HRP20120952T1 - 8-beta-supstituirani 16alfa-fluoro-estratrieni kao selektivno aktivni estrogeni - Google Patents
8-beta-supstituirani 16alfa-fluoro-estratrieni kao selektivno aktivni estrogeni Download PDFInfo
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- HRP20120952T1 HRP20120952T1 HRP20120952AT HRP20120952T HRP20120952T1 HR P20120952 T1 HRP20120952 T1 HR P20120952T1 HR P20120952A T HRP20120952A T HR P20120952AT HR P20120952 T HRP20120952 T HR P20120952T HR P20120952 T1 HRP20120952 T1 HR P20120952T1
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- 229940011871 estrogen Drugs 0.000 title 1
- 239000000262 estrogen Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 26
- 238000011282 treatment Methods 0.000 claims 15
- -1 unsaturated C1-C6-alkyl radical Chemical class 0.000 claims 15
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 8
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 238000011321 prophylaxis Methods 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 4
- 239000000333 selective estrogen receptor modulator Substances 0.000 claims 4
- 229940095743 selective estrogen receptor modulator Drugs 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 206010027304 Menopausal symptoms Diseases 0.000 claims 2
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Chemical group C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 206010020718 hyperplasia Diseases 0.000 claims 2
- 208000000509 infertility Diseases 0.000 claims 2
- 230000036512 infertility Effects 0.000 claims 2
- 231100000535 infertility Toxicity 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000006340 pentafluoro ethyl group Chemical group FC(F)(F)C(F)(F)* 0.000 claims 2
- 210000002307 prostate Anatomy 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 2
- 229920002554 vinyl polymer Polymers 0.000 claims 2
- CPEONABTMRSIKA-UHFFFAOYSA-N 1,4$l^{2}-oxazinane Chemical compound C1COCC[N]1 CPEONABTMRSIKA-UHFFFAOYSA-N 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 201000003741 Gastrointestinal carcinoma Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010030247 Oestrogen deficiency Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 229940046836 anti-estrogen Drugs 0.000 claims 1
- 230000001833 anti-estrogenic effect Effects 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 125000004181 carboxyalkyl group Chemical group 0.000 claims 1
- SYGWYBOJXOGMRU-UHFFFAOYSA-N chembl233051 Chemical group C1=CC=C2C3=CC(C(N(CCN(C)C)C4=O)=O)=C5C4=CC=CC5=C3SC2=C1 SYGWYBOJXOGMRU-UHFFFAOYSA-N 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([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
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 230000007812 deficiency Effects 0.000 claims 1
- 150000002164 estratrienes Chemical class 0.000 claims 1
- 239000000328 estrogen antagonist Substances 0.000 claims 1
- 230000003779 hair growth Effects 0.000 claims 1
- 229940088597 hormone Drugs 0.000 claims 1
- 239000005556 hormone Substances 0.000 claims 1
- 238000002657 hormone replacement therapy Methods 0.000 claims 1
- 208000015210 hypertensive heart disease Diseases 0.000 claims 1
- 210000000987 immune system Anatomy 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 201000002313 intestinal cancer Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 208000015124 ovarian disease Diseases 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 230000002265 prevention Effects 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
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 230000000638 stimulation Effects 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
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- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
- C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
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- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0062—Estrane derivatives substituted in position 17 alfa not substituted in position 17 beta
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Claims (28)
1. Derivati 8β-supstituiranog estra-1,3,5(10)-triena opće formule I
[image]
naznačeni time da radikali R3, R8, R13, R16 kao i R17 i R17', nezavisno jedan od drugoga, imaju slijedeća značenja:
R3 predstavlja atom vodika ili skupinu R18, gdje
R18 predstavlja ravni lanac ili razgranati lanac, zasićeni ili nezasićeni radikal C1-C6- alkila, trifluorometil skupinu,
radikal arila, heteroarila ili aralkila, proizvoljno supstituiran sa barem jednim radikalom nezavisno odabranim od metila, etila, trifluorometila, pentafluoroetila, trifluorometiltio, metoksi, etoksi, nitro, cijano, halo, hidroksi, amino, mono(C1-C8-alkil) ili di(C1-C8-alkil)amino pri čemu obje alkil skupine su iste ili različite, di(aralkil)amino pri čemu obje aralkil skupine su iste ili različite, karboksila, karboksialkoksi, C1-C20-acila ili C1-C20-aciloksi kao supstituenata;
radikal acila -C(=O)R19, gdje R19 je ravni lanac ili razgranati lanac C1-C10 -alkil atoma radikala koji je zasićen ili nezasićen na do tri pozicije, te je djelomično ili u potpunosti halogeniran, ili
R18 predstavlja skupinu R20SO2, gdje
R20 je R21R22 N skupina, pri čemu R21 i R22, nezavisno jedan od drugoga, predstavljaju atom vodika, radikal C1-C5-alkila, skupinu -C(=O)R23, gdje R23predstavlja nesupstituirani ili supstituirani, ravni lanac ili razgranati lanac radikal C1-C10 -alkila koji je zasićen ili nezasićen na do tri pozicije, te je djelomično ili u potpunosti halogeniran, ciklopropil, ciklobutil, ciklopentil, cikloheksil ili cikloheptil skupina, radikal C4-C15-cikloalkilalkila sa 3 do 7 atoma ugljika u cikloalkilnom dijelu i sa alkilnim dijelom sa do 8 atoma ugljika ili radikal arila, heteroarila ili aralkila proizvoljno supstituiran, sa barem jednim radikalom nezavisno odabranim od metila, etila, trifluorometila, pentafluoroetila, trifluorometiltio, metoksi, etoksi, nitro, cijano, halo-, hidroksi, amino, mono(C1-C8-alkil) ili di(C1-C8-alkil) amino pri čemu obje alkil skupine su iste ili različite, di(aralkil)amino amino pri čemu obje aralkil skupine su iste ili različite, karboksila, karboksialkoksi, C1 -C20-acila ili C1 -C20-aciloksi skupina kao supstituenata; ili,
zajedno sa N atomom, polimetilenimino radikal sa 4 do 6 C atoma ili morfolino radikal,
R8 je ravni lanac ili razgranati lanac radikala alkenila ili alkinila sa 2 do 6 atoma ugljika, koji proizvoljno može biti djelomično ili u potpunosti fluoriran,
R13 je metilna skupina ili etilna skupina,
R16 je atom fluora na α-položaju,
R17 i R17', su u svakom slučaju nezavisno jedan od drugoga, atom vodika i hidroksi skupina; ili
atom vodika i skupina R18O-, R20SO2- ili OC(=O)R23 sa R18, R20 i R23 u svakom slučaju sa značenjem koje je navedeno u R3 pri čemu izraz "aril" je radikal fenila 1- ili 2-naftila i pri čemu radikal "aralkila" je radikal koji sadrži do 14 atoma ugljika u prstenu i 1 do 8 atoma ugljika u alkilnom lancu.
2. Spojevi opće formule I prema zahtjevu 1, naznačeni time da R3 je atom vodika.
3. Spojevi opće formule I prema zahtjevu 1 ili 2, naznačeni time da R8 je vinil, etinil ili prop-1-inil skupina.
4. Spojevi opće formule I prema bilo kojem od zahtjeva 1 do 3 naznačeni time da R17 i R17' su atom vodika i atom hidroksi skupine.
5. Spojevi opće formule I prema bilo kojem od zahtjeva 1 do 4 naznačeni time da R8 je vinil, etinil ili prop-1-inil skupina, R16 je atom fluora, R17 i R17' atom vodika i atom hidroksi skupine.
6. Spojevi opće formule I prema bilo kojem od zahtjeva 1 do 5, naznačeni time da su R17 i R17' atom vodika i skupina R18-O- ili R19SO2-O- sa R18 i R19 u svakom slučaju sa značenjem koje je navedeno za R3.
7. Estratrieni opće formule I prema zahtjevu 1 ili 2, naznačeni time da su:
8β-vinil-16α-fluoro-estra-1,3,5(10)-trien-3,17α-diol
8β-vinil-16α-fluoro-estra-1,3,5(10)-trien-3,17β-diol
8. Farmaceutski pripravci naznačeni time da sadrže barem spoj prema jednom od zahtjeva 1 do 7 kao i farmaceutski kompatibilan nosač.
9. Spojevi opće formule I kako je definirano u bilo kojem od zahtjeva 1 do 7 naznačeni time da su za uporabu kao lijek.
10. Uporaba spojeva opće formule I kako je definirano u bilo kojem od zahtjeva 1 do 7 naznačena time da je za proizvodnju farmaceutskog sredstva.
11. Spoj prema zahtjevu 9 naznačen time da je za liječenje bolesti i stanja induciranih nedostatkom estrogena kod žena i kod muškaraca.
12. Spoj prema zahtjevu 9 naznačen time da je za liječenje simptoma peri- i post-menopauze.
13. Spoj prema zahtjevu 9 naznačen time da je za in-vitro liječenje neplodnosti kod žena.
14. Spoj prema zahtjevu 9 naznačen time da je za in-vivo liječenje neplodnosti kod žena.
15. Spoj prema zahtjevu 9 naznačen time da je za liječenje simptoma induciranih nedostatkom hormona kod poremećaja jajnika koji je uzrokovan operacijom, lijekom, itd.
16. Spoj prema zahtjevu 9 naznačen time da je za hormonsko nadomjesno liječenje (HRT).
17. Spoj prema zahtjevu 11 naznačen time da je u kombinaciji sa selektivnim modulatorima estrogenskih receptora (SERM), na primjer raloksifenom.
18. Spoj prema zahtjevu 9 naznačen time da je za profilaksu i liječenje reumatoidnog artritisa, multiple skleroze, te lupusa.
19. Spoj prema zahtjevu 9 naznačen time da je za profilaksu i liječenje upalnih crijevnih bolesti i naročito Crohn-ove bolesti
20. Spoj prema zahtjevu 9 naznačen time da je za profilaksu i liječenje upalnih bolesti kože i naročito psorijaze.
21. Spoj prema zahtjevu 9 naznačen time da je za profilaksu i liječenje kardiovaskularnih bolesti.
22. Spoj prema zahtjevu 9 naznačen time da je za profilaksu i liječenje arterioskleroze, povišenog krvnog pritiska i hipertenzivne bolesti srca.
23. Spoj prema zahtjevu 9 naznačen time da je za sprečavanje i liječenje hiperplazije prostate.
24. Spoj prema zahtjevu 9 naznačen time da je u kombinaciji sa antiestrogenima i/ili selektivnim modulatorima estrogenskih receptora (SERM) za profilaksu i liječenje hiperplazije prostate.
25. Spoj prema zahtjevu 9 naznačen time da je za liječenje bolesti imunološkog sustava.
26. Spoj prema zahtjevu 9 naznačen time da je za liječenje endometrioze.
27. Spoj prema zahtjevu 9 naznačen time da je za liječenje raka debelog crijeva i raka tankog crijeva.
28. Uporaba spojeva prema zahtjevu 10 naznačena time da je za ne-terapeutsku stimulaciju rasta kose.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07075600A EP2014672A1 (en) | 2007-07-12 | 2007-07-12 | 8-beta-substituted estratrienes as selectively active estrogens |
| PCT/EP2008/059115 WO2009007454A2 (en) | 2007-07-12 | 2008-07-11 | 8-beta-substituted estratrienes as selectively active estrogens |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20120952T1 true HRP20120952T1 (hr) | 2012-12-31 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20120952AT HRP20120952T1 (hr) | 2007-07-12 | 2012-11-21 | 8-beta-supstituirani 16alfa-fluoro-estratrieni kao selektivno aktivni estrogeni |
Country Status (34)
| Country | Link |
|---|---|
| US (1) | US20090029957A1 (hr) |
| EP (2) | EP2014672A1 (hr) |
| JP (1) | JP2010533152A (hr) |
| KR (1) | KR20100037593A (hr) |
| CN (1) | CN101687902B (hr) |
| AR (1) | AR067507A1 (hr) |
| AU (1) | AU2008274198A1 (hr) |
| BR (1) | BRPI0814207A2 (hr) |
| CA (1) | CA2692727A1 (hr) |
| CL (1) | CL2008002027A1 (hr) |
| CO (1) | CO6270230A2 (hr) |
| CR (1) | CR11211A (hr) |
| CU (1) | CU23885B1 (hr) |
| CY (1) | CY1113351T1 (hr) |
| DK (1) | DK2176282T3 (hr) |
| DO (1) | DOP2010000017A (hr) |
| EA (1) | EA017124B1 (hr) |
| EC (1) | ECSP109872A (hr) |
| ES (1) | ES2393942T3 (hr) |
| HN (1) | HN2010000081A (hr) |
| HR (1) | HRP20120952T1 (hr) |
| MA (1) | MA31565B1 (hr) |
| NZ (1) | NZ582490A (hr) |
| PA (1) | PA8789401A1 (hr) |
| PE (1) | PE20090825A1 (hr) |
| PL (1) | PL2176282T3 (hr) |
| PT (1) | PT2176282E (hr) |
| RS (1) | RS52541B (hr) |
| SI (1) | SI2176282T1 (hr) |
| TN (1) | TN2010000007A1 (hr) |
| TW (1) | TW200911824A (hr) |
| UA (1) | UA99918C2 (hr) |
| UY (1) | UY31220A1 (hr) |
| WO (1) | WO2009007454A2 (hr) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2012234682A1 (en) * | 2011-03-25 | 2013-10-10 | Universite Laval | Inhibitors of 17beta-HSD1, 17beta-HSD3 and 17beta-HSD10 |
| MX2019000025A (es) * | 2016-06-24 | 2019-10-30 | K&N Eng Inc | Filtro de aire compuesto. |
| USD905747S1 (en) | 2018-04-09 | 2020-12-22 | Mitsubishi Electric Corporation | Display screen with animated graphical user interface |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10019167A1 (de) * | 2000-04-12 | 2001-10-18 | Schering Ag | Substituierte Estratriene als selektiv wirksame Estrogene |
| HUP0300335A2 (hu) * | 2000-04-12 | 2003-07-28 | Schering Ag. | 8béta-hidrokarbil-szubsztituált ösztratriének mint szelektív hatású ösztrogének, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények |
-
2007
- 2007-07-12 EP EP07075600A patent/EP2014672A1/en not_active Ceased
-
2008
- 2008-07-11 CN CN200880024423XA patent/CN101687902B/zh not_active Expired - Fee Related
- 2008-07-11 WO PCT/EP2008/059115 patent/WO2009007454A2/en active Application Filing
- 2008-07-11 CL CL2008002027A patent/CL2008002027A1/es unknown
- 2008-07-11 EP EP08775031A patent/EP2176282B1/en active Active
- 2008-07-11 PA PA20088789401A patent/PA8789401A1/es unknown
- 2008-07-11 PE PE2008001165A patent/PE20090825A1/es not_active Application Discontinuation
- 2008-07-11 KR KR1020107000527A patent/KR20100037593A/ko not_active Application Discontinuation
- 2008-07-11 DK DK08775031.1T patent/DK2176282T3/da active
- 2008-07-11 EA EA201000097A patent/EA017124B1/ru not_active IP Right Cessation
- 2008-07-11 RS RS20120516A patent/RS52541B/en unknown
- 2008-07-11 US US12/171,424 patent/US20090029957A1/en not_active Abandoned
- 2008-07-11 UA UAA201001369A patent/UA99918C2/ru unknown
- 2008-07-11 PL PL08775031T patent/PL2176282T3/pl unknown
- 2008-07-11 NZ NZ582490A patent/NZ582490A/en not_active IP Right Cessation
- 2008-07-11 AU AU2008274198A patent/AU2008274198A1/en not_active Abandoned
- 2008-07-11 SI SI200830826T patent/SI2176282T1/sl unknown
- 2008-07-11 AR ARP080102978A patent/AR067507A1/es unknown
- 2008-07-11 BR BRPI0814207-6A2A patent/BRPI0814207A2/pt not_active IP Right Cessation
- 2008-07-11 PT PT08775031T patent/PT2176282E/pt unknown
- 2008-07-11 ES ES08775031T patent/ES2393942T3/es active Active
- 2008-07-11 UY UY31220A patent/UY31220A1/es not_active Application Discontinuation
- 2008-07-11 CA CA 2692727 patent/CA2692727A1/en not_active Abandoned
- 2008-07-11 TW TW097126522A patent/TW200911824A/zh unknown
- 2008-07-11 JP JP2010515526A patent/JP2010533152A/ja not_active Ceased
-
2010
- 2010-01-07 MA MA32490A patent/MA31565B1/fr unknown
- 2010-01-07 TN TNP2010000007A patent/TN2010000007A1/fr unknown
- 2010-01-12 HN HN2010000081A patent/HN2010000081A/es unknown
- 2010-01-12 CO CO10002339A patent/CO6270230A2/es active IP Right Grant
- 2010-01-12 CR CR11211A patent/CR11211A/es not_active Application Discontinuation
- 2010-01-12 CU CU20100008A patent/CU23885B1/es not_active IP Right Cessation
- 2010-01-12 EC EC2010009872A patent/ECSP109872A/es unknown
- 2010-01-12 DO DO2010000017A patent/DOP2010000017A/es unknown
-
2012
- 2012-11-14 CY CY20121101099T patent/CY1113351T1/el unknown
- 2012-11-21 HR HRP20120952AT patent/HRP20120952T1/hr unknown
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