RU2021116560A - TETRAHYDRONAPHTHALINE AND TETRAHYDROISOQUINOLINE DERIVATIVES AS ESTROGEN RECEPTOR DESTROYERS - Google Patents
TETRAHYDRONAPHTHALINE AND TETRAHYDROISOQUINOLINE DERIVATIVES AS ESTROGEN RECEPTOR DESTROYERS Download PDFInfo
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- RU2021116560A RU2021116560A RU2021116560A RU2021116560A RU2021116560A RU 2021116560 A RU2021116560 A RU 2021116560A RU 2021116560 A RU2021116560 A RU 2021116560A RU 2021116560 A RU2021116560 A RU 2021116560A RU 2021116560 A RU2021116560 A RU 2021116560A
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- CXWXQJXEFPUFDZ-UHFFFAOYSA-N Tetralin Chemical compound C1=CC=C2CCCCC2=C1 CXWXQJXEFPUFDZ-UHFFFAOYSA-N 0.000 title 1
- 102000015694 estrogen receptors Human genes 0.000 title 1
- 108010038795 estrogen receptors Proteins 0.000 title 1
- 150000003526 tetrahydroisoquinolines Chemical class 0.000 title 1
- 239000003112 inhibitor Substances 0.000 claims 12
- 230000002401 inhibitory effect Effects 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 10
- RCINICONZNJXQF-MZXODVADSA-N Intaxel 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 4
- 229960001592 Paclitaxel Drugs 0.000 claims 4
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 239000002246 antineoplastic agent Substances 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000011780 sodium chloride Substances 0.000 claims 3
- 229940028652 Abraxane 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
- 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 2
- 229960004117 Capecitabine Drugs 0.000 claims 2
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N Docetaxel 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 2
- HKVAMNSJSFKALM-XJFKSLPYSA-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-XJFKSLPYSA-N 0.000 claims 2
- 102000030951 Phosphotransferases Human genes 0.000 claims 2
- 108091000081 Phosphotransferases Proteins 0.000 claims 2
- 230000001093 anti-cancer Effects 0.000 claims 2
- 108090001123 antibodies Proteins 0.000 claims 2
- 102000004965 antibodies Human genes 0.000 claims 2
- 229960003668 docetaxel Drugs 0.000 claims 2
- 229960005167 everolimus Drugs 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 229930003347 taxol Natural products 0.000 claims 2
- -1 zolendronate Chemical compound 0.000 claims 2
- ZROHGHOFXNOHSO-BNTLRKBRSA-L (1R,2R)-cyclohexane-1,2-diamine;oxalate;platinum(2+) Chemical compound [H][N]([C@@H]1CCCC[C@H]1[N]1([H])[H])([H])[Pt]11OC(=O)C(=O)O1 ZROHGHOFXNOHSO-BNTLRKBRSA-L 0.000 claims 1
- CUWODFFVMXJOKD-UVLQAERKSA-N (2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-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-hy 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 1
- VWUXBMIQPBEWFH-WCCTWKNTSA-N (7R,8R,9S,13S,14S,17S)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol 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 1
- AOJJSUZBOXZQNB-TZSSRYMLSA-N ADRIAMYCIN 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 1
- 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 1
- 229950002421 Acolbifene Drugs 0.000 claims 1
- YBBLVLTVTVSKRW-UHFFFAOYSA-N Anastrozole Chemical compound N#CC(C)(C)C1=CC(C(C)(C#N)C)=CC(CN2N=CN=C2)=C1 YBBLVLTVTVSKRW-UHFFFAOYSA-N 0.000 claims 1
- 108010005144 Bevacizumab Proteins 0.000 claims 1
- 108010037003 Buserelin Proteins 0.000 claims 1
- 229960004562 Carboplatin Drugs 0.000 claims 1
- OLESAACUTLOWQZ-UHFFFAOYSA-L Carboplatin Chemical compound O=C1O[Pt]([N]([H])([H])[H])([N]([H])([H])[H])OC(=O)C11CCC1 OLESAACUTLOWQZ-UHFFFAOYSA-L 0.000 claims 1
- 229960004679 Doxorubicin Drugs 0.000 claims 1
- 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 1
- 229960001433 Erlotinib Drugs 0.000 claims 1
- 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 1
- 229960005420 Etoposide Drugs 0.000 claims 1
- 102100004573 FLT3 Human genes 0.000 claims 1
- 101710009074 FLT3 Proteins 0.000 claims 1
- 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 1
- 229960002258 Fulvestrant Drugs 0.000 claims 1
- 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 1
- 229960003690 Goserelin Acetate Drugs 0.000 claims 1
- 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 1
- 229950002248 Idoxifene Drugs 0.000 claims 1
- 108010089187 Ipilimumab Proteins 0.000 claims 1
- 102100013180 KDR Human genes 0.000 claims 1
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims 1
- 239000003798 L01XE11 - Pazopanib Substances 0.000 claims 1
- 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 1
- HPJKCIUCZWXJDR-UHFFFAOYSA-N Letrozole Chemical compound C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 claims 1
- 102000008135 Mechanistic Target of Rapamycin Complex 1 Human genes 0.000 claims 1
- 108010035196 Mechanistic Target of Rapamycin Complex 1 Proteins 0.000 claims 1
- 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 1
- SUDAHWBOROXANE-VIFPVBQESA-N PD 0325901-Cl Chemical compound OC[C@H](O)CONC(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F SUDAHWBOROXANE-VIFPVBQESA-N 0.000 claims 1
- 101700025987 PIK-1 Proteins 0.000 claims 1
- WRUUGTRCQOWXEG-UHFFFAOYSA-N Pamidronic acid Chemical compound NCCC(O)(P(O)(O)=O)P(O)(O)=O WRUUGTRCQOWXEG-UHFFFAOYSA-N 0.000 claims 1
- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 claims 1
- 229960004622 Raloxifene Drugs 0.000 claims 1
- 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 1
- 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 1
- 229960001603 Tamoxifen Drugs 0.000 claims 1
- BPEGJWRSRHCHSN-UHFFFAOYSA-N Temodal Chemical compound O=C1N(C)N=NC2=C(C(N)=O)N=CN21 BPEGJWRSRHCHSN-UHFFFAOYSA-N 0.000 claims 1
- 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 1
- XFCLJVABOIYOMF-QPLCGJKRSA-N Toremifene Chemical compound C1=CC(OCCN(C)C)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 XFCLJVABOIYOMF-QPLCGJKRSA-N 0.000 claims 1
- 108010010691 Trastuzumab Proteins 0.000 claims 1
- 229960004824 Triptorelin Drugs 0.000 claims 1
- 108091007928 VEGF receptors Proteins 0.000 claims 1
- 229960004528 Vincristine Drugs 0.000 claims 1
- WAEXFXRVDQXREF-UHFFFAOYSA-N Vorinostat Chemical compound ONC(=O)CCCCCCC(=O)NC1=CC=CC=C1 WAEXFXRVDQXREF-UHFFFAOYSA-N 0.000 claims 1
- 229960000237 Vorinostat Drugs 0.000 claims 1
- IKDXDQDKCZPQSZ-JHYYTBFNSA-N acetic acid;(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[(2S)-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-oxopro Chemical compound CC(O)=O.C([C@@H](C(=O)N[C@H](COC(C)(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)NNC(N)=O)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)C1=CC=C(O)C=C1 IKDXDQDKCZPQSZ-JHYYTBFNSA-N 0.000 claims 1
- 229960002932 anastrozole Drugs 0.000 claims 1
- 239000003719 aurora kinase inhibitor Substances 0.000 claims 1
- 229960000397 bevacizumab Drugs 0.000 claims 1
- LKJPYSCBVHEWIU-KRWDZBQOSA-N 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 1
- 229960000997 bicalutamide Drugs 0.000 claims 1
- 229960002719 buserelin Drugs 0.000 claims 1
- 229960004316 cisplatin Drugs 0.000 claims 1
- 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 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 102000017256 epidermal growth factor-activated receptor activity proteins Human genes 0.000 claims 1
- 108040009258 epidermal growth factor-activated receptor activity proteins Proteins 0.000 claims 1
- 229960002074 flutamide Drugs 0.000 claims 1
- 229960005277 gemcitabine Drugs 0.000 claims 1
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims 1
- 229960005386 ipilimumab Drugs 0.000 claims 1
- 229960002367 lasofoxifene Drugs 0.000 claims 1
- 229960003881 letrozole Drugs 0.000 claims 1
- 230000000051 modifying Effects 0.000 claims 1
- 229960002653 nilutamide Drugs 0.000 claims 1
- 229960001756 oxaliplatin Drugs 0.000 claims 1
- 229940046231 pamidronate Drugs 0.000 claims 1
- 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 1
- 229960000639 pazopanib Drugs 0.000 claims 1
- WBXPDJSOTKVWSJ-ZDUSSCGKSA-N pemetrexed Chemical compound C=1NC=2NC(N)=NC(=O)C=2C=1CCC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 WBXPDJSOTKVWSJ-ZDUSSCGKSA-N 0.000 claims 1
- 229960005079 pemetrexed Drugs 0.000 claims 1
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 239000003197 protein kinase b inhibitor Substances 0.000 claims 1
- 229960004964 temozolomide Drugs 0.000 claims 1
- 229960000303 topotecan Drugs 0.000 claims 1
- 229960005026 toremifene Drugs 0.000 claims 1
- LXZZYRPGZAFOLE-UHFFFAOYSA-L transplatin Chemical compound [H][N]([H])([H])[Pt](Cl)(Cl)[N]([H])([H])[H] LXZZYRPGZAFOLE-UHFFFAOYSA-L 0.000 claims 1
- 229960000575 trastuzumab Drugs 0.000 claims 1
- 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 1
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims 1
Claims (21)
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2020106142A Division RU2750484C2 (en) | 2016-12-01 | 2017-12-01 | Derivatives of tetrahydronaphtalene and tetrahydroisoquinoline as deconstructors of estrogen receptor |
Publications (1)
Publication Number | Publication Date |
---|---|
RU2021116560A true RU2021116560A (en) | 2022-12-08 |
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