DK2760878T3 - Estra-1,3,5(10),16-tetraen-3-carboxamid-derivater, fremgangsmåde til fremstilling heraf, farmaceutiske præparater, som indeholder disse, samt anvendelse heraf til fremstilling af lægemidler - Google Patents

Estra-1,3,5(10),16-tetraen-3-carboxamid-derivater, fremgangsmåde til fremstilling heraf, farmaceutiske præparater, som indeholder disse, samt anvendelse heraf til fremstilling af lægemidler Download PDF

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DK2760878T3
DK2760878T3 DK12766636.0T DK12766636T DK2760878T3 DK 2760878 T3 DK2760878 T3 DK 2760878T3 DK 12766636 T DK12766636 T DK 12766636T DK 2760878 T3 DK2760878 T3 DK 2760878T3
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estra
hydrogen
methyl
carbonyl
tetraen
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Ulrich Bothe
Naomi Barak
Matthias Busemann
Oliver Martin Fischer
Andrea Rotgeri
Ingo Hartung
Isabella Gashaw
Tobias Marquardt
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Bayer Ip Gmbh
Bayer Pharma AG
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    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
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    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
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    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
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    • A61P5/00—Drugs for disorders of the endocrine system
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Claims (9)

1. Forbindelser med formel (I),
hvor RI og R2 uafhængigt af hinanden betegner hydrogen, fluor, chlor, nitril, trifluormethyl, pentafluorethyl, methoxy, ethoxy, trifluormethoxy, -OCH2CF3, CH3S02-, CH3CH2S02-, -(C=0)CH3, carboxyl, Ci-C4-alkyl, hydroxyl, -CH2OH, -C(CH3)2OH, -CONH2, - (C=0)NHalkyl, - (C=0) N (CH3) 2, -S02NH2, -S02NH(CH3), - S02N (CH3) 2 eller erstatningen af en OH gruppe i pyridinringen med et nitrogenatom, og R3 og R4 betegner hydrogen, eller R3 betegner hydroxyl, fluor, methoxy eller ethoxy, og R4 betegner hydrogen, eller R3 betegner hydrogen, og R4 står for hydroxyl, fluor, methoxy eller ethoxy, og R5 og R6 betegner hydrogen, eller R5 betegner fluor, hydroxyl, methoxy eller ethoxy, og R6 betegner hydrogen, eller R5 betegner hydrogen, og R6 betegner fluor, og R7 betegner hydrogen, Ci-C4_alkyl, C3-Cg-cycloalkyl, cyclopropylmethyl, trifluormethyl eller 2,2,2-trifluorethyl, og R8 betegner -CRaRb -COOH, idet Ra og Rb uafhængigt af hinanden betegner hydrogen, methyl, ethyl, eller Ra og Rb i fællesskab betegner -(CH2)n- med n = 2, 3, 4 eller 5, idet op til 4 hydrogenatomer i CH2-grupperne kan være erstattet med flouratomer, eller Ra og Rb i fællesskab betegner -CH2-0-CH2-, -CH2-NH-CH2-, -CH2- N(CH3)-CH2-, -ch2ch2-o-ch2ch2-, -CH2CH2-NH-CH2CH2-, -CH2CH2-N (CH3)-CH2CH2-, eller Ra betegner hydrogen, methyl eller ethyl, og Rb i fællesskab med R7 betegner -(CH2)n- med n = 1, 2, 3, 4, idet op til 4 hydrogenatomer i CH2-grupperne kan være erstattet med fluoratomer, eller Ra i fællesskab med R7 betegner -CH2-0-CH2CH2-, -CH2-N (CH3) -CH2CH2-, og Rb betegner hydrogen, methyl eller ethyl eller -CRcRd-CReRf-COOH, idet Rc, Rd, Re, Rf betegner hydrogen, eller R°, Rd uafhængigt af hinanden betegner methyl, ethyl eller i fællesskab betegner -(CH2)n- med n = 2, 3, 4, 5 eller -CH2CH2-0-CH2CH2- og Re, Rf betegner hydrogen, eller R°, Rd betegner hydrogen, og Re, Rf uafhængigt af hinanden betegner methyl, ethyl eller i fællesskab betegner -(CH2)n- med n = 2, 3, 4, 5, -CH2CH2-0-CH2CH2-, -CH2CH2-NH-CH2CH2-, -CH2CH2- N (CH3) -CH2CH2- eller -CH2-0-CH2-, eller R° betegner methyl, ethyl, trifluormethyl, og Rd, Rc og Rf betegner hydrogen, eller Rc, Rd og Rf betegner hydrogen, og Re betegner methyl, ethyl, trifluormethyl, hydroxyl eller methoxy, eller Rc og Re i fællesskab betegner -(CH2)n- med n = 1,2,3 eller 4, og Rd og Rf betegner hydrogen eller -CH2-CH2-CHRg-COOH, idet Rg betegner hydrogen, eller Rg og R7 i fællesskab betegner -CH2- eller -CH2CH2-og deres salte, solvater og solvater af saltene.
2. Forbindelser ifølge krav 1 med formel (II) og med formel (III)
hvor RI betegner hydrogen, fluor, chlor, nitril, methoxy, ethoxy, trifluormethoxy, methyl, ethyl, trifluormethyl, -(C=0)CH3, og R3 og R4 betegner hydrogen, eller R3 betegner hydroxyl, og R4 betegner hydrogen, eller R3 betegner hydrogen, og R4 betegner hydroxyl, og R5 betegner hydrogen eller fluor, og R7 betegner hydrogen eller Ci-C4-alkyl, og R8 betegner -CRaRb -COOH, idet R8 og Rb uafhængigt af hinanden betegner hydrogen, methyl eller ethyl, eller Ra og Rb i fællesskab betegner -(CH2)n- med n = 2, 3, 4 eller 5, eller Ra betegner hydrogen, og Rb i fællesskab med R7 betegner -(CH2) n— med n = 3 eller 4 eller -CR°Rd-CReRf-COOH, idet Rc, Rd, Re, Rf betegner hydrogen, eller R°, Rd betegner hydrogen, og Re, Rf uafhængigt af hinanden betegner methyl, ethyl eller i fællesskab betegner -(CH2)n- med n = 2, 3, 4, 5 eller -CH2CH2-0-CH2CH2-, eller R° betegner methyl eller ethyl, og Rd, Re og Rf betegner hydrogen, eller R° og Re i fællesskab betegner -(CH2)n- med n = 1, 2, 3 eller 4, og Rd og Rf betegner hydrogen eller -CH2-CH2-CHRg-COOH, idet Rg betegner hydrogen, eller Rg og R7 i fællesskab betegner -CH2CH2- og deres salte, solvater og solvater af saltene.
3. Forbindelser ifølge krav 1 eller 2 med formel (II) og med formel (III) , hvor RI betegner hydrogen, fluor, chlor, nitril, methoxy, trifluormethyl, og R3 og R4 betegner hydrogen, eller R3 betegner hydroxyl, og R4 betegner hydrogen, eller R3 betegner hydrogen, og R4 betegner hydroxyl, og R5 betegner hydrogen eller fluor, og R7 betegner hydrogen, methyl eller ethyl, og R8 betegner -CRaRb-COOH, idet Ra og Rb uafhængigt af hinanden betegner hydrogen, methyl eller ethyl, eller Ra betegner hydrogen, og Rb i fællesskab med R7 betegner -(CH2) n— med n = 3 eller 4 eller -CRcRd-CReRf-COOH, idet Rc, Rd, Re, Rf betegner hydrogen, eller Rc, Rd betegner hydrogen, og Re, Rf uafhængigt af hinanden betegner methyl eller ethyl eller i fællesskab betegner -(CH2)n- med n = 2, 4, 5 eller -CH2CH2-0-CH2CH2-, eller Rc betegner methyl, og Rd, Re og Rf betegner hydrogen, eller Rc og Re i fællesskab betegner -(CH2)n- med n = 3 eller 4, og Rd og Rf betegner hydrogen eller -CH2-CH2-CHRg-COOH, idet Rg betegner hydrogen, eller Rg og R7 i fællesskab betegner -CH2CH2-og deres salte, solvater og solvater af saltene.
4. Forbindelser ifølge krav 1, 2 eller 3 med formel (II) og med formel (III), hvor Ri betegner hydrogen, fluor, methoxy, trifluormethyl, og R3 og R4 betegner hydrogen, eller R3 betegner hydroxyl og R4 hydrogen, eller R3 betegner hydrogen, og R4 betegner hydroxyl, og R5 betegner hydrogen eller fluor, og R7 betegner hydrogen eller methyl, og R8 betegner -CRaRb -COOH, hvor Ra og Rb uafhængigt af hinanden betegner hydrogen eller methyl, eller Ra betegner hydrogen, og Rb i fællesskab med R7 betegner -(CH2) 3- eller -CRcRd-CR°Rf-COOH, Rc, Rd, Re, Rf betegner hydrogen, eller R° og Rd betegner hydrogen, og Re og Rf betegner methyl eller i fællesskab betegner -(0¾) n- med n = 2 eller 4 eller -CH2CH2-0-CH2CH, eller R° betegner methyl, og Rd, Re og Rf betegner hydrogen, eller Rc og R° i fællesskab betegner -(0¾¾-^ og Rd og Rf betegner hydrogen eller -CH2-CH2-CHRg-COOH, Rg betegner hydrogen, eller Rg og R7 betegner -CH2CH2- og deres salte, solvater og solvater af saltene.
5. Forbindelser ifølge krav 1 til 4 med betegnelserne 4-[({[17-(5-fluorpyridin-3-yl)estra-l,3,5(10),16-tetråen-3-yl]carbonyl}amino) methyl]-3,4,5,6-tetrahydro-2H-pyran-4- carboxylsyre N-{[17-(5-fluorpyridin-3-yl)estra-l,3,5(10),16-tetråen-3-yl]carbonyl}-N-methyl-p-alanin 1-[({[17-(5-fluorpyridin-3-yl)estra-1,3,5(10),16-tetråen-3- yl]carbonyl}amino) methyl]cyclopropan-1-carboxylsyre 1-[({[17-(5-fluorpyridin-3-yl)estra-1,3,5(10),16-tetråen-3- yl]carbonyl}amino)methyl] cyclopentan-l-carboxylsyre 3-({[17-(5-fluorpyridin-3-yl)estra-l,3,5(10),16-tetråen-3- yl]carbonyl}amino)-2,2-dimethylpropansyre 1-{[17-(5-fluorpyridin-3-yl)estra-l,3,5(10),16-tetråen-3-yl]carbonyl}piperidin-4-carboxylsyre N-{[17-(5-fluorpyridin-3-yl)estra-l,3,5(10),16-tetråen-3-yl]carbonyl}-2-methylalanin 4-({[17-(5-fluorpyridin-3-yl)estra-1,3,5(10),16-tetråen-3-yl]carbonyl}amino)butansyre N-{[17-(5 — fluorpyridin-3-yl)estra-1,3,5(10),16-tetraen-3-yl]carbonylΙ-β-alanin N-{[17-(5 — fluorpyridin-3-yl)estra-1,3,5(10),16-tetraen-3-yl]carbonyl}glycin (IR*,2S*)-2-({[17-(5-fluorpyridin-3-yl)estra-1,3,5(10),16-tetraen-3-yl]carbonyl} amino)cyclopentan-1-carboxylsyre (S)—3—({[17-(5-fluorpyridin-3-yl)estra-1,3,5(10),16-tetraen-3-yl]carbonyl}amino) butansyre (R)—3—({[17-(5-fluorpyridin-3-yl)estra-1,3,5(10),16-tetraen-3-yl]carbonyl}amino) butansyre 3- ({[17-(5-methoxypyridin-3-yl)estra-1,3,5(10),16-tetraen-3-yl]carbonyl}amino)-2,2-dimethylpropansyre N-{[17-(5-methoxypyridin-3-yl)estra-1,3,5(10),16-tetraen-3-yl]carbonyl Ι-β-alanin N-{[17-(5-methoxypyridin-3-yl)estra- 1.3.5 (10) , 16-tetraen-3-yl]carbonyl}-N-methyl^-alanin N-{[17-(pyrimidin-5-yl)estra-1,3,5(10),16-tetraen-3-yl] carbonyl Ι-β-alanin 4- ({[17-(pyrimidin-5-yl)estra-1,3,5(10),16-tetraen-3- yl]carbonyl}amino)butansyre N-methyl-N-{[17-(pyrimidin-5-yl)estra-1,3,5(10),16-tetraen-3-yl]carbonyl}-β-alanin 2,2-dimethyl-3-({[17-(pyrimidin-5-yl)estra-1,3,5(10),16-tetraen-3-yl]carbonyl}amino) propansyre N-({17-[5-(trifluormethyl)pyridin-3-yl]estra-1,3,5(10),16-tetraen-3-yl}carbonyl)-β-alanin N-methyl-N-({17-[5-(trifluormethyl)pyridin-3-yl]estra- 1.3.5 (10) , 16-tetraen-3-yl} carbonyl)-β-alanin N-{[17-(5-fluorpyridin-3-yl}estra-l,3,5(10),16-tetraen-3-yl]carbonyl}-L-prolin N-{[17-(5-fluorpyridin-3-yl)estra-1,3,5(10),16-tetraen-3-yl]carbonyl}-D-prolin 4-({[Ιΐβ-fluor-17-(5-fluorpyridin-3-yl)estra-1,3,5(10),16-tetraen-3-yl]carbonyl} amino)butansyre N-{[17-(5-fluorpyridin-3-yl)-15a-hydroxyestra-l, 3,5(10),16-tetraen-3-yl]carbonyl}-N-methyl-β-alanin N-{[17-(5-fluorpyridin-3-yl)-15β-hydroxyestra-l,3,5(10),16-tetraen-3-yl]carbonyl}-N-methyl-β-alanin N-methyl-N-{[17-(6-methylpyridazin-4-yl)estra-1,3,5(10),16-tetraen-3-yl]carbonyl}-β-alanin N-methyl-N-{[17-(3-pyridin-3-yl)estra-1,3,5(10),16-tetraen-3-yl]carbonyl}-3-alanin 4-({[17-(5-methoxypyridin-3-yl)estra-l,3,5(10),16-tetraen-3-yl]carbonyl}amino)butansyre og deres salte, solvater og solvater af saltene.
6. Forbindelser ifølge krav 1, 2, 3, 4 eller 5 til behandling og/eller til profylakse af sygdomme.
7. Anvendelse af en forbindelse ifølge krav 1, 2, 3, 4 eller 5 til fremstilling af et lægemiddel til behandling og/eller profylakse af sygdomme.
8. Forbindelser ifølge krav 1, 2, 3, 4 eller 5 til behandling og/eller profylakse af endometriose, af uterine leiomyomer, af uterine blødningsproblemer, af dysmenoré, af prostata karcinom, af prostata hyperplasi, af akne, af serborrhea, af hårtab, af for tidlig kønsmodning, af det polycystiske ovariesyndrom, af brystkræft, af lungekræft, af karcinom i endometriet, af karcinom i nyrecellerne, af blærekarcinom, af Non-Hodgkin lymfomer, af kronisk obstruktiv lungesygdom (KOL), af adiposita eller af inflammatoriske smerter.
9. Lægemiddel indeholdende en forbindelse ifølge krav 1, 2, 3, 4 eller 5 i kombination med et eller flere aktivstoffer, navnlig med Selektive Estrogen Receptor Modulatorer (SERMs), estrogenreceptor (ER) antagonister, aromatasehæmmere, 17β HSD1 hæmmere, steroid sulfatase (STS)-hæmmere, GnRH-agonister og -antagonisten, kisspeptin receptor (KISSR)-antagonister, Selektive Androgen Receptor Modulatorer (SARMs), androgener, 5a-reduktase hæmmere, Selektive Progesteron Receptor Modulatorer (SPRMs), gestagener, antigestagener, orale kontraceptiva, hæmmere af Mitogen Aktiveret Protein (MAP) kinaser samt hæmmere af MAP kinaser kinaser (Mkk3/6, Mekl/2, Erkl/2), hæmmere af proteinkinaser B (ΡΚΒα/β/γ; Aktl/2/3), hæmmere af phosphoinositid-3-kinaser (PI3K), af de cyclin-afhængige kinase hæmmere (CDK1/2), hæmmere af den hypoxi inducerede signalvej (HIFlalpha hæmmere, aktivatorer af prolylhydroxylase), histon deacetylase (HDAC)-hæmmere, prostaglandin F receptor (FP) (PTGFR)-antagonister og non-steroide antiinflammatoriske midler (NSAIDs).
DK12766636.0T 2011-09-29 2012-09-24 Estra-1,3,5(10),16-tetraen-3-carboxamid-derivater, fremgangsmåde til fremstilling heraf, farmaceutiske præparater, som indeholder disse, samt anvendelse heraf til fremstilling af lægemidler DK2760878T3 (da)

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DE102011083725A DE102011083725A1 (de) 2011-09-29 2011-09-29 Estra-1,3,5(10),16-tetraen-3-carboxamid-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln
PCT/EP2012/068803 WO2013045407A1 (de) 2011-09-29 2012-09-24 Estra-1,3,5(10),16-tetraen-3-carboxamid-derivate, verfahren zu ihrer herstellung, pharmazeutische präparate, die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln

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US (1) US9487554B2 (da)
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JP (1) JP5791810B2 (da)
KR (1) KR20140069013A (da)
CN (1) CN103827133B (da)
AP (1) AP2014007598A0 (da)
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WO2018114672A1 (en) 2016-12-19 2018-06-28 Bayer Pharma Aktiengesellschaft [4-(phenylsulfonyl)piperazin-1-yl](1h-1,2,3-triazol-4-yl)methanones
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