HRP20231537T1 - Derivati tetrahidronaftalena i tetrahidroizokinolina kao degradatori estrogenskih receptora - Google Patents
Derivati tetrahidronaftalena i tetrahidroizokinolina kao degradatori estrogenskih receptora Download PDFInfo
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- HRP20231537T1 HRP20231537T1 HRP20231537TT HRP20231537T HRP20231537T1 HR P20231537 T1 HRP20231537 T1 HR P20231537T1 HR P20231537T T HRP20231537T T HR P20231537TT HR P20231537 T HRP20231537 T HR P20231537T HR P20231537 T1 HRP20231537 T1 HR P20231537T1
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- 229940125641 estrogen receptor degrader Drugs 0.000 title 1
- 125000003039 tetrahydroisoquinolinyl group Chemical class C1(NCCC2=CC=CC=C12)* 0.000 title 1
- CXWXQJXEFPUFDZ-UHFFFAOYSA-N tetralin Chemical compound C1=CC=C2CCCCC2=C1 CXWXQJXEFPUFDZ-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 21
- 239000003112 inhibitor Substances 0.000 claims 13
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- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 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 6
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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Claims (28)
1. Spoj koji ima strukturu:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
ili
[image]
ili farmaceutski prihvatljiva sol, enantiomer, stereoizomer ili izotopni derivat bilo kojeg od prethodno navedenih.
2. Spoj prema zahtjevu 1 naznačen time što ima strukturu:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
ili
[image]
3. Spoj prema zahtjevu 1 naznačen time što ima strukturu:
[image]
ili njegova farmaceutski prihvatljiva sol, enantiomer, stereoizomer ili izotopni derivat.
4. Spoj prema zahtjevu 1 ili 2 naznačen time što ima strukturu:
[image]
5. Spoj prema zahtjevu 1 naznačen time što ima strukturu:
[image]
ili njegova farmaceutski prihvatljiva sol, enantiomer, stereoizomer ili izotopni derivat.
6. Spoj prema zahtjevu 1 ili 2 naznačen time što ima strukturu:
[image]
7. Spoj prema zahtjevu 1 naznačen time što ima strukturu:
[image]
ili njegova farmaceutski prihvatljiva sol, enantiomer, stereoizomer ili izotopni derivat.
8. Spoj prema zahtjevu 1 ili 2 naznačen time što ima strukturu:
[image]
9. Spoj prema zahtjevu 1 naznačen time što ima strukturu:
[image]
ili njegova farmaceutski prihvatljiva sol, enantiomer, stereoizomer ili izotopni derivat.
10. Spoj prema zahtjevu 1 ili 2 naznačen time što ima strukturu:
[image]
11. Spoj prema zahtjevu 1 naznačen time što ima strukturu:
[image]
ili njegova farmaceutski prihvatljiva sol, enantiomer, stereoizomer ili izotopni derivat.
12. Spoj prema zahtjevu 1 ili 2 naznačen time što ima strukturu:
[image]
13. Farmaceutski pripravak, naznačen time što sadrži spoj prema bilo kojem od zahtjeva 1-12, i farmaceutski prihvatljiv nosač.
14. Farmaceutski pripravak prema zahtjevu 13, naznačen time što nadalje sadrži učinkovitu količinu dodatnog sredstva protiv raka.
15. Farmaceutski pripravak prema zahtjevu 14, naznačen time što je dodatno sredstvo protiv raka inhibitor FLT-3, inhibitor VEGFR, inhibitor EGFR TK, inhibitor aurora kinaze, modulator PIK-1, inhibitor Bcl-2, inhibitor HDAC, inhibitor c-MET, inhibitor PARP, inhibitor Cdk, anti-HGF protutijelo, inhibitor PI3 kinaze, inhibitor AKT, inhibitor mTORC1/2, inhibitor JAK/STAT, inhibitor kontrolne točke 1, inhibitor kontrolne točke 2, inhibitor kinaze žarišne adhezije, inhibitor kinaze MAP kinaze, ili protutijelo VEGF trap.
16. Farmaceutski pripravak prema zahtjevu 14, naznačen time što je dodatno sredstvo protiv raka docetaksel, goserelin acetat, triptorelin pamoat, buserelin, flutamid, bikalutamid, nilutamid, pamidronat, zolendronat, everolimus, pazopanib, karboplatin, cisplatin, oksaliplatin, epitilon B, fulvestrant, akolbifen, lasofoksifen, idoksifen, topotekan, pemetreksed, erlotinib, ticilimumab, ipilimumab, vorinostat, etopozid, gemcitabin, doksorubicin, 5'-deoksi-5-fluorouridin, vinkristin, temozolomid, kapecitabin, kamptotecin, PD0325901, tamoksifen, toremifen citrat, anastrazol, letrozol, bevacizumab, raloksifen, paklitaksel, abraksan ili trastuzumab.
17. Farmaceutski pripravak prema zahtjevu 14, naznačen time što
(a) dodatno sredstvo protiv raka je docetaksel, goserelin acetat, triptorelin pamoat, buserelin, flutamid, bikalutamid, nilutamid, pamidronat ili zolendronat; ili
(b) dodatno sredstvo protiv raka je everolimus, kapecitabin, docetaksel, paklitaksel ili abraksan.
18. Spoj prema bilo kojem od zahtjeva 1-12 ili farmaceutski pripravak prema zahtjevu 13 za upotrebu u liječenju raka kod subjekta.
19. Spoj ili farmaceutski pripravak za upotrebu prema zahtjevu 18, naznačen time što je rak, rak dojke.
20. Spoj prema bilo kojem od zahtjeva 1-12 ili farmaceutski pripravak prema zahtjevu 13 za upotrebu u liječenju bolesti kod subjekta, pri čemu je bolest odabrana između raka dojke, raka maternice, raka jajnika, raka prostate, raka endometrija i endometrioze.
21. Spoj ili farmaceutski pripravak za upotrebu prema bilo kojem od zahtjeva 18-20, naznačen time što liječenje nadalje uključuje upotrebu učinkovite količine dodatnog sredstva protiv raka.
22. Spoj ili farmaceutski pripravak za upotrebu prema zahtjevu 21, naznačen time što je dodatno sredstvo protiv raka inhibitor FLT-3, inhibitor VEGFR, inhibitor EGFR TK, inhibitor aurora kinaze, modulator PIK-1, inhibitor Bcl-2, inhibitor HDAC, inhibitor c-MET, inhibitor PARP, inhibitor Cdk, anti-HGF protutijelo, inhibitor PI3 kinaze, inhibitor AKT, inhibitor mTORC1/2, inhibitor JAK/STAT, inhibitor kontrolne točke 1, inhibitor kontrolne točke 2, inhibitor kinaze žarišne adhezije, inhibitor kinaze MAP kinaze, ili protutijelo VEGF trap.
23. Spoj ili farmaceutski pripravak za upotrebu prema zahtjevu 21, naznačen time što je dodatno sredstvo protiv raka docetaksel, goserelin acetat, triptorelin pamoat, buserelin, flutamid, bikalutamid, nilutamid, pamidronat, zolendronat, everolimus, pazopanib, karboplatin, cisplatin, oksaliplatin, epitilon B, fulvestrant, akolbifen, lasofoksifen, idoksifen, topotekan, pemetreksed, erlotinib, ticilimumab, ipilimumab, vorinostat, etopozid, gemcitabin, doksorubicin, 5'-deoksi-5-fluorouridin, vinkristin, temozolomid, kapecitabin, kamptotecin, PD0325901, tamoksifen, toremifen citrat, anastrazol, letrozol, bevacizumab, raloksifen, paklitaksel, abraksan ili trastuzumab.
24. Spoj ili farmaceutski pripravak za upotrebu prema zahtjevu 21, naznačen time što
(a) dodatno sredstvo protiv raka je docetaksel, goserelin acetat, triptorelin pamoat, buserelin, flutamid, bikalutamid, nilutamid, pamidronat ili zolendronat; ili
(b) dodatno sredstvo protiv raka je everolimus, kapecitabin, docetaksel, paklitaksel ili abraksan.
25. Farmaceutski pripravak prema bilo kojem od zahtjeva 14-17 za upotrebu u liječenju raka kod subjekta.
26. Farmaceutski pripravak za upotrebu prema zahtjevu 25, naznačen što je rak, rak dojke.
27. Farmaceutski pripravak prema bilo kojem od zahtjeva 14-17 za upotrebu u liječenju bolesti kod subjekta, pri čemu je bolest odabrana između raka dojke, raka maternice, raka jajnika, raka prostate, raka endometrija i endometrioze.
28. Spoj ili farmaceutski pripravak za upotrebu prema bilo kojem od zahtjeva 18-27, naznačen time što je subjekt čovjek.
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US201662429041P | 2016-12-01 | 2016-12-01 | |
US201762540049P | 2017-08-01 | 2017-08-01 | |
EP20150584.9A EP3689868B1 (en) | 2016-12-01 | 2017-12-01 | Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders |
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