutic applications |
| JP2024539269A (ja) * | 2021-10-22 | 2024-10-28 | グルータクス セラピューティクス （シャンハイ） カンパニー、リミテッド | Ｃｒｂｎ ｅ３リガーゼリガンド化合物、当該リガンド化合物に基づいて開発したタンパク質分解剤及びそれらの応用 |
| WO2023083194A1 (zh) | 2021-11-09 | 2023-05-19 | 杭州格博生物医药有限公司 | Wee1蛋白激酶降解剂及其用途 |
| CN118488948A (zh) | 2021-12-22 | 2024-08-13 | 吉利德科学公司 | Ikaros锌指家族降解剂及其用途 |
| EP4455133A4 (en) * | 2021-12-24 | 2026-04-15 | Suzhou Kintor Pharmaceuticals Inc | MULTI-PROTEIN DEGRADING AGENT WITH AN IMIDE SKELETON |
| CA3240051A1 (en) | 2021-12-30 | 2023-07-06 | Beigene Switzerland Gmbh | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| CN114085213B (zh) * | 2022-01-20 | 2022-03-25 | 苏州国匡医药科技有限公司 | 一种arv-471的制备方法 |
| PL4245756T3 (pl) | 2022-03-17 | 2025-02-17 | Gilead Sciences, Inc. | Środki degradujące palec cynkowy z rodziny ikaros i ich zastosowania |
| JP2025512788A (ja) | 2022-03-25 | 2025-04-22 | シェンチェン ファーマシン シーオー．，エルティーディー． | Ｐｒｏｔａｃ化合物の医薬組成物及びその使用 |
| US12662467B2 (en) | 2022-04-18 | 2026-06-23 | BioThery X, Inc. | Isoindolinones, pharmaceutical compositions, and therapeutic applications |
| TW202404643A (zh) | 2022-04-20 | 2024-02-01 | 大陸商同宜醫藥（蘇州）有限公司 | 化合物及用途 |
| IL316803A (en) | 2022-06-06 | 2025-01-01 | C4 Therapeutics Inc | Bicyclic glutarimide-modified cervalon-binding agents |
| CN117229286A (zh) * | 2022-06-14 | 2023-12-15 | 海创药业股份有限公司 | 一种芳香类化合物及其制备方法及在制备雌激素受体降解剂中的用途 |
| WO2023242598A1 (en) * | 2022-06-16 | 2023-12-21 | Amphista Therapeutics Limited | Bifunctional molecules for targeted protein degradation |
| CA3260847A1 (en) * | 2022-06-27 | 2024-01-04 | Relay Therapeutics, Inc. | Estrogen Alpha Receptor Degrading Agents and Their Uses |
| WO2024006776A1 (en) * | 2022-06-27 | 2024-01-04 | Relay Therapeutics, Inc. | Estrogen receptor alpha degraders and medical use thereof |
| PE20251398A1 (es) * | 2022-06-30 | 2025-05-22 | Bristol Myers Squibb Co | Compuestos de degradacion de wee1 y usos de los mismos |
| EP4554948A1 (en) * | 2022-07-12 | 2025-05-21 | Regents of the University of Michigan | Tetrahydronaphthalene derivatives as estrogen receptor degraders |
| WO2024049922A1 (en) | 2022-08-31 | 2024-03-07 | Arvinas Operations, Inc. | Vepdegestrant for use in treating cancer |
| WO2024049926A1 (en) | 2022-08-31 | 2024-03-07 | Arvinas Operations, Inc. | Dosage regimens of estrogen receptor degraders |
| EP4584258A1 (en) | 2022-09-07 | 2025-07-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
| JP2025531869A (ja) * | 2022-09-09 | 2025-09-25 | イノヴォ セラピューティクス、インコーポレイテッド | ＣＫ１αおよびＤＵＡＬ ＣＫ１α／ＧＳＰＴ１分解化合物 |
| WO2024073507A1 (en) | 2022-09-28 | 2024-04-04 | Theseus Pharmaceuticals, Inc. | Macrocyclic compounds and uses thereof |
| JP2025533592A (ja) * | 2022-09-29 | 2025-10-07 | 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司 | テトラリン系誘導体の薬学的に許容される塩、結晶型及び調製方法 |
| WO2024083716A1 (en) | 2022-10-17 | 2024-04-25 | Astrazeneca Ab | Combinations of a serd for the treatment of cancer |
| US20240180893A1 (en) | 2022-11-17 | 2024-06-06 | Astrazeneca Ab | Methods of treatment of breast cancer |
| KR102794861B1 (ko) * | 2022-11-25 | 2025-04-11 | 재단법인 대구경북첨단의료산업진흥재단 | 선택적 에스트로겐 수용체 조절제로서의 신규 화합물 |
| WO2024119081A1 (en) | 2022-12-02 | 2024-06-06 | Arvinas Operations, Inc. | Method of treating breast cancer |
| CN116751186B (zh) * | 2022-12-23 | 2024-10-18 | 南京知和医药科技有限公司 | 一种雌激素受体调节剂的制备及其用途 |
| EP4644382A4 (en) * | 2022-12-27 | 2026-04-01 | Gluetacs Therapeutics Shanghai Co Ltd | ISOINDOLINONE SKELETON-BASED COMPOUND WITH SULFUR/OXYGEN SUBSTITUTED GLUTARIMIDE AND ITS USE |
| WO2024141052A1 (zh) * | 2022-12-30 | 2024-07-04 | 江苏威凯尔医药科技有限公司 | 雌激素受体调节剂及其用途 |
| PE20260006A1 (es) | 2023-01-26 | 2026-01-06 | Arvinas Operations Inc | Protacs degradadores de kras basados en cereblon y usos relacionados con los mismos |
| WO2024167904A1 (en) | 2023-02-07 | 2024-08-15 | Arvinas Operations, Inc. | Dosage regimens of estrogen receptor degraders in combination with an mtor inhibitor |
| 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 |
| JP2026515235A (ja) | 2023-05-11 | 2026-05-14 | アストラゼネカ・アクチエボラーグ | 癌を治療するためのｐａｒｐ１阻害剤と選択的エストロゲン分解薬の併用 |
| JP2026518466A (ja) | 2023-06-02 | 2026-06-08 | アルビナス・オペレーションズ・インコーポレイテッド | エストロゲン受容体分解剤とａｋｔ阻害剤との組み合わせ |
| JP2026519559A (ja) | 2023-06-02 | 2026-06-16 | ファイザー・インク | エストロゲン受容体分解薬およびｃｄｋ４阻害剤の組合せ |
| WO2024258856A1 (en) | 2023-06-12 | 2024-12-19 | Arvinas Operations, Inc. | Solid oral dosage forms of estrogen receptor degraders |
| WO2025006569A1 (en) | 2023-06-27 | 2025-01-02 | Arvinas Operations, Inc. | Combinations of estrogen receptor degraders and cdk7 inhibitors for the treatment of cancer |
| WO2025038481A1 (en) | 2023-08-11 | 2025-02-20 | Arvinas Operations, Inc. | Vepdegestrant dosage regimen in cyp3a-inducer treatment in cancer |
| WO2025085738A1 (en) | 2023-10-18 | 2025-04-24 | Halda Therapeutics Opco, Inc. | Heterobifunctional compounds and methods of treating disease |
| WO2025090847A1 (en) * | 2023-10-25 | 2025-05-01 | Bpgbio, Inc. | Estrogen receptor degraders and their use in the treatment of cancer |
| WO2025114875A1 (en) | 2023-12-01 | 2025-06-05 | Astrazeneca Ab | Er degraders and uses thereof |
| CN120118067A (zh) * | 2023-12-08 | 2025-06-10 | 江苏威凯尔医药科技股份有限公司 | 雌激素受体调节剂及其用途 |
| WO2025193454A1 (en) | 2024-03-01 | 2025-09-18 | Prelude Therapeutics Incorporated | Brm and brg1 targeting antibody-drug conjugates and methods of use thereof |
| WO2025189056A1 (en) | 2024-03-08 | 2025-09-12 | Halda Therapeutics Opco, Inc. | Heterobifunctional compounds and their use in treating disease |
| WO2025245032A1 (en) * | 2024-05-20 | 2025-11-27 | Arvinas Operations, Inc. | Methods of manufacturing a bifunctional compound |
| WO2026017799A1 (en) | 2024-07-18 | 2026-01-22 | Centre Hospitalier Universitaire Vaudois | Substituted 3-cyanoquinolines for the prevention and treatment of sexually transmitted diseases |
| WO2026018182A1 (en) | 2024-07-19 | 2026-01-22 | Pfizer Inc. | Process for preparing a cis-1,2-diaryltetralin derivative |
| WO2026044127A1 (en) | 2024-08-22 | 2026-02-26 | Arvinas Operations, Inc. | Administration of cyp3a inhibitors in the treatment of cancer |
| WO2026052822A1 (en) | 2024-09-06 | 2026-03-12 | Amphista Therapeutics Limited | Tetrahydroisoquinoline compounds for targeted protein degradation |
| WO2026102147A1 (en) * | 2024-11-07 | 2026-05-15 | Treeline Biosciences, Inc. | Tetrahydroisoquinoline heterobifunctional bcl-xl degraders |
| WO2026102277A1 (en) * | 2024-11-08 | 2026-05-15 | Plexium, Inc. | Combination therapies comprising ikzf2 degrader compounds |
| WO2026128391A1 (en) | 2024-12-09 | 2026-06-18 | Arvinas Operations, Inc. | Combinations of vepdegestrant and cdk4/6 inhibitors for treating esr1-mutant breast cancer |
| WO2026138908A1 (zh) * | 2024-12-24 | 2026-07-02 | 海创药业股份有限公司 | 一种雌激素受体降解剂中间体及其制备方法 |
Family Cites Families (152)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| US5681835A (en) | 1994-04-25 | 1997-10-28 | Glaxo Wellcome Inc. | Non-steroidal ligands for the estrogen receptor |
| US5510357A (en) | 1995-02-28 | 1996-04-23 | Eli Lilly And Company | Benzothiophene compounds as anti-estrogenic agents |
| DE69740140D1 (de) | 1996-07-24 | 2011-04-14 | Celgene Corp | Substituierte 2-(2,6-Dioxopiperidin-3-yl)-phthalimide und Oxoisoindoline und Verfahren zur Verringerung der TNF-Alpha-Stufen |
| US5916916A (en) | 1996-10-10 | 1999-06-29 | Eli Lilly And Company | 1-aryloxy-2-arylnaphthyl compounds, intermediates, compositions, and methods |
| ZA982877B (en) | 1997-04-09 | 1999-10-04 | Lilly Co Eli | Treatment of central nervous system disorders with selective estrogen receptor modulators. |
| ATE460423T1 (de) | 1997-05-14 | 2010-03-15 | Sloan Kettering Inst Cancer | Verfahren und zubereitungen zur zerstörung bestimmter proteine |
| JP2001517664A (ja) | 1997-09-23 | 2001-10-09 | イーライ・リリー・アンド・カンパニー | ベンゾチオフェン類 |
| PT966968E (pt) * | 1998-06-16 | 2004-08-31 | Pfizer Prod Inc | Combinacoes terapeuticas compreendendo um modulador de receptor de estrogenio selectivo e prostaglandina e2 |
| US6306663B1 (en) | 1999-02-12 | 2001-10-23 | Proteinex, Inc. | Controlling protein levels in eucaryotic organisms |
| EP1176959B1 (en) | 1999-05-05 | 2006-03-08 | Merck & Co., Inc. | Novel prolines as antimicrobial agents |
| US7208157B2 (en) | 2000-09-08 | 2007-04-24 | California Institute Of Technology | Proteolysis targeting chimeric pharmaceutical |
| AU2001295041A1 (en) | 2000-09-08 | 2002-03-22 | California Institute Of Technology | Proteolysis targeting chimeric pharmaceutical |
| US7091353B2 (en) | 2000-12-27 | 2006-08-15 | Celgene Corporation | Isoindole-imide compounds, compositions, and uses thereof |
| US20030045552A1 (en) | 2000-12-27 | 2003-03-06 | Robarge Michael J. | Isoindole-imide compounds, compositions, and uses thereof |
| WO2002066512A1 (en) | 2001-02-16 | 2002-08-29 | E.I. Dupont De Nemours And Company | Angiogenesis-inhibitory tripeptides, compositions and their methods of use |
| HN2002000136A (es) | 2001-06-11 | 2003-07-31 | Basf Ag | Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis |
| US7030141B2 (en) | 2001-11-29 | 2006-04-18 | Christopher Franklin Bigge | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade |
| CA2491041A1 (en) | 2002-07-02 | 2004-01-15 | Novartis Ag | Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap) |
| EP1651595A2 (en) | 2003-05-30 | 2006-05-03 | Rigel Pharmaceuticals, Inc. | Ubiquitin ligase inhibitors |
| BRPI0506883A (pt) | 2004-01-16 | 2007-05-29 | Univ Michigan | miméticos de smac conformacionalmente comprimidos e seus usos |
| US7345081B2 (en) | 2004-03-23 | 2008-03-18 | Genentech, Inc. | Azabicyclo-octane inhibitors of IAP |
| PL2253614T3 (pl) | 2004-04-07 | 2013-03-29 | Novartis Ag | Inhibitory IAP |
| KR100926203B1 (ko) | 2004-07-02 | 2009-11-09 | 제넨테크, 인크. | Ｉａｐ의 억제제 |
| MX2007007195A (es) | 2004-12-20 | 2007-10-08 | Genentech Inc | Inhibidores de pirrolidina de iap. |
| TW200639163A (en) | 2005-02-04 | 2006-11-16 | Genentech Inc | RAF inhibitor compounds and methods |
| EA012810B1 (ru) | 2005-02-25 | 2009-12-30 | Тетралоджик Фармасеутикалс | Димерные ингибиторы ингибиторов белков апоптоза (iap) |
| CN100383139C (zh) | 2005-04-07 | 2008-04-23 | 天津和美生物技术有限公司 | 可抑制细胞释放肿瘤坏死因子的哌啶-2，6-二酮衍生物 |
| US20060252698A1 (en) | 2005-04-20 | 2006-11-09 | Malcolm Bruce A | Compounds for inhibiting cathepsin activity |
| CA2822094C (en) | 2005-08-31 | 2015-10-27 | Celgene Corporation | Isoindole-imide compounds and compositions comprising and methods of using the same |
| WO2007106670A2 (en) | 2006-03-03 | 2007-09-20 | Novartis Ag | N-formyl hydroxylamine compounds |
| WO2007101347A1 (en) | 2006-03-07 | 2007-09-13 | Aegera Therapeutics Inc. | Bir domain binding compounds |
| JP2009530415A (ja) | 2006-03-20 | 2009-08-27 | バーテックス ファーマシューティカルズ インコーポレイテッド | 医薬組成物 |
| ES2525585T3 (es) | 2006-05-05 | 2014-12-26 | The Regents Of The University Of Michigan | Intermedios para la preparación de miméticos de SMAC bivalentes |
| AU2007275415A1 (en) | 2006-07-20 | 2008-01-24 | Ligand Pharmaceuticals Incorporated | Proline urea CCR1 antagonists for the treatment of autoimmune diseases or inflammation |
| US20100056495A1 (en) | 2006-07-24 | 2010-03-04 | Tetralogic Pharmaceuticals Corporation | Dimeric iap inhibitors |
| AU2007290407A1 (en) | 2006-08-30 | 2008-03-06 | Celgene Corporation | 5-substituted isoindoline compounds |
| US8877780B2 (en) | 2006-08-30 | 2014-11-04 | Celgene Corporation | 5-substituted isoindoline compounds |
| RU2448101C2 (ru) | 2006-08-30 | 2012-04-20 | Селджин Корпорейшн | 5-замещенные изоиндолиновые соединения |
| WO2008054827A2 (en) | 2006-11-03 | 2008-05-08 | Pharmacyclics, Inc. | Bruton's tyrosine kinase activity probe and method of using |
| WO2008109057A1 (en) | 2007-03-02 | 2008-09-12 | Dana-Farber Cancer Institute, Inc. | Organic compounds and their uses |
| CA2684169C (en) | 2007-04-12 | 2012-06-19 | Joyant Pharmaceuticals, Inc. | Smac mimetic dimers and trimers useful as anti-cancer agents |
| WO2008128171A2 (en) | 2007-04-13 | 2008-10-23 | The Regents Of The University Of Michigan | Diazo bicyclic smac mimetics and the uses thereof |
| NZ598890A (en) | 2007-04-30 | 2013-10-25 | Genentech Inc | Inhibitors of iap |
| WO2008144925A1 (en) | 2007-05-30 | 2008-12-04 | Aegera Therapeutics Inc. | Iap bir domain binding compounds |
| US8648069B2 (en) | 2007-06-08 | 2014-02-11 | Abbvie Inc. | 5-substituted indazoles as kinase inhibitors |
| CN101790526A (zh) * | 2007-06-08 | 2010-07-28 | 雅培制药有限公司 | 用作激酶抑制剂的5-杂芳基取代的吲唑化合物 |
| US8415340B2 (en) | 2007-07-25 | 2013-04-09 | Bristol-Myers Squibb Company | Triazine kinase inhibitors |
| AR067813A1 (es) | 2007-08-06 | 2009-10-21 | Janssen Pharmaceutica Nv | Fenilendiaminas sustituidas como inhibidores de l ainteraccion entre mdm2 y p53 |
| EP2058312A1 (en) | 2007-11-09 | 2009-05-13 | Universita' degli Studi di Milano | SMAC mimetic compounds as apoptosis inducers |
| CA2957226C (en) | 2008-10-29 | 2018-08-14 | Celgene Corporation | Isoindoline compounds for use in the treatment of cancer |
| NZ614305A (en) | 2008-12-05 | 2015-03-27 | Abbvie Inc | Sulfonamide derivatives as bcl-2-selective apoptosis-inducing agents for the treatment of cancer and immune diseases |
| ES2443948T3 (es) * | 2008-12-19 | 2014-02-21 | Bristol-Myers Squibb Company | Compuestos de carbazol carboxamida útiles como inhibidores de quinasas |
| US8063102B2 (en) * | 2009-03-13 | 2011-11-22 | N.V. Organon | Tetrahydronaphthalen-2-ol derivatives |
| WO2010107485A1 (en) | 2009-03-17 | 2010-09-23 | The Trustees Of Columbia University In The City Of New York | E3 ligase inhibitors |
| ES2546294T7 (es) | 2009-05-26 | 2024-06-06 | Abbvie Ireland Unlimited Co | Agentes inductores de la apoptosis para el tratamiento de cáncer y enfermedades inmunitarias y autoinmunitarias |
| WO2010141805A1 (en) | 2009-06-05 | 2010-12-09 | Janssen Pharmaceutica Nv | Heterocyclic amides as modulators of trpa1 |
| WO2011008260A2 (en) | 2009-07-13 | 2011-01-20 | President And Fellows Of Harvard College | Bifunctional stapled polypeptides and uses thereof |
| EP2493879B1 (en) | 2009-10-28 | 2014-05-14 | Joyant Pharmaceuticals, Inc. | Dimeric smac mimetics |
| US8440693B2 (en) | 2009-12-22 | 2013-05-14 | Novartis Ag | Substituted isoquinolinones and quinazolinones |
| SG183257A1 (en) | 2010-02-11 | 2012-09-27 | Celgene Corp | Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same |
| EP2588129A4 (en) | 2010-06-30 | 2014-07-09 | Univ Brandeis | ON SMALL MOLECULES TARGETED PROTEIN REMOVAL |
| JP5852658B2 (ja) | 2010-09-24 | 2016-02-03 | ザ リージェンツ オブ ザ ユニバーシティー オブ ミシガン | デユビキチナーゼ阻害剤およびその使用方法 |
| CN102477017A (zh) * | 2010-11-23 | 2012-05-30 | 苏州波锐生物医药科技有限公司 | 四氢萘衍生物及其在制备预防和/或治疗乳腺癌骨质疏松症药物中的用途 |
| CN102477033A (zh) | 2010-11-23 | 2012-05-30 | 苏州波锐生物医药科技有限公司 | 苯并噻酚类化合物及其在制备预防和/或治疗乳腺癌骨质疏松症药物中的用途 |
| EP2649099A4 (en) | 2010-12-07 | 2016-10-19 | Univ Yale | SMALL MOLECULAR HYDROPHOBIC LABELING OF FUSION PROTEINS AND INDUCED REMOVAL FROM THIS |
| WO2012090104A1 (en) | 2010-12-31 | 2012-07-05 | Kareus Therapeutics, Sa | Methods and compositions for designing novel conjugate therapeutics |
| US8889684B2 (en) | 2011-02-02 | 2014-11-18 | Boehringer Ingelheim International Gmbh | Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors |
| WO2012149299A2 (en) | 2011-04-29 | 2012-11-01 | Celgene Corporaiton | Methods for the treatment of cancer and inflammatory diseases using cereblon as a predictor |
| MX352672B (es) | 2011-09-27 | 2017-12-04 | Amgen Inc | Compuestos heterocíclicos como inhibidores de mdm2 para el tratamiento del cáncer. |
| US20140309265A1 (en) | 2011-11-09 | 2014-10-16 | Ensemble Therapeutics | Macrocyclic compounds for inhibition of inhibitors of apoptosis |
| WO2013071039A1 (en) | 2011-11-09 | 2013-05-16 | Ensemble Therapeutics | Macrocyclic compounds for inhibition of inhibitors of apoptosis |
| CN103159736B (zh) | 2011-12-10 | 2015-05-13 | 通化济达医药有限公司 | 取代的吡唑激酶抑制剂 |
| DK2797888T3 (en) | 2011-12-31 | 2016-09-19 | Beigene Ltd | Fused tricyclic compounds as RAF kinase inhibitors |
| KR102438072B1 (ko) * | 2012-01-12 | 2022-08-31 | 예일 유니버시티 | E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법 |
| WO2013106646A2 (en) | 2012-01-12 | 2013-07-18 | Yale University | Compounds and methods for the inhibition of vcb e3 ubiquitin ligase |
| WO2013169858A1 (en) | 2012-05-08 | 2013-11-14 | The Broad Institute, Inc. | Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy |
| WO2013170147A1 (en) | 2012-05-11 | 2013-11-14 | Yale University | Compounds useful for promoting protein degradation and methods using same |
| EP2855483B1 (en) | 2012-05-24 | 2017-10-25 | Novartis AG | Pyrrolopyrrolidinone compounds |
| CN107540594A (zh) | 2012-05-30 | 2018-01-05 | 霍夫曼-拉罗奇有限公司 | 取代的吡咯烷‑2‑甲酰胺 |
| US9345740B2 (en) | 2012-07-10 | 2016-05-24 | Bristol-Myers Squibb Company | IAP antagonists |
| WO2014020502A2 (en) | 2012-07-31 | 2014-02-06 | Novartis Ag | Markers associated with human double minute 2 inhibitors |
| LT2882737T (lt) | 2012-08-09 | 2019-04-25 | Celgene Corporation | (s)-3-(4-((4-morfolinometil)benzil)oksi)-1-oksoizoindolin-2-il)piperidin-2,6-diono hidrochlorido kieta forma |
| EP2882740B1 (en) | 2012-08-09 | 2017-03-01 | Bristol-Myers Squibb Company | Iap antagonists |
| TWI586668B (zh) | 2012-09-06 | 2017-06-11 | 第一三共股份有限公司 | 二螺吡咯啶衍生物之結晶 |
| US9783573B2 (en) | 2012-09-18 | 2017-10-10 | Bristol-Myers Squibb Company | IAP antagonists |
| US9603889B2 (en) | 2012-10-02 | 2017-03-28 | Bristol-Myers Squibb Company | IAP antagonists |
| TW201428002A (zh) | 2012-11-09 | 2014-07-16 | 必治妥美雅史谷比公司 | 用於抑制細胞凋亡抑制劑之巨環化合物 |
| WO2014100065A1 (en) | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | Substituted imidazopyridines as hdm2 inhibitors |
| WO2014100071A2 (en) | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | Substituted pyrrolopyrimidines as hdm2 inhibitors |
| EP2752191A1 (en) | 2013-01-07 | 2014-07-09 | Sanofi | Compositions and methods using hdm2 antagonist and mek inhibitor |
| GB201311910D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel Compounds |
| NL2011274C2 (en) | 2013-08-06 | 2015-02-09 | Illumicare Ip B V 51 | Groundbreaking platform technology for specific binding to necrotic cells. |
| WO2014134201A1 (en) | 2013-02-28 | 2014-09-04 | Amgen Inc. | A benzoic acid derivative mdm2 inhibitor for the treatment of cancer |
| WO2014151863A1 (en) | 2013-03-14 | 2014-09-25 | Amgen Inc. | Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| WO2015006524A1 (en) | 2013-07-12 | 2015-01-15 | Bristol-Myers Squibb Company | Iap antagonists |
| CN115368356B (zh) | 2013-12-20 | 2025-05-09 | 阿斯特克斯治疗有限公司 | 双环杂环化合物及其治疗用途 |
| SG11201607334YA (en) * | 2014-03-13 | 2016-10-28 | Hoffmann La Roche | Therapeutic combinations with estrogen receptor modulators |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| EP4649963A3 (en) | 2014-04-14 | 2026-05-13 | Arvinas Operations, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| US20160058872A1 (en) * | 2014-04-14 | 2016-03-03 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| TW201613916A (en) | 2014-06-03 | 2016-04-16 | Gilead Sciences Inc | TANK-binding kinase inhibitor compounds |
| US20160022642A1 (en) | 2014-07-25 | 2016-01-28 | Yale University | Compounds Useful for Promoting Protein Degradation and Methods Using Same |
| US10071164B2 (en) | 2014-08-11 | 2018-09-11 | Yale University | Estrogen-related receptor alpha based protac compounds and associated methods of use |
| KR102557670B1 (ko) * | 2014-10-03 | 2023-07-20 | 코나겐 인크. | 비칼로리 감미료 및 합성 방법 |
| WO2016097071A1 (en) * | 2014-12-18 | 2016-06-23 | F. Hoffmann-La Roche Ag | Estrogen receptor modulators and uses thereof |
| JP6815318B2 (ja) | 2014-12-23 | 2021-01-20 | ダナ−ファーバー キャンサー インスティテュート，インコーポレイテッド | 二官能性分子によって標的化タンパク質分解を誘導する方法 |
| US9694084B2 (en) | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| JP6817962B2 (ja) | 2015-01-20 | 2021-01-20 | アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． | ターゲティングされたアンドロゲン受容体分解のための化合物および方法 |
| IL315294A (en) | 2015-03-03 | 2024-10-01 | Pharmacyclics Llc | Pharmaceutical formulations of proton tyrosine kinase inhibitor |
| GB201504314D0 (en) | 2015-03-13 | 2015-04-29 | Univ Dundee | Small molecules |
| AU2016232705C1 (en) | 2015-03-18 | 2021-06-17 | Arvinas, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
| GB201506871D0 (en) | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201506872D0 (en) | 2015-04-22 | 2015-06-03 | Ge Oil & Gas Uk Ltd | Novel compounds |
| WO2016197114A1 (en) | 2015-06-05 | 2016-12-08 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| EP3319944A4 (en) | 2015-07-10 | 2019-04-24 | Arvinas, Inc. | MDM2-BASED MODULATORS OF PROTEOLYSIS AND RELATED USE METHODS |
| CA2988436A1 (en) | 2015-07-13 | 2017-01-19 | Arvinas, Inc. | Alanine-based modulators of proteolysis and associated methods of use |
| CA2994969A1 (en) | 2015-08-06 | 2017-02-09 | Dana-Farber Cancer Institute, Inc. | Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses |
| EP3337476A4 (en) | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| GB201516243D0 (en) | 2015-09-14 | 2015-10-28 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| BR112018008918A8 (pt) | 2015-11-02 | 2019-02-26 | Univ Yale | compostos de quimera proteólise dirigida e métodos para preparação e uso dos mesmos |
| WO2017160990A1 (en) | 2016-03-15 | 2017-09-21 | Merrimack Pharmaceuticals, Inc. | Methods for treating er+, her2-, hrg+ breast cancer using combination therapies comprising an anti-erbb3 antibody |
| CN109153644B (zh) | 2016-03-16 | 2022-10-21 | H·李·莫菲特癌症中心研究有限公司 | 用以增强效应t细胞功能的针对cereblon的小分子 |
| US20170281784A1 (en) | 2016-04-05 | 2017-10-05 | Arvinas, Inc. | Protein-protein interaction inducing technology |
| AU2017246452C1 (en) * | 2016-04-06 | 2021-06-03 | The Regents Of The University Of Michigan | MDM2 protein degraders |
| WO2017185036A1 (en) | 2016-04-22 | 2017-10-26 | Dana Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of egfr and methods of use |
| CN121974842A (zh) | 2016-05-10 | 2026-05-05 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| SG11201809501PA (en) | 2016-06-06 | 2018-12-28 | Celgene Corp | Treatment of a hematologic malignancy with 2-(4-chlorophenyl)-n-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| EP3512842B1 (en) | 2016-09-15 | 2024-01-17 | Arvinas, Inc. | Indole derivatives as estrogen receptor degraders |
| SI3526202T1 (sl) | 2016-10-11 | 2025-04-30 | Arvinas Operations, Inc. | Spojine in postopki za ciljno razgradnjo androgenskih receptorjev |
| MX2019005007A (es) | 2016-11-01 | 2019-07-18 | Arvinas Inc | Protac dirigidos a la proteína tau y métodos asociados de uso. |
| AU2017363257B2 (en) | 2016-11-22 | 2021-08-19 | Dana-Farber Cancer Institute, Inc. | Degradation of protein kinases by conjugation of protein kinase inhibitors with E3 ligase ligand and methods of use |
| IL266842B (en) * | 2016-12-01 | 2022-09-01 | Arvinas Operations Inc | History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists |
| CN110753693A (zh) | 2016-12-23 | 2020-02-04 | 阿尔维纳斯运营股份有限公司 | Egfr蛋白水解靶向嵌合分子和相关使用方法 |
| IL325835A (en) | 2016-12-23 | 2026-03-01 | Univ Yale | Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides |
| US10806737B2 (en) | 2016-12-23 | 2020-10-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| US11191741B2 (en) | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| IL300417A (en) | 2017-01-26 | 2023-04-01 | Arvinas Operations Inc | Bifunctional benzothiophene compounds, preparations containing them and their use in therapy |
| IL319363A (en) | 2017-01-31 | 2025-05-01 | Arvinas Operations Inc | Cervalon ligands and bifunctional compounds containing them |
| MX2020003190A (es) | 2017-09-22 | 2020-11-11 | Kymera Therapeutics Inc | Degradadores de proteinas y usos de los mismos. |
| MX2021006411A (es) | 2018-12-06 | 2021-07-21 | Radius Pharmaceuticals Inc | Metodos para el tratamiento del cancer resistente a inhibidores de cinasa 4 y cinasa 6 dependiente de ciclina (cdk4/6). |
| WO2021041348A1 (en) | 2019-08-26 | 2021-03-04 | Arvinas Operations, Inc. | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
| EP3795570B1 (en) | 2019-09-23 | 2022-02-23 | Accutar Biotechnology Inc. | Substituted quinoline-8-carbonitrile derivatives having androgen receptor degradation activity and uses thereof |
| CN115003295B (zh) | 2019-12-12 | 2025-05-06 | 冰洲石生物科技公司 | 具有雌激素受体降解活性的新型色满衍生物及其用途 |
| AU2021342287A1 (en) | 2020-09-14 | 2023-04-13 | Arvinas Operations, Inc. | Crystalline forms of a compound for the targeted degradation of estrogen receptor |
| IL303143A (en) | 2020-12-14 | 2023-07-01 | Arvinas Operations Inc | Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders |
| KR20240040769A (ko) | 2021-07-26 | 2024-03-28 | 아비나스 오퍼레이션스, 인코포레이티드 | 이작용성 화합물을 제조하는 방법 |
| CN113816927B (zh) | 2021-11-23 | 2022-02-25 | 苏州国匡医药科技有限公司 | 一种arv-471中间体的制备方法 |
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