DK2623510T3 - 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-derivater, fremgangsmåde til fremstilling heraf og deres anvendelse til behandling af sygdomme - Google Patents

17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-derivater, fremgangsmåde til fremstilling heraf og deres anvendelse til behandling af sygdomme Download PDF

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DK2623510T3
DK2623510T3 DK12194455.7T DK12194455T DK2623510T3 DK 2623510 T3 DK2623510 T3 DK 2623510T3 DK 12194455 T DK12194455 T DK 12194455T DK 2623510 T3 DK2623510 T3 DK 2623510T3
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pentafluoroethyl
hydroxy
dien
estra
phenyl
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Wolfgang Schwede
Ulrich Klar
Carsten Moeller
Andrea Rotgeri
Wilhelm Bone
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Bayer Ip Gmbh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/567—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/36—Antigestagens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
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  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Steroid Compounds (AREA)
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Claims (33)

1. Forbindelse med formel I
hvor R1 står for enten en gruppe Y eller for en phenylring substitueret en gang eller dobbelt med en gruppe Y, Y er udvalgt af gruppen bestående af SR2, S(0)R3, S(0)2R3, S (0) (NH) R3, S (0) (NR4) R3, S(0)2NR9R10, R2 står for hydrogen, Ci-C6_alkyl, C7-Cio-aralkyl eller aryl, R3 står for Ci-C6-alkyl eller aryl, R4 står for en gruppe S (0) 2R6, R6 står for phenyl eller 4-methylphenyl, X betegner et oxygenatom, NOR7 eller NNHS02R7, R7 er udvalgt af gruppen bestående af hydrogen, Ci-Cio-alkyl, aryl R9, R10 uafhængigt af hinanden er udvalgt af gruppen bestående af hydrogen, Ci-Cio-alkyl eller aryl eller sammen med nitrogenatomet betegner en 3- til 8-leddet, mættet eller umættet heterocyklisk ring og de adskilte stereoisomerer heraf, deres salte, solvater eller solvater af saltene, inklusiv alle krystalmodifikationer.
2. Forbindelse ifølge krav 1, hvori R1 står for enten en gruppe Y eller for en phenylring substitueret en gang med en gruppe Y, Y er udvalgt af gruppen bestående af SR2, S(0)R3, S(0)2R3, S (0) (NH) R3, S(0)(NR4)R3, S(0)2NR9R10, og R2 står for hydrogen eller Ci-C6-alkyl, R3 står for Ci-C6-alkyl, og X betegner et oxygenatom, R6 betegner phenyl eller 4-methylphenyl, og R9, R10 uafhængigt af hinanden betegner hydrogen eller C1-C6- alkyl eller phenyl og de adskilte stereoisomerer heraf, deres salte, solvater eller solvater af saltene.
3. Forbindelse ifølge krav 1, hvori R1: betegner S(0)2R3, og X: betegner 0.
4. Forbindelse ifølge krav 3, hvori R3: betegner Ci-C6-alkyl.
5. Forbindelse ifølge krav 1, hvori R1: betegner S (0) (NH)R3, og X: betegner 0 og de adskilte stereoisomerer heraf.
6. Forbindelse ifølge krav 5, hvori R3: betegner Ci-C6-alkyl og de adskilte stereoisomerer heraf.
7. Forbindelse ifølge krav 6, hvori R3: betegner methyl og de adskilte stereoisomerer heraf.
8. Forbindelse ifølge krav 1, hvori R1: betegner SOR3, og X: betegner 0 og de adskilte stereoisomerer heraf.
9. Forbindelse ifølge krav 8, hvori R3: betegner Ci-C6-alkyl og de adskilte stereoisomerer heraf.
10. Forbindelse ifølge krav 9, hvori R3: betegner methyl og de adskilte stereoisomerer heraf.
11. Forbindelse ifølge krav 1, hvori R1: betegner SR2, og X: betegner O.
12. Forbindelse ifølge krav 11, hvori R2: betegner hydrogen.
13. Forbindelse ifølge krav 11, hvori R2: betegner C1-C6-alkyl.
14. Forbindelse ifølge krav 13, hvori R2: betegner methyl.
15. Forbindelse ifølge krav 11, hvori R2: betegner aryl.
16. Forbindelse ifølge krav 15, hvori R2: betegner phenyl.
17. Forbindelse ifølge krav 11, hvori R2: betegner C7-C10-aralkyl.
18. Forbindelse ifølge krav 17, hvori R2: betegner benzyl.
19. Forbindelser ifølge krav 2, hvori R2 betegner methyl, ethyl eller hydrogen.
20. Forbindelser ifølge krav 1 hvori R3 betegner Ci-C6-alkyl.
21. Forbindelser ifølge krav 4 hvori R3 betegner methyl eller ethyl.
22. Forbindelser ifølge krav 1 hvori R6 betegner phenyl.
23. Forbindelser ifølge krav 1 hvori X er et oxygenatom.
24. Forbindelser ifølge krav 1 hvori Y står for SR2 eller S(0)2R3 eller S (O) (NH)R3 med R2 lig med hydrogen, methyl eller ethyl og R3 lig med methyl eller ethyl.
25. Forbindelser ifølge krav 1 hvori Y står for S(0)2R3.
26. Forbindelser ifølge krav 1 (11β, 17β)-17-hydroxy-ll-[4-(methylsulfanyl) phenyl]-17-(pentafluorethyl)estra-4,9-dien-3-on; (11β, 17β)-11-[4-(ethylsulfanyl) phenyl]-17-hydroxy-17-(pentafluorethyl)estra-4,9-dien-3-on; (11β,17β)-17-hydroxy-ll-{4-[(RS)-methylsulfinyl]phenyl}-17-(pentafluorethyl)estra-4,9-dien-3-on; (11β, 17β)-11-[4-(ethylsulfonyl)phenyl]-17-hydroxy-17-(pentafluorethyl)estra-4,9-dien-3-on; (11β, 17 β)-11-[4-(benzylsulfanyl)phenyl]-17-hydroxy-17-(pentafluorethyl)estra-4,9-dien-3-on; N—[{4 —[(11β,17β)-17-hydroxy-3-oxo-17-(pentafluorethyl)estra- 4, 9-dien-ll-yl]phenyl} (RS) (methyl)oxido-λ6-sulfanyliden]-4-methylbenzensulfonamid; (11 β,17 β)-17-hydroxy-l1-[4-(RS-methylsulfonimidoyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-on; (11β, 17β)-17-hydroxy-l1-[4'-(methylsulfanyl) biphenyl-4-yl]-17-(pentafluorethyl)estra-4,9-dien-3-on; (11β, 17 β)-17-hydroxy-l1-[4'-(methylsulfony1)biphenyl-4-yl]-17-(pentafluorethyl)estra-4,9-dien-3-on; N—[{4'—[(11β,17β)-17-hydroxy-3-oxo-17-(pentafluorethyl)estra-4,9-dien-ll-yl]biphenyl-4-yl}(RS)(methyl)oxido-λ6-sulfanyliden]-4-methylbenzensulfonamid; (11β,17 β)-17-hydroxy-l1-[4'-(RS-methylsulfonimidoyl)biphenyl-4-yl]-17-(pentafluorethyl)estra-4,9-dien-3-on; (11β, 17β) -17-hydroxy-17-(pentafluoroethyl)—11—(4' — sulfanylbiphenyl-4-yl)estra-4,9-dien-3-on; 4'—[(11β,17β))-17-hydroxy-3-oxo-17-(pentafluorethyl)estra-4,9-dien-11-yl]-N,N-dimethylbiphenyl-4-sulfonamid; 4-[(11β,17β)-17-hydroxy-3-oxo-17-(pentafluorethyl)estra-4,9-dien-11-yl]-N,N-dimethylbenzensulfonamid.
27. Forbindelse ifølge et af de foregående krav til behandling og profylakse af sygdomme.
28. Forbindelse ifølge et af kravene 1-26 til behandling og profylakse af uterusfibroider, af endometriose, kraftige menstruationsblødninger, meningiomer, hormonafhængige mammakarcinomer og af problemer associeret med menopausen eller til fertilitetskontrol og nødkontraception.
29. Anvendelse af en forbindelse ifølge et af kravene 1 - 26 til fremstilling af et lægemiddel til behandling og/eller profylakse af sygdomme.
30. Anvendelse af en forbindelse ifølge et af kravene 1-26 til fremstilling af et lægemiddel til behandling og/eller profylakse af uterusfibroider, af endometriose, kraftige menstruationsblødninger, meningiomer, hormonafhængige mammakarcinomer og af problemer associeret med menopausen eller til fertilitetskontrol og nødkontraception.
31. Lægemiddel indeholdende en forbindelse som defineret i et af kravene 1 - 26 i kombination med et yderligere aktivstof.
32. Lægemiddel indeholdende en forbindelse som defineret i et af kravene 1 - 26 i kombination med et inert, ikketoksisk, farmaceutisk egnet hjælpestof.
33. Lægemiddel ifølge krav 31 eller 32 til behandling og/eller profylakse af uterusfibroider, af endometriose, kraftige menstruationsblødninger, meningiomer, hormonafhængige mammakarcinomer og af problemer associeret med menopausen eller til fertilitetskontrol og nødkontraception.
DK12194455.7T 2009-07-20 2010-07-07 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-derivater, fremgangsmåde til fremstilling heraf og deres anvendelse til behandling af sygdomme DK2623510T3 (da)

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DE102009034362A DE102009034362A1 (de) 2009-07-20 2009-07-20 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
EP10735198A EP2432798B1 (de) 2009-07-20 2010-07-07 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-derivat, verfahren zu seine herstellung und seine verwendung zur behandlung von krankheiten

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DK12194455.7T DK2623510T3 (da) 2009-07-20 2010-07-07 17-hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-derivater, fremgangsmåde til fremstilling heraf og deres anvendelse til behandling af sygdomme
DK10735198.3T DK2432798T3 (da) 2009-07-20 2010-07-07 17-hydroxy-17-pentaflourethyl-estra-4,9(10)-dien-11-aryl-derivat, fremgangsmåde til fremstilling heraf og anvendelse heraf til behandling af sygdomme
DK17176264.4T DK3252069T3 (da) 2009-07-20 2010-07-07 (11.beta.,17.beta.)-17-hydroxy-11-[4-(methylsulfonyl)phenyl]-17-(pentalfuoromethyl)estra-4,9-dien-3-oner til behandling af sygdomme

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DK17176264.4T DK3252069T3 (da) 2009-07-20 2010-07-07 (11.beta.,17.beta.)-17-hydroxy-11-[4-(methylsulfonyl)phenyl]-17-(pentalfuoromethyl)estra-4,9-dien-3-oner til behandling af sygdomme

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DE102009034362A1 (de) * 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
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