DK2580210T5 - Østrogenreceptormodulatorer og anvendelser deraf - Google Patents

Østrogenreceptormodulatorer og anvendelser deraf Download PDF

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DK2580210T5
DK2580210T5 DK11793115.4T DK11793115T DK2580210T5 DK 2580210 T5 DK2580210 T5 DK 2580210T5 DK 11793115 T DK11793115 T DK 11793115T DK 2580210 T5 DK2580210 T5 DK 2580210T5
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substituted
unsubstituted
phenyl
methyl
methylpyrrolidin
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DK11793115.4T
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DK2580210T3 (da
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Mehmet Kahraman
Steven P Govek
Johnny Y Nagasawa
Nicholas D Smith
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Seragon Pharmaceuticals Inc
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    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
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Claims (16)

1. Forbindelse af formel (VI), eller et farmaceutisk acceptabelt salt, eller solvat deraf:
Formel (VI) hvor, R1 er H, F, Ci-C4alkyl, eller Ci-C4fluoralkyl; R3 er H, halogen, Ci-C4alkyl, C3-C6cykloalkyl, eller Ci-C4fluoralkyl; hvert R4 er uafhængigt valgt fra H, halogen, -CN, -OH, -OR9, -SR9, -S(=0)R10, -S(=0)2R10, -C(=0)R10, -C(=0)0H, -C(=0)0R10, -C(=0)NHR10, -C(=O)N(R10)2, substitueret eller ikke-substitueret Ci-C6alkyl, substitueret eller ikke-substitueret Ci-C6fluoralkyl, substitueret eller ikke-substitueret Ci-C6fluoralkoxy, substitueret eller ikke-substitueret Ci-C6alkoxy, og substitueret eller ikke-substitueret Ci-C6heteroalkyl; hvert R5 er uafhængigt valgt fra H, halogen, -CN, -OH, -OR9, -SR9, -S(=0)R10, -S(=0)2R10, substitueret eller ikke-substitueret Ci-Cealkyl, substitueret eller ikke-substitueret Ci-C6fluoralkyl, substitueret eller ikke-substitueret Ci-C6fluoralkoxy, substitueret eller ikke-substitueret Ci-Cealkoxy, og substitueret eller ikke-substitueret Ci-C6heteroalkyl; hvert R6 er uafhængigt valgt fra H, halogen, -CN, -OH, -OR9, -SR9, -S(=0)R10, -S(=0)2R10, substitueret eller ikke-substitueret Ci-Cealkyl, substitueret eller ikke-substitueret Ci-C6fluoralkyl, substitueret eller ikke-substitueret Ci-C6fluoralkoxy, substitueret eller ikke-substitueret Ci-Cealkoxy, og substitueret eller ikke-substitueret Ci-C6heteroalkyl;
er azetidinyl eller pyrrol id inyl; R7 er H eller Ci-C4alkyl; hvert R8 er uafhængigt valgt fra F, Cl, -CN, -OH, -OR9, -SR9, -S(=0)R10, -S(=0)2R10, substitueret eller ikke-substitueret Ci-C6alkyl, substitueret eller ikke-substitueret Ci-C6fluoralkyl, substitueret eller ikke-substitueret Ci-Cefluoralkoxy, substitueret eller ikke-substitueret Ci-C6alkoxy, og substitueret eller ikke-substitueret Ci-C6heteroalkyl; eller 1 R8 taget sammen med R1 sammen med de mellemliggende atomer forbinder R8 til R1 for at danne en 5-, 6-, eller 7-leddet ring; hvert R9 er uafhængigt valgt fra H, -C(=0)R10, -C(=0)0R10, -C(=0)NHR10, substitueret eller ikke-substitueret Ci-C6alkyl, substitueret eller ikke-substitueret Ci-C6heteroalkyl, substitueret eller ikke-substitueret Ci-Cefluoralkyl, substitueret eller ikke-substitueret C3-Ciocykloalkyl, substitueret eller ikke-substitueret C2-Cioheterocykloalkyl, substitueret eller ikke-substitueret aryl, substitueret eller ikke-substitueret heteroaryl, -Ci-C2alkylen-(substitueret eller ikke-substitueret C3-Ciocykloalkyl), -Ci-C2alkylen-(substitueret eller ikke-substitueret C2-Cioheterocykloalkyl), -Ci-C2alkylen-(substitueret eller ikke-substitueret aryl), og -Ci-C2alkylen-(substitueret eller ikke-substitueret heteroaryl); eller hvert R10 er uafhængigt valgt fra substitueret eller ikke-substitueret Ci-Cealkyl, substitueret eller ikke-substitueret Ci-C6heteroalkyl, substitueret eller ikke-substitueret Ci-C6fluoralkyl, substitueret eller ikke-substitueret C3-Ciocykloalkyl, substitueret eller ikke-substitueret C2-Cioheterocykloalkyl, substitueret eller ikke-substitueret aryl, substitueret eller ikke-substitueret heteroaryl, -Ci-C2alkylen-(substitueret eller ikke-substitueret C3-Ciocykloalkyl), -Ci-C2alkylen-(substitueret eller ikke-substitueret C2-Cioheterocykloalkyl), -Ci-C2alkylen-(substitueret eller ikke-substitueret aryl), og -Ci-C2alkylen-(substitueret eller ikke-substitueret heteroaryl); Y er -Ο-, -S-, eller -NR11-; R11 er H, -C(=0)R10, substitueret eller ikke-substitueret Ci-C6alkyl, substitueret eller ikke-substitueret Ci-C6fluoralkyl, eller substitueret eller ikke-substitueret Ci-C6heteroalkyl; X er -O-, -S-, -CH2-, -NH- eller -N(Ci-C6alkyl)-; m er 0, 1, 2, 3 eller 4; n er 0, 1, 2, eller 3; p er 0, 1, 2, 3 eller 4; t er 1, 2, 3 eller 4.
2. Forbindelsen ifølge krav 1, eller et farmaceutisk acceptabelt salt, eller solvat deraf, hvor: R1 er H eller Ci-C4alkyl; R3 er Ci-C4alkyl eller Ci-C4fluoralkyl; hvert R4 er uafhængigt valgt fra H, halogen, -CN, -OH, -OR9, -SR9, -S(=0)R10, -S(=0)2R10, Ci-C4alkyl, Ci-C4fluoralkyl, Ci-C4fluoralkoxy, Ci-C4alkoxy, og Ci-C4heteroalkyl; hvert R5 er uafhængigt valgt fra H, F, Cl, -OH, -CH3, -CF3, -OCF3 og -OCH3; hvert R6 er uafhængigt valgt fra H, F, Cl, -OH, -CH3, -CF3, -OCF3 og -OCH3; R7 er H; hvert R8 er uafhængigt valgt fra F, Cl, -OH, Ci-C4alkyl, Ci-C4fluoralkyl, Ci-C4fluoralkoxy, Ci-C4alkoxy, og Ci-C4heteroalkyl; Y er -O- eller -S-; X er -O-, -S-, -CH2-, -NH- eller -N(CH3)-; p er 0, 1, eller 2.
3. Forbindelsen ifølge krav 1 eller krav 2, eller et farmaceutisk acceptabelt salt, eller solvat deraf, hvor:
4. Forbindelsen ifølge et hvilket som helst af kravene 1-3, eller et farmaceutisk acceptabelt salt, eller solvat deraf, hvor forbindelsen af formel (VI) har strukturen af formel (VIII):
Formel (VIII)
5. Forbindelsen ifølge et hvilket som helst af kravene 1-3, eller et farmaceutisk acceptabelt salt, eller solvat deraf, hvor forbindelsen af formel (VI) har strukturen af formel (IX):
Formel (IX)
6. Forbindelsen ifølge krav 1 eller krav 2, eller et farmaceutisk acceptabelt salt, eller solvat deraf, hvor forbindelsen af formel (VI) har strukturen af formel (X):
hvert R8 er uafhængigt valgt fra F, Cl, -OH, -CH3, -CH2CH3, -CH(CH3)2, -CF3, -CH2CF3, -OCFs, -OCH2CF3, -OCHs, -OCH2CH3, -CH2OCH3, -CH2OCH2CH3, og -CH2OH.
7. Forbindelsen ifølge et hvilket som helst af kravene 1-6, eller et farmaceutisk acceptabelt salt, eller solvat deraf, hvor: R1 er H eller -CH3; R3 er -CH3 eller -CF3; R9 er H; X er -O-.
8. Forbindelsen ifølge et hvilket som helst af kravene 1-5, eller et farmaceutisk acceptabelt salt, eller solvat deraf, hvor:
9. Forbindelse ifølge krav 1, der er: 3-(3-Hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; (S)-3-(3-Hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol (R)-3-(3-Hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(3-Hydroxyphenyl)-4-methyl-2-(4-(2-((R)-3-methylpyrrolidin-l- yl)ethoxy)phenyl)-2H-chromen-6-ol; 3-(3-Hydroxyphenyl)-4-methyl-2-(4-((R)-2-((R)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(3-Hydroxyphenyl)-4-methyl-2-(4-(2-((S)-3-methylpyrrolidin-l- yl)ethoxy)phenyl)-2H-chromen-6-ol; 3-(3-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((S)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(3-hydroxyphenyl)-4-methyl-2-(4-((R)-2-((S)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; 2-(4-((S)-2-(3,3-Dimethylpyrrolidin-l-yl)propoxy)phenyl)-3-(3- hydroxyphenyl)-4-methyl-2H-chromen-6-ol; 2- (4-(2-(3,3-Dimethylpyrrolid in-l-yl)ethoxy)phenyl)-3-(3-hydroxyphenyl)- 4-methyl-2H-chromen-6-ol; 3- (3-Hydroxyphenyl)-4-methyl-2-(4-(2-((R)-2-methylpyrrolidin-l-yl)ethoxy)phenyl)-2H-chromen-6-ol; 3-(3-Hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-2-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(3-Hydroxyphenyl)-4-methyl-2-(4-((S)-2-((S)-2-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(3-Hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-7-ol; 3- (4-Hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-7-ol;
4- Methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l-yl)propoxy)phenyl)-3-phenyl-2H-chromen-6-ol; 3-(4-Fluorphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; (S)-3-(4-Fluorphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; (R)-3-(4-Fluorphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(4-Hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(3-Fluorphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(3-Fluor-4-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3- methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol; 2- (2-Fluor-4-((S)-2-((R)-3-methylpyrrolidin-l-yl)propoxy)phenyl)-3-(3-hydroxyphenyl)-4-methyl-2H-chromen-6-ol; 3- (3-Hydroxy-4-methylphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(3-Hydroxy-2-methylphenyl)-4-methyl-2-(4-((S)-2-((R)-3- methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(4-Hydroxy-2-methylphenyl)-4-methyl-2-(4-((S)-2-((R)-3- methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(4-Hydroxy-3-methylphenyl)-4-methyl-2-(4-((S)-2-((R)-3- methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(3-Fluor-5-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3- methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(4-Chlorphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(2-Fluor-4-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3- methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(3,4-Difluorphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(3,5-Difluor-4-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3- methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(2,4-Difluor-3-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3- methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(3,4-Difluor-5-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3- methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(2-Chlor-4-Fluorphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(2,4-Difluorphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrc>lidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; 3- (4-Bromphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol;
4- Methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l-yl)propoxy)phenyl)-3-(o-tolyl)-2H-chromen-6-ol; 3-(4-Fluor-3-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3- methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol; 3- (4-Ethynylphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol;
4- Methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l-yl)propoxy)phenyl)-3-(4-(methylsulfonyl)phenyl)-2H-chromen-6-ol; 3-(2-Fluor-3-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3- methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol;
5- Fluor-3-(3-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(2-Fluor-5-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3- methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(4-Fluorphenyl)-4-methyl-2-(4-((S)-2-((R)-2-methylpyrrc>lidin-l- yl)propoxy)phenyl)-2H-chromen-6-ol; 2- (4-((S)-2-((R)-3-Fluoropyrrolidin-l-yl)propoxy)phenyl)-3-(3-hydroxyphenyl)-4-methyl-2H-chromen-6-ol; 3- (4-Hydroxyphenyl)-2-(4-((S)-2-((R)-3-methylpyrrolidin-l-yl)propoxy)phenyl)-4-(trifluormethyl)-2H-chromen-6-ol; 3-(3-Hydroxyphenyl)-2-(4-((S)-2-((R)-3-methylpyrrolidin-l- yl)propoxy)phenyl)-4-(trifluormethyl)-2H-chromen-6-ol; 3-(3-Hydroxy-4-(trifluormethyl)phenyl)-4-methyl-2-(4-((S)-2-((R)-3- methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol; 3-(4-Hydroxy-3-(trifluormethyl)phenyl)-4-methyl-2-(4-((S)-2-((R)-3- methylpyrrolidin-l-yl)propoxy)phenyl)-2H-chromen-6-ol; eller et farmaceutisk acceptabelt salt deraf.
10. Farmaceutisk sammensætning omfattende en forbindelse ifølge et hvilket som helst af kravene 1-9, eller et farmaceutisk acceptabelt salt deraf.
11. Den farmaceutiske sammensætning ifølge krav 10, hvor den farmaceutiske sammensætning er formuleret til intravenøs injektion, subkutan injektion, oral administration, eller topikal administration.
12. Den farmaceutiske sammensætning ifølge krav 10, hvor den farmaceutiske sammensætning er i form af en tablet, en pille, en kapsel, en væske, en suspension, en gel, en dispersion, en opløsning, en emulsion, en salve, eller en lotion.
13. Forbindelsen ifølge et hvilket som helst af kravene 1-9, eller et farmaceutisk acceptabelt salt deraf til anvendelse i behandlingen afen østrogenreceptor-afhængig eller østrogenreceptor-medieret sygdom eller tilstand hos pattedyr.
14. Forbindelsen til anvendelse ifølge krav 13, hvor den østrogen receptorafhængige eller østrogenreceptor-medierede sygdom eller tilstand er valgt fra kræft, central nervesystem (CNS) -defekter, kardiovaskulær system-defekter, hæmatologisk system-defekter, immun- og inflammationssygdomme, modtagelighed over for infektion, stofskiftedefekter, neurologiske defekter, psykiatriske defekter og forplantningsdefekter.
15. Forbindelsen til anvendelse ifølge krav 13, hvor den østrogen receptorafhængige eller østrogenreceptor-medierede sygdom eller tilstand er valgt fra knoglekræft, brystkræft, lungekræft, kolorektalkræft, endometrialkræft, prostatakræft, æggestokskræft, livmoderkræft, alkoholisme, migræne, aortaaneurisme, modtagelighed over for myokardieinfarkt, aortaklapsklerose, kardiovaskulær sygdom, kranspulsåresygdom, hypertension, dyb venetrombose, Graves sygdom, arthritis, multiple sklerose, cirrose, hepatitis B, kronisk leversygdom, knogledensitet, cholestase, hypospadi, fedme, osteoarthritis, osteopeni, osteoporose, Alzheimers sygdom, Parkinsons sygdom, migræne, svimmelhed, anorexia nervosa, forstyrrelser af opmærksomhed, aktivitet og impulsitivitet (ADHD), demens, klinisk depression, psykose, menarchealderen, endometriose, og infertilitet.
16. Forbindelsen ifølge et hvilket som helst af kravene 1-9, eller et farmaceutisk acceptabelt salt deraf, til anvendelse i behandlingen af kræft hos pattedyr.
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